High drug load tablet

Abstract

The present invention pertains to a high drug load tablet comprising as active ingredient Compound I of formula or a pharmaceutically acceptable salt thereof in an amount from about 30% to 80% in weight of the active moiety based on the total weight of the tablet.

1 - 15 . (canceled)  
   
   
       16 . A tablet comprising a pharmacologically effective amount of Compound I of formula (1)  
     
       
         
         
             
             
         
       
     
     or a pharmaceutically acceptable salt thereof in an amount from about 30% to 80% in weight of the active moiety based on the total weight of the tablet.  
   
   
       17 . A tablet according to  claim 16  wherein Compound I of formula (1) or a pharmaceutically acceptable salt thereof is present in an amount from about 50% to 80% in weight of the active moiety based on the total weight of the tablet.  
   
   
       18 . A tablet according to  claim 17  wherein Compound I of formula (1) is in the monomesylate salt form.  
   
   
       19 . A tablet according to  claim 18  wherein Compound I of formula (1) monomesylate is in the beta crystal form thereof.  
   
   
       20 . A tablet according to  claim 16  wherein the tablet comprises one or more pharmaceutically acceptable excipients suitable for the preparation of tablets.  
   
   
       21 . A tablet according to  claim 20  wherein the excipient comprises at least one binder.  
   
   
       22 . A tablet according to  claim 20  wherein the excipients comprise: 
 at least one binder in a total amount of about 1% to 25% in weight based on the total weight of the tablet,    at least one disintegrant in a total amount of about 10% to 35% in weight based on the total weight of the tablet    at least one glidant in a total amount of about 0.5% to 3% in weight based on the total weight of the tablet, and/or    at least one lubricant in a total amount of about 0.5% to 2% in weight based on the total weight of the tablet.    
   
   
       23 . A tablet according to  claim 21  wherein the binder comprises microcrystalline cellulose or hydroxypropylmethyl cellulose or a mixture thereof.  
   
   
       24 . A tablet according to  claim 22  wherein the disintegrant comprises cross-linked polyvinylpyrrolidinone.  
   
   
       25 . A tablet according to  claim 22  wherein the glidant comprises colloidal silicon dioxide and/or colloidal anhydrous silica.  
   
   
       26 . A tablet according to  claim 22  wherein the lubricant comprises magnesium stearate.  
   
   
       27 . A process for the preparation of a tablet according to  claim 16 , which process comprises 
 (i) mixing the Compound I of formula (1) or pharmaceutically acceptable salts thereof and pharmaceutically acceptable excipients;    (ii) wet-granulating;    (iii) mixing with pharmaceutically acceptable excipients to form a mixture; and    (iv) compressing the mixture obtained in step (iii) to form a tablet.    
   
   
       28 . The process according to  claim 27  wherein the tablet is coated.  
   
   
       29 . A tablet according to  claim 16  prepared by a wet-granulation process.  
   
   
       30 . A method of treating a subject which comprises administering a tablet according to  claim 16  comprising a pharmacologically effective amount of Compound I of formula (1) to a subject in need of such a treatment.