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Claims for Patent: 8,957,113

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Claims for Patent: 8,957,113

Title:Tranexamic acid formulations
Abstract: Disclosed are immediate release oral tranexamic acid formulations and methods of treatment therewith.
Inventor(s): Moore; Keith A. (Loveland, OH), Heasley; Ralph A. (Webster Grove, MN), Greiwe; Jeffrey S. (Ft. Thomas, KY), Facemire; John W. (Douglasville, GA), Modest; Jason D. (Minneapolis, MN)
Assignee: Ferring B.V. (Hoofddorp, NL)
Application Number:13/016,800
Patent Claims: 1. An oral dosage form comprising tranexamic acid or a pharmaceutically acceptable salt thereof, present in an amount that provides a dose of about 650 mg of tranexamic acid, and a pharmaceutically acceptable excipient; said dosage form providing 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@50 RPM in 900 ml water at 37.+-.0.5.degree. C., wherein from about 0% to 95% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released by about 15 minutes; from about 30% to about 95% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released by about 30 minutes; from about 70% to about 95% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released by about 45 minutes; and about 100% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released at about 60 minutes.

2. The oral dosage form of claim 1, wherein the dosage form provides a mean transit time of said tranexamic acid of 7.21.+-.1.01 hours when orally administered across a patient population after single dose oral administration providing a 1300 mg dose of tranexamic acid.

3. The oral dosage form of claim 1, wherein the dosage form provides a mean absorption time of said tranexamic acid of 3.70.+-.0.94 hours when orally administered across a patient population after single dose oral administration providing a 1300 mg dose of tranexamic acid.

4. The oral dosage form of claim 1, wherein the pharmaceutically acceptable excipient comprises a diluent.

5. The oral dosage form of claim 4, wherein said diluent is selected from the group consisting of dextrose, sucrose, starch, powdered cellulose, lactose, mannitol, microcrystalline cellulose, and combinations thereof.

6. The oral dosage form of claim 1, wherein the pharmaceutically acceptable excipient comprises a glidant, a surface active agent, a coloring agent, a flavoring agent, a lubricant, or combination thereof.

7. A method of treating a patient in need of tranexamic acid therapy for treating menorrhagia comprising orally administering to said patient a dose of two oral dosage forms according to claim 1.

8. The method of claim 7, wherein said oral dosage forms provide a mean time to maximum plasma concentration (T.sub.max) at about 2 to about 4 hours after single dose oral administration providing a 1300 mg dose of tranexamic acid to humans.

9. The method of claim 7, wherein the dosage forms provides a mean transit time of said tranexamic acid of 7.21.+-.1.01 hours after single dose oral administration providing a 1300 mg dose of tranexamic acid to humans.

10. The method of claim 7, wherein the oral dosage form of claim 7, wherein the dosage form provides a mean absorption time of said tranexamic acid of 3.70.+-.0.94 hours after single dose oral administration providing a 1300 mg dose of tranexamic acid to humans.

11. The method of claim 7, wherein said oral dosage forms provide a mean maximum plasma concentration (C.sub.max) of tranexamic acid of about 9 to about 15 mcg/ml after single dose oral administration providing a 1300 mg dose of tranexamic acid to humans.

12. The method of claim 7, wherein the dosage forms are administered to said patient three times a day.

13. The method of claim 7, wherein the pharmaceutically acceptable excipient comprises a diluent.

14. The method of claim 13, wherein said diluent is selected from the group consisting of dextrose, sucrose, starch, powdered cellulose, lactose, mannitol, microcrystlline cellulose, and combinations thereof.

15. The method of claim 7, wherein the pharmaceutically acceptable excipient comprises a glidant, a surface active agent, a coloring agent, a flavoring agent, a lubricant, or combination thereof.

16. An oral dosage form according to claim 1, said dosage form providing a bioavailability of said tranexamic acid of greater than 40%.

17. The dosage form according to claim 1, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is in the form of a tablet.

18. The dosage form according to claim 1, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

19. The dosage form according to claim 18, wherein the tranexamic acid is present in an amount from about 50% by weight to about 95% by weight of the dosage form.

20. The dosage form according to claim 19, wherein the tranexamic acid is present in an amount from about 60% by weight to about 90% by weight of the dosage form.

21. The dosage form according to claim 1, wherein the dosage form is coated with a film.

22. The dosage form according to claim 1, wherein said the film comprises one or more film forming agents selected from hydroxypropyl cellulose, a cellulose ester, a cellulose ether, one or more acrylic polymers, hydroxypropyl methylcellulose, and cationic methacrylate copolymers.

23. An oral dosage form comprising tranexamic acid or a pharmaceutically acceptable salt thereof, present in an amount that provides a dose of about 650 mg of tranexamic acid, and a pharmaceutically acceptable excipient; said dosage form providing 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@50 RPM in 900 ml water at 37.+-.0.5.degree. C., wherein from about 0% to 95% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released by about 15 minutes; from about 30% to about 100% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released by about 30 minutes; from about 70% to about 100% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released by about 45 minutes; and about 100% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof is released at about 60 minutes.

24. The dosage form according to claim 23, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is in the form of a tablet.

25. The dosage form according to claim 23, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.

26. The dosage form according to claim 25, wherein the tranexamic acid is present in an amount from about 50% by weight to about 95% by weight of the dosage form.

27. The dosage form according to claim 26, wherein the tranexamic acid is present in an amount from about 60% by weight to about 90% by weight of the dosage form.

28. The dosage form according to claim 23, wherein the dosage form is coated with a film.

29. The dosage form according to claim 23, wherein said the film comprises one or more film forming agents selected from hydroxypropyl cellulose, a cellulose ester, a cellulose ether, one or more acrylic polymers, hydroxypropyl methylcellulose, and cationic methacrylate copolymers.

30. A method of treating a patient in need of tranexamic acid therapy for treating menorrhagia comprising orally administering to said patient a dose of two oral dosage forms according to claim 23.
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