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Dissolution properties of praziquantel-beta-cyclodextrin systems

S K el-Arini1, H Leuenberger

  • 1National Research Center, Cairo, Egypt.

Pharmaceutical Development and Technology
|October 1, 1996
PubMed
Summary

Praziquantel (PZQ) dissolution improved with beta-cyclodextrin (beta-CD) systems. Solvent-method complexes showed varied dissolution compared to physical mixtures, influenced by drug loading and preparation method.

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Area of Science:

  • Pharmaceutical Sciences
  • Physical Chemistry
  • Materials Science

Background:

  • Praziquantel (PZQ) is a poorly water-soluble drug crucial for treating schistosomiasis.
  • Improving the dissolution and bioavailability of such drugs is a significant pharmaceutical challenge.
  • Beta-cyclodextrin (beta-CD) is a common host molecule used to enhance the solubility and dissolution of poorly soluble drugs.

Purpose of the Study:

  • To characterize the dissolution behavior of praziquantel (PZQ) from beta-cyclodextrin (beta-CD) systems.
  • To investigate the effect of drug loading (20-100% w/w) on PZQ release kinetics.
  • To compare the dissolution profiles of PZQ-beta-CD inclusion complexes and physical mixtures.

Main Methods:

  • Preparation of PZQ-beta-CD systems using solvent method and physical mixing.
  • Dissolution testing of prepared systems and pure PZQ.
  • Analysis of dissolution parameters and release kinetics.
  • Application of percolation theory and thermal analysis for mechanism interpretation.

Main Results:

  • All PZQ-beta-CD systems demonstrated enhanced dissolution compared to free PZQ.
  • Solvent-method systems exhibited different dissolution characteristics and mechanisms than physical mixtures.
  • At high drug loading, solvent-method systems showed higher dissolution than physical mixtures.
  • At low drug loading, physical mixtures exhibited a significantly higher dissolution rate than pure PZQ.
  • Inclusion systems showed improved dissolution rates, but to a lesser extent than physical mixtures.

Conclusions:

  • Beta-cyclodextrin complexation effectively improves praziquantel dissolution.
  • The preparation method (solvent vs. physical mixture) significantly impacts dissolution behavior and kinetics.
  • Drug loading and polymer weight fraction are critical factors controlling PZQ release from beta-CD systems.
  • Percolation theory provides a framework for understanding the complex release mechanisms observed.

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