New Organic Salt from Levofloxacin-Citric Acid: What Is the Impact on the Stability and Antibiotic Potency?

左氧氟沙星-柠檬酸的新有机盐:对稳定性和抗生素效力有何影响?

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作者:Ilma Nugrahani, Agnesya Namira Laksana, Hidehiro Uekusa, Hironaga Oyama

Abstract

This research dealt with the composition, structure determination, stability, and antibiotic potency of a novel organic salt composed of levofloxacin (LF) and citric acid (CA), named levofloxacin-citrate (LC). After a stoichiometric proportion screening, the antibiotic-antioxidant reaction was conducted by slow and fast evaporation methods. A series of characterizations using thermal analysis, powder X-ray diffractometry, vibrational spectroscopy, and nuclear magnetic resonance confirmed LC formation. The new organic salt showed a distinct thermogram and diffractogram. Next, Fourier transform infrared indicated the change in N-methylamine and carboxylic stretching, confirmed by 1H nuclear magnetic resonance spectra to elucidate the 2D structure. Finally, single-crystal diffractometry determined LC as a new salt structure three-dimensionally. The attributive improvements were demonstrated on the stability toward the humidity and lighting of LC compared to LF alone. Moreover, the antibiotic potency of LF against Staphylococcus aureus (Gram-positive) and Escherichia coli (Gram-negative) enhanced ~1.5-2-fold by LC. Hereafter, LC is a potential salt antibiotic-antioxidant combination for dosage formulas development.

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