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Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence01:27

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Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...

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Hot-melt extrusion technology and pharmaceutical application.

Matthew Wilson1, Marcia A Williams, David S Jones

  • 1Queen's University Belfast, School of Pharmacy, 97 Lisburn Road, Belfast BT9 7BL, UK. mwilson21@qub.ac.uk

Therapeutic Delivery
|July 31, 2012
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Summary
This summary is machine-generated.

Hot-melt extrusion (HME) enhances drug solubility and bioavailability by molecularly dispersing poorly soluble drugs in a polymer carrier. This pharmaceutical manufacturing technique is crucial for developing advanced drug-delivery systems.

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Area of Science:

  • Pharmaceutical Technology
  • Materials Science
  • Drug Delivery

Background:

  • Hot-melt extrusion (HME) is a widely adopted manufacturing process with a long history in the plastics and medical device industries.
  • Its application in pharmaceuticals is growing, driven by the need to improve the solubility and bioavailability of novel drug compounds.
  • HME is particularly effective for creating advanced drug-delivery systems, including solid dosage forms and transdermal patches.

Purpose of the Study:

  • To highlight the increasing significance of hot-melt extrusion (HME) in pharmaceutical manufacturing.
  • To explain the mechanism of HME in improving drug solubility and bioavailability.
  • To address the challenges and advancements in HME for drug-delivery systems.

Main Methods:

  • HME utilizes heat, pressure, and agitation within an extrusion channel to mix and process materials.
  • Twin-screw extruders are commonly employed for solid dosage forms, providing both dispersive and distributive mixing with high shear.
  • The process disperses drug particles within a polymer matrix, achieving molecular dispersion.

Main Results:

  • HME facilitates the molecular dispersion of poorly soluble drugs within polymer carriers.
  • This dispersion significantly enhances drug dissolution rates and improves overall bioavailability.
  • A key challenge is stabilizing amorphous drugs to prevent recrystallization during storage.

Conclusions:

  • Hot-melt extrusion is a vital process for enhancing drug solubility and creating effective solid dispersions.
  • The pharmaceutical industry is seeing increased development of specialized HME equipment and materials.
  • HME offers a significant pathway for the development of advanced pharmaceutical formulations and drug-delivery systems.