表面活性剂显著改善了黄素无形固体分散的口服生物可用性及其潜在机制
Jinhua Yuan1, Siyi Mao1, Xiuzhen Ma1
1School of Pharmacy, Minzu University of China, Beijing 100081, China.
Pharmaceutics
|December 31, 2025
概括
无形固体分散 (ASD) 中的表面活性剂通过维持超和和稳定无形药物形式,极大地提高了药物的生物可用性. 了解这些药物-聚合物-表面活性剂相互作用是合理的ASD设计和预测性能的关键.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 无形固体分散 (ASDs) 使用表面活性剂来增强药物溶解和生物可用性.
- 对ASD表面活性剂机制的清晰理解对于有效的配方设计和预测体外-体内相关性 (IVIVC) 至关重要.
研究的目的:
- 研究不同表面活性剂对ASD中药物聚合物相互作用的影响.
- 阐明表面活性剂改善药物溶解,细胞吸收和口服生物可用性的机制.
- 为合理的ASD发展建立体外表现和体内药理动力学之间的关系.
主要方法:
- 使用旋转蒸发制备二元 (药物/聚合物) 和三元 (药物/聚合物/表面活性剂) ASD.
- 使用光谱技术 (1H NMR,FT-IR) 进行药物-聚合物-表面活性剂相互作用的表征.
- 进行了体外溶解研究,细胞吸收测定和体内药理动力学评估.
主要成果:
- 表面活性剂显著影响了药物聚合物相互作用和ASD纳米结构的形成.
- 库尔/P188/SLS ASD表现出优异的超和度,持续的无形沉物稳定性和增强的细胞吸收.
- 对于含有特定表面活性剂的ASD配方,观察到改善的口服生物可用性,这与维持高能药物状态有关.
结论:
- 表面活性剂对ASD的表现至关重要,通过超和,纳米结构形成和无形沉物稳定性来保持高能药物状态.
- 这些机制共同增强细胞吸收和口服生物可用性,突显了药物-聚合物-表面活性剂相互作用的重要性.
- 该研究提供了关于表面活性剂功能的重要见解,以指导合理的ASD配方并改善IVIVC预测.
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