Hot-Melt Extrusion of Modified Release Multiparticulates

Life Sciences : Drug Delivery

Available for licensing

Inventors

  • James McGinity, Ph.D. , College of Pharmacy
  • Sandra Schilling , College of Pharmacy

Background/unmet need

Dosage forms comprising multiparticulates have significant advantages, including enhanced bioavailability, more constant blood plasma levels, lower risk of dangerous high local drug concentration, and favorable pharmacokinetics. Post-processing of multiparticulates into a monolithic dosage form is necessary to increase safety and patient compliance.

Multiparticulates can be incorporated into capsules or tablets as the single dosage form. Tablets are favorable because capsules are easily tampered with, more expensive, and less stable. However, it has been difficult to effectively incorporate multiparticulates with modified-release properties into tablets. Tableting involves the exposure of multiparticulates to high unidirectional compaction forces that may cause rupture of functional coatings and particle deformation. Thus, there is a need for a process that maintains the integrity of multiparticulates, thereby enabling a monolithic dosage form that is easy to produce, more stable, less expensive, and better for patients.

Invention Description

Researchers at The University of Texas at Austin have developed a novel method of pharmaceutical preparation that utilizes hot-melt extrusion of multiparticulates. The present invention seeks to combine the benefits of a monolithic dosage form that releases multiple unit dosage systems after administration.

The present invention comprises a modified release pharmaceutical formulation and a method of preparation for the embedding of multiparticulates into a polymeric or wax-like matrix. Said multiparticulates comprise an effective amount of a therapeutic compound and a drug-release controlling principle and/ or a drug-protecting principle.

Benefits/Advantages

  • Carrier material dissolves independently of release rate of microparticulates; thus, a very precise drug release rate controlled by the particles can be achieved
  • Maintains integrity and release properties of microparticulates
  • Easy to implement using standard melt-extrusion techniques and ingredients
  • Potentially cheaper monolithic dosage form than capsules
  • Could enable tamper-proof formulations of microparticulates

Market potential/applications

This technology can be used to deliver a variety of drugs orally in a wide range of drug release profiles.

Development Stage

Lab/bench prototype

IP Status

  • 3 foreign patents application filed
  • 3 foreign patents issued
  • 1 U.S. patent issued: 9,192,578
  • 1 U.S. patent issued: 9,827,202