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单次肌肉注射后,三种温度下氟苯尼考及其代谢产物氟苯尼考胺在鲫鱼(Carassius auratus)体内的药代动力学

Pharmacokinetics of florfenicol and its metabolite florfenicol amine in crucian carp (Carassius auratus) at three temperatures after one single intramuscular injection.

作者信息

Yang Fan, Yang Fang, Kong Tao, Wang Guoyong, Bai Dongying, Liu Baobao

机构信息

College of Animal Science and Technology, Henan University of Science and Technology, Luoyang, China.

Key Disciplines Open Laboratory of Environmental and Animal Products Safety, Henan University of Science and Technology, Luoyang, China.

出版信息

J Vet Pharmacol Ther. 2018 Oct;41(5):739-745. doi: 10.1111/jvp.12672. Epub 2018 Jun 12.

DOI:10.1111/jvp.12672
PMID:29892973
Abstract

The pharmacokinetic profiles of florfenicol (FF) or florfenicol amine (FFA) in crucian carp were compared at different water temperatures after single intramuscular administration of FF at 10 mg/kg bodyweight. The concentrations of FF and FFA were determined by a high-performance liquid chromatography method, and then, the concentration versus time data were subjected to compartmental analysis using a one-compartment open model. At the water temperatures of 10, 20, and 25°C, the peak concentrations (C s) of FF were 2.28, 2.29, and 2.34 μg/ml, respectively, while those of FFA were 0.42, 0.71, and 0.82 μg/ml, respectively. And the absorption half-life (t ) of FF was 0.21, 0.19, and 0.21 hr, while the elimination half-life (t ) was 31.66, 24.77, and 21.48 hr, respectively. For FFA, the formation half-life (t ) was 3.85, 8.97, and 12.43 hr, while the t was 58.34, 30.27, and 21.22 hr, respectively. The results presented here demonstrated that the water temperature had effects on the elimination of both FF and FFA and the formation of FFA. Based on the T > MIC values calculated here, to treat the infections of bacterial with MIC value ≤ 0.5 μg/ml, FF intramuscularly given at 10 mg/kg bodyweight with a 72-hr interval is sufficient at the water temperature of 10°C, while the intervals of 60 and 48 hr were needed at 20 and 25°C, respectively. But to treat bacterial with higher MIC values, more FF or FF at 10 mg/kg BW but with shorter intervals should be intramuscularly given to the infected fish.

摘要

在以10毫克/千克体重单次肌肉注射氟苯尼考(FF)后,比较了不同水温下鲫鱼体内氟苯尼考(FF)和氟苯尼考胺(FFA)的药代动力学特征。采用高效液相色谱法测定FF和FFA的浓度,然后使用一室开放模型对浓度-时间数据进行房室分析。在水温为10、20和25℃时,FF的峰浓度(Cmax)分别为2.28、2.29和2.34微克/毫升,而FFA的峰浓度分别为0.42、0.71和0.82微克/毫升。FF的吸收半衰期(t1/2ka)为0.21、0.19和0.21小时,消除半衰期(t1/2ke)分别为31.66、24.77和21.48小时。对于FFA,生成半衰期(t1/2bf)为3.85、8.97和12.43小时,t1/2ke分别为58.34、30.27和21.22小时。此处呈现的结果表明,水温对FF和FFA的消除以及FFA的生成均有影响。基于此处计算的T>MIC值,对于治疗MIC值≤0.5微克/毫升的细菌感染,在水温为10℃时,以10毫克/千克体重肌肉注射FF,间隔72小时就足够了,而在20℃和25℃时,分别需要间隔60小时和48小时。但对于治疗MIC值较高的细菌感染,应给感染的鱼肌肉注射更多的FF或10毫克/千克体重的FF,但间隔时间要更短。

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