2012 Fiscal Year Final Research Report
Effect of Food on the Intestinal PEPT1-mediated Drug Absorption
| Project/Area Number |
22590505
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Applied pharmacology
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| Research Institution | Takasaki University of Health and Welfare |
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Principal Investigator |
MORIMOTO Kaori 高崎健康福祉大学, 薬学部, 講師 (90401009)
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| Co-Investigator(Kenkyū-buntansha) |
MORIMOTO Kaori 高崎健康福祉大学, 薬学部, 講師 (90401009)
OGIHARA Takuo 高崎健康福祉大学, 薬学部, 教授 (80448886)
KANO Takashi 高崎健康福祉大学, 薬学部, 助教 (70509257)
IDOTA Yoko 高崎健康福祉大学, 薬学部, 研究員 (90629594)
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| Project Period (FY) |
2010 – 2012
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| Keywords | 医薬品副作用 / 薬物相互作用 |
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| Research Abstract |
In the present study, we found that oseltamivir, an ester-type prodrug of neuraminidase inhibitor [3R,4R,5S]-4-acetamido-5-amino-3-(1-ethylpropoxy)-1-cyclohexene -1-carboxylic acid (Ro 64-0802), was effectively taken up by PEPT1 in vitro and that oseltamivir absorption in rats was greatly reduced by simultaneous administration of milk, casein , or glysylsarcosin. In addition, clinical stud iesin healthy volunteers showed that milk significantly reduced the maximum plasma concentrations (Cmax) and the area under the plasma concentration -time curves from 0 to 2 hour (AUC0-2) of both oseltamivir and Ro 64-0802. However, the extent of interaction was different between rats and humans, possibly because of sepecies difference in the PEPT1 expression and its contribution. Same interactions for known PEPT1 substrates were also seen in rat in vivo. These might be a first finding that suggests clinical drug-food interaction via PEPT1.
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Research Products
(18 results)
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[Journal Article] Effect of milk on the pharmacokinetics of oseltamivir in healthy volunteers2011
Author(s)
Morimoto K, Kishimura K, Nagami T, Kodama N, Ogama Y, Yokoyama M, Toda S, Chiyoda T, Shimada R, Inano A, Kano T, Tamai I, Ogihara T
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Journal Title
J. Pharm. Sci
Volume: Vol.100
Pages: 3854-3861
DOI
Peer Reviewed
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