普罗布考混合胶束的制备及其大鼠体内药动学研究  

Preparation of Probucol Loaded Mixed Micelles and Its Pharmacokinetic Behavior In Rats

作　　者：蒋世军[1,2] 刘秀洁[1] 黄健[2] 高芳[2] 顾王文[2] 崔景斌[1] 

机构地区：[1]华东理工大学药学院,上海200237 [2]中国科学院上海药物研究所,上海201203

出　　处：《中国现代应用药学》2012年第1期46-49,共4页Chinese Journal of Modern Applied Pharmacy

基　　金：国家重点基础研究发展计划(2009CB930304)

摘　　要：目的制备普罗布考混合胶束(Probucol loaded mixed micelles,PMM)用于提高其口服生物利用度。方法选择磷脂、脱氧胆酸钠为辅料,以共沉淀法制备普罗布考混合胶束(PMM),并对其体外理化特性以及体内药动学行为进行评价。结果制备了普罗布考混合胶束,其优化处方组成为磷脂︰脱氧胆酸钠︰普罗布考(3︰4︰1)。PMM平均粒径为82.28 nm,多分散系数为0.179,药物主要以非晶型状态存在于PMM中。大鼠体内药动学研究表明,与原料药相比,口服PMM后,普罗布考的峰浓度和口服生物利用度分别提高了2.28倍和4.43倍。结论混合胶束能够显著提高普罗布考的口服生物利用度,为解决难溶性药物的口服吸收问题提供了一种有效策略。OBJECTIVE Development of probucol loaded mixed micelles （PMM） for enhancing its oral bioavailability. METHODS PMM was prepared with soybean phosphatidylcholine （EPC） and sodium deoxycholate （SD） by a co-precipitation method. The in vitro properties and in vivo pharmacokinetic behavior of PMM was evaluated. RESULTS The formulation of PMM was optimized as EPC ： SD ： probucol （3 ： 4 ： 1）. PMM was self-assembled with average diameter of 82.28 nm and polydispersity index of 0.179. Probucol may exhibit as amorphous state in PMM. The in vivo pharmacokinetical results indicated that the peak concentration （Cmax） and area under concentration-time curve （AUC） was significantly improved by 2.28-fold and 4.43-fold, respectively. CONCLUSION The oral bioavailability of probucol was significantly improved by PMM, which could be potential for enhancing the oral absorption of insoluble drugs.

关 键 词：普罗布考 混合胶束 差示扫描量热法 X-射线衍射技术 生物利用度 

分 类 号：R943.43[医药卫生—药剂学] R969.1[医药卫生—药学]