IP Library Granted Patent US 10,603,336
Granted Patent B2
US 10,603,336 · App. 16/192,681 · Granted Mar 31, 2020

Methods and compositions for administration of iron

Inventors: Mary Jane Helenek (Brookville, NY); Marc L. Tokars (Douglassville, PA); Richard P. Lawrence (Calverton, NY)
Assignee: American Regent, Inc.
A61K31/7135A61K31/715A61K31/721C07H23/00
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Quick Facts
Patent No.
US 10,603,336
App. No.
16/192,681
Granted
Mar 31, 2020
Kind
B2
Abstract

The present invention generally relates to treatment of iron-related conditions with iron carbohydrate complexes. One aspect of the invention is a method of treatment of iron-related conditions with a single unit dosage of at least about 0.6 grams of elemental iron via an iron carbohydrate complex. The method generally employs iron carbohydrate complexes with nearly neutral pH, physiological osmolarity, and stable and non-immunogenic carbohydrate components so as to rapidly administer high single unit doses of iron intravenously to patients in need thereof.

Claims (35)

1. A method of treating a disease, disorder, or condition characterized by iron deficiency or dysfunctional iron metabolism resulting in reduced bioavailability of dietary iron, comprising administering to a subject in need thereof an iron carbohydrate complex in a single dosage of at least 9 mg of elemental iron per kg of body weight, wherein:

a) the disease, disorder or condition is an anemia selected from among:

iron deficiency anemia;

anemia of chronic disease; and

an anemia due to impaired iron absorption or poor nutrition;

b) the iron carbohydrate complex is substantially non-immunogenic, and has substantially no cross reactivity with anti-dextran antibodies;

c) the iron carbohydrate complex is an iron polyisomaltose complex or an iron polyglucose sorbitol carboxymethyl ether complex; and

d) the disease, disorder or condition is not Restless Leg Syndrome.

2. The method of claim 1 , wherein the iron carbohydrate complex is an iron polyisomaltose complex.

3. The method of claim 2 , wherein the polyisomaltose is reduced polyisomaltose.

4. The method of claim 1 , wherein the iron carbohydrate complex is administered in about 15 minutes or less.

5. The method of claim 1 , wherein the single dose of the iron carbohydrate complex is at least about 0.6 grams of elemental iron.

6. The method of claim 1 , wherein the iron carbohydrate complex is administered parenterally.

7. The method of claim 1 , wherein the iron carbohydrate complex is administered intravenously.

8. The method of claim 1 , wherein the anemia comprises iron deficiency anemia.

9. The method of claim 1 , wherein the anemia comprises an iron deficiency anemia associated with chronic blood loss, acute blood loss, pregnancy, childbirth, childhood development, psychomotor and cognitive development in children, breath holding spells, heavy uterine bleeding, menstruation, chronic recurrent hemoptysis, idiopathic pulmonary siderosis, chronic internal bleeding, gastrointestinal bleeding, parasitic infections, chronic kidney disease, dialysis, surgery or acute trauma, chronic ingestion of alcohol, chronic ingestion of salicylates, chronic ingestion of steroids, chronic ingestion of non-steroidal anti-inflammatory agents, or chronic ingestion of erythropoiesis stimulating agents.

10. The method of claim 1 , wherein the anemia is of a chronic disease selected from among rheumatoid arthritis, cancer, Hodgkin's leukemia, non-Hodgkin's leukemia, cancer chemotherapy, inflammatory bowel disease, ulcerative colitis, thyroiditis, hepatitis, systemic lupus erythematosus, polymyalgia rheumatica, scleroderma, mixed connective tissue disease, Sjogren's syndrome, congestive heart failure/cardiomyopathy, and idiopathic geriatric anemia.

11. The method of claim 1 , wherein the anemia is due to impaired iron absorption or poor nutrition.

12. The method of claim 1 , wherein the anemia is associated with Crohn's Disease, gastric surgery, ingestion of drug products that inhibit iron absorption, or chronic use of calcium.

13. The method of claim 1 , wherein the iron carbohydrate complex is an iron polyglucose sorbitol carboxymethyl ether complex.

14. The method of claim 13 , wherein the iron carbohydrate complex has a crystal size of 6.2 to 7.3 nm.

15. The method of claim 13 , wherein the iron carbohydrate complex has an average colloidal particle size of about 30 nm.

16. The method of claim 13 , wherein the iron carbohydrate complex has a molecular weight of approximately 750 kD.

17. The method of claim 13 , wherein the iron carbohydrate complex has a blood half-life of approximately 10-14 hours.

18. The method of claim 13 , wherein the iron carbohydrate complex has neutral pH and isotonic osmolarity.

19. The method of claim 13 , wherein the iron carbohydrate complex is administered in about 15 minutes or less.

20. The method of claim 13 , wherein the single dose of the iron carbohydrate complex is at least about 0.6 grams of elemental iron.

21. The method of claim 13 , wherein administration of the single dose is repeated.

22. The method of claim 13 , further comprising a second administration of said iron carbohydrate complex upon recurrence of at least one symptom of the disease, disorder, or condition.

23. The method of claim 22 , wherein the second administration is 3-4 days after the first administration.

24. The method of claim 22 , wherein the second administration is one week after the first administration.

25. The method of claim 13 , wherein the iron carbohydrate complex is a polyglucose sorbitol carboxymethyl ether-coated non-stoichiometric magnetite complex.

26. The method of claim 25 , wherein the iron carbohydrate complex has a crystal size of 6.2 to 7.3 nm.

27. The method of claim 25 , wherein the iron carbohydrate complex has an average colloidal particle size of about 30 nm.

28. The method of claim 25 , wherein the iron carbohydrate complex has a molecular weight of approximately 750 kD.

Assignments (2)
CHANGE OF NAME Recorded Jan 11, 2019
From: LUITPOLD PHARMACEUTICALS, INC.
To: AMERICAN REGENT, INC.
Reel/Frame 048067/0271 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 29, 2018
From: HELENEK, MARY JANE; TOKARS, MARC L.; LAWRENCE, RICHARD P.
To: LUITPOLD PHARMACEUTICALS, INC.
Reel/Frame 047629/0603 →
Continuity (12)
Continuation 15958930 · Apr 20, 2018
Division 14683415 · Apr 10, 2015
Continuation 13847254 · Mar 19, 2013
Continuation 12787283 · May 25, 2010
Continuation 11620986 · Jan 8, 2007
Continuation 16192681
Continuation 14683415 · Apr 10, 2015
Continuation 13847254 · Mar 19, 2013
Continuation 12787283 · May 25, 2010
Continuation 11620986 · Jan 8, 2007
Provisional Application 60757119 · Jan 6, 2006
Related Publication 20190083524A1 · Mar 21, 2019