Plasma disposition and faecal excretion of netobimin metabolites and enantiospecific disposition of albendazole sulphoxide produced in ewes

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dc.contributor.authorGökbulu, Cengiz
dc.contributor.buuauthorÇırak, Veli Y.
dc.contributor.buuauthorŞenlik, Bayram
dc.contributor.departmentUludağ Üniversitesi/Veteriner Fakültesi/Parazitoloji Anabilim Dalı.tr_TR
dc.contributor.orcid0000-0003-2964-2245tr_TR
dc.contributor.scopusid6602404057tr_TR
dc.contributor.scopusid9332720500tr_TR
dc.date.accessioned2021-12-07T05:54:33Z
dc.date.available2021-12-07T05:54:33Z
dc.date.issued2006
dc.description.abstractNetobimin (NTB) was administered orally to ewes at 20 mg/kg bodyweight. Blood and faecal samples were collected from 1 to 120 h post-treatment and analysed by high-performance liquid chromatography (HPLC). Using a chiral phase-based HPLC, plasma disposition of albendazole sulphoxide (ABZSO) enantiomers produced was also determined. Neither NTB nor albendazole (ABZ) was present and only ABZSO and albendazole sulphone (ABZSO(2)) metabolites were detected in the plasma samples. Maximum plasma concentrations (C <(max)) of ABZSO (4.1 +/- 0.7 mu g/ml) and ABZSO(2) (1.1 +/- 0.4 mu g/ml) were detected at (t (max)) 14.7 and 23.8 h, respectively following oral administration of netobimin. The area under the curve (AUC) of ABZSO (103.8 +/- 22.8 (mu g h)/ml) was significantly higher than that ABZSO(2)(26.3 +/- 10.1 (mu g h)/ml) (p < 0.01). (-)-ABZSO and (+)-ABZSO enantiomers were never in racemate proportions in plasma. The AUC of (+)-ABZSO (87.8 +/- 20.3 (mu g h)/ml) was almost 6 times larger than that of (-)-ABZSO (15.5 +/- 5.1 (mu g h)/ml) (p < 0.001). Netobimin was not detected, and ABZ was predominant and its AUC was significantly higher than that of ABZSO and ABZSO(2), following NTB administration in faecal samples (p > 0.01). Unlike in the plasma samples, the proportions of the enantiomers of ABZSO were close to racemic and the ratio of the faecal AUC of (-)-ABZSO (172.22 +/- 57.6 (mu g h)/g) and (+)-ABZSO (187.19 +/- 63.4 (mu g h)/g) was 0.92. It is concluded that NTB is completely converted to ABZ by the gastrointestinal flora and absorbed ABZ is completely metabolized to its sulphoxide and sulphone metabolites by first-pass effects. The specific behaviour of the two enantiomers probably reflects different enantioselectivity of the enzymatic systems of the liver that are responsible for sulphoxidation and sulphonation of ABZ.en_US
dc.identifier.citationGökbulut, C. vd. (2006). ''Plasma disposition and faecal excretion of netobimin metabolites and enantiospecific disposition of albendazole sulphoxide produced in ewes''. Veterinary Research Communications, 30(7), 791-805.en_US
dc.identifier.endpage805tr_TR
dc.identifier.issn0165-7380
dc.identifier.issn1573-7446
dc.identifier.issue7tr_TR
dc.identifier.pubmed17004041tr_TR
dc.identifier.scopus2-s2.0-33749189352tr_TR
dc.identifier.startpage791tr_TR
dc.identifier.urihttps://doi.org/10.1007/s11259-006-3336-y
dc.identifier.urihttps://link.springer.com/article/10.1007%2Fs11259-006-3336-y
dc.identifier.urihttp://hdl.handle.net/11452/23018
dc.identifier.volume30tr_TR
dc.identifier.wos000240831200007tr_TR
dc.indexed.pubmedPubmeden_US
dc.indexed.scopusScopusen_US
dc.indexed.wosSCIEen_US
dc.language.isoenen_US
dc.publisherSpringeren_US
dc.relation.collaborationYurt içitr_TR
dc.relation.journalVeterinary Research Communicationsen_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergien_US
dc.rightsinfo:eu-repo/semantics/closedAccessen_US
dc.subjectVeterinary sciencesen_US
dc.subjectOvisen_US
dc.subjectPharmacokineticsen_US
dc.subjectEnantiomersen_US
dc.subjectNetobiminen_US
dc.subjectAlbendazole sulphoxideen_US
dc.subjectEwesen_US
dc.subjectAlbendazoleen_US
dc.subjectAnthelminticsen_US
dc.subjectGoatsen_US
dc.subjectCattleen_US
dc.subjectFenbendazoleen_US
dc.subjectP-Glycoproteinen_US
dc.subjectLiver-microsomesen_US
dc.subjectRuminal biotransformationen_US
dc.subjectHaemonchus-contortusen_US
dc.subjectPharmacokinetic behavioren_US
dc.subjectSheepen_US
dc.subject.emtreeNetobiminen_US
dc.subject.emtreeLiver enzymeen_US
dc.subject.emtreeDrug metaboliteen_US
dc.subject.emtreeAlbendazole sulfoxideen_US
dc.subject.emtreeAlbendazole sulfoneen_US
dc.subject.emtreeAlbendazoleen_US
dc.subject.emtreeSulfoxidationen_US
dc.subject.emtreeSulfonationen_US
dc.subject.emtreeStructure analysisen_US
dc.subject.emtreeStatistical significanceen_US
dc.subject.emtreeSheepen_US
dc.subject.emtreeRacemic mixtureen_US
dc.subject.emtreeNonhumanen_US
dc.subject.emtreeIntestine floraen_US
dc.subject.emtreeHigh performance liquid chromatographyen_US
dc.subject.emtreeFirst pass effecten_US
dc.subject.emtreeEnantioselectivityen_US
dc.subject.emtreeEnantiomeren_US
dc.subject.emtreeAnimal experimenten_US
dc.subject.emtreeArea under the curveen_US
dc.subject.emtreeDrug structureen_US
dc.subject.emtreeDrug metabolismen_US
dc.subject.emtreeArticleen_US
dc.subject.emtreeDrug feces levelen_US
dc.subject.emtreeDrug dose regimenen_US
dc.subject.emtreeDrug dispositionen_US
dc.subject.emtreeDrug blood levelen_US
dc.subject.emtreeBody weighten_US
dc.subject.emtreeChiral chromatographyen_US
dc.subject.emtreeControlled studyen_US
dc.subject.emtreeDrug absorptionen_US
dc.subject.meshSheep diseasesen_US
dc.subject.meshSheepen_US
dc.subject.meshHelminthiasis, animalen_US
dc.subject.meshGuanidinesen_US
dc.subject.meshFemaleen_US
dc.subject.meshAdministration, oralen_US
dc.subject.meshFecesen_US
dc.subject.meshDose-response relationship, drugen_US
dc.subject.meshChromatography, high pressure liquiden_US
dc.subject.meshArea under curveen_US
dc.subject.meshAnthelminticsen_US
dc.subject.meshAnimalsen_US
dc.subject.meshAlbendazoleen_US
dc.subject.scopusAlbendazole; Fasciola Hepatica; Anthelmintic Agenten_US
dc.subject.wosVeterinary sciencesen_US
dc.titlePlasma disposition and faecal excretion of netobimin metabolites and enantiospecific disposition of albendazole sulphoxide produced in ewesen_US
dc.typeArticle
dc.wos.quartileQ3en_US

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