Preparation, Evaluation, In vitro Anti-diabetic and Stability Studies of Glibenclamide Loaded Cocrystals

Background Glibenclamide (BCS Class-II .Drug) has poor solubility and high permeability. In the co-crystallization technique, drugs are combined with a suitable coformer via H- bonding. Glibenclamide cocrystals have been prepared with various coformers but glibenclamide cocrystals with vanillic acid have not been prepared yet.Objective To prepare glibenclamide cocrystals with vanillic acid coformer and evaluate them using various techniques, along with in vivo antidiabetic studies and stability studies.Method Cocrystals containing glibenclamide were produced with vanillic acid coformer by the solvent evaporation method in a 1:1 molar ratio.Result In FTIR analysis, an H-bond is formed between the amide group of the drug and the carboxylic acid group of the coformer. With the help of DSC and HSM, the melting point of cocrystals was observed at a different point compared to the melting point of glibenclamide drug and vanillic acid coformer. In the XRD analysis of cocrystals, peaks with high intensity were observed at different points than that of the drug and coformer, confirming the crystalline nature of the formulation. During in vitro dissolution studies, cocrystals showed a better dissolution profile compared to the marketed formulation and the pure drug in both acidic and alkaline media. In vivo anti-diabetic studies were conducted using male Wistar rats, confirming that the glucose reduction percentage from cocrystals was more than that of the pure drug. During stability studies, no significant changes occurred in the dissolution profile of the formulation, which indicated that the formulation was stable after storage at an ambient temperature.Conclusion The results obtained from various characterization techniques indicate that glibenclamide cocrystals formed from vanillic acid enhance the solubility of glibenclamide.