Stabilized lanthanum carbonate compositions

Abstract

Stabilized lanthanum carbonate compositions containing a monosaccharide or disaccharide stabilizing agent are disclosed. Subjects having hyperphosphatemia can be treated by administering a pharmaceutical composition containing a therapeutically effective amount of the stabilized lanthanum carbonate formulation.

1 . A stabilized lanthanum carbonate composition comprising lanthanum carbonate having the general formula:
   La 2 (CO 3 ) 3 .xH 2 O   
       wherein x has a value from 0 to 10, in an amount effective to treat hyperphosphatemia, and at least one pharmaceutically acceptable monosaccharide or disaccharide stabilizer in an amount sufficient to stabilize lanthanum carbonate against substantial decarboxylation to lanthanum hydroxycarbonate, wherein the monosaccharide or disaccharide is sucrose, glucose, galactose, fructose, dextrose, ribose, maltose, sorbitol, xylitol, mannitol, lactose, dextrates, or a mixture thereof and is present in an amount of from about 20% to about 80% by weight based on the total weight of the composition. 
     
     
         2 . The stabilized composition of  claim 1 , wherein the monosaccharide or disaccharide is dextrates, which is present in an amount of from about 40% to about 80% by weight based on the total weight of the composition. 
     
     
         3 . The stabilized composition of  claim 1 , further comprising a lubricant. 
     
     
         4 . The stabilized composition of  claim 3 , wherein the lubricant is magnesium stearate, talc, polyethylene glycol, silica, colloidal anhydrous silica, colloidal silicon dioxide, hydrogenated vegetable oil, glyceryl behenate or glyceryl monostearate. 
     
     
         5 . The stabilized composition of  claim 3 , further comprising a glidant. 
     
     
         6 . The stabilized composition of  claim 5 , wherein the glidant is silica, colloidal anhydrous silica, colloidal silicon dioxide, or talc. 
     
     
         7 . The stabilized composition of  claim 6 , comprising the following ingredients: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Ingredient 
                   % by weight 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   lanthanum carbonate 
                   26.5 
                 
                     
                   dextrates 
                   69.3 
                 
                     
                   colloidal silicon dioxide 
                   2 
                 
                     
                   talc 
                   1.7 
                 
                     
                   magnesium stearate 
                   0.5 
                 
                     
                     
                 
             
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
               
            
           
         
       
       wherein the lanthanum carbonate is hydrated having a water content approximately equivalent to 4-5 moles of water. 
     
     
         8 . The stabilized composition of  claim 6 , comprising the following ingredients: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Ingredient 
                   % by weight 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   lanthanum carbonate 
                   63.6 
                 
                     
                   colloidal silicon dioxide 
                   2 
                 
                     
                   talc 
                   1 
                 
                     
                   sorbitol 
                   30.4 
                 
                     
                   glyceryl dibehenate 
                   3.0 
                 
                     
                     
                 
             
                
                
                
               
               
                
               
            
             
                
                
                
                
                
                
               
            
           
         
       
       wherein the lanthanum carbonate is hydrated having a water content approximately equivalent to 4-5 moles of water. 
     
     
         9 . The stabilized composition of  claim 6 , comprising the following ingredients: 
       
         
           
                 
                 
                 
               
                     
                     
                 
                     
                   Ingredient 
                   % by weight 
                 
                     
                     
                 
                     
                 
                 
                 
                 
               
                     
                   lanthanum carbonate 
                   45.8 
                 
                     
                   dextrates 
                   51.1 
                 
                     
                   colloidal silicon dioxide 
                   2.1 
                 
                     
                   magnesium sterate 
                   1.0 
                 
                     
                     
                 
             
                
                
                
               
               
                
               
            
             
                
                
                
                
                
               
            
           
         
       
       wherein the lanthanum carbonate is hydrated having a water content approximately equivalent to 4-5 moles of water.