Enhanced dissolution and solubility of Epalrestat with β-Cyclodextrin ternary complex using Arginine
The objective of present is work to achieve improvement in solubility and dissolution using Epalrestat with β-cyclodextrin ternary complex with addition of L-arginine. Kneading method with and without incorporation of L-arginine was used to obtain the solid systems (binary and ternary complex) of Epalrestat with β-cyclodextrin and characterized for DSC, PXRD, SEM. Phase solubility, saturation solubility, dissolution and stability studies were carried out. The effect of L-arginine was investigated on complexation efficiency of β-cyclodextrin towards Epalrestat in an aqueous media through phase solubility according to Higuchi and Connors. Phase solubility studies showed AL (linear) type of solubility curve in presence of L-arginine, the complexation efficiency and association constant of β-cyclodextrin towards Epalrestat were promoted by L-arginine signifying its use as a ternary component. Dissolution rate of Epalrestat and solubility were significantly improved by complexation with β-cyclodextrin as compared to Epalrestat alone. Ternary complex incorporated with L-arginine proved better than binary complex. Hence, L-arginine could be exploited as a ternary component to improve the solubility of Epalrestat via β-cyclodextrin complexation.
Keywords: Epalrestat, solubility enhancement, inclusion complexes, β-cyclodextrin, L-arginine.
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