Penetration of amoxycillin into the respiratory tract tissues and secretions in pigs

Abstract

The pharmacokinetic properties of amoxycillin, and its penetration into respiratory tract tissues (alveolar macrophages, bronchial secretions, bronchial mucosa, lung tissue and lymph nodes), were determined in 20 healthy female pigs weighing 29 to 55 kg, after a single intravenous dose of 8·6 mg kg −1 bodyweight. Following intravenous administration the plasma concentration-time curves were best described by a three-compartment open model. The elimination half-life and the mean residence time were 2·5 and 1.4 hours, respectively. The volume of distribution at steady state was 0·52 litres kg −1, and the body clearance was 0·40 litres hour −1 kg −1. In all structures (except alveolar macrophages) amoxycillin concentration peaked at the first sampling point, one hour after drug administration. The tissue to plasma ratio (based on AUC values) were 0·33 for bronchial secretions, 0·37 for bronchial mucosa, 0·39 for lung tissue and 0·68 for lymph nodes. Traces of amoxycillin were found in alveolar macrophages, but the concentrations were below the limit of quantification. The concentration of amoxycillin in secretions and tissue decreased by a slower rate than the concentration in plasma, resulting in increasing secretion- and tissue-to-plasma concentration ratios.