Pharmaceutical composition comprising licarbazepine acetate

Abstract

A pharmaceutical composition comprising licarbazepine acetate, especially eslicarbazepine acetate, in combination with suitable excipients, in particular a binder, and a disintegrant. Also disclosed is a granulation process, especially a wet granulation process, for making the pharmaceutical composition.

1 .- 73 . (canceled) 
     
     
         74 . A pharmaceutical composition comprising eslicarbazepine acetate in combination with a binder and a disintegrant, wherein eslicarbazepine acetate is present in an amount of from about 82 to about 89 wt %, the binder is present in an amount of from about 5 to about 8 wt %, and the disintegrant is present in an amount of from about 5 to about 8 wt %. 
     
     
         75 . The pharmaceutical composition of  claim 74 , wherein the binder is povidone, hypromellose, hydroxypropyl cellulose, methyl-cellulose, pregelatinized maize starch or gelatine, or a combination thereof. 
     
     
         76 . The pharmaceutical composition of  claim 75 , wherein the binder comprises povidone. 
     
     
         77 . The pharmaceutical composition of  claim 74 , wherein the disintegrant is croscarmellose sodium, crospovidone, low substituted hydroxypropyl cellulose, microcrystalline cellulose, carboxymethyl cellulose sodium, carboxymethylcellulose calcium, sodium starch glycolate, or a combination thereof. 
     
     
         78 . The pharmaceutical composition of  claim 77 , wherein the disintegrant comprises croscarmellose sodium. 
     
     
         79 . The pharmaceutical composition of  claim 74 , further comprising a lubricant. 
     
     
         80 . The pharmaceutical composition of  claim 79 , wherein the lubricant is present in an amount of from about 1 to about 3 wt %. 
     
     
         81 . The pharmaceutical composition of  claim 79 , wherein the lubricant is magnesium stearate, sodium lauryl sulphate, or a combination thereof. 
     
     
         82 . The pharmaceutical composition of  claim 81 , wherein the lubricant comprises magnesium stearate. 
     
     
         83 . The pharmaceutical composition of  claim 74 , wherein the pharmaceutical composition is prepared by a wet granulation process and comprises granules of eslicarbazepine acetate. 
     
     
         84 . The pharmaceutical composition of  claim 83 , wherein the disintegrant is intragranular or extragranular. 
     
     
         85 . The pharmaceutical composition of  claim 83 , wherein at least part of the disintegrant is intragranular and at least part of the disintegrant is extragranular. 
     
     
         86 . The pharmaceutical composition of  claim 85 , wherein from about 20 to about 80 wt % of the total amount of the disintegrant is present in the granules. 
     
     
         87 . The pharmaceutical composition of  claim 85 , wherein from about 40 to about 60 wt % of the total amount of the disintegrant is in the granules. 
     
     
         88 . The pharmaceutical composition of  claim 85 , wherein from about 45 to about 55 wt % of the total amount of the disintegrant is in the granules. 
     
     
         89 . The pharmaceutical composition of  claim 85 , wherein about 50 wt % of the total amount of the disintegrant is in the granules. 
     
     
         90 . The pharmaceutical composition of  claim 74 , wherein the pharmaceutical composition exhibits a dissolution of at least 60% at about 30 minutes at a temperature of 37±0.5° C. and a pH of about 4.5 using a paddle apparatus at a speed of about 100 rpm. 
     
     
         91 . The pharmaceutical composition of  claim 74 , wherein the pharmaceutical composition has an apparent density of from about 0.5 to about 1.5 g/mL. 
     
     
         92 . The pharmaceutical composition of  claim 74 , wherein the pharmaceutical composition is in an oral dosage form. 
     
     
         93 . The pharmaceutical composition of  claim 92 , wherein the oral dosage form is a tablet or capsule.