地拉罗司-烟酰胺共晶的制备、表征及性质研究

沙莎; 吴丽莎; 刘桂永; 郭伟; 王英新; 颜世强

引用本文:	沙莎,吴丽莎,刘桂永,郭伟,王英新,颜世强.地拉罗司-烟酰胺共晶的制备、表征及性质研究[J].中国现代应用药学,2025,42(6):75-79.
	sha sha,Wu Li Sha,liu gui yong,guo wei,wang ying xin,yan shi qiang.Preparation, Characterization and Properties of Deferasirox-Nicotinamide Co-crystal[J].Chin J Mod Appl Pharm(中国现代应用药学),2025,42(6):75-79.

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地拉罗司-烟酰胺共晶的制备、表征及性质研究
沙莎¹, 吴丽莎², 刘桂永¹, 郭伟¹, 王英新¹, 颜世强¹
1.山东达因海洋生物制药股份有限公司;2.威海海洋职业学院

摘要:

目的制备地拉罗司-烟酰胺药物共晶(物质的量之比1:1)，提高地拉罗司溶解度。方法以地拉罗司及烟酰胺为原料，采用研磨法，制备得到地拉罗司-烟酰胺共晶。应用1H-NMR分析、粉末X射线衍射法、差示扫描量热法、热重法、傅里叶变换红外光谱法等对制备得到的共晶进行表征。对共晶溶解性、稳定性和引湿性进行了研究。结果相较地拉罗司原料药，共晶在水中的溶解度提高近27倍。结论地拉罗司-烟酰胺药物共晶理化成药性良好。

关键词: 地拉罗司药物共晶制备表征性质

DOI：

分类号:R914

基金项目:山东省自然科学基金重点项目(ZR2020KH002)

Preparation, Characterization and Properties of Deferasirox-Nicotinamide Co-crystal

sha sha¹, Wu Li Sha², liu gui yong¹, guo wei¹, wang ying xin¹, yan shi qiang¹

1.Shandong Dyne Marine Biopharmaceutical Co.，Ltd.;2.Weihai Ocean Vocational College

Abstract:

OBJECTIVE To prepare deferasirox -nicotinamide co-crystal（1:1）for improvement of the solubility of poorly water‐soluble deferasirox. METHODS The co-crystal was obtained by the liquid‐assisted grinding method.The structure of co-crystal was characterized by 1H-NMR,power x-ray diffraction,differential scanning calorimetry,thermal gravimetric analysis and fourier transform infrared spectrum,respectively.The solubility,stability and hygroscopicity of the co-crystal were also studied. RESULTS The results showed that the solubility of co-crystal in water was increased to 27 times as compared with deferasirox. CONCLUSION The physical and chemical properties of deferasirox -nicotinamide co-crystal are good.

Key words: deferasirox co-crystal preparation characterization properties