芍药甘草汤中6种活性成分在正常、胃溃疡大鼠体内药动学比较  

Comparison of in vivo pharmacokinetics of six active constituents from Shaoyao Gancao Decoction in normal and gastric ulcer rats

作　　者：李和蓉 金阳 张环 伍天苔 温健 唐超 程雪怡 刘文 LI He-rong;JIN Yang;ZHANG Huan;WU Tian-tai;WEN Jian;TANG Chao;CHENG Xue-yi;LIU Wen(College of Pharmacy,Guizhou Medical University,Guiyang 550025,China;Guizhou Provincial Key Laboratory for Pharmaceutics/State Key Laboratory for Efficacy and Utilization of Medicinal Plants Co-founded by Guizhou Province and MOST,Guizhou Medical University,Guiyang 550004,China)

机构地区：[1]贵州医科大学药学院,贵州贵阳550025 [2]贵州医科大学,贵州省药物制剂重点实验室/省部共建药用植物功效与利用国家重点实验室,贵州贵阳550004

出　　处：《中成药》2024年第11期3572-3578,共7页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金资助项目(82060704);贵州医科大学附属医院国家自然科学基金面上基金培育计划(gyfynsfc-2021-5)。

摘　　要：目的比较芍药甘草汤中芍药苷、芍药内酯苷、甘草苷、异甘草苷、甘草素和甘草酸在正常、胃溃疡大鼠体内药动学。方法6只大鼠随机分为2组,建立75%乙醇诱导胃溃疡模型,取胃组织。12只大鼠随机分为2组,灌胃给药(9.9 g/kg),于不同时间点取血,UPLC-MS/MS法测定血药浓度,计算药动学参数。结果与正常组比较,模型组各活性成分T_(max)延长(P<0.05,P<0.01);芍药苷T_(1/2)、MRT_(0~t)延长(P<0.05,P<0.01),C_(max)、AUC升高(P<0.05,P<0.01),Vd/F、CL/F降低(P<0.05,P<0.01);芍药内酯苷C_(max)、AUC升高(P<0.05,P<0.01),CL/F降低(P<0.05);甘草苷MRT延长(P<0.05),AUC升高(P<0.05),CL/F降低(P<0.01);异甘草苷MRT延长(P<0.05,P<0.01),Vd/F降低(P<0.05);甘草素药动学参数(除T_(max)外)无明显变化(P>0.05);甘草酸T_(1/2)、MRT_(0~∞)延长(P<0.05,P<0.01),C_(max)、AUC升高(P<0.05,P<0.01),CL/F降低(P<0.01)。结论胃溃疡对芍药甘草汤中活性成分体内吸收、代谢的速度和程度有一定影响。AIM To compare the in vivo pharmacokinetics of paeoniflorin,paeoniflorin,liquiritin,isoliquiritin,liquiritigenin and glycyrrhizic acid from Shaoyao Gancao Decoction in normal and gastric ulcer rats.METHODS Six rats were randomly assigned into two groups,after which the 75%ethanol-induced gastric ulcer model was established,the gastric tissues were collected.Twelve rats were randomly assigned into two groups and given intragastric administration(9.9 g/kg),after which blood collection was made at different time points,UPLC-MS/MS method was adopted in the determination of plasma concentrations,and main pharmacokinetic parameters were calculated.RESULTS Prolonged T max(P<0.05,P<0.01)of various active constituents,prolonged T_(1/2),MRT_(0-t)(P<0.05,P<0.01),increased C_(max),AUC(P<0.05,P<0.01)and decreased Vd/F,CL/F(P<0.05,P<0.01)of paeoniflorin,increased C_(max),AUC(P<0.05,P<0.01)and decreased CL/F(P<0.05)of albiflorin,prolonged MRT(P<0.05),increased AUC(P<0.05)and decreased CL/F(P<0.01)of liquiritin,prolonged MRT(P<0.05,P<0.01)and decreased Vd/F(P<0.05)of isoliquiritin,no obviously changed pharmacokinetic parameters(except for T_(max))of liquiritigenin(P>0.05),and prolonged T_(1/2),MRT_(0-∞)(P<0.05,P<0.01),increased C_(max),AUC(P<0.05,P<0.01)and decreased CL/F(P<0.01)of glycyrrhizic acid were observable in the model group as compared with those in the normal group.CONCLUSION Gastric ulcer exhibits certain influences on the velocities and degrees of in vivo absorption and metabolism of active constituents from Shaoyao Gancao Decoction.

关 键 词：芍药甘草汤 活性成分 胃溃疡 体内药动学 UPLC-MS/MS 

分 类 号：R969.1[医药卫生—药理学]