Physical characterization of multiparticulate systems

ABSTRACT The search for new pharmaceutical dosage forms and different drug delivery systems already used in therapeutics is a global trend, serving as an opportunity to expand the portfolio for the pharmaceutical industry. In this context, multiparticulate systems, such as pellets, granules, and minitablets, represent an attractive alternative, given the range of possibilities they provide. Among the methods used in the production of these systems, we highlight the process of extrusion-spheronization for pellet manufacture, wet granulation and hot-melt extrusion for the obtention of granules, and direct compression for minitablets. Although highly versatile, depending on the technology chosen, many processes and formulation variables can influence the ensuing stages of manufacture, as well as the final product. Therefore, the characterization of these small units is of fundamental importance for achieving batch homogeneity and optimal product performance. Analyses, including particle size distribution, morphology, density, porosity, mechanical strength and disintegration, are example tests used in this characterization. The objective of this review was to address the most widely used tests for the physical evaluation of multiparticulate systems.

摘要：寻找已应用于临床治疗领域的新型药物剂型与多样化给药系统是全球行业趋势，同时可为制药企业拓展产品组合提供重要机遇。在此背景下，微丸、颗粒、迷你片剂等多单元给药系统凭借其丰富的应用可能性，成为极具吸引力的替代方案。在这类系统的诸多制备方法中，本文重点提及以下工艺：用于制备微丸的挤出滚圆法、用于制备颗粒的湿法制粒与热熔挤出法，以及用于制备迷你片剂的直接压片法。尽管该类制备技术通用性极强，但根据所选技术的不同，诸多制备工艺与处方变量均会对后续制备步骤及最终产品质量产生影响。因此，对这些微小单元进行表征，对于保障批次均一性与实现产品最优性能至关重要。此类表征常用的检测项目包括：粒径分布、形貌、密度、孔隙率、机械强度与崩解时限。本综述旨在梳理当前用于多单元给药系统物理评价的最常用检测方法。