Related Experiment Videos
The release of naproxen in fatty suppository bases by beta-cyclodextrin complexation
N Celebi1, M Iscanoglu, T Degim
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Gazi University, Ankara, Turkey.
Die Pharmazie
|December 1, 1991
Summary
Beta-cyclodextrin (beta-CD) inclusion complexes enhanced naproxen release from fatty suppositories. The drug release kinetics followed a square root of time model, indicating diffusion-controlled release.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Naproxen is a nonsteroidal anti-inflammatory drug (NSAID) commonly used for pain and inflammation relief.
- Fatty suppository bases are frequently used for rectal drug administration, but can exhibit slow drug release.
- Beta-cyclodextrin (beta-CD) is a cyclic oligosaccharide known for its ability to form inclusion complexes with various molecules, potentially modifying their physicochemical properties.
Purpose of the Study:
- To investigate the impact of beta-cyclodextrin (beta-CD) complexation on the in vitro release of naproxen from fatty suppository bases.
- To prepare and characterize naproxen-beta-cyclodextrin (1:1 molar ratio) inclusion complexes.
- To evaluate the release kinetics of naproxen from suppositories formulated with intact drug versus the naproxen-beta-CD complex.
Main Methods:
- Naproxen-beta-CD inclusion complexes were prepared using kneading, co-precipitation, and grinding methods.
- Suppositories were formulated using Witepsol H15 and Massa Estarinum B bases, containing either intact naproxen or the naproxen-beta-CD complex.
- In vitro drug release studies were conducted using standard dissolution apparatus.
- Release data were analyzed using kinetic models to determine the release mechanism.
Main Results:
- Solid inclusion complexes of naproxen and beta-CD were successfully prepared.
- Suppositories containing the naproxen-beta-CD complex demonstrated altered naproxen release profiles compared to those with intact naproxen.
- The in vitro release data best fitted the square root of time model (Q vs. t^0.5), suggesting a diffusion-controlled release mechanism.
Conclusions:
- Beta-cyclodextrin complexation can modify and potentially enhance the release rate of naproxen from fatty suppository bases.
- The square root of time model indicates that drug release from these formulations is primarily governed by diffusion.
- This study highlights the potential of cyclodextrin complexation as a strategy to improve naproxen delivery via suppositories.