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 70% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 45 minutes, and about 100% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 120 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. 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 about 100% by weight of the tranexamic acid or pharmaceutically acceptable salt thereof released at about 120 minutes.
21. The tranexamic acid tablet formulation of claim 20 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
22. The tranexamic acid tablet formulation of claim 20 , wherein formulation provides a dose of about 650 mg of tranexamic acid per tablet.
23. The tranexamic acid tablet formulation of claim 22 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
24. The tranexamic acid tablet formulation of claim 20 , wherein the modified release material comprises hydroxypropylmethylcellulose.
25. The tranexamic acid tablet formulation of claim 24 , wherein formulation provides a dose of about 650 mg of tranexamic acid per tablet.
26. The tranexamic acid tablet formulation of claim 25 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
27. The tranexamic acid tablet formulation 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.
28. The tranexamic acid tablet formulation of claim 27 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
29. The tranexamic acid tablet formulation of claim 28 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
30. The tranexamic acid tablet formulation 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.
31. The tranexamic acid tablet formulation 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.
32. The tranexamic acid tablet formulation of claim 20 , wherein the modified release material is present in an amount from about 10% to about 35% by weight of the formulation.
33. The tranexamic acid tablet formulation 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.
34. The tranexamic acid tablet formulation of claim 33 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
35. The tranexamic acid tablet formulation of claim 33 , wherein the modified release material comprises hydroxypropylmethylcellulose.
36. The tranexamic acid tablet formulation of claim 35 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
37. An oral dosage form comprising a tranexamic acid tablet formulation according to claim 1 coated with a film.
38. The oral dosage form of claim 37 , 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.
39. The oral dosage form of claim 37 , wherein the film comprises a film-forming agent forming agent that comprises a (diethylaminoethyl)methacrylate/methyl-butyl-methacrylate copolymer.
40. The oral dosage form of claim 39 , wherein the film forming agent comprises Eudragit E.
41. The oral dosage form of claim 37 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
42. The oral dosage form of claim 37 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
43. The oral dosage form of claim 42 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
44. The oral dosage form of claim 37 , wherein the modified release material comprises hydroxypropylmethylcellulose.
45. The oral dosage form of claim 44 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
46. The oral dosage form of claim 45 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
47. The oral dosage form of claim 37 , wherein the formulation is in the form of a matrix tablet which comprises a drug mixed together with a granulated modified release material.
48. The oral dosage form of claim 47 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
49. The oral dosage form of claim 48 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
50. The oral dosage form of claim 37 , 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.
51. The oral dosage form of claim 37 , 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.
52. The oral dosage form of claim 37 , wherein the modified release material is present in an amount from about 10% to about 35% by weight of the formulation.
53. The oral dosage form of claim 37 , 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.
54. The oral dosage form of claim 53 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
55. The oral dosage form of claim 53 , wherein the modified release material comprises hydroxypropylmethylcellulose.
56. The oral dosage form of claim 55 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
57. An oral dosage form comprising a tranexamic acid tablet formulation according to claim 20 coated with a film.
58. The oral dosage form of claim 57 , 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.
59. The oral dosage form of claim 57 , wherein the film comprises a film-forming agent forming agent that comprises a (diethylaminoethyl)methacrylate/methyl-butyl-methacrylate copolymer.
60. The oral dosage form of claim 59 , wherein the film forming agent comprises Eudragit E.
61. The oral dosage form of claim 57 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
62. The oral dosage form of claim 57 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
63. The oral dosage form of claim 62 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
64. The oral dosage form of claim 57 , wherein the modified release material comprises hydroxypropylmethylcellulose.
65. The oral dosage form of claim 64 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
66. The oral dosage form of claim 65 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
67. The oral dosage form of claim 57 , wherein the formulation is in the form of a matrix tablet which comprises a drug mixed together with a granulated modified release material.
68. The oral dosage form of claim 67 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
69. The oral dosage form of claim 68 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
70. The oral dosage form of claim 57 , 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.
71. The oral dosage form of claim 57 , 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.
72. The oral dosage form of claim 57 , wherein the modified release material is present in an amount from about 10% to about 35% by weight of the formulation.
73. The oral dosage form of claim 57 , 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.
74. The oral dosage form of claim 73 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
75. The oral dosage form of claim 73 , wherein the modified release material comprises hydroxypropylmethylcellulose.
76. The oral dosage form of claim 75 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
77. 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.
78. 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 20 , wherein the formulation provides a dose of about 650 mg of tranexamic acid per tablet.
79. A method of treating menorrhagia comprising administering to a patient in need of such treatment at least one oral dosage form according to claim 37 , wherein the oral dosage form provides a dose of about 650 mg of tranexamic acid.
80. A method of treating menorrhagia comprising administering to a patient in need of such treatment at least one oral dosage form according to claim 57 , wherein the oral dosage form provides a dose of about 650 mg of tranexamic acid.