利沃素酸盐的新比例:结构,物理化学特性和功效研究
Ilma Nugrahani1, Hidehiro Uekusa2, Hironaga Oyama2
1School of Pharmacy, Bandung Institute of Technology, West Java, 40132, Indonesia.
Heliyon
|July 23, 2024
概括
开发了一种新的勒沃素 (LF) 和酸 (CA) 盐 (2:1比),以减少胃肠道刺激. 这种新型LFCA水合盐显示出与1:1比率相比较的稳定性,溶解性和功效,提供了更安全的抗生素选择.
科学领域:
- 制药化学 制药化学 制药化学
- 固态化学 固态化学
- 药物的配方 药物的配方
背景情况:
- 利沃素 (LF) 盐与酸 (CA) 在1:1摩尔比率的形成提高了稳定性和功效.
- 酸 (CA) 可以引起胃肠道刺激,需要降低其度.
研究的目的:
- 准备和表征一种新的levofloxacin-citric acid (LF-CA) 盐,使用降低的CA摩尔比率 (2:1).
- 为了研究新的LF-CA盐的结构,可溶性,稳定性和功效.
- 评估新盐作为更安全,更有效的抗生素配方的潜力.
主要方法:
- 用溶剂滴下磨砂和缓慢蒸发技术制备盐.
- 电热分析,差分扫描热度计和粉末X射线衍光计用于固态特性.
- 福利埃变换光谱光度和单晶X射线衍光度用于化学相互作用和3D结构确定.
- 稳定性,可溶性和强度测试. 稳定性,可溶性和强度测试.
主要成果:
- 成功合成了一种新的LF-CA盐,LFCA (2:1) - 4.5水合物,包含4.5个水分子.
- 确认了新的固态形成,并确定了LF和CA之间的化学相互作用.
- 新的LFCA (2:1) 水合物表现出与已建立的1:1 LF-CA盐相比的可溶性,稳定性和功效,以及与单独LF相比的优越性质.
结论:
- 新型LFCA (2:1) - 4.5水合盐在酸含量降低的情况下提供了改善的物理化学特性.
- 这种新的盐配方显示出开发一种更稳定,更安全,更有效的基于levofloxacin的抗生素的潜力.
- 这种减少的CA盐的进一步开发有望为增强的药物配方提供希望.
相关概念视频
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