【摘要】 目的:探讨CBN中葛根素和人参皂甙Rg1在正常和脑缺血再灌大鼠体内的药代动力学过程。方法:脑缺血再灌组大鼠结扎双侧颈总动脉不完全脑缺血30分钟,复灌同时股静脉注射100mg·Kg-1药物。正常组注射等剂量药物。HPLC法测定给药后不同时间点血浆样品中葛根素和人参皂甙Rg1的含量,并作动力学计算。结果:CBN中葛根素在正常大鼠体内为一室模型,半衰期是17.8min;在脑缺血再灌大鼠体内为二室模型,分布和消除半衰期分别是8.0min和38.4min;药时曲线下面积(AUC,mg·L-1·min),表观分布容积(Vdss·L·kg-1),平均驻留时间(MRTmin)正常组分别为:744,4.18,26.0;脑缺血再灌组分别为:3015,1.39,40.0。人参皂甙Rg1在正常大鼠和脑缺血再灌大鼠体内为二室模型,分布和消除相半衰期分别为8.2,2,700.8min;18.6,4297min。药时曲线下面积(AUC,mg·L-1·min),表观分布容积(Vdss·L·kg-1),平均驻留时间(MRTmin)正常组分别为:531.5,7.05,164.7;脑缺血再灌组分别为:1678,2.39,73.3。结论:静脉注射CBN后,葛根素和人参皂甙Rg1在缺血再灌大鼠体内的消除时间较在正常大鼠体内延长。更多还原

【Abstract】 Object:To explore the pharmacokinetics of puerarin(Pur)and ginsenoside Rg1in normal rats and cerebral ischemia-reperfusion ratas,which are the two active components in Natural Cerebral Nutrition(CBN)-a new Chinese herbal drug injection.Method:In cerebral ischemia-reperfusion model,the rats were operated by occulation of bilateral carotids for 30min and reperfusion,immediately i.v.100mg ·kg -1 CBN,before plasma samples are collected at different time.The normal group rats were sampled after administration of equivalent dose CBN.The concentration of Pur and Rg1are determined by HPLC-UV.Result:The pharmacokinetic process of Pur in normal group is described as one-compartment model,its half life time is17.8min;in cerebral ischemia-reperfusion group as two-compart-ment model,its distributio n and excretion half life time are seperately8.0min and38.4min.Other parameters of Pur such as AUC(mg ·L -1 ·min),V dss (L·kg -1 ),MRT(min)are744,4.18,26.0in normal group and3015,1.39,40.0in pathological group.The pharmacokinetic pro-cess of Rg1is described as two-compartment model in normal and pathological group.its dis-tribution and excretion half life times are individually8.2,700.8min in normal group and18.6,4297min in pathological group.Other parameters of Rg1such as AUC(mg ·L -1 ·min),V dss (L·kg -1 ),MRT(min)are531.5,7.05,164.7in normal group and1678,2.39,73.3in pathological group.Conclusion:there are different disposition process of Pur and Rg1between normal rats and cerebral ischemia reperfusion rats,which indicates that patients ’ condition should be con-sidered in clinic application.更多还原