三越麻黄颗粒小鼠药物动力学研究

Pharmacokinetic analysis of Sanyuemahuang Granule in rats

目的:对三越麻黄颗粒的体内药动学进行研究。方法:在药效学实验的基础上以制剂对小鼠腹腔毛细血管通透性的影响为指标,采用药理效应法考察了该颗粒剂在体内的药动学指标。结果:三越麻黄颗粒体内的药动学指标符合一室模型,采用药理效应法计算后得到以下药动学参数:体存相当药量的吸收速度常数(Ka)为1.06h-1,达峰时(Tmax)为1.57 h,t1/2(Ka)为0.656 h,消除速度常数(ke)为0.628 h-1,t1/2(Ke)为1.10 h;采用效应半衰期法计算得到以下药动学参数:消除速度常数(ke)为0.537 h-1,t1/2(Ke)为1.29 h;根据效应—时间曲线得到以下效应动力学参数:药物效应起效速度常数(Ka)为2.149 h-1,达峰时(Tmax)为1.36 h,t1/2(Ka)为0.32 h,消除速度常数(ke)为0.139 h-1,t1/2(Ke)为5.0 h。结论:三越麻黄颗粒剂起效较快而消除较慢,体存相当药量的药动学参数仅为表观参数,需结合药效的变化来讨论其具体的意义。

AIM： To analysis the pharmacokinetic process of Sanyuemahuang Granule（Herba Ephedrae,Gypsum fibrosum,Semen Armeniacae amarum,Radix Isatidis,Rhizome et Radix Glycyrrhizae,Pericarpium Citri reticulatae,Radix Bupleuri,Rhizoma Belamcandae,Herba Houttuyniae and Bulbus Fritillariae thunbergii） in rats.METHODS： The permeability of the rat’s abdominal cavity capillary was selected as the marker;the pharmacokinetics process of Sanyuemahuang Granule was studied by the Smolen method.RESULTS： The pharmacokinetics model of Sanyuemahuang Granule was one compartment model.According to the Smolen method,the pharmacokinetics parameter of the correspondent dosage in body was as follows： the absorption velocity constant（ka） was 1.06 h^-1,Tmax was 1.57 h,t1/2（ka） was 0.656 h,the elimination rate constant（ke） was 0.628 h^-1,t1/2（ke） was 1.10 h.According to the effect half life method,the elimination rate constant（ke） was 0.537 h^-1,t1/2（ke） was 1.29 h.According to the time-effect curve,the effecting velocity constant（ka） was 2.149 h^-1,Tmax is 1.36 h,t1/2（ka） was 0.32 h,the elimination velocity constant（ke） was 0.139 h^-1,t1/2（ke） was 5.0 h.CONCLUSION： The results show that the granule has quick-actting effects and slow clearance rate.But the pharmacokinetics parameters,calculated by the Smolen method are apparent parameters.The pharmacokinetics meaning of every parameter should be further explored.