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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 oil in rats. Methods: The silybin injection was used as a control. The pharmacokinetic software of 3P97 was used to fit the pharmacokinetic model and to calculate the pharmacokinetic parameters. The relative uptake (Re), total target (Te), drug Distribution efficiency (Rte) Evaluation of silybin fat emulsion in rats tissue distribution and targeting. Results: The silybin emulsion distributed in rats according to the two-compartment model. The main pharmacokinetic parameters 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 and spleen was 2.417 and 2.042, respectively, and Rte was 2.241 and 1.890 respectively. Conclusion: Compared with silybin injection, silybin fat emulsion can increase the tendency of the liver and spleen, which is beneficial to improve the curative effect.