甘草酸和甘草次酸对芍药苷在大鼠体内药动学参数的影响  

Effects of glycyrrhizic acid and glycyrrhetinic acid on in vivo pharmacokinetic parameters of paeoniflorin in rats

作　　者：刘卉[1] 单进军[1,2,3] 康安[1,2,3] 恽菲[1] 陈乐天[1,2,3] 张雯[1] 狄留庆[1,2,3] 

机构地区：[1]南京中医药大学,江苏南京210046 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210046 [3]南京市中药微丸产业化工程技术研究中心,江苏南京210029

出　　处：《中草药》2013年第12期1610-1614,共5页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81273655);江苏高校优势学科建设工程资助项目(ysxk-2010);江苏高校优势学科建设工程资助项目开发课题(2011ZYX3-001;002;0077);江苏省"青蓝工程"中药复方新型给药系统研究科技创新团队支持计划[(2008)30号]

摘　　要：目的研究甘草酸及其代谢产物甘草次酸对芍药中主要活性成分芍药苷在大鼠体内药动学特征的影响,探索芍药与甘草配伍用药的合理性。方法大鼠单独ig给予芍药苷或分别与甘草酸、甘草次酸联合用药,于不同时间点采集血样,LC-MS测定芍药苷血药浓度,建立药物浓度-时间曲线,采用DAS2.1.1软件计算、分析药动学参数。结果甘草酸能减小芍药苷Cmax、tmax,降低芍药苷AUC;甘草次酸能增加芍药苷Cmax、tmax,显著提高芍药苷AUC。结论甘草提高芍药苷生物利用度可能与甘草酸的代谢产物甘草次酸的作用相关。Objective To explore the potential effects of glycyrrhizic acid and its active metabolite glycyrrhetinic acid on the in vivo pharmacokinetic parameters of paeoniflorin in rats,and to investigate the rationality of the compatibility of Paeonia lactiflora and Glycyrrhizae Radix et Rhizome.Methods After the ig administration of paeoniflorin alone or with glycyrrhizic acid and glycyrrhetinic acid respectively,blood samples were collected at different time points and assayed by LC-MS,and the plasma concentration-time profiles of paeoniflorin were established.The pharmacokinetic parameters were calculated and analyzed with DAS2.1.1 software.Results Glycyrrhizic acid could reduce the Cmax,tmax,and AUC of paeoniflorin,while glycyrrhetinic acid could increase the parameters.Conclusion Glycyrrhizae Radix et Rhizome could increase the bioavailability of paeoniflorin through the activity of glycyrrhetinic acid which is the active metabolite of glycyrrhizic acid.

关 键 词：甘草酸 甘草次酸 芍药苷 药动学 生物利用度 

分 类 号：R969.1[医药卫生—药理学]