一贯煎定时释药缓释微丸的制备及其体外释放性质的考察  

Preparation of Yiguanjian time-controlled release pellets and their in vitro release characterization

作　　者：彭博[1] 唐开冲 郭军[1] 孙天慧[1] 李三鸣[1] 

机构地区：[1]沈阳药科大学药学院

出　　处：《中国药剂学杂志（网络版）》2008年第6期357-363,共7页Chinese Journal of Pharmaceutics：Online Edition

摘　　要：目的制备一贯煎定时释药缓释微丸并考察其体外释药特性。方法将复方中药提取精制后以挤出滚圆法制备一贯煎微丸,采用水溶胀性材料为内包衣溶胀层,乙基纤维素水分散体(Surelease)为外包衣控释层,用流化床进行包衣,制备一贯煎定时释药缓释微丸,并考察影响其体外释药的各种因素。结果以低取代羟丙基纤维素(L-HPC)为溶胀层包衣材料,保持溶胀层包衣增重20%不变,分别制备控释层包衣增重为0%、20%和24%的包衣微丸,均匀混合,制得一贯煎定时释药缓释硬胶囊制剂;释放度测定结果表明,一贯煎定时释药缓释微丸中2个主要成分梓醇和阿魏酸体外释放的f2值为78.2,两成分的释放无显著性差异,并具有明显的缓释特征。结论制备的一贯煎定时缓释微丸可以使其中的不同成分在缓释的同时达到同步释放,符合传统中药理论。Objective To prepare Yiguanjian(traditional Chinese medicines) time-controlled release pellets and investigate drug release behavior in vitro. Method Yiguanjian pellets were prepared by extrusion-spheronization method after refining the extracted material medica. Thereafter, using water swelling material as the inner swelling layer and ethylcellulose aqueous dispersion(Surelease) as the outer controlled layer, Yiguanjian sustained-release pellets were prepared in a fluid-bed coater. Factors influencing the in vitro drug release was investigated. Results Keeping low-substituted hydroxypropyl cellulose(L-HPC) as the coating material of the inner swelling layer with a weight increase of 20 %, three different kinds of Yiguanjian sustained release pellets were prepared by keeping the weight ratio of the outer Surelease coating membrane at 0 %, 20 % and 24 %, respectively. Yiguanjian sustained-release capsules were developed by mixing the above three kinds of coated pellets at an equivalent ratio. No significant difference was found in the in vitro release behavior of catalpol and ferulic acid from Yiguanjian sustained-release pellets, with f2 value of 78.2, with apparent sustained release properties. Conclusion Various components could be released synchronously from Yiguanjian sustained-release pellets in a sustained manner. This comforms to the theory of traditional Chinese medicine.

关 键 词：药剂学 一贯煎 缓释 微丸 流化床 定时释药 

分 类 号：TQ461[化学工程—制药化工]