title: Controlling the Release of Indomethacin from Glass Solutions Layered with a Rate Controlling Membrane Using Fluid-Bed Processing. Part 2: The Influence of Formulation Parameters on Drug Release.
abstract: This study aimed to investigate the pharmaceutical performance of an indomethacin-polyvinylpyrrolidone (PVP) glass solution applied using fluid bed processing as a layer on inert sucrose spheres and subsequently top-coated with a release rate controlling membrane consisting of either ethyl cellulose or Eudragit RL. The implications of the addition of a pore former (PVP) and the coating medium (ethanol or water) on the diffusion and release behavior were also considered. In addition, the role of a charge interaction between drug and controlled release polymer on the release was investigated. Diffusion experiments pointed to the influence of pore former concentration, rate controlling polymer type, and coating solvent on the permeability of the controlled release membranes. This can be translated to drug release tests, which show the potential of diffusion tests as a preliminary screening test and that diffusion is the main factor influencing release. Drug release tests also showed the effect of coating layer thickness. A charge interaction between INDO and ERL was demonstrated, but this had no negative effect on drug release. The higher diffusion and release observed in ERL-based rate controlling membranes was explained by a higher hydrophilicity, compared to EC.
authors.affiliation: Drug Delivery and Disposition, KU Leuven , Campus Gasthuisberg O&N2, Herestraat 49, Box 921, 3000 Leuven, Belgium.
authors.forename: Aswin
authors.initials: A
authors.lastname: Dereymaker
authors.affiliation: Drug Delivery and Disposition, KU Leuven , Campus Gasthuisberg O&N2, Herestraat 49, Box 921, 3000 Leuven, Belgium.
authors.forename: Jirka
authors.initials: J
authors.lastname: Pelgrims
authors.affiliation: Drug Delivery and Disposition, KU Leuven , Campus Gasthuisberg O&N2, Herestraat 49, Box 921, 3000 Leuven, Belgium.
authors.forename: Frederik
authors.initials: F
authors.lastname: Engelen
authors.affiliation: Applied and Analytical Chemistry, Institute for Materials Research (IMO), Hasselt University , Campus Diepenbeek, Agoralaan 1- Building D, 3590 Diepenbeek, Belgium.
authors.forename: Peter
authors.initials: P
authors.lastname: Adriaensens
authors.affiliation: Drug Delivery and Disposition, KU Leuven , Campus Gasthuisberg O&N2, Herestraat 49, Box 921, 3000 Leuven, Belgium.
authors.forename: Guy
authors.identifier: 0000-0001-9166-6075
authors.initials: G
authors.lastname: Van den Mooter
mesh_terms: D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004058:Diffusion; D065546:Drug Liberation / Q000187:drug effects*; D005079:Excipients / Q000737:chemistry; D005898:Glass / Q000737:chemistry*; D057927:Hydrophobic and Hydrophilic Interactions; D007213:Indomethacin / Q000737:chemistry*; D008566:Membranes / Q000737:chemistry*; D011108:Polymers / Q000737:chemistry; D012995:Solubility; D012996:Solutions / Q000737:chemistry; D012997:Solvents / Q000737:chemistry; D014867:Water / Q000737:chemistry
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D011108:Polymers; D012996:Solutions; D012997:Solvents; D014867:Water; C058665:Eudragit RL; C013517:ethyl cellulose; D002482:Cellulose; D007213:Indomethacin
keywords: controlled release; drug diffusion; drug release; fluid bed coating; solid dispersions; solid-state nuclear magnetic resonance