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Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats


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タイトル: Biodistribution and Pharmacokinetics of O-Palmitoyl Tilisolol, a Lipophilic Prodrug of Tilisolol, after Intravenous Administration in Rats
著者: Kawakami, Shigeru / Ohshima, Nao / Hirayama, Ryu / Hirai, Masami / Kitahara, Takashi / Sakaeda, Toshiyuki / Mukai, Takahiro / Nishida, Koyo / Nakamura, Junzo / Nakashima, Mikiro / Sasaki, Hitoshi
発行日: 2002年 8月
出版者: Pharmaceutical Society of Japan
引用: Biological & Pharmaceutical Bulletin v.25(8) p.1072-1076, 2002
抄録: The purpose of this study was to modify the biodistribution and pharmacokinetics of tilisolol, a β-blocker, using the palmitoyl prodrug approach. After intravenous administration of tilisolol and O-palmitoyl tilisolol in rats, drug concentrations were determined in blood, bile, urine, and several tissues. The concentration-time profiles of tilisolol and O-palmitoyl tilisolol were analyzed pharmacokinetically. The blood concentrations of O-palmitoyl tilisolol after intravenous administration of O-palmitoyl tilisolol were about 10-fold higher than those of tilisolol after intravenous administration of tilisolol. The biliary excretion rates of O-palmitoyl tilisolol and tilisolol after intravenous administration of O-palmitoyl tilisolol were about 10- to 100-fold larger than those of tilisolol after intravenous administration of tilisolol. In addition, the hepatic uptake clearance of O-palmitoyl tilisolol after intravenous administration of O-palmitoyl tilisolol was 3.6-fold higher than that of tilisolol after the intravenous administration of tilisolol. In the in vitro experiments, it was demonstrated that the distribution ratios between blood cells and plasma (blood/plasma) of O-palmitoyl tilisolol and tilisolol was 95.7 and 55.5%, respectively. These findings suggest that O-palmitoyl tilisolol exists as a binding form with biological components, especially blood cells, in systemic circulation. In conclusion, the palmitoyl prodrug approach is useful as a drug delivery system to deliver the parent drug to the liver.
キーワード: prodrug / tilisolol / pharmacokinetic / liver / β-blockers / stability
URI: http://hdl.handle.net/10069/8376
ISSN: 09186158
DOI: 10.1248/bpb.25.1072
PubMed ID: 12186412
関連リンク : http://dx.doi.org/10.1248/bpb.25.1072
資料タイプ: Journal Article
原稿種類: publisher
出現コレクション:050 学術雑誌論文

引用URI : http://hdl.handle.net/10069/8376

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