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Immediate release pellets with lipid binders obtained by solvent-free cold extrusion
Julia Krause1, Markus Thommes, Jörg Breitkreutz
1Institute of Pharmaceutics and Biopharmaceutics, Heinrich-Heine-University, Düsseldorf, Germany.
Summary
Solid lipid binders offer a non-toxic, solvent-free alternative for pharmaceutical pellet formulations. This cold extrusion method yields immediate-release pellets with high drug load and stable drug release profiles.
Area of Science:
- Pharmaceutical Technology
- Drug Delivery Systems
- Materials Science
Background:
- Lipid-based drug delivery systems are increasingly utilized in pharmaceutical development.
- Traditional extrusion methods often rely on wet binders, requiring solvent evaporation and potentially impacting sensitive drugs.
Purpose of the Study:
- To investigate solid lipid binders as non-toxic extrusion aids for pharmaceutical pellet formulations.
- To evaluate the feasibility of a solvent-free cold extrusion/spheronisation process using lipid binders.
Main Methods:
- Preparation of immediate-release pellets using various binary, ternary, and quaternary mixtures of powdered lipids and sodium benzoate.
- Comparison of lipid binders with conventional binders like microcrystalline cellulose and kappa-carrageenan.
- Assessment of pellet properties including shape, size distribution, drug load, drug release, and stability.
Main Results:
- Developed pellets exhibited favorable properties such as spherical shape, narrow size distribution, and high drug load (80% sodium benzoate).
- Drug release exceeded 90% within 40 min for some formulations.
- Sufficient drug release stability was observed, with minimal changes after storage at elevated temperatures.
Conclusions:
- Lipid binders are promising alternatives to conventional extrusion aids for producing pharmaceutical pellets.
- The solvent-free cold extrusion/spheronisation process is suitable for thermal-sensitive and hygroscopic drugs.
- Optimized lipid mixtures, particularly hard fat, glycerol distearate, and glycerol trimyristate, yield pellets with excellent characteristics and immediate release profiles.
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