11. Hot Melt Extrusion: A Process Overview and Use in Manufacturing Solid Dispersions of Poorly Water-Soluble Drugs

  1. Dennis Douroumis1 and
  2. Alfred Fahr2
  1. Shu Li,
  2. David S. Jones and
  3. Gavin P. Andrews

Published Online: 4 FEB 2013

DOI: 10.1002/9781118444726.ch11

Drug Delivery Strategies for Poorly Water-Soluble Drugs

Drug Delivery Strategies for Poorly Water-Soluble Drugs

How to Cite

Li, S., Jones, D. S. and Andrews, G. P. (2013) Hot Melt Extrusion: A Process Overview and Use in Manufacturing Solid Dispersions of Poorly Water-Soluble Drugs, in Drug Delivery Strategies for Poorly Water-Soluble Drugs (eds D. Douroumis and A. Fahr), John Wiley & Sons Ltd, Oxford, UK. doi: 10.1002/9781118444726.ch11

Editor Information

  1. 1

    School of Science, University of Greenwich, UK

  2. 2

    Friedrich-Schiller University of Jena, Germany

Publication History

  1. Published Online: 4 FEB 2013
  2. Published Print: 21 JAN 2013

ISBN Information

Print ISBN: 9780470711972

Online ISBN: 9781118444726

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Keywords:

  • Oral Drug Delivery;
  • Poorly water-soluble drugs;
  • Solid Dispersions;
  • Amorphous drugs;
  • Melt extrusion;
  • Twin screw extrusion;
  • Drug-polymer miscibility;
  • co-crystals

Summary

The high numbers of active pharmaceutical ingredients (APIs) within pharmaceutical pipelines that possess limited bioavailability is a major concern for the pharmaceutical industry. For APIs possessing high permeability but poor solubility, the formation of solid dispersions is an attractive approach to overcome such issues. Over the last decade, hot melt extrusion, a technology originating from the plastics industry, has become an interesting and versatile tool to manufacture solid dispersions. With an increasing number of publications and patents, hot-melt extrusion has been extensively demonstrated to provide efficient manufacture of solid dispersions with tailored drug release and bioavailability enhancement. In particular, hot-melt extrusion is considered economic and labour friendly over other processing techniques owing to its solventless and continuous fashion of operation. This chapter, introduces the basics of the HME technology including its equipment, operating principles, product characterization, and the selection of formulation materials. Different mechanisms of solubility enhancement and their evaluation post-manufacture are also featured. Moreover, selected pharmaceutical applications described in the scientific literature are reviewed with emphasis on improved API aqueous solubility.

The high numbers of active pharmaceutical ingredients (APIs) within pharmaceutical pipelines that possess limited bioavailability are a major concern for the pharmaceutical industry. For APIs possessing high permeability but poor solubility, the formation of solid dispersions is an attractive approach to overcome such issues. Over the last decade, hot melt extrusion, a technology originating in the plastics industry, has become an interesting and versatile tool to manufacture solid dispersions. With an increasing number of publications and patents, hot melt extrusion has been extensively demonstrated to provide the efficient manufacture of solid dispersions with tailored drug release and bioavailability enhancement. In particular, hot melt extrusion is considered economic and labour-friendly over other processing techniques owing to its solventless and continuous fashion of operation. This chapter introduces the basics of the HME technology, including equipment, operating principles, product characterization, and the selection of formulation materials. Different mechanisms of solubility enhancement and their evaluation post-manufacture are also featured. Moreover, selected pharmaceutical applications described in the scientific literature are reviewed with an emphasis on improved API aqueous solubility.