应用共溶性和共结晶方法来提高阿西克洛维尔的溶解度
Elham Azad Khiabani1, Abolghasem Jouyban2,3, Anahita Fathi Azarbayjani4,5
1Student Research Committee, Urmia University of Medical Sciences, Urmia, Iran.
BMC chemistry
|July 31, 2025
概括
这项研究通过使用共结晶和共溶性来增强口服阿西克洛维尔 (ACY) 溶解度. 亚克洛维尔-甲酸共晶体实现了三倍的溶解度增加,显示出口服剂型的前景.
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:
- 乙克洛维尔 (ACY) 具有较差的水溶性和透性,限制了口服药物输送.
- 有效的口服配方需要增强抗病毒药物的可溶性和生物可用性,如ACY.
研究的目的:
- 通过共结晶和共溶性来改善阿西克洛维尔的可溶性,用于口服剂型 (片剂,溶液).
- 评估不同辅形剂和辅溶剂系统在增强ACY溶解性的有效性.
主要方法:
- 通过溶剂蒸发进行共结晶,使用酸,酸和酸作为共同形成剂.
- 使用差分扫描热度计 (DSC),X射线衍射 (XRD) 和里埃变换红外光谱 (FT-IR) 进行溶解性增强评估.
- 使用二元溶剂混合物,包括PEG 400和水,进行共融性研究.
主要成果:
- 鉴定出乙烯基酸 (ACY-AA) 和乙烯基酸 (ACY-TA) 是潜在的共晶体.
- ACY-AA共晶体表现出最高的可溶性增强,达到近三倍的增长.
- 一个PEG 400+水辅溶剂系统 (0.5:0.5比) 提供了ACY溶解度的两倍增加.
结论:
- 协结晶和协溶性都是提高阿西克洛维尔可溶性的有效策略.
- 选择合适的辅形剂和辅溶剂对于开发改进的口服阿西克洛维尔配方至关重要.
- 这些方法为制造阿西克洛维尔先进的口服药物递送系统提供了潜力.
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