伊维菌素在吉富罗非鱼体内的药物动力学  

Pharmacokinetics of ivermectin in GIFT tilapia(Oreochromis niloticus)

作　　者：李世凯[1,2] 江敏[1] 吴昊[1] 彭晓叶[1] 张健龙[1] 谢芹[1] 刘利平[1] LI Shikai JIANG Min WU Hao PENG Xiaoye ZHANG Jianlong XIE Qin LIU Liping(College of Fisheries and Life Science, Shanghai Ocean University, Shanghai 201306, China Guizhou Fisheries Research Institute ,Guiyang,Guizhou 550025 ,China)

机构地区：[1]上海海洋大学水产与生命学院,上海201306 [2]贵州省水产研究所,贵州贵阳550025

出　　处：《西北农林科技大学学报（自然科学版）》2016年第8期32-40,共9页Journal of Northwest A&F University(Natural Science Edition)

基　　金：欧盟科研架构计划项目(EU-FP7-SEAT222889);上海市教委重点学科建设项目(J50701);上海市高校知识服务平台项目(ZF1206)

摘　　要：【目的】研究伊维菌素(IVM)在吉富罗非鱼体内的药物动力学,为其在罗非鱼养殖中的合理应用提供依据。【方法】将吉富罗非鱼按1mg/kg的给药剂量肌肉注射IVM,采用高效液相色谱法于给药后不同时间点对各组织进行采样检测,通过DAS 3.0药物代谢动力学软件分析IVM在吉富罗非鱼体内的药代动力学参数。【结果】在肌肉注射给药方式下,吉富罗非鱼血液中IVM质量浓度C随时间t的药物动力学模型符合一级吸收二室开放模型,其药物动力学方程为:C血液=0.215e-0.016(t-0.22)+0.198e0-0.413e-1.294(t-0.22)。肌肉注射给药后,IVM在血液及肌肉、肾脏、精巢和肝脏的峰含量(Cmax)分别为0.424mg/L及0.757,0.618,0.571,1.514mg/kg;达峰时间(Tmax)分别为8,24,8,16和24h;AUC(0-∞)分别为506.134,89.445,143.794,99.824和507.977mg/(L·h);MRT(0-∞)分别为1 810.979,176.789,194.868,312.487和259.84h;t1/2z分别为1 208.304,155.129,67.049,231.330和165.918h;各组织的药物代谢动力学方程分别为:C肌肉=4.219e-0.037t+0.217e-0.004t-4.436e-0.049t;C肾脏=0.001e-0.005t+0.713e-0.004t-0.714e-0.031t;C精巢=3.479e-0.096t+0.25e-0.003t-3.729e-0.119t;C肝脏=1.764(e-0.004t-e-0.132t)。【结论】IVM在吉富罗非鱼体内的药物动力学特征表现为:吸收快、分布广、消除缓慢。因此初步确定在水温(26±1)℃下肌肉注射1mg/kg IVM,其休药期为25d。【Objective】This paper studied pharmacokinetics of ivermectin in GIFT tilapia（Oreochromis niloticus）to provide basis for its rational application.【Method】Ivermectin was given to GIFT tilapia（Oreochromis niloticus）through a single intramuscular administration at dose of 1mg/kg,then tilapia tissues samples were taken at different time points and analyzed by high-performance liquid chromatography（HPLC）before the pharmacokinetics parameters were calculated using DAS 3.0software.【Result】With intramuscular administration,the best pharmacokinetic model of blood was two-compartmental open model with first-order absorption：Cblood=0.215e^-0.016（t-0.22）＋0.198e0-0.413e^-1.294（t-0.22）.After administration,non-compartmental pharmacokinetic parameters in blood,muscle,kidney,spermary and liver were：Cmax0.424mg/L and 0.757,0.618,0.571,1.514mg/kg,Tmax8,24,8,16 and 24h,AUC（0-∞）506.134,89.445,143.794,99.824 and 507.977mg/（L·h）,MRT（0-∞）1 810.979,176.789,194.868,312.487 and 259.84 h,and t1/2z1 208.304,155.129,67.049,231.330 and 165.918 h,respectively.The pharmacokinetics equations in muscle,kidney,spermary and liver were Cmuscle=4.219e^-0.037t＋0.217e^-0.004t-4.436e^-0.049 t,Ckidney=0.001e^-0.005t＋0.713e^-0.004t-0.714e^-0.031 t,Cspermary=3.479e^-0.096t＋0.25e^-0.003t-3.729e^-0.119 t,and Cliver=1.764（e^-0.004t-e^-0.132t）.【Conclusion】The pharmacokinetic characteristics of IVM in GIFT tilapia were fast absorption,wide distribution and slow elimination.When water temperature was（26±1）℃and intramuscular administration dose was 1mg/kg,drug withdrawal time in muscle was 25 d.

关 键 词：伊维菌素 吉富罗非鱼 药物动力学 高效液相色谱 休药期 

分 类 号：S948[农业科学—水产养殖]