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Preparation and physicochemical characterization of cocrystals for enhancing the dissolution rate of glimepiride

Iman S Jaafar , Ameera A Radhi


Aim: Glimepiride (Glmp) is an oral hypoglycemic drug used for the treatment of type 2 diabetes mellitus. It has low and unpredictable bioavailability that is mainly caused by its poor aqueous solubility and low dissolution rate. Accordingly, the objective of the present study was to improve the dissolution rate of Glmp by cocrystallization with suitable water-soluble coformers. Methods: Glmp was screened with three potential coformers, namely citric acid, tartaric acid, and oxalic acid dihydrate. Formulations were prepared at Glmp: coformer molar ratio of (1:1) and (1:2) using the solvent evaporation method. The obtained products were then characterized by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), and in vitro dissolution studies. Results and discussion: Data obtained from DSC, PXRD, and FTIR spectra suggested cocrystal formation. Cocrystals also achieved a remarkably higher dissolution rate than the parent drug. F4 containing Glmp: tartaric acid (1:2) was selected as the optimum formulation. Conclusion: In the present study, Glimepiride cocrystals are introduced as a promising strategy for a possible transition to a suitable drug product.

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