Abstract:
Diacerein (DIA) is an approved treatment for osteoarthritis. However, its clinical effectiveness is limited because of its
poor aqueous solubility, which causes bioavailability issues. The current study aimed to augment the functionality of DIA using a
cocrystallization approach. A newly developed cocrystal of DIA with β-resorcylic acid (RA) was produced at different ratios via the
antisolvent crystallization technique. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform
IR (FT-IR) spectroscopy, and scanning electron microscopy (SEM) were carried out to investigate the formation of the cocrystals.
The cocrystallized samples were further evaluated for their biopharmaceutical properties. The DSC study demonstrated a “W”-type
phase diagram with a sharp endothermic event at a DIA:RA molar ratio of 1:3. A distinct PXRD pattern at the optimized ratio
confirmed the formation of a novel cocrystal, and this was confirmed using FT-IR analysis. SEM analysis revealed the topographical
variation of the prepared cocrystal, suggesting the generation of a new solid phase. Physicomechanical properties such as apparent
solubility, dissolution, packability, compressibility, compactibility, and stability exhibited the improved functionality of the prepared
cocrystal compared with pure DIA. Significant enhancement of bioavailability (3.2-fold) was observed for the prepared cocrystal
relative to DIA alone. Hence, the fast dissolving capability and improved tabletability and bioavailability of the DIA−RA cocrystal
make it a more favorable candidate for better dosage form development
