Binary and ternary complexes of norfloxacin to improve the solubility of the active pharmaceutical ingredient

PONCE-PONTE, MICAELA; ALOISIO, CAROLINA; ROMERO-GUERRA, DIANA MARCELA; GRACIA-VÁSQUEZ, SANDRA; GARNERO, CLAUDIA; LONGHI, MARCELA

Therapeutic Delivery

Future Science

Año: 2018 vol. 9 p. 639 - 639

2041-5990

im: Binary and ternary complexes with hydroxypropyl-β-cyclodextrin (HPβCD), using glutamic acid (GA), proline or lysine as the third component, were developed to increase the solubility and the dissolution rate of norfloxacin (NOR). Methods/results: Complexation was evaluated by phase solubility studies, obtaining the highest NOR solubility with GA and HPβCD. Thermal analysis suggested that different kinds of interactions occur among NOR, HPβCD and each amino acid, and when the systems were prepared by kneading or by means of freeze-drying technique. Dissolution studies, performed on simulated gastric fluid and subsequent simulated intestinal fluid, showed the highest rate of NOR from NOR?HPβCD?GA. Conclusion: NOR:HPβCD:GA was the best approach for improving the bioavailability of NOR.