中文摘要：

采用反溶剂重结晶法对疏水性药物依贝沙坦了进行微粉化研究。实验考察了依贝沙坦的质量浓度、体系温度、溶液与反溶剂的体积比以及搅拌转速等因素对微粉化过程的影响。结果表明较优的微粉化条件为：溶液中依贝沙坦的浓度0.01 g/mL,体系温度15℃,溶液与反溶剂体积比1∶20,搅拌转速1000 r/min;鼓风干燥后得到的依贝沙坦微粉粒度分布在1～2μm。红外分析显示所制得的样品与原料药化学结构基本相同;XRD分析结果表明微粉化产品的晶型为原料药的结晶形转变为无定形;溶剂残留检测结果表明微粉化后的依贝沙坦中甲醇的残留量符合药典标准;溶解速率实验表明微粉化后的依贝沙坦微粉溶解速率显著提高。

英文摘要：

Micronization of irbesartan （IBS） has been studied using an anti-solvent recrystallization method. The influence of varying the IBS concentration, system temperature, solution/anti-solvent volume ratio, stirring speed and drying method on the particle size and morphology was investigated. The optimum micronization conditions were found to be as follows： irbesartan concentration of 0.01 g/mL, system temperature of 15 ℃, solution/anti-solvent ratio of 1：20, stirring speed of 1000 r/min and use of oven drying. The as-prepared particles had a particle size distribution of 1 - 2 μm. IR spectra indicated that the micronized IBS powder had the same chemical composition as that of the crude drug. XRD revealed that the micronized product was amorphous while the crude drug was crystalline. Solvent residue test results showed that the product meets the standards of the Chinese Pharmacopoeia （2005）. Dissolution rate experiments showed that the dissolution rate of the irbesartan was significantly increased after micronization.