硫酸阿米卡星在德国牧羊犬体内的比较药代动力学研究  

Comparative pharmacokinetics of amikacin sulfate in German shepherd dog

作　　者：代珍青[1] 林远清[2] 于艳英[1] 曾东平[1] 孙永学[1] 

机构地区：[1]华南农业大学兽医学院广东省兽药研制与安全评价重点实验室,广东广州510642 [2]广东省公安厅警犬基地,广东佛山528240

出　　处：《中国兽医科学》2010年第12期1291-1295,共5页Chinese Veterinary Science

基　　金：华南农业大学横向研究课题开发项目(2009)

摘　　要：将9只健康成年德国牧羊犬随机分成3组,按随机正交试验设计,经静脉注射、肌肉注射和皮下注射硫酸阿米卡星注射液(10 mg/kg),以比较不同给药途径在德国牧羊犬体内的药代动力学特征。血浆样品经三氯乙酸提取后,采用LC-MS/MS法测定血药浓度,使用药代动力学程序3p97软件对药-时数据进行处理。结果显示,静脉注射硫酸阿米卡星的药-时数据符合二室开放模型,主要药代动力学参数为:t1/2α=0.121 h,t1/2β=1.612 h,Vc=0.095 L/kg,CLs=0.080 L/(kg.h),AUC=129.2μg/mL.h。肌肉注射和皮下注射硫酸阿米卡星的药-时数据均符合一级吸收二室模型,主要药代动力学参数分别为:t1/2α=0.486 h和0.636 h,t1/2β=1.404 h和1.782 h,tmax=0.785 h和0.894 h,Cmax=44.59μg/mL和31.42μg/mL,AUC=117.0μg/mL.h和105.1μg/mL.h,F=91.32%和81.02%。结果表明,静脉注射分布迅速且广泛,消除较快;肌肉注射和皮下注射吸收迅速完全,消除均迅速,生物利用度高;肌肉注射较皮下注射达峰时间短、峰浓度高和生物利用度高。The comparative pharmacokinetics of amikacin sulfate were carried out in 9 German shepherd dogs using a randomized orthogonal design with a single intravenous,intramuscular and subcutaneous injection of 10mg/kg.Plasma samples were extracted by trichloroacetic acid（TCA）,the concentrations of amikacin sulfate were determined by LC-MS/MS and the concentration-time data were analyzed with 3p97 program.A two-compartment open model was best to fit for the concentration-time data after intravenous injection and its main parameters were as follows：t1/2β=1.612h,Vc=0.095 L/kg,CLs= 0.080 L/（kg·h）,AUC=129.2μg/mL·h.A two-compartment model with first order absorption best described the concentration-time data after intramuscular and subcutaneous injections.Their main parameters were as follows：t1/2α =0.486 h and 0.636 h,t1/2β =1.404 h and 1.782 h,tmax =0.785 h and 0.894 h,Cmax=44.59μg/mL and 31.42μg/mL,AUC=117.0μg/mL·h and 105.1μg/mL·h,F=91.32%and 81.02%,respectively.The results showed that the amikacin sulfate was rapidly and widely distributed after intravenous injection,but had a rapid absorption and elimination and a high bioavailability after intramuscular and subcutaneous injections.Compared to the subcutaneous injection,the tmax was shorter,and the Cmax and the bioavailability was higher after intramuscular injection.

关 键 词：阿米卡星 德国牧羊犬 药代动力学 LC-MS/MS法 

分 类 号：S859.796[农业科学—临床兽医学]