药理效应法测定穿山龙总皂苷的药动学参数

Determination of Pharmacokinetics Parameters of Total Saponins from Dioscoreae Nipponicae Rhizoma by Pharmacological Effect Method

目的:考察穿山龙总皂苷在大鼠体内的药动学特征。方法:采用尿酸钠诱导的大鼠急性痛风性关节炎模型,以白细胞介素-1β(IL-1β)和肿瘤坏死因子-α(TNF-α)作为测定指标,利用酶联免疫吸附法按试剂盒说明书测定IL-1β和TNF-α含量,采用符合中药整体观思想的药理效应法研究穿山龙总皂苷的药动学。结果:穿山龙总皂苷口服给药后主要药动学参数为药-时曲线下面积(AUC_(0-t))121.84 ng·h·L^(-1),药-时曲线下总面积(AUC_(0-∞))542.56 ng·h·L-1,平均滞留时间(MRT_(0-t))5.92 h,平均总滞留时间(MRT_(0-∞))45.95 h,达峰时间(t_(max))1.96 h,药峰浓度(C_(max))13.21 ng·L^(-1)。结论:穿山龙总皂苷的表观动力学过程符合一室开放模型。

Objective： To investigate pharmacokinetic characteristics of total saponins from Dioscoreae Nipponicae Rhizoma in rats. Method： Rat acute gout arthritis model induced by monosodium urate crystal suspension was used,taking inflammatory levels of interleukin-1β （IL-1β） and tumor necrosis factor-α （TNF-α） as indexes,pharmacological effect method was adopted to estimate pharmacokinetic characteristics of total saponins from Dioscoreae Nipponicae Rhizoma in rats. Result： Main pharmacokinetic parameters were as following：AUC0-t of 121.84 ng·h·L^-1,AUC0-∞ of 542.56 ng·h·L^-1,MRT0-t of 5.92 h,MRT0-∞ of 45.95 h,tmax of 1.96 h,Cmax of 13.21 ng·L^-1. Conclusion： Apparent kinetics of total saponins from Dioscoreae Nipponicae Rhizoma in rats accords with single compartment model.