在食状态模拟肠液中,pH对药物溶解度的间接影响
Mare Oja1, Sepanta Ehtemam1, Hristina Mircheva2
1Drug Delivery and Disposition, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, Leuven, Belgium.
International journal of pharmaceutics
|February 9, 2026
概括
通过改变肠液结构,pH间接影响药物溶解度. 在模拟的肠液中,油酸盐的存在显著增加了药物明显溶解度,突出了溶解度研究中需要现实的液体组成的需要.
科学领域:
- 药理动力学和药物新陈代谢
- 物理化学 物理化学
- 合体和接口科学科学
背景情况:
- 已知药物电离和pH值会影响溶解度.
- pH也可以通过改变肠液中的体结构来间接影响药物溶解度.
研究的目的:
- 为了研究间接pH对未充电药物的表面溶解度的影响.
- 评估脂质如单烯和酸对模拟肠液中药物溶解性的影响.
主要方法:
- 在4.5至7.5.5的pH范围内测试了13种未加电的药物.
- 使用养状态模拟肠液 (SIF) 含有塔罗霍拉酸,莱西丁和各种脂质 (单,酸).
- 分析了药物的溶解性,分别是小粒体和总脂质阶段.
主要成果:
- 酸显著提高了药物的表面溶解度,特别是在pH值6.5以下,这是由于油酸的形成和脂质滴滴的产生.
- 单烯对药物溶解度的影响很小.
- 总和细胞药物溶解率的比率增加了50倍,与药物脂性相关.
结论:
- 间接的pH影响,特别是酸的影响,对于准确的药物溶解度评估至关重要.
- 模拟的肠液成分应优化以模仿体内条件,以可靠地预测溶解度.
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