Pharmaceutical composition comprising rimeporide for treating diseases associated with insulin resistance and beta-cell dysfunction

Abstract

The invention relates to a pharmaceutical composition comprising as active ingredient an effective amount of 2-Methyl-4,5-di-(methylsulfonyI)-benzoyl-guanidine, or derivatives thereof, for the prophylaxis and therapy of Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy. Another object of the invention concerns the use of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, or derivatives thereof, for the enhancement of insulin sensitivity and the preservation or increase of β-cell compensation.

1 . Pharmaceutical composition comprising as active ingredient an effective amount of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, and/or a physiologically acceptable salt and/or solvate thereof, for the prophylactic or therapeutic treatment and/or monitoring of diseases that are associated with insulin resistance and/or β-cell dysfunction, optionally together with pharmaceutically tolerable adjuvants. 
     
     
         2 . Pharmaceutical composition according to  claim 1 , wherein the diseases are Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy, preferably Type II diabetes mellitus. 
     
     
         3 . Pharmaceutical composition according to  claim 1 , wherein the active ingredient is the 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine salt selected from the group of hydrochloride, methanesulfonate, hemi-sulfate, hemi-fumerate and hemi-malate. 
     
     
         4 . Pharmaceutical composition according to  claim 1 , wherein the active ingredient is 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine hydrochloride hydrate. 
     
     
         5 . Pharmaceutical composition according to  claim 1 , wherein the active ingredient is combined with at least another active ingredient. 
     
     
         6 . Pharmaceutical composition according to  claim 1  for oral or parenteral administration, preferably oral administration. 
     
     
         7 . Pharmaceutical composition according to  claim 1  for daily administration in a dose range from 20 to 100 mg per kg of body weight. 
     
     
         8 . A method for the prophylaxis or treatment and/or monitoring of diseases that are associated with insulin resistance and/or β-cell dysfunction, comprising administering to the patient an effective amount of 2-methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, and/or a physiologically acceptable salt and/or solvate thereof. 
     
     
         9 . A method for enhancement of insulin sensitivity and/or the preservation or increase of β-cell compensation, comprising administering to the patient an effective amount of 2-methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, and/or a physiologically acceptable salt and/or solvate thereof. 
     
     
         10 . A method according to  claim 9 , wherein the insulin Sensitivity is at least doubled. 
     
     
         11 . A method according to  claim 9 , wherein the pancreatic β-cell compensation is preserved, at least 70% of baseline prior usage. 
     
     
         12 . A method according to  claim 11 , wherein 2-methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, and/or a physiologically acceptable salt and/or solvate thereof is administered for a period of at least 1 week. 
     
     
         13 . A method for treating Type II diabetes mellitus, the Metabolic syndrome, diabetic nephropathy and/or neuropathy, wherein an effective amount of 2-Methyl-4,5-di-(methylsulfonyl)-benzoyl-guanidine, and/or a physiologically acceptable salt and/or solvate thereof, is administered to a mammal in need of such treatment.