Pharmaceutical compositions for ulcer

Abstract

Pharmaceutical compositions for the therapy and the prevention of ulcer and dyspepsia relapses comprising as essential components the following components a) and b): component a): one or more components selected from the conventional anti-ulcer products; component b): organic compounds containing the —ONO 2 function, or inorganic compounds containing the —NO group, characterized in that they are NO nitric oxide donors.

1 . Pharmaceutical compositions comprising as components the following: 
 component a):                          wherein in the (A) formula 
 R=H, OCH 3 , OCHF 2 ;  
 R 1 =CH 3 , OCH 3 ;  
 R 2 =H, CH 3 ;  
 R 3 =CH 3 , CH 2 —CF 3 , (CH 2 ) 3 —OCH 3 ;  
   component b): one or more organic compounds containing the —ONO 2  group, or one or more inorganic compounds containing the —NO group, or mixtures thereof, said compounds being characterized in that they are NO nitric oxide donors, i.e., when they are brought into contact in vitro with cells of the vasal endothelium, platelets, and after incubation of 5 minutes at a temperature of 37° C., are capable to release NO and to activate the cGMP synthesis (Guanosine cyclic 3′,5′-(hydrogen phosphate)):    
     
     
         2 . Pharmaceutical compositions according to  claim 1 , wherein the molar ratio between the components a) and b) varies from 1:0.1 to 1:5.  
     
     
         3 . Pharmaceutical compositions according to  claim 1 , wherein in component a) the compounds are the following: 
 formula (A): 
 R—OCH 3 , R 1 =CH 3 , R 2 =CH 3 , R 3 =CH 3 , Omeprazole residue;  
 as in Omeprazole, but with R=OCHF 2 , R 1 =OCH 3 , R 2 =H, Pantoprazole residue;  
 as in Omeprazole, but with R=H, R 2 =H, R 3 =(CH 2 ) 3 —OCH 3 , Rabeprazole residue;  
 as in Rabeprazole, but with R 3 =CH 2 —CF 3 , Lansoprazole residue.  
   
     
     
         4 . Pharmaceutical compositions according to  claim 1 , wherein the isomers of one or more compounds of each component are used.  
     
     
         5 . Pharmaceutical compositions according to  claim 1 , wherein said pharmaceutical compositions comprise organic or inorganic salts of component a).  
     
     
         6 . Pharmaceutical compositions according to  claim 1 , wherein said pharmaceutical compositions comprise nitrate salts of component a).  
     
     
         7 . Pharmaceutical compositions according to  claim 5 , wherein the salts of component a) contain at least one anion mole/compound mole.  
     
     
         8 . Pharmaceutical compositions according to  claim 6 , wherein the salts of component a) contain at least one anion mole/compound mole.  
     
     
         9 . Pharmaceutical compositions according to  claim 1 , wherein the organic compounds containing the —ONO 2  groups usable in component b) are selected from the following ones: clonitrate, erytrityltetranitrate, mannitol hexanitrate, nicorandyl, nitroglycerin, pentaerythritoltetranitrate, pentrinitrol, propatylnitrate trolnitrate phosphate and prostaglandin nitroderivatives.  
     
     
         10 . Pharmaceutical compositions according to  claim 1  wherein the inorganic compounds containing the —NO group of component b) are selected from the following: nitrate salts of alkaline, earth-alkaline or III group metals and nitroprussiate salts.  
     
     
         11 . Pharmaceutical compositions according to  claim 10  wherein the nitrate salts are sodium or potassium nitrate.  
     
     
         12 . Pharmaceutical compositions according to  claim 1  for oral, parenteral or transdermic administration.  
     
     
         13 . Pharmaceutical compositions according to  claim 12  wherein the component b) is administered contemporaneously, subsequently or previously to component a).  
     
     
         14 . A method of treating a patient with ulcer or dyspepsia relapses, said method comprising administering a therapeutically effective amount of the pharmaceutical composition according to  claim 1 .  
     
     
         15 . Pharmaceutical compositions obtainable by combining the compositions according to  claim 1  with conventional gastroprotective agents.  
     
     
         16 . Compositions according to  claim 15  wherein the conventional gastroprotective agents are selected from prostaglandins, bismuth salts and antibiotics.  
     
     
         17 . A method of treating a patient with ulcer or dyspepsia relapses, said method comprising administering a therapeutically effective amount of the pharmaceutical composition according to  claim 15 .  
     
     
         18 . Pharmaceutical compositions according to  claim 2 , wherein the molar ratio between the components a) and b) varies from 1:0.5 to 1:2.