Characterization of systems with amino-acids and oligosaccharides as modifiers of biopharmaceutical properties of furosemide

AYALA, ALEJANDRO P.; GARNERO, CLAUDIA; AYALA, ALEJANDRO P.; GARNERO, CLAUDIA; LONGHI, MARCELA R.; STERREN, VANESA; ZOPPI, ARIANA; LONGHI, MARCELA R.; MIRANDA, JULIETA ABRAHAM; ZOPPI, ARIANA; STERREN, VANESA; MIRANDA, JULIETA ABRAHAM

JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

ELSEVIER SCIENCE BV

Año: 2018 vol. 149 p. 143 - 150

0731-7085

Furosemide is the most commonly prescribed diuretic drug in spite of its suboptimal biopharmaceutical properties. In this work, the addition of different amino-acids was studied with the aim of selecting an enhancer of the furosemide solubility. The best results were obtained with arginine. Also, binary (furosemide:arginine) and ternary (furosemide:arginine:β-cyclodextrin and furosemide:arginine:maltodextrin) systems were prepared by the kneading method and they were compared with their corresponding physical mixtures. These new systems were characterized by Fourier transform infrared and Raman spectroscopy, X-ray powder diffractometry, scanning electron microscopy, thermogravimetric analysis, and differential scanning calorimetry. In addition, dissolution studies were performed in simulated gastric fluid. The best results in relation to improving biopharmaceutical properties were obtained with a binary combination of furosemide and arginine, demonstrating that this system could result in a suitable candidate for the development of a promising pharmaceutical formulation of the drug.