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Synthesis, Characterization, and Properties of Rivaroxaban New Crystalline Forms
Crystal Research and Technology ( IF 1.5 ) Pub Date : 2021-06-19 , DOI: 10.1002/crat.202000243
Lihai Zhai 1, 2 , Zhaohua Zhang 1 , Lihong Guo 1, 2 , Zhiying Zhu 1 , Changkai Hu 1 , Guimin Zhang 1, 2
Affiliation  

In this paper, two new Rivaroxaban crystalline forms are reported and characterized by the single-crystal X-ray diffraction (SXRD), powder X-ray diffraction (PXRD), thermogravimetric analysis, and differential scanning calorimetry (TGA/DSC), which are synthesized with formic acid and acetic acid, named as forms F and G, respectively. The intermolecular forces for forms F and G are analyzed by Hirshfeld surface analysis method, showing that the force of O···H is significantly stronger than that of H···H. Furthermore, the stability, solubility, and bioavailability of the two crystal forms are also studied. The clinical experiments show that form F is more effective than other reported crystal forms in inhibiting the activity of thrombin and thrombosis, which is expected to replace the marketed crystalline forms in clinical application.

中文翻译:

利伐沙班新晶型的合成、表征和性质

本文报道了两种新的利伐沙班晶型,并通过单晶 X 射线衍射 (SXRD)、粉末 X 射线衍射 (PXRD)、热重分析和差示扫描量热法 (TGA/DSC) 对其进行了表征。用甲酸和乙酸合成,分别命名为形式 F 和 G。用 Hirshfeld 表面分析法分析了 F 型和 G 型的分子间作用力,表明 O...H 的作用力明显强于 H...H 的作用力。此外,还研究了两种晶型的稳定性、溶解性和生物利用度。临床实验表明,晶型F在抑制凝血酶活性和血栓形成方面比其他报道的晶型更有效,有望在临床应用中取代市售晶型。
更新日期:2021-06-19
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