米非司酮胃滞留缓释微丸片的制备及其体外释药研究

发布时间：2018-04-09 07:29

本文选题：米非司酮　切入点：胃滞留缓释微丸片　出处：《中国药学杂志》2017年09期

【摘要】：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。
[Abstract]:Objective to prepare Mifepristone sustained-release pellets and investigate their drug release properties in vitro.Methods Mifepristone loaded pellets core was prepared by extrusion round method and coated with sustained release function layer and adhesive function layer to obtain Mifepristone gastric retention sustained release pellets, and Mifepristone quick release pellets were prepared by wet granulation.Mifepristone sustained release pellets and mifepristone rapid release pellets were mixed and pressed into tablets. The in vitro release of mifepristone gastric retention sustained release pellets was investigated from many aspects.Results the inflection point of the change of mifepristone solubility with pH was pH 3.0, the dissolution rate and instantaneous solubility of mifepristone pellets were increased due to micro-pulverization of mifepristone, and the rapid release rate of mifepristone sustained release pellets was higher than that of common tablets.The duration of sustained release was longer than that of ordinary tablets, and the retention time in pig gastric mucosa was also prolonged, and the stability under accelerated conditions was not different from that of conventional mifepristone tablets.Conclusion the bioavailability of the new Mifepristone sustained-release pellets in vitro was higher than that of the common tablets, and the individual difference was decreased.
【作者单位】：南方医科大学药学院;南方医科大学中心实验室;
【基金】：广东省科技厅对外科技合作项目:中德合作-缓控释给药技术研发平台(NO粤科规划字[2012]98号)
【分类号】：R943

【相似文献】