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 : 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. 
       
     
     
         2 : A tablet according to  claim 1  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. 
     
     
         3 : A tablet according to  claim 2  wherein Compound I of formula (1) is in the monomesylate salt form. 
     
     
         4 : A tablet according to  claim 3  wherein Compound I of formula (1) monomesylate is in the beta crystal form thereof. 
     
     
         5 : A tablet according to  claim 1  wherein the tablet comprises one or more pharmaceutically acceptable excipients suitable for the preparation of tablets. 
     
     
         6 : A tablet according to  claim 5  wherein the excipient comprises at least one binder. 
     
     
         7 : A tablet according to  claim 5  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. 
 
     
     
         8 : A tablet according to  claim 6  wherein the binder comprises microcrystalline cellulose or hydroxypropylmethyl cellulose or a mixture thereof. 
     
     
         9 : A tablet according to  claim 7  wherein the disintegrant comprises cross-linked polyvinylpyrrolidinone. 
     
     
         10 : A tablet according to  claim 7  wherein the glidant comprises colloidal silicon dioxide and/or colloidal anhydrous silica. 
     
     
         11 : A tablet according to  claim 7  wherein the lubricant comprises magnesium stearate. 
     
     
         12 : A process for the preparation of a tablet according to  claim 1 , which process comprises
 (i) mixing the Compound I of formula (I) 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.   
     
     
         13 : The process according to  claim 12  wherein the tablet is coated. 
     
     
         14 : A tablet according to  claim 1  prepared by a wet-granulation process. 
     
     
         15 : A method of treating a subject which comprises administering a tablet according to  claim 1  comprising a pharmacologically effective amount of Compound I of formula (1) to a subject in need of such a treatment.