基本氨基酸对叶酸可溶性的影响
Karen Pérez-Carreón1, Luz María Martínez1, Marcelo Videa1
1School of Engineering and Sciences, Tecnologico de Monterrey, Campus Monterrey, Ave. Eugenio Garza Sada 2501 Sur. Monterrey N.L., Monterrey 64849, Mexico.
Pharmaceutics
|November 25, 2023
概括
叶酸 (FA) 溶解度通过与基本氨基酸 (氨酸和氨酸) 形成二元配方,显著提高. 这种共同形态化策略为改善药物应用中的FA生物可用性提供了一个有希望的方法.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 生物化学 生物化学
背景情况:
- 叶酸 (FA) 对于预防神经管缺陷至关重要,但溶解性差 (IV类BCS药物).
- 提高FA溶解度对于有效的制药配方至关重要.
- 氨基酸 (AA) 可以通过共同形态化或盐形成来提高难以溶解药物的溶解性.
研究的目的:
- 研究基本氨基酸 (氨酸和氨酸) 对叶酸溶解度的影响.
- 为了确定FA-AA二进制配方的最佳摩尔比率.
- 描述产生的配方的物理和化学特性.
主要方法:
- 导电度量定位用于确定最大限度地提高FA可溶性的有效摩尔比率.
- 用不同的方法制备了FA与阿尔金宁和氨酸的二元配方.
- 描述包括差异扫描热度计 (DSC),里埃变换红外光谱 (FTIR) 和X射线衍射 (XRD) 来确认无形系统.
主要成果:
- 发现 1:2.5 FA:AA 摩尔比最大限度地提高了阿尔金宁和氨酸的溶解度.
- 二进制配方显示出明显增强的溶解度,与纯FA相比增加了5500-6000倍.
- 制备方法影响了无形二进制系统的形态特性.
结论:
- 与基本氨基酸 (氨酸和氨酸) 共同成形有效地提高了叶酸溶解度.
- 开发的FA-AA二进制系统代表了改善FA生物可用性的有希望的策略.
- 了解形态特性是潜在的药物扩展的关键.
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