Importance of bile acids for novel oral absorption system containing polyamines to improve intestinal absorption

Masateru Miyake, Takanori Minami, Hajime Toguchi, Masaaki Odomi, Ken ichi Ogawara, Kazutaka Higaki, Toshikiro Kimura

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

The synergetic improving effect of bile acids with spermine (SPM), a major polyamine, on the absorption of rebamipide, a poorly soluble and poorly absorbable drug (BCS Class IV), was evaluated in rats and beagle dogs. Although the absorption of rebamipide was improved by the addition of polyamines alone in normal rats, it was not improved in bile duct ligated (BDL) rats. The combinatorial use of sodium taurocholate (STC), a bile acid, with SPM improved the absorption of rebamipide even in BDL rats. In the beagle dogs, the oral administration of SPM alone did not enhance the absorption of rebamipide, but the combinatorial use of STC with SPM improved the absorption as well as in the BDL rats. These results indicate that bile acids are indispensable for the novel formulation containing SPM to improve the absorption of rebamipide after oral administration.

Original languageEnglish
Pages (from-to)130-133
Number of pages4
JournalJournal of Controlled Release
Volume115
Issue number2
DOIs
Publication statusPublished - Oct 10 2006

Keywords

  • Beagle dog
  • Bile acid
  • Bile duct ligated rat
  • Intestinal absorption
  • Polyamine

ASJC Scopus subject areas

  • Pharmaceutical Science

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