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Issue 2, 2017
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Crystallization and relaxation dynamics of amorphous loratadine under different quench-cooling temperatures

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Abstract

In this paper, four amorphous samples of loratadine were prepared by quench-cooling the melted drug at different temperatures. With these samples, the crystallization tendencies were tested by powder X-ray diffraction (PXRD), and non-isothermal cold crystallization kinetics was investigated by using differential scanning calorimetry (DSC) and the molecular dynamics both in super-cooled liquid and in glassy states was analyzed by using broadband dielectric spectroscopy (BDS) at a temperature range from 213 to 393 K. From the PXRD results, it was established that the four amorphous loratadine samples were apt to crystallize at a temperature below the glass transition temperature. From the DSC results, it was found that the non-isothermal crystallization mechanism of these four loratadine forms was similar. However, the fast crystallization tendency (low physical stability) was also observed for the amorphous loratadine which was obtained at a low quench-cooling temperature. The tendency was analyzed based on the BDS results which demonstrated that rapid molecular mobility could generate a low physical stability and was closely related to Johari–Goldstein relaxation. These results suggested that loratadine had a weak frustration against crystallization and its physical stability was affected by the quench-cooling temperature. This study laid a foundation for choosing the right technique to prepare the amorphous form of loratadine and improving its physical stability.

Graphical abstract: Crystallization and relaxation dynamics of amorphous loratadine under different quench-cooling temperatures

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Article information


Submitted
27 Jul 2016
Accepted
29 Nov 2016
First published
29 Nov 2016

CrystEngComm, 2017,19, 335-345
Article type
Paper

Crystallization and relaxation dynamics of amorphous loratadine under different quench-cooling temperatures

R. Chang, Q. Fu, Y. Li, M. Wang, W. Du, C. Chang and A. Zeng, CrystEngComm, 2017, 19, 335
DOI: 10.1039/C6CE01645F

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