Tranexamic acid formulations
View Patent ↗Disclosed are modified release oral tranexamic acid formulations and methods of treatment therewith.
1. A tranexamic acid tablet formulation comprising:
tranexamic acid or a pharmaceutically acceptable salt thereof; and
a modified release material;
wherein the tranexamic acid or pharmaceutically acceptable salt thereof is present in an amount from about 50% to about 95% by weight of the formulation;
wherein the modified release material is present in an amount from about 5% to about 50% by weight of the formulation; and
wherein said tablet formulation 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 @ 50 RPM in 900 ml water at 37±0.5° C., of less than about 40% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 15 minutes, and not less than about 50% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 90 minutes.
2. The tranexamic acid tablet formulation of claim 1 , wherein said tablet formulation 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 @ 50 RPM in 900 ml water at 37±0.5° C., of less than about 40% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 15 minutes, less than about 70% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 45 minutes, and not less than about 50% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 90 minutes.
3. The tranexamic acid tablet formulation of claim 1 , wherein said 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° C., of about 0% to about 40% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 15 minutes, from about 20% to about 60% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 30 minutes, from about 40% to about 65% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 45 minutes, from about 50% to about 95% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 60 minutes, and not less than about 60% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 90 minutes.
4. The tranexamic acid tablet formulation of claim 1 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
5. The tranexamic acid tablet formulation of claim 1 , wherein formulation provides a dose of about 650 mg of tranexamic acid per tablet.
6. The tranexamic acid tablet formulation of claim 5 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
7. The tranexamic acid tablet formulation of claim 1 , wherein the modified release material comprises hydroxypropylmethylcellulose.
8. The tranexamic acid tablet formulation of claim 7 , wherein formulation provides a dose of about 650 mg of tranexamic acid per tablet.
9. The tranexamic acid tablet formulation of claim 8 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
10. The tranexamic acid tablet formulation of claim 1 , wherein the formulation is in the form of a matrix tablet which comprises a drug mixed together with a granulated modified release material.
11. The tranexamic acid tablet formulation of claim 10 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
12. The tranexamic acid tablet formulation of claim 11 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
13. The tranexamic acid tablet formulation 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 formulation.
14. The tranexamic acid tablet formulation 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 formulation.
15. The tranexamic acid tablet formulation of claim 1 , wherein the modified release material is present in an amount from about 10% to about 35% by weight of the formulation.
16. The tranexamic acid tablet formulation 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 formulation;
the formulation is in the form of a matrix tablet which comprises a granulated drug mixed together with the modified release material and
the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
17. The tranexamic acid tablet formulation of claim 16 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
18. The tranexamic acid tablet formulation of claim 16 , wherein the modified release material comprises hydroxypropylmethylcellulose.
19. The tranexamic acid tablet formulation of claim 18 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
20. An oral dosage form comprising a tranexamic acid tablet formulation according to claim 1 coated with a film.
21. The oral dosage form of claim 20 , wherein the film comprises a film-forming agent present in an amount in the range from about 2% tablet weight to about 4% tablet weight.
22. The oral dosage form of claim 20 , wherein the film comprises a film-forming agent forming agent that comprises a (diethylaminoethyl) methacrylate/methyl-butyl-methacrylate copolymer.
23. The oral dosage form of claim 22 , wherein the film forming agent comprises Eudragit E.
24. The oral dosage form of claim 20 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
25. The oral dosage form of claim 20 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
26. The oral dosage form of claim 25 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
27. The oral dosage form of claim 20 , wherein the modified release material comprises hydroxypropylmethylcellulose.
28. The oral dosage form of claim 27 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
29. The oral dosage form of claim 28 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
30. The oral dosage form of claim 20 , wherein the formulation is in the form of a matrix tablet which comprises a drug mixed together with a granulated modified release material.
31. The oral dosage form of claim 30 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
32. The oral dosage form of claim 31 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
33. The oral dosage form of claim 20 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is present in an amount from about 60% to about 90% by weight of the formulation.
34. The oral dosage form of claim 20 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is present in an amount from about 60% to about 80% by weight of the formulation.
35. The oral dosage form of claim 20 , wherein the modified release material is present in an amount from about 10% to about 35% by weight of the formulation.
36. The oral dosage form of claim 20 , wherein:
the tranexamic acid or pharmaceutically acceptable salt thereof is present in an amount from about 60% to about 90% by weight of the formulation;
the formulation is in the form of a matrix tablet which comprises a granulated drug mixed together with the modified release material and
the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
37. The oral dosage form of claim 36 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
38. The oral dosage form of claim 36 , wherein the modified release material comprises hydroxypropylmethylcellulose.
39. The oral dosage form of claim 38 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
40. A method of treating menorrhagia comprising administering to a patient in need of such treatment at least one tablet of the tranexamic acid formulation of claim 1 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
41. A method of treating menorrhagia comprising administering to a patient in need of such treatment at least one oral dosage form according to claim 20 , wherein the oral dosage form provides a dose of about 650 mg of tranexamic acid.