Physicochemical and dissolution properties of ezetimibe-aspirin binary system in development of fixed-dose combinations

The objective of this work was to investigate binary pharmaceutical mixtures of ezetimibe (EZT) and aspirin (ASA) in order to identify whether the occurrence of eutectic in this system has an effect on EZT dissolution improvement. Ezetimibe-aspirin (EZT-ASA) solid dispersions prepared by grinding in the whole range of compositions were characterized using differential scanning calorimetry (DSC) for purpose to describe solid-liquid phase equilibrium diagram. The occurrence of interactions between ingredients was excluded by Fourier transform infrared spectroscopy and X-ray powder diffractometry. Dissolution studies have shown that the mixtures containing from 10 to 60 mass% of EZT (53.5 mass% of EZT in eutectic composition) have released ezetimibe faster than a sample of pure drug. Moreover, ASA is released more quickly from all obtained dispersions than from powder alone. Our studies have shown that obtained mixtures are useful to obtain the fixed-dose combinations, capable to deliver these two APIs together in a single system with enhanced dissolution of EZT and ASA.

Automated summary

The study demonstrated that the solid dispersions of ezetimibe and aspirin prepared in this work can release the drugs more quickly, proving the effectiveness of this formulation in enhancing drug dissolution.