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首页> 外文期刊>Acta Crystallographica, Section B. Structural science, crystal engineering and materials >Agomelatine-hydroquinone (1:1) cocrystal: novel polymorphs and their thermodynamic relationship
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Agomelatine-hydroquinone (1:1) cocrystal: novel polymorphs and their thermodynamic relationship

机译：聚茂物丁醇 - 氢醌（1：1）COCRYSTAL：新型多晶型物及其热力学关系

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Polymorphism of active pharmaceutical ingredients (APIs) is of significance in the pharmaceutical industry because it can affect the quality, efficacy and safety of the final drug product. In this regard, polymorphic behavior of cocrystals is no exception because it can influence the development of cocrystals as potential drug formulations. The current contribution aims to introduce two novel polymorphs [forms (III) and (IV)] of agomelatine-hydroquinone (AGO-HYQ) cocrystal and to describe the thermodynamic relationship between the cocrystal polymorphs. All polymorphs were characterized using powder X-ray diffraction, differential scanning calorimetry, hot-stage microscopy and solubility measurements. In addition, the crystal structure of form (II), which has been previously solved from powder diffraction data [Prohens et al. (2016), Cryst. Growth Des. 16, 1063-1070] and form (III) were determined from the single-crystal X-ray diffraction data. Thermal analysis revealed that AGO-HYQ cocrystal form (III) exhibits a higher melting point and a lower heat of fusion than those of form (II). According to the heat of fusion rule, the polymorphs are enantiotropically related, with form (III) being stable at higher temperatures. Our results also show that the novel form (IV) is the most stable form at ambient conditions and it transforms into form (II) on heating, and therefore, the two polymorphs are enantiotropically related. Furthermore, solubility and van't Hoff plot results suggest that the transition points are approximately 339 K for the pair form (IV)-(II) and 352 K for the pair form (II)-(III).
机译：活性药物成分（API）的多态性在制药行业中具有重要意义，因为它可能会影响最终药品的质量，功效和安全性。在这方面，Cocrystals的多态性行为也不例外，因为它可以影响Cocrystals作为潜在药物制剂的发育。目前的贡献目的是引入聚焦 - 羟基醌（auti-hyq）Cocrystal的两种新型多晶型物[形式（III）和（IV）]，并描述Cocrystal多晶型物之间的热力学关系。使用粉末X射线衍射，差示扫描量热法，热阶段显微镜和溶解度测量来表征所有多晶型物。另外，以前从粉末衍射数据求解的形式（II）的晶体结构[Prohens等人。 （2016），渐变。生长des。从单晶X射线衍射数据确定16,1063-1070]和形式（III）。热分析表明，Hyq Cocrystal形式（III）表现出较高的熔点和比形式（II）的融合的较低热量。根据融合规则的热量，多晶型物是对脱色的相关性，其形式（III）在较高温度下稳定。我们的研究结果还表明，新型形式（IV）是环境条件下最稳定的形式，其在加热中转化为形式（II），因此，两种多晶型物在对脱色相关。此外，溶解度和VACOT HOFF绘图结果表明，对于一对形式（II） - （II） - （III），过渡点为一对形式（IV） - （II）和352k，[（II） - （III）。

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