Preparation and compositions of highly bioavailable zerovalent sulfur and uses thereof

Abstract

The present invention features sulfur-rich compositions and preparations thereof that are safe and effective as hydrogen sulfide prodrugs of high bioavailability. The invention also includes methods of treating pathological conditions associated with oxidative stress using sulfur-rich compositions. The invention further includes sulfur-rich compositions as antidotes and medical food for preserving and promoting general health.

What is claimed is: 
     
         1 . A composition comprising 90-99.9% (w/w) elemental alpha sulfur and 0.01-10% (w/w) highly polar components, and optionally comprising one or more pharmaceutically acceptable excipients. 
     
     
         2 . The composition of  claim 1 , said composition comprising about 99% (w/w) zerovalent sulfur and about 1% (w/w) highly polar components, wherein said highly polar components are selected from sodium sulfate, sodium polythionates, and sodium thiosulfate. 
     
     
         3 . The composition of  claim 1 , wherein said highly polar components are selected from the group consisting of sodium polythionate, potassium polythionate, ammonium polythionate, calcium polythionate, sodium thiosulfate, potassium thiosulfate, ammonium thiosulfate, calcium thiosulfate, sodium sulfate, potassium sulfate, ammonium sulfate, sodium bisulfite, potassium bisulfite, ammonium bisulfite, calcium bisulfite, sodium chloride, potassium chloride, ammonium chloride, calcium chloride, sodium acetate, sodium palmitate, potassium palmitate, and ammonium laurate. 
     
     
         4 . A composition comprising an elemental alpha sulfur and one or more highly polar components in a ratio from about 10 to about 150 parts elemental alpha sulfur to 1 part highly polar components (w/w) for enteral, topical, or parenteral administration. 
     
     
         5 . The composition of  claim 4 , wherein said composition is formulated for enteral administration and said elemental alpha sulfur and said highly polar components are present together in an amount of 400 mg. 
     
     
         6 . The composition of  claim 5 , wherein said composition is a capsule. 
     
     
         7 . The composition of  claim 2 , wherein said composition is formulated for topical administration, and said composition comprises 1-20% zerovalent sulfur content. 
     
     
         8 . The composition of  claim 7 , wherein said composition is a cream. 
     
     
         9 . The composition of  claim 8 , wherein said cream comprises (i) 5-20% zerovalent sulfur content and (ii) polyethylene glycol or petroleum jelly. 
     
     
         10 . The composition of  claim 9 , wherein said cream comprises 5-15% zerovalent sulfur content. 
     
     
         11 . The composition of  claim 4 , further comprising a third agent. 
     
     
         12 . The composition of  claim 11 , wherein said third agent is a cardiovascular disease drug, an anti-inflammatory drug, an anti-neurodegenerative drug, or an anticancer/anti-proliferative drug. 
     
     
         13 . The composition of  claim 11 , wherein said elemental alpha sulfur, said highly polar components, and said third agent are present in an effective amount to treat a condition associated with oxidative stress. 
     
     
         14 . The composition of  claim 11 , wherein said third agent is a dietary supplement. 
     
     
         15 . The composition of  claim 11 , wherein said elemental alpha sulfur, said highly polar components, and said third agent are present in an effective amount to promote or maintain general health. 
     
     
         16 . A method for preparing the composition of  claim 1 , said method comprising:
 (a) providing a first inorganic compound comprising sulfur in the  − 2 (minus two) oxidation state,   (b) reacting said first inorganic compound with a second compound comprising sulfur in the  + 4 (plus four) oxidation state and optionally an acid,   wherein said reacting produces the composition of  claim 1 .   
     
     
         17 . The method of  claim 16 , wherein said first inorganic compound is sodium hydrogen sulfide or sodium sulfide. 
     
     
         18 . The method of  claim 16 , wherein said second inorganic compound is sodium metabisulfite, sodium bisulfite, or sodium sulfite. 
     
     
         19 . The method of  claim 16 , wherein said acid is concentrated sulfuric acid.