PMID: 8583383Sep 1, 1995Paper

The influence of uptake from the gastrointestinal tract and first-pass effect on oral bioavailability of (Z)-alkyloxyimino penicillins

The Journal of Pharmacy and Pharmacology
L MizenG Woodnutt

Abstract

We have investigated the contribution of uptake from the gastrointestinal tract and first-pass effect to the poor oral bioavailability of a series of (Z)-alkyloxyimino penicillins in mice. Investigative studies in gut sacs and perfused small intestine demonstrated that these penicillins were able to pass across the mucosal epithelium although to a lesser extent than amoxycillin and cyclacillin, both of which exhibit excellent oral bioavailability in man and animals. In the jejunal gut sacs the mucosal to serosal flux for BRL 44154 was approximately half that of amoxycillin and four times less than that of cyclacillin, and for all, uptake was pH dependent. The serosal to mucosal fluxes were however similar for these compounds and significantly lower than mucosal to serosal fluxes, suggesting involvement of carrier mechanisms in uptake from the mucosal surface. The order of results for the alkyloxyimino penicillins paralleled that observed for oral bioavailability in the mouse. For the alkyloxyimino penicillins, between 5.5 and 9.9% was taken up from the perfused intestine, values which were significantly less than those for amoxycillin (13.2%) and cyclacillin (33.3%). However, uptake was concentration-dependent for BRL 44154 as ...Continue Reading

References

Nov 1, 1977·The Journal of Pharmacy and Pharmacology·A TsujiT Yamana
Aug 1, 1977·The Journal of Physiology·C Dixon, L W Mizen
Aug 1, 1987·Journal of Clinical Pharmacology·Z Gregus, C D Klaassen
Mar 1, 1988·The Journal of Antimicrobial Chemotherapy·L Mizen, G Woodnutt

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Citations

Mar 14, 1998·Journal of Chromatography. B, Biomedical Sciences and Applications·P O ErahP N Shaw
Mar 10, 2006·Clinical Microbiology and Infection : the Official Publication of the European Society of Clinical Microbiology and Infectious Diseases·D M Livermore

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