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恩诺沙星在鸡体内的药代动力学及残留情况

Pharmacokinetics and residues of enrofloxacin in chickens.

作者信息

Anadón A, Martínez-Larrañaga M R, Díaz M J, Bringas P, Martínez M A, Fernàndez-Cruz M L, Fernández M C, Fernández R

机构信息

Department of Toxicology, Faculty of Veterinary Medicine, Universidad Complutense de Madrid, Spain.

出版信息

Am J Vet Res. 1995 Apr;56(4):501-6.

PMID:7785830
Abstract

The pharmacokinetic properties of enrofloxacin were determined in broiler chickens after single IV and orally administered doses of 10 mg/kg of body weight. After IV and oral administrations, the plasma concentration-time graph was characteristic of a two-compartment open model. The elimination half-life and the mean +/- SEM residence time of enrofloxacin for plasma were 10.29 +/- 0.45 and 9.65 +/- 0.48 hours, respectively, after IV administration and 14.23 +/- 0.46 and 15.30 +/- 0.53 hours, respectively, after oral administration. After single oral administration, enrofloxacin was absorbed slowly, with time to reach maximal plasma concentration of 1.64 +/- 0.04 hours. Maximal plasma concentration was 2.44 +/- 0.06 micrograms/ml. Oral bioavailability was found to be 64.0 +/- 0.2%. Statistically significant differences between the 2 routes of administration were found for the pharmacokinetic variables--half-lives of the distribution and elimination phase and apparent volume of distribution and volume of distribution at steady state. In chickens, enrofloxacin was extensively metabolized into ciprofloxacin. Residues of enrofloxacin and the major metabolite ciprofloxacin in fat, kidney, liver, lungs, muscles, and skin were measured in chickens that received an orally administered dose of 10 mg/kg once daily for 4 days. The results indicate that enrofloxacin and ciprofloxacin residues were cleared slowly. Mean muscle, liver, and kidney concentrations of the metabolite ciprofloxacin ranging between 0.020 and 0.075 micrograms/g persisted on day 12 in chickens after dosing. However, at the time of slaughter (12 days), enrofloxacin residues were only detected in liver and mean +/- SEM concentration was 0.025 +/- 0.003 micrograms/g.

摘要

在体重为10mg/kg的肉鸡单次静脉注射和口服恩诺沙星后,测定了其药代动力学特性。静脉注射和口服给药后,血浆浓度-时间图符合二室开放模型特征。静脉注射后,恩诺沙星的消除半衰期和血浆平均±标准误驻留时间分别为10.29±0.45小时和9.65±0.48小时;口服给药后分别为14.23±0.46小时和15.30±0.53小时。单次口服给药后,恩诺沙星吸收缓慢,达到最大血浆浓度的时间为1.64±0.04小时。最大血浆浓度为2.44±0.06μg/ml。口服生物利用度为64.0±0.2%。在药代动力学变量方面,即分布相和消除相半衰期、表观分布容积和稳态分布容积,发现两种给药途径之间存在统计学显著差异。在鸡体内,恩诺沙星广泛代谢为环丙沙星。对每天口服10mg/kg剂量,连续给药4天的鸡,测定其脂肪、肾脏、肝脏、肺、肌肉和皮肤中恩诺沙星及其主要代谢产物环丙沙星的残留量。结果表明,恩诺沙星和环丙沙星残留清除缓慢。给药后第12天,鸡体内代谢产物环丙沙星在肌肉、肝脏和肾脏中的平均浓度在0.020至0.075μg/g之间。然而,在屠宰时(12天),仅在肝脏中检测到恩诺沙星残留,平均±标准误浓度为0.025±0.003μg/g。

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