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• W1999517054 abstract "The efflux process due to p-glycoprotein-like mechanisms of ciprofloxacin (CIP) and grepafloxacin (GRX) has been studied in situ in rats and in vitro in Caco-2 cells. The results were modelled by a curve fitting procedure which allowed the characterization of the passive (Pd) and carrier mediated parameters (Vm and Km) from the raw data without initial velocities estimation. CIP absorption in rat was characterized as a passive diffusion at the assayed concentrations. Although the involvement of an efflux transporter cannot be ruled out, its relevance in the transport of the fluoroquinolone is negligible. In GRX absorption, an efflux process is implicated and it is detected in both absorption models. GRX permeability depends on the intestinal segment, reflecting the previously reported different expression level of the efflux transporters along the gut in rat. A first attempt to correlate the in vitro and the in situ data has been done. The mathematical model has been constructed using very simplistic assumptions and it will require further refinement but, nevertheless, the results are promising and demonstrate that a good modelling approach helps to identify the system critical parameters and how the system behaviour change when the parameters are modified as it happens when we move from the in vitro to the in situ level. Predicted versus experimental permeability values show a good correlation, demonstrating that the relevance of the secretion process in situ in rat can be predicted from the in vitro cell results." @default.
• W1999517054 created "2016-06-24" @default.
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• W1999517054 date "2006-01-03" @default.
• W1999517054 modified "2023-09-26" @default.
• W1999517054 title "Mathematical modelling of in situ and in vitro efflux of ciprofloxacin and grepafloxacin" @default.
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• W1999517054 doi "https://doi.org/10.1016/j.ijpharm.2005.09.014" @default.
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