Comparison of salmeterol xinafoate microparticle production by conventional and novel antisolvent crystallization
作者： Darragh Murnane , Christopher Marriott , Gary P. Martin
DOI: 10.1016/J.EJPB.2007.09.016
关键词: Particle size 、 Differential scanning calorimetry 、 Crystallization 、 Supersaturation 、 Polyethylene glycol 、 PEG 400 、 Chemical engineering 、 Organic chemistry 、 PEG ratio 、 Microparticle 、 Materials science
摘要: Abstract The production of microparticles for inhalation has relied on jet-milling while the potential crystallization remained underexplored until relatively recently. Aqueous antisolvent salmeterol xinafoate (SX) from poly(ethylene glycol) (PEG) and other organic (co)solvent systems was compared in order to evaluate factors determining resultant microparticle properties. SX crystallized by addition water solutions PEG 400, 6000, propan-2-ol, acetone methanol. Crystalline particles were characterized laser diffraction sizing, scanning electron microscopy differential calorimetry; PEG-media viscometry. Crystallization 400 produced crystals that exhibited a narrower size distribution than those conventional solvents. 6000 demonstrated smaller median particle ( D v ,0.5) = 0.92 ± 0.04 μm) = 4.50 ± 0.61 μm). Crystals (Span = 2.49 ± 0.10) possessed (PSD) (Span = 10.42 ± 0.85). displayed plate-like habit with growth limited two dimensions irrespective initial solvent employed. importance rate generation supersaturation PSD determined using HPLC analysis. DSC showed PEG-crystallized be free metastable crystal phases contrast propan-2-ol. shown follow classical nucleation theory method represents viable alternative use solvents microparticles.
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