Mechanism of Enhancement of Percutaneous Absorption of Molsidomine by Oleic Acid

Masayuki Yamada, Yoshiaki Uda, Yusuke Tanigawara

Research output: Contribution to journalArticle

61 Citations (Scopus)

Abstract

The mechanism of percutaneous absorption of molsidomine, enhanced by a two-component system consisting of oleic acid and propylene glycol, was studied in vitro and in vivo in rats. About 10—20% of the oleic acid was absorbed from the skin independently of the oleic acid-propylene glycol ratio. In contrast, about 95% of molsidomine and propylene glycol were transdermally absorbed from the two-component system containing 10% oleic acid in 6h. The permeability (percent of dose) of molsidomine through the excised rat skin was comparable to that of propylene glycol (both about 80% in 24h). These results suggest that the molsidomine and propylene glycol permeated simultaneously through rat skin. Our proposed mechanism of percutaneous absorption of molsidomine assumes that oleic acid and propylene glycol penetrate into the stratum corneum and improve the permeability of the skin by dissolving hard lipoidal components, and then molsidomine, dissolved in the propylene glycol, passes through the modified stratum corneum.

Original languageEnglish
Pages (from-to)3399-3406
Number of pages8
JournalChemical and Pharmaceutical Bulletin
Volume35
Issue number8
DOIs
Publication statusPublished - 1987 Jan 1
Externally publishedYes

Keywords

  • controlled-release transdermal dosage form
  • molsidomine
  • oleic acid
  • percutaneous absorption enhancer
  • percutaneous absorption mechanism
  • propylene glycol
  • stratum corneum

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

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