TRANEXAMIC ACID FORMULATIONS
Disclosed are modified release oral tranexamic acid formulations and methods of treatment therewith.
1 . A tranexamic acid 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 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.
2 . The 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.
3 . The formulation of claim 1 , wherein the formulation releases about 10% to about 25% by weight of the 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° C.
4 . The formulation of claim 1 , wherein the formulation releases about 1% of the tranexamic acid or pharmaceutically acceptable salt thereof every minute when measured in-vitro utilizing the USP 27 Apparatus Type II paddle method at 50 RPM in 900 ml water at 37±0.5° C.
5 . The formulation of claim 1 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
6 . The formulation of claim 1 , wherein a mean maximum plasma concentration (C max ) of tranexamic acid of from about 5 to about 17.5 mcg/ml is provided following administration of two oral dosage forms of the formulation, each providing a dose of about 650 mg of tranexamic acid.
7 . The formulation of claim 1 , wherein the formulation is in the form of an oral dosage form.
8 . The formulation of claim 8 , wherein the oral dosage form provides a dose of about 650 mg of tranexamic acid.
9 . The formulation of claim 9 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
10 . The 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 formulation of claim 10 , wherein the tablet provides a dose of about 650 mg of tranexamic acid.
12 . The formulation of claim 11 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
13 . The 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 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.
16 . The 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.
17 . The 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 modified release material is present in an amount from about 10% to about 35% 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 tablet provides a dose of about 650 mg of tranexamic acid.
18 . The formulation of claim 17 , wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.
19 . A method of treating menorrhagia comprising administering to a patient in need of such treatment the tranexamic acid formulation of claim 1 , wherein the formulation is in the form of at least one oral dosage form, each providing a dose of about 650 mg of tranexamic acid.
20 . A method of treating menorrhagia comprising administering to a patient in need of such treatment the tranexamic acid formulation of claim 1 , wherein the formulation is in the form of at least one matrix tablet which comprises a granulated drug mixed together with the modified release material and each tablet provides a dose of about 650 mg of tranexamic acid.