Tranexamic acid formulations

Abstract

Disclosed are modified release oral tranexamic acid formulations and methods of treatment therewith.

What is claimed is: 
     
         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.