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Optimization of primaquine diphosphate tablet formulation for controlled drug release using the mixture experimental
Marcelo Dutra Duque1, Rogério Nepomuceno Kreidel, Maria Elena Santos Taqueda
1Department of Pharmacy, Faculty of Pharmaceutical Sciences, University of Sao Paulo, Sao Paulo, Brazil. marceloduque@usp.br
Pharmaceutical Development and Technology
|June 8, 2012
Summary
This study optimized primaquine diphosphate (PDP) release from hydrophilic matrix tablets using response surface methodology. The developed formulation achieved controlled PDP release, demonstrating the effectiveness of mixture experimental design for optimizing drug dissolution.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Controlled drug release systems are crucial for improving therapeutic efficacy and patient compliance.
- Primaquine diphosphate (PDP) requires optimized delivery systems to manage its therapeutic profile.
Purpose of the Study:
- To develop a hydrophilic matrix tablet for controlled release of primaquine diphosphate (PDP).
- To optimize tablet composition using mixture experimental design and response surface methodology (RSM).
- To achieve a drug release profile approximating zero-order kinetics.
Main Methods:
- Development of hydrophilic matrix tablets using hydroxypropylmethylcellulose and polyethylene glycol.
- Application of a 20-run, four-factor mixture experimental design with constraints.
- In vitro dissolution studies in phosphate buffer (pH 6.8) and kinetic analysis using the Korsmeyer-Peppas model.
Main Results:
- Optimized formulation released 85.22% of primaquine diphosphate over 8 hours.
- Drug release mechanism was confirmed to involve both diffusion and erosion via the Korsmeyer-Peppas model (Adj-R(2) = 0.99295).
- Experimental data closely matched predictions from statistical analysis.
Conclusions:
- Mixture experimental design effectively optimizes primaquine diphosphate dissolution from hydrophilic matrix tablets.
- The developed formulation provides controlled release, approaching zero-order kinetics.
- The study validates the use of RSM for optimizing drug delivery systems based on polymer matrices.
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