View : 357 Download: 0

Full metadata record

DC Field Value Language
dc.contributor.author박혜영-
dc.contributor.author이화정-
dc.contributor.author이정연-
dc.date.accessioned2019-02-28T16:30:03Z-
dc.date.available2019-02-28T16:30:03Z-
dc.date.issued2019-
dc.identifier.issn1999-4923-
dc.identifier.otherOAK-24399-
dc.identifier.urihttps://dspace.ewha.ac.kr/handle/2015.oak/249411-
dc.description.abstractPaclitaxel (PTX) is an anticancer agent that is used to treat many cancers but it has a very low oral bioavailability due, at least in part, to the drug efflux transporter, P-glycoprotein (P-gp). Therefore, this study was performed to enhance oral bioavailability of PTX. In this study, we investigated the effects of several piperazine derivatives on P-gp function in vitro. Compound 4 was selected as the most potent P-gp inhibitor from the in vitro results for examining the pharmacokinetic (PK) changes of PTX in rats. Compound 4 increased the AUC(inf) of PTX without alterations in the C(max )value. The elimination half-life was extended and the oral clearance decreased. Additionally, the T-max was delayed or widened in the treatment groups. Therefore, the bioavailability (BA) of PTX was improved 2.1-fold following the co-administration of 5 mg/kg of the derivative. A piperazine derivative, compound 4, which was confirmed as a substantial P-gp inhibitor in vitro increased the BA of PTX up to 2-fold by a lingering absorption, in part due to inhibition of intestinal P-gp and a low oral clearance of PTX. These results suggest that co-administering compound 4 may change the PK profile of PTX by inhibiting P-gp activity in the body.-
dc.languageEnglish-
dc.publisherMDPI-
dc.subjectpiperazine derivatives-
dc.subjectP-glycoprotein inhibitor-
dc.subjectpharmacokinetics-
dc.subjectbioavailability-
dc.subjectpaclitaxel-
dc.titleEffects of Piperazine Derivative on Paclitaxel Pharmacokinetics-
dc.typeArticle-
dc.relation.issue1-
dc.relation.volume11-
dc.relation.indexSCIE-
dc.relation.indexSCOPUS-
dc.relation.journaltitlePHARMACEUTICS-
dc.identifier.doi10.3390/pharmaceutics11010023-
dc.identifier.wosidWOS:000459732200023-
dc.identifier.scopusid2-s2.0-85060520166-
dc.author.googleLee, Jaeok-
dc.author.googleChae, Song Wha-
dc.author.googleOh, A. Reum-
dc.author.googleYoo, Ji Hye-
dc.author.googleChoo, Hea-Young Park-
dc.author.googleRhie, Sandy Jeong-
dc.author.googleLee, Hwa Jeong-
dc.contributor.scopusid박혜영(34972649500)-
dc.contributor.scopusid이화정(57102029300;35069834100)-
dc.contributor.scopusid이정연(57191753089)-
dc.date.modifydate20210929132912-
Appears in Collections:
약학대학 > 약학과 > Journal papers
Files in This Item:
There are no files associated with this item.
Export
RIS (EndNote)
XLS (Excel)
XML


qrcode

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

BROWSE