Composition

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.

What is claimed is: 
     
         1 . A pharmaceutical composition, in the form of an oral dosage form, the composition comprising licarbazepine acetate in combination with a binder and a disintegrant, wherein the composition comprises granules of the licarbazepine acetate, and wherein at least part of the disintegrant is intragranular and at least part of the disintegrant is extragranular. 
     
     
         2 . The pharmaceutical composition of  claim 1  wherein the composition comprises a total amount of disintegrant of about 0.5 to about 70 wt %. 
     
     
         3 . The pharmaceutical composition of  claim 1  wherein about 20 to about 80 wt % of the total amount of disintegrant is present in the granules. 
     
     
         4 . The pharmaceutical composition of  claim 1  wherein the disintegrant is croscarmellose sodium, crospovidone, low substituted hydroxypropyl cellulose, microcrystalline cellulose, carboxymethyl cellulose sodium, carboxymethylcellulose calcium, sodium starch glycolate, or a mixture of one or more thereof. 
     
     
         5 . The pharmaceutical composition of  claim 1  wherein the composition comprises about to 0.5 to about 70 wt % binder. 
     
     
         6 . The pharmaceutical composition of  claim 1  wherein the binder is povidone, hypromellose, hydroxypropyl cellulose, methyl-cellulose, ethyl-cellulose, pregelatinized maize starch or gelatine, or a mixture of one or more thereof. 
     
     
         7 . The pharmaceutical composition of  claim 1  wherein the licarbazepine acetate is eslicarbazepine acetate. 
     
     
         8 . A pharmaceutical preparation comprising licarbazepine acetate in combination with a binder and a disintegrant, wherein the preparation has a bulk density of at least about 0.3g/mL. 
     
     
         9 . The pharmaceutical preparation of  claim 8  wherein the licarbazepine acetate is present in granules. 
     
     
         10 . The pharmaceutical preparation of  claim 8  wherein the licarbazepine acetate is eslicarbazepine acetate. 
     
     
         11 . A pharmaceutical composition manufactured from a preparation of  claim 8 . 
     
     
         12 . The pharmaceutical composition of  claim 11  wherein part of the disintegrant is present in the granules and the remaining part of the disintegrant is extragranular. 
     
     
         13 . The pharmaceutical composition of  claim 11  wherein the composition is a tablet. 
     
     
         14 . A pharmaceutical composition of  claim 11  wherein the composition has an apparent density of about 0.5 to about 1.5 g/mL. 
     
     
         15 . A method of preparing a pharmaceutical oral dosage form, the method comprising the following steps:
 mixing licarbazepine acetate with a pharmaceutically acceptable granulation liquid;   forming granules from the licarbazepine acetate and the granulation liquid;   optionally mixing the granules with one or more pharmaceutically suitable excipients to form a preparation; and   forming an oral dosage form.   
     
     
         16 . The method of  claim 15  wherein the licarbazepine acetate has a bulk density of about 0.25 to about 0.4 g/mL prior to the granule forming step and wherein the preparation has a bulk density of at least about 0.4 g/mL prior to forming the oral dosage form. 
     
     
         17 . The method of  claim 15  wherein the oral dosage form is a tablet. 
     
     
         18 . The method of  claim 15  wherein the oral dosage form has an apparent density of about 0.5 to about 1.5 g/mL. 
     
     
         19 . A method of preparing a pharmaceutical oral dosage form, the method comprising the following steps:
 mixing licarbazepine acetate with at least one excipient including part of the total amount of binder;   dissolving or dispersing the remaining proportion of the total amount of the binder in a suitable granulation liquid;   granulating the mixture from the mixing step using the granulation liquid produced in the dissolving or dispersing step to produce granules;   optionally contacting the granules with at least one excipient to form a preparation, and   optionally forming an oral dosage form.   
     
     
         20 . A pharmaceutical composition obtainable by a method of  claim 15 . 
     
     
         21 . A pharmaceutical composition obtainable by a method of  claim 19 .