Solid pharmaceutical composition comprising telithromycin

Abstract

The invention relates to a novel solid pharmaceutical composition of telithromycin which facilitates swallowing by the patient.

1 . A solid pharmaceutical composition comprising telithromycin or an addition salt thereof with a pharmaceutically acceptable acid, as an active ingredient, which consists of:
 between about 0.1 and 80% by weight of telithromycin or an addition salt thereof with a pharmaceutically acceptable acid, and   about 10 to 50% by weight of at least one diluent having a plastic behavior.   
     
     
         2 . The composition of  claim 1 , which also comprises:
 about 2.5 to 3.5% by weight of at least one binder,   about 3 to 8% by weight of at least one disintegrating agent, and   about 0.6 to 1% by weight of at least one lubricant.   
     
     
         3 . The composition of  claim 1 , which comprises:
 between about 50 and 80% by weight of telithromycin or an addition salt thereof with a pharmaceutically acceptable acid,   about 20 to 30% by weight of at least one diluent having a plastic behavior, and   about 2.8 to 3% by weight of at least one binder,   about 3.5 to 6% by weight of at least one disintegrating agent, and   about 0.6 to 1% by weight of at least one lubricant.   
     
     
         4 . The composition of  claim 1 , wherein the diluent having a plastic behavior is microcrystalline cellulose. 
     
     
         5 . The composition of  claim 2 , wherein:
 the binder is selected from the group consisting of povidone K25, povidone K30, copovidone, hydroxypropylcellulose, and mixtures thereof,   the disintegrating agent is selected from the group consisting of sodium croscarmellose, crospovidone, sodium carboxymethyl starch, and mixtures thereof, and   the lubricant is selected from the group consisting of magnesium stearate, micronized stearic acid, and mixtures thereof.   
     
     
         6 . The composition of  claim 2 , wherein:
 the binder is selected from the group consisting of povidone K25, povidone K30, and mixtures thereof,   the disintegrating agent is sodium croscarmellose, and   the lubricant is magnesium stearate.   
     
     
         7 . The composition of  claim 1 , which comprises:
 from about 60 to 70% by weight of telithromycin,   from about 20 to 30% by weight of microcrystalline cellulose,   from about 2.8 to 3% by weight of a povidone selected from the group consisting of povidone K25, povidone K30, and mixtures thereof,   from about 3.5 to 6% by weight of sodium croscarmellose, and   from about 0.6 to 1% by weight of magnesium stearate.   
     
     
         8 . The composition of  claim 1 , which is in the form of a tablet. 
     
     
         9 . The composition of  claim 8  wherein the tablet is coated with a film-coating. 
     
     
         10 . The composition of  claim 9 , wherein said film-coating comprises at least one component selected from the group consisting of hypromellose, polyethylene glycol, titanium dioxide, talc, yellow iron oxide, red iron oxide, and mixtures thereof. 
     
     
         11 . The composition of  claim 1 , which comprises from about 50 mg to 600 mg of telithromycin. 
     
     
         12 . The composition of  claim 11 , which comprises about 400 mg of telithromycin. 
     
     
         13 . The composition of  claim 12 , which comprises about 300 mg of telithromycin.