Biopharmaceutical Characterization of Nebulized Antimicrobial Agents in Rats. 4. Aztreonam
Sandrine Marchand1, Nicolas Grégoire2, Julien Brillault2
1Inserm U1070, Pôle Biologie Santé, Poitiers, France Université de Poitiers, UFR Médecine-Pharmacie, Poitiers, France CHU Poitiers, Service de Toxicologie-Pharmacocinétique, Poitiers, France sandrine.marchand@univ-poitiers.fr.
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.
