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基于环德克斯的包容复合物来增强因达帕米德的可溶性和口服生物可用性:实验和计算方法

Khaldoun A Al-Sou'od¹, Gaith M Al-Qudah¹, Rajab Abu-El-Halawa¹

¹Department of Chemistry, Al al-Bayt University, Mafraq, Jordan.

Drug development and industrial pharmacy

|December 9, 2025

概括

这项研究使用循环德克斯特林包容复合物增强了因达帕米德的溶解性,而硫乙烯-β-CD显示出最有前途的结果. 这种方法提高了难溶性利尿剂的口服生物可用性.

科学领域:

制药科学制药科学
药物运输药物运输药物运输
物理化学物理化学

背景情况:

作为利尿剂的英达帕米德,由于水溶性较低,口服生物可用性较差,这是BCSII类药物的常见问题.
循环二烯含有复合物提供了一种可行的策略,以提高水溶性较差的药物的可溶性和有效性.

研究的目的:

通过与各种环极素形成包含综合体,增强因达巴胺的溶解性和稳定性.
通过综合实验计算方法,提供对主机-客机相互作用和稳定性的机制性理解.

主要方法:

使用阶段溶解性研究对五种环极素 (α-CD,β-CD,γ-CD,HP-β-CD,SBE-β-CD) 的系统评估.
热力学分析 (van't Hoff) 和固态表征 (SEM,XRD,HPLC). 热力学分析 (van't Hoff) 和固态表征 (SEM,XRD,HPLC). 热力学分析 (van't Hoff) 和固态表征 (SEM,XRD,HPLC). 热力学分析 (van't Hoff) 和固态表征 (SEM,XRD,HPLC). 热力学分析 (van't Hoff) 和固态表征 (SEM,XRD,HPLC).
分子建模 (MM+,PM3) 以评估结合能和宿主-客人相互作用.

主要成果:

硫乙-β-CD (SBE-β-CD) 产生了最高的因达巴胺溶解度 (约. 8.7倍) 通过 1:1 纳入复合体.
纳入过程是自发的,外热的,热驱动的,SBE-β-CD显示最稳定的结合 (ΔE = -28.8 kcal·mol−1).
鉴定证实了因达巴胺转化为无形状态,表明有效的复合.

结论:

修改后的环极素,特别是SBE-β-CD,显著提高了因达巴胺的溶解性,溶解性和潜在的口服生物利用性.
该研究为选择水溶性较差药物的辅助剂和过程提供了机制基础和实际框架.

关键词:

伊达帕米德是什么意思循环德克斯特林 (Cyclodextrins) 是一个循环德克斯特林.药物输送系统是药物输送系统.包括性复杂化包括性复杂化分子建模分子建模口服生物可用性口服生物可用性

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