Use of Trimetazidine in Preparation of Drugs for Preventing and Treating Liver Diseases

Abstract

This present invention discloses a new use of trimetazidine as a hepatoprotective drug in prevention and treatment of liver diseases, wherein trimetazidine is capable of inhibiting activation of resting T lymphocytes to activated lymphocytes, reducing release of cytokines, and reducing the hepatocyte injury caused by the immune system; capable of inhibiting fatty acid metabolism in hepatocytes and optimizing energy process in hepatocytes; and capable of maintaining normal function of mitochondrial permeability transition pores and reducing hepatocyte apoptosis. Clinical research and trial results suggest that, when administered to patients suffering from liver diseases and conditions, trimetazidine is capable of providing significant hepatoprotective function, and effectively decreasing transaminase levels (including alanine aminotransferase, aspartate transaminase, etc.), with such features as shortening the course of disease, reducing the mortality rate, easy and safe use, and low treatment cost. Trimetazidine is eliminated unchanged mainly through urine, with the elimination half-life of approximately 6 hours, and without hepatic metabolism. Therefore, trimetazidine has minimal liver toxicity, while having significant hepatoprotective effect.

1 . A method of treating a liver disease, comprising administering to a subject in need thereof a pharmaceutical composition comprising an effective amount of trimetazidine or a pharmaceutically acceptable salt thereof as an active ingredient, wherein said liver disease is cirrhosis. 
     
     
         2 . The method according to  claim 1 , wherein the pharmaceutical composition is orally administered to the subject. 
     
     
         3 . The method according to  claim 1 , wherein the pharmaceutical composition is parentally administered to the subject. 
     
     
         4 . The method according to  claim 1 , wherein the pharmaceutical composition is administered to the subject 1-4 times daily. 
     
     
         5 . The method according to  claim 1 , wherein the pharmaceutical composition is administered to the subject 2 or 3 times daily. 
     
     
         6 . The method according to  claim 1 , wherein the subject is administered with about 30-180 mg daily of trimetazidine or a pharmaceutically acceptable salt thereof. 
     
     
         7 . The method according to  claim 1 , wherein the subject is administered with about 60 mg daily of trimetazidine or a pharmaceutically acceptable salt thereof. 
     
     
         8 . The method according to  claim 1 , wherein active ingredient of the pharmaceutically composition consists essentially of trimetazidine or a pharmaceutically acceptable salt thereof. 
     
     
         9 . The method according to  claim 1 , wherein active ingredient of the pharmaceutically composition consists of trimetazidine or a pharmaceutically acceptable salt thereof. 
     
     
         10 . The method according to  claim 1 , wherein the pharmaceutically composition further comprises a pharmaceutically acceptable carrier. 
     
     
         11 . (canceled) 
     
     
         12 . (canceled) 
     
     
         13 . The method according to  claim 1 , wherein the subject has liver failure. 
     
     
         14 . (canceled) 
     
     
         15 . The method according to  claim 1 , wherein the subject is not suffering from angina pectoris, coronary insufficiency, old myocardial infarction, coronary heart disease, vertigo or tinnitus. 
     
     
         16 . The method according to  claim 1 , wherein the pharmaceutically composition reduces activation of resting T lymphocytes to activated lymphocytes in the subject. 
     
     
         17 . The method according to  claim 1 , wherein the pharmaceutically composition reduces fatty acid metabolism in hepatocytes and promotes aerobic oxidation of glucose in the subject. 
     
     
         18 . The method according to  claim 1 , wherein the pharmaceutically composition reduces β-oxidation in hepatocytes and reduces formation of ROS in the subject. 
     
     
         19 . The method according to  claim 1 , wherein the pharmaceutically composition reduces blood alanine aminotransferase (ALT) level in the subject by at least 100 U/L after 15 days of treatment. 
     
     
         20 . The method according to  claim 1 , wherein the pharmaceutically composition reduces blood aspartate transaminase (AST) level in the subject by at least 100 U/L after 15 days of treatment.