Ishizaka T, Honda H, Kikuchi Y, Ono K, Katano T, Koishi M
Faculty of Pharmaceutical Sciences, Science University of Tokyo, Japan.
J Pharm Pharmacol. 1989 Jun;41(6):361-8. doi: 10.1111/j.2042-7158.1989.tb06478.x.
New hybrid powders have been produced by the dry processing of six drugs (oxyphenbutazone, prednisolone, theophylline, indomethacin, phenacetin and aspirin), with potato starch used as a core material, by means of an electric mortar and a powder surface reforming system designed to produce hybrid powders. The hybrid powders obtained immediately after production differed in their structure from interactive mixtures. With the hybrid powders the drug was spread on the surface of the core particle by friction and collision that occurred in the dry process, but with interactive mixtures the drug simply adhered as intact particles to the surface of diluent particles. Scanning electron microscopy and powder X-ray diffractometry indicated that the mechanochemical phenomenon was essential for the production of the hybrid powders. With time, a shape change in the adhering drug was observed as a relaxation process took place, with recrystallization resulting from the release of accumulated energy. The change with time might depend upon the method of producing powders and the physical properties of the drug used, e.g. the smooth layer of indomethacin produced by the powder surface reforming system reverted to fine particles tightly adhering to the starch surface, though no change was observed with prednisolone.
通过使用电动研钵和旨在生产混合粉末的粉末表面改性系统，以马铃薯淀粉为核心材料，对六种药物（羟苯丁酮、泼尼松龙、茶碱、吲哚美辛、非那西丁和阿司匹林）进行干法处理，制备出了新型混合粉末。生产后立即获得的混合粉末在结构上与相互作用混合物不同。对于混合粉末，药物通过干法过程中发生的摩擦和碰撞散布在核心颗粒表面，但对于相互作用混合物，药物只是作为完整颗粒附着在稀释剂颗粒表面。扫描电子显微镜和粉末X射线衍射表明，机械化学现象对于混合粉末的生产至关重要。随着时间的推移，随着弛豫过程的发生，观察到附着药物的形状发生变化，积累能量的释放导致了重结晶。随时间的变化可能取决于粉末的生产方法和所用药物的物理性质，例如，粉末表面改性系统产生的吲哚美辛光滑层恢复为紧密附着在淀粉表面的细颗粒，而泼尼松龙则未观察到变化。
