Department of Pharmaceutics Science, Shenyang Pharmaceutical University, Shenyang 110016, China.
Department of Functional Food and Wine, Shenyang Pharmaceutical University, Shenyang 110016, China.
Int J Pharm. 2022 Sep 25;625:122075. doi: 10.1016/j.ijpharm.2022.122075. Epub 2022 Aug 2.
Microcrystalline cellulose (MCC) is a diluent for oral solid dosage forms. The wet granulation process was selected to prepare losartan potassium tablets using MCC as a model for a predictive study. It was found that the hardness of the tablets could not satisfy the quality standards. In this study, the effect of the high-shear granulation process on the compressibility of MCC was characterized by plotting the compression characteristics curve, as well as the mechanism of the effect from the perspectives of mechanical properties, powder properties. The solid-state properties were also analyzed. Combined with the Heckel equation, the Ryshkewitch-Duckworth equation, the energy method, PXRD, SEM, and other evaluation methods, the results suggest that the high-shear granulation process reduced the compressibility of MCC, which may be caused by the reduced plastic deformation capacity of MCC and the change of the particle morphology structure. The method applied in this study can also be applied to other excipients, which is an important guideline for solving possible problems and process selections during the preparation stage of solid formulations.
微晶纤维素（MCC）是口服固体制剂的稀释剂。选择湿法制粒工艺，以 MCC 为模型进行预测性研究，制备氯沙坦钾片。结果发现片剂的硬度不能满足质量标准。本研究通过绘制压缩特性曲线，从机械性能、粉末性能等方面考察高剪切制粒工艺对 MCC 可压缩性的影响机制。还对其固态性能进行了分析。结合 Heckel 方程、Ryshkewitch-Duckworth 方程、能量法、PXRD、SEM 等评价方法，结果表明，高剪切制粒工艺降低了 MCC 的可压缩性，这可能是由于 MCC 的塑性变形能力降低和颗粒形态结构的变化所致。本研究中应用的方法也可应用于其他赋形剂，这为解决固体制剂制备阶段可能出现的问题和工艺选择提供了重要指导。
