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Please use this identifier to cite or link to this item: http://hdl.handle.net/1942/22756

Title: Stearic acid and high molecular weight PEO as matrix for the highly water soluble metoprolol tartrate in continuous twin-screw melt granulation
Authors: Monteyne, Tinne
Adriaensens, Peter
Brouckaert, Davinia
Remon, Jean-Paul
Vervaet, Chris
De Beer, Thomas
Issue Date: 2016
Publisher: ELSEVIER SCIENCE BV
Citation: INTERNATIONAL JOURNAL OF PHARMACEUTICS, 512(1), p. 158-167
Abstract: Granules with release-sustaining properties were developed by twin screw hot melt granulation (HMG) using a combination of stearic acid (SA) and high molecular weight polyethylene oxide (PEO) as matrix for a highly water soluble model drug, metoprolol tartrate (MPT). Earlier studies demonstrated that mixing molten SA and PEO resulted in hydrogen bond formation between hydroxyl groups of fatty acid molecules and ether groups in PEO chains. These molecular interactions might be beneficial in order to elevate the sustained release effect of drugs from a SA/PEO matrix. This study aims to investigate the continuous twin screw melt granulation technique to study the impact of a SA/PEO matrix on the dissolution rate of a highly water soluble drug (MPT). Decreasing the SA/PEO ratio improved the release-sustaining properties of the matrix. The solid state of the granules was characterized using differential scanning calorimetry (DSC), nuclear magnetic resonance (NMR), X-ray diffraction (XRD), Raman spectroscopy, Fourier transform infrared (FTIR) and near infrared chemical imaging (NIR-CI) in order to understand the dissolution behavior. The results revealed a preferential interaction of the MPT molecules with stearic acid impeding the PEO to form hydrogen bonds with the stearic acid chains. However, this allowed the PEO chains to recrystallize inside the stearic acid matrix after granulation, hence, elevating the release-sustaining characteristics of the formulation.
Notes: [Monteyne, Tinne; Brouckaert, Davinia; De Beer, Thomas] Univ Ghent, Lab Pharmaceut Proc Analyt Technol, Dept Pharmaceut Anal, Fac Pharmaceut Sci, Ottergemsesteenweg 460, B-9000 Ghent, Belgium. [Adriaensens, Peter] Hasselt Univ, Inst Mat Sci, Lab Appl & Analyt Chem, Campus Diepenbeek,Agoralaan,Bldg D, Diepenbeek, Belgium. [Remon, Jean-Paul; Vervaet, Chris] Univ Ghent, Fac Pharmaceut Sci, Dept Pharmaceut, Lab Pharmaceut Technol, Ottergemsesteenweg 460, B-9000 Ghent, Belgium.
URI: http://hdl.handle.net/1942/22756
DOI: 10.1016/j.ijpharm.2016.07.035
ISI #: 000384863700016
ISSN: 0378-5173
Category: A1
Type: Journal Contribution
Validation: ecoom, 2017
Appears in Collections: Research publications

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