Pharmaceutical Surface Science Research Group, Department of Pharmacy and Pharmacology, University of Bath, Claverton Down, Bath, BA2 7AY, UK.
Pharm Res. 2009 Dec;26(12):2657-66. doi: 10.1007/s11095-009-9982-3. Epub 2009 Sep 26.
Engineering of inhalation particles incorporating, in each individual particle, a combination of a long-acting beta-agonist and a glucocorticosteroid in a pre-determined and constant ratio for delivery via a dry powder inhaler (DPI).
Individual crystalline particles containing both the glucocorticosteroid fluticasone propionate (FP) and long-acting beta-agonist salmeterol (SX) were prepared, in a ratio of 10:1, using the solution atomization and crystallization by sonication (SAX) process. Combination drug particles were characterized by particle size, morphology, crystallinity and aerosolisation efficiency using inertial impaction.
Combination drug particles were spherical and crystalline, with a median diameter of 4.68 +/- 0.01 microm. Aerosolisation of formulations containing combination drug particles resulted in greater uniformity in delivery ratios of both actives across all stages of the impactor before and after storage.
Actives in a pre-determined dose ratio can be crystallised in a single particle using the SAX process.
通过干粉吸入器（DPI）将长效β-激动剂和糖皮质激素以预定的恒定比例结合到吸入颗粒中，从而对吸入颗粒进行工程设计。
使用溶液雾化和超声结晶（SAX）工艺，制备含有糖皮质激素丙酸氟替卡松（FP）和长效β-激动剂沙美特罗（SX）的单个结晶颗粒，两者的比例为 10:1。使用惯性撞击法对组合药物颗粒的粒径、形态、结晶度和空气动力学效率进行了特征描述。
组合药物颗粒为球形且结晶，中值直径为 4.68 ± 0.01 微米。含有组合药物颗粒的制剂的空气动力学化导致在储存前后撞击器的所有阶段中，两种活性剂的输送比例更加均匀。
可以使用 SAX 工艺在单个颗粒中结晶出预定剂量比例的活性剂。
