Biopharmaceutical Characterization of Nebulized Antimicrobial Agents in Rats. 4. Aztreonam

Antimicrob Agents Chemother. 2016 Apr 22;60(5):3196-8. doi: 10.1128/AAC.00165-16. Print 2016 May.

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.

MeSH terms

  • Administration, Inhalation
  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / pharmacology*
  • Anti-Infective Agents / administration & dosage
  • Anti-Infective Agents / pharmacology*
  • Aztreonam / administration & dosage
  • Aztreonam / pharmacology*
  • Lung / drug effects
  • Male
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Aztreonam