Enhancing Norfloxacin’s Solubility and Antibacterial Activity through Pharmaceutical Salt Formation with Fluorobenzoic Acids

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Authors: Shuhui Wang, Jiashu He, Chenyu Ruan, Panyue Cao, Ziyi Zhang, Chengjun Jiang
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Abstract

Norfloxacin (NOR), a broad-spectrum fluoroquinolone antibiotic, is widely used to treat bacterial infections.However, its clinical application is hindered by poor aqueous solubility and low oral bioavailability.To address these limitations, this study developed two novel pharmaceutical salts of NOR using 4fluorobenzoic acid (4-FA) and 2-fluorobenzoic acid (2-FA) as counterions.The salts were synthesized via slow evaporation crystallization, and their structures were characterized by single-crystal X-ray diffraction (SCXRD).Comprehensive solid-state analyses, including powder X-ray diffraction (PXRD), Fourier-transform infrared (FT-IR) spectroscopy, and differential scanning calorimetry (DSC), confirmed the successful formation of the salts.Notably, the salt formation significantly improved NOR's solubility and dissolution behavior.Furthermore, these modifications enhanced NOR's antibacterial efficacy, as evidenced by stronger bacterial inhibition and reduced minimum inhibitory concentration (MIC) values.This study demonstrates a promising strategy for optimizing the biopharmaceutical performance of NOR through salt formation.

Fields of Study & Subjects

Crystallization and Solubility Studies Drug Solubulity and Delivery Systems Crystallography and molecular interactions

Publication details

Journal / source
OALib
Volume
13
Issue
02
Pages
1–14
Publication date
1 January 2026