CN101330911A - Hydroxy-polycarboxylic acid esters: action on nerves and use on skin and mucocutaneous organs or sites - Google Patents
Hydroxy-polycarboxylic acid esters: action on nerves and use on skin and mucocutaneous organs or sites Download PDFInfo
- Publication number
- CN101330911A CN101330911A CNA2006800476420A CN200680047642A CN101330911A CN 101330911 A CN101330911 A CN 101330911A CN A2006800476420 A CNA2006800476420 A CN A2006800476420A CN 200680047642 A CN200680047642 A CN 200680047642A CN 101330911 A CN101330911 A CN 101330911A
- Authority
- CN
- China
- Prior art keywords
- acid
- hydroxy
- polycarboxylate
- ester
- hydroxyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 150000002148 esters Chemical class 0.000 title claims abstract description 172
- 239000002253 acid Substances 0.000 title claims abstract description 60
- 210000005036 nerve Anatomy 0.000 title claims abstract description 19
- 210000000056 organ Anatomy 0.000 title claims description 17
- 230000009471 action Effects 0.000 title description 4
- 229920005646 polycarboxylate Polymers 0.000 claims abstract description 58
- 239000000203 mixture Substances 0.000 claims abstract description 57
- 230000009286 beneficial effect Effects 0.000 claims abstract description 41
- 238000000034 method Methods 0.000 claims abstract description 41
- 239000002537 cosmetic Substances 0.000 claims abstract description 9
- 238000011200 topical administration Methods 0.000 claims abstract description 4
- 238000004519 manufacturing process Methods 0.000 claims abstract 2
- -1 hydroxy Homocitrate Chemical compound 0.000 claims description 82
- 201000010099 disease Diseases 0.000 claims description 54
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 54
- 238000011282 treatment Methods 0.000 claims description 37
- 239000003814 drug Substances 0.000 claims description 30
- 208000003251 Pruritus Diseases 0.000 claims description 23
- 206010048768 Dermatosis Diseases 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 22
- 208000017520 skin disease Diseases 0.000 claims description 22
- 201000004624 Dermatitis Diseases 0.000 claims description 19
- XKJVEVRQMLKSMO-SSDOTTSWSA-N (2R)-homocitric acid Chemical compound OC(=O)CC[C@](O)(C(O)=O)CC(O)=O XKJVEVRQMLKSMO-SSDOTTSWSA-N 0.000 claims description 17
- ODBLHEXUDAPZAU-UHFFFAOYSA-N isocitric acid Chemical compound OC(=O)C(O)C(C(O)=O)CC(O)=O ODBLHEXUDAPZAU-UHFFFAOYSA-N 0.000 claims description 17
- 239000000126 substance Substances 0.000 claims description 17
- 230000000699 topical effect Effects 0.000 claims description 17
- UOOVRBDQAYHMRJ-UHFFFAOYSA-N 1,1-dihydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(C(O)=O)C(O)(O)C(O)=O UOOVRBDQAYHMRJ-UHFFFAOYSA-N 0.000 claims description 16
- 230000032683 aging Effects 0.000 claims description 15
- 208000010668 atopic eczema Diseases 0.000 claims description 15
- 230000003444 anaesthetic effect Effects 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- 229940079593 drug Drugs 0.000 claims description 11
- 210000004209 hair Anatomy 0.000 claims description 10
- 210000001215 vagina Anatomy 0.000 claims description 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 9
- 208000002193 Pain Diseases 0.000 claims description 8
- 230000036407 pain Effects 0.000 claims description 8
- ZMJBYMUCKBYSCP-UHFFFAOYSA-N Hydroxycitric acid Chemical compound OC(=O)C(O)C(O)(C(O)=O)CC(O)=O ZMJBYMUCKBYSCP-UHFFFAOYSA-N 0.000 claims description 7
- 230000029663 wound healing Effects 0.000 claims description 7
- 206010061218 Inflammation Diseases 0.000 claims description 6
- 210000000436 anus Anatomy 0.000 claims description 6
- 230000004054 inflammatory process Effects 0.000 claims description 6
- 210000002445 nipple Anatomy 0.000 claims description 6
- 210000003899 penis Anatomy 0.000 claims description 6
- 201000004681 Psoriasis Diseases 0.000 claims description 5
- 208000015181 infectious disease Diseases 0.000 claims description 5
- 230000002757 inflammatory effect Effects 0.000 claims description 5
- 206010020649 Hyperkeratosis Diseases 0.000 claims description 4
- 102000002274 Matrix Metalloproteinases Human genes 0.000 claims description 4
- 108010000684 Matrix Metalloproteinases Proteins 0.000 claims description 4
- 208000000260 Warts Diseases 0.000 claims description 4
- 230000001139 anti-pruritic effect Effects 0.000 claims description 4
- 230000003902 lesion Effects 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 4
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 4
- 201000010153 skin papilloma Diseases 0.000 claims description 4
- 208000025157 Oral disease Diseases 0.000 claims description 3
- 206010040925 Skin striae Diseases 0.000 claims description 3
- 208000024693 gingival disease Diseases 0.000 claims description 3
- RWSXRVCMGQZWBV-WDSKDSINSA-N glutathione Chemical compound OC(=O)[C@@H](N)CCC(=O)N[C@@H](CS)C(=O)NCC(O)=O RWSXRVCMGQZWBV-WDSKDSINSA-N 0.000 claims description 3
- 150000001261 hydroxy acids Chemical class 0.000 claims description 3
- 206010021198 ichthyosis Diseases 0.000 claims description 3
- 239000003589 local anesthetic agent Substances 0.000 claims description 3
- 208000030194 mouth disease Diseases 0.000 claims description 3
- 201000004700 rosacea Diseases 0.000 claims description 3
- 208000002874 Acne Vulgaris Diseases 0.000 claims description 2
- 206010007882 Cellulitis Diseases 0.000 claims description 2
- 108010016626 Dipeptides Proteins 0.000 claims description 2
- XQFRJNBWHJMXHO-RRKCRQDMSA-N IDUR Chemical compound C1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=O)C(I)=C1 XQFRJNBWHJMXHO-RRKCRQDMSA-N 0.000 claims description 2
- 206010061304 Nail infection Diseases 0.000 claims description 2
- 108010038807 Oligopeptides Proteins 0.000 claims description 2
- 102000015636 Oligopeptides Human genes 0.000 claims description 2
- 241001303601 Rosacea Species 0.000 claims description 2
- 208000031439 Striae Distensae Diseases 0.000 claims description 2
- 206010048222 Xerosis Diseases 0.000 claims description 2
- 206010000496 acne Diseases 0.000 claims description 2
- 150000001413 amino acids Chemical class 0.000 claims description 2
- 230000003255 anti-acne Effects 0.000 claims description 2
- 230000001773 anti-convulsant effect Effects 0.000 claims description 2
- 230000001387 anti-histamine Effects 0.000 claims description 2
- 230000002924 anti-infective effect Effects 0.000 claims description 2
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 2
- 230000001166 anti-perspirative effect Effects 0.000 claims description 2
- 230000002682 anti-psoriatic effect Effects 0.000 claims description 2
- 230000000656 anti-yeast Effects 0.000 claims description 2
- 239000001961 anticonvulsive agent Substances 0.000 claims description 2
- 239000000935 antidepressant agent Substances 0.000 claims description 2
- 229940005513 antidepressants Drugs 0.000 claims description 2
- 229960003965 antiepileptics Drugs 0.000 claims description 2
- 229940121375 antifungal agent Drugs 0.000 claims description 2
- 239000000739 antihistaminic agent Substances 0.000 claims description 2
- 239000003213 antiperspirant Substances 0.000 claims description 2
- 239000003908 antipruritic agent Substances 0.000 claims description 2
- 239000002249 anxiolytic agent Substances 0.000 claims description 2
- 238000004061 bleaching Methods 0.000 claims description 2
- 239000002327 cardiovascular agent Substances 0.000 claims description 2
- 229940125692 cardiovascular agent Drugs 0.000 claims description 2
- 239000003246 corticosteroid Substances 0.000 claims description 2
- 229960003180 glutathione Drugs 0.000 claims description 2
- 239000005556 hormone Substances 0.000 claims description 2
- 229940088597 hormone Drugs 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 150000004715 keto acids Chemical class 0.000 claims description 2
- 229920001184 polypeptide Polymers 0.000 claims description 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 2
- 206010040872 skin infection Diseases 0.000 claims description 2
- 239000011782 vitamin Substances 0.000 claims description 2
- 235000013343 vitamin Nutrition 0.000 claims description 2
- 229940088594 vitamin Drugs 0.000 claims description 2
- 229930003231 vitamin Natural products 0.000 claims description 2
- 239000003357 wound healing promoting agent Substances 0.000 claims description 2
- 230000002195 synergetic effect Effects 0.000 claims 10
- 230000001953 sensory effect Effects 0.000 claims 2
- 230000000475 sunscreen effect Effects 0.000 claims 2
- 239000000516 sunscreening agent Substances 0.000 claims 2
- OEJZZCGRGVFWHK-WVZVXSGGSA-N (-)-homoisocitric acid Chemical compound OC(=O)[C@H](O)[C@@H](C(O)=O)CCC(O)=O OEJZZCGRGVFWHK-WVZVXSGGSA-N 0.000 claims 1
- HKLZEUZLOMYCCX-UHFFFAOYSA-N 3,4-dihydroxybutane-1,2,4-tricarboxylic acid Chemical compound OC(=O)C(O)C(O)C(CC(O)=O)C(O)=O HKLZEUZLOMYCCX-UHFFFAOYSA-N 0.000 claims 1
- 208000003643 Callosities Diseases 0.000 claims 1
- 108010024636 Glutathione Proteins 0.000 claims 1
- 239000004909 Moisturizer Substances 0.000 claims 1
- 206010040829 Skin discolouration Diseases 0.000 claims 1
- GUGOEEXESWIERI-UHFFFAOYSA-N Terfenadine Chemical compound C1=CC(C(C)(C)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 GUGOEEXESWIERI-UHFFFAOYSA-N 0.000 claims 1
- 240000008042 Zea mays Species 0.000 claims 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 claims 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 150000007513 acids Chemical class 0.000 claims 1
- 229940035676 analgesics Drugs 0.000 claims 1
- 239000000730 antalgic agent Substances 0.000 claims 1
- 230000000844 anti-bacterial effect Effects 0.000 claims 1
- 230000001430 anti-depressive effect Effects 0.000 claims 1
- 230000003474 anti-emetic effect Effects 0.000 claims 1
- 230000000843 anti-fungal effect Effects 0.000 claims 1
- 230000000840 anti-viral effect Effects 0.000 claims 1
- 230000001153 anti-wrinkle effect Effects 0.000 claims 1
- 239000002111 antiemetic agent Substances 0.000 claims 1
- 230000000949 anxiolytic effect Effects 0.000 claims 1
- 235000005822 corn Nutrition 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 210000000613 ear canal Anatomy 0.000 claims 1
- 150000002337 glycosamines Chemical class 0.000 claims 1
- 230000003699 hair surface Effects 0.000 claims 1
- 229960005015 local anesthetics Drugs 0.000 claims 1
- 206010025482 malaise Diseases 0.000 claims 1
- 230000001333 moisturizer Effects 0.000 claims 1
- 210000004400 mucous membrane Anatomy 0.000 claims 1
- 239000008375 oral care agent Substances 0.000 claims 1
- 206010040882 skin lesion Diseases 0.000 claims 1
- 231100000444 skin lesion Toxicity 0.000 claims 1
- 235000000346 sugar Nutrition 0.000 claims 1
- 150000008163 sugars Chemical class 0.000 claims 1
- 210000003905 vulva Anatomy 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 description 84
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 78
- 150000001721 carbon Chemical group 0.000 description 70
- 239000002674 ointment Substances 0.000 description 46
- 238000002360 preparation method Methods 0.000 description 46
- 230000000694 effects Effects 0.000 description 44
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 34
- 230000035807 sensation Effects 0.000 description 33
- 235000019615 sensations Nutrition 0.000 description 33
- 210000003491 skin Anatomy 0.000 description 33
- 125000000217 alkyl group Chemical group 0.000 description 28
- 125000003710 aryl alkyl group Chemical group 0.000 description 28
- 125000003118 aryl group Chemical group 0.000 description 28
- QOSMNYMQXIVWKY-UHFFFAOYSA-N Propyl levulinate Chemical compound CCCOC(=O)CCC(C)=O QOSMNYMQXIVWKY-UHFFFAOYSA-N 0.000 description 27
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 27
- 230000003796 beauty Effects 0.000 description 20
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 19
- 239000001069 triethyl citrate Substances 0.000 description 19
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 19
- 235000013769 triethyl citrate Nutrition 0.000 description 19
- 229940040563 agaric acid Drugs 0.000 description 18
- OEJZZCGRGVFWHK-UHFFFAOYSA-N homoisocitric acid Chemical compound OC(=O)C(O)C(C(O)=O)CCC(O)=O OEJZZCGRGVFWHK-UHFFFAOYSA-N 0.000 description 16
- DXPPIEDUBFUSEZ-UHFFFAOYSA-N 6-methylheptyl prop-2-enoate Chemical compound CC(C)CCCCCOC(=O)C=C DXPPIEDUBFUSEZ-UHFFFAOYSA-N 0.000 description 14
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 14
- 125000003545 alkoxy group Chemical group 0.000 description 14
- 239000007765 cera alba Substances 0.000 description 14
- 235000019504 cigarettes Nutrition 0.000 description 14
- 229910052500 inorganic mineral Inorganic materials 0.000 description 14
- 239000011707 mineral Substances 0.000 description 14
- 239000002480 mineral oil Substances 0.000 description 14
- 235000010446 mineral oil Nutrition 0.000 description 14
- 229920006395 saturated elastomer Polymers 0.000 description 14
- 229940089491 hydroxycitric acid Drugs 0.000 description 13
- 238000005406 washing Methods 0.000 description 13
- 230000001225 therapeutic effect Effects 0.000 description 12
- XFTRTWQBIOMVPK-YFKPBYRVSA-N Citramalic acid Natural products OC(=O)[C@](O)(C)CC(O)=O XFTRTWQBIOMVPK-YFKPBYRVSA-N 0.000 description 9
- HZLCGUXUOFWCCN-UHFFFAOYSA-N 2-hydroxynonadecane-1,2,3-tricarboxylic acid Chemical compound CCCCCCCCCCCCCCCCC(C(O)=O)C(O)(C(O)=O)CC(O)=O HZLCGUXUOFWCCN-UHFFFAOYSA-N 0.000 description 8
- BVKZGUZCCUSVTD-UHFFFAOYSA-N carbonic acid Chemical compound OC(O)=O BVKZGUZCCUSVTD-UHFFFAOYSA-N 0.000 description 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 8
- 239000006071 cream Substances 0.000 description 8
- HDDLVZWGOPWKFW-UHFFFAOYSA-N trimethyl 2-hydroxypropane-1,2,3-tricarboxylate Chemical compound COC(=O)CC(O)(C(=O)OC)CC(=O)OC HDDLVZWGOPWKFW-UHFFFAOYSA-N 0.000 description 8
- 230000006378 damage Effects 0.000 description 7
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 7
- 210000000214 mouth Anatomy 0.000 description 7
- UZXDUPHUPLOWQH-UHFFFAOYSA-N 4-hydroperoxy-2-(2-hydroperoxy-2-oxoethyl)-2-hydroxy-4-oxobutanoic acid Chemical compound C(C(=O)OO)C(CC(=O)OO)(C(=O)O)O UZXDUPHUPLOWQH-UHFFFAOYSA-N 0.000 description 6
- 125000003047 N-acetyl group Chemical group 0.000 description 6
- 230000003078 antioxidant effect Effects 0.000 description 6
- XFTRTWQBIOMVPK-UHFFFAOYSA-N citramalic acid Chemical compound OC(=O)C(O)(C)CC(O)=O XFTRTWQBIOMVPK-UHFFFAOYSA-N 0.000 description 6
- 210000004905 finger nail Anatomy 0.000 description 6
- 239000000499 gel Substances 0.000 description 6
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 6
- 230000002045 lasting effect Effects 0.000 description 6
- 239000001630 malic acid Substances 0.000 description 6
- 235000011090 malic acid Nutrition 0.000 description 6
- LOTBYPQQWICYBB-UHFFFAOYSA-N methyl n-hexyl-n-[2-(hexylamino)ethyl]carbamate Chemical compound CCCCCCNCCN(C(=O)OC)CCCCCC LOTBYPQQWICYBB-UHFFFAOYSA-N 0.000 description 6
- VYLZSGQQVHTICN-UHFFFAOYSA-N tribenzyl 2-hydroxypropane-1,2,3-tricarboxylate Chemical compound C=1C=CC=CC=1COC(=O)CC(C(=O)OCC=1C=CC=CC=1)(O)CC(=O)OCC1=CC=CC=C1 VYLZSGQQVHTICN-UHFFFAOYSA-N 0.000 description 6
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 description 5
- 239000003963 antioxidant agent Substances 0.000 description 5
- 235000006708 antioxidants Nutrition 0.000 description 5
- YSAVZVORKRDODB-PHDIDXHHSA-N diethyl (2r,3r)-2,3-dihydroxybutanedioate Chemical compound CCOC(=O)[C@H](O)[C@@H](O)C(=O)OCC YSAVZVORKRDODB-PHDIDXHHSA-N 0.000 description 5
- 229960004194 lidocaine Drugs 0.000 description 5
- 208000024891 symptom Diseases 0.000 description 5
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 4
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 4
- 241001597008 Nomeidae Species 0.000 description 4
- 229940061720 alpha hydroxy acid Drugs 0.000 description 4
- 230000008859 change Effects 0.000 description 4
- 239000007788 liquid Substances 0.000 description 4
- 210000004877 mucosa Anatomy 0.000 description 4
- 230000001537 neural effect Effects 0.000 description 4
- 239000007764 o/w emulsion Substances 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- 230000037303 wrinkles Effects 0.000 description 4
- SHCSOTQTAIXSJZ-UHFFFAOYSA-N 1,1,2-trihydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)C(O)(O)C(O)=O SHCSOTQTAIXSJZ-UHFFFAOYSA-N 0.000 description 3
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 3
- MWBPRDONLNQCFV-UHFFFAOYSA-N Tri-allate Chemical group CC(C)N(C(C)C)C(=O)SCC(Cl)=C(Cl)Cl MWBPRDONLNQCFV-UHFFFAOYSA-N 0.000 description 3
- 125000004423 acyloxy group Chemical group 0.000 description 3
- 229960000520 diphenhydramine Drugs 0.000 description 3
- LZCLXQDLBQLTDK-BYPYZUCNSA-N ethyl (2S)-lactate Chemical compound CCOC(=O)[C@H](C)O LZCLXQDLBQLTDK-BYPYZUCNSA-N 0.000 description 3
- ZANNOFHADGWOLI-UHFFFAOYSA-N ethyl 2-hydroxyacetate Chemical compound CCOC(=O)CO ZANNOFHADGWOLI-UHFFFAOYSA-N 0.000 description 3
- 239000008311 hydrophilic ointment Substances 0.000 description 3
- 239000006210 lotion Substances 0.000 description 3
- 230000002085 persistent effect Effects 0.000 description 3
- 230000002265 prevention Effects 0.000 description 3
- 208000011580 syndromic disease Diseases 0.000 description 3
- NOOLISFMXDJSKH-UTLUCORTSA-N (+)-Neomenthol Chemical compound CC(C)[C@@H]1CC[C@@H](C)C[C@@H]1O NOOLISFMXDJSKH-UTLUCORTSA-N 0.000 description 2
- 206010002091 Anaesthesia Diseases 0.000 description 2
- 241000216654 Armillaria Species 0.000 description 2
- 244000248349 Citrus limon Species 0.000 description 2
- 235000005979 Citrus limon Nutrition 0.000 description 2
- NOOLISFMXDJSKH-UHFFFAOYSA-N DL-menthol Natural products CC(C)C1CCC(C)CC1O NOOLISFMXDJSKH-UHFFFAOYSA-N 0.000 description 2
- 208000001840 Dandruff Diseases 0.000 description 2
- 206010012434 Dermatitis allergic Diseases 0.000 description 2
- ZDQWESQEGGJUCH-UHFFFAOYSA-N Diisopropyl adipate Chemical compound CC(C)OC(=O)CCCCC(=O)OC(C)C ZDQWESQEGGJUCH-UHFFFAOYSA-N 0.000 description 2
- 208000006877 Insect Bites and Stings Diseases 0.000 description 2
- 208000001818 Pseudofolliculitis barbae Diseases 0.000 description 2
- 241000121220 Tricholoma matsutake Species 0.000 description 2
- 239000003513 alkali Substances 0.000 description 2
- 150000001280 alpha hydroxy acids Chemical group 0.000 description 2
- 230000005260 alpha ray Effects 0.000 description 2
- 230000037005 anaesthesia Effects 0.000 description 2
- 208000002399 aphthous stomatitis Diseases 0.000 description 2
- 150000001277 beta hydroxy acids Chemical class 0.000 description 2
- 230000005250 beta ray Effects 0.000 description 2
- 230000015572 biosynthetic process Effects 0.000 description 2
- FZCHYNWYXKICIO-FZNHGJLXSA-N cortisol 17-valerate Chemical compound C1CC2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(=O)CO)(OC(=O)CCCC)[C@@]1(C)C[C@@H]2O FZCHYNWYXKICIO-FZNHGJLXSA-N 0.000 description 2
- 239000007854 depigmenting agent Substances 0.000 description 2
- MHDVGSVTJDSBDK-UHFFFAOYSA-N dibenzyl ether Chemical compound C=1C=CC=CC=1COCC1=CC=CC=C1 MHDVGSVTJDSBDK-UHFFFAOYSA-N 0.000 description 2
- VKNUORWMCINMRB-UHFFFAOYSA-N diethyl malate Chemical compound CCOC(=O)CC(O)C(=O)OCC VKNUORWMCINMRB-UHFFFAOYSA-N 0.000 description 2
- YSEKNCXYRGKTBJ-UHFFFAOYSA-N dimethyl 2-hydroxybutanedioate Chemical compound COC(=O)CC(O)C(=O)OC YSEKNCXYRGKTBJ-UHFFFAOYSA-N 0.000 description 2
- 238000001035 drying Methods 0.000 description 2
- 230000005670 electromagnetic radiation Effects 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- LZCLXQDLBQLTDK-UHFFFAOYSA-N ethyl 2-hydroxypropanoate Chemical compound CCOC(=O)C(C)O LZCLXQDLBQLTDK-UHFFFAOYSA-N 0.000 description 2
- 208000014617 hemorrhoid Diseases 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000005865 ionizing radiation Effects 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- 238000013532 laser treatment Methods 0.000 description 2
- 229940041616 menthol Drugs 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- 231100000862 numbness Toxicity 0.000 description 2
- 230000000474 nursing effect Effects 0.000 description 2
- 229920001542 oligosaccharide Polymers 0.000 description 2
- 150000002482 oligosaccharides Chemical class 0.000 description 2
- 230000004792 oxidative damage Effects 0.000 description 2
- 229920000642 polymer Chemical group 0.000 description 2
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 description 2
- 229960004919 procaine Drugs 0.000 description 2
- 229960002429 proline Drugs 0.000 description 2
- 150000003254 radicals Chemical class 0.000 description 2
- 230000035945 sensitivity Effects 0.000 description 2
- 230000009759 skin aging Effects 0.000 description 2
- 230000000638 stimulation Effects 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- 208000004371 toothache Diseases 0.000 description 2
- DXRFOGXSSDRZFP-UHFFFAOYSA-N tripentyl 2-hydroxypropane-1,2,3-tricarboxylate Chemical class CCCCCOC(=O)CC(O)(C(=O)OCCCCC)CC(=O)OCCCCC DXRFOGXSSDRZFP-UHFFFAOYSA-N 0.000 description 2
- FJMKXRHMJBDWHX-UHFFFAOYSA-N 2-(2-hexadecoxy-2-oxoethyl)-2-hydroxybutanedioic acid Chemical compound CCCCCCCCCCCCCCCCOC(=O)CC(O)(C(O)=O)CC(O)=O FJMKXRHMJBDWHX-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 208000037259 Amyloid Plaque Diseases 0.000 description 1
- 208000019751 Anorectal disease Diseases 0.000 description 1
- 208000016583 Anus disease Diseases 0.000 description 1
- 208000035484 Cellulite Diseases 0.000 description 1
- 229920001661 Chitosan Polymers 0.000 description 1
- 241001517488 Clavus Species 0.000 description 1
- 102000008186 Collagen Human genes 0.000 description 1
- 108010035532 Collagen Proteins 0.000 description 1
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 108010014258 Elastin Proteins 0.000 description 1
- 102000016942 Elastin Human genes 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 206010015150 Erythema Diseases 0.000 description 1
- 239000001856 Ethyl cellulose Substances 0.000 description 1
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 description 1
- RGHNJXZEOKUKBD-SQOUGZDYSA-N Gluconic acid Natural products OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 description 1
- 229920002683 Glycosaminoglycan Polymers 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 description 1
- 239000004354 Hydroxyethyl cellulose Substances 0.000 description 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000007117 Oral Ulcer Diseases 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 206010049752 Peau d'orange Diseases 0.000 description 1
- 206010051246 Photodermatosis Diseases 0.000 description 1
- 229920001273 Polyhydroxy acid Polymers 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 206010039792 Seborrhoea Diseases 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 206010043189 Telangiectasia Diseases 0.000 description 1
- 238000010306 acid treatment Methods 0.000 description 1
- 150000008279 aldosamines Chemical class 0.000 description 1
- 150000004716 alpha keto acids Chemical class 0.000 description 1
- 229940024606 amino acid Drugs 0.000 description 1
- 235000001014 amino acid Nutrition 0.000 description 1
- 238000004176 ammonification Methods 0.000 description 1
- SWLVFNYSXGMGBS-UHFFFAOYSA-N ammonium bromide Chemical compound [NH4+].[Br-] SWLVFNYSXGMGBS-UHFFFAOYSA-N 0.000 description 1
- 230000036592 analgesia Effects 0.000 description 1
- 229940035674 anesthetics Drugs 0.000 description 1
- 239000002260 anti-inflammatory agent Substances 0.000 description 1
- 229940121363 anti-inflammatory agent Drugs 0.000 description 1
- 229940125713 antianxiety drug Drugs 0.000 description 1
- 239000003429 antifungal agent Substances 0.000 description 1
- 239000004599 antimicrobial Substances 0.000 description 1
- 239000003443 antiviral agent Substances 0.000 description 1
- 235000019606 astringent taste Nutrition 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 229960001631 carbomer Drugs 0.000 description 1
- 230000036232 cellulite Effects 0.000 description 1
- 239000012459 cleaning agent Substances 0.000 description 1
- 239000002131 composite material Substances 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 230000018109 developmental process Effects 0.000 description 1
- LCKIPSGLXMCAOF-UHFFFAOYSA-N dibenzyl 2,3-dihydroxybutanedioate Chemical compound C=1C=CC=CC=1COC(=O)C(O)C(O)C(=O)OCC1=CC=CC=C1 LCKIPSGLXMCAOF-UHFFFAOYSA-N 0.000 description 1
- 125000004177 diethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- XEBCWEDRGPSHQH-UHFFFAOYSA-N diisopropyl tartrate Chemical compound CC(C)OC(=O)C(O)C(O)C(=O)OC(C)C XEBCWEDRGPSHQH-UHFFFAOYSA-N 0.000 description 1
- PVRATXCXJDHJJN-UHFFFAOYSA-N dimethyl 2,3-dihydroxybutanedioate Chemical compound COC(=O)C(O)C(O)C(=O)OC PVRATXCXJDHJJN-UHFFFAOYSA-N 0.000 description 1
- LSFNVBFEFPZYFU-UHFFFAOYSA-N dioctyl 2,3-dihydroxybutanedioate Chemical compound CCCCCCCCOC(=O)C(O)C(O)C(=O)OCCCCCCCC LSFNVBFEFPZYFU-UHFFFAOYSA-N 0.000 description 1
- CHNUEARJLWZWOD-UHFFFAOYSA-N dipentyl 2,3-dihydroxybutanedioate Chemical compound CCCCCOC(=O)C(O)C(O)C(=O)OCCCCC CHNUEARJLWZWOD-UHFFFAOYSA-N 0.000 description 1
- WCHBXSPACACNBJ-UHFFFAOYSA-N dipropyl 2,3-dihydroxybutanedioate Chemical compound CCCOC(=O)C(O)C(O)C(=O)OCCC WCHBXSPACACNBJ-UHFFFAOYSA-N 0.000 description 1
- 229920002549 elastin Polymers 0.000 description 1
- 231100000321 erythema Toxicity 0.000 description 1
- 229920001249 ethyl cellulose Polymers 0.000 description 1
- 235000019325 ethyl cellulose Nutrition 0.000 description 1
- 229940116333 ethyl lactate Drugs 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 230000005284 excitation Effects 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 239000000174 gluconic acid Substances 0.000 description 1
- 235000012208 gluconic acid Nutrition 0.000 description 1
- 235000003969 glutathione Nutrition 0.000 description 1
- 239000008309 hydrophilic cream Substances 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 229940071826 hydroxyethyl cellulose Drugs 0.000 description 1
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 description 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- 210000000088 lip Anatomy 0.000 description 1
- 210000003141 lower extremity Anatomy 0.000 description 1
- 229940049920 malate Drugs 0.000 description 1
- OJURWUUOVGOHJZ-UHFFFAOYSA-N methyl 2-[(2-acetyloxyphenyl)methyl-[2-[(2-acetyloxyphenyl)methyl-(2-methoxy-2-oxoethyl)amino]ethyl]amino]acetate Chemical compound C=1C=CC=C(OC(C)=O)C=1CN(CC(=O)OC)CCN(CC(=O)OC)CC1=CC=CC=C1OC(C)=O OJURWUUOVGOHJZ-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 201000003152 motion sickness Diseases 0.000 description 1
- 210000002200 mouth mucosa Anatomy 0.000 description 1
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical group CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 1
- 229940101309 nervine Drugs 0.000 description 1
- 239000003605 opacifier Substances 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 230000008845 photoaging Effects 0.000 description 1
- 230000035479 physiological effects, processes and functions Effects 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- UBYZGUWQNIEQMH-SBBOJQDXSA-M potassium;(2s,3s,4s,5r)-2,3,4,5,6-pentahydroxy-6-oxohexanoate Chemical compound [K+].OC(=O)[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O UBYZGUWQNIEQMH-SBBOJQDXSA-M 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 150000004492 retinoid derivatives Chemical class 0.000 description 1
- 208000008742 seborrheic dermatitis Diseases 0.000 description 1
- 239000002453 shampoo Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 229940095064 tartrate Drugs 0.000 description 1
- 208000009056 telangiectasis Diseases 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 210000000515 tooth Anatomy 0.000 description 1
- SJOHMMKAEJOQRW-UHFFFAOYSA-N tribenzyl 1,2-dihydroxypropane-1,2,3-tricarboxylate Chemical compound C=1C=CC=CC=1COC(=O)CC(O)(C(=O)OCC=1C=CC=CC=1)C(O)C(=O)OCC1=CC=CC=C1 SJOHMMKAEJOQRW-UHFFFAOYSA-N 0.000 description 1
- RFTVDKFKJAOMOP-UHFFFAOYSA-N tripropan-2-yl 1,1,2-trihydroxypropane-1,2,3-tricarboxylate Chemical compound CC(C)OC(=O)CC(O)(C(=O)OC(C)C)C(O)(O)C(=O)OC(C)C RFTVDKFKJAOMOP-UHFFFAOYSA-N 0.000 description 1
- ZORQQMOCWSOKCJ-UHFFFAOYSA-N tripropan-2-yl 1,2-dihydroxypropane-1,2,3-tricarboxylate Chemical compound CC(C)OC(=O)CC(O)(C(=O)OC(C)C)C(O)C(=O)OC(C)C ZORQQMOCWSOKCJ-UHFFFAOYSA-N 0.000 description 1
- FQAZRHVERGEKOS-UHFFFAOYSA-N tripropan-2-yl 2-hydroxypropane-1,2,3-tricarboxylate Chemical compound CC(C)OC(=O)CC(O)(C(=O)OC(C)C)CC(=O)OC(C)C FQAZRHVERGEKOS-UHFFFAOYSA-N 0.000 description 1
- 208000013464 vaginal disease Diseases 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
Landscapes
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
A composition and method for producing a beneficial effect on nerves associated with at least one of a cosmetic, dermatological, and dental indication and another condition in a patient. The compositions comprise a hydroxy-polycarboxylate and are formulated for topical administration to a patient to produce a beneficial effect. The method comprises topically applying to the area of the patient in need of the beneficial effect a hydroxy-polycarboxylic acid ester in an amount effective to produce the beneficial effect.
Description
The cross reference of related application
[0002] according to the 119th (e) money of the 35th piece of united states patent law of United States code (35U.S.C. § 119 (e)), authorize the U.S. Provisional Patent Application of submitting in 17 days October in 2005 that the application requires the 60/727th, the priority that No. the 60/759th, 525, No. 419 and the U.S. Provisional Patent Application submitted on January 17th, 2006.
Background of invention
[0003] the application relates to the purposes of the compositions that comprises hydroxyl-polycarboxylate (hydroxy-oligocarboxylicester), and it can be useful beauty treatment section disease (cosmetic conditions), odontopathy, dermatosis indication and other disease to neural effect (particularly relating to sensation and slight anesthesia character) wherein to alleviate or to improve that said composition is used for topical administration.
[0004] title is the United States Patent (USP) the 5th of " amphoteric composition of alpha-hydroxy acid and polymer form and therapeutic use thereof ", 091, No. 171, the preventative and therapeutic treatment of the amphoteric composition that adopts the polymer form that comprises alpha-hydroxy acid, α keto acid related compound or hydroxy acid has been described to alleviate beauty treatment section's disease and skin condition of illness.Title is No. the 5th, 547,988, the United States Patent (USP) of " alleviating the skin aging sign with glycolic, lactic acid or citric acid ", described 'alpha '-hydroxy acids and alleviated or improve purposes with inherent aging and external aging relevant skin, fingernail and hair variation sign.Title is No. the 5th, 385,938, the United States Patent (USP) of " method that adopts glycolic treatment wrinkle ", has described the purposes of glycolic topical therapeutic wrinkle.Title is the United States Patent (USP) the 5th of " phenyl α acyloxy alkanoic acid, derivant and therapeutic use thereof ", 258, No. 391, described the topical compositions that comprises phenyl α acyloxy alkanoic acid and derivant and strengthened fingernail, skin, lip and the cornified purposes of other mucosas.
[0005] title is No. the 5th, 665,776, the United States Patent (USP) of " the auxiliary enhancing local action of medicine ", has described the purposes that hydroxy carboxylic acid strengthens the therapeutical effect of cosmetics or pharmaceutical formulation.Title is the United States Patent (USP) the 5th of " the Alpha-hydroxy acid esters that is used for skin aging ", 686, No. 489, described the Alpha-hydroxy acid esters by stimulate the corium composition for example the biosynthesis of glycosaminoglycans, proteoglycan, collagen protein and elastin laminin increase the purposes that skin thickness and treatment comprise the aging relevant body wall variation of senile plaque, skin line, wrinkle, photoaging and aging skin.Title is No. the 5th, 889,054, the United States Patent (USP) of " method that adopts beta hydroxy acid treatment wrinkle ", has described the purposes that the compositions that comprises beta-hydroxy acid is used for topical therapeutic and aging relevant skin variation.Title is the United States Patent (USP) the 6th of " adopting hydroxy carboxylic acid or related compound to be used for the treatment of the method that aging with the inherence and external aging relevant skin changes ", 060, No. 512, described the compositions that comprises hydroxy carboxylic acid and be used for the purposes that aging with the inherence and the external aging relevant skin of topical therapeutic changes.Both titles are the United States Patent (USP) the 6th, 335, No. 023 and 6,740, No. 327 of " oligosaccharide glycuronic acid and topical use thereof ", have described the compositions that comprises the oligosaccharide glycuronic acid and have been used for topical therapeutic cosmetics symptom and dermopathic purposes.Title is the United States Patent (USP) the 6th of " method that adopts aging with the inherence and the external aging relevant skin of hydroxy carboxylic acid or related compound treatment to change ", 767, No. 924, described the compositions that in the both sexes system, comprises polyhydroxy acid and be used for topical therapeutic and the interior purposes that changes at the aging and external relevant skin that wears out.
[0006] Shang Mian patent does not have one to describe or hinted by the topical administration hydroxy polycarboxylic acid esters, such as hydroxydicarboxylic acid's ester or hydroxyl tricarboxylic ester effect or the effect to one or more nerves.
The invention summary
[0007] although hydroxyl-monocarboxylate does not act on nerve, but one aspect of the present invention is based on following discovery: with hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester and more preferably the hydroxyl tricarboxylic ester be locally applied to mucosa, organ or position for example behind the lip, produce sensuously and slight anesthetic action and to be used for can be useful beauty treatment section or dentistry disease, skin indication or another kind of disease to neural effect wherein.
[0008] another aspect of the invention is to use to comprise and be used for topical to alleviate or to improve the method for compositions that comprises pain, pruritus, inflammation, erythema, dermatitis, eczema, psoriasis with nerve, skin or tooth system diseases associated, symptom or syndrome and be used for the hydroxyl-polycarboxylate of wound healing.Described hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester and more preferably the hydroxyl tricarboxylic ester be the antioxidant neutral compound, comprise, for example diethyl tartrate., triethyl citrate, citric acid three propyl ester and citric acid three isopropyl esters.
[0009] of the present invention on the one hand be again to the patient with beauty treatment section disease, dermatosis indication and dentistry indication and another disease in the method for at least a relevant nerve generation beneficial effect, this method is included in the amount local application hydroxyl-polycarboxylate of the zone of needs of patients beneficial effect with effective generation beneficial effect.
[0010] be on the other hand again to the patient with beauty treatment section disease, dermatosis indication and dentistry indication and another disease at least a relevant nerve produce the method for beneficial effect, this method is included in the zone that the needs beneficial effect amount local application patient hydroxyl-polycarboxylate with effective generation beneficial effect, and wherein beneficial effect is at least a in sensation (sensuous) effect to nerve and the slight anesthetic action.
Definition
[0011] as used herein, singulative " ", " one " and " being somebody's turn to do " comprise plural object, unless context clearly indicates in addition.Mean one or more when for example relating to disease, disease, indication, symptom or syndrome and plant such disease, disease, indication, symptom or syndrome.
[0012] as used herein, term " beneficial effect " means the needed effect of benefit to planning, no matter be prevention or the inhibitory action of alleviating disease or the positive effect that needs, potentiation for example, happy typically sensation or consciousness or incentive action.
[0013] as used herein, " slight anesthetic action " is to such an extent as to still have the effect that to a certain degree sensation level of sensitivity has beneficial effect for nerve, the organ or tissue of wherein anesthesia.
[0014] as used herein, " sensorial effect " is for the excitation sense of gratification or the effect of the sense aspect of taking the lead, and level of sensitivity has beneficial effect.
[0015] as used herein, term " treatment ", " treatment " etc. refer to the beneficial effect that can be pharmacology, physiology, dermatological and/or sensorial effect that obtains requiring.Beneficial effect can be preventative preventing aspect disease or disease or the symptom wholly or in part, and/or partially or completely cure disease or disease and/or be attributable to disease or the side effect of disease and/or situation in sensation treatment in cause aspect the enhanced sensation it can is curative.Therefore, for example " treatment " or " treatment " be included in animal, preferably in mammal and more preferably any treatment of the disease in the people or disease, and comprise: (a) but be present in can easy ill disease or the disease patient's who is not still diagnosed strictly according to the facts disease or disease in prevention; (b) suppress disease or disease, for example suppress its development; (c) alleviate, alleviate or improve disease or disease, for example cause that disease or disease alleviate; All these, beneficial effect wherein is to need inhibitory action." treatment " or " treatment " also comprises existence or the enhancing that causes the sensation situation, and beneficial effect wherein is that the positive that needs strengthens sensation, consciousness or incentive action.
Detailed Description Of The Invention
[0016] the present invention is based on following discovery: when hydroxyl-polycarboxylate is used in the part, preferred hydroxydicarboxylic acid's ester or more preferably the hydroxyl tricarboxylic ester can be to mucocutaneous organs or for example lip, mouth, gums, nostril, nipple, cysthus, vagina, penis and anus sensigenous, consciousness and slightly anesthetic action of position for example during citric acid three propyl ester.The applicant also has been found that for example gluconic acid ethyl ester and ethyl lactate not sensigenous or slight anesthetic action under the same conditions of hydroxyl monocarboxylate by comparison.By hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester the or more preferably sensation that produces of hydroxyl tricarboxylic ester and consciousness effect are different from fully by for example paralysis effect that causes of lignocaine and procaine of local anesthetic.The sensation, consciousness and the slight anesthetic action that are produced by hydroxyl of the present invention-polycarboxylate continue a few minutes usually to several hours.Nervine like this sensation or effect have many beauty treatments section, dentistry and Dermatology purposes.For example, will comprise hydroxyl-polycarboxylate, preferably comprise hydroxydicarboxylic acid's ester more preferably comprise the lipstick of hydroxyl tricarboxylic ester or lip gloss local application patient's lip after, sensation or consciousness can be provided.Can have useful application to neural sensation and some anesthetic action like this by what hydroxyl-polycarboxylate produced, for example alleviate the pruritus and the pain of lip, mouth, gums, nostril, nipple, cysthus, vagina, penis and anus, and be used for eczema, hemorrhoid, drying or with cysthus and the aging relevant disease of associated change of vagina.
[0017] one aspect of the invention is to the patient with beauty treatment section disease, dermatosis indication and dentistry indication and another disease at least a relevant nerve produce the method for beneficial effect, this method is included in the amount local application hydroxyl-polycarboxylate of the zone of needs of patients beneficial effect with effective generation beneficial effect.
[0018] be on the other hand to the patient with beauty treatment section disease, dermatosis indication and dentistry indication and another disease at least a relevant nerve produce the method for beneficial effect, method is included in the zone that the needs beneficial effect amount local application patient hydroxyl-polycarboxylate with effective generation beneficial effect, and wherein beneficial effect is at least a in the sensorial effect of nerve and the slight anesthetic action.
[0019] hydroxyl-polycarboxylate comprises at least a in diethyl malate, triethyl citrate, citric acid three propyl ester, citric acid three isopropyl esters, glucosaccharic acid diethylester (diethyl glucate) and the glucosaccharic acid dipropyl (dipropyl glucate) and their any combination.
[0020] another aspect of the present invention is hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester or more preferably the hydroxyl tricarboxylic ester cure and the disease that alleviates the pain relevant, infection, inflammation and mucocutaneous organs or the position purposes of aphtha and toothache for example with wound healing.For oral disease, hydroxyl-polycarboxylate is formulated as solution or gel is used to wash mouthful, gargles or massage.
[0021] hydroxyl-polycarboxylate of the present invention is the antioxidant neutral compound.Of the present invention be antioxidant hydroxyl-polycarboxylate on the one hand again, be preferably hydroxydicarboxylic acid's ester or more preferably for the conduct of hydroxyl tricarboxylic ester by daylight, chemicals, laser treatment, free radical, electromagnetic radiation, the ionizing radiation for example mucocutaneous organs that causes of alpha ray, β ray, X-ray, gamma-rays or damage, insect bite or stimulation or the preventative nursing of other oxidative damages or the purposes of treatment of position, skin, hair or fingernail.
[0022] of the present invention is the application of hydroxyl-polycarboxylate at skin or mucocutaneous organs, position or damage location more on the one hand, and it is used for local prevention or treatment is selected from acne; Rosacea; Skin defective; Cellulitis (cellulite); Dermatosis; Dermatitis; Skin or nail infection; The dandruff; Xerosis cutis; Axersis; Eczema; Herpes; Ichthyosis (ichthyosis); Pseudofolliculitis barbae (pseudofolliculitis barbae); Pruritus; Psoriasis; Striae gravidarum (stretchmarks); Wart; Oral cavity or Gum disease; Zest, inflammatory, unsound, damage or unusual mucosa, skin, hair, fingernail, nostril, auditory meatus, anus or vaginal disorder; Unsmooth and the rough surface of skin, fingernail and hair; Reactivity, zest or telangiectasis skin; Be used for skin bleaching and blast and wound healing.
[0023] hydroxyl-polycarboxylate of the present invention is represented one group of organic compound that contains one or more hydroxyl and 2-10 carboxyl in molecule.Preferred hydroxyl-polycarboxylate contains one or more hydroxyl and 2-3 carboxyl in molecule.Most preferred hydroxyl-polycarboxylate contains one or more hydroxyl and 3 carboxyls in molecule, for example triethyl citrate and citric acid three propyl ester.
[0024] hydroxyl-polycarboxylate of the present invention can be described as follows.
[0025] (A) hydroxydicarboxylic acid's ester
[0026] hydroxydicarboxylic acid's ester can be divided into two groups, and one group is that monohydroxy dicarboxylic ester and another group are the dihydroxy dicarboxylic ester.
[0027] (1) monohydroxy dicarboxylic ester
The monohydroxy dicarboxylic ester contains a hydroxyl and two carboxyls.Universal architecture can be expressed as with following formula I:
R
1OOC C(OH)R
2 CHR
4 COOR
3 (I)
R wherein
1And R
3Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2And R
4Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the monohydroxy dicarboxylic ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0028] if the universal architecture of formula I can not comprise concrete monohydroxy dicarboxylic ester, chemical compound will be represented by its chemical name.
[0029] following is representational hydroxydicarboxylic acid's ester:
[0030] 2-hydroxyl fourth-1,4-two acid esters (malate): malic acid dimethyl ester, diethyl malate, malic acid dipropyl, malic acid diisopropyl ester, malic acid diamyl ester, malic acid dioctyl ester, malic acid diisooctyl ester and malic acid dibenzyl ester.
[0031] 2-hydroxy-2-methyl-Ding-1,4-two acid esters (citramalic acid ester): citramalic acid dimethyl ester, citramalic acid diethylester, citramalic acid dipropyl, citramalic acid diisopropyl ester, citramalic acid diamyl ester, citramalic acid dioctyl ester, citramalic acid diisooctyl ester and citramalic acid dibenzyl ester.
[0032] (2) dihydroxy dicarboxylic ester
[0033] the dihydroxy dicarboxylic ester contains two hydroxyls and two carboxyls.Universal architecture can be expressed as with Formula Il:
R
1OOC C(OH)R
2C(OH)R
4COOR
3 (II)
R wherein
1And R
3Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2And R
3Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the dihydroxy dicarboxylic ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0034] if the universal architecture of formula II can not comprise concrete dihydroxy dicarboxylic ester, chemical compound will be represented by its chemical name.
[0035] following is representational dihydroxy dicarboxylic ester:
[0036] 2,3-dihydroxy fourth-1,4-two acid esters (tartrate): dimethyl tartrate, diethyl tartrate., dipropyl tartrate, tartaric acid diisopropyl ester, diamyl tartrate, tartaric acid dioctyl ester, tartaric acid diisooctyl ester and tartaric acid dibenzyl ester.
[0037] (B) hydroxyl tricarboxylic ester
[0038] the hydroxyl tricarboxylic ester can be divided into three groups; (1) monohydroxy tricarboxylic ester, (2) dihydroxy tricarboxylic ester and (3) trihydroxy tricarboxylic ester.
[0039] (1) monohydroxy tricarboxylic ester
[0040] the monohydroxy tricarboxylic ester contains 1 hydroxyl and 3 carboxyls and can be divided into 4 groups, (a) citrate, (b) 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester, (c) Homocitric acid ester and (d) homoisocitric acid ester.
[0041] (a) citrate
[0042] universal architecture of citrate can be expressed as following formula III:
R
1OOC CHR
2C(OH)(COOR
3)CHR
4 COOR
5 (III)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2And R
4Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That citrate can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0043] if the universal architecture of formula III can not comprise concrete citrate, chemical compound will be represented by its chemical name.
[0044] following is representational citrate:
[0045] 3-hydroxyl-3-carboxyl penta-1,5-two acid esters (citrate): trimethyl citrate, triethyl citrate, citric acid three propyl ester, citric acid triisopropyl ester, tripentyl citrates, trioctyl lemon acid, citric acid three isooctyl acrylate, citric acid tribenzyl ester and citric acid three cigarette esters (trinicotinyl citrate).
[0046] 2-n-hexadecyl-3-hydroxyl-3-carboxyl penta-1,5-two acid esters (armillaria Matsutake acid esters (agaricate esters), n-hexadecyl citrate): agaric acid trimethyl, agaric acid triethyl, agaric acid three propyl ester, agaric acid triisopropyl ester, agaric acid triamyl, agaric acid three monooctyl esters, agaric acid three isooctyl acrylate, agaric acid tribenzyl ester and agaric acid three cigarette esters.
[0047] (b) 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester
[0048] universal architecture of 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester can be expressed as with following formula IV:
R
1OOC C(OH)R
2 CR
4(COOR
3)CHR
6 COOR
3 (IV)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4And R
6Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0049] if the universal architecture of formula IV can not comprise concrete 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester, chemical compound will be represented by its chemical name.
[0050] following is representational 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester:
[0051] 2-hydroxyl-3-carboxyl penta-1,5-two acid esters (1-Hydroxy-1,2,3-propanetricarboxylic acid. ester): 1-Hydroxy-1,2,3-propanetricarboxylic acid. trimethyl, 1-Hydroxy-1,2,3-propanetricarboxylic acid. triethyl, 1-Hydroxy-1,2,3-propanetricarboxylic acid. three propyl ester, 1-Hydroxy-1,2,3-propanetricarboxylic acid. triisopropyl ester, 1-Hydroxy-1,2,3-propanetricarboxylic acid. triamyl, 1-Hydroxy-1,2,3-propanetricarboxylic acid. three monooctyl esters, 1-Hydroxy-1,2,3-propanetricarboxylic acid. three isooctyl acrylate, 1-Hydroxy-1,2,3-propanetricarboxylic acid. tribenzyl ester and 1-Hydroxy-1,2,3-propanetricarboxylic acid. three cigarette esters.
[0052] (c) Homocitric acid ester
The universal architecture of Homocitric acid ester can be expressed as with following formula V:
R
1OOC CHR
2C(OH)(COOR
3)CHR
4 CHR
6 COOR
5 (V)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4And R
6Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the Homocitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0053] if the universal architecture of formula V can not comprise concrete Homocitric acid ester, chemical compound will be represented by its chemical name.
[0054] following is representational Homocitric acid ester:
[0055] 3-hydroxyl-3-carboxyl oneself-1,6-two acid esters (Homocitric acid ester): Homocitric acid trimethyl, Homocitric acid triethyl, Homocitric acid three propyl ester, Homocitric acid triisopropyl ester, Homocitric acid triamyl, Homocitric acid three monooctyl esters, Homocitric acid three isooctyl acrylate, Homocitric acid tribenzyl ester and Homocitric acid three cigarette esters.
[0056] (d) homoisocitric acid ester
[0057] universal architecture of homoisocitric acid ester can be expressed as with following formula VI:
R
1OOC C(OH)R
2CR
4(COOR
3)CHR
6 CHR
7COOR
5 (VI)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4, R
6And R
7Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the homoisocitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0058] if the universal architecture of formula VI can not comprise concrete homoisocitric acid ester, chemical compound will be represented by its chemical name.
[0059] following is representational homoisocitric acid ester:
[0060] 2-hydroxyl-3-carboxyl oneself-1,6-two acid esters (homoisocitric acid ester): homoisocitric acid trimethyl, homoisocitric acid triethyl, homoisocitric acid three propyl ester, homoisocitric acid triisopropyl ester, homoisocitric acid triamyl, homoisocitric acid three monooctyl esters, homoisocitric acid three isooctyl acrylate, homoisocitric acid tribenzyl ester and homoisocitric acid three cigarette esters.
[0061] (2) dihydroxy tricarboxylic ester
[0062] the dihydroxy tricarboxylic ester contains 2 hydroxyls and 3 carboxyls.The dihydroxy tricarboxylic ester that has 5 subgroups: (a) hydroxycitric acid ester; (b) hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester; (c) hydroxyl Homocitric acid ester; (d) hydroxyl homoisocitric acid ester; (e) 4,5-dihydroxy-3-carboxyl hexane-1,6-two acid esters.
[0063] (a) hydroxycitric acid ester
[0064] universal architecture can be expressed as with following formula VII:
R
1OOC C(OH)R
2C(OH)(COOR
3)CHR
4 COOR
5 (VII)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2And R
4Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the hydroxycitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0065] if the universal architecture of formula VII can not comprise concrete hydroxycitric acid ester, chemical compound will be represented by its chemical name.
[0066] following is representational hydroxycitric acid ester:
[0067] 2,3-dihydroxy-3-carboxyl penta-1,5-two acid esters (hydroxycitric acid ester): hydroxycitric acid trimethyl, hydroxycitric acid triethyl, hydroxycitric acid three propyl ester, hydroxycitric acid triisopropyl ester, hydroxycitric acid triamyl, hydroxycitric acid three monooctyl esters, hydroxycitric acid three isooctyl acrylate, hydroxycitric acid tribenzyl ester and hydroxycitric acid three cigarette esters.
[0068] 2-n-hexadecyl-2,3-dihydroxy-3-carboxyl penta-1,5-two acid esters and 4-n-hexadecyl-2,3-dihydroxy-3-carboxyl penta-1,5-two acid esters (hydroxyl armillaria Matsutake acid esters, n-hexadecyl hydroxycitric acid ester): hydroxyl agaric acid trimethyl, hydroxyl agaric acid triethyl, hydroxyl agaric acid three propyl ester, hydroxyl agaric acid triisopropyl ester, hydroxyl agaric acid triamyl, hydroxyl agaric acid three monooctyl esters, hydroxyl agaric acid three isooctyl acrylate, hydroxyl agaric acid tribenzyl ester and hydroxyl agaric acid three cigarette esters.
[0069] (b) hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester
[0070] universal architecture can be expressed as with following formula VIII:
R
1OOC C(OH)R
2CR
4(COOR
3)C(OH)R
6COOR
5 (VIII)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4And R
6Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0071] if the universal architecture of formula VIII can not comprise concrete hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester, chemical compound will be represented by its chemical name.
[0072] following is representational hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester:
[0073] 2,4-dihydroxy-3-carboxyl penta-1,5-two acid esters (hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. ester): hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. trimethyl, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. triethyl, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. three propyl ester, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. triisopropyl ester, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. triamyl, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. three monooctyl esters, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. three isooctyl acrylate, hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. tribenzyl ester and hydroxyl 1-Hydroxy-1,2,3-propanetricarboxylic acid. three cigarette esters.
[0074] (c) hydroxyl Homocitric acid ester
[0075] because there are 3 kinds of universal architectures that can be expressed as with following formula IX, X and XI in the position of second hydroxyl:
R
1OOC C(OH)R
2C(OH)(COOR
3)CHR
4 CHR
6 COOR
5 (IX)
R
1OOC CHR
2C(OH)(COOR
3)C(OH)R
4 CHR
6 COOR
5 (X)
R
1OOC CHR
2C(OH)(COOR
3)CHR
4 C(OH)R
6 COOR
5 (XI)
Wherein in each of formula IX, X and XI, R
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4And R
6Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That hydroxyl Homocitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0076] if the universal architecture of formula IX, X or XI can not comprise concrete hydroxyl Homocitric acid ester, chemical compound will be represented by its chemical name.
[0077] following is representational hydroxyl Homocitric acid ester:
[0078] 2,3-dihydroxy-3-carboxyl own-1,6-two acid esters, 3,4-dihydroxy-3-carboxyl own-1,6-two acid esters and 3,5-dihydroxy-3-carboxyl oneself-1,6-two acid esters (hydroxyl Homocitric acid ester): hydroxyl Homocitric acid trimethyl, hydroxyl Homocitric acid triethyl, hydroxyl Homocitric acid three propyl ester, hydroxyl Homocitric acid triisopropyl ester, hydroxyl Homocitric acid triamyl, hydroxyl Homocitric acid three monooctyl esters, hydroxyl Homocitric acid three isooctyl acrylate, hydroxyl Homocitric acid tribenzyl ester and hydroxyl Homocitric acid three cigarette esters.
[0079] (d) hydroxyl homoisocitric acid ester
[0080] because there are 2 kinds of universal architectures that can be expressed as with following formula XII and XIII in the position of second hydroxyl:
R
1OOC C(OH)R
2CR
4(COOR
3)C(OH)R
6 CHR
7 COOR
5 (XII)
R
1OOC C(OH)R
2CR
4(COOR
3)CHR
6C(OH)R
7COOR
5 (XIII)
Wherein in each of formula XII and XIII, R
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4, R
6And R
7Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That hydroxyl homoisocitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0081] if the universal architecture of formula XII or XIII can not comprise concrete hydroxyl homoisocitric acid ester, chemical compound will be represented by its chemical name.
[0082] following is representational hydroxyl homoisocitric acid ester:
[0083] 2,4-dihydroxy-3-carboxyl own-1,6-two acid esters and 2,5-dihydroxy-3-carboxyl oneself-1,6-two acid esters (hydroxyl homoisocitric acid ester): hydroxyl homoisocitric acid trimethyl, hydroxyl homoisocitric acid triethyl, hydroxyl homoisocitric acid three propyl ester, hydroxyl homoisocitric acid triisopropyl ester, hydroxyl homoisocitric acid triamyl, hydroxyl homoisocitric acid three monooctyl esters, hydroxyl homoisocitric acid three isooctyl acrylate, hydroxyl homoisocitric acid tribenzyl ester and hydroxyl homoisocitric acid three cigarette esters.
[0084] (e) 4,5-dihydroxy-3-carboxyl oneself-1,6-two acid esters
[0085] universal architecture can be expressed as with following formula XIV:
R
1OOC CHR
2CR
4(COOR
3)C(OH)R
6 C(OH)R
7COOR
5 (XIV)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4, R
6And R
7Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.4,5-dihydroxy-3-carboxyl oneself-1, that 6-two acid esters can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0086] concrete 4 if the universal architecture of formula XIV can not comprise, 5-dihydroxy-3-carboxyl oneself-1,6-two acid esters, chemical compound will be represented by its chemical name.
[0087] following be representational 4, and 5-dihydroxy-3-carboxyl is own-1,6-two acid esters: 4,5-dihydroxy-3-carboxyl own-1,6-diacid trimethyl, 4,5-dihydroxy-3-carboxyl oneself-1,6-diacid triethyl, 4,5-dihydroxy-3-carboxyl own-1,6-diacid three propyl ester, 4,5-dihydroxy-3-carboxyl oneself-1,6-diacid triisopropyl ester, 4,5-dihydroxy-3-carboxyl own-1,6-diacid triamyl, 4,5-dihydroxy-3-carboxyl oneself-1,6-diacid three monooctyl esters, 4,5-dihydroxy-3-carboxyl own-1,6-diacid three isooctyl acrylate, 4,5-dihydroxy-3-carboxyl oneself-1,6-diacid tribenzyl ester and 4,5-dihydroxy-3-carboxyl oneself-1,6-diacid three cigarette esters.
[0088] (3) trihydroxy tricarboxylic ester
[0089] the trihydroxy tricarboxylic ester contains 3 hydroxyls and 3 carboxyls.The trihydroxy tricarboxylic ester that has 3 subgroups: (a) dihydroxy citrate, (b) dihydroxy Homocitric acid ester and (c) dihydroxy homoisocitric acid ester.
[0090] (a) dihydroxy citrate
[0091] universal architecture can be expressed as with following formula XV:
R
1OOC C(OH)R
2C(OH)(COOR
3)C(OH)R
4 COOR
5 (XV)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2And R
4Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That the dihydroxy citrate can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0092] if the universal architecture of formula XV can not comprise concrete dihydroxy citrate, chemical compound will be represented by its chemical name.
[0093] following is representational dihydroxy citrate: 2,3,4-trihydroxy-3-carboxyl penta-1,5-two acid esters (dihydroxy citrate): dihydroxy trimethyl citrate, dihydroxy triethyl citrate, dihydroxy citric acid three propyl ester, dihydroxy citric acid triisopropyl ester, dihydroxy tripentyl citrates, dihydroxy trioctyl lemon acid, dihydroxy citric acid three isooctyl acrylate, dihydroxy citric acid tribenzyl ester and dihydroxy citric acid three cigarette esters.
[0094] (b) dihydroxy Homocitric acid ester
[0095] because there are 3 kinds of universal architectures that can be expressed as following formula XVI, XVII and XVIII in the position of second and the 3rd hydroxyl:
R
1OOC C(OH)R
2C(OH)(COOR
3)C(OH)R
4 CHR
6 COOR
5 (XVI)
R
1OOC C(OH)R
2C(OH)(COOR
3)CHR
4C(OH)R
6 COOR
5 (XVII)
R
1OOC CHR
2C(OH)(COOR
3)C(OH)R
4 C(OH)R
6 COOR
5 (XVIII)
Wherein in each of formula XVI, XVII and XVIII, R
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4And R
6Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That dihydroxy Homocitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[0096] if the universal architecture of formula XVI, XVII or XVIII can not comprise concrete dihydroxy Homocitric acid ester, chemical compound will be represented by its chemical name.
[0097] following is representational dihydroxy Homocitric acid ester:
[0098] 2,3,4-trihydroxy-3-carboxyl own-1,6-two acid esters, 2,3,5-trihydroxy-3-carboxyl own-1,6-two acid esters and 3,4,5-trihydroxy-3-carboxyl oneself-1,6-two acid esters (dihydroxy Homocitric acid ester): dihydroxy Homocitric acid trimethyl, dihydroxy Homocitric acid triethyl, dihydroxy Homocitric acid three propyl ester, dihydroxy Homocitric acid triisopropyl ester, dihydroxy Homocitric acid triamyl, dihydroxy Homocitric acid three monooctyl esters, dihydroxy Homocitric acid three isooctyl acrylate, dihydroxy Homocitric acid tribenzyl ester and dihydroxy Homocitric acid three cigarette esters.
[0099] (c) dihydroxy homoisocitric acid ester
[00100] universal architecture can be expressed as with following formula XIX:
R
1OOC C(OH)R
2 CR
4(COOR
3)C(OH)R
6 C(OH)R
7 COOR
5 (XIX)
R wherein
1, R
3And R
5Be aralkyl or the aryl that has the alkyl of 1-19 carbon atom or have 6-19 carbon atom independently; R
2, R
4, R
6And R
7Independently for H, have the alkyl of 1-19 carbon atom or have the aralkyl or the aryl of 6-19 carbon atom; The H that is connected in any carbon atom can replace with I, F, Cl, Br or the alkoxyl with 1-19 carbon.That dihydroxy homoisocitric acid ester can be used as is saturated or undersaturated, stereoisomerism or non-stereomeric, straight shape or ramose chain or annular form present.
[00101] if universal architecture formula XIX can not comprise concrete dihydroxy homoisocitric acid ester, chemical compound will be represented by its chemical name.
[00102] following is representational dihydroxy homoisocitric acid ester: 2,4,5-trihydroxy-3-carboxyl oneself-1,6-two acid esters (dihydroxy homoisocitric acid ester): dihydroxy homoisocitric acid trimethyl, dihydroxy homoisocitric acid triethyl, dihydroxy homoisocitric acid three propyl ester, dihydroxy homoisocitric acid triisopropyl ester, dihydroxy homoisocitric acid triamyl, dihydroxy homoisocitric acid three monooctyl esters, dihydroxy homoisocitric acid three isooctyl acrylate, dihydroxy homoisocitric acid tribenzyl ester and dihydroxy homoisocitric acid three cigarette esters.
[00103] common, the applicant has been found that the sensation that produced by the hydroxyl tricarboxylic ester and consciousness effect are more much better than and the persistent period is longer than the described effect that is produced by hydroxydicarboxylic acid's ester.In the hydroxyl tricarboxylic ester of identical family, the applicant has been found that also the sensation and the consciousness effect that are produced by the ester than long-chain are longer than the much better than and persistent period that is produced described effect by the ester than short chain.For example, citric acid three propyl ester produce sensation and consciousness effect much better than and that the persistent period is longer than trimethyl citrate.
[00104] also cosmetics, medicinal and other topical drugs can be joined and be used for collaborative or potentiation in the present composition.Topical drug comprises, for example (is not limited to) hydroxy acid, keto acid and related compound; Phenyl α acyloxy alkanoic acid and derivant, N-acyl group-aldose amine (aldosamines), N-acylamino acid and relevant N-acyl compounds; Local analgesia medicine and anesthetics; Anti-acne drug; Antimicrobial drug; Anti-yeast medicine; Antifungal agent; Antiviral agents; Anti-infective; The anti-dandruff medicine; Anti-dermatitis medicine; Antieczematic; Antihistaminic; The antipruritic medicine; Bendectin; Motion sickness drug; Anti-inflammatory agent; Anti-hyperkeratosis medicine; Antiperspirant; Antipsoriatic; Anti-rosacea medicine; Seborrhea; Hair conditioner and hair therapy medicine; Defying age and crease-resistant medicine; Antianxiety drugs; Anticonvulsant; Antidepressants; Sun-proof and opacifier; Skin lightening agent; Depigmenting agent; Astringency; Cleaning agent; Clavus; Callus and remove the wart agent; Skin plentiful (plumping) agent; (volumizing) agent of preserving moisture that skin is plentiful; The Firm agent; Matrix metalloproteinase (MMP) inhibitor; The local cardiovascular drug of using; Wound-healing agent; Gingival or mouth care medicine; Aminoacid; The peptide class; Dipeptides; Tripeptides; Glutathion and derivant thereof; Oligopeptide; Polypeptide; Saccharide; Aminosaccharide; Vitamin; Corticosteroid; Tanning agent; Hormone and retinoid.
[0101] logical method preparation
[0102] can hydroxyl-polycarboxylate of the present invention will be contained, preferred hydroxydicarboxylic acid's ester, more preferably the compositions of hydroxyl tricarboxylic ester is formulated as solution, gel, lotion, cream, ointment, shampoo, spray, rod, pad, powder, face shield (masque), mouthwass or collutory, vagina gel or vagina preparation, or to being used for mucocutaneous position etc., such as acceptable other forms of oral mucosa, lip, nostril, cysthus, vagina, penis and nipple.
[0103] for the preparation liquid composite, with at least a hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester and more preferably the hydroxyl tricarboxylic ester be dissolved in water, ethanol, propylene glycol, butanediol and/or other local acceptable vehicle.It is about 100% that the concentration of hydroxyl-polycarboxylate can be about 0.1%-of total composition weight, and about 1%-that preferred concentration is total composition weight is about 40%, and preferred concentration is about 2%-about 20% of total composition weight.
[0104] in order to prepare the topical compositions of lotion, cream or ointment form, liquid form hydroxyl-polycarboxylate directly can be mixed with the substrate that requires, perhaps can at first be dissolved in ethanol, propylene glycol and/or other solvents, and make so the solution that obtains mixes with substrate or pharmaceutically acceptable vehicle with preparation lotion, cream or ointment.Concentration is identical with above requirement.
[0105] also topical compositions of the present invention can be formulated as the gel form.By in the solution that contains hydroxyl-polycarboxylate of the present invention, adding the gelling forming agent, such as chitosan, methylcellulose, ethyl cellulose, polyvinyl alcohol, polyquaternary amine ion, hydroxyethyl-cellulose, hydroxypropyl cellulose, hydroxypropyl emthylcellulose, carbomer or ammonification glycyrrhetate preparation typical gels agent compositions.The preferred concentration of gellant can be about 0.2%-about 2% of total composition weight.
[0106] in order to prepare the part that is used for collaborative or potentiation with associating compositions, cosmetics, medicinal or other Topically active medicines are added in the described preparation by dissolving or mixing, combine with above any compositions.
[0107] those skilled in the art can be easy to other form compositionss that fusion, preparation or preparation are used to transmit The compounds of this invention according to the disclosure.
[0108] contain hydroxyl-polycarboxylate, the compositions that preferably contains hydroxydicarboxylic acid's ester and more preferably contain the hydroxyl tricarboxylic ester can locally apply to mucocutaneous organs or the position is used for sensigenous and consciousness effect.Mucocutaneous organs or position comprise lip, mouth, gums, nostril, nipple, cysthus, vagina, penis and anus.Such as noted above, sensation that is produced by hydroxyl-polycarboxylate and consciousness effect are different from fully by for example numbness effect that causes of lignocaine and procaine of local anesthetic.The sensation and the consciousness effect that are produced by hydroxyl-polycarboxylate continue a few minutes usually to several hours.For example, will comprise hydroxydicarboxylic acid's ester preferably comprise the lipstick of hydroxyl tricarboxylic ester or lip that lip gloss is locally applied to patient after, sensation or consciousness can be provided.For example, cream or the ointment that contains 10% triethyl citrate, citric acid three propyl ester or citric acid three isopropyl esters can be locally applied to lip.After 1-2 minute, lip will experience sensation and consciousness happiness, follow very slight anesthetic action, and the people feel that lip blow-up on volume is plentiful.Such sensation continues about 10 minutes to 2 hours usually.
[0109] be useful to neural effect to many other beauty treatment sections, dentistry and dermatosis indication like this, for example alleviate the pruritus and the pain of lip, mouth, gums, nostril, nipple, cysthus, vagina, penis and anus, and be useful the disease relevant with the aging relevant variation of eczema, hemorrhoid, drying or cysthus and vagina.
[0110] contain hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester and more preferably the compositions of hydroxyl tricarboxylic ester also can locally apply to mucosa or cutaneous lesion.For example, but contain and the cream of 10% citric acid, three propyl ester or citric acid three isopropyl esters or ointment every day be locally applied to eczema or psoriasis damage 4-16 week 2 times.The pruritus relevant with eczema or psoriasis disappears in a few minutes after local application usually.
[0111] another aspect of the present invention is hydroxyl-polycarboxylate, preferred hydroxydicarboxylic acid's ester, the disease that alleviates the pain relevant with wound healing, infection and/or inflammation and mucocutaneous organs or position with more preferably hydroxyl tricarboxylic ester be the purposes of oral ulcer and toothache for example.For oral disease, hydroxyl-polycarboxylate is formulated as solution or gel form is used for the oral cavity and cleans, gargle or massage.
[0112] according to the anti-oxidant properties of hydroxyl-polycarboxylate, another aspect of the present invention is their application, and be preferably antioxidant hydroxydicarboxylic acid ester or more preferably for antioxidant hydroxyl tricarboxylic ester as to by daylight, chemicals, laser treatment, free radical, electromagnetic radiation, the ionizing radiation for example mucocutaneous organs that causes of alpha ray, β ray, X-ray, gamma-rays or damage, insect bite or stimulation or the preventative nursing of other oxidative damages or the purposes of treatment of position, skin, hair or fingernail.
[0113] now the preferred embodiments of the invention is described in detail according to following embodiment concrete, indefiniteness.
[0114] embodiment 1
[0115] glycolic ethyl ester 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% glycolic ethyl ester in the hydrophobic ointment (can not wash ointment) of unavailable water washing.
[0116] 10% glycolic ethyl ester ointment more than the local application on the lip of the male subject at an age 73.In next not sensation or consciousness in 30 minutes.This as a result the signify hydroxy monocarboxylate nerve at mucocutaneous position is not produced any effect.
[0117] embodiment 2
[0118] L-ethyl lactate 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains the 10%L-ethyl lactate can not washing in the ointment.
The above 10%L-ethyl lactate of local application ointment on the lip of the male subject at an age 73.In next not sensation or consciousness in 30 minutes.This result shows that different hydroxyl monocarboxylates does not produce any effect to the nerve at mucocutaneous position.
[0119] embodiment 3
DL-diethyl malate 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains the 10%DL-diethyl malate can not washing in the ointment.
[0120] the above 10%DL-diethyl malate of local application ointment on the lip of the male subject at an age 73.After 1-2 minute, lip has experienced lasting about 10-about 20 minutes sensation and sense of fullness.Effect signify hydroxy dicarboxylic ester to nervus labialis can provide useful effect like this, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0121] embodiment 4
[0122] D-diethyl tartrate. 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains the 10%D-diethyl tartrate. can not washing in the ointment.
[0123] the above 10%D-diethyl tartrate. of local application ointment on the lip of the male subject at an age 73.After 1-2 minute, lip has experienced lasting about 10-about 20 minutes slight sensation and sense of fullness.Effect to nervus labialis shows that the dihydroxy dicarboxylic ester can provide useful effect like this, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0124] embodiment 5
[0125] L-diethyl tartrate. 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains at the 10%L-diethyl tartrate. that can not wash in the ointment.
The above 10%L-diethyl tartrate. of local application ointment on the lip of the male subject at an age 73.After 1-2 minute, lip has experienced lasting about 10-about 20 minutes slight sensation and sense of fullness.Effect to nervus labialis shows that the dihydroxy dicarboxylic ester can provide useful effect like this, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0126] embodiment 6
[0127] triethyl citrate 10g and propylene glycol 10ml are mixed with hydrophilic ointment or oil in water emulsion 80g.Therefore the compositions of preparation contains 10% triethyl citrate in water-soluble oil in water emulsion.
[0128] 10% triethyl citrate cream more than the local application on the lip of the male subject at an age 73.After 1-2 minute, lip has experienced lasting about 20-about 30 minutes sensation and sense of fullness.Effect to nervus labialis shows that the monohydroxy tricarboxylic ester can provide useful effect like this, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0129] embodiment 7
[0130] triethyl citrate 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% triethyl citrate can not washing in the ointment.
[0131] 7 volunteer, 4 male and 3 women, 10% triethyl citrate cream more than the local application on its lip.After 1-2 minute, lip has experienced lasting about 20-about 30 minutes sensation and sense of fullness.Like this effect of nervus labialis is shown, in the preparation different with embodiment 6 and the monohydroxy tricarboxylic ester that uses by several experimenters useful effect can be provided, it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0132] embodiment 8
[0133] triethyl citrate 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% triethyl citrate can not washing in the ointment.
[0134], suffers from allergic eczema and follow above 10% triethyl citrate of local application on male patient's the right rear leg pruritus skin of serious skin pruritus an age 73.After a few minutes, pruritus stops and keeping not having pruritus at 4 hours subsequently skin.This result shows that the monohydroxy tricarboxylic ester can provide useful antipruritic effect, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0135] embodiment 9
[0136] triethyl citrate 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% triethyl citrate can not washing in the ointment.
[0137] 10% trimethyl citrate ointment more than the local application on the lip of the male subject at an age 73.After 1-2 minute, lip has experienced very slight sensation and sense of fullness.Effect to nervus labialis shows that another kind of monohydroxy tricarboxylic ester can provide useful effect like this, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0138] embodiment 10
[0139] makes lignocaine 5g be dissolved among the warm propylene glycol 20ml and make so the solution that obtains mixes with the ointment of 50 parts of 75g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 5% lignocaine can not washing in the ointment.
[0140] 5% lidocaine ointment agent more than the local application on the lip of the male subject at an age 73.A few minutes the posterior lip stolidity and insensible numb effect continue several hours.Such numbness or anesthetic action are different from sensation and the consciousness effect that is produced by hydroxyl-polycarboxylate fully.
[0141] embodiment 11
[0142] citric acid three propyl ester 10g are mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% citric acid, three propyl ester can not washing in the ointment.
[0143] 10% citric acid, three propyl ester ointments more than the local application on the lip of the male subject at an age 73.A few minutes posterior lip experienced lasting about 1.5-about 2 hours sensation and consciousness.Effect to nervus labialis shows that another kind of monohydroxy tricarboxylic ester can provide useful effect like this, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0144] embodiment 12
[0145] citric acid three propyl ester 10g and propylene glycol 20ml are mixed with hydrophilic ointment or oil in water emulsion 70g.Therefore the compositions of preparation contains 10% citric acid, three propyl ester in water-soluble oil in water emulsion.
[0146], suffers from allergic eczema and follow on male patient's the right lower limb of following pruritus eczema damage of serious skin pruritus above 10% citric acid, three propyl ester of local application an age 73.After a few minutes, the pruritus complete obiteration also keeps not having pruritus at 4 hours subsequently skin.The different monohydroxy tricarboxylic ester that this result is presented in the different preparations can provide useful antipruritic effect, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0147] embodiment 13
[0148] citric acid three isopropyl ester 10g are mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% citric acid, three isopropyl esters can not washing in the ointment.
[0149] 10% citric acid, three isopropyl ester ointments more than the local application on the lip of the male subject at an age 74.A few minutes posterior lip experienced and continued about 1 hour sensation and consciousness.This result shows that different monohydroxy tricarboxylic esters can provide useful effect, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0150] embodiment 14
[0151] tribenzyl citrate 10g is mixed with the ointment of 50 parts of 90g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% tribenzyl citrate can not washing in the ointment.
[0152] 10% tribenzyl citrate ointment more than the local application on the lip of the male subject at an age 74.A few minutes posterior lip experienced slight sensation and consciousness.That this result shows is different, aromatics monohydroxy tricarboxylic ester can provide useful effect, and it is the representative to various beauty treatment section's diseases and other beneficial effects of dermatosis indication.
[0153] embodiment 15
[0154] a kind of typical associating compositions of following preparation.
Hydrocortisone-17-valerate 0.2g is dissolved among liquid triethyl citrate 15g and the propylene glycol 10ml.The solution that makes so obtain mixes with the ointment of 50 parts of 74.8g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 15% triethyl citrate and 0.2% hydrocortisone-17-valerate can not washing in the ointment.
[0155] the above ointment of local application on the male patient's at an age 74 pruritus and eczema skin.Pruritus disappears after a few minutes, and compositions has antiinflammatory action in addition.The result shows that said composition is useful to topical therapeutic pruritus, eczema and other inflammatory dermatosiss.
[0156] embodiment 16
[0157] the another kind of typical associating compositions of following preparation.
Make menthol 1g be dissolved in liquid citric acid three isopropyl ester 10g and and propylene glycol 10ml in.The solution that makes so obtain mixes with the ointment of 50 parts of 79g confession mineral tallows, 40 parts in mineral oil and 10 parts of preparations of cera alba.Therefore the compositions of preparation contains 10% citric acid, three isopropyl esters and 1% menthol can not washing in the ointment.
[0158] the above ointment of local application on the male patient's at an age 74 pruritus and eczema skin.Pruritus weakens after a few minutes, and compositions has the effect of alleviating to eczema damage.The result shows that said composition is useful to topical therapeutic pruritus, eczema and other inflammatory dermatosiss.
[0159] embodiment 17
[0160] the another kind of typical associating compositions of following preparation.
Make among the water-soluble 100ml of diphhydramine hydrochloride 58g (0.2 mole) and follow to stir and slowly add 5N NaOH 40ml (0.2 mole) down.Formation is as the diphenhydramine free alkali of oily white precipitate.Do not have separated free alkali, the limit is stirred and add N-acetyl group-L-proline-4 8g (0.3 mole) and N-acetyl group-D-glycosamine 44g (0.2 mole) down in oily mixture, and mixture becomes clear and bright solution.Add propylene glycol 100ml and water 50ml so that cumulative volume is 400ml (444g).Said preparation contains diphenhydramine 14.5%, N-acetyl group-L-proline 12% and the N-acetyl group-D-glycosamine 11% in propylene glycol/water solution.Above preparation 22g and tribenzyl citrate 10g are mixed with hydrophilic ointment or oil-in-water cream 68g.Therefore the compositions of preparation has pH 3.8 and contains at 10% tribenzyl citrate, 3% diphenhydramine, 2.6%N-acetyl group-L-proline and the 2.4%N-acetyl group-D-glycosamine that can wash in the cream.
[0161] the above compositions of local application on the male patient's at an age 74 pruritus and eczema skin.Pruritus disappears after a few minutes.The result shows that said composition is useful to topical therapeutic pruritus, eczema and other inflammatory dermatosiss.
[0162] it will be appreciated by those skilled in the art that to make and change and do not deviate from the inventive concept of its wide region embodiment described above.Therefore, should be appreciated that to the invention is not restricted to disclosed specific embodiments, and plan comprises as the change in the spirit and scope of the invention of accessory claim book definition.
Claims (26)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US72741905P | 2005-10-17 | 2005-10-17 | |
| US60/727,419 | 2005-10-17 | ||
| US60/759,525 | 2006-01-17 | ||
| US11/548,945 | 2006-10-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101330911A true CN101330911A (en) | 2008-12-24 |
Family
ID=40206354
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2006800476420A Pending CN101330911A (en) | 2005-10-17 | 2006-10-13 | Hydroxy-polycarboxylic acid esters: action on nerves and use on skin and mucocutaneous organs or sites |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101330911A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115919683A (en) * | 2023-01-05 | 2023-04-07 | 上海其然生物科技有限公司 | A kind of transparent composition and its preparation method and application |
-
2006
- 2006-10-13 CN CNA2006800476420A patent/CN101330911A/en active Pending
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115919683A (en) * | 2023-01-05 | 2023-04-07 | 上海其然生物科技有限公司 | A kind of transparent composition and its preparation method and application |
| CN115919683B (en) * | 2023-01-05 | 2024-11-12 | 上海其然生物科技有限公司 | A transparent composition and its preparation method and application |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US6824786B2 (en) | Compositions comprising phenyl-glycine derivatives | |
| AU2002317053B2 (en) | Dermal therapy using phosphate derivatives of electron transfer agents | |
| CN101166510B (en) | External preparation for skin | |
| JP2003503436A (en) | Oligosaccharide aldonic acids and their topical use | |
| US20100068161A1 (en) | Topical composition for the protection and/or treatment of radiation related skin damages | |
| TWI682782B (en) | Methods and compositions for topical delivery for skin care | |
| JPH08208488A (en) | Skin preparation for external use | |
| JP2012072172A (en) | Topical therapy composition comprising n-acetyl aldosamine or n-acetylamino acid | |
| WO2005095959A2 (en) | Methods for treating dermatological conditions in a patient | |
| JP2009511630A (en) | Hydroxy oligocarboxylic acid ester: Action on nerves and application to organs or sites of skin and mucocutaneous skin | |
| US20040147452A1 (en) | Non-amphoteric glutathione derivative compositions for tropical application | |
| US11090205B2 (en) | Methods and compositions for treatment of skin conditions | |
| JP2004508317A (en) | Cosmetic composition and method | |
| JPH04500824A (en) | Skin treatment methods to reverse the effects of photoaging | |
| CN101330911A (en) | Hydroxy-polycarboxylic acid esters: action on nerves and use on skin and mucocutaneous organs or sites | |
| JPH08104635A (en) | External pharmaceutical preparation containing zinc phytate as active ingredient | |
| FR2823671A1 (en) | Dermatological compositions, useful for treating acne or atopic dermatitis, comprise synergistic combination of nicotinic acid or its amide and sphingoid base | |
| EP1916993B1 (en) | Cosmetic composition containing a protease activator | |
| CN111372595A (en) | Methods and compositions for treating skin | |
| US12440508B2 (en) | Methods and compositions for therapeutic skin treatments in dermatological procedures affecting skin's barrier | |
| US20220110967A1 (en) | Methods and compositions for therapeutic skin treatments in dermatological procedures affecting skin's barrier | |
| WO2006119540A1 (en) | Preparation for treating psoriasis | |
| AU2006246350A1 (en) | Preparation for treating psoriasis | |
| HK1109873B (en) | External preparation for skin |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20081224 |