Advanced Drug Delivery Group, Sydney Pharmacy School, Faculty of Medicine and Health, Pharmacy and Bank Building A15, The University of Sydney, NSW 2006, Australia.
Advanced Drug Delivery Group, Sydney Pharmacy School, Faculty of Medicine and Health, Pharmacy and Bank Building A15, The University of Sydney, NSW 2006, Australia; School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.
Int J Pharm. 2022 Jan 5;611:121341. doi: 10.1016/j.ijpharm.2021.121341. Epub 2021 Dec 2.
Raman spectroscopy was used to evaluate the effects of temperature and humidity on the physicochemical stability of inhalable spray-dried (SD) powders containing budesonide (BUD) and crystalline or amorphous lactose. Powders prepared by spray drying of BUD-lactose solution or suspension containing lactose crystals in BUD solution were stored for 0, 1 and 7 days at 25 °C/60 RH or 40 °C/75 RH. Bulk powders along with the large and small particle size fractions collected on stages 2 and 5, respectively, of the Next Generation Impactor (NGI) were chemically characterised. SD powder from solution contained BUD and lactose in amorphous form and both components were homogeneously distributed in bulk and in the particles collected from the two NGI stages. In contrast, SD powder from suspension showed heterogeneous distribution of lactose and drug in the particles containing crystalline lactose. After 1 day of storage at either condition, recrystallisation and changes in the chemical composition of the particles for the SD powder from solution occurred. The number of drug-only particles increased by 70 on stage 5, whereas most particles on stage 2 still contained both drug and lactose. These changes were not observed in the SD powder from suspension after storage, confirming superior stability of the SD powder obtained from suspension.
拉曼光谱用于评估温度和湿度对含有布地奈德（BUD）和结晶或无定形乳糖的可吸入喷雾干燥（SD）粉末理化稳定性的影响。通过喷雾干燥 BUD-乳糖溶液或含有 BUD 溶液中乳糖晶体的悬浮液制备的粉末，在 25°C/60%RH 或 40°C/75%RH 下储存 0、1 和 7 天。对散装粉末以及分别在下一代撞击器（NGI）的第 2 级和第 5 级上收集的大粒径和小粒径级分进行化学表征。来自溶液的 SD 粉末含有无定形形式的 BUD 和乳糖，两种成分在散装和从两个 NGI 级分收集的颗粒中均匀分布。相比之下，来自悬浮液的 SD 粉末显示出含有结晶乳糖的颗粒中乳糖和药物的不均匀分布。在任何条件下储存 1 天后，来自溶液的 SD 粉末的颗粒发生再结晶和化学成分变化。第 5 级的仅含药物的颗粒数量增加了 70%，而第 2 级的大多数颗粒仍含有药物和乳糖。在悬浮液的 SD 粉末储存后没有观察到这些变化，证实了悬浮液获得的 SD 粉末具有更好的稳定性。
