Clopidogrel hydrogen sulfate dispersible tablets and preparation method thereof

Abstract

The invention discloses an anti-platelet aggregation drug-clopidogrel hydrogen sulfate tablet dispersible tablet and a preparation method thereof. The clopidogrel hydrogen sulfate tablet dispersible tablet consists of 30 percent to 55 percent of clopidogrel hydrogen sulfate and 45 percent to 70 percent of auxiliary materials according to the weight percentage. The auxiliary materials comprise disintegrant, loading agent, lubricant and taste-modifying agent, wherein, the disintegrant accounts for 5 percent to 20 percent of the total weight percentage of the prescription. The preparation method of the clopidogrel hydrogen sulfate tablet dispersible tablet is wet granulation tabletting press method or direct powder pressing method. Compared with other forms of preparation, the invention has the advantages of good dispersing state, short disintegration time, fast drug dissolvability, convenient drug administration, low production cost, good portability, high stability, etc.

Description

technical field [0001] The invention relates to an anti-platelet aggregation drug clopyrrole hydrogen sulfate dispersible tablet and a preparation method thereof. Background technique [0002] As a new generation of antiplatelet drugs, clopidogrel is biotransformed into active metabolites by cytochrome P450 in the liver, and selectively inhibits the binding of adenosine diphosphate (ADP) to its platelet receptors and the subsequent ADP-mediated Activation of the glycoprotein GP II b / III a complex, thereby inhibiting platelet aggregation. It is clinically used to treat atherosclerotic diseases, acute coronary syndrome, prevent in-stent restenosis and thrombotic complications after coronary stent implantation. [0003] Clopyrrole is administered in the form of bisulfate, and the currently disclosed clopyrrole preparations include tablets, capsules, drop pills, and injections. Have not yet seen the relevant literature report of clopirrole hydrogen sulfate dispersible tablet. ...

AI Technical Summary

Problems solved by technology

Chinese patent CN200610063151.7 discloses a solid preparation of clopyrrole sulfate and a preparation method thereof. Glycerol palmitic stearate is used as a lubricant in the components to solve the problem that clopyrrole is degraded into clopyrrole acid, but The effect is not ideal

The preparation of the tablet adopts dry compression method. In order to make the drug fully mixed, a large number of excipients are added and a tablet with a specification of 25mg is finally obtained through a very complicated process, which will undoubtedly increase the cost and cycle of drug production. In addition, the routine clinical dosage of clopidogrel tablets is 75 mg / time, which is equivalent to taking three tablets at a time for 25 mg tablets, which is obviously not conducive to improving the compliance of patients.

In the existing dosage forms, ordinary tablets often affect the full absorption of drugs due to slow disintegration and dissolution; although liquid preparations absorb quickly, they need to be injected, which is inconvenient to use and has poor stability, and is inconvenient to pack, transport and store.

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