Pharmacokinetics and residues of enrofloxacin in chickens

A. Anadón From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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M. R. Martínez-Larrañaga From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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M. J. Díaz From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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P. Bringas From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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M. A. Martínez From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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M. L. Femández-Cruz From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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M. C. Fernández From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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R. Fernández From the Institute of Pharmacology and Toxicology, CSIC, Department of Toxicology, Faculty of Vetennary Medicine, Universidad Complutense de Madrid, 28040 Madrid, Spain.

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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 μg/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 μg/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 μg/g.

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 μg/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 μg/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 μg/g.

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