龙胆苦苷及龙胆提取物在大鼠体内药动学对比研究

Comparative Study on Pharmacokinetics of Gentiopicroside and Gentianae Radix Extract in Rats

目的:研究龙胆苦苷及龙胆提取物在大鼠体内药动学过程的差异,评价龙胆中其他成分对龙胆苦苷药动学的影响。方法:大鼠分别灌胃给予龙胆苦苷及龙胆提取物后,以龙胆苦苷为指标,建立高效液相色谱法测定大鼠血浆中龙胆苦苷的血药浓度,采用DAS 2.1.1药动学软件计算主要药动学参数。结果:大鼠灌胃给予龙胆苦苷及龙胆提取物后,龙胆苦苷的血药浓度-时间曲线符合二室模型,Cmax分别为(16.53±0.37)g/mL和(16.61±0.49)g/mL,Tmax分别为0.25 h和1.5 h,t1/2(α)分别为(0.20±0.04)h和(0.69±0.14)h,t1/2(β)分别为(0.64±0.08)h和(0.80±0.11)h,AUC0～∞分别为(18.20±1.97)g.h/mL和(39.20±1.18)g.h/mL,CL分别为(2.75±0.32)L/(h.kg)和(1.22±0.04)L.(h.kg)。结论:大鼠灌胃给予龙胆苦苷及龙胆提取物后龙胆苦苷的药动学参数存在明显差异。

Objective ：To compare the pharmacokinetics of gentiopicroside and Gentianae Radix extract in rats and assess the effect of other components in Gentianae Radix on the pharmacokinetics of gentiopicroside. Methods ： The rats were oral administrated with gen- tiopicroside and Gentianae Radix extract, the content of gentiopicroside was chosen as index and determined by HPLC. The pharmacoki- etic parameters were calculated with DAS 2.1.1 program. Results ： The concentration-time curve of gentiopicroside and Gentianae Ra-dix extract was described by two compartment model. The main pharmacokinetic parameters of gentiopicroside and Gentianae Radix ex-tract were ： Cmax （ 16.53 ± 0.37） g/mL and （ 16.61 -± 0.49） g/mL, Tmax 0.25 h and 1.5 h,t1/2（α） （0.20 ± 0.04） h and （0.69 ± 0. 14）h,t1/2（β） （0.64 ± 0.08）h and （0.80 ± 0. 11）h,AUC0-∞（18.20 ± 1.97）g · h/mL and （39.20 ±1.18）g · h/mL,CL（2.75 ± 0.32） L/（ h · kg） and （1.22 ± 0.04）L（ h · kg） ,respectively. Conclusion：There are significantly differences in pharmacokinetic pa-rameters between gentiopieroside and Gentianae Radix extract in rats.