Phosphate-Binding Polymers for Oral Administration

Abstract

Phosphate-binding polymers are provided for removing phosphate from the gastrointestinal tract. The polymers are orally administered, and are useful for the treatment of hyperphosphatemia.

1 . A pharmaceutical composition comprising a carrier and a crosslinked, water insoluble polyallylamine homopolymer, wherein said polyallylamine homopolymer comprises repeat units represented by the structural formula: 
     
       
         
         
             
             
         
       
     
     wherein n is an integer, and wherein the homopolymer is fully protonated, partially protonated or unprotonated. 
   
   
       2 . The pharmaceutical composition of  claim 1 , wherein said polyallylamine homopolymer is crosslinked with an epichlorohydrin crosslinking agent. 
   
   
       3 . The pharmaceutical composition of  claim 2 , wherein the amount of said crosslinking agent is about 2% to about 20% by weight of the polymer. 
   
   
       4 . The pharmaceutical composition of  claim 1 , wherein said polyallylamine homopolymer is fully or partially protonated. 
   
   
       5 . The pharmaceutical composition of  claim 4 , wherein said polyallylamine homopolymer is protonated with HCl. 
   
   
       6 . The pharmaceutical composition of  claim 5 , wherein said polyallylamine homopolymer is partially protonated. 
   
   
       7 . The pharmaceutical composition of  claim 1 , wherein said pharmaceutical composition consists essentially of one or more carriers and said polyallylamine homopolymer. 
   
   
       8 . The pharmaceutical composition of  claim 1 , wherein said pharmaceutical composition consists of one or more carriers and said polyallylamine homopolymer. 
   
   
       9 . The pharmaceutical composition of  claim 1 , wherein said pharmaceutical composition is in the form of a tablet or a capsule. 
   
   
       10 . A method for removing phosphate from a patient, comprising orally administering to said patient a therapeutically effective amount of a composition comprising a crosslinked, water insoluble polyallylamine homopolymer, wherein said polyallylamine homopolymer comprises repeat units represented by the structural formula: 
     
       
         
         
             
             
         
       
     
     wherein n is an integer, and wherein the homopolymer is fully protonated, partially protonated or unprotonated. 
   
   
       11 . The method of  claim 10 , wherein said polyallylamine homopolymer is crosslinked with an epichlorohydrin crosslinking agent. 
   
   
       12 . The method of  claim 11 , wherein the amount of said crosslinking agent is about 2% to about 20% by weight of the polymer. 
   
   
       13 . The method of  claim 10 , wherein said polyallylamine homopolymer is fully or partially protonated. 
   
   
       14 . The method of  claim 13 , wherein said polyallylamine homopolymer is protonated with HCl. 
   
   
       15 . The method of  claim 14 , wherein said polyallylamine homopolymer is partially protonated.