Preparation of Chloramphenicol/Amino Acid Combinations Exhibiting Enhanced Dissolution Rates and Reduced Drug-Induced Oxidative Stress

STERREN, VANESA B.; AIASSA, VIRGINIA; GARNERO, CLAUDIA; LINCK, YAMILA GARRO; CHATTAH, ANA K.; MONTI, GUSTAVO A.; LONGHI, MARCELA R.; ZOPPI, ARIANA

AAPS PHARMSCITECH

SPRINGER

Año: 2017

1530-9932

hlorampbenicol is an old antibiotic agent that is re-emerging as a valuablealtemative for the treatment of mullidrug-resistant pathogens. However, it exhibits suboptimal biopharmaceurical properties and toxicity profiles. Ln this work, chloramphenicol was cornbined with essentia l amino acids (arginine, cysteine, glycine. and leucine) with the aim of improving its dissolurion rate and reduce its toxicity towards leukocytes. The chloramphenicollamino acid solid samples were prepared by freeze-drying method and characterized in the solid state by using Fourier transform infrared spech·oscopy, powder Xray diffraction, differential scanning caJorimetry, scanuing electron microscopy, and solidstatenuclear magnetic resonance. The dissolution properties, antimicrobial activity, reactive oxygen species production, and stability of the diffe rent samples were studied. The dissolution rate of all combinations was significantly increased in comparison to tbat of the pure active pharmaceutical in