氟灭酸药物共晶制备及晶体结构  

Flufenamic acid cocrystal preparation and structure study

作　　者：李静璇 陈旸 高玲焕 乔宁 LI Jing-xuan;CHEN Yang;GAO Ling-huan;QIAO Ning(College of Materials Science and Engineering,North China University of Science and Technology,Hebei Tangshan 063210,China;College of Basic Medical Sciences,North China University of Science and Technology,Hebei Tangshan 063210,China)

机构地区：[1]华北理工大学材料科学与工程学院,河北唐山063210 [2]华北理工大学基础医学院,河北唐山063210

出　　处：《中国医院药学杂志》2020年第11期1217-1222,共6页Chinese Journal of Hospital Pharmacy

基　　金：河北省科技计划项目(编号:16211505);华北理工大学博士科研基金(编号:28405399);华北理工大学大学生创新创业训练计划(编号:X2019080)。

摘　　要：目的:选取氟灭酸为活性药物成分,选取茶碱、烟酰胺、邻苯甲酰磺酰亚胺为共晶形成物,将氟灭酸分别与上述共晶形成物制备药物共晶,并研究其晶体结构。方法:使用低毒性的乙醇溶剂,分别采用溶剂挥发法及研磨法制备氟灭酸药物共晶;采用红外光谱,X线衍射仪,荧光光谱仪对样品进行测试,鉴定共晶生成,分析样品结构。结果:两种方法制得的共晶样品红外光谱发生特征峰移动,X线图谱出现新的特征峰,荧光发射波长及发射强度改变,证明氟灭酸可与上述3种共晶形成物通过其分子结构上的羰基、氨基等官能团间生成氢键连接而制备药物共晶。但是研磨法所得共晶样品的表征结果显示有原料残留,共晶纯度不高。结论:溶剂挥发法与研磨法均可制备氟灭酸共晶,其中溶液法所得共晶样品纯度较高,晶体结构较优。OBJECTIVE Flufenamic acid was selected as active pharmaceutical ingredient.Theophylline,nicotinamide,saccharin were selected as cocrystal coformers.Flufenamic acid cocrystal was prepared with above three coformers and its structure was studied.METHODS Use ethanol as solvent,flufenamic acid cocrystal was prepared by solvent evaporation method and grinding method.Samples were characterized by Attenuated Total Reflectance-FTIR,X-ray diffraction and fluorescence spectrometer to verify the formation of cocrystal and analyze its crystalline structure.RESULTS The formation of flufenamic acid cocrystal was demonstrated by its IR character peaks shift,new XRD character peaks,and change of maximal fluorescence emission wavelength and strength.The cocrystal was formed through hydrogen bond between the carbonyl group,amino group of flufenamic acid and coformers.Characterization results show that the grinding samples have some residue of starting materials.CONCLUSION Flufenamic acid cocrystal can be prepared through evaporation method and grinding method.Evaporation method generates cocrystal sample with higher purity and better crystal structure.

关 键 词：氟灭酸 药物共晶 溶剂挥发 研磨法 共晶结构 

分 类 号：R943[医药卫生—药剂学]