阿塞克洛芬雅和L-阿尔金因盐的合成,表征和生物活性
Masood Shah1, Muhammad Naveed Umar1, Muhammad Zahoor2
1Department of Chemistry, University of Malakand at Chakdara, Dir Lower Khyber Pakhtunkhwa, Pakistan.
这项研究将一种新型的阿塞克洛菲纳克盐与l-氨酸合成,增强药物特性. 新盐表现出强大的抗炎和细胞毒性活性,表明药物的药理动力学得到改善.
科学领域:
- 制药化学 制药化学 制药化学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 分子盐合成是改善食品和药物管理局 (FDA) 批准的药物的生物可用性和溶解性的关键策略.
- 阿塞克洛芬雅 (ACF) 是一种具有有限可溶性的非类固醇抗炎药物 (NSAID),通常需要配方策略来增强其治疗疗效.
研究的目的:
- 为了合成和表征一种新型的aceclofenac分子盐,使用l-arginine (ARG) 作为辅制剂.
- 评估合成的阿塞克洛芬亚克-l-阿尔金因 (ACF-ARG) 盐的物理化学特性和生物活性.
主要方法:
- 快速溶剂蒸发沉技术用于ACF-ARG盐合成,其摩尔比为1:1.
- 描述涉及福里埃变换红外光谱 (FTIR),差分扫描热量计 (DSC),粉末X射线衍射 (PXRD) 和热重力分析 (TGA).
主要成果:
- FTIR和DSC分析证实了阿塞克洛芬雅和l-阿尔金因之间的相互作用和盐形成.
- PXRD揭示了ACF-ARG盐的独特结晶相,与母化合物不同.
- TGA表示合成盐的无水性质.
- 该ACF-ARG盐表现出显著的抗炎和细胞毒性活性.
结论:
- 使用像l-arginine这样的共同形成剂的药物联合结晶是一种开发新药配方的有希望的方法.
- 合成的阿塞克洛芬亚克-l-阿尔金因盐为增强药物的药理动力学和治疗潜力提供了一种新的策略.
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