Compositions and methods for treating hyperkalemia

Patent metadata

Field	Value
Publication number	US-2016175344-A1
Application number	US-201615052186-A
Country	US
Kind code	A1
Filing date	Feb 24, 2016
Priority date	Dec 23, 2014
Publication date	Jun 23, 2016
Grant date	—

Abstract

The present invention is directed to compositions and methods of removing potassium or treating hyperkalemia by administering pharmaceutical compositions of cation exchange polymers with low crosslinking for improved potassium excretion and for beneficial physical properties to increase patient compliance.

First claim

What is claimed is:

1 . A calcium salt of a crosslinked potassium binding polymer having the following structure:

or a pharmaceutically acceptable salt thereof,
wherein the mole ratio of m to n is from about 70:1 to about 60:1; and
wherein the crosslinked potassium binding polymer is characterized by a crosslinking of about 1.8%, wherein the term about means ±10%.

2 . The crosslinked potassium binding polymer of claim 1 , wherein the ratio of m to n is about 68:1.

3 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer is characterized by a swelling ratio in water of between about 3 grams of water per gram of polymer to about 8 grams of water per gram of polymer.

4 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer is characterized by a swelling ratio in water of between about 3 grams of water per gram of polymer to about 4.5 grams of water per gram of polymer.

5 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer is characterized by a swelling ratio in water of about 3.3 grams of water per gram of polymer.

6 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer is characterized by a swelling ratio in water of about 4.3 grams of water per gram of polymer.

7 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer further comprises substantially spherical particles having a median diameter from about 5 μm to about 130 μm.

8 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.9) between about 80 μm to about 130 μm.

9 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.9) between about 90 μm to about 120 μm.

10 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.9) between about 40 μm to about 70 μm.

11 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.9) between about 50 μm to about 60 μm.

12 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.5) between about 60 μm to about 90 μm.

13 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.5) between about 70 μm to about 80 μm.

14 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.5) between about 20 μm to about 50 μm.

15 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.5) between about 30 μm to about 40 μm.

16 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.1) between about 20 μm to about 70 μm.

17 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.1) between about 30 μm to about 60 μm.

18 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.1) between about 5 μm to about 30 μm.

19 . The crosslinked potassium binding polymer of claim 7 , wherein the particles have an average particle size Dv(0.1) between about 6 μm to about 23 μm.

20 . The crosslinked potassium binding polymer of claim 1 , wherein ratio of Dv(0.9):Dv(0.5) is about two or less and the ratio of Dv(0.5):Dv(0.1) is about five or less.

21 . The crosslinked potassium binding polymer of claim 1 , wherein the ratio of Dv(0.9):Dv(0.5) and the ratio of Dv(0.5):Dv(0.1) are each independently about two or less.

22 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer has a potassium exchange capacity from about 1 mEq to about 4 mEq per gram of potassium binding polymer.

23 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer has a Mouth Feel score greater than 3.5.

24 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer has a Mouth Feel score greater than 4.5.

25 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer has a Mouth Feel score greater than 5.0.

26 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer is characterized by a crosslinking of about 1.8%, wherein the term about means ±5%.

27 . The crosslinked potassium binding polymer of claim 1 , wherein the potassium binding polymer is characterized by a crosslinking of 1.8%.

28 . A pharmaceutical composition comprising a crosslinked potassium binding polymer of claim 1 and a pharmaceutically acceptable carrier, diluent, or excipient.

Assignees

• Ardelyx Inc

Inventors

• Charmot Dominique
• Davidson James P
• Lin Fangling
• Jacobs Jeffrey W
• Blinova Natalia
• Labonte Eric
• Langsetmo Ingrid
• Blanks Robert C

Classifications

• A61K9/0056

  Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals · CPC title

• A61K31/795 Primary

  Polymers containing sulfur · CPC title

• A61K9/0095

  Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches (A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006) · CPC title

• A61K9/10

  Dispersions; Emulsions · CPC title

• A61K9/14

  Particulate form, e.g. powders, {Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles (microspheres A61K9/16; microcapsules A61K9/50; nanocapsules, nanoparticles of the matrix type A61K9/51)} · CPC title