Novel Process

Abstract

The invention relates to a stable pharmaceutical composition useful in the treatment of respiratory disorders such as asthma, rhinitis and chronic obstructive pulmonary disease (COPD) and a novel micronisation process for manufacturing a stable formulation for formoterol or its enantiomers and a carrier/diluent comprising a carbohydrate such as lactose.

1 . A process for preparing a pharmaceutical composition comprising, in admixture, an active ingredient which is micronised formoterol or an enantiomer thereof, optionally in the form of a salt or solvate of a salt, and a micronised carrier/diluent, which process comprises
 preparing a mixture of micronised active ingredient and carrier/diluent,   followed by addition of further pre-micronised carrier/diluent which is mixed in at low energy, and   either subjecting the mixture to agglomeration and spheronisation, or adding coarse carrier/diluent.   
   
   
       2 . A process according to  claim 1  in which formoterol is in the form of its fumarate dihydrate salt. 
   
   
       3 . A process according to  claim 1  or  2  in which the formoterol is in the form of the single R,R-enantiomer. 
   
   
       4 . A process according to any one of  claims 1  to  3  in which the carrier is a coarse carbohydrate. 
   
   
       5 . A process according to any of  claims 1  to  4  in which the carrier is lactose. 
   
   
       6 . A pharmaceutical composition comprising, in admixture, an active ingredient which is micronised formoterol optionally in the form of a salt or solvate or a solvate of a salt, and a micronised pharmaceutically acceptable carrier/diluent, the composition having a high storage stability. 
   
   
       7 . A pharmaceutical composition according to  claim 6  in which formoterol is in the form of its fumarate dihydrate salt. 
   
   
       8 . A pharmaceutical composition according to  claims 6  and  7  in which the formoterol is in the form of the single R,R-enantiomer. 
   
   
       9 . A pharmaceutical composition according to any one of  claims 6  to  8  in which the carrier/diluent is lactose. 
   
   
       10 . A pharmaceutical composition according to any one of  claims 6  to  9  in which the particle size of the formoterol is less than 10 um. 
   
   
       11 . A pharmaceutical composition according to any one of  claims 6  to  10  for use for the treatment or prophylaxis of a respiratory disorder. 
   
   
       12 . A pharmaceutical composition according to any one of  claims 6  to  11  for use for the treatment or prophylaxis of asthma, rhinitis or COPD. 
   
   
       13 . A method of treating a respiratory disorder in a mammal which comprises administering to a patient a pharmaceutical composition according to any one of  claims 6  to  12 .