Cetirizine release from cyclodextrin formulated compressed chewing gum

Abstract

Beside the efficient effect on masking cetirizine bitter taste, the cyclodextrins (CDs) as well could have influence on the release from the formulation. In vitro release profiles of cetirizine from compressed chewing gums containing α-, β- and γ-CD were investigated using a three cell chewing apparatus. Different cetirizine/CD formulations were produced and analysed with respect to type of CD (α-, β- and γ-CD), the molar ratio between cetirizine and CD and the formulation of cetirizine (complex or physical mixture). Release experiments from all compressed chewing gum formulations gave similar release patterns, but with variations in the total amount released. Chewing gum formulated with cetirizine alone, demonstrated a release of 75% after 8 min of chewing. The presence of CDs resulted in increased cetirizine release. The analysis of variance (ANOVA) demonstrated that parameters with the most important influence on the release were the molar ratio of cetirizine/CD (P < 0.05) and the formulation of cetirizine/CD (complex or physical mixture) (P < 0.05). The compressed chewing gum formulations with 1:5 molar ratio of cetirizine/CD in complexed form demonstrated the highest release. Even though the statistical analysis (ANOVA) demonstrated significance in the release (P < 0.05) for the complex/physical mixture factor, this difference was negligible compared to the release from chewing gums containing cetirizine without CD. This makes physical mixtures suitable for use in cetirizine/CD formulations instead the complexes with respect to release yield. Thus unnecessary expenses for the complex preformulation may be avoided.

Keywords::

• Cetirizine
• chewing gum
• cyclodextrin
• complex
• drug release

Acknowledgements

The authors are thankful to Fertin Pharma, Vejle, Denmark for providing with cetirizine dihydrochloride, all ingredients for the chewing gum and the access to the instruments for making the chewing gum and chewing apparatus for performing the drug release studies. The authors acknowledge Associate Professor Bent Roensholdt (Aalborg University, Aalborg, Denmark) for the help with the statistical analysis.

Declaration of interest

The authors report no conflict of interest.