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Published on: October 29, 2013
Novel polymer series for pharmaceutical applications: alpha-hydroxycarboxylic acid modified polymethacrylates
Felix Claussen1, Johannes Andreas Blechar1, Jozef Al-Gousous2
1Department Pharmaceutical Technology and Biopharmaceutics, Johannes Gutenberg-University Mainz, Staudinger Weg 5, 55128 Mainz, Germany.
Novel enteric polymers were developed by modifying Eudragit® L 100 and L 100-55. These new polymers offer faster drug release after gastric emptying, addressing limitations of current enteric coatings.
Area of Science:
- Polymer Chemistry
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Enteric-coated dosage forms frequently exhibit delayed drug release post-gastric emptying.
- Existing enteric polymers like Eudragit® L 100 and L 100-55 have limitations in release kinetics.
Purpose of the Study:
- To develop novel enteric polymers with improved drug release characteristics.
- To overcome the sluggish drug release associated with conventional enteric coatings.
Main Methods:
- Esterification of Eudragit® L 100 and L 100-55 with α-hydroxycarboxylic acids (l-lactic, d,l-lactic, glycolic acid).
- Characterization of polymer properties, including pKa value and dissolution pH threshold.
- Formulation of paracetamol-loaded capsules coated with modified and standard polymers.
- In vitro dissolution testing in acidic and buffered media.
Main Results:
- Modified polymers exhibited a reduced pKa, leading to faster dissolution.
- The dissolution pH threshold decreased from pH 5.5 to approximately pH 5.
- Paracetamol release was significantly enhanced from capsules coated with novel polymers at pH 6.5 compared to Eudragit® L 100 and L 100-55.
Conclusions:
- A new series of enteric polymers was successfully synthesized.
- These novel polymers demonstrate potential for faster drug release, overcoming limitations of current enteric coatings.
- The modified polymers maintain acid resistance while improving dissolution profiles.
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