Aqueous iron carbohydrate complexes, their production and medicaments containing them

• US 10,519,252 B2
• Filed: 03/15/2013
• Issued: 12/31/2019
• Est. Priority Date: 10/23/2002
• Status: Expired due to Term

• Current Assignee: Vifor (International) AG (CSL Limited)
• Original Assignee: Vifor (International) AG (CSL Limited)
• Inventors: Geisser, Peter, Philipp, Erik, Richle, Walter
• Primary Examiner(s): Pak, John
• Application Number:
  US13/835,400
• Publication Number:
  US 20130203698A1
• Time in Patent Office: 2,482 Days
• Field of Search: 514502, 514 54, 514 58, 514 59, 514777, 514814
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/295 Iron group metal compounds
• CPC Class Codes: A61K 31/718 Starch or degraded starch, e.g. amylose, amylopectin
• CPC Class Codes: A61K 33/26 Iron; Compounds thereof
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/61 the organic macromolecular compound being a polysaccharide or a derivative thereof
• CPC Class Codes: A61P 7/06 Antianaemics
• CPC Class Codes: C08B 30/18 Dextrin , e.g. yellow canari, white dextrin, amylodextrin or maltodextrin; Methods of depolymerisation, e.g. by irradiation or mechanically
• CPC Class Codes: C08B 31/185 Derivatives of oxidised starch, e.g. crosslinked oxidised starch
• CPC Class Codes: C08B 37/0009 alpha-D-Glucans, e.g. polydextrose, alternan, glycogen; (alpha-1,4)(alpha-1,6)-D-Glucans; (alpha-1,3)(alpha-1,4)-D-Glucans, e.g. isolichenan or nigeran; (alpha-1,4)-D-Glucans; (alpha-1,3)-D-Glucans, e.g. pseudonigeran; Derivatives thereof

Abstract

Water soluble Iron carbohydrate complex obtainable from an aqueous solution of iron(III) salt and an aqueous solution of the oxidation product of one or more maltrodextrins using an aqueous hypochlorite solution at a pH-value within the alkaline range, where, when one maltodextrin is applied, its dextrose equivalent lies between 5 and 20, and when a mixture of several maltodextrins is applied, the dextrose equivalent of the mixture lies between 5 and 20 and the dextrose equivalent of each individual maltodextrin contained in the mixture lies between 2 and 40, process for its production and medicament for the treatment and prophylaxis of iron deficiency conditions.

Claims

1. An iron (III) carboxymaltodextrin complex wherein said iron (III) carboxymaltodextrin complex comprises polynuclear iron (III)-hydroxide 4(R)-(poly-(1→

4)-O-α

-D-glucopyranosyl)-oxy-2(R),3(S),5(R),6-tetrahydroxy-hexanoate and has a weight average molecular weight in the range of from 80 kDa to 400 kDa, and wherein said 4(R)-(poly-(1→

4)-O-α

-D-glucopyranosyl)-oxy-2(R),3(S),5(R),6-tetrahydroxy-hexanoate is derived from the oxidation of maltodextrin, wherein when one maltodextrin is applied its dextrose equivalent lies between 5 and 20, and when a mixture of several maltodextrins is applied, the dextrose equivalent of the mixture lies between 5 and 20 and the dextrose equivalent of each individual maltodextrins contained in the mixture lies between 2 and 40.

2. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight in the range of from 80 kDa to 350 kDa.

3. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight in the range of from 80 kDa to 300 kDa.

4. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight in the range of from 118 kDa to 271 kDa.

5. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 271,000 Da.

6. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 141,000 Da.

7. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 140,000 Da.

8. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 189,000 Da.

9. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 118,000 Da.

10. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 178,000 Da.

11. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 137,000 Da.

12. The iron (III) carboxymaltodextrin complex of claim 1, having a weight average molecular weight of 170,000 Da.

13. A medicament comprising the iron (III) carboxymaltodextrin complex of claim 1 and a pharmaceutically acceptable carrier, excipient, or additive.

14. The medicament of claim 13, wherein said medicament is an aqueous solution.

15. The medicament of claim 14, wherein said aqueous solution is a brine solution.

16. The medicament of claim 14, wherein said iron (III) carboxymaltodextrin complex is present in said aqueous solution in an amount of from 1% to 20% by weight, based on the total weight of the aqueous solution.

17. The medicament of claim 14, wherein said iron (III) carboxymaltodextrin complex is present in said aqueous solution in an amount of 5% by weight, based on the total weight of the aqueous solution.

18. A method for treating an iron deficiency condition comprising the step of administering to a subject in need thereof a pharmaceutically effective amount of the medicament of claim 13.

19. The method of claim 18, wherein said iron deficiency condition is iron deficiency anaemia.

20. The method of claim 18, wherein said medicament is administered parenterally or orally.

21. The method of claim 18, wherein said medicament is administered intravenously or intramuscularly.

22. The method of claim 18, wherein said medicament is administered via injection.

23. The method of claim 18, wherein said medicament is administered via infusion.

24. The method of claim 18, wherein said medicament is administered in the form of a single dose.

25. The method of claim 24, wherein said single dose comprises from 500 to 1000 mg of iron.

26. The method of claim 25, wherein said single dose is applied during the course of one hour.