Phosphate-binding chitosan and uses thereof

Abstract

The present invention provides compositions and methods for removing phosphate from a subject using chitosan. The present invention also provides compositions and methods for treating hyperphosphatemia based on phosphate-binding chitosan.

1 - 65 . (canceled) 
     
     
         66 . A pharmaceutical composition formulated for treating hyperphosphatemia comprising a therapeutically effective amount of chitosan,
 wherein the chitosan has a degree of de-acetylation greater than about 95% and is characterized with an ability to bind at least about 60 mg phosphate per gram of chitosan in an in vitro phosphate-binding assay, and   wherein the therapeutically effective amount of chitosan ranges from greater than 3.0 grams to about 20 grams per dose.   
     
     
         67 . The pharmaceutical composition of  claim 66 , wherein the hyperphosphatemia is associated with chronic kidney disease and/or end-stage renal disease. 
     
     
         68 . The pharmaceutical composition of  claim 66 , wherein the hyperphosphatemia is associated with one or more disorders of phosphate metabolism and/or impaired phosphate transport function. 
     
     
         69 . The pharmaceutical composition of  claim 66 , wherein the therapeutically effective amount ranges from greater than 3.0 to about 10 grams chitosan per dose. 
     
     
         70 . The pharmaceutical composition of  claim 66 , wherein the chitosan is characterized with the ability to bind at least about 90 mg phosphate per gram in the in vitro phosphate-binding assay. 
     
     
         71 . The pharmaceutical composition of  claim 66 , wherein the chitosan is characterized with the ability to bind at least about 120 mg phosphate per gram in the in vitro phosphate-binding assay. 
     
     
         72 . The pharmaceutical composition of  claim 66 , wherein the chitosan is characterized with the ability to bind at least about 150 mg phosphate per gram in the in vitro phosphate-binding assay. 
     
     
         73 . The pharmaceutical composition of  claim 66 , wherein the chitosan is characterized with the ability to bind at least about 180 mg phosphate per gram in the in vitro phosphate-binding assay. 
     
     
         74 . The pharmaceutical composition of  claim 66 , wherein the chitosan is present in a form of a plurality of particles. 
     
     
         75 . The pharmaceutical composition of  claim 74 , wherein the plurality of particles have a mean volume particle size less than about 100 cubic microns. 
     
     
         76 . The pharmaceutical composition of  claim 74 , wherein the plurality of particles have a median volume particle size less than about 100 cubic microns. 
     
     
         77 . The pharmaceutical composition of  claim 74 , wherein the plurality of particles comprise one or more particles having a roundness greater than about 10. 
     
     
         78 . The pharmaceutical composition of  claim 77 , wherein at least about 0.3% of the plurality of particles have a roundness greater than 10. 
     
     
         79 . The pharmaceutical composition of  claim 66 , wherein the pharmaceutical composition is formulated for oral administration. 
     
     
         80 . The pharmaceutical composition of  claim 66 , wherein the pharmaceutical composition is a nutritional supplement. 
     
     
         81 . The pharmaceutical composition of  claim 66 , wherein the pharmaceutical composition further comprises a carrier. 
     
     
         82 . The pharmaceutical composition of  claim 81 , wherein the carrier is selected from the group consisting of a starch, a gum, an alginate, a silicate, dextrose, gelatin, lactose, mannitol, sorbitol, sucrose, tragacanth, cellulose, methyl cellulose, microcrystalline cellulose, a methylhydroxybenzoate, a propylhydroxybenzoate, polyvinylpyrrolidone and talc. 
     
     
         83 . The pharmaceutical composition of  claim 66 , wherein the pharmaceutical composition is in a form of a cachet, a hard gelatin capsule, a soft gelatin capsule, an elixir, a lozenge, a pill, a powder, a sachet, a sterile packaged powder, a suspension, a syrup, or a tablet. 
     
     
         84 . A nutritional supplement comprising chitosan, wherein the chitosan has a degree of de-acetylation greater than about 95% and is characterized with an ability to bind at least about 60 mg phosphate per gram of chitosan in an in vitro phosphate-binding assay, and wherein the chitosan is present in a form of a plurality of particles having a mean volume particle size less than about 100 cubic microns. 
     
     
         85 . The nutritional supplement of  claim 84 , wherein the plurality of particles comprise one or more particles having a roundness greater than about 10. 
     
     
         86 . The nutritional supplement of  claim 84 , wherein at least 0.3% of the plurality of particles have a roundness greater than about 10. 
     
     
         87 . A nutritional supplement comprising chitosan,
 wherein the chitosan has a degree of de-acetylation greater than about 95% and is characterized with an ability to bind at least about 60 mg phosphate per gram of chitosan in an in vitro phosphate-binding assay, and   wherein the chitosan is present in a form of a plurality of particles having a median volume particle size less than about 100 cubic microns.   
     
     
         88 . The nutritional supplement of  claim 87 , wherein the plurality of particles have a mean volume particle size less than about 100 cubic microns. 
     
     
         89 . The nutritional supplement of  claim 87 , wherein the plurality of particles comprise one or more particles having a roundness greater than about 10. 
     
     
         90 . The nutritional supplement of  claim 87 , wherein at least 0.3% of the plurality of particles have a roundness greater than about 10.