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制备了丙酸倍氯米松醋酸乙酯溶剂化物(1)及其微粉,用以制备丙酸倍氯米松混悬型气雾剂。分别对1及微粉的理化性质和制备的气雾剂的行为进行了考察。X衍射、热重分析及红外光谱测定结果证实醋酸乙酯以结合形式存在于1中。EtOAc/1结合百分比约为9%。采用微粉化工艺制得3批样品的粒径分别为1.68±0.62、2.34±1.63、2.44±0.56μm。且微粉化过程无结合溶剂损失及晶型转化发生。外冲程实验表明,该气雾剂在肺深部的沉积达45%以上。
Beclomethasone acetate ethyl acetate solvate (1) and its fine powder were prepared for the preparation of beclomethasone propionate aerosol. The physical and chemical properties of 1 and the micropowder and the prepared aerosol behavior were investigated respectively. X-ray diffraction, thermogravimetric analysis and infrared spectroscopy confirmed that ethyl acetate was present in the bound form. The EtOAc / 1 binding percentage is about 9%. The particle size of three batches of samples obtained by the micronization process were 1.68 ± 0.62, 2.34 ± 1.63 and 2.44 ± 0.56μm, respectively. And the micronization process without loss of solvent and crystalline conversion occurs. External stroke experiments show that the aerosol deposition in the deep lung more than 45%.