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Hot Melt Extrudates Formulated Using Design Space: One Simple Process for Both Palatability and Dissolution Rate
Lorena F B Malaquias1, Heidi L Schulte1, Juliano A Chaker2
1Laboratory of Food, Drug and Cosmetics (LTMAC), School of Health Sciences, University of Brasília, 70910-900 Brasília, Federal District, Brazil.
Journal of Pharmaceutical Sciences
|August 30, 2017
Summary
Optimized itraconazole (ITZ) formulations using hot melt extrusion (HME) with polymer blends significantly improved dissolution rates and taste masking. The study identified a specific polymer combination for enhanced oral drug delivery.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Itraconazole (ITZ) oral formulations often face challenges with palatability and dissolution.
- Hot melt extrusion (HME) is a promising technique for improving drug formulation properties.
Purpose of the Study:
- To optimize itraconazole (ITZ) solid oral formulations for enhanced palatability and dissolution rate.
- To investigate the synergistic effects of combining different polymers (Plasdone®, Klucel® ELF, Soluplus®) using HME.
Main Methods:
- Utilized a simplex centroid mixture design for polymer combination.
- Employed laboratory hot melt extrusion (HME) without recirculation.
- Characterized formulations using physicochemical assays, dissolution rate testing, and electronic tongue (e-tongue) for palatability.
Main Results:
- HME processing resulted in homogeneous, dense extrudates with amorphized itraconazole.
- Significant increases in dissolution rate were observed, particularly with poly(1-vinylpyrrolidone-co-vinyl acetate) (PVP/VA) and 2-hydroxypropyl ether cellulose (HPC) combinations.
- Improved taste masking was achieved, especially with higher proportions of polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol (SOL) and HPC.
Conclusions:
- Polymer combinations in HME systems act synergistically to enhance itraconazole formulation properties.
- The optimized formulation predicted to contain ITZ 25.0%, SOL 33.2%, HPC 28.9%, and PVP/VA 12.9% (w/w) offers a promising approach for improved oral drug delivery.
- HME is an effective technology for developing palatable and highly soluble itraconazole formulations.
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