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

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

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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 (Cltot) was 0.21 ± 0.18 L ⁄h⁄kg, and the areas under the concentration–time curves (AUCs) were 18.79 ± 4.57 lg.h⁄mL. Following i.m. administration, the mean t1 ⁄ 2el and AUC values were 2.94 ± 0.78 h and 17.21 ± 4.36 lg.h⁄mL. The bioavailability was high (91.76% ± 12.68%), with a peak plasma mean concentration (Cmax) of 2.85 ± 0.89 lg ⁄mL attained at 1.56 ± 0.71 h (Tmax). The in vitro protein binding percentage was 27.84%. Calculation of efficacy predictors showed that levofloxacin might have a good therapeutic profile against Gramnegative and Gram-positive bacteria, with an MIC £ 0.1 lg ⁄mL.


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