Solubility behavior and biopharmaceutical classification of novel high-solubility ciprofloxacin and norfloxacin pharmaceutical derivatives

BREDA, SUSANA ANDREA; JIMENEZ KAIRUZ, ALVARO FEDERICO; MANZO, RUBÉN HILARIO; OLIVERA, MARIA EUGENIA

Elsevier

Lugar: Holanda; Año: 2009 vol. 371 p. 106 - 106

he hydrochlorides of the 1:3 aluminum:norfloxacin and aluminum:ciprofloxacin complexes were characterized according to the Biopharmaceutics Classification System (BCS) premises in comparison with their parent compounds. The pH?solubility profiles of the complexeswere experimentally determined at 25 and 37 ◦C in the range of pH 1?8 and compared to that of uncomplexed norfloxacin and ciprofloxacin. Both complexes are clearly more soluble than the antibiotics themselves, even at the lowest solubility pHs. The increase in solubility was ascribed to the species controlling solubility, which were analyzed in the solid phases at equilibrium at selected pHs. Additionally, permeability was set as low, based on data reported in the scientific literature regarding oral bioavailability, intestinal and cell cultures permeabilities and also considering the influence of stoichiometric amounts of aluminum. The complexes fulfill theBCS criterion to be classified as class 3 compounds (high