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dc.contributor.author이화정*
dc.contributor.author이정연*
dc.date.accessioned2017-10-27T11:44:57Z-
dc.date.available2017-10-27T11:44:57Z-
dc.date.issued2017*
dc.identifier.issn1976-9148*
dc.identifier.otherOAK-21267*
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/237066-
dc.description.abstractPaclitaxel (PTX) is one of the most frequently used anticancer agent for treating refractory ovarian cancer, metastatic breast cancer and non-small cell lung cancer. However, its oral administration is impeded by very low bioavailability (<5%) due to the Pglycopprotein (P-gp) efflux pump effect. This study investigated in vitro and in vivo P-gp inhibitory effects of adamantyl derivatives AC-603 and AC-786 in rats. Two adamantyl derivatives tested in this study increased the cytotoxicity of daunomycin (DNM) in P-gp overexpressed cell line by inhibiting P-gp efflux function. Pharmacokinetics of PTX with orally co-administered P-gp inhibitors were assessed in rats to improve PTX absorption. The pharmacokinetic parameters of PTX were determined in rats after intravenous (2 mg/kg) or oral (25 mg/kg) administration in the presence or absence of verapamil (a positive control), AC-603 or AC-786 (0.5 mg/kg or 5 mg/kg). Compared to control group (PTX alone), experimental groups (PTX with AC-603 or AC-786) significantly increased the area under the plasma concentration-time curve of PTX following oral administration by 1.7-2.2 fold. The volume of distribution and total clearance of PTX were decreased, while other parameters were not significantly changed. In conclusion, co-administration of AC-603 or AC-786 enhanced the relative bioavailability of orally administered PTX as compared to control. © 2017 The Korean Society of Applied Pharmacology.*
dc.languageEnglish*
dc.publisherKorean Society of Applied Pharmacology*
dc.subjectAdamantyl derivatives*
dc.subjectOral bioavailability*
dc.subjectP-glycoprotein*
dc.subjectPaclitaxel*
dc.subjectVerapamil*
dc.titleEffects of adamantyl derivatives on pharmacokinetic behavior of paclitaxel in rats*
dc.typeArticle*
dc.relation.issue5*
dc.relation.volume25*
dc.relation.indexSCIE*
dc.relation.indexSCOPUS*
dc.relation.indexKCI*
dc.relation.startpage553*
dc.relation.lastpage558*
dc.relation.journaltitleBiomolecules and Therapeutics*
dc.identifier.doi10.4062/biomolther.2016.191*
dc.identifier.wosidWOS:000409152400012*
dc.identifier.scopusid2-s2.0-85029183854*
dc.author.googleKim K.M.*
dc.author.googleLee K.*
dc.author.googleJang K.*
dc.author.googleMoon Y.S.*
dc.author.googleLee H.J.*
dc.author.googleRhie S.J.*
dc.contributor.scopusid이화정(57102029300)*
dc.contributor.scopusid이정연(57191753089)*
dc.date.modifydate20240220111424*
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약학대학 > 약학과 > Journal papers
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