CN107432870A - A kind of aspartic acid capsule and preparation method thereof - Google Patents
A kind of aspartic acid capsule and preparation method thereof Download PDFInfo
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- CN107432870A CN107432870A CN201610350582.5A CN201610350582A CN107432870A CN 107432870 A CN107432870 A CN 107432870A CN 201610350582 A CN201610350582 A CN 201610350582A CN 107432870 A CN107432870 A CN 107432870A
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- Prior art keywords
- capsule
- aspartic acid
- particle
- auxiliary material
- acid
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- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 title claims abstract description 45
- 235000003704 aspartic acid Nutrition 0.000 title claims abstract description 45
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 title claims abstract description 45
- 239000002775 capsule Substances 0.000 title claims abstract description 29
- 238000002360 preparation method Methods 0.000 title claims abstract description 14
- 239000000463 material Substances 0.000 claims abstract description 35
- 239000002245 particle Substances 0.000 claims description 18
- 235000021355 Stearic acid Nutrition 0.000 claims description 12
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 12
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims description 12
- 239000008117 stearic acid Substances 0.000 claims description 12
- 239000002994 raw material Substances 0.000 claims description 10
- 239000000853 adhesive Substances 0.000 claims description 9
- 230000001070 adhesive effect Effects 0.000 claims description 9
- 125000004079 stearyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 239000000945 filler Substances 0.000 claims description 3
- 239000001993 wax Substances 0.000 claims description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 2
- 241000238631 Hexapoda Species 0.000 claims description 2
- 229920002472 Starch Polymers 0.000 claims description 2
- 235000013871 bee wax Nutrition 0.000 claims description 2
- 239000012166 beeswax Substances 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- 238000007873 sieving Methods 0.000 claims description 2
- 239000008107 starch Substances 0.000 claims description 2
- 235000019698 starch Nutrition 0.000 claims description 2
- 239000004615 ingredient Substances 0.000 claims 5
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 3
- 238000004659 sterilization and disinfection Methods 0.000 claims 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 238000001125 extrusion Methods 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 238000004806 packaging method and process Methods 0.000 claims 1
- 210000000952 spleen Anatomy 0.000 claims 1
- 230000001954 sterilising effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 3
- 230000000857 drug effect Effects 0.000 abstract 2
- 238000007905 drug manufacturing Methods 0.000 abstract 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 description 8
- 229910052700 potassium Inorganic materials 0.000 description 8
- 239000011591 potassium Substances 0.000 description 8
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 7
- 238000010521 absorption reaction Methods 0.000 description 7
- 239000003826 tablet Substances 0.000 description 7
- 239000000047 product Substances 0.000 description 5
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- 210000004027 cell Anatomy 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 239000008363 phosphate buffer Substances 0.000 description 4
- 239000000243 solution Substances 0.000 description 4
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 4
- 238000004090 dissolution Methods 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- 208000019025 Hypokalemia Diseases 0.000 description 2
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 2
- 206010029164 Nephrotic syndrome Diseases 0.000 description 2
- NPYPAHLBTDXSSS-UHFFFAOYSA-N Potassium ion Chemical compound [K+] NPYPAHLBTDXSSS-UHFFFAOYSA-N 0.000 description 2
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 2
- 229910021529 ammonia Inorganic materials 0.000 description 2
- 239000001569 carbon dioxide Substances 0.000 description 2
- 229910002092 carbon dioxide Inorganic materials 0.000 description 2
- 230000019522 cellular metabolic process Effects 0.000 description 2
- FPAFDBFIGPHWGO-UHFFFAOYSA-N dioxosilane;oxomagnesium;hydrate Chemical compound O.[Mg]=O.[Mg]=O.[Mg]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O.O=[Si]=O FPAFDBFIGPHWGO-UHFFFAOYSA-N 0.000 description 2
- 235000019441 ethanol Nutrition 0.000 description 2
- 210000003722 extracellular fluid Anatomy 0.000 description 2
- 238000010438 heat treatment Methods 0.000 description 2
- 210000002977 intracellular fluid Anatomy 0.000 description 2
- 239000000314 lubricant Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 239000008108 microcrystalline cellulose Substances 0.000 description 2
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 2
- 229940016286 microcrystalline cellulose Drugs 0.000 description 2
- 230000002107 myocardial effect Effects 0.000 description 2
- 208000009928 nephrosis Diseases 0.000 description 2
- 231100001027 nephrosis Toxicity 0.000 description 2
- 238000005453 pelletization Methods 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 229910001414 potassium ion Inorganic materials 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- 235000020985 whole grains Nutrition 0.000 description 2
- 206010001497 Agitation Diseases 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- 239000004375 Dextrin Substances 0.000 description 1
- 229920001353 Dextrin Polymers 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 206010028372 Muscular weakness Diseases 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 239000004677 Nylon Substances 0.000 description 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 description 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 208000004756 Respiratory Insufficiency Diseases 0.000 description 1
- 206010039020 Rhabdomyolysis Diseases 0.000 description 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 230000001594 aberrant effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 230000006793 arrhythmia Effects 0.000 description 1
- 206010003119 arrhythmia Diseases 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 150000001768 cations Chemical class 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 235000019425 dextrin Nutrition 0.000 description 1
- 208000021264 digitalis poisoning Diseases 0.000 description 1
- 239000012738 dissolution medium Substances 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 229940030606 diuretics Drugs 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 208000003243 intestinal obstruction Diseases 0.000 description 1
- 230000003834 intracellular effect Effects 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 238000012423 maintenance Methods 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 230000028161 membrane depolarization Effects 0.000 description 1
- FJQXCDYVZAHXNS-UHFFFAOYSA-N methadone hydrochloride Chemical compound Cl.C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 FJQXCDYVZAHXNS-UHFFFAOYSA-N 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000004118 muscle contraction Effects 0.000 description 1
- 230000036473 myasthenia Effects 0.000 description 1
- 208000018360 neuromuscular disease Diseases 0.000 description 1
- 229920001778 nylon Polymers 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 229960003104 ornithine Drugs 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- KHPXUQMNIQBQEV-UHFFFAOYSA-N oxaloacetic acid Chemical compound OC(=O)CC(=O)C(O)=O KHPXUQMNIQBQEV-UHFFFAOYSA-N 0.000 description 1
- 239000003182 parenteral nutrition solution Substances 0.000 description 1
- 229940127557 pharmaceutical product Drugs 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 239000002243 precursor Substances 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 201000004193 respiratory failure Diseases 0.000 description 1
- 230000000284 resting effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000012047 saturated solution Substances 0.000 description 1
- 208000026775 severe diarrhea Diseases 0.000 description 1
- 239000000741 silica gel Substances 0.000 description 1
- 229910002027 silica gel Inorganic materials 0.000 description 1
- 210000002784 stomach Anatomy 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000013589 supplement Substances 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 230000018405 transmission of nerve impulse Effects 0.000 description 1
- 230000004102 tricarboxylic acid cycle Effects 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention relates to a kind of aspartic acid capsule preparations, the preparation by weight, is prepared by the supplementary material of following components：Aspartic acid:Auxiliary material=5:（2~3）.Feature of the present invention is that drug production process is simplified, easy to operate, the capsule filling micropill of preparation, and drug effect release is fast, and stability is good, and the medicine drug effect produced is high.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, and in particular to a kind of aspartic acid capsule preparations and preparation method thereof.
Background technology
Potassium is intracellular dominant cation, required for cells survival, has a variety of physiological actions.98% potassium is present in into the cell, and extracellular fluid only contains 2%.Potassium in extracellular fluid mainly exists with ionic condition, and potassium divided by ionic condition are present outer in intracellular fluid, and a part is combined with protein, and another part is combined with sugar and phosphate.Potassium all plays an important role in cell metabolism, the maintenance for maintaining intracellular fluid osmotic pressure, holding intraor extracellular acid-base balance, the transmission of nerve impulse, contraction of muscle, myocardial excitability, self-disciplining and conductibility and normal organ function etc..
Precursor of the L-aminobutanedioic acid as internal oxaloacetic acid, plays an important role in tricarboxylic acid cycle, and participates in ornithine circulation, ammonia and carbon dioxide is combined generation urea, reduces the content of ammonia and carbon dioxide in blood.L-aminobutanedioic acid is strong with cellular affinity, potassium ion can be made to return into the cell, promote cell depolarization and cell metabolism, maintain its normal function as the carrier of potassium ion.Clinically many reasons can cause hypopotassaemia, such as hypoalimentation, vomiting, severe diarrhea, using row's potassium diuretics, lose caused hypopotassaemia reason after potassium nephrosis and prolonged application glucocorticoid and supplement hypertonic glucose.Low potassium can influence the resting potential of myocardial cell membrane, inspire aberrant conduction and reentry phenomenon, form severe arrhythmia, increase the incidence of digitalis poisoning；The neuro-muscular disorders such as myasthenia, paralysis, respiratory insufficiency can be caused simultaneously, can also result in rhabdomyolysis, electrocardiographic abnormality and intestinal obstruction.Long-term Diagnostic value causes renal damage (Diagnostic value nephrosis).
Aspartic acid is the kind that Italian pharmacopeia is recorded, and is also recorded in the 32nd edition big pharmacopeia of Martindale（The32th
Edition Martindial Pharmacopeia）With《Japanese pharmaceutical product collection》.Japan has more pharmacy corporations to produce this product, and Tian Bian drugmakers produce the tablet, powder and parenteral solution of this product, and republicanism medicine company, colleague's medicine produce tablet of this product etc..
Aspartic acid piece regular size is 10mg, and drugloading rate is larger, and aspartic acid raw material draws moist, easy change capsule shells water content with very strong.
The content of the invention
Situation of the invention based on the easy moisture absorption in aspartic acid pelletization, studies by repetition test, finally draws a kind of aspartic acid capsule and preparation method thereof.In its preparation process, the hygroscopicity of material substantially reduces the aspartic acid capsule of the present invention, the stability increase of finished product, reduces aspartic acid capsule and prepares difficulty and production cost.
The aspartic acid capsule of the present invention, including particle and capsulae vacuus, the particle contain aspartic acid and pharmaceutically acceptable auxiliary material, and the pharmaceutically acceptable auxiliary material includes waxy auxiliary material.By adding waxy auxiliary material, it can be obviously improved in pelletization, the problem of the material moisture absorption.In addition, particle also includes other appropriate auxiliary materials.Wherein, the waxy auxiliary material is the one or more in tristerin, glycerin monostearate, stearic acid, insect wax, beeswax, octadecyl alcolol.
Other described auxiliary materials include the auxiliary materials such as filler, adhesive, glidant, and specifically, filler may be selected from the one or more of sucrose, mannitol, starch, microcrystalline cellulose, lactose, dextrin etc.；Adhesive may be selected from PVP, hydroxypropyl methyl cellulose, absolute ethyl alcohol, various concentration second alcohol-water solution etc. one or more；Glidant may be selected from the one or more of talcum powder, differential silica gel etc..
Specifically, particle includes following component, and its content is to account for the percentages of weight：
Aspartic acid 30~90%；
Waxy auxiliary material 0.5~20%；
Other auxiliary material surpluses.
Preferably, the content of each part of particle is（To account for the percentages of every weight）：Aspartic acid 50~70%；Waxy auxiliary material 5~10%；Other auxiliary material surpluses.In addition, the aspartic acid capsule of the present invention, in addition to capsulae vacuus, the weight of the capsulae vacuus are the 1.0~5.0% of particle weight.
The present invention also provides a kind of preparation method of the aspartic acid piece, comprises the following steps：
（1）Prepare described L-aminobutanedioic acid capsule granulation；
（2）Prepare the capsulae vacuus of described L-aminobutanedioic acid capsule
（3）It is filled.
Wherein, step（1）It is middle to use wet granulation.Concretely comprise the following steps：Auxiliary material is weighed, adds ethanol in proper amount, is dissolved by heating, as adhesive；Weigh the auxiliary materials such as aspartic acid and adhesive to be well mixed, add solution obtained above, stir, sieving granulation, dry, whole grain, classification.
Waxy auxiliary material of the present invention, is not only able to reduce the hygroscopicity of material, while also has the effect of lubricant and adhesive concurrently.
It is an advantage of the invention that：Compared with prior art, aspartic acid capsule of the invention can significantly reduce the hygroscopicity of material so as to increase the stability of finished product, not receive the influence of the factors such as mechanical pressure during preparation, compared with being more beneficial for disperseing rapidly in the gastrointestinal tract for tablet, dissolution and absorption.Reduce aspartic acid capsule and prepare difficulty and production cost.
Brief description of the drawings
Fig. 1：The sucting wet curve of aspartic acid（25℃）
Fig. 2：Aspartic acid self-control capsule of the present invention and reference tablet stripping curve figure in water
Fig. 3：Aspartic acid self-control capsule of the present invention and reference tablet stripping curve figure in pH1.2 hydrochloric acid solutions
Fig. 4：Aspartic acid self-control capsule of the present invention and reference tablet stripping curve figure in pH4.0 phosphate buffers
Fig. 5：Aspartic acid self-control capsule of the present invention and reference tablet stripping curve figure in pH6.8 phosphate buffers
Embodiment
The present invention is further illustrated below by specific embodiment, following embodiments are to be used to illustrate rather than limitation of the present invention, and the scope of protection of present invention is belonged to according to the simple modifications that the essence of the present invention is carried out to the present invention.
Embodiment 1
Preparation method：
（1）The configuration of adhesive：Stearic acid 30g is weighed, adds 210g ethanol（95%）In, heating dissolves stearic acid, as adhesive；
（2）Granulation：Weigh aspartic acid, microcrystalline cellulose is well mixed, add adhesive, stir, with 18 mesh nylon screens pelletize；The drying 4 hours of 60 DEG C of heated-air circulation oven；16 mesh whole grains, add talcum powder and be well mixed；
In the present embodiment：
（1）Stearic acid dosage in particle prescription is 6%, and stearic acid is hydrophobic material, after being mixed with aspartic acid, reduces aspartic acid surface area, reduces the hygroscopicity of mixed material.
（2）Stearic acid is wax material, has the function that lubricant.
Stearic acid can reduce the hygroscopicity of material in this prescription.
Embodiment 2
According to the method described in embodiment 1, aspartic acid piece is prepared using following compositions.As a result on the basis of plain piece, stomach dissolved type moisture-proofing coating weight gain about 3%.
Experimental example 1
The measure of material sucting wet curve
1. test specimen
Aspartic acid raw material（It crushed 100 mesh sieves）；Stearic acid（It crushed 100 mesh sieves）；Octadecyl alcolol（It crushed 100 mesh sieves）
2. experimental method
（1）The saturated solution of different salt is respectively configured, puts in drier, makes to reach certain humidity in closed environment.
（2）Aspartic acid raw material about 3.0g is weighed, is put in measuring cup, tiling makes thickness be less than 5mm, puts in each drier, places 10 days, and taking-up is weighed, and calculates moisture absorption weightening.
（3）Aspartic acid and stearic acid are pressed 9 with method：After 1 ratio ground and mixed is uniform, about 3.0g is weighed, puts title
In measuring bottle, tiling makes thickness be less than 5mm, puts in each drier, places 10 days, and taking-up is weighed, and calculates and inhales
Wet weightening.
（4）Aspartic acid and octadecyl alcolol are pressed 9 with method：After 1 ratio ground and mixed is uniform, about 3.0g is weighed, puts title
In measuring bottle, tiling makes thickness be less than 5mm, puts in each drier, places 10 days, and taking-up is weighed, and calculates moisture absorption weightening.
3. result of the test
Experimental result is shown in Table 1, Fig. 1.
The moisture absorption of table 1 weightening experimental result
According to experimental result, aspartic acid raw material critical relative moisture is about 59%, moisture absorption substantially reduces after mixing stearic acid and octadecyl alcolol, and critical relative moisture is increased to 65%, 63%, and stearic acid or octadecyl alcolol are obviously improved the hygroscopicity of aspartic acid raw material with aspartic acid raw material hybrid energy.
Experimental example 2
The determination experiment of dissolution rate
1. sample
Aspartic acid capsule of the present invention, is prepared according to the embodiment of the present invention 1.
2. experimental method
With Chinese Pharmacopoeia four general rule measure aspartic acid piece dissolution rates of version in 2015.Respectively with water, pH1.2 hydrochloric acid solutions, pH4.0 phosphate buffers, pH6.8 phosphate buffers（Configured by Japanese official method）900ml is dissolution medium, as a result as shown in Fig. 2~5.
3. experimental result
It can be seen from Fig. 2~5, aspartic acid capsule of the present invention is good compared with reference stripping curve result of extraction.
Claims (8)
1. a kind of aspartic acid capsule, including particle and capsulae vacuus, the particle contain aspartic acid and pharmaceutically acceptable auxiliary material, it is characterised in that the pharmaceutically acceptable auxiliary material.
2. the L-aminobutanedioic acid k particle according to claim 1, it is characterised in that contain aspartic acid 50~70%, auxiliary material 5~10% in the particle.
3. the L-aminobutanedioic acid k particle according to claim 1, it is characterised in that described auxiliary material is the one or more in tristerin, glycerin monostearate, stearic acid, insect wax, beeswax, octadecyl alcolol.
4. the L-aminobutanedioic acid k particle according to claim 1, it is characterised in that particle is also containing other appropriate auxiliary materials.
5. the L-aminobutanedioic acid particle according to claim 4, it is characterised in that other described auxiliary materials include diluent, adhesive, glidant etc..
6. the aspartic acid capsule according to claim 1, its capsulae vacuus is made by bone, severe edema due to hypofunction of the spleen solution.
7. the L-aminobutanedioic acid k particle according to claim 1, it is characterised in that the weight of the capsulae vacuus is the 1.0~5.0% of particle weight.
8. according to the preparation method of any described aspartic acid capsule of claim 1~7, comprise the following steps：
（1）Supplementary material is weighed
By raw material according to technological requirement, weigh standby；
（2）Raw material primary dcreening operation
By major ingredient L-aminobutanedioic acid, potassium hydroxide, and supplementary product starch, hydroxypropylcellulose carry out primary dcreening operation, and sieve mesh is 300-350 mesh；
（3）Crush
It is by the major ingredient and auxiliary material of sieving, particle diameter degree is big, do not crushed by the raw material of scalping, the rotating speed of pulverizer is 4000-6000r/min, a length of 2-3min during crushing；
（4）Fine screen
Major ingredient after crushing and auxiliary material are subjected to fine screen, the sieve mesh of fine screen is 400-450 mesh；
（5）Dispensing
Major ingredient is mixed, is incorporated auxiliary material after well mixed, then major ingredient is well mixed with auxiliary material；
（6）It is prepared by filler
The raw material mixed will be mixed, using extrusion-round as a ball micropill for being prepared into capsule filling, the condition of preparation is 25-30 DEG C of temperature, temperature is 45-55%, and rate of extrusion is 500-600 grains/min, and round as a ball rotating speed is 1200-1500r/min, the round as a ball time is 60-90s, and drying temperature is 50-60 DEG C；
（7）Fill capsule
The micropill prepared is fitted into capsule, capsule is bonded；
（8）Sterilization
Capsule after bonding is carried out disinfection；
（9）Packaging
Finished product is packed.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201610350582.5A CN107432870A (en) | 2016-05-25 | 2016-05-25 | A kind of aspartic acid capsule and preparation method thereof |
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| CN201610350582.5A CN107432870A (en) | 2016-05-25 | 2016-05-25 | A kind of aspartic acid capsule and preparation method thereof |
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Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1439629A (en) * | 2003-03-21 | 2003-09-03 | 于航 | Laevo potassium aspartate material and preparation therefrom and preparing method thereof |
| US20090130075A1 (en) * | 2003-04-08 | 2009-05-21 | Janeel Henderson | Energy generating composition |
| CN103181917A (en) * | 2011-12-30 | 2013-07-03 | 北京京卫信康医药科技发展有限公司 | Potassium aspartate pharmaceutical composition and preparation method thereof |
| CN104069082A (en) * | 2013-03-25 | 2014-10-01 | 辽宁药联制药有限公司 | Potassium aspartate tablet and preparation method thereof |
-
2016
- 2016-05-25 CN CN201610350582.5A patent/CN107432870A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1439629A (en) * | 2003-03-21 | 2003-09-03 | 于航 | Laevo potassium aspartate material and preparation therefrom and preparing method thereof |
| US20090130075A1 (en) * | 2003-04-08 | 2009-05-21 | Janeel Henderson | Energy generating composition |
| CN103181917A (en) * | 2011-12-30 | 2013-07-03 | 北京京卫信康医药科技发展有限公司 | Potassium aspartate pharmaceutical composition and preparation method thereof |
| CN104069082A (en) * | 2013-03-25 | 2014-10-01 | 辽宁药联制药有限公司 | Potassium aspartate tablet and preparation method thereof |
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Application publication date: 20171205 |