Dissolution improvement of an active pharmaceutical ingredient in a polymer melt by hot melt extrusion
-
Laura Restrepo-Uribe
,
Nicolas Ioannidis
Abstract
Dissolution of poorly water-soluble active pharmaceutical ingredients (APIs) in polymeric melts plays an important role in the manufacturing of solid dispersions and solid solutions. The understanding of the dissolution is essential for selecting the processing equipment, the operating conditions, and the polymer excipients. The methodology presented in this work for ketoprofen (KTO) and polymer excipients serves as a screening process to select the best API-polymer formulation for hot melt extrusion (HME) to target a specific release profile. KTO dispersion within the polymer was characterized by differential scanning calorimetry (DSC), X-ray diffraction (XRD), and dissolution tests. Thermal characterization shows that a single phase amorphous solid solution (one glass transition temperature [Tg]) was achieved under the HME processing conditions and screw configuration; and with the combination of polymer excipients, an extended release profile of KTO was accomplished, releasing 100% of KTO in 24 h.
Acknowledgements
The authors gratefully acknowledge the technical support of the professionals from the Instituto de Capacitación e Investigación del Plástico y del Caucho (ICIPC), the pharmaceutical company Procaps S.A., and Universidad del Norte. The support and valuable technical discussions provided by Dr. Costas Gogos from the Polymer Processing Institute (PPI) are greatly appreciated. Dr. Shaukat Ali from BASF and Charlie Martin from Leistritz are gratefully acknowledged for the donation of polymeric excipients and the loan of a pharmaceutical twin screw extruder (Nano 16), respectively. The authors acknowledge the financial support of Colciencias grants 562-2012 and 156-2016, ICIPC, Procaps S.A. and Universidad del Norte. The infrastructure support of Universidad EAFIT is greatly appreciated.
Conflict of interest statement: The authors declare to have no conflicts of interest regarding this article.
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Articles in the same Issue
- Frontmatter
- Material properties
- Thermo-oxidative and thermal degradation kinetics of silica/polymethyl methacrylate composites with electrostatic interaction phase interfaces
- Study of the rheology and foaming processes of poly(vinyl chloride) plastisols with different foaming agents
- The non-isothermal crystallization behavior of polyamide 6 and polyamide 6/HDPE/MAH/L-101 composites
- Preparation and assembly
- Preparation and properties of biodegradable polymer/nano-hydroxyapatite bioceramic scaffold for spongy bone regeneration
- Properties of EPDM/PP thermoplastic vulcanizates produced by an intermeshing-type internal mixer comparing with a co-rotating twin-screw extruder
- Applications and characterization of silicalite-1/polydimethylsiloxane composite membranes for the pervaporation of a model solution and fermentation broth
- Electroless plate of polyaniline-silver composite layer on polyester fibers
- Surface modification of polymeric flat sheet membranes by adding oligomeric fluoroalcohol
- Engineering and processing
- Processing polymer nanocomposites with natural additives for medical applications
- Dissolution improvement of an active pharmaceutical ingredient in a polymer melt by hot melt extrusion
- Determination of the fundamental dimension development in building direction for laser-sintered parts
