黄芩苷在家兔感染性脑水肿模型中的药代动力学研究

 目的：研究黄芩苷在家兔获得脑水肿前后，体内药代动力学参数的变化。方法：18只家兔随机分为两组，一组感染百日咳菌液获得脑水肿模型，另一组为正常对照组，静脉注射60mg/kg黄芩甙，于注射后不同时间内抽取血样，采用高效液相色谱法测定，黄芩甙血药浓度测定值用3P87程序包进行拟合。结果：静脉注射黄芩甙后，在家兔体内代谢符合二室开放模型。对照组与脑水肿模型组的主要药动力学参数：t_1/2α分别为0.1196h和0.2158h；t_1/2β分别为2.381h和2.562h；V_d分别为1.006L·kg^-1和1.414L·kg^-1；CL分别为1.843L·h^-1·kg^-1和1.877L·h^-1·kg^-1。结论：用黄芩苷治疗脑水肿时，要考虑其药代动力学参数的变化。

Pharmacokinetic study of baicalin in rabbits with inflammatory brain edema

OBJECTIVE:To study the varity of pharmacokinetic parameters of baicalin in normal rabbits and in rabbits with inflammatory brain edema and to evaluate its clinical use for the treatment of brain edema.METHOD:18 rabbits were randomizedly divided into two groups PB brain edema group and control.After injecting 60 mg.kg－1 baicalin,serum samples were collected at 0,0.25，0.5，1，2，4，6，8h.A high performance liquid chromatography method was used to determine the serum concentrations. The data obtained were fitted with 3P87 pharmacokinetic program.RESULTS:The result showed that the disposition of baicalin in rabbits was conformed to a two-compartment model.The main pharmacokinetic parameters of control group and brain edema group were t1／2α　0.1196h and 0.2158h，t1／2β 2.381h and 2.562 h，Vd 1.006L.kg－1and 1.414L.kg－1，CL 1.843 L.h－1.kg－1and1.877L.h－1.kg－1，respectively. CONCLUSION：The pharmacokinetic parameters of baicaclin in rabbits with brain edema were different from control group. It has longer t1／2α and higher apparent volume of distribution.