CN1511524A - Indapamide slow-releasing capsule and its preparing process - Google Patents
Indapamide slow-releasing capsule and its preparing process Download PDFInfo
- Publication number
- CN1511524A CN1511524A CNA021592934A CN02159293A CN1511524A CN 1511524 A CN1511524 A CN 1511524A CN A021592934 A CNA021592934 A CN A021592934A CN 02159293 A CN02159293 A CN 02159293A CN 1511524 A CN1511524 A CN 1511524A
- Authority
- CN
- China
- Prior art keywords
- indapamide
- piller
- sucrose
- eudragit
- recipe quantity
- 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
- NDDAHWYSQHTHNT-UHFFFAOYSA-N indapamide Chemical compound CC1CC2=CC=CC=C2N1NC(=O)C1=CC=C(Cl)C(S(N)(=O)=O)=C1 NDDAHWYSQHTHNT-UHFFFAOYSA-N 0.000 title claims abstract description 29
- 229960004569 indapamide Drugs 0.000 title claims abstract description 29
- 239000002775 capsule Substances 0.000 title claims abstract description 13
- 238000000034 method Methods 0.000 title description 4
- 229930006000 Sucrose Natural products 0.000 claims abstract description 26
- 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 claims abstract description 26
- 238000002360 preparation method Methods 0.000 claims abstract description 13
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 claims abstract description 10
- 239000006187 pill Substances 0.000 claims abstract description 10
- 239000001069 triethyl citrate Substances 0.000 claims abstract description 10
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims abstract description 10
- 235000013769 triethyl citrate Nutrition 0.000 claims abstract description 10
- 238000005303 weighing Methods 0.000 claims abstract description 10
- 239000003814 drug Substances 0.000 claims abstract description 8
- 239000000463 material Substances 0.000 claims abstract description 8
- 229920003155 Eudragit® RL 100 Polymers 0.000 claims abstract description 6
- 229920003159 Eudragit® RS 100 Polymers 0.000 claims abstract description 6
- 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 claims abstract description 6
- 238000002156 mixing Methods 0.000 claims abstract description 4
- 239000005720 sucrose Substances 0.000 claims description 22
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 14
- 239000011248 coating agent Substances 0.000 claims description 14
- 238000000576 coating method Methods 0.000 claims description 14
- 239000000725 suspension Substances 0.000 claims description 10
- 229920003134 Eudragit® polymer Polymers 0.000 claims description 8
- VVQNEPGJFQJSBK-UHFFFAOYSA-N Methyl methacrylate Chemical compound COC(=O)C(C)=C VVQNEPGJFQJSBK-UHFFFAOYSA-N 0.000 claims description 8
- 235000010603 pastilles Nutrition 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- 229940079593 drug Drugs 0.000 claims description 5
- 239000006188 syrup Substances 0.000 claims description 4
- 235000020357 syrup Nutrition 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 3
- 238000007873 sieving Methods 0.000 claims description 2
- 206010020772 Hypertension Diseases 0.000 abstract description 5
- 229960004793 sucrose Drugs 0.000 abstract 4
- 238000005507 spraying Methods 0.000 abstract 2
- 206010013786 Dry skin Diseases 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 238000001035 drying Methods 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 208000004880 Polyuria Diseases 0.000 description 3
- 230000035619 diuresis Effects 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 2
- 230000003276 anti-hypertensive effect Effects 0.000 description 2
- BHPQYMZQTOCNFJ-UHFFFAOYSA-N Calcium cation Chemical compound [Ca+2] BHPQYMZQTOCNFJ-UHFFFAOYSA-N 0.000 description 1
- 208000007530 Essential hypertension Diseases 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 210000004204 blood vessel Anatomy 0.000 description 1
- 229910001424 calcium ion Inorganic materials 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 230000000916 dilatatory effect Effects 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000003203 everyday effect Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001764 infiltration Methods 0.000 description 1
- 230000008595 infiltration Effects 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000008024 pharmaceutical diluent Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 210000002460 smooth muscle Anatomy 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 238000011287 therapeutic dose Methods 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
Images
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
The present invention relates to medicine for treating hypertension, and is especially slow-releasing Indapamide capsule and its preparation process. Indapamide capsule is prepared with Indapamide 0.3-1 wt%, cane sugar pill 75-95 wt%, Eudragit RS-100 0.5-10 wt%, Eudragit RL-100 0.5-10 wt%, triethyl citrate 0.1-1wt%, talcum powder 1-8wt% and cane sugar 1-10 wt%. The preparation process includes weighing the materials, spraying Indapamide and slow releasing material to cane sugar pill to form slow releasing pill and capsulizing. Or, the preparation process includes weighing the materials, spraying Indapamide and slow releasing material to cane sugar pill to form slow releasing pill A and B of different releasing rates, mixing and capsulizing.
Description
Technical field the present invention relates to a kind of antihypertensive, specifically is indapamide slow release capsule and preparation technology thereof.
The background technology indapamide is a calcium ion antagonist, have blood vessel dilating smooth muscle and diuresis, being mainly used in the treatment of essential hypertension, has been a line medicine of hypertension treatment by U.S. hypertension whole nation joint committee, Britain hypertension association and world health organisation recommendations.Animal experiment shows: indapamide has antihypertensive function and diuresis to the experimental hypertension animal, and this effect is relevant with dosage, shows hypotensive effect when low dosage, and high dose shows diuresis.This product toxic and side effects is lower in the therapeutic dose scope, and the human oral post-absorption rapidly and fully, peak reaching time of blood concentration is 0.5 hour, and eliminating the half-life is 17.8 hours.Although indapamide only need be taken once every day, because the oral post-absorption of ordinary preparation is rapid, promptly reach peak concentration in the short time, cause patient's blood pressure lowering too fast and be difficult to bear.Therefore having only could head it off by slow controlled-release technology.
Summary of the invention purpose of the present invention just provides a kind of indapamide slow release capsule and preparation technology thereof, delay the infiltration rate of indapamide, blood drug level is controlled in the effective blood drug concentration scope, thereby the side effect that prevention causes more greatly because of blood concentration fluctuation improve patient's compliance.
Technical scheme of the present invention is that the indapamide slow release capsule is prepared from (by weight percentage) by following material:
Indapamide 0.3～1%
Sucrose piller (15～30 order) 75～95%
Eudragit?RS?100 0.5～10％
Eudragit?RL?100 0.5～10％
Triethyl citrate 0.1～1%
Pulvis Talci 1～8%
Sucrose 1～10%
According to technique scheme, indapamide is a white powder, and molecular weight is 365.83, and molecular formula is C
16H
16ClN
3O
3S.Be dissolved in ethanol, ethyl acetate, water insoluble.The sucrose piller is pharmaceutical carrier and diluent.Eudragit RS 100 and Eudragit RL 100 are slow-release material, they are insoluble in water, but the energy swelling forms the duct in coating, the medicine of coating inboard discharges by these ducts, just can adjust rate of releasing drug by proportioning and the covering amount of regulating these two kinds of materials.Sucrose is binding agent, and Pulvis Talci is an antiplastering aid, and triethyl citrate is a plasticizer, prevents that slow-release pill from film rupture taking place in put procedure.
The capsular preparation technology of indapamide slow release provided by the invention is:
(1) sucrose that takes by weighing recipe quantity water gaging such as adds and makes 50% syrup, adds an amount of ethanol and recipe quantity indapamide again to make suspension, and is stand-by; Other takes by weighing recipe quantity sucrose piller and places the high-efficiency coating pot, by the coating operation above-mentioned suspension evenly is sprayed on the sucrose piller, dry back the pastille piller, the back of sieving is stand-by; Take by weighing Eudragit RS 100, Eudragit RL 100, the triethyl citrate of recipe quantity, add an amount of ethanol and make suspension, evenly be sprayed on the pastille piller by the coating operation then, dry back slow-release pill, survey content, pack capsulae vacuus into promptly.(2) take by weighing each composition of part recipe quantity,, by the proper proportion mixing, pack capsulae vacuus into promptly then by A, the B piller that (1) described preparation technology makes different rate of releasing drug.
Description of drawings Fig. 1 is that indapamide slow release capsule and ordinary tablet release profiles compare.
The present invention is further described below by embodiment for the specific embodiment.
Example 1
Indapamide 1.5g
Sucrose piller (15～30 order) 250g
Eudragit?RS?100 15g
Eudragit?RL?100 2g
Triethyl citrate 2g
Pulvis Talci 15g
Sucrose 15g
Preparation: get recipe quantity sucrose, add and wait water gaging to make 50% syrup, add the recipe quantity indapamide, mixing, the one-tenth suspension is stand-by; Other gets recipe quantity sucrose piller, puts in the high-efficiency coating pot, regulates 30～40 ℃ of inlet temperature, and above-mentioned suspension evenly is sprayed on the sucrose piller by the coating operation, in 50～60 ℃ of dryings 8 hours, crosses 20 mesh sieves, the pastille piller, stand-by; Get recipe quantity Eudragit RS 100, Eudragit RL 100, triethyl citrate adds the recipe quantity dissolve with ethanol, evenly be sprayed on the above-mentioned pastille piller by the coating operation, in 50～60 ℃ of dryings 8 hours, cross 15 mesh sieves, get slow-release pill, measure content, encapsulated 1000, promptly.
Example 2
A grain B grain adds up to
Indapamide 0.6g 0.9g 1.5g
Sucrose piller (15～30 order) 100g 150g 250g
Eudragit?RS?100 5g 10g 15g
Eudragit?RL?100 0.5g 1.5g 2g
Triethyl citrate 0.8g 1.2g 2g
Pulvis Talci 7g 8g 15g
Sucrose 7g 8g 15g
Preparation: get the sucrose of A grain, B grain recipe quantity respectively, add and wait water gaging to make 50% syrup, add the indapamide of A grain, B grain recipe quantity more respectively, the one-tenth suspension is stand-by; Get the sucrose piller of A grain, B grain recipe quantity in addition respectively, put in the high-efficiency coating pot, regulate 30～40 ℃ of inlet temperature, above-mentioned suspension evenly is sprayed on the sucrose piller by the coating operation,, crosses 20 mesh sieves in 50～60 ℃ of dryings 8 hours, get A, B pastille piller, stand-by; Get A grain, Eudragit RS 100, the Eudragit RL 100 of B grain recipe quantity, triethyl citrate more respectively, add an amount of dissolve with ethanol, evenly be sprayed on above-mentioned A, the B pastille piller by the coating operation, in 50～60 ℃ of dryings 8 hours, cross 15 mesh sieves, get A, B slow-release pill, mix the back and measure content, encapsulated 1000, promptly.
Getting slow releasing capsule of the present invention and commercially available ordinary tablet respectively, is solvent with 37 ± 0.5 ℃ dilute hydrochloric acid liquid 500ml, is that 100r/min measures release to change basket method rotating speed, and measurement result sees Table 1.
Table 1, indapamide slow release capsule and ordinary tablet release in vitro degree are relatively
The ordinary tablet slow releasing capsule
Time (h) example 1 example 2
0.5 100 - -
2 - 10.8 10.2
4 - 23.8 22.9
6 - 36.9 35.8
8 - 50.5 48.1
10 - 62.7 60.5
12 - 73.1 72.1
14 - 80.8 79.5
16 - 86.6 86.3
18 - 92.8 93.5
20 - 96.3 97.2
22 - 98.5 99.2
24 - 100.1 100.4
Can find out that from table 1 the indapamide ordinary tablet all discharged in 30 minutes, and slow releasing capsule of the present invention can maintain slowly release in 24 hours, therefore have tangible slow release effect.
Claims (2)
1, a kind of indapamide slow release capsule is to be prepared from (by weight percentage) by following material:
Indapamide 0.3～1%
Sucrose piller (15～30 order) 75～95%
Eudragit?RS?100 0.5～10％
Eudragit?RL?100 0.5～10％
Triethyl citrate 0.1～1%
Pulvis Talci 1～8%
Sucrose 1～10%
2, the capsular technology of the described indapamide slow release of a kind of preparation claim 1 is: the sucrose that (1) takes by weighing recipe quantity water gaging such as adds and makes 50% syrup, adds an amount of ethanol and recipe quantity indapamide again to make suspension, and is stand-by; Other takes by weighing recipe quantity sucrose piller and places the high-efficiency coating pot, by the coating operation above-mentioned suspension evenly is sprayed on the sucrose piller, dry back the pastille piller, the back of sieving is stand-by; Take by weighing Eudragit RS 100, Eudragit RL 100, the triethyl citrate of recipe quantity, add an amount of ethanol and make suspension, evenly be sprayed on the pastille piller by the coating operation then, dry back slow-release pill, survey content, pack capsulae vacuus into promptly.(2) take by weighing each composition of part recipe quantity,, by the proper proportion mixing, pack capsulae vacuus into promptly then by A, the B piller that (1) described preparation technology makes different rate of releasing drug.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA021592934A CN1511524A (en) | 2002-12-30 | 2002-12-30 | Indapamide slow-releasing capsule and its preparing process |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA021592934A CN1511524A (en) | 2002-12-30 | 2002-12-30 | Indapamide slow-releasing capsule and its preparing process |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1511524A true CN1511524A (en) | 2004-07-14 |
Family
ID=34237416
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA021592934A Pending CN1511524A (en) | 2002-12-30 | 2002-12-30 | Indapamide slow-releasing capsule and its preparing process |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1511524A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008136016A1 (en) * | 2007-05-08 | 2008-11-13 | Medreich Limited | A stable controlled release oral solid dosage form composition and a process thereof |
-
2002
- 2002-12-30 CN CNA021592934A patent/CN1511524A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008136016A1 (en) * | 2007-05-08 | 2008-11-13 | Medreich Limited | A stable controlled release oral solid dosage form composition and a process thereof |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US3922339A (en) | Sustained release medicant | |
| CN1084616C (en) | Film coated tablet of paracetamol and domperidone | |
| JP2003502359A (en) | New formulation | |
| CN1403077A (en) | Slow-release preparation | |
| CZ369292A3 (en) | Per-orally applicable form of a medicament for treating central states of dopamine insufficiency | |
| CN1328460A (en) | drug combination preparation | |
| CN113081994B (en) | A kind of compound medicine for treating Parkinson's disease and preparation method thereof | |
| EP1976490A1 (en) | Zaltoprofen-containing sustained release tablet and process for the preparation thereof | |
| CN103788043B (en) | The brilliant IV type of nicousamide, its method for making and its pharmaceutical composition and purposes | |
| AU588258B2 (en) | Controlled release nifedipine preparation | |
| CN110041326A (en) | Berberine hydrochloride and fumaric acid eutectic object and preparation method and its composition and purposes | |
| JPH08175983A (en) | Diclofenac sodium persistent pharmaceutical and its production | |
| CN1511524A (en) | Indapamide slow-releasing capsule and its preparing process | |
| CN102137664A (en) | Solid pharmaceutical preparations with active ingredients separated by boundaries | |
| CN106890166B (en) | Skin external preparation containing calcium receptor active compound | |
| CN101040850A (en) | Colchicine sustained-release pellets and the preparing method | |
| RU2411035C2 (en) | Modified release 6-methyl-2-ethyl-hydroxypyridine succinate dosage form | |
| CN107820424B (en) | Combination dosage forms of MU opioid receptor antagonists and opioid agents | |
| WO2003015807A1 (en) | Side effct-relieving agents and/or hypoglycemic effect enhancers for thiazolidine derivatives | |
| CN111728972A (en) | Metronidazole vitamin B6 composition | |
| CN110693845A (en) | Preparation process of metformin hydrochloride sustained-release tablet | |
| CN110787143A (en) | Metformin hydrochloride tablet and application thereof | |
| CN111714479A (en) | A pharmaceutical composition containing bexarotene | |
| CN109833299A (en) | A kind of micronization roxatidine acetate pharmaceutical salts pellet and preparation method thereof and its application | |
| KR20110012638A (en) | Pharmaceutical composition for improving bile secretion and liver function improvement by liver disease |
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 |