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Hot-Melt Extrusion: Enhancing Drug Efficacy and Bioavailability
To be effective, solid oral drugs need to be highly soluble so they exhibit good bioavailability, and they also need to have high patient compliance—that is, the size, taste, and amount of pills needed must be acceptable to the person taking them. Currently, 90% of new molecules and roughly 40% of the top solid oral drugs marketed in the U.S. and Europe exhibit low solubility.1
Hot-melt extrusion (HME) can help achieve the needed high efficacy, overcome bioavailability issues of an active pharmaceutical ingredient (API), and tailor release profiles. HME is a straightforward technique in which solid dispersion of drug particles or molecules in a polymer matrix is achieved. Depending on the processing conditions and the chemical and physical properties of polymers and APIs, different types of dispersions are possible.
In this 28-page compendium, we introduce the versatility of HME, answer questions about what happens when materials are heated, share how to design a solvent-free HME process, and describe how to produce different dosage forms.
Highlights include:
- Introduction to pharmaceutical hot-melt extrusion
- Physical and thermal characterization of the formulation
- HME process design and development
- Downstream processing and resulting dosage forms
- HME process examples
1M. Rodriguez-Aller, D. Guillarme, J. L. Veuthey, and R. Gurny, “Strategies for formulating and delivering poorly water-soluble drugs,” J Drug Deliv Sci Technol, vol. 30, pp. 342–351, 2015, doi: 10.1016/j.jddst.2015.05.009.