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恩诺沙星在犬体内静脉注射和口服给药后恩诺沙星及其代谢产物环丙沙星的药代动力学

Pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin after intravenous and oral administration of enrofloxacin in dogs.

作者信息

Küng K, Riond J L, Wanner M

机构信息

Institute of Veterinary Physiology, University of Zurich, Switzerland.

出版信息

J Vet Pharmacol Ther. 1993 Dec;16(4):462-8. doi: 10.1111/j.1365-2885.1993.tb00212.x.

Abstract

Four dogs were given 5 mg/kg body weight enrofloxacin intravenously (i.v.) and orally (p.o.) in a cross-over study. Plasma concentrations of the active ingredient enrofloxacin and its main metabolite ciprofloxacin were determined by a reversed phase liquid chromatographic method. Pharmacokinetic parameters of both substances were calculated by use of statistical moments and were compared to those of enrofloxacin described in the veterinary literature. Mean enrofloxacin t1/2 lambda z was 2.4 h, mean Cls was 27.1 ml/min.kg, and mean Vss was 7.0 l/kg. After i.v. and p.o. administration, concentrations of ciprofloxacin exceeding minimal inhibitory concentrations of several microorganisms were reached (Cmax = 0.2 microgram/ml, tmax = 2.2 h after intravenous administration; Cmax = 0.2 microgram/ml, tmax = 3.6 h after oral administration). A considerable part of the antimicrobial activity is due to ciprofloxacin, the main metabolite of enrofloxacin.

摘要

在一项交叉研究中,给4只狗静脉注射(i.v.)和口服(p.o.)5 mg/kg体重的恩诺沙星。采用反相液相色谱法测定活性成分恩诺沙星及其主要代谢产物环丙沙星的血浆浓度。使用统计矩计算两种物质的药代动力学参数,并与兽医文献中描述的恩诺沙星的药代动力学参数进行比较。恩诺沙星的平均t1/2λz为2.4小时,平均清除率(Cls)为27.1 ml/(min·kg),平均稳态分布容积(Vss)为7.0 l/kg。静脉注射和口服给药后,环丙沙星的浓度达到了几种微生物的最低抑菌浓度以上(静脉注射后Cmax = 0.2微克/毫升,tmax = 2.2小时;口服给药后Cmax = 0.2微克/毫升,tmax = 3.6小时)。相当一部分抗菌活性归因于环丙沙星,它是恩诺沙星的主要代谢产物。

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