부산대학교 도서관

An improved agglomerate formulation with melatonin and fine lactose for dry powder inhalation using Turbuhaler® was developed. Co-grinding lactose with 1 % magnesium stearate prior to air jet mixing served as a key factor to improve the in vitro aerosolization and in vivo efficacy. Elevated mixing pressure facilitated the dispersion and homogenization of the cohesive mixture for even distribution of agglomerate size after spheroidization and subsequent higher emitted dose with lower variation. Magnesium stearate was employed as a tertiary component to adjust the interparticle force for better aerosolization. At optimized mixing pressure, co-grinding lactose with magnesium stearate before jet mixing displayed further improvement of fine particle fraction to 71.6 ± 3.1 %. The superior fine particle deposition efficiency contributed to rapid onset of action and a high bioavailability of 67.0 % after intratracheal administration to rats. Overall, an inhalable melatonin dry powder formulation exhibiting good aerosol property and lung deposition with clinical translation potential was developed. [Display omitted] • Ternary dry powder agglomerate formulation for inhalation was developed. • Air jet mixing efficiently disperses the cohesive mixture for spheroidization. • Elevated mixing pressure contributes to higher emitted dose with lower variation. • The fine particle fraction of 71.6 ± 3.1% for melatonin was achieved. • Rapid onset of action with a bioavailability of 67.0% was realized. [ABSTRACT FROM AUTHOR]