Synthesis, Characterization, and Properties of Rivaroxaban New Crystalline Forms

IF 1.5 4区 材料科学 Q3 CRYSTALLOGRAPHY
L. Zhai, Zhaohua Zhang, Lihong Guo, Zhiying Zhu, Changkai Hu, Guimin Zhang
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引用次数: 3

Abstract

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.
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结晶形式,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,它们分别由甲酸和乙酸合成,命名为F型和G型。采用Hirshfeld表面分析方法对F和G的分子间作用力进行了分析,结果表明O··H的作用力明显强于H··H。此外,还研究了两种晶型的稳定性、溶解度和生物利用度。临床实验表明,F型在抑制凝血酶活性和血栓形成方面比其他已报道的晶体形式更有效,有望在临床应用中取代已上市的晶体形式。
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来源期刊
自引率
6.70%
发文量
121
审稿时长
1.9 months
期刊介绍: The journal Crystal Research and Technology is a pure online Journal (since 2012). Crystal Research and Technology is an international journal examining all aspects of research within experimental, industrial, and theoretical crystallography. The journal covers the relevant aspects of -crystal growth techniques and phenomena (including bulk growth, thin films) -modern crystalline materials (e.g. smart materials, nanocrystals, quasicrystals, liquid crystals) -industrial crystallisation -application of crystals in materials science, electronics, data storage, and optics -experimental, simulation and theoretical studies of the structural properties of crystals -crystallographic computing
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