Charpentier Paul A, Jia Ming, Lucky Rahima A
Department of Chemical and Biochemical Engineering, University of Western Ontario, N6A 5B9, London, Ontario, Canada.
AAPS PharmSciTech. 2008;9(1):39-46. doi: 10.1208/s12249-007-9004-x. Epub 2008 Jan 8.
The purpose of this research was to micronize beclomethasone-17,21-dipropionate (BDP), an anti-inflammatory inhaled corticosteroid commonly used to treat asthma, using the rapid expansion of supercritical solution (RESS) technique. The RESS technique was chosen for its ability to produce both micron particles of high purity for inhalation, and submicron/nano particles as a powder handling aid for use in next generation dry powder inhalers (DPIs). Particle formation experiments were carried out with a capillary RESS system to determine the effect of experimental conditions on the particle size distribution (PSD). The results indicated that the RESS process conditions strongly influenced the particle size and morphology; with the BDP mean particle size decreasing to sub-micron and nanometer dimensions. An increase in the following parameters, i.e. nozzle diameter, BDP mol fraction, system pressure, and system temperature; led to larger particle sizes. Aerodynamic diameters were estimated from the SEM data using three separate relations, which showed that the RESS technique is promising to produce particles suitable for pulmonary delivery.
本研究的目的是使用超临界溶液快速膨胀（RESS）技术将倍氯米松-17,21-二丙酸酯（BDP）微粉化，BDP是一种常用于治疗哮喘的抗炎吸入性皮质类固醇。选择RESS技术是因为它既能生产用于吸入的高纯度微米颗粒，又能生产作为下一代干粉吸入器（DPI）粉末处理助剂的亚微米/纳米颗粒。使用毛细管RESS系统进行颗粒形成实验，以确定实验条件对粒度分布（PSD）的影响。结果表明，RESS工艺条件对颗粒尺寸和形态有很大影响；BDP平均粒径减小至亚微米和纳米尺寸。以下参数的增加，即喷嘴直径、BDP摩尔分数、系统压力和系统温度，导致颗粒尺寸增大。使用三种不同的关系从扫描电子显微镜数据估计空气动力学直径，结果表明RESS技术有望生产出适合肺部给药的颗粒。
