A kind of clopidogrel bisulfate tablet and preparation method thereof

Abstract

The invention relates to a hydrogen sulfate clopidogrel tablet and a preparation method thereof. The method comprises the following steps: firstly, preparing hydrogen clopidogrel and hydroxy propyl cellulose into micro-capsules by utilizing a drying-in-liquid method, then mixing with common auxiliary material in pharmacy, and preparing the tablet by tabletting.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a clopidogrel bisulfate tablet and a preparation method thereof. Background technique [0002] Clopidogrel is a platelet aggregation inhibitor that selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb / IIIa complex to achieve Inhibition of platelet aggregation. Clopidogrel is a prodrug that undergoes oxidation to form 2-oxo-clopidogrel, which is then hydrolyzed to form the active metabolite (a thiol derivative); oxidation is primarily mediated by cytochrome P450 isoenzymes 2B6 and 3A4 regulate, and 1A1, 1A2 and 2C19 also have certain regulatory effects. In vitro isolation of this active metabolite shows that it rapidly and irreversibly binds to platelet receptors, thereby inhibiting platelet aggregation. Clopidogrel reduces the chance of arterial blockage by in...

AI Technical Summary

Problems solved by technology

Two main problems in tablet production are: 1) Poor stability: clopidogrel bisulfate has a carboxylate structure, is unstable to damp heat, is easily hydrolyzed and degreased, and forms clopidogrel acid, especially, US6914141 points out lubricating Magnesium stearate can accelerate the degradation of clopidogrel; 2) clopidogrel bisulfate tablets are easy to stick and punch during production.

Polyethylene glycol has a low melting point, and the tableting process itself will melt and cause tablet sticking

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