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恩诺沙星口服给药后在大口黑鲈(Micropterus salmoides)体内的药代动力学及组织残留情况

Pharmacokinetics and tissue residues of enrofloxacin in the largemouth bass (Micropterus salmoides) after oral administration.

作者信息

Shan Qi, Wang Jingxin, Zheng Guangming, Zhu Xinping, Yang Yuanhao, Ma Lisha, Zhao Cheng, Li Lichun, Yin Yi

机构信息

Key Laboratory of Recreational Fisheries Research, Ministry of Agriculture and Ministry of Agriculture Laboratory of Quality & Safety Risky Assessment for Aquatic Product, Pearl River Fisheries Research Institute, Chinese Academic of Fishery Science, Guangzhou, China.

School of Public Health, Guangdong Pharmaceutical University, Guangzhou, China.

出版信息

J Vet Pharmacol Ther. 2020 Mar;43(2):147-152. doi: 10.1111/jvp.12794. Epub 2019 Jul 20.

Abstract

The study was carried out to evaluate the pharmacokinetic disposition of enrofloxacin (ENF) with a single dose of 20 mg/kg after oral administration in largemouth bass (Micropterus salmoides) at 28°C. The concentrations of ENF and of its metabolite ciprofloxacin (CIP) in plasma, liver, and muscle plus skin in natural proportions were determined using HPLC. The concentration-time data for ENF in plasma were best described by a two-compartment open model. After oral administration, the maximum ENF concentration (C ) of 10.99 μg/ml was obtained at 0.60 hr. The absorption half-life (T ) of ENF was calculated to be 0.07 hr whereas the elimination half-life (T ) of the drug was 90.79 hr. The estimates of area under the plasma concentration-time curve (AUC) and apparent volume of distribution (Vd/F) were 1,185.73 μg hr/ml and 2.21 L/kg, respectively. ENF residues were slowly depleted from the liver and muscle plus skin of largemouth bass with the T of 124.73 and 115.14 hr, respectively. Very low levels of ciprofloxacin were detected in the plasma and tissues. A withdrawal time of 24 days was necessary to ensure that the residues of ENF + CIP in muscle plus skin were less than the maximal residue limit (MRL) of 100 μg/kg established by the European Union.

摘要

本研究旨在评估在28°C条件下,对大口黑鲈(Micropterus salmoides)口服20 mg/kg单剂量恩诺沙星(ENF)后的药代动力学特征。采用高效液相色谱法测定血浆、肝脏以及按自然比例混合的肌肉和皮肤中ENF及其代谢产物环丙沙星(CIP)的浓度。血浆中ENF的浓度-时间数据最适合用二室开放模型描述。口服给药后,在0.60小时时获得最大ENF浓度(Cmax)为10.99μg/ml。ENF的吸收半衰期(T1/2ka)经计算为0.07小时,而该药物的消除半衰期(T1/2β)为90.79小时。血浆浓度-时间曲线下面积(AUC)和表观分布容积(Vd/F)的估计值分别为1,185.73μg·hr/ml和2.21 L/kg。ENF在大口黑鲈的肝脏以及肌肉和皮肤中的残留量缓慢下降,其T1/2分别为124.73和115.14小时。在血浆和组织中检测到极低水平的环丙沙星。为确保肌肉和皮肤中ENF + CIP的残留量低于欧盟规定的100μg/kg最大残留限量(MRL),需要24天的休药期。

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