Method of making phosphate-binding polymers for oral administration
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 method for removing phosphate from a patient comprising orally administering to said patient a therapeutically effective amount of a composition comprising at least one polymer characterized by a repeat unit having the formula:
or a copolymer thereof, wherein each n is an integer, each R, independently, is H or a lower alkyl, alkylamino, or aryl group, and each X − is a carbonate or bicarbonate anion.
2. The method of claim 1 wherein said polymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.
3. The method of claim 2 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.
4. The method of claim 2 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.
5. The method of claim 1 wherein the polymer is a copolymer comprising a second repeat unit having the formula:
wherein each n, independently, is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.
6. The method of claim 5 wherein said copolymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.
7. The method of claim 6 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.
8. The method of claim 6 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.
9. A method for removing phosphate from a patient comprising orally administering to said patient a therapeutically effective amount of a composition comprising a copolymer characterized by a repeat unit having the formula:
and a second repeat unit having the formula:
wherein said copolymer is crosslinked with epichlorohydrin, wherein epichlorohydrin is present in said composition from about 2% to about 20% by weight and wherein each n is an integer, each R is H, and each X − 0 is a carbonate or bicarbonate anion.
10. A pharmaceutical composition comprising a carrier and a therapeutically effective amount of at least one polymer characterized by a repeat unit having the formula:
or a copolymer thereof, wherein each n is an integer, each R, independently, is H or a lower alkyl, alkylamino, or aryl group, and each X − is a carbonate or bicarbonate anion.
11. The pharmaceutical composition of claim 10 wherein said polymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.
12. The pharmaceutical composition of claim 11 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.
13. The pharmaceutical composition of claim 11 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.
14. The pharmaceutical composition of claim 10 wherein the polymer is a copolymer comprising a second repeat unit having the formula:
wherein each n, independently, is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.
15. The pharmaceutical composition of claim 14 wherein said copolymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 0.5% to about 75% by weight.
16. The pharmaceutical composition of claim 15 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.
17. The pharmaceutical composition of claim 15 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.
18. A pharmaceutical composition comprising a carrier and a therapeutically effective amount of a copolymer characterized by a repeat unit having the formula:
and a second repeat unit having the formula:
wherein said copolymer is crosslinked with epichlorohydrin, wherein epichlorohydrin is present in said composition from about 2% to about 20% by weight and wherein each n is an integer, each R is H, and each X − is a carbonate or bicarbonate anion.