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Published on: August 9, 2022
Saturated phosphatidylcholine as matrix former for oral extended release dosage forms
Marina Kolbina1, Roland Bodmeier1, Martin Körber2
1College of Pharmacy, Freie Universität Berlin, Kelchstr. 31, 12169 Berlin, Germany.
Saturated phosphatidylcholine (Phospholipon® 90H) shows promise as an extended-release excipient in matrix tablets. This phospholipid enables direct compression and controlled drug release for various drugs, offering tunable release profiles.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Phospholipids are increasingly explored as functional excipients in drug delivery systems.
- Developing effective extended-release formulations requires careful selection of matrix formers to control drug dissolution.
Purpose of the Study:
- To assess saturated phosphatidylcholine (Phospholipon® 90H) as an extended-release excipient in matrix tablets.
- To evaluate its suitability for drugs with varying aqueous solubility.
Main Methods:
- Matrix tablets were prepared by direct compression using Phospholipon® 90H and three model drugs: theophylline, caffeine, and diprophylline.
- Drug release kinetics were studied at different drug loadings and tablet dimensions.
- Dissolution robustness was tested under varying agitation and ionic strength conditions.
Main Results:
- Phospholipon® 90H exhibited favorable powder flow and compaction properties, allowing direct compression.
- Extended drug release, governed by diffusion (Fick's law), was achieved and tunable by drug loading and tablet size.
- Caffeine release varied from 1.5 to 18 hours based on drug loading (10-70%).
- The matrix tablets demonstrated robust dissolution profiles across different agitation speeds and ionic strengths.
- Drug release was pH-dependent, showing faster release at acidic pH due to matrix-former protonization.
Conclusions:
- Saturated phosphatidylcholine is a suitable excipient for creating extended-release matrix tablets.
- Its properties allow for controlled diffusion-based drug release, adaptable to drug solubility and formulation design.
- The excipient demonstrates good performance stability in various physiological conditions.
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