芍药苷对甘草酸及甘草次酸大鼠体内药动学的影响

 目的 研究芍药苷对甘草酸及其活性代谢产物甘草次酸吸收动力学的影响。方法 将大鼠单独或与芍药苷联合灌胃给予甘草酸后，不同时间点采集血样，建立药物浓度-时间曲线，药动学参数采用Topfit 2.0软件计算分析。结果 与单独给药相比，联合给药后甘草酸达峰浓度 (ρ_max) 与AUC分别降低至单独给药的9%和33%，达峰时间 (t_max) 显著延长，清除率(CL)增加，分布更为广泛；甘草次酸仅出现半衰期 (t_1/2) 显著延长，而其他药动学参数无明显变化。结论 芍药苷对甘草酸的吸收速度和程度均有显著性抑制，对甘草次酸吸收动力学影响较小。

Effect of Paeoniflorin on the Pharmacokinetics of Glycyrrhizic Acid and Glycyrrhetinic Acid in Rats

OBJECTIVE To explore the effect of paeoniflorin on the pharmacokinetics of glycyrrhizic acid and its active metabolite glycyrrhetinic acid after oral administration.METHODS After the administration of glycyrrhizic acid alone or with paeoniflorin,blood samples were collected,and the plasma concentration-time profiles of glycyrrhizic acid and glycyrrhetinic acid were established.Pharmacokinetic parameters were calculated and analyzed with Topfit 2.0 software.RESULTS When glycyrrhizic acid was co-administered with paeoniflorin,the ρmax and AUC of glycyrrhizic acid decreased to 9% and 33% of those of glycyrrhizic acid administered alone,respectively;the tmax prolonged markedly,CL increased,and Vd became larger.For glycyrrhetinic acid,only the t1/2 prolonged significantly while other PK parameters had little change.CONCLUSION Paeoniflorin dramatically inhibits the absorption rate and extent of glycyrrhizic acid in rats when simultaneously orally administered,but has only small effect on the absorption of glycyrrhetinic acid.