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Claims for Patent: 7,947,739

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Claims for Patent: 7,947,739

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:12/714,181
Patent Claims: 1. A tranexamic acid tablet formulation, comprising: tranexamic acid or a pharmaceutically acceptable salt thereof; and a modified release material, wherein the modified release material comprises a polymer selected from the group consisting of hydroxyalkylcelluloses, alkylcelluloses, cellulose ethers, partial esters thereof, and mixtures thereof; wherein the modified release material is present in the formulation in an amount from about 10% to about 35% by weight of the formulation; wherein the formulation 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., of less than about 70% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 45 minutes, and about 100% by weight tranexamic acid or pharmaceutically acceptable salt thereof released by about 120 minutes; and wherein each tablet of the formulation provides a dose of about 650 mg of tranexamic acid.

2. The tranexamic acid formulation of claim 1, wherein the formulation provides a mean 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., of about 15% to about 29% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 15 minutes, about 56% to about 69% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 45 minutes, and about 89% to about 100% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 90 minutes.

3. The tranexamic acid tablet formulation of claim 1, wherein the tablet is a matrix tablet which comprises a pregranulated drug mixed together with the modified release material.

4. The tranexamic acid tablet formulation of claim 1, wherein the modified release material comprises a hydroxyalkylcellulose or a cellulose ether.

5. The tranexamic acid tablet formulation of claim 1, wherein the modified release material comprises hydroxypropylmethylcellulose.

6. The tranexamic acid tablet formulation of claim 1, wherein the modified release material is present in an amount of about 15% by weight of the formulation.

7. The tranexamic acid tablet formulation of claim 5, wherein the modified release material is present in an amount of about 15% by weight of the formulation.

8. The tranexamic acid tablet formulation of claim 1, wherein a single administration of the formulation comprising a dose of 1300 mg of tranexamic acid provides a mean maximum plasma concentration (C.sub.max) of tranexamic acid in a range from about 9 mcg/ml to about 14.5 mcg/ml following the administration.

9. The tranexamic acid tablet formulation of claim 1, wherein administration of the formulation comprising a dose of 1300 mg of tranexamic acid three times daily provides a mean maximum plasma concentration (C.sub.max) of tranexamic acid in a range from about 12.5 mcg/ml to about 25 mcg/ml after multi-dose administration.

10. The tranexamic acid tablet formulation of claim 1, wherein said formulation provides a mean T.sub.max at from about 2 hours to about 3.5 hours after single dose oral administration.

11. A tranexamic acid tablet formulation, comprising: tranexamic acid or a pharmaceutically acceptable salt thereof; and an effective amount of a modified release material, wherein the modified release material comprises a polymer selected from the group consisting of hydroxyalkylcelluloses, alkylcelluloses, cellulose ethers, partial esters thereof, and mixtures thereof; wherein the modified release material is present in the formulation in an amount from about 10% to about 35% by weight of the formulation; wherein the formulation releases from about 10% to about 25% by weight tranexamic acid or pharmaceutically acceptable salt thereof every 15 minutes when measured in vitro utilizing the USP 27 Apparatus Type II Paddle Method @ 50 RPM in 900 ml water at 37.+-.0.5.degree. C. such that about 100% of tranexamic acid or pharmaceutically acceptable salt thereof is released by about 120 minutes; and wherein each tablet of the formulation provides a dose of about 650 mg of tranexamic acid.

12. The tranexamic acid tablet formulation of claim 1, wherein administration of the formulation comprising a dose of 1300 mg of tranexamic acid three times daily provides a mean maximum plasma concentration (C.sub.max) of about 10 mcg/ml to about 20 mcg/ml after multi-dose administration.

13. The tranexamic acid tablet formulation of claim 1, wherein a single administration of the formulation comprising a dose of 1300 mg of tranexamic acid provides a mean maximum plasma concentration (C.sub.max) of tranexamic acid in a range from about 9 mcg/ml to about 17.5 mcg/ml.

14. The tranexamic acid tablet formulation of claim 5, wherein the hydroxypropylmethylcellulose is present in an amount of about 10% to about 35% by weight of the formulation.

15. The tranexamic acid tablet formulation of claim 14, wherein the hydroxypropylmethylcellulose is present in an amount of about 15% by weight of the formulation.

16. A tranexamic acid tablet formulation, comprising: tranexamic acid or a pharmaceutically acceptable salt thereof; and hydroxypropylmethylcellulose in an amount from about 10% to about 35% by weight of the formulation; wherein the formulation 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., of less than about 70% by weight tranexamic acid or pharmaceutically acceptable salt thereof released at about 45 minutes, and about 100% by weight tranexamic acid or pharmaceutically acceptable salt thereof released by about 120 minutes; and wherein each tablet of the formulation provides a dose of about 650 mg of tranexamic acid.

17. The tranexamic acid tablet formulation of claim 16, wherein the hydroxypropylmethylcellulose is present in an amount of about 15% by weight of the formulation.

18. A tranexamic acid tablet formulation according to claim 11, comprising: tranexamic acid or a pharmaceutically acceptable salt thereof; and hydroxypropylmethylcellulose in an amount from about 10% to about 35% by weight of the formulation; wherein the formulation releases from about 10% to about 25% by weight tranexamic acid or pharmaceutically acceptable salt thereof every 15 minutes when measured in vitro utilizing the USP 27 Apparatus Type II Paddle Method @ 50 RPM in 900 ml water at 37.+-.0.5.degree. C. such that about 100% of tranexamic acid or pharmaceutically acceptable salt thereof is released by about 120 minutes; and wherein each tablet of the formulation provides a dose of about 650 mg of tranexamic acid.

19. The tranexamic acid tablet formulation of claim 18, wherein the hydroxypropylmethylcellulose is present in an amount of about 15% by weight of the formulation.
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