Abstract
A novel chemical structure named pharmaceutical cocrystal was synthesized with the purpose to enhance the solubility of levofloxacin (LVFX). Nicotinic acid (NA) was selected as cocrystal coformer (CCF). The cocrystal was successfully obtained by solvent evaporation method combined with ultrasonic technology. The crystal structure of LVFX-NA is triclinic with a P1 space group, unit cell parameters a = 7.1392 Å, b = 10.0188 Å, c = 17.5394 Å, α=86.109 (7), β=86.082 (6), γ=73.809 (7), z = 2, R1=0.0518, ωR2=0.1425. The supramolecular structure of LVFX-NA is mainly controlled by OH···N and CH···O intermolecular hydrogen bond. Moreover, intramolecular hydrogen bonds CH···F have also been found in the cocrystal structural units. The obtained cocrystal exhibits unique properties of thermoanalysis, Fourier transform infrared (FT-IR) spectrum and X-ray powder diffraction (PXRD) spectrum, demonstrated the new formed crystal material. Equilibrium solubility measurement revealed that LVFX-NA exhibited improved aqueous solubility, that is 5.02 times higher than the original LVFX.
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