Ph-controlled pulsatile delivery system, methods for...

A - Human Necessities – 61 – K

Patent

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A61K 9/00 (2006.01) A61K 9/20 (2006.01) A61K 9/28 (2006.01) A61K 9/50 (2006.01) A61K 31/00 (2006.01) A61K 39/00 (2006.01) A61K 47/30 (2006.01)

Patent

CA 2617051

The invention relates to delivery systems that allow for the pulsatile release of a substance, such as a drug, in response to a change in pH. More specifically, it relates to drug administration to the GI tract, in particular to site-specific intestinal drug delivery via the oral route. Provided is a pH- controlled pulsatile release system (PPRS) comprising a core surrounded by a coating layer, wherein said core comprises an active substance and wherein said coating layer comprises a pH-sensitive coating material wherein a swellable agent is embedded. Said swellable agent is capable of taking up at least 1.1 times, preferably at least 5 times, more preferably at least 10 times its weight in water. Also provided is a pharmaceutical composition comprising a PPRS, in particular a colon-specific PPRS.

La présente invention concerne des systèmes de distribution qui permettent la libération pulsatile d'une substance, telle qu'un médicament, en réponse à un changement de pH. Plus particulièrement, elle concerne l'administration de médicaments dans le tube digestif, en particulier la distribution de médicaments intestinaux spécifiques à un site par voie orale. L'invention concerne un système de distribution pulsatile commandé par le pH (PPRS) comprenant un noyau entouré d~une couche de revêtement, ledit noyau comprenant une substance active et ladite couche de revêtement comprenant un matériau de revêtement sensible au pH dans lequel un agent gonflable est inclus. Ledit agent gonflable peut absorber au moins 1,1 fois, de préférence au moins 5 fois, mieux encore, au moins 10 fois son poids en eau. L'invention concerne également une composition pharmaceutique comprenant un PPRS, en particulier un PPRS spécifique au côlon.

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