摘要
目的 制备依帕司他药物共晶,提高依帕司他水溶性。方法 以依帕司他为原料,4,4’-联吡啶为共晶前驱体,采用溶剂挥发法,制备得到依帕司他共晶。应用1H-NMR分析、X射线单晶衍射法、粉末X射线衍射法、差示扫描量热法、热重法等对制备得到的共晶进行表征。对共晶溶解性及引湿性进行了研究。结果 相较依帕司他原料药,共晶在水中的溶解度提高近40倍。结论 依帕司他共晶水溶性提升显著。
OBJECTIVE To prepare the eutectic of epalrestat and improve its water solubility.METHODS Using epalrestat as starting material and 4,4'-bipyridine as eutectic precursor,the epalrestat co-crystal was obtained by solvent volatilization.The structure of prepared co-crystal was characterized by 1H-NMR,X-ray single-crystal diffraction,power X-ray diffraction,differential scanning calorimetry and thermal gravimetric analysis respectively.The solubility and hygroscopicity of the co-crystal were also studied.RESULTS The solubility of epalrestat co-crystal in water was increased to nearly 40 times as compared with epalrestat raw materials.CONCLUSION The solubility of epalrestat co-crystal increased significantly.
作者
吴丽莎
孙慧慧
李银塔
元泉
王韶华
颜世强
WU Lisha;SUN Huihui;LI Yinta;YUAN Quan;WANG Shaohua;YAN Shiqiang(Weihai Ocean Vocational College,Weihai 264300,China;Shandong Dyne Marine Biopharmaceutical Co.Ltd.,Weihai 264300,China;Rongcheng Technology Transfer Service Center,Weihai 264300,China)
出处
《中国现代应用药学》
北大核心
2025年第13期2258-2262,共5页
Chinese Journal of Modern Applied Pharmacy
基金
山东省自然科学基金重点项目(ZR2020KH002)。
关键词
依帕司他
4
4’-联吡啶
共晶制备
表征
性质
epalrestat
4,4'-bipyridine
co-crystal preparation
characterization
properties
