Synergistic compositions and methods for potentiating anti-oxidative activity

Abstract

The present invention relates to synergistic compositions for protection against oxidative damage, consisting essentially of antacids in conjunction with antioxidants. The invention further relates to method for preventing oxidative damage using the compositions of the invention.

What is claimed is: 
     
         1 . A composition comprising:
 (a) at least one antacid;   (b) at least one antioxidant, wherein the relative amount of the at least one antioxidant in the composition is from 30 to 95% w/w of the composition; and, optionally,   (c) at least one pharmaceutically acceptable carrier.   
     
     
         2 . The composition of  claim 1 , being identified for use in protecting against excess gastric acidity. 
     
     
         3 . The composition according to  claim 1 , wherein said at least one antacid comprises at least one classical antacid in a dose capable of neutralizing 100 ml of 0.009 M HCl, such that the composition is capable of elevating the pH in a stomach by at least one pH unit, said elevating the pH being from a pH of 2 to a pH of at least 3. 
     
     
         4 . The composition of  claim 1 , wherein said at least one antacid comprises at least one classical antacid selected from a group consisting of sodium bicarbonate, potassium hydroxide, aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxycarbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum aminoacetate, dihydroxyaluminum aminoacetic acid, calcium carbonate, calcium phosphate, hydrated magnesium aluminate activated sulfate, magnesium aluminate, magnesium aluminosilicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide and magnesium trisilicate. 
     
     
         5 . The composition of  claim 1 , wherein said at least one antacid comprises at least one H2-receptor antagonist and/or proton pump inhibitor. 
     
     
         6 . The composition of  claim 1 , wherein the relative amount of said at least one antacid in the composition is from about 5 to about 90% w/w of the total antacid and antioxidant weight. 
     
     
         7 . The composition of  claim 1 , wherein said antioxidant is a polyphenol. 
     
     
         8 . The composition of  claim 7 , wherein said polyphenol is selected from the group consisting of chalcones, phenolic acid, anthocyanins, flavonols, flavanols, flavanones, flavanonols, hydrolyzed tannins, proanthocyanidins, phenolamines, lignans, lignine, betalains, stilbenes, cyclic diterpenes, monoterpenes, sesquiterpenes, sesamolin and isoflavones. 
     
     
         9 . The composition of  claim 7 , wherein said polyphenol is selected from a group consisting of anthocyanins, flavonols, flavanols, flavanones, flavanonols, hydrolyzed tannins, proanthocyanidins, lignine, and stilbenes. 
     
     
         10 . A pharmaceutical composition, comprising:
 (a) at least one pharmaceutically active ingredient;   (b) at least one antacid;   (c) at least one antioxidant, wherein the relative amount of the at least one antioxidant in the composition is from 30 to 95% w/w of the composition; and, optionally,   (d) at least one pharmaceutically acceptable carrier, diluent or stabilizer.   
     
     
         11 . The composition according to  claim 10 , wherein said at least one antacid comprises at least one classical antacid in a dose capable of neutralizing 100 ml of 0.009 M HCl, such that the composition is capable of elevating the pH in a stomach by at least one pH unit, said elevating the pH being from a pH of 2 to a pH of at least 3. 
     
     
         12 . The composition of  claim 10 , wherein said at least one antacid comprises at least one classical antacid selected from a group consisting of sodium bicarbonate, potassium hydroxide, aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxycarbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum aminoacetate, dihydroxyaluminum aminoacetic acid, calcium carbonate, calcium phosphate, hydrated magnesium aluminate activated sulfate, magnesium aluminate, magnesium aluminosilicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide and magnesium trisilicate. 
     
     
         13 . The composition of  claim 10 , wherein said at least one antacid comprises said at least one antacid comprises at least one H2-receptor antagonist and/or proton pump inhibitor. 
     
     
         14 . The composition of  claim 10 , wherein the relative amount of said at least one antacid in the composition is from about 5 to about 90% w/w of the total antacid and antioxidant weight. 
     
     
         15 . The composition of  claim 10 , wherein said antioxidant is a polyphenol. 
     
     
         16 . The composition of  claim 15 , wherein the polyphenol is selected from the group consisting of chalcones, phenolic acid, anthocyanins, flavonols, flavanols, flavanones, flavanonols, hydrolyzed tannins, proanthocyanidins, phenolamines, lignans, lignine, betalains, stilbenes, cyclic diterpenes, monoterpenes, sesquiterpenes, sesamolin and isoflavones. 
     
     
         17 . The composition of  claim 15 , wherein the polyphenol is selected from a group consisting of anthocyanins, flavonols, flavanols, flavanones, flavanonols, hydrolyzed tannins, proanthocyanidins, lignine, and stilbenes. 
     
     
         18 . A method for protecting a subject from oxidative damage, the method comprising administering to the subject a composition comprising:
 (a) at least one antacid in a dose sufficient to elevate pH in a stomach;   (b) at least one antioxidant in a dose sufficient to decrease free radical generation in the stomach; and, optionally   (c) at least one carrier, diluent or stabilizer.   
     
     
         19 . The method of  claim 18 , wherein said administering results in inhibition of peroxidation reactions in a gastrointestinal tract of the subject. 
     
     
         20 . The method of  claim 18 , wherein said administering results in attenuation of generation of free radicals and/or peroxides in a gastrointestinal tract of the subject. 
     
     
         21 . The method of  claim 18 , wherein said at least one antacid comprises at least one classical antacid in a dose capable of neutralizing 100 ml of 0.009 M HCl, such that the composition is capable of elevating the pH in a stomach by at least one pH unit, said elevating the pH being from a pH of 2 to a pH of at least 3. 
     
     
         22 . The method of  claim 18 , wherein the composition is administered orally. 
     
     
         23 . The method of  claim 18 , wherein the antacid comprises at least one classical antioxidant selected from the group consisting of sodium bicarbonate, potassium hydroxide, aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxycarbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum aminoacetate, dihydroxyaluminum aminoacetic acid, calcium carbonate, calcium phosphate, hydrated magnesium aluminate activated sulfate, magnesium aluminate, magnesium aluminosilicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide and magnesium trisilicate. 
     
     
         24 . The method of  claim 18 , wherein said at least one the antacid comprises at least one antacid comprises at least one H2-receptor antagonist and/or proton pump inhibitor. 
     
     
         25 . The method of  claim 18 , wherein the relative amount of the antacid in the composition is from about 5 to about 90% w/w of the total antacid and antioxidant weight. 
     
     
         26 . The method of  claim 18 , wherein said antioxidant is a polyphenol, and the relative amount of said at least one antioxidant in the composition is from 30 to 95% w/w of the composition. 
     
     
         27 . The method of  claim 18 , wherein said antioxidant is a polyphenol selected from the group consisting of chalcones, phenolic acid, anthocyanins, flavonols, flavanols, flavanones, flavanonols, hydrolyzed tannins, proanthocyanidins, phenolamines, lignans, lignine, betalains, stilbenes, cyclic diterpenes, monoterpenes, sesquiterpenes, sesamolin and isoflavones. 
     
     
         28 . A method for protecting a subject from excess gastric acidity, the method comprising administering to the subject a composition comprising:
 (a) at least one antacid in a dose sufficient to elevate pH in a stomach;   (b) at least one antioxidant in a dose sufficient to decrease free radical generation in the stomach; and, optionally   (c) at least one carrier, diluent or stabilizer.   
     
     
         29 . The method of  claim 28 , wherein said at least one antacid comprises at least one classical antacid in a dose capable of neutralizing 100 ml of 0.009 M HCl, such that the composition is capable of elevating the pH in a stomach by at least one pH unit, said elevating the pH being from a pH of 2 to a pH of at least 3. 
     
     
         30 . The method of  claim 28 , wherein the antacid comprises at least one classical antioxidant selected from the group consisting of sodium bicarbonate, potassium hydroxide, aluminum carbonate, aluminum hydroxide, aluminum phosphate, aluminum hydroxycarbonate, dihydroxy aluminum sodium carbonate, aluminum magnesium glycinate, dihydroxy aluminum aminoacetate, dihydroxyaluminum aminoacetic acid, calcium carbonate, calcium phosphate, hydrated magnesium aluminate activated sulfate, magnesium aluminate, magnesium aluminosilicates, magnesium carbonate, magnesium glycinate, magnesium hydroxide, magnesium oxide and magnesium trisilicate. 
     
     
         31 . The method of  claim 28 , wherein said at least one antacid comprises at least one H2-receptor antagonist and/or proton pump inhibitor. 
     
     
         32 . The method of  claim 28 , wherein the relative amount of the antacid in the composition is from about 5 to about 90% w/w of the total antacid and antioxidant weight. 
     
     
         33 . The method of  claim 28 , wherein said antioxidant is a polyphenol, and the relative amount of said at least one antioxidant in the composition is from 30 to 95% w/w of the composition. 
     
     
         34 . The method of  claim 28 , wherein said antioxidant is a polyphenol selected from the group consisting of chalcones, phenolic acid, anthocyanins, flavonols, flavanols, flavanones, flavanonols, hydrolyzed tannins, proanthocyanidins, phenolamines, lignans, lignine, betalains, stilbenes, cyclic diterpenes, monoterpenes, sesquiterpenes, sesamolin and isoflavones.