PMID: 9178187May 1, 1997Paper

Characteristics of cefdinir uptake by rabbit small intestinal brush-border membrane vesicles

The Journal of Pharmacy and Pharmacology
S KitagawaS Sato

Abstract

Aminocephalosporins with peptide-like structures have been shown to be absorbed by the intestinal peptide carrier. We investigated the transport mechanism of cefdinir, an oral monocarboxylic acid cephalosporin, using rabbit small intestinal brush-border membrane vesicles. Transport of cefdinir showed a slow and almost linear uptake rate for concentrations up to 30 mM with and without and inward H+ gradient. No overshoot phenomenon was observed in the presence of an inward H+ gradient. The uptake rate increased only slightly with decreasing extravesicular pH, and a protonophore had little effect on the uptake. Aminocephalosporins such as cephalexin only slightly inhibited cefdinir uptake even in the presence of an inward H+ gradient, and vice-versa. Monocarboxylic acids such as acetic acid and salicylic acid had little effect on cefdinir uptake. These findings suggest that in contrast with other oral cephalosporins cefdinir uptake through the brush-border membrane is slow and involves a mechanism similar to passive diffusion.

References

May 1, 1990·The Journal of Pharmacy and Pharmacology·M SugawaraT Arita
Dec 1, 1988·The Journal of Antibiotics·H SakamotoS Kuwahara
Apr 1, 1984·Journal of Pharmacobio-dynamics·S YamashitaH Sezaki
Nov 1, 1981·Journal of Pharmacobio-dynamics·K YamaokaT Uno
Feb 1, 1996·Biological & Pharmaceutical Bulletin·S Kitagawa, Y Sugaya

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