Osmotic continuous dispensing oral delivery system...

A - Human Necessities – 61 – K

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A61K 9/22 (2006.01) A61K 9/00 (2006.01) A61K 31/13 (2006.01) A61K 31/135 (2006.01)

Patent

CA 1312016

4-16168/=/CGC 1232 OSMOTIC CONTINUOUS DISPENSING ORAL DELIVERY SYSTEM CONTAINING A MODERATELY WATER-SOLUBLE METOPROLOL SALT HAVING IMPROVED CORE COMPOSITION AND USE THEREOF ABSTRACT OF THE DISCLOSURE An osmotic dispensing oral delivery system containing a moderately water-soluble metoprolol salt for total delivery of between about 50 and about 500 mg of metoprolol wherein from about 60 up to about 90 percent of said metoprolol is released in the gastro-intestinal tract at a substantially continuous rate of about 5 to about 12 percent by weight per hour comprising: a) a semipermeable shaped wall membrane substantially imper- meable to said salt and permeable to gastrointestinal fluid, b) a core compartment within and defined by said wall, said core containing a solid osmotically active composition comprising: about 7.5 to about 15 percent by weight poly-N-vinylpyrrolidone; up to about 5 percent by weight of a tabletting lubricant; and about 92.5 to about 80 percent by weight of said metoprolol salt, based on the core composition weight and c) at least one passageway in the wall, for dispensing the metoprolol salt, in communication with said core compart- ment and the external environment, and a method of use thereof in conditions responsive to beta1- adrenoreceptor blocking agents.

551655

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