Characterization of the pharmacokinetic disposition of levofloxacin in stallions after intravenous and intramuscular administration


Goudah A., El-Sooud K. A., Shim J. -., Shin H. -., HASSIBELNABY A. M. A.

JOURNAL OF VETERINARY PHARMACOLOGY AND THERAPEUTICS, cilt.31, sa.5, ss.399-405, 2008 (SCI-Expanded) identifier identifier identifier

Özet

The target of the present study was to investigate the plasma disposition kinetics of levofloxacin in stallions (n = 6) following a single intravenous (i.v.) bolus or intramuscular (i.m.) injection at a dose rate of 4 mg/kg bwt, using a two-phase crossover design with 15 days as an interval period. Plasma samples were collected at appropriate times during a 48-h administration interval, and were analyzed using a microbiological assay method. The plasma levofloxacin disposition was best fitted to a two-compartment open model after i.v. dosing. The half-lives of distribution and elimination were 0.21 +/- 0.13 and 2.58 +/- 0.51 h, respectively. The volume of distribution at steady-state was 0.81 +/- 0.26 L/kg, the total body clearance (Cl-tot) was 0.21 +/- 0.18 L/h/kg, and the areas under the concentration-time curves (AUCs) were 18.79 +/- 4.57 mu g.h/mL. Following i.m. administration, the mean t(1/2el) and AUC values were 2.94 +/- 0.78 h and 17.21 +/- 4.36 mu g.h/mL. The bioavailability was high (91.76% +/- 12.68%), with a peak plasma mean concentration (C-max) of 2.85 +/- 0.89 mu g/mL attained at 1.56 +/- 0.71 h (T-max). The in vitro protein binding percentage was 27.84%. Calculation of efficacy predictors showed that levofloxacin might have a good therapeutic profile against Gram-negative and Gram-positive bacteria, with an MIC <= 0.1 mu g/mL.