Mechanochemical synthesis of a novel eutectic of the antimicrobial nitazoxanide with improved dissolution performance.

N. R. SPERANDEO

PHARMACEUTICAL SCIENCES

Tuoms Press, Tabriz University of Medical Sciences

Año: 2021 vol. 27 p. 585 - 585

1356-6881

ackground: Nitazoxanide (NTZ) is a broad spectrum antimicrobial agent with poor aqueous solubility and low bioavailability. Thus, the generation of new solid forms of NTZ is relevant to improve its unfavorable properties. The present study deals with the application of mechanochemistry for the preparation of alternate solid forms of NTZ, using saccharine (SAC) as coformer.Methods: NTZ-SAC mixtures were prepared by neat and liquid-assisted grinding (LAG) and characterized using differential scanning calorimetry (DSC), hot stage microscopy (HSM), X-ray Powder Diffraction (XRPD), 13C Solid-state Nuclear Magnetic Resonance (SSNMR) and Diffuse Reflectance Infrared Fourier Transform (DRIFT) spectroscopy. Powder dissolution (PD) profiles were obtained with USP apparatus 2 in buffer phosphate pH 6.5 with 0.25% Tween 80 - 0.25% triethanolamine and in 0.25% sodium lauryl sulfate, at 37 ºC  0.5 ºC and 75 rpm. Drug release was characterized in terms of dissolution efficiency (DE)