{"title":"利伐沙班新晶型的合成、表征和性质","authors":"L. Zhai, Zhaohua Zhang, Lihong Guo, Zhiying Zhu, Changkai Hu, Guimin Zhang","doi":"10.1002/crat.202000243","DOIUrl":null,"url":null,"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.","PeriodicalId":10797,"journal":{"name":"Crystal Research and Technology","volume":null,"pages":null},"PeriodicalIF":1.5000,"publicationDate":"2021-06-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"3","resultStr":"{\"title\":\"Synthesis, Characterization, and Properties of Rivaroxaban New Crystalline Forms\",\"authors\":\"L. Zhai, Zhaohua Zhang, Lihong Guo, Zhiying Zhu, Changkai Hu, Guimin Zhang\",\"doi\":\"10.1002/crat.202000243\",\"DOIUrl\":null,\"url\":null,\"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.\",\"PeriodicalId\":10797,\"journal\":{\"name\":\"Crystal Research and Technology\",\"volume\":null,\"pages\":null},\"PeriodicalIF\":1.5000,\"publicationDate\":\"2021-06-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Crystal Research and Technology\",\"FirstCategoryId\":\"88\",\"ListUrlMain\":\"https://doi.org/10.1002/crat.202000243\",\"RegionNum\":4,\"RegionCategory\":\"材料科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"CRYSTALLOGRAPHY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Crystal Research and Technology","FirstCategoryId":"88","ListUrlMain":"https://doi.org/10.1002/crat.202000243","RegionNum":4,"RegionCategory":"材料科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"CRYSTALLOGRAPHY","Score":null,"Total":0}
Synthesis, Characterization, and Properties of Rivaroxaban New Crystalline Forms
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.
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