|Table of Contents|

Quantitative Analysis and Thermal Stability of the CrystalForm of Rivaroxaban as an Anticoagulant(PDF)

《南京师大学报（自然科学版）》[ISSN:1001-4616/CN:32-1239/N]

Issue:
2021年01期
Page:
136-140
Research Field:
·药学·
Publishing date:

Info

Title:
Quantitative Analysis and Thermal Stability of the CrystalForm of Rivaroxaban as an Anticoagulant
Author(s):
Ma Yuxuan; Wang Na; Wang Bing; Li Gang
School of Food and Pharmaceutical Engineering,Test & Analysis Center,Nanjing Normal University,Nanjing 210023,China
Keywords:
Rivaroxaban; quantitative analysis; qualitative analysis; thermal stability analysis
PACS:
R927
DOI:
10.3969/j.issn.1001-4616.2021.01.019
Abstract:
In this paper,X-ray powder diffractometer(PXRD)was used to qualitatively and quantitatively analyze the crystal formⅠand crystal form Ⅱ in the mixed crystal of Riveraban. The thermal stability of crystal form Ⅱ was determined by differential scanning Calorimeter(DSC)combined with X-ray powder diffractometer in situ high temperature attachment. X-ray powder diffraction K value method is used for quantitative analysis,the results show that the method is convenient,rapid,simple and practical,and the thermal analysis shows that the phase transformation of crystal form Ⅱ occurs at about 190 ℃ and gradually changes to crystal form Ⅰ.

References:

[1] PICCINI J P,PATEL M R,MAHAFFEY K W,et al. Rivaroxaban,an oral direct factor Xa inhibitor[J]. Expert opinion on investigational drugs,2008,17:925-937.
[2]LAUX V,PERZBORN E,KUBITZA D,et al. Preclinical and clinical characteristics of rivaroxaban:a novel,oral,direct factor Xa inhibitor[J]. Seminars in thrombosis and hemostasis,2007,33:515-523.
[3]陈怡琳,施仲伟. 抗凝新药利伐沙班临床研究进展[J]. 心血管病学进展,2009(5):92-95.
[4]刘薇,董金华. 利伐沙班(rivaroxaban)[J]. 中国药物化学杂志,2011,21(6):508,510.
[5]刘晓,崔一民. 新型抗凝血药物——利伐沙班[J]. 中国药房,2010(1):89-92.
[6]江丽华,黄嘉利,陈丽华. 利伐沙班用于非瓣膜性心房颤动患者抗凝治疗的疗效及安全性[J]. 中国医院用药评价与分析,2019,19(3):304-305,308.
[7]BURNESS C B,MCKEAGE K. Dabigatran etexilate[J]. Drugs,2012,72:963-986.
[8]李庆勇,牛锁成,何贵生,等. 阿哌沙班治疗非瓣膜性房颤有效性和安全性的Meta分析[J]. 重庆医学,2014,43(4):437-439.
[9]赵亚男,陈小青,朱侃,等. 抗癌药达沙替尼的热稳定性与晶型研究[J]. 药学学报,2011,46(9):1104-1107.
[10]黄日,王涛,杨茜,等. 阿奇霉素掩味干乳的表征及体内外评价[J]. 药学学报,2017,52(5):795-801.
[11]李钢,苏国强,徐群为. 降糖新药那格列奈的一种新晶型结构[J]. 药物分析杂志,2001(5):342-344.
[12]张国顺,张丽,龚宁波,等. 利伐沙班多晶型研究[C]. 北京:全国晶型药物研发技术学术研讨会,2014.
[13]XU Y,WU S P,LIU X J,et al. Crystal characterization and transformation of the forms Ⅰ and Ⅱ of anticoagulant drug rivaroxaban[J]. Crystal research technology,2017,52:1600379.
[14]高晶,滕再进,束俭辉,等. 固体制剂生产过程中的药物晶型转变[J]. 中国新药杂志,2018,27(9):1000-1005.
[15]BAYER INTELLECTUAL PROPERTY CO.,LTD. Novel polycrystalline and amorphous 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidine-5-yl}-methyl)-2-thiophene carboxylamides:CN,101282968[P]. 2008-10-08.



[16]李大雄,柯鸿,樊小波,等. 一种利伐沙班新晶型及其制备方法与用途:CN,104211693A[P]. 2014-12-17.

[17]谢梦雨,戴苏云,沈晓敏,等. X-射线粉末衍射K值法测定钴粉中α-Co的含量[J]. 南京师大学报(自然科学版),2017,40(4):93-97,102.

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Last Update: 2021-03-15