Patent ID: 8101209
Filing Date: 2012-01-24
Classification: A61K,A61P,Y10S

Abstract:
1. Microparticulate oral pharmaceutical dosage form for the delayed and controlled release of at least one active principle (AP)—excluding perindopril—this active principle having an absorption window in vivo that is essentially limited to the upper parts of the gastrointestinal tract, wherein the dosage form comprises “reservoir” microcapsules of active principle, each coated with one single, composite coating film, wherein the single, composite coating film comprises at least one hydrophilic polymer A carrying groups that are ionized at neutral pH, and at least one hydrophobic compound B; wherein the at least one hydrophobic compound B is selected from the group consisting of hydrogenated vegetable oils, vegetable waxes, wax yellow, wax white, wax microcrystalline, lanolin, anhydrous milk fat, hard fat suppository base, lauroyl macrogolglycerides, cetyl alcohol, polyglyceryl diisostearate, diester or triester of glycerol with at least one fatty acid and mixtures thereof; wherein the microcapsules have a diameter of between 200 and 800 microns; wherein the weight ratio B/A is between 0.5 and 1.5; wherein the release of the active principle is governed by two different triggering mechanisms, wherein the first triggering mechanism releases the at least one active principle based on a variation in pH, wherein the second triggering mechanism releases the at least one active principle after a predetermined residence time in the stomach, wherein the dissolution behavior of the pharmaceutical dosage in vitro is such that: