Full metadata record
DC Field | Value | Language |
---|---|---|
dc.contributor.author | 이화정 | * |
dc.contributor.author | 이정연 | * |
dc.date.accessioned | 2017-10-27T11:44:57Z | - |
dc.date.available | 2017-10-27T11:44:57Z | - |
dc.date.issued | 2017 | * |
dc.identifier.issn | 1976-9148 | * |
dc.identifier.other | OAK-21267 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/237066 | - |
dc.description.abstract | Paclitaxel (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.language | English | * |
dc.publisher | Korean Society of Applied Pharmacology | * |
dc.subject | Adamantyl derivatives | * |
dc.subject | Oral bioavailability | * |
dc.subject | P-glycoprotein | * |
dc.subject | Paclitaxel | * |
dc.subject | Verapamil | * |
dc.title | Effects of adamantyl derivatives on pharmacokinetic behavior of paclitaxel in rats | * |
dc.type | Article | * |
dc.relation.issue | 5 | * |
dc.relation.volume | 25 | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.index | KCI | * |
dc.relation.startpage | 553 | * |
dc.relation.lastpage | 558 | * |
dc.relation.journaltitle | Biomolecules and Therapeutics | * |
dc.identifier.doi | 10.4062/biomolther.2016.191 | * |
dc.identifier.wosid | WOS:000409152400012 | * |
dc.identifier.scopusid | 2-s2.0-85029183854 | * |
dc.author.google | Kim K.M. | * |
dc.author.google | Lee K. | * |
dc.author.google | Jang K. | * |
dc.author.google | Moon Y.S. | * |
dc.author.google | Lee H.J. | * |
dc.author.google | Rhie S.J. | * |
dc.contributor.scopusid | 이화정(57102029300) | * |
dc.contributor.scopusid | 이정연(57191753089) | * |
dc.date.modifydate | 20240220111424 | * |