摘要
目的通过行星式球磨法制备盐酸依福地平共研磨物以提高盐酸依福地平的溶出度。方法将盐酸依福地平与不同辅料进行共研磨,对不同的研磨时间、辅料的用量、辅料的形状及共研磨物粉体学性质等进行考察,使用了Peppas公式验证共研磨物的溶出机理,并用川北方程验证辅料流动性对共研磨物溶出的影响,从而筛选最优处方。结果 MCC PH101、MCC KG802、CL-CMC-Na与难溶性药物盐酸依福地平以质量比3∶1的比例共研磨后,能很好的改善其体外溶出度。结论棒状或纤维状辅料与盐酸依福地平可以产生"网络状"结构的共研磨物,既有效的防止了微粉化后药物自身的聚集,也改善了其溶出机制,大幅度提高了盐酸依福地平的溶出度。
Objective To improve the solubility of efonidipine hydrochloride using a planetary ball-milling technique. Methods Efonidipine hychloride was co-milled with different excipients, and the influence of different co-milling time on the dissolution rate, different content of excipients, the characteristic of excipients, powder properties of co-millings were studied. Peppas equation was used to explain the mechanism of dissolution, and Kawakita equation was applied to investigate the influence of flowability on dissolution. The optimized formulation was obtained. Results Efonidipine hydrochloride co-millings with MCC PH101, MCC KG802 and Cl-CMC-Na at 1∶3 ratio displayed a rapid-release characteristics. Conclusions co-millings of efondipine hydrochloride with clavate or threadiness excipients can produce a network like structure, which can not only effectively prevent the aggregation of micronized drug after co-milling but also improve the dissolution rate of efonidipine hydrochloride.
出处
《中国药剂学杂志（网络版）》
2015年第5期162-172,共11页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
盐酸依福地平
共研磨
溶出机制
粉体学性质
pharmaceutics
efonidipine hydrochloride
co-milling
dissolution mechanism
powder property
