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恩诺沙星在韩国鲶鱼(鲇鱼)体内的药代动力学

Pharmacokinetics of enrofloxacin in Korean catfish (Silurus asotus).

作者信息

Kim M-S, Lim J-H, Park B-K, Hwang Y-H, Yun H-I

机构信息

Division of Veterinary Pharmacology and Toxicology, College of Veterinary Medicine, Chungnam National University, Daejeon, Korea.

出版信息

J Vet Pharmacol Ther. 2006 Oct;29(5):397-402. doi: 10.1111/j.1365-2885.2006.00783.x.

DOI:10.1111/j.1365-2885.2006.00783.x
PMID:16958784
Abstract

The objective of this study was to evaluate the pharmacokinetic profile of enrofloxacin and its active metabolite, ciprofloxacin, in Korean catfish after intravenous and oral administrations. Enrofloxacin was administered to Korean catfish by a single intravenous and oral administrations at the dose of 10 mg/kg body weight. The plasma concentrations from intravenous and oral administrations of enrofloxacin were determined by LC/MS. Pharmacokinetic parameters from both routes were described to have a two-compartmental model. After intravenous and oral administrations of enrofloxacin, the elimination half-lives (t(1/2,beta)), area under the drug concentration-time curves (AUC), oral bioavailability (F) were 17.44 +/- 4.66 h and 34.13 +/- 11.50 h, 48.1 +/- 15.7 microgxh/mL and 27.3 +/- 12.4 microgxh/mL, and 64.59 +/- 4.58% respectively. The 3.44 +/- 0.81 h maximum concentration (C(max)) of 1.2 +/- 0.2 microg/mL. Ciprofloxacin, an active metabolite of enrofloxacin, was detected at all the determined time-points from 0.25 to 72 h, with the C(max) of 0.17 +/- 0.08 microg/mL for intravenous dose. After oral administration, ciprofloxacin was detected at all the time-points except 0.25 h, with the C(max) of 0.03 +/- 0.01 microg/mL at 6.67 +/- 2.31 h. Ciprofloxacin was eliminated with terminal half-life t(1/2,beta) of 52.08 +/- 17.34 h for intravenous administration and 52.43 +/- 22.37 h for oral administration.

摘要

本研究的目的是评估恩诺沙星及其活性代谢产物环丙沙星在韩国鲶鱼静脉注射和口服给药后的药代动力学特征。以10 mg/kg体重的剂量对韩国鲶鱼进行单次静脉注射和口服恩诺沙星。通过液相色谱/质谱法测定恩诺沙星静脉注射和口服给药后的血浆浓度。两种给药途径的药代动力学参数均采用二室模型描述。恩诺沙星静脉注射和口服给药后,消除半衰期(t(1/2,β))、血药浓度-时间曲线下面积(AUC)、口服生物利用度(F)分别为17.44±4.66小时和34.13±11.50小时、48.1±15.7μg·xh/mL和27.3±12.4μg·xh/mL、64.59±4.58%。最大浓度(C(max))为1.2±0.2μg/mL,出现在3.44±0.81小时。恩诺沙星的活性代谢产物环丙沙星在0.25至72小时的所有测定时间点均被检测到,静脉给药时C(max)为0.17±0.08μg/mL。口服给药后,除0.25小时外,在所有时间点均检测到环丙沙星,在6.67±2.31小时时C(max)为0.

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