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In vitro nimesulide absorption from different formulations.

F Meriani1, N Coceani, C Sirotti

  • 1Materials Engineering Department DIMCA, University of Trieste, Piazzale Europa 1, I-34127 Trieste, Italy.

Journal of Pharmaceutical Sciences
|February 6, 2004
PubMed
Summary
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An activated nimesulide/polyvinylpyrrolidone system significantly improved drug absorption compared to simple solid nimesulide and a reference solution. This formulation overcomes both wettability and solubility issues, enhancing bioavailability.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Biopharmaceutics

Background:

  • Poor water solubility of drugs like nimesulide limits bioavailability.
  • Developing effective formulations is crucial for enhancing drug absorption.
  • In vitro models are essential for evaluating drug permeation.

Purpose of the Study:

  • To compare the in vitro absorption of different nimesulide formulations.
  • To evaluate the efficacy of an activated nimesulide/polyvinylpyrrolidone system.
  • To model and understand drug absorption mechanisms.

Main Methods:

  • In vitro absorption experiments using an everted rat intestine model.
  • Comparison of nimesulide ethanol-triacetin solution, activated system, and reference solution.

Related Experiment Videos

  • Development of a mathematical model based on Fick's second law for drug absorption.

    • Main Results:

    • The activated nimesulide/polyvinylpyrrolidone system demonstrated superior performance over the reference solution.
    • This activated system effectively addressed both wettability and solubility challenges of nimesulide.
    • Polymeric particles adhered to intestinal villi, creating a localized high drug concentration layer.

    Conclusions:

    • The activated nimesulide/polyvinylpyrrolidone system is a promising formulation for improving nimesulide bioavailability.
    • Mathematical modeling provides insights into drug permeation and the nature of the drug-rich layer.
    • The study validated a common data correction technique used in drug concentration measurements.