瓜蒌薤白胃内漂浮微丸的制备及体外释放度测定

Preparation of Gualou-Xiebai intragastric floating pellets and determination of their release in vitro

目的以挤出滚圆法制备瓜蒌薤白胃内漂浮微丸(18~24目)(简称微丸),并探讨其体外释放特性。方法在单因素实验的基础上,以微晶纤维素(MCC)、十八醇、羟丙甲纤维素-K4M(HPMC-K4M)、HPMCK15M占处方中固体辅料的百分比为考察因素,以微丸的漂浮时间为指标,采用星点设计-效应面优化法优化处方。以释放介质中3,29-二苯甲酰基栝楼仁三醇的含量为指标,测定微丸的体外释放度,并探讨其释放特性。结果微丸的最佳处方为:瓜蒌薤白提取物干浸膏25 g、MCC 6 g、十八醇11 g、HPMC-K4M 3 g、HPMC-K15M 11 g、70%乙醇溶液作润湿剂、40%聚乙烯吡咯烷酮(PVP-K30)溶液作黏合剂。所制得的微丸体外漂浮时间可达到12 h,累积释放率数据用一级释放模型拟合度较高(r>0.97)。结论本实验制得的微丸具有良好的漂浮性能和缓释效果,该制备方法可行。

Objective To prepare Gualou-Xiebai intragastric floating pellets(18-24 mesh)by extrusion-spheronization method,and investigate their release characteristics in vitro.Methods Using the floating time of pellets as indicator and the percentage of microcrystalline cellulose(MCC),octadecanol,hydroxypropyl methylcellulose-K4M(HPMC-K4M)and HPMC-K15M in the solid excipients of the prescription as affecting factors on the basis of single factor experiments,the formulation was optimized by star design-response surface optimization method.Taking the content of 3,29-dibenzoyl karounitriol in the release medium as the index,the release rate of the pellets in vitro was determined and the release characteristics were explored.Results The optimum prescription of these pellets was as follows:Gualou-Xiebai dry extract 25 g,MCC 6 g,octadecanol 11 g,HPMC-K4M 3 g,HPMC-K15M 11 g,70%ethanol solution as wetting agent,and 40%polyvinylpyrrolidone(PVP-K30)solution as binder.The floating time in vitro of the pellets prepared by this prescription was 12 hours,and the cumulative release rate data fitted well with the first-order release model(r>0.97).Conclusion The Gualou-Xiebai intragastric floating pellets prepared in this study had good floating property and sustained release effect,indicating that the preparation method is feasible.