title: Modulation of the dissolution profiles from Geomatrix multi-layer matrix tablets containing drugs of different solubility.
abstract: A new multi-layer tablet design has recently been proposed for constant drug release: Geomatrix Technology (Jago Pharma, Muttenz, Switzerland). It consists in the application of a drug-free barrier layer on one or both bases of an active core (hydrophilic matrix). The partial coating modulates the core hydration process and reduces the surface area available for drug release. The result is an extended release that draws close to a linear profile. The device was mainly intended for soluble drugs, while an excessive reduction of the release rate may be obtained with drugs of low solubility. In this study a new time-dependent polymeric barrier is proposed to control the release of sparingly soluble drugs. Two different barrier compositions (one swellable and one erodible) are applied on active cores containing drugs of different water solubility, Trapidil, Ketoprofen and Nicardipine hydrochlorides, and the drug dissolution patterns of the different multi-layer devices are compared. During dissolution, the swellable barrier swells and gels, but is not eroded, thus acting as a modulating membrane during the release process. The erodible barrier, instead, is progressively removed by the dissolution medium, exposing in time an increasing extent of the planar surface(s) of the core to interaction with the outer environment and to drug release. Both types of coatings are able to control drug release from the devices: the swellable barrier shows a stronger modulation efficiency and is more suitable to modify the delivery pattern of highly soluble drugs; the erodible barrier shows a time-dependent coating effect that provides better control of the dissolution profile of sparingly soluble drugs.
authors.affiliation: Department of Pharmaceutical Chemistry, University of Pavia, Italy.
authors.forename: U
authors.initials: U
authors.lastname: Conte
authors.forename: L
authors.initials: L
authors.lastname: Maggi
mesh_terms: D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D006801:Humans; D066298:In Vitro Techniques; D007660:Ketoprofen / Q000008:administration & dosage / Q000493:pharmacokinetics; D008422:Materials Testing; D009529:Nicardipine / Q000008:administration & dosage / Q000493:pharmacokinetics; D011108:Polymers; D012995:Solubility; D013607:Tablets; D014192:Trapidil / Q000008:administration & dosage / Q000493:pharmacokinetics; D014867:Water
chemical_list: D001672:Biocompatible Materials; D003692:Delayed-Action Preparations; D011108:Polymers; D013607:Tablets; D014867:Water; D007660:Ketoprofen; D009529:Nicardipine; D014192:Trapidil