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目的制备米非司酮胃滞留缓释微丸片,并对其体外释药性质进行考察。方法采用挤出滚圆法制备米非司酮载药丸芯,对载药丸芯进行缓释功能层和黏附功能层包衣,得到米非司酮胃滞留缓释微丸;采用湿法制粒制备米非司酮速释颗粒,将米非司酮胃滞留缓释微丸、米非司酮速释颗粒外加辅料混合后压制成片剂,并从多个方面对米非司酮胃滞留缓释微丸片的体外释放进行考察。结果米非司酮溶解度随pH变化的拐点为pH 3.0;米非司酮原料微粉化导致其溶解速率提升和瞬时溶解度增加;米非司酮胃滞留缓释微丸片的速释部分释放速率比普通片更高,缓释部分比普通片持续时间更长,在猪胃黏膜上的滞留时间也大大延长;加速条件下的稳定性与上市包装的米非司酮普通片无差异。结论制备的新型米非司酮胃滞留缓释微丸片体外释药研究显示该微丸片的生物利用度高于普通片,使个体差异降低。
Objective To prepare mifepristone gastrorectal sustained-release pellets and investigate its in vitro release properties. Methods The mifepristone contained pellets were prepared by extrusion spheronization, the sustained-release functional layer and the adhesion functional layer were coated with drug-loaded pellets to obtain mifepristone gastrorectal sustained-release pellets. Chitosan immediate release granules, the mifepristone gastric retention sustained-release pellets, mifepristone immediate release granules plus excipients mixed into tablets, and in many aspects of mifepristone gastrorectal sustained-release pellets In vitro release tablets were investigated. Results The inflection point of mifepristone solubility with pH was pH 3.0. Micronization of mifepristone resulted in the increase of dissolution rate and instantaneous solubility of mifepristone. The rate release fraction of mifepristone sustained-release pellets was Ordinary tablets higher, sustained-release part of the longer than ordinary tablets, the residence time in the pig stomach mucosa also greatly extended; stability under accelerated conditions and the market packaging mifepristone tablets no difference. Conclusion The in vitro release of the new mifepristone gastrorectal sustained-release pellets showed that the bioavailability of the pellets was higher than that of ordinary tablets, and the individual differences were reduced.