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药物共晶、盐和多晶型物:先进的表征技术。

Pharmaceutical cocrystals, salts and polymorphs: Advanced characterization techniques.

机构信息

Medical University of Warsaw, Faculty of Pharmacy with the Laboratory Medicine Division, Department of Inorganic and Analytical Chemistry, Banacha 1, 02-093 Warsaw, Poland.

Medical University of Warsaw, Faculty of Pharmacy with the Laboratory Medicine Division, Department of Inorganic and Analytical Chemistry, Banacha 1, 02-093 Warsaw, Poland.

出版信息

Adv Drug Deliv Rev. 2017 Aug 1;117:111-146. doi: 10.1016/j.addr.2017.09.014. Epub 2017 Sep 18.

Abstract

The main goal of a novel drug development is to obtain it with optimal physiochemical, pharmaceutical and biological properties. Pharmaceutical companies and scientists modify active pharmaceutical ingredients (APIs), which often are cocrystals, salts or carefully selected polymorphs, to improve the properties of a parent drug. To find the best form of a drug, various advanced characterization methods should be used. In this review, we have described such analytical methods, dedicated to solid drug forms. Thus, diffraction, spectroscopic, thermal and also pharmaceutical characterization methods are discussed. They all are necessary to study a solid API in its intrinsic complexity from bulk down to the molecular level, gain information on its structure, properties, purity and possible transformations, and make the characterization efficient, comprehensive and complete. Furthermore, these methods can be used to monitor and investigate physical processes, involved in the drug development, in situ and in real time. The main aim of this paper is to gather information on the current advancements in the analytical methods and highlight their pharmaceutical relevance.

摘要

新药开发的主要目标是获得具有最佳物理化学、药学和生物学性质的药物。制药公司和科学家会修饰原料药(APIs),通常是共晶、盐或精心选择的多晶型物,以改善母体药物的性质。为了找到药物的最佳形式,应使用各种先进的表征方法。在这篇综述中,我们描述了这些专门用于固体药物形式的分析方法。因此,讨论了衍射、光谱、热和药物表征方法。它们都是研究原料药内在复杂性所必需的,从大块到分子水平,获得关于其结构、性质、纯度和可能的转化的信息,并使表征高效、全面和完整。此外,这些方法可用于原位和实时监测和研究药物开发过程中涉及的物理过程。本文的主要目的是收集关于分析方法的最新进展的信息,并强调其在药学方面的相关性。

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