Ahmed Mahmoud Abdelhaleem Ali
Beni Suef University, Egypt
Title: Quetiapine-nicotinamide co-amorphous dispersion: A new strategy for improving physicochemical properties and ex-vivo performance of a model antipsychotic drug
Biography
Biography: Ahmed Mahmoud Abdelhaleem Ali
Abstract
The goals of this research were focused on improving the water solubility and dissolution rate of quetiapine fumarate to enable faster oral and buccal bioavailability and enhanced antipsychotic properties. The coamorphous dispersion strategy was achieved using nicotinamide as highly soluble conformer. The prepared quetiapine/ nicotinamide coamorphous dispersions (QNCD) were characterized using scanning electron microscopy (SEM) differential scanning calorimetry (DSC), Fourier transform infra red sepectroscopy (FTIR) and X-ray powder diffraction (XRPD). Static disc intrinisic dissolution rate and ex-vivo diffusion through inverted intestinal tissues were conducted and compared to pure quetiapine. The results demonstrated a highly soluble (QNCD) formed between quetiapine fumarate and nicotinamide at 1:3 molar ratio through H-bonding interactions. The equilibrium solubility results showed 3 folds increase in solubility of quetiapine from the dispersions. High intrinsic dissolution rate (0.603 mg cm-2 min-1) and faster flux rate (0.041 mg cm-2 h-1) were obtained from the dispersion compared to pure quetiapine fumarate (0.284 mg cm-2 min-1) and (0.027 mg cm-2 h-1), repectively. The newly prepared QNCD proved to be effective in improving the drug physicochemical properties and enhanced its ex-vivo diffusion properties. Therefore, this approach could be a considerable solution for new delivery systems of quetiapine by virtue of its augmented physicochemical attributes and improved ex-vivo diffusion which is expected to raise its extra-vascular bioavailability.