Singleoraldosepharmacokineticsofdecursin,decursinolangelate,anddecursinolinrats.PubMedNCBI
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Abstract
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PlantaMed.2013Mar79(34):27580.doi:10.1055/s00321328202.Epub2013Jan30.
Singleoraldosepharmacokineticsofdecursin,decursinolangelate,and
decursinolinrats.
LiL1,ZhangJ,XingC,KimSH,LJ.
Authorinformation
Abstract
Decursinanddecursinolangelatearethemajorcomponentsinthealcoholicextractoftherootof
AngelicagigasNakai.Ourpreviousworkconvincinglydemonstratedthatbothdecursinand
decursinolangelatewererapidlyconvertedtodecursinolinmiceafteradministrationbyeither
oralgavageori.p.injection.Inthecurrentstudy,wecomparedforthefirsttimetheplasma
profilesofdecursinol,whenequalmolesofdecursin/decursinolangelateordecursinolwere
giventoratsbyoralgavage,andinvestigatedtheeffectofdifferentformulasandotherchemicals
inAngelicagigasextractonthebioavailabilityofdecursinol.Ourresultsshowthatgavageof
decursinolledtoafasterattainmentofplasmadecursinolpeak(Tmax~0.7h)andmuchhigher
peaklevelsthananequalmolaramountadministeredasdecursin/decursinolangelatemixtureor
asAngelicagigasethanolextract,resultingin23foldhigherbioavailabilityasestimatedbythe
areaunderthecurveoftherespectiveregimens(65012vs.27033hng/mLfordecursinoland
decursin/decursinolangelatetreatmentgroups,respectively).Comparedtoaformulabasedon
ethanolPEG400Tween80,carboxylmethylcellulosewasalessoptimizedvehicle.Inaddition,
wedetectedpeaklevelsofdecursinanddecursinolangelateintheplasmaofratsadministered
withdecursin/decursinolangelateorAngelicagigasextractinthenMrange(Tmax~0.5h)witha
newlyestablishedsensitiveUHPLCMS/MSmethod.Furthermore,ourdatasupporttheliver,
insteadofintestine,asamajororgansitewheredecursinanddecursinolangelatewere
hydrolyzedtodecursinolwithaS9microsomalinvitrometabolismassay.Takentogether,our
studyprovidedimportantPK,LCMS/MSmethodology,formulationandmetabolisminsightsina
rodentmodelfortherationaldesignofinvivoefficacystudiesofthecorrespondingchemicalsin
thefuture.
GeorgThiemeVerlagKGStuttgartNewYork.
PMID:23364885[PubMedindexedforMEDLINE]
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http://www.ncbi.nlm.nih.gov/pubmed/23364885
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Singleoraldosepharmacokineticsofdecursin,decursinolangelate,anddecursinolinrats.PubMedNCBI
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