Oral dosage form containing a pde 4 inhibitor as an active ingredient and polyvinylpyrrolidon as excipient

Abstract

Disclosed is a method of treatment of COPD by oral administration of roflumilast.

1 . A method for the treatment of chronic obstructive pulmonary disease (COPD), comprising:
 orally administering to a patient in need thereof a solid dosage form in tablet or pellet form of N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxybenzamide (roflumilast) or a salt thereof, and one or more suitable pharmaceutical excipients; and   wherein said dosage form provides about quantitative release of the roflumilast or salt thereof from said dosage form within about 60 minutes as determined by methods described in the US Pharmacopeia.   
     
     
         2 . The method of treatment according to  claim 1  wherein said dosage form contains 500 μg of roflumilast or salt thereof per dosage unit. 
     
     
         3 . The method of treatment according to  claim 3 , wherein said dosage form also contains polyvinylpyrrolidone as a binder. 
     
     
         4 . The method of treatment according to  claim 1 , wherein the PDE 4 inhibitor is roflumilast. 
     
     
         5 . The method of treatment according to  claim 1 , wherein the dosage form is a tablet. 
     
     
         6 . The method of treatment according to  claim 1 , wherein the dosage form is a tablet and the PDE4 inhibitor is roflumilast. 
     
     
         7 . The method of treatment according to  claim 1 , wherein the dosage form provides about quantitative release of the roflumilast or salt thereof from said dosage form within about 60 minutes as determined by the methods described in the US Pharmacopeia at USP XXV, apparatus 2. 
     
     
         8 . The method of treatment according to  claim 1 , wherein the dosage form provides at least about 78% release of the roflumilast or salt thereof from said dosage form within about 15 minutes as determined by methods described in the US Pharmacopeia. 
     
     
         9 . The method of treatment according to  claim 8 , wherein the dosage form provides at least about 78% release of the roflumilast or salt thereof from said dosage form within about 15 minutes as determined by the methods described in the US Pharmacopeia at USPP XXV, apparatus 2. 
     
     
         10 . The method of treatment according to  claim 1 , wherein the dosage form provides a plasma concentration of roflumilast having an AUC of more than about 35 μg/1× hr. 
     
     
         11 . The method of treatment according to  claim 1 , wherein the dosage form provides a plasma concentration of roflumilast having a Cmaxof more than about 6.5 μg/1. 
     
     
         12 . The method of treatment according to  claim 1 , wherein the dosage form provides a plasma concentration of roflumilast having an AUC of more than about 35 μg/1× hr and a Cmax of more than about 6.5 μg/1.