Five distinct crystal forms of rifaximin have been identified and characterised by X-ray powder diffraction, solid state 13C NMR, and HATR-IR spectroscopy. Changes in the crystal structure may produce differences of two to three orders of magnitude in the rate of intrinsic dissolution, solubility and bioavailability of rifaximin. Alteration of the pharmacokinetic parameters is of particular interest; the Cmax values of the crystal forms range from 1.1 to 1085.31 ng ml-1 and the AUC0-24 h values range from 10 to 4795 ng h ml-1. These findings are relevant to the therapeutic use of rifaximin.
G. C. Viscomi, M. Campana, M. Barbanti, F. Grepioni, M. Polito, D. Confortini, et al. (2008). Crystal forms of rifaximin and their effect on pharmaceutical properties. CRYSTENGCOMM, 10, 1074-1081 [10.1039/b717887e].
Crystal forms of rifaximin and their effect on pharmaceutical properties
GREPIONI, FABRIZIA;POLITO, MARCO;ROSINI, GOFFREDO;RIGHI, PAOLO;BRAGA, DARIO
2008
Abstract
Five distinct crystal forms of rifaximin have been identified and characterised by X-ray powder diffraction, solid state 13C NMR, and HATR-IR spectroscopy. Changes in the crystal structure may produce differences of two to three orders of magnitude in the rate of intrinsic dissolution, solubility and bioavailability of rifaximin. Alteration of the pharmacokinetic parameters is of particular interest; the Cmax values of the crystal forms range from 1.1 to 1085.31 ng ml-1 and the AUC0-24 h values range from 10 to 4795 ng h ml-1. These findings are relevant to the therapeutic use of rifaximin.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
