水飞蓟宾脂肪乳在大鼠体内的药物代谢动力学及组织分布

Pharmacokinetics and Tissue Distribution of Silybin Lipid Emulsion in Rats

目的:研究水飞蓟宾脂肪乳在大鼠体内的药物代谢动力学及组织分布。方法:采用水飞蓟宾注射液为对照,3P97药物代谢动力学软件拟合药物代谢动力学模型并计算药物代谢动力学参数,采用相对摄取率(Re)、总靶向系数(Te)、药物分布效率(Rte)评价飞蓟宾脂肪乳在大鼠体内的组织分布及靶向性。结果:水飞蓟宾脂肪乳在大鼠体内分布符合二室模型,其主要药动学参数为:t_(1/2α)=(0.623 7±0.097 8)h,t_(1/2β)=(19.751 3±2.137 2)h,CL=(0.002 4±0.000 9)m L/(kg·h),AUC_(0→∞)=(239.011 7±15.261 3)mg/(h·L)。肝脏和脾脏中的Re分别为2.417和2.042,Rte分别为2.241和1.890。结论:与水飞蓟宾注射液相比,水飞蓟宾脂肪乳能提高对肝脏、脾脏的趋向性,有利于提高其疗效。

Objective： To study the pharmacokinetics and tissue distribution of silybin lipid emulsion in rats. Methods： With silybin injection as reference,pharmacokinetic model and parameters were calculated by 3P97. In vivo tissue distribution and targeting of silybin lipid emulsion in rats were evaluated by Te, Re, Rte. Results： Pharmacokinetic data fitted a two-compartment model, main pharmacokinetic parameters of silybin lipid emulsion were as follows： t_（1 / 2α）=（ 0. 623,7 ± 0. 097,8） h,t_（1 / 2β）=（ 19. 751,3 ± 2. 137,2） h,CL =（ 0.002,4±0.000,9） m L /（ kg·h）,AUC_（0→∞）=（ 239.011,7±15.261,3） mg /（ h·L）. Re in liver,spleen were 2.417,2.042,Rte in liver,spleen were 2.241,1.890. Conclusion： Compared to silybin injection,silybin lipid emulsion could improve tendency for liver and spleen,and help improving its therapeutic effect.