Abstract
The objective of this study was to determine the pharmacokinetics of tildipirosin in rabbits after a single intravenous (i.v.) and intramuscular (i.m.) injection at a dose of 4mg/kg. Twelve white New Zealand rabbits were assigned to a randomized, parallel trial design. Blood samples were collected prior to administration and up to 14days postadministration. Plasma concentrations of tildipirosin were quantified using a validated ultra-high-performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method. The pharmacokinetic parameters were calculated using a noncompartmental model in WinNonlin 5.2 software. Following i.v. and i.m. administration, the elimination half-life (T1/2λ ) was 81.17±9.28 and 96.68±15.37hr, respectively, and the mean residence time (MRTlast ) was 65.44±10.89 and 67.06±10.49hr, respectively. After i.v. injection, the plasma clearance rate (Cl) and volume of distribution at steady state (Vdss ) were 0.28±0.10 Lkg-1 h-1 and 17.78±5.15L/kg, respectively. The maximum plasma concentration (Cmax ) and time to reach maximum plasma concentration (Tmax ) after i.m. administration were 836.2±117.9ng/ml and 0.33±0.17hr, respectively. The absolute bioavailability of i.m. administration was 105.4%. Tildipirosin shows favorable pharmacokinetic characteristics in rabbits, with fast absorption, extensive distribution, and high bioavailability. These findings suggest that tildipirosin might be a potential drug for the prevention and treatment of respiratory diseases in rabbits.
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