Synchrotron XRD based Structural analysis of Novel Fleroxacin Cocrystals synthesized using coformers

Abstract

Cocrystals have emerged as an exciting avenue in the pharmaceutical industry for altering the behavior of drugs while preserving the molecular structures of the active pharmaceutical ingredients (APIs). However, the preparation of pharmaceutical cocrystals remains relatively uncommon, presenting a potential opportunity for innovation. In this study, we developed cocrystals of Fleroxacin, a fluoroquinolone antibiotic belonging to the quinolone antibiotic class used in treating bacterial infections. Our approach involved co-crystallizing Fleroxacin with coformers (nicotinamide, salicylamide, and acetaminophen). The combination of Fleroxacin with different coformers allows us to explore chemical properties and the crystal efficacy. To achieve cocrystal formation, we employed a novel catalyst, pure glacial acetic acid, in conjunction with a ball milling machine. This methodology is particularly notable as it represents a first-time application of pure glacial acetic acid for co-crystallization and the co-crystallization of Fleroxacin. The cocrystals characteristics were analyzed using Synchrotron Powder X-ray Diffraction. The results showed the formation of novel cocrystals of Fleroxacin. The findings of this study contribute to the expanding body of knowledge on co-crystallization techniques and their potential applications in pharmaceutical development, especially for carboxylic acid-based drugs and drugs with very poor water solubilities but great permeabilities.