Solid preparation of clopidogrel or pharmaceutically acceptable salt thereof

Abstract

The invention relates to a solid preparation of clopidogrel or a pharmaceutically acceptable salt thereof, and the adopted technical scheme is as follows: taking the clopidogrel or the pharmaceutically acceptable salt as a principal agent, taking lactose, partially pregelatinized starch, hydroxypropyl methyl cellulose, silicon dioxide and talcum powder as excipients, and directly pressing powder into tablets.

Description

technical field [0001] The invention relates to a solid preparation of an anticoagulant drug clopidogrel or a pharmaceutically active salt thereof and a preparation method thereof. technical background [0002] Clopidogrel is a novel thienopyridine antiplatelet drug with a chemical structure similar to ticlopidine except that there is one more carboxymethyl group on the side chain. Clopidogrel is metabolized in vivo, and its active metabolites can selectively and irreversibly bind to a purine adenosine diphosphate (ADP) receptor on the surface of the platelet membrane, blocking the inhibitory effect of ADP on adenylate cyclase , thereby promoting the phosphorylation of cAMP-dependent, PGE1-stimulated vasodilator-stimulated phosphoprotein (VASP), inhibiting the activation of fibrinogen receptor (GPIIb / IIIa) and inhibiting platelet aggregation. In addition, clopidogrel can reduce the expression of platelet selectin (P-selectin, CD62, a marker of platelet degranulation), and i...

AI Technical Summary

Problems solved by technology

Clopidogrel has no biological activity in vitro, and needs to be transformed by hepatic cytochrome P450 enzymes (probably mainly CYP1A subfamily) to produce active metabolites, which have not yet been identified