Poly(2-ethyl-2-oxazoline) as matrix excipient for drug formulation by hot melt extrusion and injection molding

Macromol Rapid Commun. 2012 Oct 15;33(19):1701-7. doi: 10.1002/marc.201200332. Epub 2012 Aug 14.

Abstract

Here we evaluate poly(2-ethyl-2-oxazoline)s (PEtOx) as a matrix excipient for the production of oral solid dosage forms by hot melt extrusion (HME) followed by injection molding (IM). Using metoprolol tartrate as a good water-soluble model drug we demonstrate that drug release can be delayed by HME/IM, with the release rate controlled by the molecular weight of the PEtOx. Using fenofibrate as a lipophilic model drug we demonstrate that relative to the pure drug the dissolution rate is strongly enhanced by formulation in HME/IM tablets. For both drug molecules we find that solid solutions, i.e. molecularly dissolved drug in a polymeric matrix, are obtained by HME/IM.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Calorimetry, Differential Scanning
  • Chemistry, Pharmaceutical
  • Drug Carriers / chemistry*
  • Fenofibrate / chemistry*
  • Metoprolol / chemistry
  • Polyamines / chemistry*
  • Water / chemistry

Substances

  • Drug Carriers
  • Polyamines
  • poly(2-ethyl-2-oxazoline)
  • Water
  • Metoprolol
  • Fenofibrate