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从倍半水合物的水合-脱水机制研究中获得的泼尼松龙新晶相的证据。

Evidence of a New Crystalline Phase of Prednisolone Obtained from the Study of the Hydration-Dehydration Mechanisms of the Sesquihydrate.

作者信息

Lemercier Aurélien, Couvrat Nicolas, Cartigny Yohann, Sanselme Morgane, Corvis Yohann, Espeau Philippe, Coquerel Gérard

机构信息

SMS, UR 3233, Université Rouen Normandie, 76000 Rouen, France.

CNRS, INSERM, UTCBS, Chemical and Biological Technologies for Health Group, Université Paris Cité, 75006 Paris, France.

出版信息

Pharmaceutics. 2023 Jun 9;15(6):1694. doi: 10.3390/pharmaceutics15061694.

DOI:10.3390/pharmaceutics15061694
PMID:37376142
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10301155/
Abstract

The dehydration of prednisolone sesquihydrate is studied and characterized by different physico-chemical analysis methods. The meticulous study of this dehydration led to the highlighting of a new solid form (form 3), metastable, never identified before. In a second step, the rehydration of anhydrous forms 1 and 2 of prednisolone is studied, in particular by Dynamic Vapor Sorption. It is then demonstrated that neither of the two forms is sensitive to humidity. By means of solid-gas equilibria, the sesquihydrate can only be obtainable from the isomorphic anhydrous form. Finally, a classification of the sesquihydrate is made, taking into account, in particular, the activation energy determined during dehydration.

摘要

通过不同的物理化学分析方法对泼尼松龙倍半水合物的脱水过程进行了研究和表征。对该脱水过程的细致研究揭示了一种新的固体形态（形态3），它是亚稳态的，之前从未被识别过。在第二步中，研究了泼尼松龙无水形态1和2的再水化过程，特别是通过动态蒸汽吸附法进行研究。结果表明，这两种形态对湿度均不敏感。借助固气平衡，倍半水合物只能从同构无水形态获得。最后，对倍半水合物进行了分类，尤其考虑了脱水过程中测定的活化能。

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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/43ed/10301155/dc6983440af1/pharmaceutics-15-01694-g011.jpg

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