Claims for Patent: 10,414,831

Summary for Patent: 10,414,831

Title:	Stable iron oligosaccharide compound
Abstract:	The invention relates to an iron oligosaccharide compound with improved stability comprising a hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, the content of dimes saccharide in said hydrogenated oligosaccharide being 2.9% by weight or less, based on the total weight of the hydrogenated oligosaccharide. In further aspects is provided a process for preparing said compound as well as the use of said compound for preparation of a composition for treatment of iron deficiency anaemia.
Inventor(s):	Andreasen; Hans (Holb.ae butted.k, DK)
Assignee:	PHARMACOSMOS HOLDING A/S (Holb.ae butted.k, DK)
Application Number:	16/178,943
Patent Claims:	1. A hydrogenated oligosaccharide, which hydrogenated oligosaccharide when combined with ferric oxyhydroxide is capable of forming a stable iron oligosaccharide compound, wherein said hydrogenated oligosaccharide comprises a mixture of hydrogenated dextran oligosaccharides having the following molecular weight distribution: (i) a weight average molecular weight (Mw) between 500 and 3,000 Daltons, (ii) a dimer saccharide content of 2.9% by weight or less, based on the total weight of the hydrogenated oligosaccharide, (iii) a number average molecular weight (Mn) above 500 Daltons; (iv) 90% by weight of said hydrogenated dextran oligosaccharides have molecular weights of less than 3,500 Daltons, and (v) the Mw of the 10% by weight fraction containing the hydrogenated dextran oligosaccharides having the highest molecular weights is below 4,500 Daltons. 2. An iron oligosaccharide compound comprising a hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, wherein said hydrogenated oligosaccharide comprises a mixture of hydrogenated dextran oligosaccharides having the following molecular weight distribution: (i) a weight average molecular weight (Mw) between 500 and 3,000 Daltons, (ii) a number average molecular weight (Mn) above 500 Daltons; (iii) 90% by weight of said hydrogenated dextran oligosaccharides have molecular weights of less than 3,500 Daltons, and (iv) the Mw of the 10% by weight fraction containing the hydrogenated dextran oligosaccharides having the highest molecular weights is below 4,500 Daltons, (v) a dimer saccharide content of 2.9% by weight or less, based on the total weight of the hydrogenated oligosaccharide, and wherein the apparent molecular weight (M.sub.P) of the iron oligosaccharide compound is between 120,000 and 180,000 Daltons. 3. The iron oligosaccharide compound of claim 2, wherein the M.sub.P of the iron oligosaccharide compound is between 130,000 and 180,000 Daltons. 4. The iron oligosaccharide compound of claim 2, wherein the M.sub.P of the iron oligosaccharide compound is between 130,000 and 160,000 Daltons. 5. The iron oligosaccharide compound of claim 2, wherein the M.sub.P of the iron oligosaccharide compound is measured by size exclusion chromatography. 6. The iron oligosaccharide compound of claim 2, wherein said iron oligosaccharide compound is sterilized by autoclaving. 7. The iron oligosaccharide compound of claim 2, wherein the Mw of said hydrogenated oligosaccharide is 1,600 Daltons or less. 8. The iron oligosaccharide compound of claim 2, wherein the Mn of said hydrogenated oligosaccharide is 1,600 Daltons or less. 9. The iron oligosaccharide compound of claim 2, wherein 90% by weight of said hydrogenated dextran oligosaccharides have molecular weights of less than 2,700 Daltons. 10. The iron oligosaccharide compound of claim 2, wherein the Mw of the 10% by weight fraction containing the hydrogenated dextran oligosaccharides having the highest molecular weights is below 3,200 Daltons. 11. The iron oligosaccharide compound of claim 2, wherein the content of dimer saccharide in the hydrogenated oligosaccharide is 2.5% by weight or less, based on the total weight of the hydrogenated oligosaccharide. 12. The iron oligosaccharide compound of claim 2, wherein the content of dimer saccharide in the hydrogenated oligosaccharide is 2.3% by weight or less, based on the total weight of the hydrogenated oligosaccharide. 13. The iron oligosaccharide compound of claim 2, wherein the content of monomer saccharide in said hydrogenated oligosaccharide is 0.5% by weight or less, based on the total weight of the hydrogenated oligosaccharide. 14. The iron oligosaccharide compound of claim 2, wherein the amount of iron (Fe) in the iron oligosaccharide compound is more than 10% by weight and is 50% by weight or less. 15. The iron oligosaccharide compound of claim 2, further comprising the salt of an organic hydroxy acid. 16. The iron oligosaccharide compound of claim 15, wherein the organic hydroxy acid is citric acid. 17. A composition comprising the iron oligosaccharide compound of claim 2 and at least one pharmaceutically acceptable carrier. 18. The composition of claim 17, wherein said composition has an iron content of 1-20% w/v. 19. The composition of claim 17, wherein said composition has an iron content of 10% w/v. 20. The composition of claim 18, which is an injection liquid adapted for administration in a human. 21. The composition of claim 19, which is an injection liquid adapted for administration in a human. 22. The composition of claim 20, which is an aqueous liquid comprising the iron oligosaccharide compound in dissolved or dispersed form. 23. The composition of claim 21, which is an aqueous liquid comprising the iron oligosaccharide compound in dissolved or dispersed form. 24. An iron oligosaccharide compound comprising a hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, wherein said hydrogenated oligosaccharide comprises a mixture of hydrogenated dextran oligosaccharides having the following molecular weight distribution: (i) a weight average molecular weight (Mw) between 500 and 1,600 Daltons, (ii) a number average molecular weight (Mn) is above 500 Daltons, (iii) 90% by weight of said hydrogenated dextran oligosaccharides have molecular weights of less than 2,700 Daltons, (iv) the Mw of the 10% by weight fraction of the hydrogenated dextran oligosaccharides having the highest molecular weights is below 3,200 Daltons, and (v) a dimer saccharide content of 2.3% by weight or less, based on the total weight of the hydrogenated oligosaccharide, (vi) the content of monomer saccharide in said hydrogenated oligosaccharide is 0.5% by weight or less, based on the total weight of the hydrogenated oligosaccharide, and wherein the apparent molecular weight (M.sub.P) of the iron oligosaccharide compound is 130,000 to 160,000 Daltons. 25. The iron oligosaccharide compound of claim 24, wherein the Mw of said hydrogenated oligosaccharide is approximately 1,000 Daltons. 26. The iron oligosaccharide compound of claim 24, wherein the amount of iron (Fe) in the iron oligosaccharide compound is 25% by weight. 27. The iron oligosaccharide compound of claim 24, further comprising the salt of an organic hydroxy acid. 28. The iron oligosaccharide compound of claim 27, wherein the organic hydroxy acid is citric acid. 29. A composition comprising an injection liquid adapted for administration in a human which comprises the iron oligosaccharide compound of claim 24 in an amount of 1-20% (w/v) iron and at least one pharmaceutically acceptable carrier. 30. The composition of claim 29, which is an aqueous liquid comprising the iron oligosaccharide compound in dissolved or dispersed form.