Prolonged Release Pharmaceutical Composition Containing 3-(3-Dimethylamino-1-Ethyl-2-Methyl-Propyl)Phenol

Abstract

A pharmaceutical formulation for prolonged 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.

Description

CROSS REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation co-pending application Ser. No. 10 / 831,368, filed Apr. 26, 2004, which in turn was a continuation of international patent application no. PCT / EP02 / 11809, filed Oct. 22, 2002, designating the United States of America, and published in German as WO 03 / 035053, the entire disclosure of which is incorporated herein by reference. Priority is claimed based on Federal Republic of Germany patent application nos. DE 101 52 469.2, filed Oct. 24, 2001, and DE 102 48 309.4, filed Oct. 16, 2002.BACKGROUND OF THE INVENTION[0002]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.[0003]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 f...

AI Technical Summary

Benefits of technology

The present invention provides a pharmaceutical formulation with slow release of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol or a pharmaceutically acceptable salt thereof. The formulation contains a matrix with slow release of the active ingredient, which is achieved by using hydrophilic or hydrophobic polymers as pharmaceutically acceptable matrix forming agents. The formulation provides long-lasting therapeutic efficacy over a relatively long period of time due to the slow release of the active ingredient. It also allows for rapid onset of pain relief in the patient and maintains an adequate level of active ingredient in the blood plasma for at least 12 hours. The formulation combines the properties of a formulation with immediate release of active ingredient and a formulation with slow release, providing effective pain relief and long-lasting therapeutic action.

Problems solved by technology

However, the need for frequent dosing easily leads to errors in administration and to undesirable variations in concentration in the plasma which are detrimental to patient compliance and the therapeutic benefit, particularly when treating chronically painful conditions.

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