溶解-析出原理在减小固体制剂中难溶性药物粒径的应用

利用弱碱性和弱酸性药物在溶液中的溶解度受pH影响的特点,加入适宜的酸化剂(或碱化剂)使之溶解,再加入载体材料和碱化剂(或酸化剂),通过湿法制粒得到粒径较小的难溶性药物固体制剂。采用该方法制备了难溶性药物利培酮、吲达帕胺或格列吡嗪的颗粒剂和片剂,并与采用预粉碎原药制备的产品比较。结果表明,本法能显著减小药物颗粒的粒径,并明显提高难溶性药物片剂的溶出速率。

Application of Dissolution-precipitation to Reduction in the Diameter of Slightly Soluble Drugs in Solid Preparation

The solubility of alkalescent and weakly acidic drugs can be affected by pH of the solution.So by adding appropriate acidulant(or alkalizer) to dissolve the drugs,then adding the carrier and alkalizer(or acidulant),the solid preparation of the slightly soluble drug with small particle size can be prepared by wet granulation method.The granules and tablets of slightly soluble drug(risperidone,indapamide or glipizide) were prepared by this method as well as the preparations with pre-pulverized bulk drugs.The results showed that the diameter of the granule prepared by this method was significantly reduced as well as the dissolution rate of the tablets was significantly increased.