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Vol. 289, Issue 1, 149-155, April 1999
Institute of Pharmaceutical Sciences, Hiroshima University School
of Medicine, Hiroshima, Japan
Effects of cytochrome P-450 3A- and P-glycoprotein (P-gp)-related
compounds, erythromycin, midazolam, ketoconazole, verapamil, and
quinidine, on transport of rhodamine 123 (Rho-123), a P-gp substrate,
were studied in rat intestine and in Caco-2 cells. Ileum was mainly
used in rat studies because this segment showed greater P-gp-mediated
Rho-123 transport. In an in vitro everted rat ileum, all the compounds
examined significantly inhibited the transport of Rho-123 from serosal
to mucosal surfaces across the intestine, with different inhibitory
potencies among these compounds. In an in vivo rat study, the
exsorption of Rho-123 from blood to the intestinal lumen, which was
evaluated as exsorption clearance of Rho-123 under a steady-state
plasma concentration of Rho-123, was also inhibited when these
compounds were added to the intestinal lumen. Similarly,
transepithelial transport of Rho-123 from the basolateral to apical
side across Caco-2 cell monolayers was inhibited by these compounds. A
linear relationship was observed in their inhibitory potencies on
Rho-123 transport between in vitro and in vivo studies using rat ileum
and between studies with rat ileum and Caco-2 cells. P-gp-mediated
transport across the intestine was found to be inhibited not only by
P-gp-related but also by all the cytochrome P-450 3A-related compounds
examined. Within experimental error, the relative inhibitory potencies
were the same between the studies with rat ileum (in vivo, in vitro) and those with Caco-2 cells. Thus, it is suggested that the function of
P-gp and its sensitivity to these drugs may be similar in rat intestine
and Caco-2 cells.
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