Preparation method of the solid formulation of Clopidogrel bisulfate

摘要

A solid formulation of clopidogrel bisulfate and its preparation method are disclosed. The formulation includes clopidogrel bisulfate as active ingredient, colloidal silicon dioxide as anti-adherent/coating and the carriers selected from diluent, binder, glidant, disintegrant and/or lubricant.

主权项

1. A method for preparing a pharmaceutical composition of Clopidogrel bisulfate, comprising the steps of:
(a) mixing Colloidal Silicon Dioxide and Clopidogrel bisulfate to form a premix granule; wherein the premix granule contains the following components: Clopidogrel bisulfate having an average particle size of 10-100 μm, and Colloidal Silicon Dioxide for covering Clopidogrel bisulfate, wherein the weight of Colloidal Silicon Dioxide is 0.5%-10% w/w of that of Clopidogrel bisulfate; wherein the average particle size of Clopidogrel bisulfate is 10-100 μm; and wherein the particle size of Colloidal Silicon Dioxide is 7-16 nm and with a surface area of 200-400 m2/g; (b) mixing the premix granule obtained from step (a) with diluents, followed by adding an alcohol solution of a binder for wet granulation to obtain a wet granule; (c) drying the wet granule obtained from step (b) followed by screening to obtain a dry granule; (d) mixing the dry granule obtained from step (c) with 0.2-0.5 weight % Colloidal Silicon Dioxide as a glidant, disintegrant and lubricants, followed by compressing to obtain a Clopidogrel bisulfate tablet; and (e) Optionally coating the tablet obtained from step (d) to obtain a film-coated final tablet.