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Claims for Patent: 7,229,636

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Claims for Patent: 7,229,636

Title:Cyanocobalamin low viscosity aqueous formulations for intranasal delivery
Abstract:A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum.times.100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.
Inventor(s): Quay; Steven C. (Edmonds, WA), Aprile; Peter C. (East Northport, NY), Go; Zenaida O. (Clifton, NJ), Sileno; Anthony P. (Brookhaven Hamlet, NY)
Assignee: Nastech Pharmaceutical Company Inc. (Bothell, WA)
Application Number:10/787,385
Patent Claims: 1. A stable pharmaceutical aqueous solution of cyanocobalamin comprised of cyanocobalamin and water, a preservative selected from the group consisting of benzyl alcohol, parabens thimerosal, chlorobutanol, benzethonium chloride, and benzalkonium chloride, and combinations thereof, a buffer selected from the group consisting of citric acid, sodium citrate, monopotassium phosphate, disodium phosphate, potassium biphthalate, sodium hydroxide, sodium acetate, acetic acid, and combinations thereof, and a humectant selected from the group consisting of sorbitol, propylene glycol, and glycerin, and combinations thereof, wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution contains no mercury or mercury compounds.

2. The aqueous solution of cyanocobalamin of claim 1, wherein the solution is comprised of citric acid, and sodium citrate and water and has a pH of about 4-6.

3. The aqueous solution of claim 2 wherein the pH of the solution is about 5.

4. The aqueous solution of claim 2 further comprised of claim 1 wherein the humectant is propylene glycol.

5. The aqueous solution of claim 1 wherein the humectant is sorbitol.

6. The aqueous solution of claim 1 wherein the humectant is glycerin.

7. The aqueous solution of claim 6 wherein the glycerin is present at a concentration of about 2.23%.

8. The aqueous solution of claim 2 wherein the preservative is selected from the group consisting of benzyl alcohol, chlorobutanol and benzalkonium chloride.

9. The aqueous solution of claim 8 wherein the preservative includes chlorobutanol.

10. The aqueous solution of claim 9 wherein the preservative includes benzalkonium chloride.

11. The aqueous solution of claim 10 wherein the benzalkonium chloride is present in solution at a concentration of about 0.02%.

12. The aqueous solution of claim 2 wherein cyanocobalamin is present at about concentration 0.5% percent of total weight, citric acid is present at a concentration of about 0.12%, and sodium citrate is present at a concentration of about 0.32%.

13. The aqueous solution of claim 12 wherein the pH of the solution is about 5.

14. The aqueous solution of claim 12 wherein the humectant includes sorbital.

15. The aqueous solution of claim 14 wherein the humectant includes propylene glycol.

16. The aqueous solution of claim 15 wherein the humectant includes glycerin.

17. The aqueous solution of claim 16 wherein glycerin is present in solution at a concentration of about 2.23%.

18. The aqueous solution of claim 12 wherein the preservative is selected from the group consisting of benzyl alcohol chlorobutanol and benzalkonium chloride.

19. The aqueous solution of claim 18 wherein the preservative includes chlorobutanol.

20. The aqueous solution of claim 19 wherein the preservative includes benzalkonium chloride.

21. The aqueous solution of claim 20 wherein the benzalkonium chloride is present in solution at a concentration of about 0.02%.

22. The aqueous solution of claim 1 wherein the solution of cyanocobalamin has at least about 12% bioavailability relative to an intramuscular injection of cyanocobalamin.

23. A stable pharmaceutical aqueous solution of cyanocobalamin comprised of cyanocobalamin at a concentration of about 0.5% of total weight of solution, citric acid at a concentration of about 0.12%, sodium citrate at a concentration of about 0.32%, glycerin at a concentration of about 2.23%, benzalkonium chloride at concentration of about 0.02% and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that mercury and mercury containing compounds are not present.

24. A method for administering cyanocobalamin comprised of infusing the nose with an aqueous solution of cyanocobalamin, wherein the solution of cyanocobalamin comprises a preservative selected from the group consisting of benzyl alcohol, parabens thimerosal, chlorobutanol, benzethonium chloride, and benzalkonium chloride, and combinations thereof, a buffer selected from the group consisting of citric acid, sodium citrate, monopotassium phosphate, disodium phosphate, potassium biphthalate, sodium hydroxide, sodium acetate, and acetic acid, combinations thereof, and a humectant selected from the group consisting of sorbitol, propylene glycol, and glycerin, and combinations thereof, and has a viscosity of less than 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin of about 7% relative to an intramuscular injection of cyanocobalamin, with the proviso that mercury and mercury containing compounds are not present in the solution.

25. The method of claim 24 wherein the buffer includes citric acid and sodium citrate wherein the solution has a pH of from about 4-6.

26. The method of claim 25 wherein the pH of the solution is about 5.

27. The method of claim 25 wherein cyanocobalamin is present in solution at a concentration of between 0.5-1% by weight.

28. The method of claim 27 wherein the concentration of cyanocobalamin in solution is about 0.5%.

29. The method of claim 25 wherein the citric acid is present in solution at a concentration of about 0.12%, and the sodium citrate is present in solution at a concentration of about 0.32%, in water.

30. A method for administering cyanocobalamin comprised of infusing the nose with an aqueous solution of cyanocobalamin wherein said aqueous solution of cyanocobalamin is comprised of cyanocobalamin at a concentration of about 0.5% of total weight of solution, citric acid at a concentration of about 0.12%, sodium citrate at a concentration of about 0.32%, glycerin at a concentration of about 2.23%, benzalkonium chloride at concentration of about 0.02% and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin, with the proviso that the solution of cyanocobalamin contains no mercury or mercury-containing compounds.

31. A method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a solution of cyanocobalamin so that the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum.times.100) is increased to at least about 1.1, wherein said aqueous solution of cyanocobalamin is comprised of cyanocobalamin at a concentration of about 0.5% of total weight of solution, citric acid at a concentration of about 0.12%, sodium citrate at a concentration of about 0.32%, glycerin at a concentration of about 2.23%, benzalkonium chloride at concentration of about 0.02% and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin, with the proviso that the cyanocobalamin solution contains no mercury or mercury-containing compounds.
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