喹烯酮在猪、鸡体内的药代动力学研究

Studies on the Pharmacokinetics of Quinocetone in Pigs and Chickens

猪6头,鸡10只,单剂量0 4065mg·kg-1(比活度24 6μci mg-1)静注给药,一个月后,单剂量31 15mg·kg-1(比活度5 187μci·mg-1)口服给药,进行代谢动力学研究。依据本实验建立的方法,以液体闪烁谱仪计数法进行含量测定。喹烯酮以原药的形式代谢排泄,静注给药符合二室开放模型:猪,T1/2α=0 1899h,T1/2β=4 5528h,Kel=0 8654h-1,AUC=0 00925mg·h-1·L-1;鸡,T1/2α=0 1637h,T1/2β=3 8189h,Kel=1 6834h-1,AUC=0 005046mg·h-1·L-1。口服给药符合一级吸收一室开放模型:猪,T1/2Ka=0 4678h,T1/2β=3 7445h,Tp=1 3367h,Cmax=0 000713μg·ml-1,AUC=0 00303mg·L-1·h-1;鸡,T1/2Ka=0 5142h,T1/2β=4 6637h,Tp=1 8459h,Cmax=0 000897μg·m-1,AUC=0 00773mg·L-1·h-1,说明喹烯酮口服给药后,其吸收较快,消除相对也较快,生物利用度低。

Normal pigs and chickens were given quinocetone iv 04065 mg·kg-1(rate radioactive degree 246μci·mg-1)and po 3115 mg·kg-1(rate radioactive degree 5187 μci·mg-1)after a month.The concentrations of quinocetone were determined by an liquid flamed chromatographic machine methed developed in our laboratory.The method is simple,sensitive and available for pharmacokinetics studies.The excretion type of quinocetone was also the beginning type.Plasma drug concentrationtime course of quinocetone after iv administration of quinocetone was found to be fitted to two compartment open model and its pharmacokinetic parameters were as follows:pigs,T1/2α=01899h,T1/2β=45528h,Kel=08654h-1,AUC=000925 mg·h-1·L-1;chickens,T1/2a=01637 h,T1/2β=38189 h,Kel=16834 h-1,AUC=0005046 mg·h-1·L-1.Plasma drug concentrationtime course of quinocetone after po administration of quinocetone was found to be fitted to one compartment open model with first order absorption and its pharmacokinetic parameters were as follows:pigs,T1/2Ka=04678 h,T1/2K=37445 h,Tp=13367 h,Cmax=0.000713 μg·ml-1,AUC=000303 mg·L-1·h-1;chickens,T1/2Ka=05142 h,T1/2K=46637 h,Tp=18459 h,Cmax=0000897 μg·ml-1,AUC=000773 mg·L-1·h-1.The experiment showed that the absorption and excretion of quinocetone were fast and its availability was low after po administration.