Tranexamic acid formulations
View Patent ↗Disclosed are immediate release oral tranexamic acid formulations and methods of treatment therewith.
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° 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 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 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° 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 .