Generated: May 23, 2017
|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.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.