双吡啶单肟HI-6药代动力学的动物种间相关性

Interspecies correlation of the pharmacokinetics of bispyridinum mono-oxime HI-6 on different animals

给5种哺乳动物iv双吡啶单肟HI—6 20mg/kg,其药物代谢动力学均呈二室开放模型,部分药动学参数可表示为体重的指数函数。将5种动物的采血时间转换为生理等价时间,建立了预测人血浆中HI—6浓度的经验函数式。经人体资料验证,预测值与实测值基本一致。

To find interspccies regularity of disposition of HI-6 [1-(2-hydroxy-imino-methyl-pyridinium)-2-(4-carboxy-amido-pyridinium)-dimethyl ether dichloridc] in mammals and provide a basis for extrapolating the pharmacokinetics of HI-6 in human from the results of animals,interspecies correlation of the pharmacokinetics of the drug in mice,rats,guinea pigs,rabbits,and dogs were studied.The kinetic profiles of the drug,after iv administration of 20mg/kg to the animals,can be described by a two-compartment open model.It is suitable for some pharmacokineticparameters to be expressed as power function of the body weight.By converting the blood sampling time in animals into the physiological equivalent time in the light of the results described,an empirical formula of predicting the plasma concentrations of the drug after iv adr ministration to human was derived.The predicted values calculated according to the formula accorded with observed values in human.