Controlled release tramadol formulations

Abstract

A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.

1 - 41 . (canceled)  
   
   
       42 . A solid controlled release oral dosage form, comprising: 
 a therapeutically effective amount of tramadol or a pharmaceutically acceptable salt thereof incorporated into a controlled release matrix, said controlled release matrix comprising an alkylcellulose or an acrylic resin or a mixture thereof;    said dosage form providing a therapeutic effect for at least about 24 hours.    
   
   
       43 . The controlled release dosage form as claimed in  claim 42 , wherein said controlled release matrix comprises a polymethacrylate.  
   
   
       44 . The controlled release dosage form as claimed in  claim 42 , wherein said controlled release matrix comprises a water insoluble cellulose.  
   
   
       45 . The controlled release dosage form as claimed in  claim 43 , wherein said controlled release matrix further comprises a water soluble cellulose.  
   
   
       46 . The controlled release dosage form as claimed in  claim 44 , wherein said controlled release matrix further comprises a polyvinylpyrrolidone.  
   
   
       47 . The controlled release dosage form as claimed in  claim 42 , comprising from about 50 to 800 mg of tramadol or a pharmaceutically acceptable salt thereof, calculated as the hydrochloride salt.  
   
   
       48 . The controlled release dosage form as claimed in  claim 42 , having a dissolution rate in-vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0.1N hydrochloric acid at 37° C. and using UV detection at 270 nm, from about 0 to about 50% tramadol released after 1 hour; from about 0 to about 75% tramadol released after 2 hours; from about 10 to about 95% tramadol released after 4 hours; from about 35 to about 100% after 8 hours; from about 55 to about 100% tramadol released after 12 hours; from about 70 to about 100% tramadol released after 16 hours; and greater than 90% tramadol released after 24 hours, by weight.  
   
   
       49 . The controlled release dosage form as claimed in  claim 42 , having a dissolution rate in-vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0.1N hydrochloric acid at 37° C. and using UV detection at 270 nm, from about 0 to about 30% tramadol released after 1 hour; from about 0 to about 40% tramadol released after 2 hours; from about 3 to about 55% tramadol released after 4 hours; from about 10 to about 65% after 8 hours; from about 20 to about 75% tramadol released after 12 hours; from about 30 to about 88% tramadol released after 16 hours; from about 50 to about 100% tramadol released after 24 hours and greater than 80% tramadol released after 36 hours, by weight.  
   
   
       50 . The controlled release dosage form as claimed in  claim 42 , having a dissolution rate in-vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0.1N hydrochloric acid at 37° C. and using UV detection at 270 nm, from about 15 to about 25% tramadol released after 1 hour; from about 25 to about 35% tramadol released after 2 hours; from about 30 to about 45% tramadol released after 4 hours; from about 40 to about 60% after 8 hours; from about 55 to about 70% tramadol released after 12 hours; and from about 60 to about 75% tramadol released after 16 hours, by weight.  
   
   
       51 . The dosage form according to  claim 42 , which provides a T max  from about 3 to about 6 hours.  
   
   
       52 . The dosage form according to  claim 42 , which provides a W 50  from about 10 to about 33 hours.  
   
   
       53 . The dosage form according to  claim 44  wherein said water insoluble cellulose comprises ethylcellulose.  
   
   
       54 . The dosage form of  claim 42 , comprising 100 mg tramadol hydrochloride.  
   
   
       55 . The dosage form of  claim 42 , comprising 200 mg tramadol hydrochloride.  
   
   
       56 . The dosage form of  claim 42 , comprising 300 mg tramadol hydrochloride.  
   
   
       57 . The dosage form of  claim 42 , comprising 400 mg tramadol hydrochloride.  
   
   
       58 . The dosage form of  claim 42 , comprising 600 mg tramadol hydrochloride.  
   
   
       59 . The dosage form of  claim 42 , further comprising a coating.  
   
   
       60 . The dosage form of  claim 59 , wherein the coating is a film coating.  
   
   
       61 . The dosage form of  claim 42 , wherein said controlled release matrix is in a form of multiparticulates.