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Details for Patent: 9,023,878

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Details for Patent: 9,023,878

Title:2-iminobiotin formulations and uses thereof
Abstract: The disclosure relates to improving the aqueous solubility of 2-iminobiotin. In a particular aspect, the invention pertains to formulations suitable for administration of 2-iminobiotin to mammals suffering from disorders or conditions that benefit from said administration.
Inventor(s): Leufkens; Paul W. T. J. ('s-Hertogenbosch, NL)
Assignee: Neurophyxia B.V. ('S-Hertogenbosch, NL)
Filing Date:May 26, 2011
Application Number:13/700,090
Claims:1. An aqueous, soluble formulation of 2-iminobiotin, having a pH between around 3 and around 7, and comprising 0.75 mg or more of 2-iminobiotin and at least 1 mM citric acid, citrate or a mixture of citric acid and citrate.

2. The formulation of claim 1, comprising at least 20 mM of citric acid, citrate, or a mixture of citric acid and citrate.

3. A method of treating perinatal asphyxia in a neonate, the method comprising: utilizing the formulation of claim 1 to treat the neonate.

4. The method according to claim 3, wherein the formulation is administered to the neonate's mother prior to and/or during labor.

5. The method according to claim 4, further comprising: subjecting the neonate to hypotheimia.

6. The method of claim 3, wherein the formulation is administered to the neonate's mother prior to and/or during labor.

7. The method according to claim 3, further comprising: subjecting the neonate to hypothermia.

8. A method of treating a neonate for complications associated with childbirth, the method comprising: administering the formulation of claim 1 to the neonate to treat the effects of complications during childbirth.

9. The method according to claim 8, further comprising: subjecting the neonate to hypothermia.

10. A method of treating a neonate for perinatal asphyxia, the method comprising: administering the formulation of claim 1 to the neonate to treat the perinatal asphyxia, and subjecting the neonate to hypothermia.

11. An aqueous, soluble formulation of 2-iminobiotin, having a pH between 3 and 6, and comprising between 0.5 mg/ml and 5 mg/ml of 2-iminobiotin and at least 1 mM citric acid, citrate or a mixture of citric acid and citrate.

12. The formulation of claim 11, wherein the citric acid, citrate, or mixture of citric acid and citrate is present at a concentration of between 10 mM and 20 mM.

13. An aqueous, soluble formulation of 2-iminobiotin, having a pH between 3 and 7, and comprising: between 0.5 mg/ml to 10 mg/ml of 2-iminobiotin and at least 1 mM citric acid, citrate, or a mixture of citric acid and citrate.

14. The formulation of claim 13 further comprising: between around 2.5 to around 40% of a substituted beta-cyclodextrin.
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