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dc.contributor.authorBista, Sudeep Raj
dc.contributor.authorHaywood, Alison
dc.contributor.authorHardy, Janet
dc.contributor.authorLobb, Michael
dc.contributor.authorTapuni, Angela
dc.contributor.authorNorris, Ross
dc.contributor.editorCostas Ioannides
dc.date.accessioned2018-10-05T01:30:51Z
dc.date.available2018-10-05T01:30:51Z
dc.date.issued2015
dc.identifier.issn0049-8254
dc.identifier.doi10.3109/00498254.2014.971093
dc.identifier.urihttp://hdl.handle.net/10072/67299
dc.description.abstract1. Fentanyl is a highly lipophilic opioid commonly used to treat cancer pain. Plasma protein binding (PPB) of fentanyl in human plasma is reported as 80-85%, however it is unclear whether fentanyl binds primarily to albumin (ALB) or a-1 acid glycoprotein (AAG) and no studies have been conducted on the metabolite, nor-fentanyl. Fentanyl is also known to bind to plasticware and ultrafiltration (UF) devices which impacts adversely on binding experiments. 2. PPB of fentanyl and nor-fentanyl to ALB and AAG in isotonic phosphate buffer solution and seeded human plasma was quantified. PPB was also performed in plasma samples obtained from cancer patients receiving transdermal fentanyl. The adsorption of fentanyl and nor-fentanyl to UF devices and plasticware commonly used in PPB studies was also assessed. 3. Fentanyl was shown to bind primarily to ALB as opposed to AAG, with nor-fentanyl exhibiting negligible binding to plasma proteins. Total PPB of fentanyl was 86-89% in seeded human plasma. PPB in 56 cancer patient samples was 95.1? .52% for fentanyl and 32.4? 1.9% for nor-fentanyl. 4. UF was shown to be a reliable and convenient method for PPB studies, thereby removing the need for complex testing for adsorption of the drug to plasticware during UF.
dc.description.peerreviewedYes
dc.description.publicationstatusYes
dc.languageEnglish
dc.language.isoeng
dc.publisherInforma Healthcare
dc.publisher.placeUnited Kingdom
dc.relation.ispartofstudentpublicationN
dc.relation.ispartofpagefrom207
dc.relation.ispartofpageto212
dc.relation.ispartofissue3
dc.relation.ispartofjournalXenobiotica
dc.relation.ispartofvolume45
dc.rights.retentionY
dc.subject.fieldofresearchPharmaceutical Sciences
dc.subject.fieldofresearchBiochemistry and Cell Biology
dc.subject.fieldofresearchPharmacology and Pharmaceutical Sciences
dc.subject.fieldofresearchcode111504
dc.subject.fieldofresearchcode0601
dc.subject.fieldofresearchcode1115
dc.titleProtein binding of fentanyl and its metabolite nor-fentanyl in human plasma, albumin and α-1 acid glycoprotein
dc.typeJournal article
dc.type.descriptionC1 - Articles
dc.type.codeC - Journal Articles
gro.facultyGriffith Health, School of Pharmacy and Pharmacology
gro.hasfulltextNo Full Text
gro.griffith.authorHaywood, Alison
gro.griffith.authorNorris, Ross LG.
gro.griffith.authorBista, S R.


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