Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Universitaetsstr. 1, 40225 Duesseldorf, Germany.
Int J Pharm. 2010 May 10;390(2):117-27. doi: 10.1016/j.ijpharm.2009.12.062. Epub 2010 Jan 25.
The compression behavior of high- and low drug strength pellets containing kappa-carrageenan as pelletisation aid was investigated. Model drugs and fillers with different compression mechanisms were used and the effects of compression force and turret speed were examined. Regardless of the compression behavior of their starting components, all pellet formulations exhibited minimal to absent fragmentation and underwent compression by deformation, confirmed by increased equivalent diameter and aspect ratio and decreased roundness factor of the pellets retrieved after de-aggregation of tablets prepared from lubricated pellets. The retrieved pellets showed also higher fracture resistance in three of the tested formulations and no statistically significant difference in the remaining one thus excluding significant crack formation. A densification mechanism was suggested by decreased total porosity and reduced median pore radius of the compressed pellets. No effect of the process parameters on the degree of pellet deformation was reported. The tensile strength of the tablets prepared from unlubricated pellets increased slightly with increased compression force. Compression of pellets with high density silicified microcrystalline cellulose (SMCC HD 90) as embedding powder protected them from severe deformation and resulted in tablets with sufficient tensile strength, minimal friability, negligible elastic recovery and short disintegration time. The percentage of the pellets and the compression force affected the tensile strength of the prepared tablets whereas no influence of the turret speed and the pre-compression force was observed.
考察了作为制粒助剂的κ-卡拉胶的高、低药物强度丸芯的压缩行为。使用了具有不同压缩机制的模型药物和赋形剂,并考察了压缩力和转塔速度的影响。无论起始成分的压缩行为如何,所有丸剂配方均表现出最小至不存在的碎片化,并通过变形进行压缩,这通过从经润滑丸剂制备的片剂的解聚中回收的丸剂的等效直径和纵横比增加以及圆度因子降低得到证实。在测试的三个配方中,回收的丸剂还表现出更高的断裂阻力,而在另一个配方中没有统计学上的显著差异,从而排除了明显的裂纹形成。通过压缩丸剂的总孔隙率降低和中值孔径减小,提出了致密化机制。过程参数对丸剂变形程度没有影响。未润滑丸剂制备的片剂的拉伸强度随压缩力的增加略有增加。高密硅化微晶纤维素(SMCC HD 90)作为嵌入粉末的丸芯的压缩保护它们免受严重变形,并导致片剂具有足够的拉伸强度、最小的脆性、可忽略的弹性回复和短的崩解时间。丸剂的百分比和压缩力影响所制备片剂的拉伸强度,而转塔速度和预压缩力没有影响。