Delayed release pharmaceutical composition containing 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol

a technology of dimethylamino-1-ethyl-2-methylpropylphenol and pharmaceutical composition, which is applied in the direction of drug compositions, biocide, microcapsules, etc., can solve the problems of undesirable concentration variation and errors in administration, and achieve good therapeutic efficacy and high repeatability of release properties
US20050058706A1Inactive Publication Date: 2005-03-17GRUNENTHAL GMBH
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
GRUNENTHAL GMBH
Publication Date
2005-03-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

A pharmaceutical formulation for delayed release of the active ingredient 3-(3-dimethylamino-1-ethyl-2-methylpropyl)phenol or a pharmaceutically acceptable salt thereof in a matrix containing between 1 and 80 wt. % of at least one pharmaceutically acceptable hydrophilic or hydrophobic polymer as a matrix forming agent and exhibiting in vivo the following release rate: 3 to 35% by weight (based on 100% by weight active ingredient) 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 0.5 hours; 5 to 50% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 1 hour; 10 to 75% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 2 hours; 15 to 82% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 3 hours; 30 to 97% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 6 hours; more than 50% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 12 hours; more than 70% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 18 hours, and more than 80% by weight 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol released after 24 hours.
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Description

BACKGROUND OF THE INVENTION The present invention relates to a slow-release pharmaceutical formulation, containing 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol or a pharmaceutically acceptable salt thereof in a matrix. 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol is known from European patent no. EP 693,475 as an analgesic pharmaceutical composition and can be administered orally. Conventional formulations for oral administration of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol lead to rapid release of the active ingredient in the gastrointestinal tract, so its analgesic action begins rapidly. At the same time, a rapid reduction in the action is observed. Therefore, the treatment of pronounced chronic pain with 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol formerly required administration of the pharmaceutical composition at relatively short intervals, for example four to eight times daily, to ensure an adequately high concentration of active ingredient in the pa...

Claims

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