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Co-extruded solid solutions as immediate release fixed-dose combinations
L Dierickx1, B Van Snick1, T Monteyne2
1Laboratory of Pharmaceutical Technology, Ghent University, Belgium.
Summary
Co-extrusion successfully created multilayer fixed-dose combination tablets with immediate drug release. This novel oral dosage form effectively combines hydrophilic acetylsalicylic acid and hydrophobic fenofibrate.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Developing fixed-dose combination (FDC) oral dosage forms presents challenges, especially with drugs of differing water solubilities.
- Achieving immediate release from multiple layers in a single dosage form requires careful selection of polymers and manufacturing processes.
- Co-extrusion offers a promising technique for creating complex multilayer drug delivery systems.
Purpose of the Study:
- To develop a multilayer FDC solid oral dosage form using co-extrusion.
- To incorporate drugs with different water solubilities, acetylsalicylic acid (hydrophilic) and fenofibrate (hydrophobic), into distinct layers.
- To ensure immediate release from both layers of the developed dosage form.
Main Methods:
- Polymers were screened for hot-melt extrusion processability, macroscopic properties, drug stability, and in vitro release.
- Acetylsalicylic acid (ASA) and fenofibrate (FF) were used as model hydrophilic and hydrophobic drugs, respectively.
- Co-extrusion was employed to create multilayer tablets, followed by characterization using DSC, XRD, and Raman mapping.
Main Results:
- Successful co-extrusion of multilayer dosage forms was achieved with specific polymer combinations (e.g., Kollidon® PF 12/Kollidon® VA 64 core, Soluplus®/Kollidon® VA 64/Kollidon® 30 coat).
- All developed formulations exhibited good inter-layer adhesion and complete drug release within 15-60 minutes.
- Physicochemical analysis confirmed molecular dispersion of drugs and minimal intermigration between layers.
Conclusions:
- Co-extrusion is a viable method for producing multilayer FDC oral dosage forms with immediate release profiles.
- The study successfully demonstrated the combination of hydrophilic and hydrophobic drugs in a single dosage form with controlled release characteristics.
- The developed FDC tablets show potential for improved patient compliance and therapeutic efficacy.
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