摘要
目的制备乙水杨胺-草酸共晶,研究共晶在磷酸盐缓冲溶液(phosphate buffer saline,PBS)以及模拟胃液(simulated gastric juice,SGF)中的溶解度。方法采用溶液结晶法,将乙水杨胺和草酸加热溶于乙酸乙酯,缓慢降温至室温,析晶、抽滤、干燥,即获得乙水杨胺-草酸共晶。应用单晶X射线衍射(SCXRD)、粉末X射线衍射(PXRD)、差示扫描量热法(DSC)对乙水杨胺-草酸共晶进行了结极表征,然后测试溶解度。结果乙水杨胺与草酸以2∶1的化学计量比通过形成共晶,共晶在磷酸盐缓冲溶液以及模拟胃液中的溶解度分别为乙水杨胺的2.0倍和2.5倍。结论通过公认安全的草酸形成难溶性药物的共晶,为改善药物溶解度提供了理论依据。
OBJECTIVE To prepare ethenzamide-oxalic acid cocrystal and study the solubility of cocrystal in phosphate buffer saline(PBS)and simulated gastric juice(SGF).METHODS By using solution crystallization method,ethenzamide and oxalic acid were dissolved in ethyl acetate,and the solution was slowly cooled to room temperature,the ethenzamide-oxalic acid cocrystal was obtained through crystallization,filtration and drying.The structure of cocrystal was characterized by single crystal X-ray diffraction(SCXRD),powder X-ray diffraction(PXRD),differential scanning calorimeter(DSC),then solubility was tested.RESULTS The cocrystal was finally formed with ethenzamide and oxalic acid by the stoichiometric ratio of 2∶1.The solubilities for studied cocrystal in PBS and SGF appeared to be approximately 2.0 and 2.5 times-fold higher than ethenzamide.CONCLUSION The study provides a theoretical basis for improving the solubility of drugs by forming the cocrystal of insoluble drugs with oxalic acid,which is generally recognized as safe additives.
作者
蒋成君
张晋娜
申静
程桂林
JIANG Chengjun;ZHANG Jinna;SHEN Jing;CHENG Guilin(School of Biological and Chemical Engineering,Zhejiang University of Science and Technology,Hangzhou 310023,China;Academy of Chinese Medical Sciences,Zhejiang Chinese Medical University,Hangzhou 310053,China)
出处
《中国现代应用药学》
CAS
CSCD
北大核心
2020年第10期1177-1181,共5页
Chinese Journal of Modern Applied Pharmacy
基金
浙江省基础公益研究计划项目(LGJ20B060001)
浙江中医药大学校级科研基金项目(2019ZG48)。
关键词
乙水杨胺
共晶
草酸
溶解性质
结极表征
ethenzamide
cocrystal
oxalic acid
solubility
structure characterization
