Trospium containing compositions

Abstract

The invention relates to a method for treating a disease characterized by a constrictive airway comprising administering to a patient in need thereof via inhalation a pharmaceutical composition comprising trospium, wherein said patient achieves an effective therapy for at least 10 hours. The trospium composition is preferably a particulate formulation useful for administration via a dry powder inhaler. In a preferred embodiment, the composition further comprises a second active agent, such as a beta-2 agonist. A particularly preferred second active agent is formoterol, wherein the trospium, formoterol composition is manufactured by spray drying a mixture comprising trospium and formoterol.

1 . A method for treating a disease characterized by a constrictive airway comprising administering to a patient in need thereof via inhalation a pharmaceutical composition comprising trospium, wherein said patient achieves an effective therapy for at least 10 hours.  
     
     
         2 . The method of  claim 1  wherein said disease is chronic obstructive pulmonary disease.  
     
     
         3 . The method of  claim 1  wherein said composition comprises a dose of trospium of between about 50 to 1200 micrograms.  
     
     
         4 . The method of  claim 1  wherein said composition comprises a dose of trospium of between about 200 to 800 mcg.  
     
     
         5 . The method of  claim 1  wherein said composition comprises an aqueous solution of trospium hydrochloride.  
     
     
         6 . The method of  claim 1  wherein said composition comprises a particulate formulation comprising trospium.  
     
     
         7 . The method of  claim 1  wherein said composition comprises a dry particulate formulation of trospium wherein said formulation is administered with a dry powder inhaler.  
     
     
         8 . The method of  claim 1  wherein said composition comprises a dry particulate formulation of trospium characterized by a fine particle fraction of at least 50% and wherein said formulation is administered with a dry powder inhaler.  
     
     
         9 . The method of  claim 8  wherein said trospium formulation comprises micronized trospium.  
     
     
         10 . The method of  claim 8  wherein said trospium formulation comprises spray dried trospium.  
     
     
         11 . The method of  claim 10  wherein said trospium formulation has a tap density of less than 0.4 g/cm 3 .  
     
     
         12 . The method of  claim 11  wherein said trospium formulation has a mass mean aerodynamic diameter of less than 5 microns.  
     
     
         13 . The method of  claim 12  wherein said trospium formulation further comprises leucine, a phospholipid or combinations thereof.  
     
     
         14 . The method of  claim 13  wherein said formulation comprises at least about 70% by weight of leucine.  
     
     
         15 . The method of  claim 14  wherein said formulation contains less than about 10% by weight of trospium.  
     
     
         16 . The method of  claim 14  wherein said formulation comprises about 5% by weight trospium hydrochloride; between about 5 and 10% by weight of phospholipid and between about 85 and 90% by weight of leucine.  
     
     
         17 . The method of  claim 16  wherein the dose of trospium administered is about 50 to 1200 mcg.  
     
     
         18 . The method of  claim 16  wherein the dose of trospium administered is about 200 to 800 mcg.  
     
     
         19 . The method of  claim 17  wherein the patient achieves an effective therapy for at least about 15 hours.  
     
     
         20 . The method of  claim 17  wherein the patient achieves an effective therapy for at least about 24 hours.  
     
     
         21 . The method of  claim 8  wherein the formulation is administered once per day.  
     
     
         22 . The method of  claim 1  further comprising the administration of a second active agent.  
     
     
         23 . The method of  claim 22  wherein the second active agent is a beta-2 agonist.  
     
     
         24 . The method of  claim 23  wherein the second active agent is formoterol.  
     
     
         25 . The method of  claim 23  wherein the second active agent is administered separately from the trospium formulation.  
     
     
         26 . The method of  claim 24  wherein the second active agent is incorporated into the trospium formulation.  
     
     
         27 . The method of  claim 24  wherein the composition comprises a spray dried formulation comprising trospium, formoterol, leucine and, optionally, a phospholipid.  
     
     
         28 . A pharmaceutical composition for inhalation comprising trospium and formoterol.