Clopidogrel hydrogensulfate composition and preparation method thereof

A technology for clopidogrel hydrogen sulfate and pharmaceutical preparations, applied in the field of medicine and biology, can solve problems such as poor stability, stickiness, unsuitability for industrial production, etc., and achieve the effects of improved stability and easy storage

Active Publication Date: 2012-01-11
北京先通源医药科技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clopidogrel bisulfate can exist in polymorphic crystals of various forms, and the crystal form involved in the present invention is I crystal form, but the existing clopidogrel bisulfate I crystal preparation has serious sticking impact during the preparation process. Phenomenon, and poor stability, not suitable for industrial production

Method used

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  • Clopidogrel hydrogensulfate composition and preparation method thereof
  • Clopidogrel hydrogensulfate composition and preparation method thereof
  • Clopidogrel hydrogensulfate composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] formula:

[0105] Clopidogrel bisulfate 97.875 g

[0106] Microcrystalline Cellulose 70 g

[0107] Mannitol 52 g

[0108] Hypromellose 18 g

[0109] Stearic acid 3.5 g

[0110] Silica 9.3 g

[0111] Preparation method:

[0112] 1) Pass clopidogrel bisulfate, microcrystalline cellulose, mannitol, and hydroxypropyl cellulose through a 60-mesh sieve for subsequent use; pass stearic acid and silicon dioxide through a 100-mesh sieve for subsequent use; Clopidogrel, microcrystalline cellulose, mannitol, and 2 / 3 of the formula amount of hydroxypropyl cellulose were added and mixed in equal amounts, passed through a 16-mesh sieve with a dry preparation machine to granulate, and set aside; the formula amount was weighed separately The hydroxypropyl cellulose of stearic acid, silicon dioxide and 1 / 3 formula quantity are added in the granule of above-mentioned dry granule, mix well, detect the content of intermediate with high performance liquid chromatography; 2) tabletting...

Embodiment 2

[0114] formula:

[0115] Clopidogrel Bisulfate 80 g

[0116] Microcrystalline cellulose 80 g

[0117] Mannitol 55 g

[0118] Hypromellose 15 g

[0119] Stearic acid 2 g

[0120] Silica 10 g

[0121] Preparation method:

[0122] 1) Pass clopidogrel bisulfate, microcrystalline cellulose, mannitol, and hydroxypropyl cellulose through a 60-mesh sieve for subsequent use; pass stearic acid and silicon dioxide through a 100-mesh sieve for subsequent use; Clopidogrel, microcrystalline cellulose, mannitol, and 2 / 3 of the formula amount of hydroxypropyl cellulose were added and mixed in equal amounts, passed through a 16-mesh sieve with a dry preparation machine to granulate, and set aside; the formula amount was weighed separately The hydroxypropyl cellulose of stearic acid, silicon dioxide and 1 / 3 formula quantity are added in the granule of above-mentioned dry granule, mix well, detect the content of intermediate with high performance liquid chromatography; 2) tabletting 3) fil...

Embodiment 3

[0124] formula:

[0125] Clopidogrel Bisulfate 110 g

[0126] Microcrystalline cellulose 60 g

[0127] Mannitol 48 g

[0128] Hypromellose 20 g

[0129] Stearic acid 4 g

[0130] Silica 9 g

[0131] Preparation method:

[0132] 1) Pass clopidogrel bisulfate, microcrystalline cellulose, mannitol, and hydroxypropyl cellulose through a 60-mesh sieve for subsequent use; pass stearic acid and silicon dioxide through a 100-mesh sieve for subsequent use; Clopidogrel, microcrystalline cellulose, mannitol, and 2 / 3 of the formula amount of hydroxypropyl cellulose were added and mixed in equal amounts, passed through a 16-mesh sieve with a dry preparation machine to granulate, and set aside; the formula amount was weighed separately The hydroxypropyl cellulose of stearic acid, silicon dioxide and 1 / 3 formula quantity are added in the granule of above-mentioned dry granule, mix well, detect the content of intermediate with high performance liquid chromatography; 2) tabletting 3) fil...

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Abstract

The invention aims at disclosing a clopidogrel hydrogensulfate medicament preparation and a preparation method thereof. In the medicament preparation disclosed by the invention, clopidogrel hydrogensulfate is utilized as a main medicament component, and a filler, a disintegrating agent, a lubricating agent, a flow agent and an antisticking agent are utilized as auxiliary materials. The invention also provides a preparation method of clopidogrel hydrogensulfate. The formulation technology of the preparation is good in reproducibility and practicability and suitable for industrial production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation and a preparation method thereof, in particular to a clopidogrel bisulfate preparation and a preparation method thereof, belonging to the field of medical biotechnology. Background technique [0002] Clopidogrel bisulfate, whose chemical name is methyl(+)-(S)-α-o-chlorophenyl-6,7-dihydrothiophene[3,2-c]pyridine-5(4H)acetate Bisulfate, molecular formula: C 16 h 16 ClNO 2 S·H 2 SO 4 , the structural formula: [0003] Clopidogrel bisulfate is clinically used as an antithrombotic drug, selectively inhibiting the binding of adenosine diphosphate (ADP) to its platelet receptor and the secondary ADP-mediated glycoprotein GPlllb / llla complex activation, thereby inhibiting platelet aggregation. In addition, clopidogrel bisulfate can also inhibit platelet aggregation induced by other agonists by blocking platelet activation caused by released ADP. Compared with other antiplatelet drugs, clopidogrel ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4365A61K9/28A61K47/38A61K47/10A61K47/12A61K47/04A61P7/02A61P9/10
Inventor 齐慧
Owner 北京先通源医药科技股份有限公司
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