Pharmacokinetics of gamithromycin after intravenous and subcutaneous administration in pigs

The aim of this study was to investigate the pharmacokinetic properties of gamithromycin in pigs after an intravenous (i.v.) or subcutaneous (s.c.) bolus injection of 6 mg/kg body weight. The plasma concentrations of gamithromycin were determined using a validated high-performance liquid chromatography-tandem mass spectrometry method, and the pharmacokinetics were noncompartmentally analysed. Following i.v. administration, the mean area under the plasma concentration-time curve extrapolated to infinity (AUC(inf)) and the mean elimination half-life (t(1/2 lambda z)) were 3.67 +/- 0.75 mu g.h/mL and 16.03 h, respectively. The volume of distribution at steady state (V-ss) and the plasma clearance were 31.03 +/- 6.68 L/kg and 1.69 +/- 0.33 L/h.kg, respectively. The mean residence time (MRTinf) was 18.84 +/- 4.94 h. Gamithromycin administered subcutaneously to pigs demonstrated a rapid and complete absorption, with a mean maximal plasma concentration (C-max) of 0.41 +/- 0.090 mu g/ml at 0.63 +/- 0.21 h and a high absolute bioavailability of 118%. None of the reported pharmacokinetic variables significantly differed between both administration routes. (C) 2013 Elsevier Ltd. All rights reserved.