Sunderland Pharmacy School, Sunderland University, UK.
Int J Pharm. 2012 Sep 15;434(1-2):175-82. doi: 10.1016/j.ijpharm.2012.05.050. Epub 2012 May 30.
The aim of this work was to produce pellets using a standard formulation by means of extrusion and spheronization. Three different spheroniser friction plate patterns (i.e. cross-hatch, radial, striated edge pattern) have been used in order to investigate whether the plate pattern affects physical properties of the pellets such as pellet size distribution, yield, shape, mechanical strength, density and drug dissolution. Extrusion was performed with a screen extruder and the screen size was varied to determine whether the extrudate produced could affect the physical properties of pellets. The plate load was also varied. Diclofenac sodium was chosen as a model drug. The pattern of the friction plate used in the spheronization of extrudates affected the properties of the pellets. Yield values varied by up to 20%, and for an otherwise optimised formulation the use of a striated edge plate appeared advantageous in this respect. However, these pellets had a reduced mechanical strength despite their lower porosity, which might be disadvantageous. In addition, other factors such as the amount of extrudate loaded into the spheroniser, the maintenance of a constant moisture content within the spheroniser and the size of the extruder screen influenced these findings significantly. The only physical property of the pellets that did not respond to the various changes in the manufacturing process of the pellets is the pellet shape, which remained spherical. The dissolution of the drug appeared to be related to the median pellet size and was only marginally affected by changes in the spheronization process.
本工作旨在通过挤出和滚圆法使用标准配方制备丸粒。为了研究摩擦板的图案是否会影响丸粒的物理性质，如丸粒的粒径分布、收率、形状、机械强度、密度和药物溶出度，使用了三种不同的滚圆机摩擦板图案（即交叉、放射状、条纹边缘图案）。挤出是在筛式挤出机中进行的，并且改变了筛网的尺寸，以确定挤出物是否会影响丸粒的物理性质。还改变了板载。选择双氯芬酸钠作为模型药物。在挤出物的滚圆过程中使用的摩擦板图案会影响丸粒的性质。收率值变化高达 20%，对于优化的配方，使用条纹边缘板在这方面似乎有利。然而，尽管这些丸粒的孔隙率较低，但它们的机械强度降低，这可能是不利的。此外，其他因素，如装入滚圆机的挤出物的量、滚圆机内保持恒定的水分含量以及挤出机筛网的尺寸，对这些发现有显著影响。唯一对丸粒制造过程中的各种变化不敏感的丸粒物理性质是丸粒的形状，其保持球形。药物的溶出似乎与中值丸粒粒径有关，并且受滚圆过程变化的影响很小。
