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Claims for Patent: 9,060,939

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Claims for Patent: 9,060,939

Title:Tranexamic acid formulations
Abstract: Disclosed are modified release oral tranexamic acid formulations and methods of treatment therewith.
Inventor(s): Moore; Keith A. (Loveland, OH), Heasley; Ralph A. (Webster Grove, MO), Greiwe; Jeffrey S. (Ft. Thomas, KY), Facemire; John W. (Douglasville, GA), Modest; Jason D. (Minneapolis, MN)
Assignee: Ferring B.V. (Hoofddorp, NL)
Application Number:13/230,902
Patent Claims: 1. A dosage form comprising tranexamic acid or a pharmaceutically acceptable salt thereof; and hydroxypropylmethylcellulose in an amount from about 5% to about 35% of the dosage form; wherein the dosage form is suitable for oral administration on a two or three times a day basis; wherein the dosage form provides a dose of about 650 mg of tranexamic acid; and wherein the dosage form provides an in vitro dissolution release rate of the tranexamic acid or pharmaceutically acceptable salt thereof, when measured by a USP 27 Apparatus Type II Paddle Method at 50 RPM in 900 ml water at 37.+-.0.5.degree. C., wherein from about 0 to about 40% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released at about 15 minutes; and less than about 70% by weight tranexamic acid or pharmaceutically acceptable salt thereof is released at about 45 minutes.

2. The dosage form of claim 1, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

3. The dosage form of claim 1, wherein the dosage form is in the form of a matrix tablet which comprises tranexamic acid, or a pharmaceutically acceptable salt thereof together with the hydroxypropylmethylcellulose.

4. The dosage form of claim 3, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

5. The dosage form of claim 1, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is present in an amount from about 60% to about 90% by weight of the dosage form.

6. The dosage form of claim 5, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

7. The dosage form of claim 1, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is present in an amount from about 60% to about 80% by weight of the dosage form.

8. The dosage form of claim 7, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

9. The dosage form of claim 1, wherein the hydroxypropylmethylcellulose is present in an amount from about 5% to about 30% by weight of the dosage form.

10. The dosage form of claim 9, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

11. The dosage form of claim 9, wherein the dosage form is in the form of a matrix tablet which comprises tranexamic acid, or a pharmaceutically acceptable salt thereof together with the hydroxypropylmethylcellulose.

12. The dosage form of claim 11, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

13. The dosage form of claim 1, wherein the hydroxypropylmethylcellulose is present in an amount from about 5% to about 10% by weight of the dosage form.

14. The dosage form of claim 13, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

15. The dosage form of claim 13, wherein the dosage form is in the form of a matrix tablet which comprises tranexamic acid, or a pharmaceutically acceptable salt thereof together with the hydroxypropylmethylcellulose.

16. The dosage form of claim 15, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

17. The dosage form of claim 1, wherein the hydroxypropylmethylcellulose is present in an amount from about 10% to about 30% by weight of the dosage form.

18. The dosage form of claim 17, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

19. The dosage form of claim 1, wherein the hydroxypropylmethylcellulose is present in an amount of about 15% by weight of the dosage form.

20. The dosage form of claim 19, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

21. The dosage form of claim 1, wherein said dosage form provides an in vitro dissolution release rate of the tranexamic acid or pharmaceutically acceptable salt thereof, when measured by the USP 27 Apparatus Type II Paddle Method @ 50 RPM in 900 ml water at 37.+-.0.5.degree. C., wherein about 0% to about 40% by weight tranexamic acid or pharmaceutically acceptable salt thereof released is at about 15 minutes, from about 20% to about 60% by weight tranexamic acid or pharmaceutically acceptable salt thereof is released at about 30 minutes, from about 40% to about 65% by weight tranexamic acid or pharmaceutically acceptable salt thereof is released at about 45 minutes, from about 50% to about 95% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 60 minutes, and not less than about 60% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 90 minutes.

22. The dosage form of claim 1, wherein the dosage form provides a mean maximum plasma concentration (C.sub.max) of tranexamic acid of from about 6.5 to about 15 mcg/ml after single dose oral administration of two of the dosage forms to humans.

23. The dosage form of claim 1, wherein the dosage form provides a mean maximum plasma concentration (C.sub.max) of tranexamic acid of from about 9 to about 14.5 mcg/ml after single dose oral administration of two of the dosage forms to humans.

24. The dosage form of claim 1, which provides a mean maximum plasma concentration (C.sub.max) of tranexamic acid of from about 10 to about 20 mcg/ml after steady state oral administration of about 1300 mg of tranexamic acid or pharmaceutically acceptable salt thereof included in two of the dosage forms to humans.

25. The dosage form of claim 1, which provides mean time to maximum plasma concentration (T.sub.max) at from about 1 to about 5.5 hours after oral administration of one or more of the dosage forms to humans.

26. The dosage form of claim 1, which provides mean time to maximum plasma concentration (T.sub.max) at from about 2 to about 4 hours after oral administration of one or more of the dosage forms to humans.

27. The dosage form of claim 1, which provides mean time to maximum plasma concentration (T.sub.max) at from about 2 to about 3.5 hours after oral administration of one or more of the dosage forms to humans.

28. The dosage form of claim 1, wherein the dosage form provides a mean transit time of said tranexamic acid of 7.70.+-.0.72 hours when orally administered across a patient population.

29. The dosage form of claim 1, wherein the dosage form provides a mean absorption time of said tranexamic acid of 4.18.+-.0.70 hours when orally administered across a patient population.

30. The dosage form of claim 1, which provides for a bioavailability of greater than 40% after oral administration to humans.

31. A method of treating menorrhagia comprising administering to a patient in need of such treatment a dosage form according to claim 1.

32. The method of claim 31, comprising orally administering to a patient in need of such treatment two of the dosage forms.

33. The method of claim 31, comprising orally administering to a patient in need of such treatment two of the dosage forms on a two or three times a day basis.

34. The method of claim 31, comprising orally administering to a patient in need of such treatment two of the dosage forms on a three times a day basis.
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