In vitro Evaluation of Cinnarizine as a Competing Agent to .BETA.-Cyclodextrin Inclusion Complexes: Effect of Cinnarizine on the Membrane Permeation Rate of Progesterone from Its .BETA.-Cyclodextrin Inclusion Complex

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Other Title
  • β－シクロデキストリン包接化合物に対する競合包接阻害物質としてのシンナリジンの　Ｉｎ　ｖｉｔｒｏ評価：プロゲステロン膜透過速度に対する効果
  • ベータ シクロデキストリン ホウセツ カゴウブツ ニ タイスル キョウゴウ ホウセツ ソガイ ブッシツ ト シテノ シンナリジン ノ in vitro ヒョウカ プロゲステロンマク トウカ ソクド ニ タイスル コウカ

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Abstract

  The use of competing agents is considered a powerful tool for the development of a drug-delivery system with drug/cyclodextrin inclusion complexes. However, there are very few studies examining this issue. To explain this phenomenon, it was thought that a competing agent with a sufficiently high stability constant had not yet been reported. In this study, cinnarizine (CN), which has a high stability constant with β-cyclodextrin (β-CD) and unique solubility characteristics, was selected, and its ability as a competing agent was examined in a membrane permeability study. The permeability study showed that the permeation rates of the drugs flurbiprofen, progesterone, and spironolactone decreased with their stability constants with the addition of β-CD. In one of the drugs, progesterone (Pro), the decrease was restored by the addition of CN. The amount of CN added was a 1:1 molar ratio to the amount of Pro. However, no similar action was induced with the addition of DL-phenylalanine (Phe) in the permeation study at the 1:5 (Pro:Phe) molar ratio. These finding indicate that CN acts as a competing agent, and its action is much stronger than that of Phe.<br>

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 128 (1), 89-95, 2008

    The Pharmaceutical Society of Japan

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