药理效应法测定黄芩苷及清热合剂的药动学参数

To determine pharmacokinetics parameters of baicalin and QRHJ by pharmacology effect method

目的药理效应法测定黄芩苷及清热合剂的药动学参数。方法采用小鼠热板致痛模型,以镇痛效应为指标,测定黄芩苷及清热合剂的药物动力学参数。结果黄芩苷及清热合剂口服给药后体存药量的表观动力学过程符合一室开放模型,主要药物动力学参数黄芩苷为:Ke=0.131 h-1,Ka=0.428 h-1,t1/2=5.299 h,Tmax=4.000 h,Cmax=509.900 mg.kg-1,AUC=65.196 mg.h.kg-1,CL/F=5.802(mg.kg-1)/[h.(mg.kg-1)-1];清热合剂为:Ke=0.103 h-1,Ka=0.505 h-1,t1/2=6.725 h,Tmax=6.000 h,Cmax=7.000 mg.kg-1,AUC=39 075.500 mg.h.kg-1,CL/F=0.158(mg.kg-1)/[h.(mg.kg-1)-1]。结论清热合剂及黄芩苷体存量的表观动力学过程均符合一室开放模型,中药复方清热合剂的达峰时间明显慢于单方黄芩苷。

Objective To determine pharmacokinetics parameters of baicalin and QRHJ with pharmacodynamics effect. Methods Pain model induced with hot plate in mice was used, and lapping hindfoot time was taken as index to estimate main pharmacokinetics parameters of Baicalin and QRHJ. Results After baicalin and QRHJ po. in mice, apparent dynamics fit one-compartment open model, the main pharmacokinetics parameters of baicalin were： Ke=0.131h^-1,Ka=0.428h^-1,t1/2=5.299h,Tmax=4.000h,Cmax=509.900mg·kg^-1,AUC=65.196mg·h·kg^-1.CL/F=5.802（mg·kg^-1）/[h·（mg·kg^-1）^-1]; and QRHJ were： Ke=0.103h^-1,Ka=0.505h^-1,t1/2=6.725h,Tmax=6.000h,Cmax=7.000mg·kg^-1,AUC=39075.500mg·h·kg^-1,CL/F=0.158（mg·kg^-1）/[h·（mg·kg^-1）^-1]. Conclusion Apparent dynamics of baicalin and QRHJ both fit one-compartment open model, Tmax of QRHJ was much longer than Tmax of baicalin.