汉黄芩素白蛋白微球在大鼠体内的药代动力学及组织分布

目的:研究汉黄芩素白蛋白微球在大鼠体内的药动学及组织分布情况.方法:以汉黄芩素溶液为参比,用3P97软件计算大鼠尾静脉给予汉黄芩素白蛋白微球后,其在大鼠体内的药动学模型及药动学参数,用靶向效率评价其在大鼠体内的组织分布及靶向性.结果:汉黄芩素白蛋白微球在大鼠体内的药动学模型符合二室模型,主要药动学参数t1/2α=(0.550 0±0.128 2)h,t1/2β=(14.776 1±1.578 2)h,CL=(0.005 96±0.001 4) mL·h·kg-1,AUC0→∞＝(126.331 7±9.501 2) ng·h·L-1.其在肝脏,脾脏,心脏,肺脏及肾脏的靶向效率分别为2.21,2.02,0.58,0.64,0.26.结论:与汉黄芩素溶液相比,汉黄芩素白蛋白微球能提高对肝脏,脾脏的趋向性,有利于提高其治疗作用.

In vivo Pharmacokinetics and Tissue Distribution of Wogonin Albumin Microspheres in Rats

Objective:To study on in vivo pharmacokinetics and tissue distribution of wogonin albumin microspheres in rats.Method: The concentration of wogonin in plasma of rats was determined by HPLC and pharmacokinetics parameters after tail intravenous administration were calculated by software program 3P97 with wogonin solution as reference.Targeting efficiency(Te) was used to evaluate in vivo tissue distribution and targeting of wogonin albumin microspheres in rats.Result: Pharmacokinetic model of wogonin albumin microspheres in rats was in line with a two-compartment model,and main pharmacokinetic parameters were as follows: t1/2α=(0.550 0±0.128 2) h,t1/2β=(14.776 1±1.578 2) h,CL=(0.005 96±0.001 4) mL·h·kg-1,AUC0→∞=(126.3317±9.5012) mg·h·L-1.Compared with wogonin solution,Te in live,spleen,heart,hung and kidney were 2.21,2.02,0.581,0.64,0.26,respectively.Conclusion: Compared with wogonin solution,wogonin albumin microspheres could improve tendency in liver and spleen,and it could enhance therapeutic effect of wogonin albumin microspheres in rats.