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准备和描述与甲胺合剂的利芬素同形材料:一个实验理论研究

Luís H S Queiroz¹, Ranna S Barros¹, Francisco F de Sousa²

¹NUPFARQ, Programa de Pós-Graduação em Ciência dos Materiais (PPGCM), Centro de Ciências de Imperatriz (CCIM), Universidade Federal do Maranhão (UFMA), Imperatriz, Maranhão 65.900-410, Brazil.

Molecular pharmaceutics

|February 16, 2024

概括

一种新的共成形药物配方,即里芬素 (RIF) 和甲胺 (TRIS),显著增强了RIF.

科学领域:

材料科学材料科学材料科学
制药科学制药科学
计算化学计算化学

背景情况:

利芬素 (RIF) 是一种必需的抗生素,其水溶性较差,限制了其生物利用性.
同形系统提供了一种有前途的策略,可以提高难溶性药物的溶性和稳定性.
了解药物-辅形体相互作用对于设计有效的辅形体配方至关重要.

研究的目的:

合成和表征一种新的共成形系统里法素 (RIF) 和甲胺 (TRIS).
通过使用DFT计算,研究RIF-TRIS同形系统的结构,电子,热力学和分子间特性.
评估新型共形材料的物理稳定性,热性能和可溶性增强.

主要方法:

通过缓慢蒸发方法合成的同形系统.
使用粉末X射线衍射 (PXRD),密度函数理论 (DFT) 计算,热重力测量 (TGA) 和差分扫描热量测量 (DSC) 的表征.
进行了溶解性研究,并与晶体里芬素进行了比较.

主要成果:

由PXRD验证的新RIF-TRIS共变体的形成.
DFT计算预测了RIF和TRIS之间的键相互作用,与实验频谱一致.
同形系统在加速条件下 (ICH) 呈现出极好的物理稳定性,在180天内保持无形,RIF溶解度增加了5.5倍.

结论:

成功开发了一种新的,稳定的RIF-TRIS同形系统.
同形形式显著提高了利芬素的溶解性,并表现出良好的物理和热稳定性.
这种RIF-TRIS共成形材料具有开发改进的药物配方的潜力.

关键词:

DFT计算的计算方法它是共变形的.这种药物是里法皮辛 (rifampicin).溶解度溶解度溶解度溶解度甲胺 (Tromethamine) 是一种甲胺.

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