Hydrolysis of 3', 5'-Dioctanoyl-5-fluoro-2'-deoxyuridine (FdUrd-C8) in Rabbit and Human Plasma and Its Release from Oily Solution
スポンサーリンク
概要
- 論文の詳細を見る
Hydrolysis of 3', 5'-dioctanoyl-5-fluoro-2'-deoxyuridine (FdUrd-C8), a lipophilic prodrug of 5-fluoro-2'-deoxyuridine (FdUrd), 3'-octanoyl-5-fluoro-2'-deoxyuridine (3'-octanoyl FdUrd) and 5'-octanoyl-5-fluoro-2'-deoxyuridine (5'-octanoyl FdUrd) in the rabbit and human plasma and release of FdUrd-C8 and its hydrolyzed species from Lipiodol Ultra-Fluid (Lipiodol), an oily lymphographic agent, containing FdUrd-C8 were examined. The rates of hydrolysis of FdUrd-C8,3'-octanoyl FdUrd and 5'-octanoyl FdUrd in the rabbit plasma were fast and almost the same among the three compounds ; half lives were 2.4,3.6 and 3.9 min for 5'-octanoyl FdUrd, FdUrd-C8 and 3'-octanoyl FdUrd, respectively. In the human plasma, however, the rates of hydrolysis were much different among the three compounds and were slower than those in the rabbit plasma ; half lives were 11.5,130 and 1020 min for 5'-octanoyl FdUrd, FdUrd-C8 and 3'-octanoyl FdUrd, respectively. Ratios of the rate constant of 5'-octanoyl FdUrd to that of 3'-octanoyl FdUrd were 1.6 and 85.7 in the rabbit plasma and in the human plasma, respectively. In a release study, although detected species in a release medium were different between the rabbit plasma and the human plasma and the amount of each species reflected the characteristics of esterase in each plasma, the total amounts of compounds released were almost the same both in the rabbit plasma and the human plasma. The existence of bovine serum albumin in a release medium increased the amount of compounds released from a Lipiodol solution to a greater extent than the existence of porcine liver esterase in the release medium. The FdUrd-C8 content in Lipiodol affected the duration of release but not the amount of compounds released.
- 公益社団法人日本薬学会の論文
著者
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Hayashi Yoshie
Department Of Pharmacy Kyoto University Hospital Faculty Of Medicine Kyoto University
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Hayashi Yoshie
京都大学医学部附属病院 薬剤
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FUKUSHIMA Shoji
Department of Pathology, Osaka City University Medical School
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Kawaguchi Takeo
Department of Cardiology, Odawara Municipal Hospital
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NAKANO Masahiro
Department of Physics, Kyoto University
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Nakano M
Department Of Information Science University Of Occupational And Environmental Health
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Fukushima Shoji
Faculty Of Pharmaceutical Sciences Kobe-gakuin University
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HAYASHI Yoshiki
Department of Pharmacy, Kumamoto University Hospital
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KANEKO Mika
Department of Pharmaceutical Services, Kumamoto University Hospital
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Nakano M
Department Of Biologicalsciences Teikyo University Of Science And Technology
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Fukushima Shoji
Department Of Pharmacy Kumamoto University Hospital
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Nakano Masahiro
Department Of Biologicalsciences Teikyo University Of Science And Technology
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川口 健夫
城西大学
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Huang Ye
Department Of Pharmacy Kyoto University Hospital Faculty Of Medicine Kyoto University
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Kaneko M
Department Of Pharmaceutical Services Kumamoto University Hospital:faculty Of Pharmaceutical Science
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Kaneko Mika
Department Of Forensic Medicine Yamagata University School Of Medicine
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Hayashi Yoshiki
Department Of Hematology Osaka City General Hospital
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Fukushima Shoji
Department Of Pathology Osaka City University Medical School
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Hayashi Y
Life Science Laboratories Central Research Laboratories Ajinomoto Co. Inc.:pharmaceuticals Research
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Kawaguchi Takeo
Department Of Cardiology Odawara Municipal Hospital
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Hayashi Yoshiki
Department For The Promotion Of General Education And Liberal Arts Kyoto University
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Nakano Masahiro
Deparment Of Physics Kyushu University
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Fukushima Shoji
Department Of Gastroenterological Surgery Osaka City University Graduate School Of Medicine
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