GEA-NUS Pharmaceutical Processing Research Laboratory, Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore.
School of Pharmacy, Monash University Malaysia, Jalan Lagoon Selatan, Bandar Sunway, 47500 Subang Jaya, Selangor, Malaysia.
J Pharm Sci. 2022 Aug;111(8):2158-2171. doi: 10.1016/j.xphs.2022.05.001. Epub 2022 May 6.
The stability of pharmaceuticals is an important product quality attribute. Of the known factors affecting stability, moisture is often perceived as the most common cause of drug degradation by hydrolysis or other reactions facilitated by moisture as a medium. Excipients are a critical entity in formulations to enable drug delivery as well as efficient manufacture of pharmaceutical dosage forms. Yet to this end, there is limited application and understanding of the role of excipients in protecting moisture sensitive drugs. An improved understanding of moisture-excipient interactions is important when selecting excipients for formulations containing moisture sensitive drugs. This review outlines the role of excipients as a moisture protectant in oral solid dosage forms. It focuses on the moisture interactions of excipients in order to highlight the potential of certain excipients as moisture protectants. More specifically, the mechanisms by which excipients can reduce drug degradation (e.g. acting as a physical barrier, reducing moisture availability and mobility) are discussed. A summary of analytical tools to evaluate moisture-excipient interactions is also provided.
药品的稳定性是一个重要的产品质量属性。在已知影响稳定性的因素中，水分通常被认为是最常见的导致药物通过水解或其他反应降解的原因，而这些反应是由水分作为介质促进的。赋形剂是配方中的关键成分，可实现药物输送以及高效制造药物剂型。然而，在这方面，对于赋形剂在保护对湿度敏感的药物方面的作用的应用和理解有限。在选择含有对湿度敏感药物的配方的赋形剂时，更好地了解水分-赋形剂相互作用非常重要。本综述概述了赋形剂在口服固体制剂中作为水分保护剂的作用。它侧重于赋形剂的水分相互作用，以突出某些赋形剂作为水分保护剂的潜力。更具体地说，讨论了赋形剂可以降低药物降解的机制（例如作为物理屏障、减少水分的可用性和迁移性）。还提供了评估水分-赋形剂相互作用的分析工具的摘要。
