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首页> 外文期刊>Crystal growth & design >Furosemide:Triethanolamine Salt as a Strategy To Improve the Biopharmaceutical Properties and Photostability of the Drug
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Furosemide:Triethanolamine Salt as a Strategy To Improve the Biopharmaceutical Properties and Photostability of the Drug

机译：呋塞米：三乙醇胺盐作为改善药物生物药物特性和药物光稳定性的策略

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摘要

With the purpose of enhancing the biopharmaceutical properties of the furosemide, a pharmaceutical salt was obtained and characterized by combining the drug and triethanolamine. The solid system was prepared using different techniques such as kneading, grinding, and slow evaporation. It was characterizated by X-ray powder diffraction, solid-state nuclear magnetic resonance, infrared and Raman spectroscopy, thermal analysis, and scanning electron microscopy. The results showed that the same pharmaceutical compound in solid state was obtained through the different preparation techniques. The crystalline structure was fully elucidated by single-crystal X-ray diffraction. The salt formation was confirmed by two-dimensional nuclear magnetic resonance experiments, which revealed the transference of the OH proton of the drug to triethanolamine. Besides, the solubility studies demonstrated an increase in the drug solubility attributed not only to a pH change but also to a soluble salt formation in solution. In addition, the combination of the drug with triethanolamine produces an enhancement of the chemical photostability, whereas the physical photostability and the hygroscopicity status were not modified. Finally, this new solid form of furosemide constitutes an interesting strategy to improve the biopharmaceutical properties and stability of furosemide, with potential application in pharmaceutical formulations.
机译：目的是提高呋塞米的生物制药特性，得到药物盐，其特征在于组合药物和三乙醇胺。使用不同的技术如捏合，研磨和缓慢蒸发制备固体系统。其特征在于X射线粉末衍射，固态核磁共振，红外和拉曼光谱，热分析和扫描电子显微镜。结果表明，通过不同的制备技术获得固态的相同药物化合物。通过单晶X射线衍射完全阐明结晶结构。通过二维核磁共振实验证实盐形成，揭示了药物的OH质子转移到三乙醇胺的转移。此外，溶解度研究证明了药物溶解度的增加不仅归因于pH变化，而且归因于溶液中可溶性盐形成。此外，药物与三乙醇胺的组合产生了化学光稳定性的增强，而物理光稳定性和吸湿性状态未被修饰。最后，这种新的固体形式的呋塞米构成了改善呋塞米生物制药性和呋塞米的稳定性的有趣策略，潜在的药物制剂。

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  • 来源
    《Crystal growth & design》 |2019年第4期|共9页
  • 作者

    Abraham Miranda Julieta; Garnero Claudia; Chattah Ana K.; Santiago de Oliveira Yara; Ayala Alejandro P.; Longhi Marcela R.;

  • 作者单位

    Univ Nacl Cordoba Unidad Invest &

    Desarrollo Tecnol Farmaceut UNITE CONICET Fac Ciencias Quim Ciudad Univ RA-5000 Cordoba Argentina;

    Univ Nacl Cordoba Unidad Invest &

    Desarrollo Tecnol Farmaceut UNITE CONICET Fac Ciencias Quim Ciudad Univ RA-5000 Cordoba Argentina;

    Univ Nacl Cordoba Fac Matemat Astron &

    Fis Ciudad Univ XSOOOHUA Cordoba Argentina;

    Univ Fed Ceara Dept Pharm BR-65455900 Fortaleza Ceara Brazil;

    Univ Fed Ceara Dept Phys BR-65455900 Fortaleza Ceara Brazil;

    Univ Nacl Cordoba Unidad Invest &

    Desarrollo Tecnol Farmaceut UNITE CONICET Fac Ciencias Quim Ciudad Univ RA-5000 Cordoba Argentina;

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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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