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氟苯尼考在鳕鱼( Gadus morhua)中的药代动力学及其对鳗弧菌的体外抗菌活性

Pharmacokinetics of florfenicol in cod Gadus morhua and in vitro antibacterial activity against Vibrio anguillarum.

作者信息

Samuelsen Ole Bent, Bergh Oivind, Ervik Arne

机构信息

Institute of Marine Research, Department of Aquaculture, PO Box 1870 Nordnes, 5817 Bergen, Norway.

出版信息

Dis Aquat Organ. 2003 Sep 24;56(2):127-33. doi: 10.3354/dao056127.

Abstract

The pharmacokinetic profile of the antibacterial agent florfenicol was studied in plasma after intravenous (i.v.) injection and in plasma, muscle and liver following oral (p.o.) administration to cod Gadus morhua, held in seawater at 8 degrees C and weighing 100 to 200 g. Following i.v. injection, the plasma drug concentration-time profile showed 2 distinct phases. The plasma distribution half-life (t1/2alpha) was estimated to be 1.6 h, the elimination half-life (t1/2beta) to be 43 h, the total body clearance (ClT) to be 0.015 1 kg(-1) h(-1) and mean residence time (MRT) to be 74 h. The volume of distribution at steady state, Vd(ss), was calculated to be 1.1 l kg(-1). Following p.o. administration, the bioavailability was estimated to be 91%, the peak plasma concentrations (Cmax) to be 10.8 microg ml(-1) and the time to peak plasma concentrations (Tmax) to be 7 h. Corresponding Cmax and Tmax values were 13.0 microg g(-1) and 9 h, respectively, in muscle and 12.1 microg g(-1) and 9 h, respectively, in liver. The in vitro minimum inhibitory concentration (MIC) values of florfenicol against 3 Vibrio anguillarum strains isolated from diseased cod (A-21, HI-610, HI-618) were 0.5 microg ml(-1) for all 3 strains.

摘要

在8℃海水中饲养、体重100至200克的鳕鱼(Gadus morhua)中,研究了抗菌剂氟苯尼考静脉注射(i.v.)后在血浆中的药代动力学特征,以及口服(p.o.)给药后在血浆、肌肉和肝脏中的药代动力学特征。静脉注射后,血浆药物浓度-时间曲线呈现出2个不同阶段。血浆分布半衰期(t1/2α)估计为1.6小时,消除半衰期(t1/2β)为43小时,全身清除率(ClT)为0.015 1 kg-1 h-1,平均驻留时间(MRT)为74小时。稳态分布容积Vd(ss)计算为1.1 l kg-1。口服给药后,生物利用度估计为91%,血浆峰浓度(Cmax)为10.8 μg ml-1,达血浆峰浓度时间(Tmax)为7小时。肌肉中的相应Cmax和Tmax值分别为13.0 μg g-1和9小时,肝脏中的相应值分别为12.1 μg g-(-1)和9小时。氟苯尼考对从患病鳕鱼分离出的3株鳗弧菌(A-21、HI-610、HI-618)的体外最低抑菌浓度(MIC)值,3株均为0.5 μg ml-1。

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