自微乳化系统提高广藿香醇大鼠口服生物利用度  

Self-microemulsifying drug delivery system of patchoulic alcohol to improve oral bioavailability in rats

作　　者：游秀华[1] 王荣昌[1] 汤文星[1] 李莹[1] 何志坚[1] 胡海燕[1] 吴传斌[1] 

机构地区：[1]中山大学药学院中山大学药物制剂工程研究开发中心,广东广州510006

出　　处：《中国中药杂志》2010年第6期694-698,共5页China Journal of Chinese Materia Medica

基　　金：广东省中医局建设中医药强省科研课题(2007096)

摘　　要：目的:通过将广藿香醇制备成自微乳化制剂,以提高其口服生物利用度。方法:从广藿香油中精制广藿香醇,以粒径和乳化时间为指标,采用伪三相图、星点设计-效应面优化法筛选和优化广藿香醇和广藿香油自微乳处方,测定广藿香醇和广藿香油自微乳化制剂、广藿香醇的大鼠体内的药代动力学参数。结果:自微乳系统的优化组成为聚氧乙烯蓖麻油-聚氧乙烯脱水山梨醇单油酸酯-紫乙二醇400-肉豆蔻酸异丙酯-广藿香醇(2∶2∶0.8∶1.95∶0.65),其中自微乳对广藿香醇的载药量为8%。在水中稀释100倍后平均粒径为30.1 nm,乳化时间为142 s。在大鼠体内药动学研究发现广藿香醇自微乳制剂、广藿香油自微乳制剂、广藿香醇的Tmax无明显差距,都在60 min左右;而2种自微乳化制剂的AUC(2 001 745.6±329 663.6),(1 594 005.6±280 150.3)μg.min.L-1明显高于广藿香醇的(1 163 153.3±232 324.3)μg.min.L-1。结论:自微乳化系统能有效提高广藿香醇大鼠口服生物利用度。Objective： To improve the oral bioavailability of patchoulic alcohol in rats by using self-microemulsifying drug delivery systems （SMEDDS）. Method： Patchoulic alcohol was separated and purified from patehoulic oil, and the SMEDDSs incluiding patchoulic alcohol or patehoulic oil were optimized by pseudo-ternary phase diagrams via central composite design-response surface methodology. Pharmaeokinetics of both SMEDDSs and patehoulic alcohol itself in rats were investigated. Result： The patehoulic alco- hol SMEDDS （Creraophor EL-Tween 80-PEG 400-isopropyl myristate-patehoulic alcohol, 2： 2： 0. 8： 1.95： 0. 65 ）was considered as the optimized formulation. The mean drop size of the system was 30. 1 nra after diluted 100 folds in water. The average self-mieroeroulsitying time was 142 s. Patehoulie alcohol SMEDDS and patchoulic oil SMEDDS showed no signficant difference in Tmax compared with patchoulic alcohol with around 60 minutes, while the AUCs of both SMEDDSs （2 001 745.6 ± 329 663.6 ） and （1 594 005.6 ± 280 150. 3） μg·min·L^-1 were significantly higher than that of patchoulic alcohol （1 163 153. 3±232 324. 3）μg·min·L^-1. Conclusion： SMEDDS can effectively improve the oral bioavailability of patehoulic alcohot in rats.

关 键 词：广藿香醇 广藿香油 自微乳化 口服生物利用度 

分 类 号：R283[医药卫生—中药学]