# US 8,273,795 B2 · Tranexamic acid formulations > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 8,273,795 B2 - Document ID: US8273795B2 - Status: Granted - Kind: B2 - Application number: 12/228,489 - Filed: 2008-08-13 - Published: 2009-02-19 - Granted: 2012-09-25 - Earliest claimed: 2004-03-04 - Assignees: Ferring B.V. - Inventors: Keith A. Moore; Ralph A. Heasley; Jeffrey S. Greiwe; John W. Facemire; Jason D. Modest - Web page: https://patentgrep.com/patent/US8273795B2 ## CPC - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/2009: {Inorganic compounds} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2059: {Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin} - A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60) - A61K 31/195: having an amino group - A61K 31/196: the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil - A61P 7/04: Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents - A61P 15/00: Drugs for genital or sexual disorders (for disorders of sex hormones A61P5/24); Contraceptives - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract Disclosed are modified release oral tranexamic acid formulations and methods of treatment therewith. ## Claims ### Claim 1 A method of treating menorrhagia, the method comprising: orally administering to a patient in need of such treatment 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; wherein the formulation is administered as two oral dosage forms, each providing a dose of about 650 mg of tranexamic acid; 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. ### Claim 2 (depends on 1) The method 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. ### Claim 3 (depends on 1) The method 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. ### Claim 4 (depends on 1) The method 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. ### Claim 5 (depends on 1) The method of claim 1, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid. ### Claim 6 (depends on 1) The method of claim 1, wherein a mean maximum plasma concentration (Cmax) of tranexamic acid of from about 5 to about 17.5 mcg/ml is provided following the administration. ### Claim 7 (depends on 1) The method 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. ### Claim 8 (depends on 1) The method 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. ### Claim 9 (depends on 1) The method 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. ### Claim 10 (depends on 1) The method of claim 1, wherein the modified release material is present in an amount from about 10% to about 35% by weight of the formulation. ### Claim 11 (depends on 1) The method 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. ### Claim 12 (depends on 11) The method of claim 11, wherein the tranexamic acid or pharmaceutically acceptable salt thereof is tranexamic acid.