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通过绿色方法制备的levofloxacin - dicarboxylate盐的固态特性和抗生素功效

Ilma Nugrahani¹, Afifah Faadilah Nuur Aini¹, Marlia Singgih Wibowo¹

¹School of Pharmacy, Bandung Institute of Technology, Indonesia.

|December 6, 2024

概括

使用溶剂滴滴研磨改进了levfloxacin (LF) 二碳酸盐盐的绿色合成 LF.

科学领域:

绿色化学绿色化学
制药科学制药科学
材料科学材料科学材料科学

背景情况:

列沃素 (Levofloxacin,简称LF) 是一种广泛使用的诺类抗生素.
提高现有药物的稳定性,溶解性和有效性对于药物开发至关重要.
新型盐形式可以增强药物输送和治疗疗效.

研究的目的:

探索新型levofloxacin二碳酸盐的绿色合成方法.
研究这些盐对利沃素稳定性,溶解性和抗菌活性的影响.
描述合成盐的固态特性和结构相互作用.

主要方法:

使用95%的乙醇制备盐的溶剂滴滴研磨 (SDG).
使用电热分析,差分扫描热度计 (DSC) 和粉末X射线衍光计 (PXRD) 进行固态特征.
通过福里埃变换红外光谱 (FTIR) 和核磁共振 (1H-NMR) 进行结构确认.

主要成果:

SDG成功地生产了勒沃素-酸 (LF-OX) 水合物,勒沃素-酸 (LF-SA) 水合物和勒沃素-马龙酸 (LF-MN) 无水盐,其摩尔比例为1:1.
在LF-OX和LF-SA水合物中观察到新的PXRD模式.
合成的LF-dicarboxylate盐与自由的levofloxacin相比,显示出更强的溶解性,稳定性和抗菌作用力.

结论:

溶剂滴滴研磨提供了一种更绿色和更有效的方法来合成利沃素二碳酸盐.
新型LF-二碳酸盐表现出优越的物理化学和生物特性.
这些发现表明,开发先进的勒沃弗洛克萨辛剂量配方有很大的潜力.

关键词:

利沃弗洛克萨辛 (Levofloxacin) 是一种药物.酸是什么酸是什么酸是什么马龙酸是什么马龙酸是什么多组件系统多组件系统.氧化酸是一种氧化酸.强度强度强度强度盐盐盐盐盐盐盐可溶性溶解度溶解度溶解度稳定的稳定性稳定的稳定性葡萄糖酸是什么葡萄糖酸是什么

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