Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
J Pharm Sci. 2010 Feb;99(2):969-81. doi: 10.1002/jps.21885.
The objective of this study was to improve the cohesive lactose powder flowability. A cohesive lactose monohydrate powder was processed in either a tumbling blender or an intensive mechanical processor with either magnesium stearate or fumed silica. No substantial changes in particle size were detected by laser diffraction following either treatment. The untreated lactose sample exhibited very poor powder flow. Only limited improvements in powder flowability were indicated after the tumbling blending, intensive mechanical processing with the fumed silica or without additives. However, the intensive mechanical processing of the lactose sample with magnesium stearate demonstrated exceptionally large increases in both poured and tapped density as well as notable improvements in all powder flowability indicators examined. Our findings support the use of intensive mechanical processing technique as an effective method to coat cohesive pharmaceutical powders with selected additives, modify the surface nature of the particles, reduce the interparticle cohesive forces and hence improve powder flowability. The subtle differences in powder flow behaviour of lactose samples between the untreated and tumbling blended powders with magnesium stearate were only detected by the powder rheometer using its dynamic mode, indicating its potential advantages over traditional powder flow characterisation approaches.
本研究旨在改善黏附乳糖粉末的流动性。将黏附乳糖一水合物粉末在翻转式混合机或强化机械处理器中用硬脂酸镁或气相法二氧化硅进行处理。处理后,激光衍射法均未检测到粒径有明显变化。未经处理的乳糖样品表现出极差的粉末流动性。仅在翻转式混合、用气相法二氧化硅或不加添加剂进行强化机械处理后,粉末流动性才有一定程度的改善。然而,用硬脂酸镁对乳糖样品进行强化机械处理则可极大地提高堆密度和振实密度,以及显著改善所有考察的粉末流动性指标。我们的研究结果支持使用强化机械处理技术作为一种有效方法,用选定的添加剂涂覆黏附性药物粉末,改变颗粒表面性质,减少颗粒间的黏附力,从而改善粉末流动性。只有使用粉末流变性仪的动态模式,才能检测到未经处理和用硬脂酸镁翻转式混合的乳糖样品之间的粉末流动性细微差异,这表明其相对于传统的粉末流动特性分析方法具有潜在优势。