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. 1993 Mar;108(3):575–576. doi: 10.1111/j.1476-5381.1993.tb12844.x

Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco-2 cell layers.

N M Griffiths 1, B H Hirst 1, N L Simmons 1
PMCID: PMC1908048  PMID: 8467353

Abstract

The bidirectional transepithelial fluxes of ciprofloxacin, an antibacterial fluoroquinolone, across the human intestinal epithelial Caco-2 cell-line show marked asymmetry. Basal-to-apical flux of ciprofloxacin (10 microM) exceeds apical-to-basal flux indicating net secretion. Net ciprofloxacin secretion is abolished by azide/2-deoxy-D-glucose treatment, displays saturation kinetics (Km = 0.89 +/- 0.23 mM, Vmax 44.3 +/- 4.9 nmol cm-2.h) and competition by other fluoroquinolones. A specific, active secretion in Caco-2 epithelia may explain the transintestinal elimination of ciprofloxacin observed in pharmacokinetic studies in man.

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Selected References

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