EP1519711A1 — Controlled-release pharmaceutical formulations

USPTO Abstract

The invention provides controlled release pharmaceutical formulations having a coated core with the core comprising a drug-containing composition and a waterswellable composition, each occupying essentially separate regions within the core. The drug-containing composition comprises a PDE4D inhibitor, or a pharmaceutically acceptable salt thereof, preferably (R)-2-[4-({[2-(benzo[1,3]dioxol-5-yloxy)-pyridine-3carbonyl]-amino}-methyl)-3-fluoro-phenoxy]-propionic acid, or a pharmaceutically acceptable salt thereof, or 2-(4-fluorophenoxy)-N-[4-(1-hydroxy-1-methyl-ethyl)benzyl]-nicotinamide, or a pharmaceutically acceptable salt thereof, and a drug entraining agent. The coating around the core is water-permeable, water-insoluble, and has at least one delivery port therethrough. The invention further provides methods of reducing the nausea and emetic effects of PDE4D inhibitors, and controlled-release formulations having improved PDE4D inhibitor in vivo and in vitro profiles.