Sustained release oral formulations

Abstract

Pharmaceutical composition capable of releasing a therapeutically effective dose of active agent, e.g., rivastigmine, in a time-controlled manner.

1 - 21 . (canceled)  
     
     
         22 . A composition according to  claim 32  comprising coated particles:  
     
     
         23 . A composition according to  claim 32  comprising coated pellets.  
     
     
         24 . A composition according to  claim 22  wherein the coating comprises a cellulose derivative.  
     
     
         25 . A composition according to  claim 24  wherein the cellulose derivative comprises ethyl cellulose and hydroxypropyl methylcellulose.  
     
     
         26 . A pharmaceutical composition according to  claim 32  wherein revastigmine is in a hydrophilic swellable substance.  
     
     
         27 . A pharmaceutical composition according to  claim 26  wherein the hydrophilic swellable substance comprises hydroxypropylmethylcellulose 100,000 cps.  
     
     
         28 . A pharmaceutical oral controlled release tablet composition comprising revastigmine having the following release characteristic in water or artificial stomach juices:  
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                     
                 
                     
                   time (minutes) 
                   amount (percentage) 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   30 
                   28-35 
                 
                     
                   60 
                   40-55 
                 
                     
                   120 
                   58-75 
                 
                     
                   180 
                   70-90 
                 
                     
                   240 
                   80-95 
                 
                     
                   300 
                   88-98 
                 
                     
                   360 
                   >92 
                 
                     
                     
                 
                     
                     
                 
             
                
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
                
                
                
               
            
           
         
       
     
     
         29 . A pharmaceutical oral controlled release tablet composition comprising revastigmine wherein in use 60 to 90% of said rivastigmine is released in artificial stomach juices within 3 hours.  
     
     
         30 . Use of rivastigmine and excipients as defined in claim  1  in the manufacture of a medicament for the treatment of patients with mild to moderately severe Dementia of the Alzheimer's type by oral administration.  
     
     
         31 . A pharmaceutical composition comprising a core coated with two films, the first inner film being a semi-permeable to water or body fluids film applied directly on said core and comprising cellulose acetate, the second outer film being a permeable to water or body fluids film comprising ethylcellulose.  
     
     
         32 . A pharmaceutical oral controlled release tablet composition comprising revastigmine wherein in use 50% to 80% of said rivastigmine is released in artificial stomach juices within 3 hours.  
     
     
         33 . A composition according to  claim 23  wherein the coating comprises a cellulose derivative.  
     
     
         34 . A composition according to  claim 33  wherein the cellulose derivative comprises ethyl cellulose and hydroxypropyl methylcellulose.