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11.12 μg/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 b...