Osmotic continuous dispensing oral delivery system...

A - Human Necessities – 61 – K

Patent

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167/252, 167/273

A61K 31/135 (2006.01) A61K 9/00 (2006.01) A61K 9/22 (2006.01) A61K 9/24 (2006.01)

Patent

CA 1334382

The present invention relates to a therapeutic delivery system of metoprolol. This delivery system is suitable for the oral administration of metoprolol in a controlled and continuous manner. About 50 to 90 % of the dose of the active agent is released into the gastrointestinal tract at a rate of about 5 to 12 % by weight per hour of the dose to be administered. The oral delivery system (OROS) according to the present invention essentially consists of the following components: a) a tablet core consisting of an osmotically active composition com- prising an effective amount of a pharmaceutically acceptable metoprolol salt in combination with a pharmaceutically acceptable tablet binder, and, optionally, an osmotically active driving agent and/or further pharmaceutically acceptable additives; b) a discrete inner layer of a water-soluble and even coating on the tablet core a) being present in an amount of between about 0.3 % and about 10 % by weight of the core; c) a semipermeable discrete outer layer impermeable to metoprolol and permeable to gastrointestinal fluid, surrounding and adhesively bonded to the inner layer a); and d) at least one passageway through both layers b) and c) for dispensing the active agent metoprolol, in communication with the tablet core a) and the external environment.

597406

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