黄芩素在小鼠体内的药动学及其组织分布研究

Pharmacokinetics and Tissue Distribution of Baicalein in Mice

建立了HPLC法测定小鼠血浆和组织中的黄芩素,并研究了小鼠静脉注射黄芩素后的药动学及组织分布特征。黄芩素在0.05～50μg/ml浓度范围内线性关系良好,提取回收率74.2%～104.2%,方法回收率88.9%～113.5%,日内、日间RSD均小于15%。静脉注射后,黄芩素在小鼠体内的药-时曲线符合二室模型,主要药动学参数:t_(1/2β)16.42 min,AUC_(0-∞)128.97 mg·min·L^(-1),Cl 0.14 L·min^(-1)·kg^(-1)。组织分布结果表明,黄芩素主要分布在肝脏和肺部组织,其次为心、肾和骨骼肌,脑和脾分布最少。

An HPLC method was established for the determination of baicalein in plasma and tissue of mice. The pharmacokinetics and tissue distribution of baicalein in mice after iv were investigated. The calibration curve was linear in the concentration range of 0.05 - 50μg/ml. The extraction recoveries were 74.2% - 104.2% and the method recoveries were 88.9 % - 113.5 %, with the intra- and inter-day RSDs less than 15 %. The concentration-time curve of baicalein after iv was in accordance with a two-compartment model and the main pharmacokinetic parameters were as follows： t1/2β 16.42 min, AUC0-β 128.97 mg·min·L^-1, Cl 0.14 L·min ·kg^-1. Baicalein was mainly distributed in liver and lung, less in heart, kidney and muscle, and least in brain and spleen.