Bisulfate clopidogrel solid preparation, particles and preparation method thereof

A technology of clopidogrel bisulfate and solid preparations, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pill delivery, etc. It can solve the problems of content decline, instability, drug color change, etc. To achieve the effect of improving the sticking problem, good stability and improving stability

Inactive Publication Date: 2010-04-07
SHENZHEN SALUBRIS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sugar or starch excipients are unstable under strong acidic conditions, so that

Method used

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  • Bisulfate clopidogrel solid preparation, particles and preparation method thereof
  • Bisulfate clopidogrel solid preparation, particles and preparation method thereof
  • Bisulfate clopidogrel solid preparation, particles and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0039] 1. A tablet with a unit tablet weight of 0.08g and a clopidogrel content of 25mg / tablet

[0040] ●prescription

[0041] composition

Content (g)

Clopidogrel bisulfate

32.6

microcrystalline cellulose

15.8

Low-substituted hydroxypropyl cellulose

10.0

polyethylene glycol 6000

13.7

Cross-linked polyvinylpyrrolidone

4.7

Magnesium stearate

2.66

Sucrose Fatty Acid Ester

0.67

[0042] ●Preparation process

[0043] 1) Put 13.7g of polyethylene glycol 6000, 32.6g of clopidogrel bisulfate, 15.8g of microcrystalline cellulose, and 10.0g of low-substituted hydroxypropyl cellulose in a ball mill and heat to between 50°C and 90°C mixed for 30 minutes;

[0044] 2) Keep the temperature of the pulverizer cavity until the mixed material is moist and softened until there is no powder, take out the soft ring material, let it cool, and sieve it with a 24-mesh sieve to obtain granules

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Abstract

The invention relates to a bisulfate clopidogrel solid preparation, particles and a preparation method thereof. Particles contained by the solid preparation are solid mixture formed from bisulfate clopidogrel, cellulose excipients and molten adhesive with the melting point between 50 and 86 DEG, and an additionally added excipient of the particles contains weak alkaline lubricants and crosslinked polyvinylpyrrolidone. The solid preparation and the particles thereof are prepared by a melting-granulating method. The solid preparation has the advantages of solving sticking-picking problems existing in the preparation process, effectively reducing the degradation of clopidogrel during storage, reducing the incidence of transforming clopidogrel dextroisomer into clopidogrel levisomer and increasing the stability and security of the solid preparation.

Description

technical field [0001] The invention relates to a solid preparation of medicine, its granules and a preparation method thereof, in particular to a solid preparation of clopidogrel hydrogen sulfate, its granules and a method for preparing the solid preparation and the granules thereof by a melting granulation method. Background technique [0002] Clopidogrel is an inducible platelet aggregation inhibitor that acts by inhibiting the binding of adenosine monophosphate to its receptors. Clopidogrel is an inactive prodrug that is metabolized by hepatic cytochrome P450 into an active metabolite to exert its drug effect. Patents FR2215948 and FR2530247 disclose that clopidogrel has significant anti-platelet aggregation and antithrombotic effects. Clopidogrel reduces the chance of arterial blockage by inhibiting platelet aggregation, achieves the effect of preventing stroke and heart attack, and can effectively treat and prevent atherosclerosis. [0003] Clopidogrel is usually giv...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/48A61K9/14A61K31/4365A61K47/38A61P7/02A61P9/10
Inventor 叶澄海谭岳尧
Owner SHENZHEN SALUBRIS PHARMA
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