Colonic delivery using zn/pectin beads with a eudragit coating.

A - Human Necessities – 61 – K

Patent

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A61K 9/50 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2678131

Drug delivery systems that can deliver therapeutic and/or diagnostic agents to the colon are disclosed. The systems include pectin beads crosslinked with zinc or any divalent cation of interest, which beads are then coated with Eudragit®-type polymers. The drug delivery systems are orally administrable, but can deliver the active agents to the colon, or, in some embodiments, to various other positions in the gastro-intestinal tract. The agents can be used to diagnose, treat, prevent, or investigate a variety of conditions, including infectious diseases, inflammatory diseases, cancers and the like. Certain agents, such as metallo-dependent enzymes, for example, .beta.-lactamase Ll from Stenotrophomonas maltophilia, as well as agents that inactivate macrolide, quinolone, fluoroquinolone or glycopeptide antibiotics, can reduce the quantity of residual antibiotics reaching the colon following antibiotic therapy.

L'invention concerne des systèmes d'administration de médicament pouvant administrer des agents thérapeutiques et/ou de diagnostic au côlon. Les systèmes comprennent des billes de pectine réticulées avec du zinc ou n'importe quel cation divalent d'intérêt, lesquelles billes sont ensuite revêtues de polymères de type Eudragit®. Les systèmes d'administration de médicament peuvent être administrés par voie orale, mais peuvent administrer les agents actifs au côlon ou, dans certains modes de réalisation, à diverses autres positions dans le tractus gastro-intestinal. Les agents peuvent être utilisés pour diagnostiquer, traiter, prévenir ou rechercher une diversité d'états, comprenant des maladies infectieuses, des maladies inflammatoires, des cancers et similaires. Certains agents, tels que les enzymes métallo-dépendantes, par exemple, la .beta.-lactamase Ll provenant de Stenotrophomonas maltophilia, ainsi que des agents inactivant les antibiotiques de macrolide, quinolone, fluoroquinolone ou glycopeptidiques, pouvant réduire la quantité d'antibiotiques résiduels atteignant le côlon à la suite d'une thérapie antibiotique.

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