摘要
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(ρmax)与AUC分别降低至单独给药的9%和33%,达峰时间(tmax)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(t1/2)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。
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.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2012年第8期599-603,共5页
Chinese Pharmaceutical Journal
基金
国家自然科学基金资助项目([2009]30873448)
中央高校基本科研业务费专项资金(DUT11LK28)
关键词
甘草酸
芍药苷
甘草次酸
药动学
glycyrrhizic acid
paeoniflorin
glycyrrhetinic acid
pharmacokinetics
