Investigation of L-leucine in reducing the moisture-induced deterioration of spray-dried salbutamol sulfate power for inhalation
| Autor: | Thomas R. Gengenbach, Hak-Kim Chan, Patricia Tang, Jiaqi Yu, Qi Tony Zhou, Ge Fiona Gao, Liang Li, Sharon S.Y. Leung |
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| Rok vydání: | 2017 |
| Předmět: |
Recrystallization (geology)
Materials science Chemistry Pharmaceutical Pharmaceutical Science Excipient Mineralogy 02 engineering and technology 030226 pharmacology & pharmacy 03 medical and health sciences 0302 clinical medicine Leucine Administration Inhalation medicine Albuterol Particle Size Aerosolization Aerosols Moisture 021001 nanoscience & nanotechnology Spray drying Particle Desiccator Powders 0210 nano-technology Mass fraction medicine.drug Nuclear chemistry |
| Zdroj: | International Journal of Pharmaceutics. 530:30-39 |
| ISSN: | 0378-5173 |
| Popis: | The aim of this study was to investigate the ability of L-leucine (LL) in preventing moisture-induced deterioration in the in vitro aerosolization performance of spray-dried (SD) salbutamol sulfate (SS). Increasing mass fraction of LL (5-80%) were co-spray dried with SS, and the physicochemical properties of the powders were characterized by laser diffraction, X-ray powder diffraction (XRD) and dynamic vapour sorption (DVS). Furthermore, the surface morphology and chemistry of fine particles was analyzed by scanning electron microscopy (SEM) and X-ray photoelectron spectroscopy (XPS). The in vitro aerosolization performance of powders stored at different relative humidity (RH) was evaluated by a next generation impactor (NGI). The SD SS powders were moderately hygroscopic and amorphous, of which the uptake of moisture upon storage caused a drop in the aerosolization performance. The results showed that 40% (w/w) LL was sufficient to eliminate the effect of moisture on the aerosolization performance at 60% RH. The formulation containing 40% (w/w) LL also maximized the aerosolization performance of SD SS powders (stored in desiccator) with the emitted fraction being 90.0±1.8%, and the fine particle fraction based on the recovered dose (FPFrecovered) and emitted dose (FPFemitted) being 78.0±3.7% and 86.6±2.9%, respectively. The underlying mechanisms were that the crystalline LL increased the degree of particle surface corrugation, and reduced particle fusion and cohesiveness to facilitate dispersion. However, there is still a great challenge to prevent the moisture-induced deterioration in the aerosolization performance at 75% RH due to the recrystallization of SD SS. In conclusion, LL is a potential excipient for reducing moisture-induced deterioration in the aerosolization performance of SD amorphous powders, but still has drawbacks in preventing the recrystallization-induced deterioration. |
| Databáze: | OpenAIRE |
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