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Published on: December 29, 2016
Polyelectrolytes in Hot Melt Extrusion: A Combined Solvent-Based and Interacting Additive Technique for Solid
Felix Ditzinger1,2, Catherine Dejoie3, Dubravka Sisak Jung4
1Department of Pharmaceutical Sciences, University of Basel, 4056 Basel, Switzerland. felix.ditzinger@fhnw.ch.
New polymeric matrices were created using carboxymethylcellulose sodium (NaCMC) and additives, enabling hot melt extrusion for poorly water-soluble drugs. This approach avoids new polymer synthesis and regulatory challenges.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
Background:
- Solid dispersions enhance oral drug delivery for poorly water-soluble compounds.
- Hot melt extrusion (HME) is a key technique for solid dispersion manufacturing, but polymer selection is limited.
- Synthesizing new polymers for HME involves toxicological and regulatory challenges.
Purpose of the Study:
- To develop novel polymeric matrices for HME by combining a known polymer with small molecular additives.
- To overcome limitations of polymer choice in HME for solid dispersions.
- To create amorphous polymer matrices suitable for drug formulation.
Main Methods:
- Carboxymethylcellulose sodium (NaCMC) was combined with additives (amino acids, meglumine, trometamol, urea).
- Matrices were characterized using Fourier transform infrared spectroscopy, differential scanning calorimetry, hot stage microscopy, and X-ray powder diffraction.
- Synchrotron X-ray diffraction was employed to assess homogeneity and crystallinity.
Main Results:
- A new polyelectrolyte matrix based on NaCMC and additives was successfully created and found viable for HME.
- Careful tuning of additive amounts was crucial for achieving an amorphous polymer matrix.
- NaCMC combined with lysine or meglumine showed particularly promising results.
Conclusions:
- This study presents an alternative strategy for creating HME-compatible polymeric matrices without synthesizing new polymers.
- The developed NaCMC-based matrices offer potential for amorphous drug formulations.
- Further research is required to incorporate drugs into these novel matrices.
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