Clopidogrel sulfate solid tablets and preparation method thereof

Abstract

The invention provides clopidogrel sulfate solid tablets and a preparation method thereof. The clopidogrel sulfate solid tablets are characterized in that clopidogrel sulfate is wrapped by sodium alginate microspheres and cooperated with trimethylchlorosilane modified superfine silica powder, and the stable solid tablets are obtained. According to the clopidogrel sulfate solid tablets, clopidogrel hydrogen sulfate serves as a main drug and cooperated with microcrystalline cellulose, vitamin E, a filling agent, a disintegrating agent, a lubricating agent, the sodium alginate microspheres and the modified superfine silica powder. Due to the fact that trimethylchlorosilane surface modification treatment is conducted on the superfine silica powder with a hollow mesoporous structure, and the sodium alginate microspheres are utilized for wrapping clopidogrel sulfate and mixed with the modified superfine silica powder, the problem that in a clopidogrel sulfate solid preparation, clopidogrel is degraded into clopidogrel carboxylic acid, and a clopidogrel dextro isomer is converted into a laevo isomer is solved, the stability of clopidogrel tablets in the storage process and safety of the clopidogrel tablets in the medical use process are guaranteed, and the therapeutical effect of the clopidogrel tablets is exerted more effectively. The preparation technology is simple and particularly suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical preparation and a preparation method thereof, in particular to a clopidogrel sulfate solid tablet and a preparation method thereof. Background technique [0002] Clopidogrel, whose chemical name is (+)-(S)-α-(2-o-chlorophenyl)-6,7-dihydrothieno[3,2-c]pyridine-5(4H)-acetic acid Methyl ester, which can selectively inhibit the binding of adenosine diphosphate (ADP) to its platelet receptor and the activation of the secondary ADP-mediated glycoprotein complex, reduces the chance of arterial blockage by inhibiting platelet aggregation, and achieves the inhibition of platelet The role of aggregation plays a role in the prevention of stroke and heart attack. It is mainly used clinically for the treatment of atherosclerosis, acute coronary syndrome, and the prevention of in-stent restenosis and thrombosis after coronary stent implantation. sexual complications, etc. [...

AI Technical Summary

Problems solved by technology

The micropowder silica gel with hollow mesoporous structure is modified by trimethylchlorosilane surface modification, and sodium alginate microspheres are used to wrap clopidogrel sulfate and mixed with modified micropowder silica gel to solve the problem of clopidogrel sulfate solid. The degradation of clopidogrel into clopidogrel acid and the conversion of clopidogrel D-isomer into L-isomer in the preparation ensure the stability of clopidogrel tablets during storage and the safety during medical use , so that it can play a more effective therapeutic role; at the same time, the added modified micro-powder silica gel can also greatly improve the processing fluidity of clopidogrel sulfate, solve the sticking problem in the preparation process, and is suitable for industrial production

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