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Modulating pH-independent release from coated pellets: effect of coating composition on solubilization processes and
Simon Ensslin1, Klaus Peter Moll, Hendrik Metz
1Technical Research & Development, Novartis Pharma AG, Basel, Switzerland.
Summary
This study optimized chlorpheniramine maleate (CPM) drug release from coated pellets by adjusting polymer blend ratios and film thickness. These factors significantly influenced release rates and enabled pH-independent drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Controlled drug release systems are crucial for therapeutic efficacy.
- Chlorpheniramine maleate (CPM) pellets require optimized coating for predictable delivery.
Purpose of the Study:
- To investigate the impact of coating parameters on CPM release from PVAc/PVA-PEG copolymer-coated pellets.
- To establish a pH-independent drug release profile through formulation adjustments.
Main Methods:
- Utilized a central composite design to study polymer blend ratio, film thickness, and plasticizer concentration.
- Employed EPR spectroscopy to monitor drug solubilization within pellets.
- Developed a predictive mathematical model for drug release.
Main Results:
- Polymer blend ratio and film thickness significantly affected CPM release and solubilization speed.
- Plasticizer concentration had a minor influence on drug release.
- Achieved pH-independent release by optimizing polymer blend and coating thickness.
Conclusions:
- Coating composition, specifically polymer blend ratio and film thickness, dictates CPM release kinetics.
- The developed mathematical model accurately predicts release profiles.
- Formulation control allows for tailored, pH-independent drug delivery, considering process and cost factors.
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