Claims for Patent: 11,478,502

Summary for Patent: 11,478,502

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:	US16/438,340
Patent Claims:	1. A method of treating iron deficiency anemia, comprising: administering to an adult human subject having iron deficiency anemia a pharmaceutical composition comprising a polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate in a single dosage unit of at least about 0.6 grams of elemental iron, wherein the pharmaceutical composition is administered intravenously in about 15 minutes or less. 2. The method of claim 1, wherein the iron deficiency anemia is associated with non-dialysis dependent chronic kidney disease, heavy uterine bleeding, or a gastrointestinal disorder. 3. The method of claim 2, wherein the pharmaceutical composition is administered as an intravenous push or infusion. 4. The method of claim 3, wherein the iron deficiency anemia is associated with non-dialysis dependent chronic kidney disease, or the gastrointestinal disorder is characterized by gastrointestinal bleeding. 5. The method of claim 3, wherein the iron deficiency anemia is associated with a gastrointestinal disorder that is Crohn's disease or inflammatory bowel disease. 6. The method of claim 3, wherein the pharmaceutical composition is administered as an intravenous push. 7. The method of claim 6, wherein the pharmaceutical composition is administered at a rate of about 100 mg elemental iron per minute. 8. The method of claim 7, wherein the pharmaceutical composition is administered in about 10 minutes or less. 9. The method of claim 7, wherein the pharmaceutical composition is administered in 8 minutes or less. 10. The method of claim 3, wherein the pharmaceutical composition is administered as an infusion. 11. The method of claim 10, wherein the pharmaceutical composition is administered at a concentration of between 2 mg and 4 mg of elemental iron per ml. 12. The method of claim 10, wherein the pharmaceutical composition is administered at a rate of between about 12.5 and 25 ml/min. 13. The method of claim 3, 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. 14. The method of claim 13, 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. 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 contains about 25% to about 50% carbohydrate. 16. The method of claim 15, wherein the pharmaceutical composition has a pH between about 5.0 to about 7.0. 17. The method of claim 15, wherein the pharmaceutical composition has physiological osmolarity. 18. The method of claim 15, 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. 19. The method of claim 18, 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. 20. The method of claim 13, 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. 21. 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. 22. The method of claim 1, wherein the single dosage unit contains at least 0.7 grams of elemental iron. 23. The method of claim 22, wherein the iron deficiency anemia is associated with non-dialysis dependent chronic kidney disease, heavy uterine bleeding, or a gastrointestinal disorder. 24. The method of claim 23, wherein said iron deficiency anemia is associated with non-dialysis dependent chronic kidney disease, and the composition is administered as an intravenous push or infusion. 25. The method of claim 23, wherein the gastrointestinal disorder is characterized by gastrointestinal bleeding, and the composition is administered as an intravenous push or infusion. 26. The method of claim 23, 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. 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 24% to 32% elemental iron. 28. The method of claim 27, 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. 29. The method of claim 26, 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. 30. The method of claim 1, wherein the single dosage unit of elemental iron is about 1000 mg. 31. A method of treating functional iron deficiency comprising: administering to an adult human subject having iron deficiency anemia a pharmaceutical composition comprising a polynuclear iron (III)-hydroxide 4(R)-(poly-(1→4)-O-α-D-glucopyranosyl)-oxy-2(R),3(R),5(R),6-tetrahydroxy-hexanoate in a single dosage unit of at least about 0.6 grams of elemental iron, wherein: the pharmaceutical composition is administered intravenously in about 15 minutes or less; and administration of the pharmaceutical composition results in an increase in Transferrin saturation (TSAT) compared to TSAT before administration of the pharmaceutical composition. 32. The method of claim 31, wherein the single dosage unit of elemental iron is about 1000 mg.