Improved solubility and permeability of both nifedipine and ketoconazole based on coamorphous formation with simultaneous dissolution behavior

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چکیده

Coamorphous formation between the hydrophobic drugs nifedipine (NIF) and ketoconazole (KTZ) was investigated with expectation of improving solubility permeability two compounds. NIF KTZ spray-dried particles (SDPs) were prepared in a range NIF/KTZ molar ratios (3/1-1/3). All SDPs an amorphous state single glass transition temperature (Tg). The Tg value (1/1) showed largest positive deviation from theoretical values calculated by Gordon–Taylor equation, resulting having highest physical stability at 40°C 75% relative humidity. Fourier transform infrared spectroscopy spectra suggested hydrogen bonding NH group tertiary amine KTZ. These findings suggest coamorphous ratio 1/1 through solid state. investigation dissolution profiles that exhibited supersaturation had improved both drugs. simultaneous precipitation KTZ, whereas (2/1) (1/2) different profiles, suggesting can be maintained aqueous solution. Furthermore, permeabilities observed permeation study using Caco-2 cell line. permeated amounts 2.3- 3.6-fold higher than those individual drug crystals, respectively. This revealed has high potential to enhance improve membrane

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ژورنال

عنوان ژورنال: Journal of Drug Delivery Science and Technology

سال: 2021

ISSN: ['1773-2247', '2588-8943']

DOI: https://doi.org/10.1016/j.jddst.2021.102715