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Design and optimization of sustained-release divalproex sodium tablets with response surface methodology
Farnaz Monajjemzadeh1, Hamed Hamishehkar, Parvin Zakeri-Milani
1Drug Applied Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
AAPS Pharmscitech
|December 28, 2012
Summary
Mixture Design efficiently optimized sustained-release divalproex sodium hydrophilic matrix tablets. This statistical approach accelerated formulation development, yielding tablets with comparable dissolution profiles to innovator products.
Area of Science:
- Pharmaceutical Sciences
- Formulation Development
- Drug Delivery Systems
Background:
- Divalproex sodium requires optimized formulations for sustained release.
- Improving the flowability of divalproex sodium is crucial for tablet manufacturing.
- Hydrophilic matrix tablets offer a viable approach for controlled drug release.
Purpose of the Study:
- To optimize sustained-release divalproex sodium hydrophilic matrix tablets using Mixture Design.
- To evaluate the impact of excipients on tablet properties and drug release.
- To compare the in vitro performance of optimized formulations with Depakine®.
Main Methods:
- Mixture Design (statistical) employed for formulation and optimization.
- Excipient selection and evaluation for flowability and tablet tensile strength.
- In vitro dissolution testing in biomimetic acidic and basic phases, analyzed by HPLC.
- Comparison of release kinetics and profiles with Depakine® using similarity factors.
Main Results:
- Mixture Design successfully identified suitable formulations with improved flowability and tensile strength.
- Optimized formulations exhibited dissolution profiles similar to Depakine®.
- The optimized formulation showed nearly zero-order release kinetics in vitro.
Conclusions:
- Mixture Design is an effective and efficient method for developing sustained-release divalproex sodium hydrophilic matrix tablets.
- This statistical approach streamlines the formulation process for direct compression tablets.
- The developed formulations demonstrate potential as generic alternatives to Depakine®.
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