New cocrystals of glibenclamide (GCM), namely, glibenclamide–hippuric acid, glibenclamide–nicotinic acid, glibenclamide–theophylline, and glibenclamide–succinic acid, were prepared using solvent assisted grinding. The formation of a new crystalline phase was preliminarily characterized by differential scanning calorimetry and powder X-ray diffraction (PXRD), which was further supported by Fourier transform infrared (FT-IR) spectroscopy and 13C solid state NMR analysis. The crystal structures of these cocrystals were determined from PXRD using BIOVIA material studio software. The data revealed the existence of new hydrogen bond interactions between -NH and the oxygen atom of the sulphamoyl group of GCM with carboxylic -CO, aromatic N (Naromatic), imidazolic -NH, and carboxylic -OH of cocrystal coformers. Equilibrium solubility and intrinsic dissolution rate studies of cocrystals in phosphate buffer of pH 7.4 showed almost 1.5–3.5 times higher solubility as compared to that of pure of GCM. This further led to improvement in both the rate and extent of absorption, thereby improving bioavailability and remarkable enhancement in antidiabetic activity. These results, therefore, demonstrate that cocrystallization was able to overcome the poor water solubility of GCM and provide a remedy for tuning its biopharmaceutical aspects.

Cocrystallization opens the door for the formulation and development of poorly soluble drugs. Exploiting this technique, novel cocrystals of gliclazide were formed, displaying a noteworthy improvement in solubility, IDR and efficacy in comparison to GL.

Objective: The present manuscript highlights the structural aspects of some polymorphic forms of nateglinide using powder x-ray diffraction (PXRD) pattern.Methods: All the polymorphic forms were isolated as microcrystalline powder, therefore, powder diffraction patterns was used as a tool to determine the crystal structure. For this, Reflux Plus module of BIOVIA Material Studio software was used. Polymorph prediction (PP) and crystal morphology analysis were performed to estimate the global minimum in lattice energy landscape and morphologically important (M. I.) facets, respectively. Besides this, to investigate the behavior of polymorphs in solution phase, in vitro studies (enthalpy of solution, solubility, intrinsic dissolution rate) were also performed. Results:A new form MS was prepared and characterized. The Form H, B, MS and S were found to exist in space group P-1, C2, P-4 and P-42C, respectively. These crystal structures were found to lie on local minima in crystal energy landscape. The stability ranking of nateglinide polymorphs follows the order: Form MS

The improvement in these physicochemical and biopharmaceutical properties corroborated the fact that the supramolecular cocrystallization may be useful in the development of pharmaceutical crystalline materials with interesting network and properties.

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