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恩诺沙星及其代谢产物环丙沙星在中国中华绒螯蟹体内的药代动力学和组织分布

Pharmacokinetics and tissue distribution of enrofloxacin and its metabolite ciprofloxacin in the Chinese mitten-handed crab, Eriocheir sinensis.

作者信息

Wu Guanghong, Meng Yong, Zhu Xiaohua, Huang Cheng

机构信息

Freshwater Fisheries Research Institute of Jiangsu Province, Nanjing 210017, People's Republic of China.

出版信息

Anal Biochem. 2006 Nov 1;358(1):25-30. doi: 10.1016/j.ab.2006.05.031. Epub 2006 Jun 12.

Abstract

The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in the Chinese mitten-handed crab after a single intramuscular injection of enrofloxacin at 5.0mg/kg body weight. The tissue concentrations of enrofloxacin and ciprofloxacin were determined simultaneously by a high-performance liquid chromatography (HPLC) method. The data were analyzed with Practical Pharmacokinetic Program 3P97. The highest average concentrations of enrofloxacin in liver, muscle, gill, and hemolymph were 3.93, 12.42, 16.73, and 11.04 microg/g (ml), respectively. The elimination half-lives (t(1/2beta)) for enrofloxacin were 92.42, 64.86, 38.80, and 52.39 h, respectively. The AUC(0-infinity) values for enrofloxacin were 304.80, 260.74, 288.30, and 269.24 microg h/ml, respectively. Ciprofloxacin could be detected in all four tissues. The respective values of main pharmacokinetics parameters Cmax, t(1/2beta), and AUC(0-infinity) were 0.52 microg/g (ml), 38.38 h, and 35.06 microg h/ml for liver; 0.24 microg/g (ml), 65.36 h, and 25.64 microg h/ml for muscle; 0.10 microg/g (ml), 112.88 h, and 11.57 microg h/ml for gill; and 0.30 microg/g (ml), 93.33 h, and 39.99 microg h/ml for hemolymph.

摘要

在中华绒螯蟹以5.0mg/kg体重单次肌肉注射恩诺沙星后,研究了恩诺沙星及其活性代谢产物环丙沙星的药代动力学。采用高效液相色谱(HPLC)法同时测定恩诺沙星和环丙沙星的组织浓度。数据用实用药代动力学程序3P97进行分析。恩诺沙星在肝脏、肌肉、鳃和血淋巴中的最高平均浓度分别为3.93、12.42、16.73和11.04μg/g(ml)。恩诺沙星的消除半衰期(t(1/2β))分别为92.42、64.86、38.80和52.39小时。恩诺沙星的AUC(0-∞)值分别为304.80、260.74、288.30和269.24μg h/ml。在所有四种组织中均能检测到环丙沙星。肝脏中环丙沙星的主要药代动力学参数Cmax、t(1/2β)和AUC(0-∞)的相应值分别为0.52μg/g(ml)、38.38小时和35.06μg h/ml;肌肉中分别为0.24μg/g(ml)、65.36小时和25.64μg h/ml;鳃中分别为0.10μg/g(ml)、112.88小时和11.57μg h/ml;血淋巴中分别为0.30μg/g(ml)、93.33小时和39.99μg h/ml。

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