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首页> 外文期刊>Crystal growth & design >Solution versus Crystal Hydration: The Case of gamma-Amino Acid Pregabalin
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Solution versus Crystal Hydration: The Case of gamma-Amino Acid Pregabalin

机译：溶液与晶体水合作用：γ-氨基酸的情况Prafabalin

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摘要

Understanding the link between solution chemistry and nucleation is essential to control crystallization processes, in particular regarding pharmaceutical compounds. In the present work, the link between the solution hydration state and crystallization of the gamma-amino acid pregabalin is presented. Pregabalin is a blockbuster pharmaceutical drug having broad therapeutic effects. Using induction time experiments in combination with the classical nucleation theory, we show that the ease of nucleation increases with solubility and water fraction of the solvent. Water was found to enhance both the kinetic and thermodynamic processes of forming a nuclei. As a result, larger clusters which represent the hydrate form were measured using dynamic light scattering in pure water. Once in the solid state, the hydrate form of pregabalin was found to be physically unstable, as it rapidly converted back into its anhydrate form, as rationalized using in-line Raman spectroscopy. Thus, the hydration and nucleation of pregabalin in solution is highly favored, as opposed to the solid-state situation, where the anhydrate is the stable form. Despite these differences, a solution-crystallization link could still be established in our work. Knowledge of the solution chemistry and structural landscape of pharmaceutical compounds is essential for the development of manufacturing routes and patent protections, and we foresee that the presented approach can be used to further reveal relationships among self-association in solution, crystallization, and hydration of a wide range of organic compounds.
机译：理解溶液化学和成核之间的联系对于控制结晶方法，特别是关于药物化合物是必不可少的。在本作工作中，介绍了溶液水合状态与γ-氨基酸普罗那甲蛋白的结晶之间的联系。 Pragabalin是一种具有广泛治疗效果的大片药物。使用诱导时间实验与经典成核理论结合，我们表明肠的易燃性随着溶剂的溶解度和水分分。发现水增强了形成核的动力学和热力学过程。结果，使用纯水中的动态光散射测量代表水合物形式的较大簇。一旦处于固态，发现普瑞巴林的水合物形式是物理上不稳定的，因为它在用线拉曼光谱法合理化的是合理化的，因为它在物理上不稳定。因此，对溶液中普雷巴林的水合和成核非常有利，而不是固态的情况，其中余量是稳定的形式。尽管存在这些差异，但仍然可以在我们的工作中建立解决方案结晶链接。了解药物化合物的溶液化学和结构景观对于制造路线和专利保护的发展至关重要，我们预见到所提出的方法可用于进一步揭示自我关联中的溶液，结晶和水合的关系。各种有机化合物。

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  • 来源
    《Crystal growth & design》 |2019年第8期|共6页
  • 作者

    Steendam Rene R. E.; Khandavilli U. B. Rao; Keshavarz Leila; Frawley Patrick J.;

  • 作者单位

    Univ Limerick Bernal Inst Synth &

    Solid State Pharmaceut Ctr SSPC Limerick Ireland;

    Univ Limerick Bernal Inst Synth &

    Solid State Pharmaceut Ctr SSPC Limerick Ireland;

    Univ Limerick Bernal Inst Synth &

    Solid State Pharmaceut Ctr SSPC Limerick Ireland;

    Univ Limerick Bernal Inst Synth &

    Solid State Pharmaceut Ctr SSPC Limerick Ireland;

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  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类 晶体学;
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