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从实际角度看对映异构相关多晶型转变的可逆性:动力学可逆/不可逆多晶型转变的热分析

Reversibility of enantiotropically related polymorphic transformations from a practical viewpoint: thermal analysis of kinetically reversible/irreversible polymorphic transformations.

作者信息

Kawakami Kohsaku

机构信息

Banyu Tsukuba Research Institute, PreClinical Development, 3 Okubo, Tsukuba, Ibaraki 300-2611, Japan.

出版信息

J Pharm Sci. 2007 May;96(5):982-9. doi: 10.1002/jps.20748.

Abstract

Although enantiotropically related polymorphic transitions are thermodynamically reversible with temperature and pressure, they may be observed as either reversible or irreversible in practical investigations. This behavior may be explained simply by a difference in the energy barrier for the transition. However, this difference may have a significant effect on strategy in formulation development. This article summarizes the characteristics of enantiotropic transitions with reference to the literature. Also provided are careful investigations of polymorphic transitions by thermal analysis, which is the most promising method to investigate transition behavior.

摘要

尽管对映变体相关的多晶型转变在热力学上随温度和压力是可逆的,但在实际研究中,它们可能被观察为可逆或不可逆的。这种行为可以简单地用转变的能垒差异来解释。然而,这种差异可能对制剂开发策略有重大影响。本文参考文献总结了对映体转变的特征。还提供了通过热分析对多晶型转变的详细研究,热分析是研究转变行为最有前景的方法。

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