Faculty of Pharmaceutical Sciences, Department of Pharmaceutics and Analytical Chemistry, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
J Pharm Sci. 2009 Nov;98(11):3903-32. doi: 10.1002/jps.21735.
Many organic molecules used as drugs can incorporate water into their crystal lattice. These compounds are also prone to processing-induced transformations (PITs) because processing often exposes the compounds to moisture, heat and mechanical stress. The aim of this review is to provide an overview of the possibilities for following and understanding hydrate/anhydrate transformations using vibrational spectroscopy (mid-infrared, near-infrared, Raman and terahertz). The review begins with a general section on hydrates, followed by considerations on the impact of these on drug products and a description of transformation mechanisms of hydrates. Moreover, a general introduction is given for the spectroscopic techniques together with a discussion of critical issues for quantification models. Unit operations that may induce transformations in hydrate systems are discussed with focus on the published work on the use of spectroscopy to derive information from these processes. Finally, the effect of excipients on PITs is discussed.
许多用作药物的有机分子可以将水纳入其晶格。这些化合物也容易发生加工诱导的转变（PIT），因为加工通常会使化合物暴露在水分、热量和机械应力下。本综述的目的是提供使用振动光谱（中红外、近红外、拉曼和太赫兹）来跟踪和理解水合物/无水物转变的可能性概述。该综述首先是一个关于水合物的一般部分，然后是关于这些水合物对药物产品的影响的考虑，以及水合物转变机制的描述。此外，还对光谱技术进行了一般性介绍，并讨论了定量模型的关键问题。讨论了可能引起水合物系统转变的单元操作，并重点介绍了使用光谱从这些过程中获取信息的已发表工作。最后，还讨论了赋形剂对 PIT 的影响。
