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利用快速扫描量热法对熔融时降解的药物化合物进行玻璃态表征。

Vitreous State Characterization of Pharmaceutical Compounds Degrading upon Melting by Using Fast Scanning Calorimetry.

作者信息

Corvis Yohann, Wurm Andreas, Schick Christoph, Espeau Philippe

机构信息

†Unité de Technologies Chimiques et Biologiques pour la Santé, Inserm U 1022 CNRS UMR 8258, Faculté des Sciences Pharmaceutiques et Biologiques, Université Paris Descartes, Sorbonne Paris Cité, 4 avenue de l'Observatoire, 75006 Paris, France.

‡Institut für Physik, Universität Rostock, Wismarsche Strasse 43-45, 18051 Rostock, Germany.

出版信息

J Phys Chem B. 2015 Jun 4;119(22):6848-51. doi: 10.1021/acs.jpcb.5b03041. Epub 2015 May 20.

Abstract

Fast scanning calorimetry, a technique mainly devoted to polymer characterization, is applied here for the first time to low molecular mass organic compounds that degrade upon melting, such as ascorbic acid and prednisolone. Due to the fast scan rates upon heating and cooling, the substances can be obtained in the molten state without degradation and then quenched into the glassy state. The hydrated form and the polymorphic Form 1 of prednisolone were investigated. It is shown that once the sesquihydrate dehydrates, a molten product is obtained. Depending on the heating rate, this molten phase may recrystallize or not into Form 1.

摘要

快速扫描量热法主要用于聚合物表征,在此首次应用于在熔化时会降解的低分子量有机化合物,如抗坏血酸和泼尼松龙。由于加热和冷却时的快速扫描速率,这些物质可以在不降解的情况下获得熔融态,然后骤冷成玻璃态。对泼尼松龙的水合形式和多晶型物晶型1进行了研究。结果表明,一旦倍半水合物脱水,就会得到一种熔融产物。根据加热速率的不同,这种熔融相可能会重结晶为晶型1,也可能不会。

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