PMID: 9165537May 1, 1997Paper

Restricted intestinal absorption of some beta-lactam antibiotics by an energy-dependent efflux system in rat intestine

Pharmaceutical Research
H SaitohK Miyazaki

Abstract

The purpose of this study was to examine factors limiting the intestinal absorption of orally inactive beta-lactam antibiotics. Permeation behaviors of various beta-lactam antibiotics across rat intestinal segments were evaluated in vitro using diffusion cells. Poorly absorbed beta-lactam antibiotics, like cephaloridine and cefoperazone, commonly exhibit greater serosal-to-mucosal permeation than mucosal-to-serosal permeation, while cephalexin permeation was greater in the mucosal-to-serosal direction. In the absence of D-glucose, secretory-oriented permeation of cephaloridine and cefoperazone disappeared. Addition of sodium azide into an experimental buffer including D-glucose significantly and selectively enhanced mucosal-to-serosal permeation of cephaloridine and cefoperazone. Although benzylpenicillin, ampicillin, and amoxicillin all showed secretory-oriented permeation, the tendency to permeation was greatest with benzylpenicillin and least with amoxicillin. Probenecid stimulated mucosal-to-serosal permeation of cephaloridine, but verapamil and p-aminohippuric acid had no significant effect on it. It has been suggested that mechanisms which induce secretory-oriented permeation of orally inactive beta-lactam antibiotics are...Continue Reading

Citations

Jan 20, 1998·Drug and Chemical Toxicology·M M Doherty, K S Pang
Jun 5, 2002·Journal of Clinical Pharmacology·Marilyn N Martinez, Gordon L Amidon
Jul 10, 2001·Journal of Veterinary Pharmacology and Therapeutics·J M Musser, K L Anderson
Oct 24, 2002·British Journal of Clinical Pharmacology·Hiroshi SaitohKatsumi Miyazaki
Apr 30, 2002·Clinical Pharmacokinetics·Margaret M Doherty, William N Charman
Sep 16, 2000·European Journal of Pharmacology·R A Van AubelF G Russel
Jun 30, 2000·Biochemical Pharmacology·F Van BambekeP M Tulkens

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