Department of Chemistry, Umeå University, Sweden.
Int J Pharm. 2011 Sep 15;416(1):110-9. doi: 10.1016/j.ijpharm.2011.06.018. Epub 2011 Jun 17.
Roll compaction is gaining importance in pharmaceutical industry for the dry granulation of heat or moisture sensitive powder blends with poor flowing properties prior to tabletting. We studied the influence of microcrystalline cellulose (MCC) properties on the roll compaction process and the consecutive steps in tablet manufacturing. Four dissimilar MCC grades, selected by subjecting their physical characteristics to principal components analysis, and three speed ratios, i.e. the ratio of the feed screw speed and the roll speed of the roll compactor, were included in a full factorial design. Orthogonal projection to latent structures was then used to model the properties of the resulting roll compacted products (ribbons, granules and tablets) as a function of the physical MCC properties and the speed ratio. This modified version of partial least squares regression separates variation in the design correlated to the considered response from the variation orthogonal to that response. The contributions of the MCC properties and the speed ratio to the predictive and orthogonal components of the models were used to evaluate the effect of the design variation. The models indicated that several MCC properties, e.g. bulk density and compressibility, affected all granule and tablet properties, but only one studied ribbon property: porosity. After roll compaction, Ceolus KG 1000 resulted in tablets with obvious higher tensile strength and lower disintegration time compared to the other MCC grades. This study confirmed that the particle size increase caused by roll compaction is highly responsible for the tensile strength decrease of the tablets.
辊压法在制药工业中越来越重要，它可以用于对热敏感或湿敏感且流动性差的粉末混合物进行干法制粒，然后再进行压片。我们研究了微晶纤维素 (MCC) 的性质对辊压过程和随后的片剂制造步骤的影响。我们通过对物理特性进行主成分分析，选择了四种不同的 MCC 等级，并包含三种速度比（进料螺杆速度与辊压辊速度的比值）进行全因子设计。然后，我们使用正交投影到潜在结构来模拟得到的辊压产品（带、颗粒和片剂）的性质，将其作为 MCC 物理性质和速度比的函数。这种偏最小二乘回归的改进版本将与考虑的响应相关的设计变化与正交于该响应的变化分开。使用 MCC 性质和速度比的贡献来评估设计变化的影响。模型表明，几个 MCC 性质，例如堆密度和可压缩性，会影响所有颗粒和片剂的性质，但仅研究了一个带的性质：孔隙率。经过辊压后，与其他 MCC 等级相比，Celus KG 1000 会使片剂具有明显更高的拉伸强度和更低的崩解时间。这项研究证实，辊压引起的粒径增加是片剂拉伸强度降低的主要原因。
