三七皂苷中R1、Rg1在正常和脑缺血再灌大鼠中的动力学变化

Pharmacokinetics of notoginsenoside R1?Rg1 in panax notoginseng sponins (PNS) in normal and cerebral ischemia-reperfusion rats

目的 :研究三七皂苷中R1、Rg1在正常和脑缺血再灌状态下大鼠体内的药代动力学变化。方法 :正常组大鼠股静脉注射三七皂苷 (5 0mg/kg) ,缺血再灌组大鼠阻断双侧颈总动脉造成不完全脑缺血 3 0min、复灌同时股静脉注射等量药物。采用反相HPLC法测定iv后不同时间点大鼠血浆中R1、Rg1浓度 ,计算其动力学参数。结果 :在正常和脑缺血再灌状态下 ,R1、Rg1动力学呈一室开放模型。正常状态下 ,R1和Rg1的t1/ 2 、AUC0～∞ 、CL(s)、Vd分别为 2 1 6± 7 9和 2 0 8± 3 7min、418 7± 85 9和 1 2 0±0 18mg/kg ;脑缺血再灌状态下 ,R1和Rg1的t1/ 2 、AUC0～∞ 、CL(s)、Vd分别为 19 2± 5 0和 2 0 0± 5 2min、416 7± 5 8 9和 13 68 0± 186 3 μg/ml·min、0 13 90± 0 0 413和 0 0 3 80± 0 0 0 60mg/kg·min、3 3 1± 0 5 4和 1 0 4± 0 15mg/kg。 结论 :在正常和脑缺血再灌状态下 ,R1、Rg1各自的动力学参数没有明显差异。R1。

To study the pharmacokinetic of notoginsenoside R1 and Rg1 in PNS in normal and cerebral ischemia reperfusion rats. Methods: The normal rats were injected PNS (50mg/kg) before plasma samples are collected at different time. The cerebral ischemia reperfusion rats were operated by occulation of bilateral carotids for 30min and reperfusion, immediately injecting PNS (50mg/kg) by femur vein. The concentration of R1 and Rg1 are determined by RP HPLC UV. The parameters were estimated by the compartment model with a statistic analysis of 3p87. Results: The pharmacokinetic course of R1 and Rg1 was fitted to a one compartment open model. In normal rats, t 1/2 ?AUC 0～∞ ?CL(s)?Vd of R1 and Rg1 were as follow: (21.6±7.9) and (20.8±3.7) min?(418.7±85.9) and (1258.3±197.7)μg/ml·min?(0.1228±0.0207) and (0.0406±0.0069)mg/kg·min?(3.64±0.64) and (1.20±0.18)mg/kg; in ischemia repurfusion rats, t 1/2 ?AUC 0～∞ ?CL(s)?Vd of R1 and Rg1 were as follow: (19.2±5.0) and (20.0±5.2)min?(415.7±58.9) and (1368.0±186.3) μg/ml.min?(0.1390±0.0413) and (0.0380±0.0060) mg/kg.min?(3.31±0.54) and (1.04±0.15)mg/kg. Conclusion: The difference of pharmacokinetic paraments of R1 and Rg1 between normal and cerebral ischemia reperfusion rats were not significant. The pharmacokinetic course between R1 and Rg1 is similarity.