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首页> 外文期刊>Journal of Crystal Growth >Increasing dissolution of trospium chloride by co-crystallization with urea
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Increasing dissolution of trospium chloride by co-crystallization with urea

机译：与尿素共结晶增加氯化钾的溶解

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摘要

The search for various solid forms of an active pharmaceutical ingredient (API) is an important step in drug development. Our aim was to prepare co-crystals of trospium chloride, an anticholinergic drug used for the treatment of incontinence, and to investigate if they have advantageous properties for drug formulation. Phase identification was done by powder X-ray diffraction and single-crystal X-ray diffraction. The chemical composition was verified by solution NMR and the dissolution rate of the prepared phases was studied by IDR (intrinsic dissolution rate). For further analysis of phase stability and transitions, combined thermal analysis and temperature-resolved X-ray powder diffraction were used. Urea was selected as a co-crystallization partner. Trospium chloride urea (1∶1) co-crystal was prepared by a solvent evaporation. From single-crystal data, the co-crystal structure was solved in a space group P2_1/c and compared to previously published structures of trospium chloride. Intrinsic dissolution rate revealed that the co-crystal dissolves 32% faster than pure API. However, its low thermal and pressure stability makes it a challenging choice for the final drug formulation.
机译：寻找各种固体形式的活性药物成分（API）是药物开发中的重要一步。我们的目的是制备用于治疗失禁的抗胆碱能药物氯化钾的共晶体，并研究它们是否对药物制剂具有有利的特性。通过粉末X射线衍射和单晶X射线衍射进行相鉴定。通过溶液NMR验证化学组成，并且通过IDR（固有溶解速率）研究所制备相的溶解速率。为了进一步分析相稳定性和相变，使用了结合的热分析和温度分辨的X射线粉末衍射。尿素被选为共结晶伙伴。通过溶剂蒸发制得氯化钾脲（1∶1）共晶体。根据单晶数据，将共晶结构解析为空间群P2_1 / c，并将其与先前发表的氯化钾的结构进行比较。固有溶解速率表明，共晶的溶解速度比纯API快32％。然而，其低的热稳定性和压力稳定性使其成为最终药物制剂的挑战性选择。

著录项

  • 来源
    《Journal of Crystal Growth》 |2014年第1期|19-26|共8页
  • 作者

    Eliska Skorepova; Michal Husak; Jan Cejka; Petr Zamostny; Bohumil Kratochvil;

  • 作者单位

    Department of Solid State Chemistry, Institute of Chemical Technology Prague, Technicka 5, Prague 6, Czech Republic;

    Department of Solid State Chemistry, Institute of Chemical Technology Prague, Technicka 5, Prague 6, Czech Republic;

    Department of Solid State Chemistry, Institute of Chemical Technology Prague, Technicka 5, Prague 6, Czech Republic;

    Department of Organic Technology, Institute of Chemical Technology Prague, Technicka 5, Prague 6, Czech Republic;

    Department of Solid State Chemistry, Institute of Chemical Technology Prague, Technicka 5, Prague 6, Czech Republic;

  • 收录信息 美国《科学引文索引》(SCI);美国《工程索引》(EI);美国《生物学医学文摘》(MEDLINE);
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

    A1.Crystal structure; A1.Solubility; A1.X-ray diffraction; A2.Growth from solutions; B1.Organic compounds;

    机译：A1。晶体结构;A1。溶解度;A1.X射线衍射;A2。解决方案的增长;B1。有机化合物;

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