肌肉注射硫酸安普霉素在猪体内的药代动力学和生物利用度研究  

Study of Pharmacokinetics and Bioavailability of the Apramycin Sulfate in Piglet after Intramuscular Injection

作　　者：胡振英[1] 张新国[1] 尚若锋[1] 徐忠赞[1] 李世宏[1] 宋中枢[1] 孙国栋 张均仁 刘俊平 

机构地区：[1]中国农业科学院兰州畜牧与兽药研究所 [2]甘肃省景泰县畜牧站 [3]甘肃省靖远县畜牧中心

出　　处：《中国兽药杂志》2001年第5期18-21,共4页Chinese Journal of Veterinary Drug

基　　金："九五"国家重点科技攻关项目子专题 ( 96 -C0 1-0 2 -0 3-0 2 )

摘　　要：对 6头健康猪单剂量静脉注射、肌肉注射国产硫酸安普霉素 ,研究其在猪体内的药代动力学和生物利用度。用微生物法测定血清药物浓度 ,结果平均回收率为 99.0 3% ,血清最低检测浓度为 0 .0 5 μg/ml,日内日间变异系数为 2 .2 %～ 5 .1 % ,且血清浓度在 0 .0 5～ 3μg/ml范围呈良好线性关系 ( r=0 .9965 )。对猪静注、肌注硫酸安普霉素 2 0 mg/kg后 ,经 MCPKP药代动力学计算机程序处理 ,体内药物运转符合开放型二室模型 ,肌肉注射 0 .85 6h后达峰药浓度 Cmax为 36.0 9±1 .2 2 μg/ml;t1/ 2 分别为 1 .5 8± 0 .67h、1 .0 6± 0 .1 1 h,CLB分别为 0 .1 5 L/kg/h、0 .1 7L/kg/h,V1分别为 0 .71 L/kg、 0 .1 L/kg,绝对生物利用度为 AUC i.m/AUC i.v=88.47%± 3.32 % 。The pharmacokinetics and bioavailability of the china made Apramycin sulfate was studied in 6 healthy piglet after intravenous injection and intramuscular injection a single dose The serum drug concentration were determined by Microbiological assay, and the main parameters were as follows: the mean recovery was 99 03%,and the minimum serum drug concentration determined by Microbiological assay was 0 05μg/ml,and the variation of the within a day and day to day were 2 2% ,5 1% It is better linear with serum drug concentration ranged from 0 05μg/ml to 3μg/ml (r=0 9965) The serum drug concentration profiles conformed to two compartment open model which took out by computer programmer Mcpkp of the pharmacokinetics after intravenous injection and intramuscular injection at 20mg/kg 0 856h after intramuscular injection ,the serum peak concentration of Apramycin(Cmax) was 36 09±1 22μg/ml The i v t 1/2 and i m t 1/2 were 1 58±0 67h and 1 06±0 11h,respectively,The i v CL B and i m CL B were 0 15L/kg/h and 0 17 L/kg/h,and then the apparent volume of distribution(V 1) were 0.71L/kg and 0.1L/kg after intravenous injection and intramuscular injection The bioavailability of Apramycin sulfate (AUC i m/AUC i v) is 88 47±3 32% The pharmaccokinetic parameters will provide a useful basis for clinical trail in animal

关 键 词：硫酸安普霉素 药代动力学 生物利用度 微生物测定法 肌肉注射 猪 

分 类 号：S858.28[农业科学—临床兽医学] S859.79[农业科学—兽医学]