控制鲁的可溶性,释放率和透率与环极素
Tatyana Volkova1, Olga Simonova1, German Perlovich1
1G.A. Krestov Institute of Solution Chemistry RAS, 153045 Ivanovo, Russia.
Pharmaceutics
|June 27, 2024
概括
这项研究使用环极素 (CD) 改善了瑞卢 (RLZ) 的溶解度. 硫乙-β-环极 (SBE-β-CD) 显示出更高的亲和力,显著增加RLZ的溶解度,并影响膜的透性.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 物理化学 物理化学
背景情况:
- 利卢 (RLZ) 是一种BCSII类药物,具有较差的水溶性,限制了其治疗功效.
- 提高溶解度和调节透性对于提高药物吸收和生物可用性至关重要.
- 环极素 (CDs) 是广泛使用的辅助剂,用于复杂化以改善药物特性.
研究的目的:
- 调查瑞卢 (RLZ) 与α-cyclodextrin (α-CD) 和sulfobutylether-β-cyclodextrin (SBE-β-CD) 的复杂化.
- 评估环极二烯复合对RLZ溶解度,溶解率和膜透性的影响.
- 探索CD和聚合物对RLZ交付的协同效应.
主要方法:
- 对RLZ与α-CD和SBE-β-CD的复杂化研究.
- 可溶性和稳定性常数的确定.
- 在实验室中使用人工膜 (纤维素,PermeaPad,聚二甲基西洛-聚碳酸盐) 的膜透性研究.
- 固体RLZ/CD复合物的制备和表征.
主要成果:
- SBE-β-CD与α-CD相比,对RLZ的亲和力更高,稳定常数表明复合物形成更强.
- 在1%的CD度下,RLZ溶解度增加了α-CD的1.7倍和SBE-β-CD的3.7倍.
- 与某些聚合物 (PG,PEG400,PEG1000) 的联合配方增强了与α-CD的可溶性,同时保持了透性.
- 穿透率在不同的人工膜上有显著差异,在水友纤维素膜上观察到的最大速率.
结论:
- 循环二烯复合,特别是与SBE-β-CD复合,有效地提高了瑞卢的溶解性.
- 选择环氧和辅助剂会影响药物的溶解性和透性.
- 了解不同膜的透特性对于预测体内药物吸收和优化输送策略至关重要.
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