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Claims for Patent: 6,509,013

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Claims for Patent: 6,509,013

Title: Method of making 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 Randall (Arlington, MA), Mandeville, III; W. Harry (Lynnfield, MA), Whitesides; George M. (Newton, MA)
Assignee: GelTex Pharmaceuticals, Inc. (Waltham, MA)
Application Number:09/542,329
Patent Claims: 1. A pharmaceutical composition consisting essentially of a carrier and at least one water insoluble, crosslinked polymer characterized by a repeat unit having the formula ##STR28##

or a copolymer thereof, wherein each n is an integer, each R, independently, is H or an alkyl, alkylamino, or aryl group optionally substituted with a quaternary ammonium, primary alkyl amine, secondary alkyl amine, primary aryl amine, secondary aryl amine, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea, or carboxylic acid ester group, or a combination thereof.

2. The pharmaceutical composition of claim 1 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight.

3. The pharmaceutical composition of claim 2 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

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

5. The pharmaceutical composition of claim 1 wherein the polymer is a copolymer comprising a second repeat unit having the formula ##STR29##

wherein each n, independently, is an integer and each R, independently, is H or a substituted or unsubstituted alkyl, alkylamino, or aryl group and each X.sup.- is an exchangeable negatively charged counterion.

6. The pharmaceutical composition of claim 5 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.

7. The pharmaceutical composition of claim 6 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

8. The pharmaceutical composition of claim 6 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

9. A pharmaceutical composition comprising a carrier and at least one water insoluble, crosslinked polymer characterized by a repeat unit having the formula ##STR30##

or a copolymer thereof, wherein n is an integer, each R, independently, is H or an alkyl, alkylamino, or aryl group optionally substituted with a quaternary ammonium, primary alkyl amine, secondary alkyl amine, primary aryl amine, secondary aryl amine, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl; aryl, hydrazine, guanidine, urea, or carboxylic acid ester group, or a combination thereof.

10. The pharmaceutical composition of claim 9 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight.

11. The pharmaceutical composition of claim 10 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

12. 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 2% to about 20% by weight.

13. The pharmaceutical composition of claim 9 wherein the polymer is a copolymer comprising a second repeat unit having the formula ##STR31##

wherein each n, independently, is an integer and R is a substituted or unsubstituted alkyl, alkylamino, or aryl group and each X.sup.- is an exchangeable negatively charged counterion.

14. The pharmaceutical composition of claim 13 wherein said polymer is crosslinked with a crosslinking agent wherein said crosslinking agent is present in said composition from about 1% to about 75% by weight.

15. The pharmaceutical composition of claim 14 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin, 1,4 butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

16. The pharmaceutical composition of claim 14 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

17. A pharmaceutical composition comprising a carrier and at least one water insoluble, crosslinked polymer characterized by a repeat unit having the formula ##STR32##

or a copolymer thereof, wherein n is an integer, and each R.sub.1 and R.sub.2, independently, is H or an alkyl, alkylamino, or aryl group optionally substituted with a quaternary ammonium, primary alkyl amine, secondary alkyl amine, primary aryl amine, secondary aryl amine, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea, or carboxylic acid ester group, or a combination thereof, and each X.sup.- is an exchangeable negatively charged counterion.

18. The pharmaceutical composition of claim 17 wherein at least one of said R groups is a hydrogen group.

19. The pharmaceutical composition of claim 17 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% weight.

20. The pharmaceutical composition of claim 19 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin 1,4-butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

21. The pharmaceutical composition of claim 19 wherein said polymer is crosslinked with a crosslinking agent, wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

22. A pharmaceutical composition comprising a carrier and at least one water insoluble, crosslinked polymer characterized by a repeat unit having the formula ##STR33##

or a copolymer thereof, wherein n is an integer, each R.sub.1 and R.sub.2, independently, is H or an alkyl group containing 1 to 20 carbon atoms optionally substituted with a quaternary ammonium, primary alkyl amine, secondary alkyl amine, primary aryl amine, secondary aryl amine, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea, or carboxylic acid ester group, or a combination thereof.

23. The pharmaceutical composition of claim 22 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight.

24. The pharmaceutical composition of claim 23 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin 1,4-butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

25. The pharmaceutical composition of claim 23 wherein said polymer is crosslinked with a crosslinking agent, wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

26. A pharmaceutical composition comprising a carrier and at least one water insoluble, crosslinked polymer characterized by a repeat unit having the formula ##STR34##

or a copolymer thereof, wherein n is an integer, each R.sub.1, R.sub.2 and R.sub.3, independently, is H, an alkyl group containing 1 to 20 carbon atoms, an aminoalkyl group, or an aryl group containing 1 to 12 atoms, each of which are optionally substituted with a quaternary ammonium, primary alkyl amine, secondary alkyl amine, primary aryl amine, secondary aryl amine, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea, or carboxylic acid ester group, or a combination thereof, and each X.sup.- is an exchangeable negatively charged counterion.

27. The pharmaceutical composition of claim 16 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight.

28. The pharmaceutical composition of claim 19 wherein said crosslinking agent is selected from the group consisting of epichlorohydrin 1,4-butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence duisocyanate, acryloyl chloride, and pyromellitic dianhydride.

29. The pharmaceutical composition of claim 27 wherein said polymer is crosslinked with a crosslinking agent, wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

30. A pharmaceutical composition comprising at least one hydrophilic, water insoluble, cross-linked aliphatic amine polymer and a pharmaceutically acceptable carrier or diluent.

31. A pharmaceutical composition consisting essentially of a carrier and at least one crosslinked, water insoluble polymer characterized by a repeat unit having the formula ##STR35##

or a copolymer thereof, wherein each n is an integer, each R, independently, is H or a alkyl, alkylamino, or aryl group optionally substituted with a quaternary ammonium, primary alkyl amine, secondary alkyl amine, primary aryl amine, secondary aryl amine, hydroxy, alkoxy, carboxamide, sulfonamide, halogen, alkyl, aryl, hydrazine, guanidine, urea, or carboxylic acid ester group, or a combination thereof, and each X.sup.- is an exchangeable negatively charged counterion.

32. The pharmaceutical composition of claim 31 wherein said polymer is crosslinked with a crosslinking agent, wherein said agent is present in said composition from about 0.5% to about 75% by weight.

33. The pharmaceutical composition of claim 32 wherein said crosslinking agent is selected from the group consisting of epichlofohydrin, 1,4 butanedioldiglycidyl ether, 1,2-ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate, toluence diisocyanate, acryloyl chloride, and pyromellitic dianhydride.

34. The pharmaceutical composition of claim 32 wherein said crosslinking agent is present in said composition from about 2% to about 20% by weight.

35. A pharmaceutical composition consisting essentially of a carrier and a crosslinked, water insoluble, polyallylamine polymer.

36. The pharmaceutical composition of claim 35 wherein the polyallylamine polymer is a homopolymer.

37. The pharmaceutical composition of claim 35 wherein the polyallylamine polymer is crosslinked with epichlorohydrin.

38. A pharmaceutical composition comprising a crosslinked, water insoluble polyallylamine homopolymer, wherein the polyallylamine homopolymer comprises repeat units represented by the structural formula: ##STR36##

wherein n is an integer.
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