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약학대학
약학과
Journal papers
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Effects of adamantyl derivatives on pharmacokinetic behavior of paclitaxel in rats
Title
Effects of adamantyl derivatives on pharmacokinetic behavior of paclitaxel in rats
Authors
Kim K.M.
;
Lee K.
;
Jang K.
;
Moon Y.S.
;
Lee H.J.
;
Rhie S.J.
Ewha Authors
이화정
;
이정연
SCOPUS Author ID
이화정
; 이정연
Issue Date
2017
Journal Title
Biomolecules and Therapeutics
ISSN
1976-9148
Citation
Biomolecules and Therapeutics vol. 25, no. 5, pp. 553 - 558
Keywords
Adamantyl derivatives
;
Oral bioavailability
;
P-glycoprotein
;
Paclitaxel
;
Verapamil
Publisher
Korean Society of Applied Pharmacology
Indexed
SCIE; SCOPUS; KCI
Document Type
Article
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.
DOI
10.4062/biomolther.2016.191
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