Claims for Patent: 11,851,504

Summary for Patent: 11,851,504

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 dimer 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):	Hans Andreasen
Assignee:	Pharmacosmos Holding AS
Application Number:	US17/142,442
Patent Claims:	1. An iron oligosaccharide compound comprising a hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, the hydrogenated oligosaccharide having a weight average molecular weight (Mw) of less than 3,000 Daltons, wherein the iron oligosaccharide compound has an in vitro half-life of 18.3 hours or more, and further wherein the hydrogenated oligosaccharide is derived from dextran. 2. The compound according to claim 1, wherein the in vitro half-life of the iron oligosaccharide compound is measured by the rate of hydrolysis of Fe3+ in 0.24 M HCI; 0.9% NaCl acidic solution, wherein the hydrolysis of Fe3+ is measured by optical absorbance at 287.3 nm and the half-life is the time at which the absorbance is half of the value compared to the absorbance at t=0. 3. The compound according to claim 1, wherein the apparent molecular weight (MP) of said compound is 120,000 to 180,000 Daltons, measured on an autoclaved aqueous solution prepared by dissolving in 1,000 ml water 400 g powder of hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, the amount of iron (Fe) of the powder being 25% by weight. 4. The compound according to claim 3, wherein the apparent molecular weight (MP) of said compound is 130,000 to 180,000 Daltons. 5. The compound according to claim 4, wherein the apparent molecular weight (MP) of said compound is 130,000 to 160,000 Daltons. 6. The compound according to claim 1, wherein said hydrogenated oligosaccharide has a weight average molecular weight (Mw) between 500 and 3,000 Daltons, a number average molecular weight (Mn) above 500 Daltons, wherein 90% by weight of said hydrogenated oligosaccharide has molecular weights less than 3,500 Daltons, and the Mw of the 10% by weight fraction of the hydrogenated oligosaccharide having the highest molecular weights is below 4,500 Daltons. 7. The compound according to claim 6, wherein the Mw of the hydrogenated oligosaccharide is between 850 and 1,150 Daltons. 8. The compound according to claim 1, wherein 90% by weight of the hydrogenated oligosaccharide have a molecular weight of less than 2,700 Daltons. 9. The compound according to claim 1, wherein the 10% fraction of said hydrogenated oligosaccharide having the highest molecular weight has a weight average molecular weight (Mw) of less than 3,200 Daltons. 10. The compound according to claim 1, wherein the weight average molecular weight (Mw) of the hydrogenated oligosaccharide is 1,600 Daltons or less. 11. The compound according to claim 10, wherein the weight average molecular weight (Mw) of the hydrogenated oligosaccharide is approximately 1,000 Daltons. 12. The compound according to claim 1, wherein the amount of iron (Fe) in the iron oligosaccharide compound is 10-50% by weight. 13. The compound according to claim 1, wherein the content of dimer saccharide in the hydrogenated oligosaccharide is 2.9% by weight or less, based on the total weight of the hydrogenated oligosaccharide. 14. The compound according to claim 13, 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. 15. The compound according to claim 14, 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. 16. The compound according to claim 1, 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. 17. A composition comprising a pharmacologically effective amount of a compound according to claim 1, and at least one pharmaceutically acceptable carrier. 18. The composition according to claim 17, wherein the composition has an iron content of 1-50% w/v. 19. The composition according to claim 18, wherein said composition has an iron content of 1-20% w/v. 20. The composition according to claim 19, wherein said composition has an iron content of 10% w/v. 21. The composition according to claim 20, which is an aqueous liquid comprising the iron oligosaccharide compound in dissolved or dispersed form. 22. An iron oligosaccharide compound comprising a hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, the monomer units of the hydrogenated oligosaccharide being joined by α 1,6-glucosidic bonds and the hydrogenated oligosaccharide having a weight average molecular weight (Mw) of between 850 and 1,150 Daltons, wherein the iron oligosaccharide compound has an in vitro half-life of 18.3 hours or more and wherein the apparent molecular weight (MP) of said compound is 130,000 to 160,000 Daltons. 23. An iron oligosaccharide compound comprising a hydrogenated oligosaccharide in stable association with ferric oxyhydroxide, the hydrogenated oligosaccharide having a weight average molecular weight (Mw) of less than 3,000 Daltons, and further wherein the iron oligosaccharide compound has an in vitro half-life of 18.3 hours or more, and the hydrogenated oligosaccharide is a hydrogenated dextran oligosaccharide. 24. The compound according to claim 1, wherein the iron oligosaccharide compound has an in vitro half-life of 20.9 hours or more, 21.6 hours or more, 21.7 hours or more, 22.5 hours or more, or 25.5 hours or more. 25. The compound according to claim 22, wherein the iron oligosaccharide compound has an in vitro half-life of 20.9 hours or more, 21.6 hours or more, 21.7 hours or more, 22.5 hours or more, or 25.5 hours or more. 26. The compound according to claim 23, wherein the iron oligosaccharide compound has an in vitro half-life of 20.9 hours or more, 21.6 hours or more, 21.7 hours or more, 22.5 hours or more, or 25.5 hours or more.