Novel combination of anticholinergic and ss mimetics for the treatment of respiratory diseases

Abstract

The present invention describes a combination of anticholinergic and β mimetics for the treatment of respiratory diseases including airway inflammation or obstruction such as chronic obstructive pulmonary disease (COPD) and asthma. It further comprises the preparation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the Novolizer®.

1 . A combination of an anticholinergic and a long-acting β2-mimetic agent for the treatment of respiratory diseases, especially of inflammatory or obstructive diseases.  
     
     
         2 . The combination according to  claim 1  wherein the anticholinergic is selected from the group consiting of racemic glycopyrrolate, an enantiomer thereof, a diasterioisomer thereof and physiologically acceptable salts or a mixture and mixtures thereof.  
     
     
         3 . The combination according to  claim 2  wherein the anticholinergic is R,R-glycopyrrolate or a physiologically acceptable salt thereof.  
     
     
         4 . The combination according to  claim 1  wherein the β2-mimetic agent is selected from the group consisting of formoterol and salmeterol and their physiologically acceptable salts.  
     
     
         5 . The combination according to  claim 4  wherein the β2-mimetic agent is formoterol or a physiologically acceptable salt thereof.  
     
     
         6 . The combination according to  claim 5  wherein the daily dose of formoterol is from 1 to 72 μg.  
     
     
         7 . The combination according to  claim 4  wherein the β2-mimetic agent is salmeterol or its physiologically acceptable salts.  
     
     
         8 . The combination according to  claim 7  wherein the daily dose of salmeterol is from 10 to 300 μg.  
     
     
         9 . The combination according to  claim 1  wherein the daily dose of R,R-glycopyrrolate is from 5 to 500 μg.  
     
     
         10 . The combination according to  claim 1  wherein the daily dose of R,R-glycopyrrolate is from 5 to 100 μg.  
     
     
         11 . A pharmaceutical for the treatment of allergies and respiratory diseases containing as active substances an anticholinergic and at least a long-acting β2 sympathomimetic.  
     
     
         12 . The pharmaceutical according to  claim 11 , wherein the anticholinergic is selected from the group consisting of racemic glycopyrrolate, an enantiomer thereor, a diastereoisomer thereof and physiologically acceptable salts and mixtures thereof.  
     
     
         13 . The pharmaceutical according to  claim 12 , that comprises R,R glycopyrrolate or a physiologically acceptable salt thereof.  
     
     
         14 . The pharmaceutical according to  claim 11 , that comprises R,R glycopyrrolate and formoterol or their physiologically acceptable salts.  
     
     
         15 . The pharmaceutical according to  claim 11 , wherein the active substances are available readily mixed in a fixed combination, if appropriate together with the usual excipients, adjuncts, and additives in a pharmaceutical form suitable for inhalative application.  
     
     
         16 . The pharmaceutical according to  claim 11 , where the active substances are available in separate packing units whereby both substances can be taken from the separate packing units in such a way that they are available for simultaneous inhalative application.  
     
     
         17 . The pharmaceutical according to  claim 16 , where the active substances can be administered independently from each other.  
     
     
         18 . The pharmaceutical according to  claim 11 , that is an inhalable aerosol with or without propellant.  
     
     
         19 . The pharmaceutical according to  claim 11  that is an inhalable dry powder.  
     
     
         20 . The pharmaceutical according to  claim 11 , that is an inhalable suspension or solution.  
     
     
         21 . The pharmaceutical according to  claim 11  presented in an inhaler.  
     
     
         22 . The pharmaceutical according to  claim 21 , comprising formoterol as β2 sympathomimetic.  
     
     
         23 . The pharmaceutical according to  claim 21 , comprising salmeterol as β2 sympathomimetic.  
     
     
         24 . The combination of  claim 6  wherein the daily dose is from 3 to 50 μg,  
     
     
         25 . The combination of  claim 24  wherein the daily dose is from 6 to 48 μg.  
     
     
         26 . The combination of  claim 8  wherein the daily dose is from 25 to 200 μg.  
     
     
         27 . The combination of  claim 26  wherein the daily dose is from 50 to 200 μg.  
     
     
         28 . The combination of  claim 9  wherein the daily dose is from 15 to 300 μg.