Claims for Patent: 11,364,260

Summary for Patent: 11,364,260

Title:	Methods and compositions for administration of iron
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.
Inventor(s):	Mary Jane Helenek, Marc L. Tokars, Richard P. Lawrence
Assignee:	American Regent Inc
Application Number:	US16/825,337
Patent Claims:	1. A method of treating iron deficiency or dysfunctional iron metabolism associated with congestive heart failure, the method comprising administering to a human having iron deficiency or dysfunctional iron metabolism associated with congestive heart failure a pharmaceutical composition comprising an iron carbohydrate complex in a single dosage unit of at least about 0.6 grams of elemental iron. 2. The method of claim 1, wherein administration of the pharmaceutical composition results in an increase in hemoglobin levels compared to hemoglobin levels before administration of the pharmaceutical composition. 3. The method of claim 1, wherein the pharmaceutical composition is administered at a rate of about 100 mg elemental iron per minute. 4. The method of claim 1, wherein the pharmaceutical composition is administered as an infusion. 5. The method of claim 4, wherein the pharmaceutical composition is administered at a concentration of between 2 mg and 4 mg of elemental iron per ml. 6. The method of claim 4, wherein the pharmaceutical composition is administered at a rate of between about 12.5 and 25 ml/min. 7. The method of claim 1, wherein the single dosage unit contains at least 0.7 grams of elemental iron. 8. The method of claim 1, wherein the iron carbohydrate complex is polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate. 9. The method of claim 8, wherein the weight average molecular weight of the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate is from about 100,000 daltons to about 350,000 daltons. 10. The method of claim 9, wherein the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate contains about 24% to 32% elemental iron. 11. The method of claim 10, wherein the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate contains about 25% to about 50% carbohydrate. 12. The method of claim 11, wherein the pharmaceutical composition has a pH between about 5.0 to about 7.0. 13. The method of claim 11, wherein the pharmaceutical composition has physiological osmolarity. 14. The method of claim 11, wherein the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate has a mean iron core size of at least about 1 nm but not greater than about 9 nm. 15. The method of claim 14, wherein the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate has a mean diameter particle size of no greater than about 35 nm. 16. The method of claim 9, wherein: the weight average molecular weight of said polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate is about 150,000 daltons; and the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate contains about 28% elemental iron and about 37% carbohydrate. 17. The method of claim 1, wherein the pharmaceutical composition is administered in about 15 minutes or less. 18. The method of claim 17, wherein administration of the pharmaceutical composition results in an increase in Transferrin saturation (TSAT) compared to TSAT before administration of the pharmaceutical composition. 19. The method of claim 1, wherein the single dosage unit contains at least 1.0 grams of elemental iron. 20. The method of claim 1, wherein the pharmaceutical composition is administered intravenously. 21. The method of claim 1, wherein the pharmaceutical composition is administered parenterally. 22. The method of claim 1, wherein iron deficiency is iron deficiency anemia. 23. A method of treating iron deficiency or dysfunctional iron metabolism associated with cardiomyopathy, the method comprising administering to a human having iron deficiency or dysfunctional iron metabolism associated with cardiomyopathy a pharmaceutical composition comprising an iron carbohydrate complex in a single dosage unit of at least about 0.6 grams of elemental iron. 24. The method of claim 23, wherein the iron carbohydrate complex is polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate. 25. The method of claim 24, wherein the weight average molecular weight of the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate is from about 100,000 daltons to about 350,000 daltons. 26. The method of claim 25, wherein the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate contains about 24% to 32% elemental iron. 27. The method of claim 26, wherein the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate contains about 25% to about 50% carbohydrate. 28. The method of claim 25, wherein: the weight average molecular weight of said polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate is about 150,000 daltons; and the polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate contains about 28% elemental iron and about 37% carbohydrate. 29. The method of claim 23, wherein the single dosage unit contains at least 1.0 grams of elemental iron. 30. The method of claim 23, wherein the pharmaceutical composition has a pH between about 5.0 to about 7.0. 31. The method of claim 23, wherein the pharmaceutical composition is administered intravenously. 32. The method of claim 23, wherein the pharmaceutical composition is administered parenterally. 33. The method of claim 23, wherein iron deficiency is iron deficiency anemia. 34. 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 human subject in need thereof an iron carbohydrate complex in a single dosage unit of at least about 0.6 grams of elemental iron; wherein the iron carbohydrate complex is selected from the group consisting of an iron carboxymaltose complex, an iron mannitol complex, an iron polymaltose complex, an iron gluconate complex, and an iron sorbitol complex; and the iron carbohydrate complex has a substantially non-immunogenic carbohydrate component and substantially no cross reactivity with anti-dextran antibodies, and the disease, disorder, or condition is iron deficiency or dysfunctional iron metabolism associated with cardiomyopathy. 35. The method of claim 34, wherein the disease, disorder or condition is not Restless Leg Syndrome. 36. The method of claim 34, wherein the single dosage unit contains at least 1.0 grams of elemental iron. 37. 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 human subject in need thereof an iron carbohydrate complex in a single dosage unit of at least about 0.6 grams of elemental iron; wherein the iron carbohydrate complex is selected from the group consisting of an iron carboxymaltose complex, an iron mannitol complex, an iron polymaltose complex, an iron gluconate complex, and an iron sorbitol complex; and the iron carbohydrate complex has a substantially non-immunogenic carbohydrate component and substantially no cross reactivity with anti-dextran antibodies, and the disease, disorder, or condition is iron deficiency or dysfunctional iron metabolism associated with congestive heart failure. 38. The method of claim 37, wherein the disease, disorder or condition is not Restless Leg Syndrome. 39. The method of claim 37, wherein the single dosage unit contains at least 1.0 grams of elemental iron.