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乳果糖:用于研究研磨诱导的固体无定形化的模型体系。

Lactulose: A Model System to Investigate Solid State Amorphization Induced by Milling.

机构信息

Université Lille Nord de France, Unité Matériaux et Transformations, Villeneuve d'Ascq, France; Institut Laue Langevin, Grenoble, France.

Université Lille Nord de France, Unité Matériaux et Transformations, Villeneuve d'Ascq, France.

出版信息

J Pharm Sci. 2019 Feb;108(2):880-887. doi: 10.1016/j.xphs.2018.09.013. Epub 2018 Sep 19.

Abstract

In this article, we show that crystalline lactulose can be amorphized directly in the solid state by mechanical milling. Moreover, compared to similar materials, the amorphization kinetics of lactulose is found to be very rapid and the amorphous state thus obtained appears to be very stable against recrystallization on heating. These features make lactulose a model compound for this type of solid state transformation. The ease of crystalline lactulose to be amorphized on milling is explained by comparing elastic constants of lactulose with those of several other disaccharides. These constants have been determined by molecular dynamics simulations. The article also shows how isothermal dissolution calorimetry can be used effectively for the determination of amorphization kinetics during grinding when the usual characterization techniques (differential scanning calorimetry and powder X-ray diffraction) fail.

摘要

在本文中,我们证明了结晶乳果糖可以通过机械研磨直接非晶化。此外,与类似的材料相比,乳果糖的非晶化动力学被发现非常快,并且所获得的无定形状态在加热时似乎对再结晶非常稳定。这些特征使得乳果糖成为这种类型的固态转变的模型化合物。通过比较乳果糖与其他几种二糖的弹性常数,解释了结晶乳果糖在研磨时容易非晶化的原因。这些常数是通过分子动力学模拟确定的。本文还展示了当通常的表征技术(差示扫描量热法和粉末 X 射线衍射法)失效时,如何使用等温溶解量热法有效地确定研磨过程中的非晶化动力学。

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