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  • Possible ciprofloxacin interactions with metal cations and its permeability through rat intestine 'In vitro'
    Kristl, Albin ; Žakelj, Simon
    Purpose. To determine the permeability mechanism of ciprofloxacin through the rat jejunum ćin vitroć. Methods. Side-by-side diffusion chambers were used to determine permeability coefficients (Papp) ... through isolated segments of rat intestine in mucosal to serosal and serosal to mucosal direction under different conditions. The paracellular permeability standard fluorescein was used during the permeability experiments. Results. There are no significant differences between the m-to-s permeability coefficients of ciprofloxacin and fluorescein obtained in the different intestinal regions indicating that thereis no regionally dependent active process involved in the ciprofloxacin absorption from the lumen. On the other hand Papp values of ciprofloxacin in the s-to-m direction are significantly higher in the lower region of the rat small intestine indicating that the expression level of the efflux proteins mediating ciprofloxacin efflux is higher in this region of the rat small intestine. Additionally, we could not find any evidence that the presence of benzbromarone (a MRP2 inhibitor) or verapamil (a PgpžMRP2 inhibitor) in incubation medium would influence the ciprofloxacin efflux properties. The m-to-s Papp values of ciprofloxacin were measured in the presence and absence of Ca2+ and Mg2+ ions in the mucosal (donor) solution. The obtained Papp values did not change regarding the Ca2+ and Mg2+ concentration, although the concentrations of these ions were even higher (10mM) than in standard Ringer buffer (1.2mM). The permeability of CIP was measured in modified Ringer buffers with pH values ranging from 6.0 to 8.0. It was established that the highest ciprofloxacin efflux can be observed at pH 6.5. This could indicate that maximal activity of the ĆCIP-sensitive pathwayĆ is at this pH. Conclusions. Ciprofloxacin is actively secreted in s-to-m direction. The probable reason for this is an efflux system called cyprofloxacin - sensitive pathway. The presence of metal cations (Ca2+, Mg2+) does not influence the absorption process of ciprofloxacin.
    Vir: Final program ([1] f.)
    Vrsta gradiva - prispevek na konferenci
    Leto - 2005
    Jezik - angleški
    COBISS.SI-ID - 1833329

vir: Final program ([1] f.)

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