Pharmacokinetics, blood partition and protein binding of DA-7867, a new oxazolidinone

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dc.contributor.authorBae, SKko
dc.contributor.authorChung, WSko
dc.contributor.authorKim, EJko
dc.contributor.authorRhee, JKko
dc.contributor.authorKwon, JWko
dc.contributor.authorKim, WBko
dc.contributor.authorLee, MGko
dc.date.accessioned2016-04-22T08:33:07Z-
dc.date.available2016-04-22T08:33:07Z-
dc.date.created2016-01-29-
dc.date.created2016-01-29-
dc.date.issued2004-04-
dc.identifier.citationBIOPHARMACEUTICS & DRUG DISPOSITION, v.25, no.3, pp.127 - 135-
dc.identifier.issn0142-2782-
dc.identifier.urihttp://hdl.handle.net/10203/206034-
dc.description.abstractThe pharmacokinetics after single intravenous and single and consecutive 2 week oral administration, tissue distribution, in vitro tissue metabolism, stability, blood partition and protein binding of DA-7867, a new oxazolidinone, were evaluated. After intravenous administration at a dose of 10 mg/kg to rats, DA-7867 was eliminated slowly with time-averaged total body clearance of 0.915 ml/min/kg. After consecutive 2 week oral administration at a dose of 2 mg/kg/day to rats, DA-7867 was accumulated in rats; the AUC was significantly greater (1430 versus 1880 mug min/ml) than that after single oral administration at a dose of 2mg/kg. The rat tissues studied had low affinity to DA-7867; the tissue-to-plasma ratios were smaller than unity after both intravenous and oral administration at a dose of 20 mg/kg. The rat tissues studied had almost negligible metabolic activity for DA-7867 based on 30 min incubation of DA-7867 with 9000g supernatant fraction of rat tissues. DA-7867 was stable for up to 24 h incubation in various buffer solutions having pHs from I to 11, Sorensen phosphate buffer of pH 7.4, and rat plasma, urine and liver homogenate and 3 h incubation in five human gastric juices. The binding of DA-7867 to 4% human serum albumin was 50.6% at DA-7867 concentrations ranging from 0.5 to 20mug/ml. The equilibrium of DA-7867 between plasma and blood cells of rabbit blood reached fast (within 30 s manual mixing), and the plasma-to-blood cell concentration ratios were independent of initial blood concentrations of DA-7867, 1-20 mug/ml; the values ranged from 1.39 to 1.63. Protein binding of DA-7867 in five fresh rats plasma was 72.3%. Copyright (C) 2004 John Wiley Sons, Ltd.-
dc.languageEnglish-
dc.publisherJOHN WILEY & SONS LTD-
dc.subjectISOLATED RAT-LIVER-
dc.subjectDRUG ELIMINATION-
dc.subjectDOSAGE REGIMENS-
dc.subjectPLASMA-
dc.subjectERYTHROCYTES-
dc.subjectMETABOLISM-
dc.subjectSTABILITY-
dc.subjectBARRIERS-
dc.subjectAGENT-
dc.titlePharmacokinetics, blood partition and protein binding of DA-7867, a new oxazolidinone-
dc.typeArticle-
dc.identifier.wosid000221127400004-
dc.type.rimsART-
dc.citation.volume25-
dc.citation.issue3-
dc.citation.beginningpage127-
dc.citation.endingpage135-
dc.citation.publicationnameBIOPHARMACEUTICS & DRUG DISPOSITION-
dc.identifier.doi10.1002/bbd.394-
dc.contributor.localauthorChung, WS-
dc.contributor.nonIdAuthorBae, SK-
dc.contributor.nonIdAuthorKim, EJ-
dc.contributor.nonIdAuthorRhee, JK-
dc.contributor.nonIdAuthorKwon, JW-
dc.contributor.nonIdAuthorKim, WB-
dc.contributor.nonIdAuthorLee, MG-
dc.type.journalArticleArticle-
dc.subject.keywordAuthorDA-7867-
dc.subject.keywordAuthorpharmacokinetics-
dc.subject.keywordAuthortissue distribution-
dc.subject.keywordAuthortissue metabolism-
dc.subject.keywordAuthorstability-
dc.subject.keywordAuthorblood partition-
dc.subject.keywordAuthorprotein binding-
dc.subject.keywordPlusISOLATED RAT-LIVER-
dc.subject.keywordPlusDRUG ELIMINATION-
dc.subject.keywordPlusDOSAGE REGIMENS-
dc.subject.keywordPlusPLASMA-
dc.subject.keywordPlusERYTHROCYTES-
dc.subject.keywordPlusMETABOLISM-
dc.subject.keywordPlusSTABILITY-
dc.subject.keywordPlusBARRIERS-
dc.subject.keywordPlusAGENT-
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