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Investigation of the solid forms of deferasirox: solvate, co-crystal, and amorphous form

机译：调查脱司叶酸的固体形式：溶剂化物，共晶和无定形形式

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摘要

Deferasirox (DFX) is an oral iron chelator. This study prepared and characterized five solid forms of DFX including monohydrate (DFX-H2O), dimethylformamide solvate (DFX-DMF), two co-crystals of DFX and isonicotinamide (INA) (DFX-INA and DFX-2INA), and amorphous DFX. Single crystals of DFX-H2O, DFX-DMF, DFX-INA, and DFX-2INA were obtained through solvent crystallization, and their structures were determined by single-crystal X-ray diffraction analysis. DFX-H2O, DFX-DMF, DFX-INA, and DFX-2INA were all monoclinic with P21/c, P21/c, P21/c, and C2/c space groups, respectively. In the four solid forms, the DFX molecule always maintained an S(6) ring motif, and its carboxylic acid moiety easily formed hydrogen bonds with the solvent or INA molecules. Solid forms were preliminarily estimated by stability and in vitro dissolution tests. DFX-INA and amorphous DFX showed good stability under ambient conditions and better dissolution characteristic compared with commercial DFX in phosphate buffer medium (pH 6.8). Thus, DFX-INA and amorphous DFX exhibited potential as preponderant solid forms of DFX for drug development.
机译：脱司索（DFX）是口服铁螯合剂。该研究制备并表征了五种固体形式的DFX，包括单水合物（DFX-H2O），二甲基甲酰胺溶剂化物（DFX-DMF），DFX和Isonicotina酰胺（INA）（DFX-INA和DFX-2NA）的两个共晶，以及无定形DFX 。通过溶剂结晶获得DFX-H2O，DFX-DMF，DFX-INA和DFX-2NA的单晶，通过单晶X射线衍射分析测定它们的结构。 DFX-H2O，DFX-DMF，DFX-INA和DFX-2NA均分别具有P21 / C，P21 / C，P21 / C和C2 / C空间组的单替摩利。在四种固体形式中，DFX分子总是保持S（6）环基序，其羧酸部分容易与溶剂或INA分子形成氢键。通过稳定性和体外溶解试验预估计固体形式。与磷酸盐缓冲介质中的商业DFX相比，DFX-INA和无定形DFX在环境条件下显示出良好的稳定性和更好的溶解特性（pH6.8）。因此，DFX-INA和无定形DFX表现出潜在的潜力作为药物发育的DFX的优势固体形式。

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  • 来源
    《RSC Advances》 |2017年第68期|共10页
  • 作者

    Du Qiaohong; Xiong Xinnuo; Suo Zili; Tang Peixiao; He Jiawei; Zeng Xia; Hou Quan; Li Hui;

  • 作者单位

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

    Sichuan Univ Coll Chem Engn Chengdu Sichuan Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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