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Phosphate-binding chitosan and uses thereof

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20120277183 patent thumbnailZoom

Phosphate-binding chitosan and uses thereof


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.
Related Terms: Hyperphosphatemia

Browse recent Cypress Pharmaceutical, Inc. patents - Madison, MS, US
Inventors: Robert L. Lewis, Charles E. Day
USPTO Applicaton #: #20120277183 - Class: 514 55 (USPTO) - 11/01/12 - Class 514 
Drug, Bio-affecting And Body Treating Compositions > Designated Organic Active Ingredient Containing (doai) >O-glycoside >Polysaccharide >Chitin Or Derivative

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The Patent Description & Claims data below is from USPTO Patent Application 20120277183, Phosphate-binding chitosan and uses thereof.

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BACKGROUND OF THE INVENTION

Like other diseases for which there is no cure, chronic kidney disease takes an ever-increasing toll on patients who have it. As the disease progresses, the kidney becomes less efficient at removing various ions from the blood. Among these ions is phosphate, which can form insoluble particles when combined with calcium. In end-stage renal disease, the final stage of chronic kidney disease, kidney function is so compromised that phosphate levels in the blood (serum) become markedly elevated. This condition, known as hyperphosphatemia, carries with it many grave health risks. For example, when serum phosphate and calcium levels are above a certain threshold, hardened deposits may form throughout the body, endangering circulation. It is therefore very important to control serum phosphate levels in patients with end-stage renal disease.

Patients with end-stage renal disease may be advised to eat a diet low in phosphate. However, phosphate is present at some level in almost all the foods we eat. For this reason, phosphate binders were developed. Phosphate binders are compounds taken orally and which act in the gastrointestinal tract to bind phosphate and keep it from being absorbed. Phosphate binders are generally taken with each meal. Phosphate binders known in the art include, for example, various salts of aluminum and calcium, as well as some chemically synthesized crosslinked polymers. There are clinical circumstances in which the administration of aluminum or calcium salts is ill-advised. In animal models, certain crosslinked polymers carry with them elevated risks of carcinogenesis.

SUMMARY

OF THE INVENTION

The present invention provides a safe and effective phosphate binder derived from a natural polymer. In particular, the present invention provides, inter alia, phosphate-binding chitosan, compositions containing phosphate-binding chitosan, and methods for treating hyperphosphatemia using chitosan.

In one aspect, the present invention provides a method for removing phosphate from a subject (e.g., a mammalian subject). The method includes administering to the subject a therapeutically effective amount of chitosan. In some embodiments, the therapeutically effective amount of chitosan is administered orally.

In some embodiments, the subject is in need of treatment for hyperphosphatemia. In some embodiments, the subject is in need of treatment for chronic kidney disease and/or end-stage renal disease. In some embodiments, the subject is in need of treatment for one or more disorders of phosphate metabolism and/or impaired phosphate transport function.

In some embodiments, the therapeutically effective amount ranges from about 0.1 to about 10 grams of chitosan per dose. In some embodiments, the therapeutically effective amount ranges from about 0.5 to about 50 grams of chitosan per day.

In some embodiments, chitosan suitable for the invention binds at least about 30 mg phosphate per gram. In some embodiments, the chitosan binds at least about 60 mg phosphate per gram. In some embodiments, the chitosan binds at least about 90 mg phosphate per gram. In some embodiments, the chitosan binds at least about 120 mg phosphate per gram. In some embodiments, the chitosan binds at least about 150 mg phosphate per gram. In some embodiments, the chitosan binds at least about 180 mg phosphate per gram.

In some embodiments, chitosan suitable for the invention is administered in a form of a plurality of particles. In some embodiments, the plurality of particles have a mean volume particle size less than about 100 cubic microns. In some embodiments, the plurality of particles have a median volume particle size less than about 100 cubic microns.

In some embodiments, the plurality of particles include one or more particles having a roundness greater than about 10. In some embodiments, at least about 0.3% of the plurality of particles have a roundness greater than 10. As used herein, “roundness” refers to a measurement describing the shape of a particle. As used in this application, roundness is defined by the following equation:

Roundness=(Perimeter2)/(4*pi*area)

Roundness is typically measured using a digital image of a population of spheres and Image Pro Plus. Circular objects have a roundness=1.

In another aspect, the present invention provides a method for treating hyperphosphatemia. The method includes administering to a subject in need of treatment for hyperphosphatemia a composition comprising chitosan. In some embodiments, the subject is in need of treatment for chronic kidney disease and/or end-stage renal disease. In some embodiments, the subject is in need of treatment for one or more disorders of phosphate metabolism and/or impaired phosphate transport function.

In some embodiments, the composition of the invention includes a therapeutically effective amount of chitosan. In some embodiments, the therapeutically effective amount is from about 0.1 to about 10 grams chitosan per dose. In some embodiments, the therapeutically effective amount is from about 0.5 to about 50 grams chitosan per day.

In some embodiments, chitosan suitable for the invention binds at least about 30 mg phosphate per gram. In some embodiments, the chitosan binds at least about 60 mg phosphate per gram. In some embodiments, the chitosan binds at least about 90 mg phosphate per gram. In some embodiments, the chitosan binds at least about 120 mg phosphate per gram. In some embodiments, the chitosan binds at least about 150 mg phosphate per gram. In some embodiments, the chitosan binds at least about 180 mg phosphate per gram.

In some embodiments, chitosan suitable for the invention is present in a form of a plurality of particles. In some embodiments, the plurality of particles have a mean volume particle size less than about 100 cubic microns. In some embodiments, the plurality of particles have a median volume particle size less than about 100 cubic microns. In some embodiments, the plurality of particles include one or more particles having a roundness greater than about 10. In some embodiments, at least about 0.3% of the plurality of particles have a roundness greater than 10.

In some embodiments, the composition suitable for the invention is administered orally. In some embodiments, the composition is a nutritional supplement. In some embodiments, the composition is administered three times daily with meals.

In some embodiments, the composition further includes a carrier. In some embodiments, the carrier suitable for the invention 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. In some embodiments, the 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.

In yet another aspect, the present invention provides a composition suitable for treating hyperphosphatemia containing a therapeutically effective amount of chitosan. In some embodiments, the hyperphosphatemia is associated with chronic kidney disease and/or end-stage renal disease. In some embodiments, the hyperphosphatemia is associated with one or more disorders of phosphate metabolism and/or impaired phosphate transport function.

In some embodiments, the therapeutically effective amount is from about 0.1 to about 10 grams chitosan per dose. In some embodiments, the therapeutically effective amount is from about 0.5 to about 50 grams chitosan per day.

In some embodiments, chitosan suitable for the invention binds at least about 30 mg phosphate per gram. In some embodiments, the chitosan binds at least about 60 mg phosphate per gram. In some embodiments, the chitosan binds at least about 90 mg phosphate per gram. In some embodiments, the chitosan binds at least about 120 mg phosphate per gram. In some embodiments, the chitosan binds at least about 150 mg phosphate per gram. In some embodiments, the chitosan binds at least about 180 mg phosphate per gram.

In some embodiments, chitosan suitable for the invention is present in a form of a plurality of particles. In some embodiments, the plurality of particles have a mean volume particle size less than about 100 cubic microns. In some embodiments, the plurality of particles have a median volume particle size less than about 100 cubic microns.

In some embodiments, the plurality of particles include one or more particles having a roundness greater than about 10. In some embodiments, at least about 0.3% of the plurality of particles have a roundness greater than 10.

In some embodiments, the composition is suitable for oral administration. In some embodiments, the composition is a nutritional supplement.

In some embodiments, the composition further includes a carrier. In some embodiments, 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. In some embodiments, the 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.

In still another aspect, the present invention provides a nutritional supplement containing chitosan, 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.

In some embodiments, the plurality of particles include one or more particles having a roundness greater than about 10. In some embodiments, at least 0.3% of the plurality of particles have a roundness greater than about 10.

In a further aspect, the present invention provides a nutritional supplement containing chitosan, 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. In some embodiments, the plurality of particles have a mean volume particle size less than about 100 cubic microns.

In some embodiments, the plurality of particles include one or more particles having a roundness greater than about 10. In some embodiments, at least 0.3% of the plurality of particles have a roundness greater than about 10.

In this application, the use of “or” means “and/or” unless stated otherwise. As used in this application, the term “comprise” and variations of the term, such as “comprising” and “comprises,” are not intended to exclude other additives, components, integers or steps. As used in this application, the terms “about” and “approximately” are used as equivalents. Any numerals used in this application with or without about/approximately are meant to cover any normal fluctuations appreciated by one of ordinary skill in the relevant art.

Other features, objects, and advantages of the present invention are apparent in the detailed description, drawings and claims that follow. It should be understood, however, that the detailed description, the drawings, and the claims, while indicating embodiments of the present invention, are given by way of illustration only, not limitation. Various changes and modifications within the scope of the invention will become apparent to those skilled in the art.

DETAILED DESCRIPTION

OF THE INVENTION

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 using a therapeutically effective amount of chitosan.

Various aspects of the invention are described in detail in the following sections. The use of sections is not meant to limit the invention. Each section can apply to any aspect of the invention. In this application, the use of “or” means “and/or” unless stated otherwise.

Phosphate-Binding Chitosan

Chitosan suitable for the invention is a linear polysaccharide composed of β-(1-4)-linked D-glucosamine (deacetylated unit) and N-acetyl-D-glucosamine (acetylated unit). Chitosan typically has a molecular weight of approximately 104 to 106 dalton or higher. Chitosan is also referred to as poly-D-glucosamine; poly-[1-4]-β-D-glucosamine or deacetylated chitin.

Typically, chitosan is derived from chitin (C8H13O5N)n, a long-chain polymer of a N-acetylglucosamine (a derivative of glucose) isolated from natural sources (e.g., cell walls of fungi, the exoskeletons of arthropods) by complete or partial deacetylation and partial depolymerization. The deacetylation of chitin to chitosan can be performed in hot concentrated NaOH solution (40-50%). Chitosan is also commercially available, for example, from Pronova Biopolymer, Inc. (Portsmouth, N.H.), e.g., as SEACURE 142, 242 or 342; from Vanson, Inc. (Redmond, Wash.) under the tradenames “Chitosan;” and from Primex Ingredients SA (Avaldsnes, Norway) under the tradenames “Chitoclear.” Other chitosan suppliers include, but are not limited to, Acroyali Holdings Qingdao Co., Ltd. (Qingdao, China); AIDP, Inc. (City of Industry, CA); AK Biotech, Ltd. (Jinan, China); AK Scientific, Inc. (Mountain View, Calif.); Barrington Chemical Corporation (Harrison, N.Y.); Beckmann Chemikalien KG (Bassum, Germany); Carbomer, Inc. (San Diego, Calif.); CCS CHEM. Co., Ltd. (Zhejiang, China); Dayang Chemicals Co., Ltd. (Hangzhou, China); DNP International (Whittier, CA); Donboo Amino Acid Co., Ltd. (Jiangsu, China); EcoTag Comercial Ltd. (Cruz Alta, Brazil); Federal Laboratories Corporation (Alden, N.Y.); Fortune Bridge Co., Inc. (Elmont, N.Y.); Gallard-Schlesinger Industries, Inc. (Plainview, N.Y.); Hongkong Henry Industry Co., Ltd. (ZheJiang, China); Jiagen Biotechnologies, Inc. (Quebec, Canada); Jinan Haohua Industry Co., Ltd. (Shandong, China); Kinbester Co., Ltd. (Xiamen, China); Kingreat Chemistry Co., Ltd. (Xiamen, China); Marcor Development Corporation (Carlstadt, N.J.); Marine Chemicals (Kerala, India); Nantong Chem-Tech. (Group) Co., Ltd. (Nantong, China); Ningbo Innopharmchem Co., Ltd. (Ningbo, China); Ningbo Pangs Lanza International Co., Ltd. (Zhejiang, China); Nutriland Group Inc. (Torrance, Calif.); NutriScience Innovations, LLC (Trumbull, Conn.); Orcas International, Inc. (Flanders, N.J.); Pacific Rainbow International, Inc. (City of Industry, Calif.); Panvo Organics Pvt. Ltd. (Tamil Nadu, India); Parchem Nutrition, Inc. (White Plains, N.Y.); Sears Phytochem Ltd. (Madhya Pradesh, India); SeaTech Bioproducts (Shrewsbury, MA); Shanghai Freemen Chemicals Co., Ltd (Shanghai, China); Shanghai Mintchem Development Co., Ltd. (Shanghai, China); Shanghai Nicechem Co., Ltd. (Shanghai, China); Shanghai Sunwise Chemical Co., Ltd. (Shanghai, China); Shanghai Wellhoned Biotech Co., Ltd. (Shanghai, China); Sinosale Hebei Co., Ltd. (Shijiazhuang, China); Spectrum Chemicals & Laboratory Products (Gardena, Calif.); Stryka Botanics (Hillsborough, N.J.); Vitajoy Bio-tech Co., Ltd. (Suzhou, China); Wilke Resources, Inc. (Lenexa, Kans.); Wintersun Chemical (Ontario, Calif.); Wright Group (Crowley, La.); Xiamen Topusing Chemical Co., Ltd. (Xiamen, China).

Chitin, chitosan and chitin derivatives are further described in Tharanathan et al., Crit. Reviews in Food Sci. & Nutrition, 43(1), pp. 61-87 (2003), which is incorporated herein by reference.

Chitosan and chitin derivatives are often described according to the degree of de-acetylation within the polysaccharide. Chitosan suitable for the invention may have a range of degrees of de-acetylation. In some embodiments, chitosan suitable for the invention has a higher degree of de-acetylation. In some embodiments, the degree of de-acetylation may be at least about 50% (e.g., at least about 60%, or at least about 70%, or at least about 80%, or at least about 85%, or at least about 87.5%, or at least about 90%, or at least about 92.5%, or at least about 95%, or at least about 97.5%, or at least about 98%, or at least about 99%, or at least about 99.5%, or at least about 99.9%). In some embodiments, the degree of de-acetylation may range between 50% and 99.9% (e.g., between 50% and 99%, or between 75% and 99.9%, or between 85% and 99.9%, or between 87.5% and 99.9%, or between 87.5% and 97.5%, or between 87.5% and 95%, or between 90% and 99.9%, or between 90% and 95%, or between 95% and 99.9%, or between 95.5% and 97.5%, or between 97% and 99.9%, or between 98% and 99.9%, or between 98% and 99.5%, or between 99.5% and 99.9%).

Chitosan suitable for the present invention also includes chitosan derivatives. Exemplary chitosan derivatives include, but are not limited to, medium or long chain N-alkyl- or N-alkanoyl-chitosan, or water-soluble chitosan. The term “medium chain N-alkyl- or N-alkanolyl” refers to C8-13—N-alkyl- or —N-alkanolyl chains, the term “long chain N-alkyl- or N-alkanoyl” refers to C14-18—N-alkyl- or —N-alkanolyl chains. Examples of water-soluble chitosan include, but are not limited to, CM-chitosan (carboxymethyl-chitosan), S-chitosan (oligosaccharide-chitosan), SCM-chitosan (N-sulfide derivative of N-deacetylated CM chitin), HP-chitosan (hydroxyl-propyl-chitosan).

Suitable chitosan for the invention also includes any conventional salts of chitosan. Examples of salts of chitosan include those with organic acids such as lower alkanoic acids, as well as mineral acids such as HCl and H2SO4.

Suitable chitosan for the invention also includes any conventional pharmaceutically acceptable acid of chitosan such as acetic, citric, formic and tartaric acid.

Suitable chitosan for the invention further includes modified chitosan. As used herein, “modified chitosan” refers to the chitosan obtained from the subsequent treatment of the initial product obtained from chitin. Exemplary modified chitosan includes, but is not limited to, semi-crystalline, microcrystalline, and nanoparticulate chitosan. Processes for obtaining modified chitosan are known in the art. Exemplary processes are described in U.S. Pat. Nos. 5,770,187, 6,740,752, 6,638,918, 7,288,532, and PCT publications WO 01/32751, WO 00/47177, the teachings of all of which are hereby incorporated by reference.

In some embodiments, chitosan suitable for the invention binds at least about 30 mg phosphate per gram chitosan. In some embodiments, chitosan suitable for the invention binds at least about 60 mg phosphate per gram. In some embodiments, chitosan suitable for the invention binds at least about 90 mg phosphate per gram. In some embodiments, chitosan suitable for the invention binds at least about 120 mg phosphate per gram. In some embodiments, chitosan suitable for the invention binds at least about 150 mg phosphate per gram. In some embodiments, chitosan suitable for the invention binds at least about 180 mg phosphate per gram chitosan. In some embodiments, chitosan suitable for the invention binds at least about 210 mg phosphate per gram. In some embodiments, chitosan suitable for the invention binds at least about 240 mg phosphate per gram.

Without wishing to be bound by any theories, it is contemplated that chitosan bind and remove phosphate through an ion exchange process. As used herein, the term “ion exchange” has its ordinary meaning in the chemical and/or pharmaceutical field. In particular, ion exchange can be a process including the release of one or more anions ionically bound to a cationic polymer and the subsequent ionic binding of another one or more anions to the polymer. As a non-limiting example, ion exchange includes the release of one or more chloride ions from a polymer such as chitosan and the subsequent binding of one or more phosphate, hydrogen phosphate, and/or dihydrogen phosphate ions to the polymer.

Particles of Chitosan

In particular, chitosan suitable for the present invention may be in a form of particles. In some embodiments, chitosan suitable for the invention are present in a form of a plurality of particles. The chitosan particulates suitable for the invention can have a broad particle size distribution. Typically, the chitosan particles can be characterized by a mean volume particle size, and/or a median volume particle size. In some embodiments, the chitosan particles suitable for the invention can have a mean volume particle size less than about 300 cubic microns, or less than about 250 cubic microns, or less than 200 cubic microns, or less than 150 cubic microns, or less than about 100 cubic microns, or less than about 75 cubic microns, or less than about 50 cubic microns. As used herein, 1 cubic micron equals to 1 μm3. In some embodiments, the chitosan particles have a mean volume particle size less than about 100 cubic microns.

In other embodiments, the chitosan particles suitable for the invention can have a median volume particle size less than about 300 cubic microns, or less than about 250 cubic microns, or less than 200 cubic microns, or less than 150 cubic microns, or less than about 100 cubic microns, or less than about 75 cubic microns, or less than about 50 cubic microns. As used herein, 1 cubic micron equals to 1 μm3. In some embodiments, the chitosan particles have a median volume particle size less than about 100 cubic microns.

In some embodiments, the chitosan particles suitable for the invention may have combinations of median volume particle size and mean volume particle size as described above. For example, the chitosan particles suitable for the invention may have a median volume particle size less than about 100 cubic microns and a mean volume particle size less than about 100 cubic microns.

A chitosan particle can also be characterized by a roundness. As used herein, the term “roundness” has its ordinary meaning in the particle size and shape measurement arts. As used in this application, roundness is defined by the following equation:



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stats Patent Info
Application #
US 20120277183 A1
Publish Date
11/01/2012
Document #
File Date
07/24/2014
USPTO Class
Other USPTO Classes
International Class
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Hyperphosphatemia


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