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Related Experiment Videos

Preparation of ibuprofen-loaded liquid suppository using eutectic mixture system with menthol.

Chul Soon Yong1, Yu-Kyoung Oh, Se Hyun Jung

  • 1College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea.

European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences
|November 30, 2004
PubMed
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This study developed an ibuprofen liquid suppository using menthol and poloxamer 188, enhancing drug solubility and rectal absorption. The novel formulation offers improved ibuprofen bioavailability compared to traditional solid suppositories.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Formulation Development

Background:

  • Improving the aqueous solubility of poorly soluble drugs like ibuprofen is crucial for effective drug delivery.
  • Liquid suppositories offer potential advantages over solid dosage forms for rectal administration.
  • Eutectic mixtures and polymers can be utilized to enhance drug solubility and formulation properties.

Purpose of the Study:

  • To develop an ibuprofen-loaded liquid suppository utilizing a eutectic mixture with menthol.
  • To investigate the effects of menthol and poloxamer 188 (P 188) on ibuprofen solubility and physicochemical properties.
  • To evaluate the pharmacokinetic performance of the developed liquid suppository compared to a solid suppository.

Main Methods:

  • Investigated ibuprofen solubility in various ratios of menthol and P 188.

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  • Assessed physicochemical properties including gelation temperature, gel strength, and bioadhesive force.
  • Conducted pharmacokinetic studies in rats comparing liquid and solid suppositories.

    • Main Results:

    • A eutectic mixture of menthol and ibuprofen (4:6 ratio) significantly increased ibuprofen solubility.
    • Poloxamer 188 further enhanced solubility, with a formulation of 15% P 188 and 1:9 menthol/ibuprofen ratio achieving 1.2 mg/ml.
    • The liquid suppository demonstrated higher Cmax and AUC, indicating enhanced rectal bioavailability in rats.

    Conclusions:

    • The developed ibuprofen liquid suppository system with P 188 and menthol is a convenient and effective rectal dosage form.
    • This formulation significantly enhances the aqueous solubility and rectal bioavailability of ibuprofen.
    • The study highlights the potential of eutectic mixtures and poloxamer gels for improving drug delivery via rectal administration.