摘要
目的制备顺丁烯二酸文拉法辛,期望找到一种能够缓释的新文拉法辛盐型,达到长效和降低不良反应的效果。方法利用加液研磨法和溶液搅拌法分别制备顺丁烯二酸文拉法辛;采用单晶X射线衍射分析(SXRD)、粉末X射线衍射分析(PXRD)、差示扫描量热分析(DSC)、热重分析(TGA)对顺丁烯二酸文拉法辛进行表征;并考察顺丁烯二酸文拉法辛在(60±1)℃高温、(90±5)%高湿、(4500±500)lx光照条件下的稳定性。结果制备获得顺丁烯二酸与文拉法辛摩尔比1∶1结合的盐,顺丁烯二酸文拉法辛在高温、高湿、光照条件下稳定。结论顺丁烯二酸文拉法辛的晶体结构和制备方法及其表征图谱可以为开发新型的文拉法辛盐提供基础数据和技术参考。
Objective To prepare a new venlafaxine maleate for extending release and decreasing the side effects of the drug. Methods Liquid assisted grinding and solution stirring method have been used to prepare the venlafaxine maleate.Single crystal X ̄ray diffraction analysis(SXRD),powder X ̄ray diffraction analysis(PXRD),differential scanning calorimetry analysis(DSC),and thermogravimetric analysis(TGA)were used to characterize venlafaxine maleate.The stability of venlafaxine maleate was also determined under high temperature(60±1)℃,high humidity(90±5)%,and strong illuminance(4500±500)lx. Results The product was prepared with venlafaxine and maleate at molar ratio 1:1.Venlafaxine maleate was stable under three conditions. Conclusion The crystal structure,preparation and characterization spectrum of venlafaxine maleate is reported in this study?which can provide basic data and technical references for further development and research of venlafaxine maleate.
作者
王英
龚宁波
杨德智
杜冠华
吕扬
WANG Ying;GONG Ningbo;YANG Dezhi;DU Guanhua;LYU Yang(Beijing Key Laboratory of Polymorphs Drugs Research Institute of Materia Medica,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing 100050,China;Beijing Key Laboratory of Drug Target and Screening Research,Institute of Materia Medica,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing 100050,China)
出处
《医药导报》
CAS
北大核心
2018年第9期1099-1102,共4页
Herald of Medicine
基金
国家重点研发计划(2016YFC1000901)
中国医学科学院医学与健康科技创新工程项目(2017-I2M-1-010)