三苯双脒肠溶片在羊体内药物代谢动力学试验

Research of pharmacokinetics for tribendimidine in sheep

为研究三苯双脒在绵羊体内动态变化的规律,采用方法如下:绵羊1次口服给药60、120、180 mg/kg体重3个剂量组,依据消除速率常数、吸收率常数、达峰时、血药浓度-时间曲线等主要药动学参数,经上海宏能软件有限公司开发的临床药物代谢动力学软件进行数据分析,符合血管外给药一级吸收一室模型,主要药动学参数为:吸收率常数Ka=0.15129h,t1/2Ka=4.74h,消除速率常数Ke=0.082 121h,t1/2Ke=8.46h,t1/2=19.03 h,达峰时tmax=8.0 h,Cmax=6257μg/L,血药浓度-时间曲线下面积AUC=300 51μg/L.h。三苯双脒肠溶片在羊体内吸收快、半衰期长等特点。说明三苯双脒肠溶片在药效试验剂量范围内比较安全。

To research the dynamic change of tribendimidine in sheep,Sheep were given three dosages（60 mg/kg,120 mg/kg,180 mg/kg）,according to absorption rate constant（Ka）,elimination rate constant（Ke）,tmax,blood drug level timetable diaphragmatic surface（AUC） and other main pharmacokinetics parameter.Using clinic pharmacokinetics software to carry out data analysis by Shanghai Hongneng software limited company to develop.The results showed that it was consistent with outside blood vessel dosaged first order absorption single compartment model,and main pharmacokinetics parameter is Ka=0.151 29 h,t1/2Ka=4.74 h,Ke=0.082 121 h,t1/2Ke=8.46 h,t1/2=19.03 h,tmax=8.0 h,Cmax=6257 μ/L,AUC=30 051 μg/L.Tribendimidine enteric tablet in sheep has resorption fast,half-life long,it showed that tribendimidine enteric tablet is safe in pharmacodynamic test dosage range.