Premium
Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco‐2 cell layers
Author(s) -
Griffiths Nina M.,
Hirst Barry H.,
Simmons Nicholas L.
Publication year - 1993
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1993.tb12844.x
Subject(s) - secretion , ciprofloxacin , caco 2 , chemistry , antibacterial agent , biology , biochemistry , cell , antibiotics
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 μ m ) exceeds apical‐to‐basal flux indicating net secretion. Net ciprofloxacin secretion is abolished by azide/2‐deoxy‐ d ‐glucose treatment, displays saturation kinetics ( K m = 0.89 ± 0.23 m m , V max 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.