【摘要】 目的:研究京尼平苷及其肠道代谢物京尼平在大鼠体内的药代动力学过程。方法:灌胃给予280 mg.kg-1的京尼平苷,RP-HPLC测定血浆中京尼平苷及京尼平,应用BAPP统计模拟计算,得出相应的药代动力学参数。结果:主要药动学参数为:京尼平苷和京尼平最大血药浓度(Cm ax)分别为(3.23±0.37)μg.mL-1,(17.41±5.27)ng.mL-1;半衰期(t1/2)分别为(1.00±0.35)h,(4.86±2.55)h;平均滞留时间(MRT)分别为(2.39±0.18)h,(7.86±3.61)h;曲线下面积(AUC i)(11.23±2.18)h.μg.mL-1,(90.60±13.44)h.ng.mL-1。结论:二者药代动力学均符合一室模型,京尼平苷在血浆中代谢消除较快,t1/2为(1.00±0.35)h;京尼平血浆浓度较低,Cm ax为(17.41±5.27)ng.mL-1。更多还原

【Abstract】 Objective: To study the pharmacokinetics of geniposide and its metabolite in rats.Method: RP-HPLC was applied to determine the concentration of geniposide and its metabolite in rat plasma after oral administration in dosage of 280 mg·kg^-1,bw;BAPP was apllied to modulate the pharmacokinetics parameters.Result: The main parameters were described as follows: C_max（3.23±0.37） μg·mL^-1,t_1/2（1.00±0.35） h,MRT（2.39±0.18） h,AUCi（11.23±2.18） h·μg·mL^-1for geniposide.C_max（（17.41±5.27）） ng·mL^-1,t_1/2（4.86±2.55） h,MRT（7.86±3.61） h,AUCi（90.60±13.44） h·ng·mL^-1 for genipin.Conclusion: The concentration-time cures were modulated by one-compartment model.The geniposide was metabolized in plasma and eliminated rapidly,t_1/2（1.00±0.35） h.The genipin concentration in plasma indicated very low,C_max（17.41±5.27） ng·mL^-1.更多还原