Pharmacokinetics of marbofloxacin in horses

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Abstract
Marbofloxacin is a fluoroquinolone antibiotic expected to be effective in the treatment of infections involving Gram‐negative and some Gram‐positive bacteria in horses. In order to design a rational dosage regimen for the substance in horses, the pharmacokinetic properties of marbofloxacin were investigated in 6 horses after i.v., subcutaneous and oral administration of a single dose of 2 mg/kg bwt and the minimal inhibitory concentrations (MIC) assessed forbacteria isolated from equine infectious pathologies. The clearance of marbofloxacin was mean ± s.d. 0.25 ± 0.05 l/kg/h and the terminal half‐life 7.56 ± 1.99 h. The marbofloxacin absolute bioavailabilities after subcutaneous and oral administration were 98 ± 11% and 62 ± 8%, respectively. The MIC required to inhibit 90% of isolates (MIC90) was 0.027 μg/ml for enterobacteriaceae and 0.21 μg/ml for Staphylococcus aureus. The values of surrogate markers of antimicrobial efficacy (AUIC, Cmax/MIC ratio, time above MIC90) were calculated and the marbofloxacin concentration profiles simulated for repeated administrations. These data were used to determine rational dosage regimens for target bacteria. Considering the breakpoint values of efficacy indices for fluoroquinolones, a marbofloxacin dosage regimen of 2 mg/kg bwt/24 h by i.v., subcutaneous or oral routes was more appropriate for enterobacteriaceae than for S. aureus.

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