Physicochemical and mechanical properties of carbamazepine cocrystals with saccharin

Abstract

The aim of present research was to investigate the physicochemical, mechanical properties, and stability characteristics of cocrystal of carbamazepine (CBZ) using saccharin (SAC) as a coformer. The cocrystals were prepared by solubility method and characterized by pH-solubility profile, intrinsic dissolution by static disk method, and surface morphology by scanning electron microscopy (SEM), crystallinity by differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD), and mechanical properties by Heckel analysis. Stability of the cocrystals were assessed by storing them at 60 ^°C for two weeks, 25 ^°C/60%RH, 40 ^°C/75%RH and 40 ^°C/94%RH for one month and compared with the stability of CBZ. The solubility profile of cocrystal was similar to CBZ. The cocrystal and CBZ have shown the same stability profile at all the conditions of studies except at 40 ^°C/94%RH. Unlike the CBZ, cocrystal was stable against dihydrate transformation. The compacts of cocrystal have a greater tensile strength and more compressibility. The Heckel analysis suggested that plastic deformation started at low compression pressure in the cocrystal than CBZ. In summary, the cocrystal form of carbamazepine provides another avenue for product development which is more stable than the parent drug.

Keywords::

• Carbamazepine
• saccharin
• solubility
• intrinsic dissolution
• dehydrate
• stability

Acknowledgments

The authors would like to thank the Oak Ridge Institute for Science and Education (ORISE) for supporting the post doctoral research program.

Declaration of interest

The authors report no conflict of interest