利福喷丁自乳化胶囊制备及释药特性研究

Study on rifapentine self-emulsifying hard capsule and its release characteristics

目的研制利福喷丁自乳化胶囊,探索固态自乳化药物释放系统(SEDDS)的释药特性。方法用正交试验设计优化由利福喷丁、OP 10-司盘85复合乳化剂、PEG 4000辅助表面活性剂组成的SEDDS处方,制备利福喷丁半固态自乳化膏体填充胶囊,测定自乳化胶囊的释放度,并考查其模拟体内吸收特性。结果该处方制备的利福喷丁自乳化胶囊能够迅速溶解并乳化,模拟体内吸收是普通利福喷丁胶囊的36倍。结论自乳化胶囊明显提高利福喷丁的释药速率并促进其体内吸收。

OBJECTIVE To prepare rifapentine self-emulsifying hard capsules and to evaluate its release characteristics of self-emulsifying drug deliver systems. METHODS Using orthogonal design, the rifapentine sell：emulsifying hard capsules formulations were optimized according to in vitro release rate with OP10-Span85 as emulsifier and PEG4000 as co-surfactant. In vitro simulated absorption method was adapted to evaluale rifapentine self-emulsifying hard capsules. RESULTS The optimized self-emulsifying hard capsule formulation was preferable. The absorption was 36 times than that of common rifapentine capsule. CONCLUSION Rifapentine self-emulsifying hard capsules is optimized by orthogonal design. It can increase absorption of drug in practice.