Multi-unit gastroretentive pharmaceutical dosage form comprising microparticles

摘要

This invention relates to an orally administrable, gastroretentive pharmaceutical dosage form which contains at least one pharmaceutically active ingredient and at least one polymeric adjuvant. The adjuvant serves to retain the dosage form in a selected region of the gastrointestinal tract for sufficient time for the pharmaceutically active ingredient to be released and absorbed. Ideally the dosage form will contain two or more pharmaceutically active ingredients which are delivered to different regions of the gastrointestinal tract.

主权项

1. An orally administrable gastroretentive pharmaceutical dosage form comprising a plurality of polymeric units, each polymeric unit comprising a cross-linked polymeric matrix which is porous and buoyant in gastric fluid, the polymeric matrix of each polymeric unit comprising:
alginate, pectin, polyacrylic acid (PAA), and polymeric microparticles comprising polymers which are cross-linked and at least one pharmaceutically active ingredient, wherein at least one of the polymers is a bioadhesive polymeric adjuvant which adheres to the mucosal lining of the stomach and wherein the polymers forming the microparticles comprise chitosan and poly(methacrylate); wherein, in use, the plurality of polymeric units initially float on the surface of the gastric fluid, then release the polymeric microparticles; and further wherein the microparticles, upon release, adhere to the mucosal surface of the stomach.