Pharmacokinetic variables and tissue residues of enrofloxacin and ciprofloxacin in healthy pigs

Am J Vet Res. 1999 Nov;60(11):1377-82.

Abstract

Objectives: To determine pharmacokinetics of enrofloxacin and its metabolite ciprofloxacin after a single i.v. and i.m. administration of enrofloxacin and tissue residues after serial daily i.m. administration of enrofloxacin in pigs.

Animals: 20 healthy male pigs.

Procedure: 8 pigs were used in a crossover design to investigate pharmacokinetics of enrofloxacin after a single i.v. and i.m. administration (2.5 mg/kg of body weight). Twelve pigs were used to study tissue residues; they were given daily doses of enrofloxacin (2.5 mg/kg, i.m. for 3 days). Plasma and tissue concentrations of enrofloxacin and ciprofloxacin were determined. Residues of enrofloxacin and ciprofloxacin were measured in fat, kidney, liver, and muscle.

Results: Mean (+/-SD) elimination half-life and mean residence time of enrofloxacin in plasma were 9.64+/-1.49 and 12.77+/-2.15 hours, respectively, after i.v. administration and 12.06+/-0.68 and 17.15+/-1.04 hours, respectively, after i.m. administration. Half-life at alpha phase of enrofloxacin was 0.23+/-0.05 and 1.94+/-0.70 hours for i.v. and i.m. administration, respectively. Maximal plasma concentration was 1.17 +/-0.23 microg/ml, and interval from injection until maximum concentration was 1.81+/-0.23 hours. Renal and hepatic concentrations of enrofloxacin (0.012 to 0.017 microg/g) persisted for 10 days; however, at that time, ciprofloxacin residues were not detected in other tissues.

Conclusions and clinical relevance: Enrofloxacin administered i.m. at a dosage of 2.5 mg/kg for 3 successive days, with a withdrawal time of 10 days, resulted in a sum of concentrations of enrofloxacin and ciprofloxacin that were less than the European Union maximal residue limit of 30 ng/g in edible tissues.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Infective Agents / administration & dosage
  • Anti-Infective Agents / blood
  • Anti-Infective Agents / pharmacokinetics*
  • Area Under Curve
  • Chromatography, High Pressure Liquid
  • Ciprofloxacin / administration & dosage
  • Ciprofloxacin / blood
  • Ciprofloxacin / pharmacokinetics*
  • Cross-Over Studies
  • Drug Residues / pharmacokinetics*
  • Enrofloxacin
  • Fluoroquinolones*
  • Injections, Intramuscular
  • Injections, Intravenous
  • Male
  • Metabolic Clearance Rate
  • Models, Biological
  • Quinolones / administration & dosage
  • Quinolones / blood
  • Quinolones / pharmacokinetics*
  • Swine

Substances

  • Anti-Infective Agents
  • Fluoroquinolones
  • Quinolones
  • Enrofloxacin
  • Ciprofloxacin