黄芩素纳米混悬液的生物利用度研究  

Bioavailability enhancement of baicalein by nanosuspension

作　　者：高缘[1] 江鲲[1] 李莉[2] 席一峰[1] 

机构地区：[1]中国药科大学中药制剂教研室,南京210009 [2]南京医科大学第二附属医院,南京210011

出　　处：《中国药科大学学报》2011年第4期314-318,共5页Journal of China Pharmaceutical University

基　　金：国家"重大新药创制"科技重大专项资助项目(No.2009ZX09310-004);中央高校基本科研业务费专项资金资助(No.JKQ2009028)~~

摘　　要：采用反溶剂重结晶结合高压均质法制备黄芩素纳米混悬液,并对其在大鼠体内的生物利用度进行研究。对大鼠分别灌胃给予等剂量黄芩素原料和黄芩素纳米混悬液,采用HPLC法测定活性代谢产物黄芩苷在大鼠体内的血药浓度,利用DAS 2.0软件计算药代动力学参数。结果表明,灌胃给予等剂量黄芩素原料和黄芩素纳米混悬液(121 mg/kg)后,大鼠血浆中黄芩苷的血药浓度-时间曲线均呈现双峰现象,cmax分别为7.18和11.12μg/mL,tmax分别为1.67和0.92 h,AUC0-24 h分别为71.40和118.63μg.h/mL。以黄芩素原料做参比,黄芩素纳米混悬液经口给药后的相对生物利用度为166.1%。黄芩素纳米混悬液可显著提高黄芩素口服给药的生物利用度。Baicalein nanosuspension was prepared by antisolvent recrystalization method combined with subse-quent homogenization.The oral bioavailability of baicalein nanosuspension in rats was also studied.The concen-tration of baicalin in rat plasma was determined by HPLC method.The pharmacokinetic parameters were calculat-ed by DAS 2.0 software.It was found that the plasma drug concentration-time curves of baicalein all showed two peaks after oral administration.The cmax,tmaxand AUC0-24 h of the raw baicalein and baicalein nanosuspension was 7.18 and 11.12 μg/mL,1.67 and 0.92 h,71.40 and 118.63 μg.h/mL,respectively.Compared with baicalein bulk,the relative bioavailability of baicalein nanosuspension was 166.1%.Nanosuspension could significantly enhance the oral bioavailability of baicalein in rats.

关 键 词：黄芩素 黄芩苷 纳米混悬液 生物利用度 药代动力学 

分 类 号：R285[医药卫生—中药学]