| 引用本文: | 吴丽莎,孙慧慧,李银塔,元泉,王韶华,颜世强.依帕司他共晶的制备、表征及性质研究[J].中国现代应用药学,2025,42(13):50-55. |
| wu li sha,sun hui hui,li yin ta,yuan quan,wang shao hua,yan shi qiang.Preparation, Characterization and Properties of Epalrestat Co-crystal[J].Chin J Mod Appl Pharm(中国现代应用药学),2025,42(13):50-55. |
|
| 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 依帕司他共晶理化成药性良好。 |
| 关键词: 依帕司他 4,4’-联吡啶 共晶制备 表征 性质 |
| DOI： |
| 分类号:R284.1；R917.101 |
| 基金项目:山东省自然科学基金重点项目（ZR2020KH002） |
|
| Preparation, Characterization and Properties of Epalrestat Co-crystal |
|
wu li sha1, sun hui hui2, li yin ta1, yuan quan2, wang shao hua3, yan shi qiang1
|
|
1.Weihai Ocean Vocational College;2.Shandong Dyne Marine Biopharmaceutical Co. Ltd.;3.Rongcheng Technology Transfer Service Center
|
| Abstract: |
| OBJECTIVE Preparing epalrestat co-crystal to improve its solubility. METHODS Using epalrestat as starting material and 4,4 '-bipyridine as eutectic precursor, the co-crystal was obtained by solvent volatilization. The structure of 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 co-crystal in water was increased to 40 times as compared with epalrestat. CONCLUSION The physical and chemical properties of epalrestat co-crystal were good. |
| Key words: epalrestat 4,4"-bipyridine co-crystal preparation characterization properties |
