Combination of anticholinergics and glucocorticoids for the long-term treatment of asthma and COPD

Abstract

The present invention describes the combination of topically inhaled medicinal formulations comprising an anticholinergic component and a glucocorticosteroid component and its use in the symptomatic and prophylactic treatment of diseases of the respiratory tract, especially with an obstructive component or underlying inflammation like asthma and chronic obstructive pulmonary disease (COPD). It further comprises the presentation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the Novolizer®.

1 . A combination of topical anticholinergics with glucocorticoids or their physiologically acceptable salts for the treatment of diseases of the respiratory tract.  
     
     
         2 . The combination according to  claim 1  wherein the anticholinergic is selected from the group consisting of racemic glycopyrrolate, one of its enantiomers or diastereoisomers or their physiologically acceptable salts or a mixture 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 glucocorticoids are selected from the group consisting of budesonide, fluticasone, ciclesonide, mometasone, flunisolide, beclometason and loteprednol and their physiologically acceptable salts.  
     
     
         5 . The combination according to  claim 4  wherein the glucocorticoid is budesonide or a physiologically acceptable salt thereof.  
     
     
         6 . The combination according to  claim 4  where the glucocorticoid is fluticasone or a physiologically acceptable salt thereof.  
     
     
         7 . (canceled)  
     
     
         8 . A pharmaceutical for the treatment of asthma and respiratory diseases containing an anticholinergic and at least a glucocorticoid or their physiologically acceptable salts.  
     
     
         9 . The pharmaceutical according to  claim 8 , wherein the anticholinergic, glucocorticoid or physiologically acceptable salt(s) thereof are available in an appropriate particle size dispersion when inhaled.  
     
     
         10 . The pharmaceutical according to  claim 8 , that is an inhalable aerosol with or without propellant.  
     
     
         11 . The pharmaceutical according to  claim 8 , that it an inhalable dry powder  
     
     
         12 . The pharmaceutical according to  claim 8 , that is an inhalable suspension or solution.  
     
     
         13 . The pharmaceutical according to  claim 8 , wherein the active ingredients are presented in fixed or free combination for simultaneous, sequential or separate administration together with excipients, adjuncts, and additives in a pharmaceutical form suitable for inhalative application.  
     
     
         14 . The pharmaceutical according to  claim 8 , presented in an inhaler.  
     
     
         15 . The pharmaceutical according to  claim 8 , where the anticholinergic is selected from the group consisting of racemic glycopyrrolate, an enantiomer thereof, a diasterioisomer thereof, physiologically acceptable salts thereof and mixtures thereof.  
     
     
         16 . The pharmaceutical according to  claim 15 , containing R,R glycopyrrolate and budesonide or their physiologically acceptable salts as active substance.  
     
     
         17 . The pharmaceutical according to  claim 15 , containing R,R glycopyrrolate and fluticasone or their physiologically acceptable salts as active substance.  
     
     
         18 . (canceled)  
     
     
         19 . (canceled)  
     
     
         20 . (canceled)  
     
     
         21 . (canceled)  
     
     
         22 . (canceled)  
     
     
         23 . (canceled)  
     
     
         24 . (canceled)  
     
     
         25 . A method for producing a pharmaceutical for the treatment of asthma/allergies and/or respiratory diseases in mammals comprising combining a topical anticholinergic and at least a glucocorticoid or physiologically acceptable salts thereof to obtain a pharmaceutical.  
     
     
         26 . The method according to  claim 25  wherein the anticholinergic is selected from the group consisting of racemic glycopyrrolate, an enantiomer thereof, a diastereoisomer thereof, a physiologically acceptable salt thereof and a mixtures thereof.  
     
     
         27 . The method according to  claim 25  wherein the anticholinergic is R,R-glycopyrrolate or a physiologically acceptable salt thereof.  
     
     
         28 . A method of treating asthma/allergies and/or respiratory diseases in a mammal comprising administering an effective amount of the pharmaceutical of  claim 25  to said mammal.  
     
     
         29 . The method according to  claim 28  wherein the mammal is selected from the group consisting of cats, dogs, and horses.  
     
     
         30 . The method according to  claim 28  wherein the disease is characterized by an obstructive component or underlying inflammation.  
     
     
         31 . The method according to  claim 30  wherein the disease is asthma or chronic obstructive pulmonary disease (COPD).  
     
     
         32 . The method according to  claim 28  wherein an adult human is treated with a daily dosage of R,R glycopyrrolate between 5 and 500 □g/day and a daily dosage of glucocorticoid is between 100 to 1.600 μg/day.  
     
     
         33 . The method of  claim 32  wherein the daily dosage of R,R glycopyrrolate is 15 to 300 μg/day.  
     
     
         34 . The method of  claim 32  wherein the daily dosage of glucocorticoid is between 200 and 400 μg/day.  
     
     
         35 . The method according to  claim 28  wherein an adult human is treated with a dosage of R,R glycopyrrolate between 5 and 100 □g/day and a daily dosage of glucocorticoid between 100 to 1.600 μg/day.  
     
     
         36 . The method of  claim 35  wherein the dosage of glucocorticoid is between 200 and 400 μg/day.  
     
     
         37 . A method of producing a medicament for inhalative administration for the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD) comprising combining an anticholinergic with a glucocorticoid or their physiologically acceptable salts to obtain a medicament.