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Related Experiment Videos

Indomethacin sustained-release suppositories containing sugar ester.

T Nakajima1, Y Takashima, A Furuya

  • 1Research Center, Taisho Pharmaceutical Co., Ltd., Saitama, Japan.

Chemical & Pharmaceutical Bulletin
|April 1, 1990
PubMed
Summary
This summary is machine-generated.

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Sugar ester (SE) addition to indomethacin (IM) suppositories improved sustained release. Optimal SE content (30%) regulated rectal fluid infiltration and disintegration for sustained IM plasma levels.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Formulation Development

Background:

  • Sustained-release drug delivery aims to maintain therapeutic drug concentrations over time.
  • Suppositories offer an alternative route for drug administration.
  • Indomethacin (IM) is a nonsteroidal anti-inflammatory drug (NSAID) often requiring controlled release.

Purpose of the Study:

  • To develop and evaluate indomethacin (IM) sustained-release suppositories using sugar ester (SE) as an additive.
  • To investigate the effect of SE content on the in vitro and in vivo performance of IM suppositories.

Main Methods:

  • Indomethacin suppositories were prepared by the fusion method using IM, SE, and Witepsol H-15 (H-15).
  • In vitro drug release was assessed using the Muranishi method and an immersion method with gauze.

Related Experiment Videos

  • In vivo drug absorption was evaluated through plasma level studies in rabbits.

    • Main Results:

    • Increasing SE content elevated the softening point of the suppositories.
    • Slow-release profiles were observed with SE content >52.5% (Muranishi method), but IM absorption was minimal.
    • All SE-containing suppositories exhibited slow-release profiles (immersion method), with release rates dependent on SE content.
    • A 30% SE content suppository demonstrated sustained indomethacin plasma levels in rabbits.

    Conclusions:

    • Sugar ester (SE) can be effectively used as an additive in indomethacin suppositories to achieve sustained release.
    • An optimal SE content of 30% is crucial for regulating rectal fluid infiltration and suppository disintegration, leading to sustained drug release and plasma levels.