Favipiravir-levofloxacin salt reaction and its impact on the physicochemical properties
Abstract
Antivirals are often combined with antibiotics to treat infectious diseases, yet studies on their multicomponent systems remain limited. This experiment aimed to develop a multicomponent system combining the antiviral favipiravir (FAV) and the antibiotic levofloxacin (LF) and to investigate its effects on physicochemical properties, antibiotic potency, and toxicity. First, the stoichiometric ratio of the new compound was determined by thermal analysis and powder X-ray diffractometry, yielding a 1:1 molar ratio. Subsequently, FTIR analysis was performed to elucidate the 2D structure, followed by the determination of the 3D structure using single-crystal X-ray diffraction. The results showed that FAV reacted with LF via wet grinding, producing a new multi-component system (FAV-LF) with a distinct thermal profile and diffractogram. The structural data indicated that the multicomponent system was a salt, which exhibited greater stability but lower solubility than the individual components. Potency tests demonstrated that the salt enhanced the antibacterial activity of LF against Gram-positive bacteria, but had no effect against Gram-negative bacteria. Furthermore, based on toxicity test predictions, the FAV-LF salt exhibited reduced mutagenicity compared with LF alone and effectively mitigated blood-brain barrier toxicity relative to FAV alone. Therefore, comprehensive experiments can further develop dosage formulations of the FAV-LF salt.
Read the paper
Related studies
- Ferulic acid regulates the AKT/GSK-3β/CRMP-2 signaling pathway in a middle cerebral artery occlusion animal model
- Novel Pharmacokinetic/Pharmacodynamic Parameters Quantify the Exposure–Effect Relationship of Levofloxacin against Fluoroquinolone-Resistant Escherichia coli
- Photochemical behavior of levofloxacin
- Correlation Between Dissolution Profiles of Salt-Form Drugs in Biorelevant Bicarbonate Buffer and Oral Drug Absorption: Importance of Dose/ Fluid Volume Ratio
- Evaluation of the synergistic potential and mechanisms of action for de novo designed cationic antimicrobial peptides
- Synthesis of [11C]levofloxacin
Go deeper in Evidence Hub
Evidence Hub adds a study data sheet (design, sample size, evidence level, key numbers), an AI summary and a chat grounded in the paper's text.