High azithromycin loading powders for inhalation and their in vivo evaluation in rats

摘要: The aim of the present work is to develop high azithromycin loading powders for inhalation with optimal physical and aerodynamic properties, test their in vivo potential rats. A five-level three-factorial central composite rotatable design was used conducting experiments. optimized powder, which had a better flowability, an diameter 3.82 microm vitro deposition 51%, obtained under selected spray-drying conditions. content powder (59.2%), met requirement drug loading. further examined study Lung microdialysis blood were simultaneously performed on each rat. ratio AUC(ELF) value between intratracheal route intravenous injection 161.6, whereas absolute bioavailability only 43.5%, targeting index 486.2. results showed that dry inhalers (DPI) could be effectively efficiently delivered specific target site achieve local concentration. In conclusion, AZI DPI offers attractive alternative able deliver concentrations antibiotic directly chosen while minimizing systemic side effects.