3-Amino-1-hydroxypropylidene-1,1-diphosphonate (APD): a novel enhancer of rectal cefoxitin absorption in rats.
The promoting action of the calcium chelating compound EDTA on intestinal drug absorption is supposed to be based on Ca2+ depletion, inducing widening of tight junctions. The aim of the present study was to evaluate the effects of the calcium-binding agent 3-amino-1-hydroxypropylidene-1,1-diphosphonate disodium salt (APD) on rectal cefoxitin absorption in rats. The extent of rectal cefoxitin absorption was enhanced by 0.5 to 6% w/v of APD, on rectal infusion as well as on bolus delivery, the latter regimen tending to result in lower bioavailabilities. A maximal cefoxitin bioavailability of 85 +/- 10% was achieved by infusion with 4% w/v of APD, compared with 14 +/- 12% without APD.
van Hoogdalem
E J
EJ
Division of Pharmacology, Sylvius Laboratories, State University of Leiden, The Netherlands.
Wackwitz
A T
AT
de Boer
A G
AG
Breimer
D D
DD
D000818:Animals; D001682:Biological Availability; D002440:Cefoxitin / Q000493:pharmacokinetics*; D004164:Diphosphonates / Q000494:pharmacology*; D007262:Infusions, Intravenous; D007275:Injections, Intravenous; D007408:Intestinal Absorption / Q000187:drug effects*; D008297:Male; D000077268:Pamidronate; D051381:Rats; D011919:Rats, Inbred Strains; D012007:Rectum / Q000378:metabolism
D004164:Diphosphonates; D002440:Cefoxitin; D000077268:Pamidronate