Table 2

Effect of various compounds on the transcellular transport and cellular accumulation of grepafloxacin by Caco-2 cell monolayers

Compound	Transcellular Transport	Accumulation
	pmol/cm²/60 min	pmol/mg of protein/60 min
Control	265.4 ± 10.8	43.0 ± 3.2
Grepafloxacin	155.7 ± 8.0^2-150	60.5 ± 1.5^2-150
Levofloxacin	182.7 ± 4.9^2-150	44.5 ± 1.2
Cyclosporin A	189.4 ± 8.8^2-150	51.9 ± 1.7
Cyclosporin A ⁺ grepafloxacin	165.5 ± 20.7^2-150	60.5 ± 1.1^2-150
Probenecid	198.4 ± 0.9	41.4 ± 2.2
Cimetidine	221.5 ± 10.5	46.2 ± 3.5
p-Aminohippurate	233.6 ± 4.9	48.6 ± 1.1

The monolayers were incubated at 37°C for 60 min with 5 μM [¹⁴C]grepafloxacin added to the basolateral side in the absence or presence of cyclosporin A (10 μM) or other compounds (1 mM). After incubation, the radioactivity of the apical medium and the solubilized cell monolayers were measured. Each column represents the mean ± S.E. of three monolayers.

↵2-150 P < .05, significantly different from control.