Jaffari Sara, Forbes Ben, Collins Elizabeth, Khoo Jiyi, Martin Gary P, Murnane Darragh
Pharm Res. 2014 Dec;31(12):3251-64. doi: 10.1007/s11095-014-1414-3.
To investigate the agglomeration behaviour of the fine (<5.0 μm) and coarse (>12.8 μm) particle fractions of salmeterol xinafoate (SX) and fluticasone propionate (FP) by isolating aerodynamic size fractions and characterising their physicochemical and re-dispersal properties.
Aerodynamic fractionation was conducted using the Next Generation Impactor (NGI). Re-crystallized control particles, unfractionated and fractionated materials were characterized for particle size, morphology, crystallinity and surface energy. Re-dispersal of the particles was assessed using dry dispersion laser diffraction and NGI analysis.
Aerosolized SX and FP particles deposited in the NGI as agglomerates of consistent particle/agglomerate morphology. SX particles depositing on Stages 3 and 5 had higher total surface energy than unfractionated SX, with Stage 5 particles showing the greatest surface energy heterogeneity. FP fractions had comparable surface energy distributions and bulk crystallinity but differences in surface chemistry. SX fractions demonstrated higher bulk disorder than unfractionated and re-crystallized particles. Upon aerosolization, the fractions differed in their intrinsic emission and dispersion into a fine particle fraction (<5.0 μm).
Micronized powders consisted of sub-populations of particles displaying distinct physicochemical and powder dispersal properties compared to the unfractionated bulk material. This may have implications for the efficiency of inhaled drug delivery.
通过分离空气动力学粒径级分并表征其物理化学和再分散特性，研究昔萘酸沙美特罗（SX）和丙酸氟替卡松（FP）的细颗粒（<5.0μm）和粗颗粒（>12.8μm）级分的团聚行为。
使用下一代撞击器（NGI）进行空气动力学分级。对重结晶对照颗粒、未分级和分级后的材料进行粒径、形态、结晶度和表面能表征。使用干式分散激光衍射和NGI分析评估颗粒的再分散情况。
雾化后的SX和FP颗粒以具有一致颗粒/团聚体形态的团聚体形式沉积在NGI中。沉积在第3级和第5级的SX颗粒比未分级的SX具有更高的总表面能，第5级颗粒表现出最大的表面能不均匀性。FP级分具有可比的表面能分布和整体结晶度，但表面化学存在差异。SX级分显示出比未分级和重结晶颗粒更高的整体无序度。雾化后，这些级分在其固有发射和分散成细颗粒级分（<5.0μm）方面存在差异。
与未分级的块状材料相比，微粉化粉末由具有不同物理化学和粉末分散特性的颗粒亚群组成。这可能对吸入药物递送的效率有影响。
