Enhancement of Rectal Absorption of Rifampicin by Sodium para-Aminosalicylate Dihydrate in Human Subjects

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  • パラアミノサリチル酸ナトリウムによるリファンピシンのヒト直腸吸収の増加
  • パラアミノ サリチルサン ナトリウム ニ ヨル リファンピシン ノ ヒト チョ

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Abstract

The suppositories of rifampicin (RFP) containing sodium para-aminosalicylate dihydrate (PAS-Na) were prepared in order to enhance the rectal absorption of RFP. By the addition of PAS-Na, the in vitro release of RFP from the suppositories was enhanced and the hardness of the suppositories decreased. The rectal absorption of RFP from the suppositories containing no PAS-Na (control suppositories) was significantly lower compared to oral administration of it (26%) in human subjects. When PAS-Na was added to the suppository (300 mg), both the area under the plasma concentration-time curve (AUC) and the maximum plasma concentration (Cmax) increased significantly compared to those of the control suppositories. The rectal absorption of PAS-Na itself from the suppositories seemed to be fast. PAS-Na might increase the absorption of RFP dissolved in the rectal fluid from the suppositories, but not affect the undissolved RFP.

Journal

  • YAKUGAKU ZASSHI

    YAKUGAKU ZASSHI 114 (11), 894-900, 1994

    The Pharmaceutical Society of Japan

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