| 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1 mg/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0.424 mg/L及0.757，0.618，0.571，1.514 mg/kg；达峰时间（Tmax）分别为8，24，8，16和24 h；AUC（0-∞）分别为506.134，89.445，143.794，99.824和507.977 mg/(L·h)；MRT（0-∞）分别为1 810.979，176.789，194.868，312.487和259.84 h；t1/2z分别为1 208.304，155.129，67.049，231.330和165.918 h；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1 mg/kg IVM，其休药期为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 |
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| 基金项目: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) |
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| Pharmacokinetics of ivermectin in GIFT tilapia (Oreochromis niloticus) |
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LI Shikai,JIANG Min,WU Hao,et al
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| Abstract: |
| 【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 1 mg/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 3.0 software.【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:Cmax 0.424 mg/L and 0.757,0.618,0.571,1.514 mg/kg,Tmax 8,24,8,16 and 24 h,AUC（0-∞） 506.134,89.445,143.794,99.824 and 507.977 mg/(L·h),MRT（0-∞） 1 810.979,176.789,194.868,312.487 and 259.84 h,and t1/2z 1 208.304,155.129,67.049,231.330 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-0.049t,Ckidney=0.001e-0.005t＋0.713e-0.004t－0.714e-0.031t,Cspermary=3.479e-0.096t＋0.25e-0.003t－3.729e-0.119t,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 1 mg/kg,drug withdrawal time in muscle was 25 d. |
| Key words: ivermectin GIFT tilapia (Oreochromis niloticus) pharmacokinetics high-performance liquid chromatography(HPLC) withdraw period |
