Poly(2-ethyl-2-oxazoline) as matrix excipient for drug formulation by hot melt extrusion and injection molding.
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.
Department of Organic Chemistry, Ghent University, Ghent, Belgium
Bart
B
Claeys
Anouk
A
Vervaeck
Chris
C
Vervaet
Jean Paul
JP
Remon
Richard
R
Hoogenboom
Bruno G
BG
De Geest
D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D004337:Drug Carriers / Q000737:chemistry*; D011345:Fenofibrate / Q000737:chemistry*; D008790:Metoprolol / Q000737:chemistry; D011073:Polyamines / Q000737:chemistry*; D014867:Water / Q000737:chemistry
D004337:Drug Carriers; D011073:Polyamines; C511916:poly(2-ethyl-2-oxazoline); D014867:Water; D008790:Metoprolol; D011345:Fenofibrate