Comparative permeability study of ciprofloxacin and ciprofloxacin aluminum complex through the rat small intestine in side-by-side diffusion chambers

GUZMAN, ML; BALLENT, M; LIFTCHIZ, A; BREDA, SA; MANZO, RH; OLIVERA, ME

Rosario, Santa Fé

Congreso; 41 Reunión Anual de La Asociación Argentina de Farmacologia Experimental- SAFE; 2009

Asociación Argentina de Farmacologia Experimental- SAFE

The purpose of this study was to investigate the in vitro intestinal absorption process of ciprofloxacin hydrochoride (CIP) and CIP-aluminum complex (CIP-Al). The permeability was determined in side-by-side diffusion chambers in different regions of the rat small intestine. The permeability class was ascertained by comparing drug tested with the low permeability internal standard, fluorescein. The apical to basolateral (AP-BL) and the BL-AP transport of the compounds was also investigated. All compounds were detected by fluorescence detector (275nm,  491nm (excitation) and 443nm, 515nm (emission) for CIP and fluorescein, respectively. CIP and CIP-Al exhibited no segmental dependent permeability through the gut wall (p=0,05). Both drugs exhibited significantly greater BL-AP than AP-BL permeability (p=0,05), indicative of net mucosal secretion, which significantly increased in the distal ileum in comparison to the proximal regions of the intestine (p=0,05). Based on comparison to fluorescein, CIP and CIP-Al were classified as low permeability drugs. The results demonstrate that aluminum complexation does not limit in vitro intestinal absorption. However, the in vivo comparative bioavailabilities obtained in mice, showed that the higher solubility of CIP-Al would play a major role in CIP-Al bioavailability.