通过与结构相似的多联体共结晶来改善thiabendazole的药物特性
1School of Chemistry and Chemical Engineering, Shanghai University of Engineering Science, Shanghai 201600, China.
Chemical & pharmaceutical bulletin
|January 14, 2026
概括
两种新的 thiabendazole (TBZ) 共同晶体使用复醇和黄醇被开发出来,显著改善了 TBZ.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 晶体学 晶体学是指结晶学.
背景情况:
- 提亚班达 (TBZ) 是一种固有的不溶于水的抗真菌剂.
- 改善TBZ的水溶性和溶解对于其治疗疗效至关重要.
- 凝结晶形成是提高难溶药物的物理化学性能的一个有前途的策略.
研究的目的:
- 准备和表征新型的 thiabendazole (TBZ) 共同晶体,使用树脂醇 (RES) 和花醇 (PHG) 作为共同晶体形成剂 (CCF).
- 研究CCF结构对TBZ共晶体的分子间相互作用,溶解性和溶解的影响.
- 探索TBZ共晶的潜力,以提高药物输送.
主要方法:
- 用于准备共晶的溶剂蒸发方法.
- 使用单晶X射线衍射 (SCXRD),粉末X射线衍射 (PXRD),热重力测量-微分扫描热量测量 (TG-DSC) 和里埃变换红外光谱法 (FT-IR) 进行全面的表征.
- 希尔什菲尔德表面分析用于研究分子间相互作用.
- 测量可溶性和溶解速度.
主要成果:
- 两种新的TBZ共晶,TBZ-RES和TBZ-PHG,已经成功合成.
- 与纯 TBZ 相比,这两种共晶都显著增强了水溶性和溶解.
- 具有2:1固态度的TBZ-PHG共晶体,由于增强的键和破坏的π-π堆叠,导致溶剂透,使溶解度得到更大的改善.
结论:
- 成功开发出了具有可溶性和溶解概况改进的新型TBZ共晶.
- 同晶前的选择显著影响了TBZ的晶体结构,分子间相互作用和物理化学性质.
- 这些发现突出了共结晶的潜力,作为一种有效的策略,以提高像TBZ这样的溶解不良药物的生物可用性.
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