Tranexamic acid formulations with reduced adverse effects

Abstract

Tranexamic acid formulated in an oral dosage form with at least one agent that decreases tranexamic acid release in the stomach. Such formulations minimize nausea, vomiting, and other adverse gastric effects that may accompany tranexamic acid therapy, for example, to treat heavy menstrual bleeding. One embodiment is an extended release formulation with waxes, polymers, etc. that prevent a bolus release of tranexamic acid in the stomach. An alternative embodiment is a delayed release formulation with polymers that prevent release of tranexamic acid in the acid environment of the stomach and delay its release until the formulation reaches the less acid environment of the intestines. Such formulations enhance patient compliance with therapy because adverse effects of tranexamic acid therapy are reduced.

1 - 24 . (canceled) 
     
     
         25 . A therapeutic method comprising providing to a patient in need of tranexamic acid therapy an ingestible solid pharmaceutically acceptable formulation comprising a therapeutic dose of tranexamic acid and at least one excipient wherein the excipient retards tranexamic acid release in the stomach and substantially releases tranexamic acid in the small intestine thereby reducing the concentration of tranexamic acid in the stomach during therapy. 
     
     
         26 . The method of  claim 25  further reducing adverse gastrointestinal side effects of therapy. 
     
     
         27 . The method of  claim 25 , wherein the at least one excipient controls release of tranexamic acid in the stomach. 
     
     
         28 . The method of  claim 25 , wherein the at least one excipient retards release of tranexamic acid in the stomach. 
     
     
         29 . The method of  claim 25 , wherein the therapeutic dose is in the range of about 375 mg tranexamic acid to about 1 gram tranexamic acid per dose. 
     
     
         30 . The method of  claim 25 , wherein the dose is administered three times a day or four times a day. 
     
     
         31 . The method of  claim 30 , wherein the dose is at least two solid tablets or one sachet containing granules. 
     
     
         32 . A therapeutic method comprising providing tranexamic acid therapy to a patient in need thereof in a pharmaceutically acceptable oral formulation comprising at least one excipient sufficient to result in a decreased stomach concentration of tranexamic acid after oral ingestion thereby decreasing at least one gastrointestinal adverse effect of said therapy. 
     
     
         33 . The method of  claim 32  comprising, decreasing a gastrointestinal adverse effect selected from the group consisting of nausea, vomiting, diarrhea, constipation, cramping bloating, and combinations thereof. 
     
     
         34 . The method of  claim 32  provided to a patient having menorrhagia. 
     
     
         35 . A method of reducing gastrointestinal adverse side effects comprising administering an effective amount of an extended release pharmaceutical composition comprising tranexamic acid and at least one agent that controls release of tranexamic acid from the composition in the gastrointestinal tract. 
     
     
         36 . A method of reducing gastrointestinal adverse side effects comprising administering an effective amount of a composition comprising tranexamic acid in an oral administrable formulation selected from the group consisting of extended release, delayed release, and combinations thereof, wherein upon oral administration tranexamic acid is substantially released in the small intestine. 
     
     
         37 . A method of reducing gastrointestinal adverse side effects comprising directing oral administration of an effective amount of a delayed release pharmaceutical composition comprising tranexamic acid and at least one agent that delays release of the tranexamic acid from the composition until the small intestine.