Biopharmaceutical characterization of nebulized antimicrobial agents in rats. 4. aztreonam

Abstract

The aim of this study was to determine aztreonam (ATM) membrane permeability using Calu-3 cells and its plasma and pulmonary epithelial lining fluid (ELF) pharmacokinetics in rats after intratracheal nebulization and intravenous administration (15 mg · kg-1). ATM exhibits low Calu-3 permeability (0.07 ± 0.02 × 10-6 cm · s-1), and a high area under the ELF/unbound plasma concentration time curve between 0 and infinity (AUCELF/AUCu,plasma) ratio of 1,069 was observed after nebulization in rats. These results confirm that ATM is a low-permeability molecule and a good candidate for nebulization.