Shur Jagdeep, Pitchayajittipong Chonladda, Rogueda Philippe, Price Robert
Department of Pharmacy & Pharmacology, University of Bath, Bath, BA2 7AY, UK.
Ther Deliv. 2013 Aug;4(8):925-37. doi: 10.4155/tde.13.69.
Influence of air-jet micronization, post-micronization conditioning and storage on the surface properties of budesonide in dry-powder inhaler formulations was investigated. Crystalline budesonide was air jet-micronized and conditioned using organic vapor. Particle engineering was also used to fabricate respirable particles of budesonide. Surface imaging by atomic force microscopy suggested that micronized material possessed process-induced surface disorder, which relaxed upon conditioning with organic vapor. Particle engineered material was devoid of such surface disorder. Surface interfacial properties of all batches were different and correlated to in vitro fine particle delivery. The surface properties and in vitro performance of the conditioned material changed upon storage of the budesonide at 44% relative humidity and 25°C, while the micronized and particle-engineered material remained stable. These data suggest that processing conditions of budesonide affected the surface properties of the material, which was demonstrated to have direct affect on dry-powder inhaler formulation performance.
研究了气流微粉化、微粉化后处理及储存对布地奈德干粉吸入剂制剂表面性质的影响。将结晶布地奈德进行气流微粉化，并使用有机蒸汽进行后处理。还采用颗粒工程技术制备了可吸入的布地奈德颗粒。原子力显微镜表面成像表明，微粉化材料具有过程诱导的表面无序，在用有机蒸汽处理后这种无序会缓解。颗粒工程材料没有这种表面无序。所有批次的表面界面性质不同，且与体外细颗粒递送相关。在44%相对湿度和25°C条件下储存布地奈德时，后处理材料的表面性质和体外性能发生了变化，而微粉化和颗粒工程材料保持稳定。这些数据表明，布地奈德的加工条件影响了材料的表面性质，这被证明对干粉吸入剂制剂性能有直接影响。
