黄芩素自微乳的制备及大鼠体内生物利用度研究  

Preparation of baicalein self-microemulsifying drug delivery systems and oral bioavailability in rat

作　　者：柯学[1,2] 严菲[3] 胡一桥[2] 

机构地区：[1]中国药科大学药剂教研室,南京210009 [2]南京大学生命科学学院,南京210093 [3]江苏省食品药品检验所,南京210008

出　　处：《中国新药杂志》2010年第5期371-376,395,共7页Chinese Journal of New Drugs

基　　金：重大新药创制科技重大专项(2009ZX09310-004)

摘　　要：目的:制备黄芩素自微乳化制剂(SMEDDS),考察其大鼠体内生物利用度。方法:采用伪三元相图法筛选自微乳的油相、表面活性剂及助表面活性剂;采用HPLC法测定大鼠血浆中药物浓度,与原料比较,对黄芩素自微乳进行大鼠体内生物利用度评价。结果:通过使用混合油相、混合表面活性剂及助表面活性剂,可获得较为理想的黄芩素自微乳。大鼠体内血药浓度-时间曲线结果表明,黄芩素自微乳的AUC是原料的3.77倍,且药时曲线的形状发生一定的改变。结论:自微乳系统可显著增加黄芩素的溶解度,有利于提高口服生物利用度,且自微乳可能改变其胃肠道吸收行为。Objective： To prepare baicalein self-microemulsifying drug delivery systems （SMEDDS） and study its oral bioavailability in rat. Methods：The pseudo-ternary phase diagrams were constructed to evaluate the effect of different oils, surfactants and cosurfactants. The baicalein concentration in rat plasma was determined by a HPLC method. , The oral bioavailability of SMEDDS in rats was studied compared with the pure baiealein. Results ： A good SMEDDS of baicalein was obtained by using composite oils, composite surfactants and cosurfacant. Compared with pure baicalein, the relative bioavailability of SMEDDS was 377%. The curve of plasma concentration versus time was changed. Conclusion： The SMEDDS resulted in a significant increase of the solubility of baicalein, which is advantageous for the oral bioavailability. The absorption behavior of baicalein from intestine may be modified by SMEDDS.

关 键 词：黄芩素 自微乳 生物利用度 

分 类 号：R943.4[医药卫生—药剂学]