Clopidogrel hydrogen sulfate tablet and preparation method thereof

Abstract

The invention relates to a clopidogrel hydrogen sulfate tablet and a preparation method thereof. Clopidogrel is more easily converted into clopidogrel acid and a clopidogrel dextroisomer is more easily converted into a levoisomer in the prior clopidogrel hydrogen sulfate tablet. The clopidogrel hydrogen sulfate tablet takes clopidogrel hydrogen sulfate as a main medicine and is matched with filling agent, disintegrant, flow agent and lubricant, and a mixture with the weight percent of 0.05-5 of one or two of vitamin C and butylated hydroxyanisole are added into the clopidogrel hydrogen sulfate tablet. The vitamin C and/or the butylated hydroxyanisole can well inhibit the clopidogrel from being converted into the clopidogrel acid and inhibit the clopidogrel dextroisomer from being converted into the levoisomer, thereby improving the stability of the clopidogrel hydrogen sulfate tablet and the safety and the effectiveness of clinical medicines.

Description

technical field [0001] The invention relates to the field of medicine, in particular 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 inhibiting platelet aggre...

AI Technical Summary

Problems solved by technology

But present clopidogrel bisulfate tablet has the following problems: the clopidogrel in the clopidogrel bisulfate tablet is more easily converted into clopidogrel acid, and the dextro isomer of clopidogrel is more easily converted into levoisomer body

Existing reports indicate that the left-handed isomer of clopidogrel has almost no anti-platelet aggregation effect, and animal test results show that the toxicity of the left-handed isomer of clopidogrel is significantly higher than that of the right-handed isomer of clopidogrel

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