胆化物-酸 天然深性溶剂 含有疏水性药物的溶剂:对消化道模型中的溶解性和透性行为的洞察
Stefano Sangiorgi1, Matilde Mancinelli2, Serena Bertoni1
1University of Bologna, Dep. of Pharmacy and BioTechnology, Via San Donato 19/2 I-40127, Italy.
International journal of pharmaceutics
|November 11, 2025
概括
天然深层阳溶剂 (NaDES) 提高溶解性和溶解性,用于溶解性较差的药物. 然而,它们在药物输送中的有效性取决于胃肠道内的药物特性和相互作用.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 绿色化学 绿色化学
背景情况:
- 难溶性药物 (BCS II类) 的生物制药性能仍然是一个挑战.
- 天然深层阳性溶剂 (NaDES) 为药物配方提供了一个有前途的绿色替代品.
- 胆化物和酸形成一个具有药物溶解潜力的NADES.
研究的目的:
- 评估六种BCSII类药物的生物制药性能,这些药物是用胆化-酸NaDES配制的.
- 评估NaDES对药物溶解度,超和透性的影响.
- 了解药物物理化学特性对基于NaDES的配方疗效的影响.
主要方法:
- 在NADES和生物相关介质 (FaSSGF,FaSSIF) 中的溶解性研究.
- 在体外稀释研究以评估超和潜力.
- 使用仿生Permeapad®屏障进行透性研究.
主要成果:
- 与消化介质相比,NaDES显著增加了药物的溶解性 (5至70倍).
- 纳德斯促进了卡巴马西平和弱基药物 (log P ≤ 4) 的超和.
- 对于中性和基本药物观察到增强的透性,但不是酸性药物.
结论:
- 胆化物-酸NADES显示出作为绿色药物输送平台的潜力.
- 药物的生物可用性增强取决于API的物理化学特性和NaDES相互作用.
- 活体中NADES的性能受结,疏水性和胃肠道液体组成的影响.
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