摘要
本文以卡马西平(1)和糖精(2)作为共晶筛选的模型系统,在本实验室自主研发的高通量共晶筛选装置上使用乙醇、乙酸乙酯、乙酸异丙酯、二氯甲烷和甲醇作为溶剂,通过蒸发结晶法、冷却结晶法或反应结晶法制备共晶,最后通过光学显微镜、粉末X射线衍射(Powder X-ray Diffraction,PXRD)和拉曼光谱仪进行样品分析。结果发现,通过该筛选平台能够进行小规模(1~2 mg)药物共晶的快速筛选,并且得到的共晶筛选结果与文献报道相一致,证明该平台在活性药物成分共晶筛选中具有较好的应用前景。
In this study,carbamazepine(1)and saccharin(2)was used as a model system for cocrystal screening.Ethanol,ethyl acetate,isopropyl acetate,dichloromethane and methanol were used as solvents in the high-throughput cocrystal screening device developed by our laboratory.The cocrystals were prepared by evaporation,cooling,or reaction crystallization methods,followed by sample analysis using Optical Microscope,Powder X-ray Diffraction(PXRD),and Raman spectroscopy.It was found that the screening platform can perform rapid screening of small-scale(1-2 mg)drug cocrystals and the results of cocrystal screening were consistent with those reported in the literature,which proved a good application prospect of this platform in the cocrystal screening of active pharmaceutical ingredients.
作者
葛阳
刘祎
吴炎凡
王学军
宗新华
GE Yang;LIU Yi;WU Yanfan;WANG Xuejun;ZONG Xinhua(Suzhou Institute of Biomedical Engineering and Technology,Chinese Academy of Sciences,Suzhou 215163)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2020年第3期405-410,共6页
Chinese Journal of Pharmaceuticals
基金
中科院百人计划项目(Y521061102)。
关键词
高通量
药物共晶
卡马西平
糖精
high-throughput
drug cocrystals
carbamazepine
saccharin
