Preparation of sorafenib self-microemulsifying drug delivery system and its relative bioavailability in rats  

作　　者：Ya-Ou Liu Jie-Ming Fan Xue-Qing Wang Qiang Zhang 

机构地区：[1]Department of Pharmacy, the First Hospital of Peking University, Beijing 100034, China [2]Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University Health Center, Beijing 100191, China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2011年第2期164-170,共7页中国药学（英文版）

基　　金：Foundation items： The 973 Project （Grant No. 2009CB930300）, Scientific and Technological Major Special Project - ＂Significant Creation of New Drugs＂ （Grant No. 2009ZX09310-001）.

摘　　要：Sorafenib is a novel antitumor drug, which is poorly absorbed in the gastrointestinal tract due to its low solubility in water. To improve the bioavailability of sorafenib, a self-microemulsifying drug delivery system （SMEDDS） formulation of sorafenib was prepared and its relative bioavailability in rats was evaluated. The blank SMEDDS was prepared from a mixture of ethyl oleate （oil phase, 20%, w/w）, Cremophol EL （surfactant, 48%, w/w）, PEG-400 （co-surfactant, 16%, w/w） and ethanol （co-surfactant, 16%, w/w）. Sorafenib was subsequently dissolved in the blank SMEDDS to obtain a somfenib SMEDDS formulation with a final sorafenib concentration at 20 mg/mL. The particle size of the emulsified sorafenib SMEDDS was about 20-25 nm. Compared with sorafenib suspension, the prepared SMEDDS formulation exhibited no effect on the Tmax, but significantly increased the AUC, Cmax and MRT and decreased the drug clearance. Most importantly, the oral bioavailability based on AUC0-72h increased about 25 times after formulating sorafenib in SMEDDS. We concluded that SMEDDS could be a promising vesicle for the oral delivery of the poorly soluble antitumor drug sorafenib.

关 键 词：SORAFENIB SMEDDS Relative bioavailability 

分 类 号：R969.1[医药卫生—药理学]