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Last Updated: April 25, 2024

Claims for Patent: 5,496,545


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Summary for Patent: 5,496,545
Title: 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.
Inventor(s): Holmes-Farley; Stephen R. (Arlington, MA), Mandeville, III; W. Harry (Lynnfield, MA), Whitesides; George M. (Newton, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Application Number:08/238,458
Patent Claims: 1. A method for removing phosphate from a patient by ion exchange 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 ##STR28## or a copolymer thereof, wherein n is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.

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 3 wherein said crosslinking agent comprises epichlorohydrin.

5. The method of claim 2 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

6. A method for removing phosphate from a patient by ion exchange 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 ##STR29## 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.sup.- is an exchangeable negatively charged counterion.

7. The method of claim 6 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.

8. The method of claim 7 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.

9. The method of claim 7 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

10. The method of claim 6 wherein the polymer is a copolymer comprising a second repeat unit having the formula ##STR30## wherein each n, independently, is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.

11. The method 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 method 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 method of claim 11 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

14. A therapeutic composition for removing phosphate from a patient by ion exchange comprising a therapeutically effective amount of at least one polymer characterized by a repeat unit having the formula ##STR31## or copolymer thereof, wherein n is an integer and each R, independently, is H or a lower alkyl, alkylamino, or aryl group.

15. The composition of claim 14 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.

16. The composition of claim 15 wherein said crosslinking agent comprises epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluene diisocyanate, acryloyl chloride, or pyromellitic dianhydride.

17. The composition of claim 16 wherein said crosslinking agent comprises epichlorohydrin.

18. The composition of claim 15 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

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