京尼平苷及其代谢物在大鼠体内的药代动力学研究Ⅰ

Pharmacokinetics of geniposide and its metabolite in rats Ⅰ

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。

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： Cmax （ 3.23 ± 0.37） mg·mL^-1, t1/2（1.00±0.35） h, MRT （2.39±0.18） h, AUCi （11.23±2.18） h·μg· mL^-1forgeniposide. Cmax （17.41 ±5.27） ng·mL^-1, t1/2（4.86±2.55） h, MRT （7.86±3.61） h, AUCi （90.60±13.44） h·ng·mL^-1 forgenipin. Conclusion： The concentration-time cures were modulated by one-compartment model. The geniposide was metabolized in plasma and eliminated rapidly, t1/2 （ 1.00 ± 0. 35 ） h. The genipin concentration in plasma indicated very low, Cmax （ 17.41 ± 5.27） ng·mL^- 1.