Percutaneous Absorption and Metabolism of Ketoprofen Isopropyl Ester via Excised Nude Mouse‘s and Monkey’s Skin

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摘要 Aim:Tostudypercutaneousabsorptionandmetabolismofketoprofenisopropylester(KPE)viaexcisednudemouse'sandmonkey'sskin.Methods:Excisedskinwaspreparedbysurgicalexcisionandenzymedigestion.Sideby-sidediffusioncellswereusedforinvitropermeationstudies.TheconcentrationsofKPEanditsmetaboliteinsampleswereassayedbyHPLC.Results:AllKPEpenetrationthroughwholethicknessskinandstrippedskinwasmetabolizedtoketoprofen(KP).theconcentrationofwhichinthereciiversolutionincreasedlinearlywithtime.Astothenudemouseskin.thesteady-statefluxofKPthroughwholethicknessskinwas2.5timesthatofKPEthroughthewhloethicknessskin,buttheKPandKPEremaininginthewholethicknessskinafterthefinishingofKPEpenetrationwas22.2timesincomperedwiththeKPremaininginthewholethicknessskinafterthefinshingofKPpenetration.TherateofformationofthesteadystateKPfromKPEthroughtdermiswassignificantlylowerthanthatofKPEthroughthewholethicknessskin.Inhemonkeyskin,therateofformationofthesteady-stateKPfromKPEthroughthewholethicknessskinwas0.7timesthatfromKPEthroughstrippedskin.TheKPandKPEremaininginthewholethicknessskinafterthefinishingofKPEpenetrationwas2.0timethatinthestrippedskinafterthefinishingofKPEpenetration.Therateoffornationofthesteady-stateKPfromKPEthroughdermiswaslowerthanthatfromKPEthroughthewholethicknessskinandthestrippedskin.theKPremainingindermisafterthefinsihingofKPEpenetrationwasalsosignificantlylowerthantheKPremaininginthewholethicknessskinandthestrippedskinafterthefinishingofKPEpenetration.Conclusion:KPestersareofbenefittoimporovethelocalactionofKP.andskinesterasemetabolismmainlydevelopsintheepidermis.
机构地区 不详
出处 《中国药学:英文版》 2003年1期
出版日期 2003年01月11日(中国期刊网平台首次上网日期,不代表论文的发表时间)
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