論文

査読有り
1995年1月

PHARMACOKINETIC DISPOSITION ANALYSIS OF LIPOPHILIC DRUGS INJECTED WITH VARIOUS LIPID CARRIERS IN THE SINGLE-PASS RAT-LIVER PERFUSION SYSTEM

INTERNATIONAL JOURNAL OF PHARMACEUTICS
  • T TAKINO
  • ,
  • E NAGAHAMA
  • ,
  • T SAKAEDA
  • ,
  • F YAMASHITA
  • ,
  • Y TAKAKURA
  • ,
  • M HASHIDA

114
1
開始ページ
43
終了ページ
54
記述言語
英語
掲載種別
研究論文(学術雑誌)
DOI
10.1016/0378-5173(94)00211-M
出版者・発行元
ELSEVIER SCIENCE BV

The hepatic disposition properties of [H-3]retinoic acid with moderate lipophilicity and having a logarithm of the n-octanol/water partition coefficient (log PCoct) of 6.61 were analyzed in comparison with those of lipid carrier systems labeled by [C-14]cholesteryl oleate in an in situ single-pass rat liver perfusion experimental system. Oil-in-water (o/w) type emulsions with mean diameters of 252 and 85 nm, liposomes with a diameter of 122 nm and a HCO-60 micellar solution were tested as lipid carriers. During a single passage through the liver, the large emulsion showed marked uptake of [C-14]cholesteryl oleate incorporated in oil droplets, while the other three carriers showed almost complete recovery in the venous outflow, suggesting their 'stealthy' nature. The outflow patterns of [H-3]retinoic acid injected with lipid carriers were analyzed on the basis of moment analysis assuming first-order release from carrier particles, with the data for [H-3]retinoic acid injected in the form of an aqueous solution. Injection with micellar solution and the small emulsion demonstrated a rapid rate of release of [H-3]retinoic acid, however, the large emulsion and liposomes showed considerable retention and delivered [H-3]retinoic acid to the liver non-parenchymal cells and to the venous outflow side, respectively, stably entrapping it.

リンク情報
DOI
https://doi.org/10.1016/0378-5173(94)00211-M
Web of Science
https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=JSTA_CEL&SrcApp=J_Gate_JST&DestLinkType=FullRecord&KeyUT=WOS:A1995PY36400005&DestApp=WOS_CPL
ID情報
  • DOI : 10.1016/0378-5173(94)00211-M
  • ISSN : 0378-5173
  • Web of Science ID : WOS:A1995PY36400005

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