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Published on: August 9, 2022
Solid lipid extrusion of sustained release dosage forms
Claudia Reitz1, Peter Kleinebudde
1Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Duesseldorf, Germany.
Summary
Solid lipid extrusion effectively prepares sustained release dosage forms using glyceryl palmitostearate or glyceryl trimyristate with theophylline. Optimized processing below lipid melting points yields stable, non-porous matrices with predictable drug release.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Sustained release dosage forms are crucial for therapeutic efficacy and patient compliance.
- Solid lipid extrusion offers a potential method for creating these advanced drug delivery systems.
Purpose of the Study:
- To investigate the solid lipid extrusion process for preparing sustained release dosage forms.
- To evaluate the impact of lipid composition and extrusion conditions on drug release profiles.
Main Methods:
- Two lipids, glyceryl palmitostearate (Precirol ATO 5) and glyceryl trimyristate (Dynasan 114), were extruded with theophylline (50% or 75%).
- Extrusion was performed below lipid melting ranges, followed by analysis using differential scanning calorimetry, scanning electron microscopy, porosity measurements, and in vitro drug dissolution.
Main Results:
- Lipid softening, rather than complete melting, was achievable, avoiding metastable polymorphs.
- Formulations of glyceryl palmitostearate/theophylline (50:50) and glyceryl trimyristate/theophylline (50:50) demonstrated sustained release.
- Extrusion temperature influenced glyceryl trimyristate matrix structure; temperatures above 50.5°C resulted in porous matrices and faster release, while 49.5°C produced non-porous matrices with stable release.
Conclusions:
- Solid lipid extrusion is a viable method for producing sustained release dosage forms.
- Controlling extrusion temperature is critical for matrix structure and drug release characteristics.
- Glyceryl trimyristate-based extrudates processed at 49.5°C offer stable, non-porous sustained release matrices.
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