Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 박혜영 | * |
dc.contributor.author | 이화정 | * |
dc.contributor.author | 이정연 | * |
dc.date.accessioned | 2019-02-28T16:30:03Z | - |
dc.date.available | 2019-02-28T16:30:03Z | - |
dc.date.issued | 2019 | * |
dc.identifier.issn | 1999-4923 | * |
dc.identifier.other | OAK-24399 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/249411 | - |
dc.description.abstract | Paclitaxel (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.language | English | * |
dc.publisher | MDPI | * |
dc.subject | piperazine derivatives | * |
dc.subject | P-glycoprotein inhibitor | * |
dc.subject | pharmacokinetics | * |
dc.subject | bioavailability | * |
dc.subject | paclitaxel | * |
dc.title | Effects of Piperazine Derivative on Paclitaxel Pharmacokinetics | * |
dc.type | Article | * |
dc.relation.issue | 1 | * |
dc.relation.volume | 11 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.journaltitle | PHARMACEUTICS | * |
dc.identifier.doi | 10.3390/pharmaceutics11010023 | * |
dc.identifier.wosid | WOS:000459732200023 | * |
dc.identifier.scopusid | 2-s2.0-85060520166 | * |
dc.author.google | Lee, Jaeok | * |
dc.author.google | Chae, Song Wha | * |
dc.author.google | Oh, A. Reum | * |
dc.author.google | Yoo, Ji Hye | * |
dc.author.google | Choo, Hea-Young Park | * |
dc.author.google | Rhie, Sandy Jeong | * |
dc.author.google | Lee, Hwa Jeong | * |
dc.contributor.scopusid | 박혜영(34972649500;57200273796) | * |
dc.contributor.scopusid | 이화정(57102029300) | * |
dc.contributor.scopusid | 이정연(57191753089) | * |
dc.date.modifydate | 20240220111424 | * |