CN1108798C - Compound preparation for curing and preventing thrombosis and apoplexy and its preparing method - Google Patents
Compound preparation for curing and preventing thrombosis and apoplexy and its preparing method Download PDFInfo
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- CN1108798C CN1108798C CN99116029A CN99116029A CN1108798C CN 1108798 C CN1108798 C CN 1108798C CN 99116029 A CN99116029 A CN 99116029A CN 99116029 A CN99116029 A CN 99116029A CN 1108798 C CN1108798 C CN 1108798C
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- ethyl cellulose
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- 150000001875 compounds Chemical class 0.000 title claims abstract description 25
- 238000002360 preparation method Methods 0.000 title claims abstract description 19
- 208000007536 Thrombosis Diseases 0.000 title claims abstract description 12
- 206010008190 Cerebrovascular accident Diseases 0.000 title claims description 10
- 208000006011 Stroke Diseases 0.000 title claims description 10
- 238000000034 method Methods 0.000 title claims description 6
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 17
- 239000000203 mixture Substances 0.000 claims description 15
- 239000001856 Ethyl cellulose Substances 0.000 claims description 14
- 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 claims description 14
- 229920002472 Starch Polymers 0.000 claims description 14
- 235000019325 ethyl cellulose Nutrition 0.000 claims description 14
- 229920001249 ethyl cellulose Polymers 0.000 claims description 14
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
- 239000008107 starch Substances 0.000 claims description 14
- 235000019698 starch Nutrition 0.000 claims description 14
- 239000005711 Benzoic acid Substances 0.000 claims description 9
- 235000010233 benzoic acid Nutrition 0.000 claims description 9
- 229960003328 benzoyl peroxide Drugs 0.000 claims description 9
- 230000002265 prevention Effects 0.000 claims description 9
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 7
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 7
- 230000001476 alcoholic effect Effects 0.000 claims description 7
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims description 7
- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 7
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 7
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 7
- 239000011734 sodium Substances 0.000 claims description 7
- 229910052708 sodium Inorganic materials 0.000 claims description 7
- 238000001035 drying Methods 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 5
- 239000008187 granular material Substances 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 5
- 239000007779 soft material Substances 0.000 claims description 5
- BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 abstract description 10
- 229960001138 acetylsalicylic acid Drugs 0.000 abstract description 10
- 229960002768 dipyridamole Drugs 0.000 abstract description 7
- IZEKFCXSFNUWAM-UHFFFAOYSA-N dipyridamole Chemical compound C=12N=C(N(CCO)CCO)N=C(N3CCCCC3)C2=NC(N(CCO)CCO)=NC=1N1CCCCC1 IZEKFCXSFNUWAM-UHFFFAOYSA-N 0.000 abstract description 7
- 230000000638 stimulation Effects 0.000 abstract description 3
- 230000000694 effects Effects 0.000 abstract description 2
- 239000007939 sustained release tablet Substances 0.000 abstract 2
- 210000001035 gastrointestinal tract Anatomy 0.000 abstract 1
- 239000003826 tablet Substances 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 3
- 238000005516 engineering process Methods 0.000 description 3
- 206010013786 Dry skin Diseases 0.000 description 2
- 230000000202 analgesic effect Effects 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 206010003210 Arteriosclerosis Diseases 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000003146 anticoagulant agent Substances 0.000 description 1
- 229940127219 anticoagulant drug Drugs 0.000 description 1
- 208000011775 arteriosclerosis disease Diseases 0.000 description 1
- -1 benzoic acid compound Chemical class 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 238000007689 inspection Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 208000010125 myocardial infarction Diseases 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 1
- 238000009423 ventilation Methods 0.000 description 1
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Abstract
本发明公开了一种治疗、预防血栓形成及中风的复方缓释片。本发明还涉及该复方缓释片的制备方法。本发明的复方缓释片中潘生丁与阿司匹林均可缓慢释放，使疗效维持较长时间，同时减轻了阿司匹林对消化道的刺激，而且制备工艺简单，成本低。The invention discloses a compound slow-release tablet for treating and preventing thrombosis and stroke. The invention also relates to a preparation method of the compound sustained-release tablet. Both dipyridamole and aspirin in the compound sustained-release tablet of the invention can be released slowly, so that the curative effect can be maintained for a long time, and at the same time, the stimulation of the aspirin on the digestive tract can be alleviated, and the preparation process is simple and the cost is low.
Description
The present invention relates to compound preparation of a kind of treatment, prevention thrombosis and apoplexy and preparation method thereof, is compound slow-release tablet of a kind of treatment, prevention thrombosis and apoplexy and preparation method thereof specifically.
2,2 ', 2 "; 2 " ' [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide (dipyridamole, the different name persantin) is a kind of clinical medicament for resisting platelet aggregation that is widely used in, is mainly used in diseases such as prevention thrombosis, arteriosclerosis and myocardial infarction recurrence.2-(acetoxyl group) benzoic acid (aspirin, different name aspirin) is a kind of traditional analgesic, antiinflammatory, analgesic.Prove that in recent years two medicines use simultaneously, thereby can be used to prevent and treat diseases such as apoplexy, arterial thrombus by anticoagulant.According to relevant patent DE3627423A, EP257344A report, respectively persantin is made slow-release pill, aspirin is made coated tablet after, get an amount of persantin piller then and a slice aspirin coated tablet together incapsulates, make compound capsule.This compound capsule is because persantin piller and aspirin coated tablet prepare respectively, and not only technology is loaded down with trivial details, the cost height, and because aspirin does not have slow releasing function a large amount of release, very big to gastral stimulation, can cause gastral untoward reaction.
The object of the present invention is to provide a kind of compound preparation with treatment, prevention thrombosis and apoplexy of slow releasing function.
Another object of the present invention is for providing a kind of technology simple, the preparation method of the compound slow-release tablet that cost is low.
The compound preparation of treatment provided by the present invention, prevention thrombosis and apoplexy is a kind of compound slow-release tablet.
The compound preparation of treatment provided by the present invention, prevention thrombosis and apoplexy be a kind ofly contain 2,2 ', 2 "; 2 " ' [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide and 2-(acetoxyl group) benzoic acid compound slow-release tablet.
The compound preparation of treatment provided by the present invention, prevention thrombosis and apoplexy is composed of the following components: 2,2 ', 2 "; 2 " ' [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide 200mg, 2-(acetoxyl group) benzoic acid 25mg, ethyl cellulose 48～72mg, microcrystalline Cellulose 48～72mg, starch 32～48mg, carboxymethyl starch sodium 9.2～13.5mg, magnesium stearate 1.85～2.80mg.
The method that the present invention prepares above-mentioned compound slow-release tablet may further comprise the steps successively: (1) is with 200mg 2,2 ', 2 ', 2 ', [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide, 25mg 2-(acetoxyl group) benzoic acid, 48～72mg ethyl cellulose, 48～72mg microcrystalline Cellulose, 32～48mg starch are crossed mix homogeneously behind 80 mesh sieves respectively.(2) be binding agent with the ethyl cellulose alcoholic solution, said mixture is made soft material, again it is crossed 16 mesh sieves and make wet granular.(3) with above-mentioned wet granular aeration-drying, through 16 mesh sieve granulate, 80 mesh sieves sieve goes to add the carboxymethyl starch sodium 9.2～13.5mg that crosses 80 mesh sieves, magnesium stearate 1.85～2.80mg, mix homogeneously, tabletting behind the fine powder.
Wherein, the concentration of used ethyl cellulose alcoholic solution is 1%～1.5%, and the temperature during wet granular aeration-drying is 50～60 ℃.
With the compound slow-release tablet that the present invention makes, as follows according to drug release determination method (two appendix releases of Chinese Pharmacopoeia nineteen ninety-five version inspection technique, first method) measurement result:
Time (hour) 12468
Cumulative release percentage ratio (%) 10～30 25～45 35～65 60～85＞80
The present invention compared with prior art, preparation technology is simple, cost is low, persantin and aspirin all can slowly discharge in the compound recipe, not only make curative effect keep the long period, have also alleviated aspirin to gastral stimulation.
Embodiment 1 (1) is 200mg 2,2 ', 2 ', 2 ', [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide, 25mg 2-(acetoxyl group) benzoic acid, 52mg ethyl cellulose, 72mg microcrystalline Cellulose, 35mg starch are crossed mix homogeneously behind 80 mesh sieves respectively.(2) be binding agent with 1.5% ethyl cellulose alcoholic solution, said mixture is made soft material, again it is crossed 16 mesh sieves and make wet granular.(3) with above-mentioned wet granular in 50 ℃ of aeration-dryings, through 16 mesh sieve granulate, add the carboxymethyl starch sodium 13.5mg that crosses 80 mesh sieves, magnesium stearate 2.80mg, mix homogeneously, tabletting behind the 80 mesh sieves sieves fine powder.
Promptly get compound slow-release tablet of the present invention.
Embodiment 2 (1) is with 200mg 2,2 ', 2 ', 2 ', [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide, 25mg 2-(acetoxyl group) benzoic acid, 60mg ethyl cellulose, 60mg microcrystalline Cellulose, 40mg starch are crossed mix homogeneously behind 80 mesh sieves respectively.(2) be binding agent with 1.3% ethyl cellulose alcoholic solution, said mixture is made soft material, again it is crossed 16 mesh sieves and make wet granular.(3) above-mentioned wet granular is dry in 55 ℃ of ventilations thousand, after 16 mesh sieve granulate, 80 mesh sieves sieve removes fine powder, add and cross 80 mesh sieve carboxymethyl starch sodium 12.3mg, magnesium stearate 2.46mg, mix homogeneously, tabletting.
Promptly get compound slow-release tablet of the present invention.
Embodiment 3 (1) is with 200mg 2,2 ', 2 ", 2 " ' [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide, 25mg 2-(acetoxyl group) benzoic acid, 69mg ethyl cellulose, 48mg microcrystalline Cellulose, 47mg starch are crossed mix homogeneously behind 80 mesh sieves respectively.(2) be binding agent with 1.0% ethyl cellulose alcoholic solution, said mixture made soft material again it is crossed 16 mesh sieves and make wet granular.(3) with above-mentioned wet granular in 60 ℃ of aeration-dryings, through 16 mesh sieve granulate, 80 mesh sieves sieves goes to add the carboxymethyl starch sodium 9.2mg that crosses 80 mesh sieves, magnesium stearate 1.85mg, mix homogeneously, tabletting behind the fine powder.
Promptly get compound slow-release tablet of the present invention.
Claims (4)
- The compound preparation of 1, a kind of treatment, prevention thrombosis and apoplexy is characterized in that this compound preparation is a kind of compound slow-release tablet, and is composed of the following components: 2,2 ', 2 ", 2 " ', [(4,8-dipiperidino pyrimido [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide 200mg, 2-(acetoxyl group) benzoic acid 25mg, ethyl cellulose 48～72mg, microcrystalline Cellulose 48～72mg, starch 32～48mg, carboxymethyl starch sodium 9.2～13.5mg, magnesium stearate 1.85～2.80mg.
- 2, a kind of method for preparing the described compound preparation of claim 1, may further comprise the steps successively: (1) is with 200mg 2,2 '; 2 "; 2 " ', [(4,8 one dipiperidino pyrimidos [5,4-d] pyrimidine-2,6-two bases) two nitrilo-s]-tetraethoxide, 25mg 2-(acetoxyl group) benzoic acid, 48～72mg ethyl cellulose, 48～72mg microcrystalline Cellulose, 32～48mg starch are crossed mix homogeneously behind 80 mesh sieves respectively.(2) be binding agent with the ethyl cellulose alcoholic solution, said mixture is made soft material, again it is crossed 16 mesh sieves and make wet granular.(3),, after 80 mesh sieves sieve removes fine powder, add the carboxymethyl starch sodium 9.2～13.5mg that crosses 80 mesh sieves, magnesium stearate 1.85～2.80mg, mix homogeneously, tabletting through 16 mesh sieve granulate with above-mentioned wet granular aeration-drying.
- 3, preparation method as claimed in claim 2, the concentration that it is characterized in that used ethyl cellulose alcoholic solution is 1%～1.5%.
- 4, preparation method as claimed in claim 2, the temperature when it is characterized in that wet granular aeration-drying are 50～60 ℃.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN99116029A CN1108798C (en) | 1999-01-26 | 1999-01-26 | Compound preparation for curing and preventing thrombosis and apoplexy and its preparing method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN99116029A CN1108798C (en) | 1999-01-26 | 1999-01-26 | Compound preparation for curing and preventing thrombosis and apoplexy and its preparing method |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1227100A CN1227100A (en) | 1999-09-01 |
| CN1108798C true CN1108798C (en) | 2003-05-21 |
Family
ID=5278880
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN99116029A Expired - Fee Related CN1108798C (en) | 1999-01-26 | 1999-01-26 | Compound preparation for curing and preventing thrombosis and apoplexy and its preparing method |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1108798C (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1093814A1 (en) * | 1999-10-22 | 2001-04-25 | Boehringer Ingelheim Pharma KG | Use of dipyridamole or mopidamol in the manufacture of a medicament for the treatment and prevention of fibrin-dependent microcirculation disorders |
| PT1350511E (en) * | 2000-12-25 | 2008-10-28 | Ube Industries | Medicinal compositions containing aspirin |
-
1999
- 1999-01-26 CN CN99116029A patent/CN1108798C/en not_active Expired - Fee Related
Non-Patent Citations (1)
| Title |
|---|
| 《南京医学院学报》，13(3) 1993-01-01 刘广余等，"阿斯匹林与双嘧哌胺醇复方制剂对血小板凝集影响的研究" * |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1227100A (en) | 1999-09-01 |
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