Pharmacokinetics of Novel Hexapeptides with Neurotensin Activity in Rats
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概要
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A high-performance liquid chromatographic method to determine (Me)Arg-Lys-Pro-Trp-tert-Leu-Leu (NT-2) with neurotensin (NT) activity in rat plasma was developed and a pharmacokinetic study was performed in rats. Quantitative analysis with high reproducibility was achieved for NT-2 over the concentration range of 1.14-500ng/ml.(Me)Arg-Lys-Pro-Trp-tert-Leu-Leu-OEt (NT-1) was rapidly hydrolyzed to NT-2 in rat plasma at 37℃. This degradation of NT-1 was observed as a pseudo first-order reaction, and the pseudo first-order rate constant was calculated to be 7.26min^<-1> (t_<1/2>=0.095min).The pharmacokinetic profiles of NT-2 after intravenous administration of NT-1 at doses of 0.1 and 0.3mg/kg were compatible with that of NT-2 after intravenous administration of NT-2 at 0.5mg/kg. Range of the half-life of the terminal phase (t_<1/2>β) of NT-2 was 0.36-0.53h.The absolute bioaveilabilities after oral administrations of NT-1 and NT-2 at a dose of 20mg/kg were 0.61±0.17 (mean ±S.E.) and 0.19±0.08%, respectively. It was found that NT-1 was more suitable for oral administration than NT-2.
- 社団法人日本薬学会の論文
- 1993-01-15
著者
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佐々木 淳
Drug Delivery System Institute Ltd. Bldg. Of Research Institute For Biosciences The Science Universt
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土屋 裕
Tsukuba Research Laboratories Eisai Co. Ltd.
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町田 良一
Tsukuba Research Laboratories, Eisai Co., Ltd.,
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徳村 忠一
Tsukuba Research Laboratories, Eisai Co., Ltd.,
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佐々木 淳
Tsukuba Research Laboratories, Eisai Co., Ltd.,
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阿部 皓一
Tsukuba Research Laboratories, Eisai Co., Ltd.,
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町田 良一
Department Of Pharmaceutical Research Eisai Co. Ltd.
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阿部 皓一
Tsukuba Research Laboratories Eisai Co. Ltd.
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徳村 忠一
Tsukuba Research Laboratories Eisai Co. Ltd.
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佐々木 淳
Tsukuba Research Laboratories Eisai Co. Ltd.
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