Pharmacokinetics and bioavailability of florfenicol following intravenous, intramuscular and oral administrations in rabbits

Vet Res Commun. 2004 Aug;28(6):515-24. doi: 10.1023/b:verc.0000040241.06642.49.

Abstract

This study examined the disposition kinetics and bioavailability of florfenicol after intravenous (i.v.), intramuscular (i.m.) and oral administration to rabbits at a dose of 30 mg/kg BW. Serial blood samples were collected through an indwelling catheter intermittently for 24 h for various routes. Plasma antibacterial concentrations were determined using a microbiological assay method with Bacillus subtilis ATCC 6633 as a reference organism. Plasma concentration-time data generated in the present study were analysed by non-compartmental methods based on statistical moment theory. Following i.v. administration, the overall elimination half-life (t1/2beta) was 1.54 h, mean residence time (MRT) was 1.69 h, mean volume of distribution at steady-state (Vdss) was 0.57 L/kg, and total body clearance (Cltot) was 0.34 L/kg/h. After i.m. and oral dosing, the terminal part of the curve should correspond to the absorption phase, instead of to the elimination phase, with terminal half-lives of 3.01 and 2.57 h, respectively. The mean absorption time (MAT) was 2.65 h for i.m. and 2.01 h for oral administration. Elimination rate constants differed with i.v., i.m. and oral administrations, suggesting a flip-flop situation. The observed mean peak plasma concentrations (Cmax obs) were 21.65 and 15.14 microg/ml achieved at a post-injection time (Tmax obs) of 0.5 h following i.m. and oral dosing, respectively. The absolute systemic availabilities were 88.25% and 50.79%, respectively, and the extent of plasma protein binding percent was 11.65%.

Publication types

  • Clinical Trial

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Bacterial Agents / administration & dosage*
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Half-Life
  • Injections, Intramuscular / veterinary
  • Injections, Intravenous / veterinary
  • Protein Binding
  • Rabbits / metabolism*
  • Thiamphenicol / administration & dosage*
  • Thiamphenicol / analogs & derivatives*
  • Thiamphenicol / blood
  • Thiamphenicol / pharmacokinetics*

Substances

  • Anti-Bacterial Agents
  • florfenicol
  • Thiamphenicol