School of Pharmaceutical Chemistry, University of Antioquia, Medellin, Colombia.
Drug Dev Ind Pharm. 2012 Oct;38(10):1159-70. doi: 10.3109/03639045.2011.645833.
It is necessary to have excipients with excellent functional properties to compensate for the poor mechanical properties and low aqueous solubility of the emerging active ingredients. Therefore, around 80% of the current drugs are not suitable for direct compression and more advanced excipients are required. Further, conventional grades of excipients cannot accommodate the technologically advanced high speed rotary tablet presses which require a powder with excellent flow, good compressibility, compactibility, particle size distribution and homogeneity of the ingredients. Co-processed excipients have been created to enhance the functional properties of the excipients and reduce their drawbacks. Co-processing is defined as the combination of two or more excipients by a physical process. Co-processed excipients are adequate for direct compression since they become multifunctional and thus, their dilution potential is high eliminating the need for many excipients in a formulation. In some cases, they are able to hold up to 50% of the drug in a formulation rendering compacts of good tableting properties. This study describes and discusses the functionality enhancement of commercial and investigational excipients through co-processing.
为了弥补新型活性成分机械性能差和水溶性低的缺陷，需要具有优异功能特性的赋形剂。因此，目前大约 80%的药物不适合直接压片，需要更先进的赋形剂。此外，传统等级的赋形剂无法适应技术先进的高速旋转压片机，而高速旋转压片机需要具有优异流动性、良好可压缩性、可压缩性、粒径分布和成分均匀性的粉末。共处理赋形剂的出现是为了增强赋形剂的功能特性并减少其缺点。共处理定义为通过物理过程将两种或多种赋形剂结合在一起。共处理赋形剂适合直接压片，因为它们变成多功能的，因此，它们的稀释潜力很高，在配方中不需要许多赋形剂。在某些情况下，它们能够在配方中容纳高达 50%的药物，从而使片剂具有良好的压片性能。本研究通过共处理描述和讨论了商业和研究用赋形剂的功能增强。
