Ferrari Franca, Cocconi Daniela, Bettini Ruggero, Giordano Ferdinando, Santi Patrizia, Tobyn Michael, Price Robert, Young Paul, Caramella Carla, Colombo Paolo
Dipartimento Farmaceutico, University of Parma, Viale delle Scienze, 43100 Parma, Italy.
AAPS PharmSciTech. 2004 Sep 8;5(4):e60. doi: 10.1208/pt050460.
The surface morphology of a-lactose monohydrate particles was modified by a new wet-smoothing process performed in a high-shear mixer using solvents. Successive steps of wetting and drying of lactose powders during rolling in the mixer's cylindrical bowl were performed. Smoothed particles were tested for size distribution, flow, and packing. The wet-smoothing process flattened the surface and rounded the edges of lactose particles. In comparison with original lactose, an improvement of powder packing and flow properties was evidenced. When the process was performed in the presence of a ternary agent such as magnesium stearate, the smoothing was improved. The evolution of rugosity during the smoothing process was assessed through a fractal descriptor of SEM picture. Atomic force microscopy and surface area measurements quantified the surface rugosity. A very significant reduction of the rugosity, more remarkable in the presence of magnesium stearate, was measured. This new process of powder wet-smoothing allows the preparation of lactose particles with different degrees of smoothed surface for the control of flow and packing properties and particle-particle interactions.
采用一种在高剪切混合器中使用溶剂进行的新型湿法平滑工艺,对一水合α-乳糖颗粒的表面形态进行了改性。在混合器的圆柱形料斗中滚动时,对乳糖粉末进行了连续的润湿和干燥步骤。对平滑后的颗粒进行了粒度分布、流动性和堆积性测试。湿法平滑工艺使乳糖颗粒的表面变平,边缘变圆。与原始乳糖相比,粉末的堆积性和流动性能得到了改善。当该工艺在硬脂酸镁等三元试剂存在下进行时,平滑效果得到了改善。通过扫描电子显微镜(SEM)图像的分形描述符评估了平滑过程中粗糙度的变化。原子力显微镜和表面积测量对表面粗糙度进行了量化。测量发现粗糙度显著降低,在硬脂酸镁存在的情况下更为明显。这种新型的粉末湿法平滑工艺能够制备具有不同程度平滑表面的乳糖颗粒,以控制流动性、堆积性以及颗粒间的相互作用。