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|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)|
|Filing Date:||Sep 15, 1997|
|Claims:||1. A method of making a pharmaceutical composition comprising cross-linked polyallylamine, said method comprising the steps of: |
(a) contacting poly(allylamine) with a difunctional crosslinking agent in an aqueous alkaline solution, said cross-linking agent being present in an amount sufficient for forming a poly(allylamine) gel, thereby producing an aqueous alkaline solution comprising polyallylamine and the cross-linking agent;
(b) maintaining the aqueous alkaline solution comprising polyallylamine and the cross-linking agent at room temperature for a sufficient period of time for cross-linking of the poly(allylamine), thereby forming cross-linked polyallylamine gel;
(c) washing the cross-linked polyallylamine with water; and
(d) at least one step selected from the group consisting of:
(i) admixing the cross-linked polyallylamine with a pharmaceutically acceptable carrier, excipient or diluent; and
(ii) enclosing the cross-linked polyallylamine within a pharmaceutically acceptable carrier.
2. The method of claim 1 wherein the difunctional cross-linking agent is selected from the group consisting of succinyl dichloride, bisphenol A diglycidyl ether, pyromellitic dianhydride, toluene diisocyanate, 1,4-butanedioldiglycidyl ether, 1,2 ethanedioldiglycidyl ether, 1,3-dichloropropane, 1,2-dichloroethane, 1,3-dibromopropane, 1,2-dibromoethane, succinyl dichloride, dimethylsuccinate and acryloyl chloride.
3. The method of claim 1 wherein the difunctional cross-linking agent is epichlorohydrin.
4. The method of claim 1 wherein the alkaline aqueous solution of poly(allylamine) is prepared by adding base to an aqueous solution of an acid salt of poly(allylamine).
5. The method of claim 4 wherein the acid salt of poly(allylamine) is the hydrochloride salt of poly(allylamine).
6. The method of claim 4 wherein the base is sodium hydroxide or potassium hydroxide.
7. The method of claim 4 wherein the alkaline aqueous solution has a pH of about 10.
8. The method of claim 1, further comprising the step of fragmenting the gel to form gel particles.