Please use this identifier to cite or link to this item: https://ahro.austin.org.au/austinjspui/handle/1/13238
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dc.contributor.authorSewell, Richard Ben
dc.contributor.authorBrook, C Wen
dc.contributor.authorMihaly, G Wen
dc.contributor.authorMorgan, Denis Jen
dc.contributor.authorSmallwood, R Aen
dc.date.accessioned2015-05-16T03:03:22Z
dc.date.available2015-05-16T03:03:22Z
dc.date.issued1994-08-17en
dc.identifier.citationBiochemical Pharmacology; 48(4): 846-9en
dc.identifier.govdoc8080458en
dc.identifier.otherPUBMEDen
dc.identifier.urihttp://ahro.austin.org.au/austinjspui/handle/1/13238en
dc.description.abstractThe contribution of intracellular storage to hepatic uptake of the high clearance drug, omeprazole, was examined in the recirculating isolated perfused rat liver preparation. Following injection of [3H]omeprazole (7.5 microCi, 5 mg) into the portal vein over 1 min, livers were perfused for 5 min (N = 3) or 30 min (N = 3) and then homogenized at 4 degrees and fractionated by differential centrifugation. Radiolabelled omeprazole and metabolites were determined by scintillation counting of fractions of eluant from HPLC. Seventy per cent of drug had been taken up by the liver at 5 min and 85% at 30 min, with unchanged drug representing 43 and 7.4%, respectively, of drug taken up. At both times, 70-75% of intracellular unchanged drug and the major metabolites were located in the cytosol, and the cytosol:perfusate concentration ratio was approximately 10:1. Mitochondrial, lysosomal and microsomal fractions contained relatively little drug. Extensive cytosolic binding of omeprazole therefore contributes substantially to the initial avid hepatic first-pass uptake of this drug.en
dc.language.isoenen
dc.subject.otherAnimalsen
dc.subject.otherCytosol.metabolismen
dc.subject.otherLiver.metabolismen
dc.subject.otherMaleen
dc.subject.otherOmeprazole.administration & dosage.metabolism.pharmacokineticsen
dc.subject.otherPortal Veinen
dc.subject.otherRatsen
dc.subject.otherRats, Sprague-Dawleyen
dc.subject.otherSubcellular Fractions.metabolismen
dc.titleIntracellular binding is an important determinant of the avid hepatic uptake of the high clearance drug omeprazole.en
dc.typeJournal Articleen
dc.identifier.journaltitleBiochemical pharmacologyen
dc.identifier.affiliationGastroenterology Unit, Austin Hospital, Melbourne, Victoria, Australiaen
dc.description.pages846-9en
dc.relation.urlhttps://pubmed.ncbi.nlm.nih.gov/8080458en
dc.type.austinJournal Articleen
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.fulltextNo Fulltext-
item.cerifentitytypePublications-
item.grantfulltextnone-
item.languageiso639-1en-
item.openairetypeJournal Article-
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