.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 9,415,007

« Back to Dashboard

Details for Patent: 9,415,007

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: PAR PHARMACEUTICAL, INC. (Woodcliff Lake, NJ)
Filing Date:Sep 12, 2014
Application Number:14/485,228
Claims:1. A method for elevating a level of vitamin B12 in a subject having vitamin B12 deficiency associated with gastric surgery, comprising: administering an aqueous solution of cyanocobalamin to the subject having vitamin B12 deficiency associated with gastric surgery, wherein the aqueous solution of cyanocobalamin comprises: cyanocobalamin; water; 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; optionally, a humectant selected from the group consisting of sorbitol, propylene glycol, and glycerin, and combinations thereof; and optionally, a preservative selected from the group consisting of benzyl alcohol, parabens thimerosal, chlorobutanol, benzethonium chloride, and benzalkonium chloride, and combinations thereof; wherein the aqueous solution of cyanocobalamin is suitable for intranasal administration, has a viscosity of less than about 1000 cPs, and a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin.

2. The method of claim 1, wherein the cyanocobalamin is at a concentration of about 0.5% by total weight of solution.

3. The method of claim 1, wherein the buffer comprises citric acid at a concentration of about 0.12% by total weight of solution and sodium citrate at a concentration of about 0.32% by total weight of solution.

4. The method of claim 3, wherein the pH of the aqueous solution of cyanocobalamin is about 4 to about 6.

5. The method of claim 4, wherein the aqueous solution of cyanocobalamin contains a humectant.

6. The method of claim 5, wherein the humectant is glycerin at a concentration of about 2.23% by total weight of solution.

7. The method of claim 1, wherein the aqueous solution of cyanocobalamin contains a preservative.

8. The method of claim 7, wherein the preservative comprises chlorobutanol or benzalkonium chloride, or combinations thereof.

9. The method of claim 8, wherein the preservative is benzalkonium chloride at a concentration of about 0.02% by total weight of solution.

10. The method of claim 1, wherein the aqueous solution of cyanocobalamin contains no mercury or mercury-containing compounds.

11. The method of claim 1, wherein the aqueous solution of cyanocobalamin comprises: cyanocobalamin at a concentration of about 0.5% by total weight of the solution, citric acid at a concentration of about 0.12% by total weight of the solution, sodium citrate at a concentration of about 0.32% by total weight of the solution, glycerin at a concentration of about 2.23% by total weight of the solution, benzalkonium chloride at concentration of about 0.02% by total weight of the solution, and water.

12. The method of claim 1, wherein the aqueous solution of cyanocobalamin comprises: cyanocobalamin at a concentration of about 0.5% by total weight of the solution, citric acid at a concentration of about 0.12% by total weight of the solution, sodium citrate at a concentration of about 0.32% by total weight of the solution, glycerin at a concentration of about 2.23% by total weight of the solution, and water.

13. A method of using a kit for elevating a level of vitamin B12 in a subject having vitamin B12 deficiency associated with gastric surgery, the kit comprising: an aqueous solution of cyanocobalamin in a container; and an actuator coupled to the container, the actuator comprising a tip for producing a spray of the aqueous solution of cyanocobalamin when the actuator is engaged; the method comprising, administering the spray from the tip to a nose of a subject having vitamin B12 deficiency associated with gastric surgery, wherein the aqueous solution of cyanocobalamin comprises: cyanocobalamin; water; 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; optionally, a humectant selected from the group consisting of sorbitol, propylene glycol, and glycerin, and combinations thereof; and optionally, a preservative selected from the group consisting of benzyl alcohol, parabens thimerosal, chlorobutanol, benzethonium chloride, and benzalkonium chloride, and combinations thereof; wherein the aqueous solution of cyanocobalamin has a viscosity of less than about 1000 cPs and a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin.

14. The method of claim 13, wherein the spray has a spray pattern ellipticity ratio of about 1.0 to about 1.4 when measured at a height of 3.0 cm from the actuator tip.

15. The method of claim 13, wherein the spray comprises droplets, and wherein less than about 5% of the droplets are less than about 10 .mu.m in size.

16. The method of claim 13, wherein the spray comprises droplets, and wherein less than about 50% of the droplets are less than about 26.9 .mu.m in size.

17. The method of claim 13, wherein the spray has a spray pattern major axis and minor axis of about 25 to about 40 mm each.

18. The method of claim 13, wherein the cyanocobalamin is at a concentration of about 0.5% by total weight of solution.

19. The method of claim 13, wherein the aqueous solution of cyanocobalamin comprises: cyanocobalamin at a concentration of about 0.5% by total weight of the solution, citric acid at a concentration of about 0.12% by total weight of the solution, sodium citrate at a concentration of about 0.32% by total weight of the solution, glycerin at a concentration of about 2.23% by total weight of the solution, benzalkonium chloride at concentration of about 0.02% by total weight of the solution, and water.

20. The method of claim 13, wherein the aqueous solution of cyanocobalamin comprises: cyanocobalamin at a concentration of about 0.5% by total weight of the solution, citric acid at a concentration of about 0.12% by total weight of the solution, sodium citrate at a concentration of about 0.32% by total weight of the solution, glycerin at a concentration of about 2.23% by total weight of the solution, and water.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc