18β-甘草酸对格列美脲在大鼠体内药动学的影响  

Effect of 18β-glycyrrhizin on pharmacokinetics of glimepiride in rats

作　　者：韩刚[1] 王成强[1] 范颖[1] 王彦雪[1] 康欣[1] 喇万英[1] 

机构地区：[1]华北煤炭医学院药学系,河北唐山063000

出　　处：《中国新药与临床杂志》2010年第7期528-531,共4页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：目的研究18β-甘草酸对格列美脲在大鼠体内药动学过程的影响,为格列美脲与甘草酸联合用药提供参考。方法 Wistar大鼠随机分为2组,对照组灌服格列美脲4 mg·kg^(-1)·d^(-1),实验组同时灌服格列美脲4 mg·kg^(-1)·d^(-1)和甘草酸150 mg·kg^(-1)·^(-1),给药后眼底静脉丛取血,高效液相色谱法测定血浆中格列美脲浓度,数据经3P97处理。结果格列美脲在0.1～5.0 mg·L^(-1)范围内线性良好。大鼠单独给予格列美脲及甘草酸与格列美脲合用时,格列美脲在大鼠体内的药动学过程均符合一房室模型。甘草酸与格列美脲合用后,格列美脲的ρ_(max)、AUC、t_(1/2)、t_(max)值较单独给予格列美脲时显著增加(P<0.05)。结论 18β-甘草酸与格列美脲合用时,甘草酸对格列美脲的消除产生抑制作用,引起格列美脲的血药浓度升高。AIM To study the effect of 18β-glycyrrhizin on pharmacokinetic of glimepiride in rats. METHODS Wistar rats were divided into two groups randomly. Rats in control group were administrated with glimepiride 4 mg·kg^-1·d^-1, and rats in experimental group were administrated with glimepiride 4 mg·kg^-1·d^-1 combined with 18β-glycyrrhizin 150 mg·kg^-1·d^-1 simultaneously. The concentration of glimepiride in rat plasma was determined by HPLC method and the main pharmacokinetic parameters were calculated with 3P97 program. RESULTS The calibration curve was linear over the range of 0.1 - 5.0 mg·L^-1. The plasma concentration-time curve of both groups was fit to one-compartment model. Compared with the control group, the main pharmacokinetic parameters of the experimental group, ρmax AUC, t1/2 and tmax were increased significantly （P 〈 0.05）. CONCLUSION 18β-glycyrrhizin may inhibit the elimination of glimepiride. The plasma concentration of glimepiride will increase when combined with 18β-glyeyrrhizin.

关 键 词：药动学 色谱法 高压液相 甘草酸 格列美脲 

分 类 号：R969.1[医药卫生—药理学]