Mechanism of Enhancement of Percutaneous Absorption of Molsidomine by Oleic Acid(Pharmaceutical)

  • YAMADA M.
    Pharmaceutical Development Laboratories, Takeda Chemical Industries, Ltd.
  • UDA YOSHIAKI
    Pharmaceutical Development Laboratories, Takeda Chemical Industries, Ltd.
  • TANIGAWARA YUSUKE
    Pharmaceutical Development Laboratories, Takeda Chemical Industries, Ltd.

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抄録

The mechanism of percutaneous absorption of molsidomine, enhanced by a two-component system consisting of oleic acid and propylene giycol, 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 giycol ratio. In contrast, about 95% of molsidomine and propylene glycol were trarisdermally 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 giycol (both about 80% in 24h). These results suggest that the molsidomine and propylene giycol permeated simultaneously through rat skin. Our proposed mechanism of percutaneous absorption of molsidomine assumes that oleic acid and propylene giycol penetrate into the stratum corneum and improve the permeability of the skin by dissolving hard lipoidal components, and then molsidomine, dissolved in the propylene giycol, passes through the modified stratum corneum.

収録刊行物

  • Chem. Pharm. Bull.

    Chem. Pharm. Bull. 35 3399-3406, 1987

    公益社団法人日本薬学会

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