Pharmacokinetics of pefloxacin in pigs after single intramuscular application
2012
Dimitrova, D., Thracian University, Stara Zagora (Bulgaria) | Katsarov, V., Thracian University, Stara Zagora (Bulgaria) | Tsoneva, D., Bulgaria Drug Agency, Sofia (Bulgaria)
Investigation of the pharmacokinetics of pefloxacin and its metabolite norfloxacin after single intramuscular application of pefloxacin mesylate at 10 mg/kg in pigs. The study was performed on eight healthy pigs, about 60 days of age. Blood plasma pefloxacin and norfloxacin concentrations were determined by a validated HPLC assay with UV detection. The primary pharmacokinetic parameters of pefloxacin were calculated by the two-compartmental method, whereas those of norfloxacin – by the non-compartmental method. The pharmacokinetic parameters of pefloxacin - mean±SEM were as followed: elimination half-life – 6.68 0.52 h, mean residence time – 9.71 0.54 h, maximum plasma concentrations – 0.594±0.12 μg/ml, time to reach C – 1/2β max max max 1.14±0.03 h, area under the plasma concentration curve from hour 0 to hour 36 AUC – 6.06±0.18 μg.h/ml. Combined effective plasma concentrations of 0-36 h pefloxacin plus norfloxacin over 0.259 μg/ml were detected until the 12th hour after injection, and levels over 0.06 μg/ml – until the 24th hour. Pefloxacin 5 % solution, applied intramuscularly to pigs at a dose of 10.0 mg/kg resulted in effective plasma antimicrobial concentrations against clinically important bacterial infections for 12–24 h.
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