Abstract:
There are provided oral mouth rinse compositions, consisting essentially of: a) 1-20 wt % of an orally acceptable peroxide, b) 0.5-15 wt % of an orally acceptable sulfate, bisulfate, pyrosulfate salt of an inorganic cation or mixtures thereof, and c) water to 100 wt %. There are further provided methods of preparing and using said compositions as well as kits for maintaining the components to prepare said compositions.

Description:
FIELD OF THE INVENTION  
       [0001]     Anti bacterial and teeth whitening mouth rinse compositions.  
       BACKGROUND OF THE INVENTION  
       [0002]     Oral mouth rinse compositions have been used for the prevention of bad breath, elimination of oral microorganisms that are responsible for bad breath, tooth decay, plaque, gum diseases such as gingivitis, and for whitening of the teeth. Oral mouth rinses containing hydrogen peroxide are well known for their ability to whiten teeth and reduce the bacterial flora in the oral cavity. Hydrogen peroxide is utilized due to its ability to decompose into water and oxygen, with the oxygen then acting as both an antimicrobial agent, and a bleaching agent to whiten teeth.  
         [0003]     In the oral cavity, the decomposition of hydrogen peroxide into water and oxygen is aided by the enzyme peroxidase (also known as catalase). One factor affecting the rate of decomposition is the amount of peroxidase present in the oral cavity, with greater concentration resulting in greater decomposition. Thus, a mouth rinse that can cause an increase in the amount of peroxidase will have greater whitening and antimicrobial effectiveness.  
         [0004]     Day U.S. Pat. No. 6,692,757 discloses a system for cleaning water lines, particularly in dental offices in which the peroxide decomposition is accelerated by the presence of an acidic sulfate. The presence of a disinfectant is also required. There is no disclosure or suggestion of oral use.  
         [0005]     A second factor that will increase the rate of hydrogen peroxide decomposition is temperature. Higher temperature will increase the reaction rate between the peroxidase and peroxide, thus causing a faster onset of whitening and microbial kill. A heated mouth rinse will whiten teeth and kill microbes to a greater extent than an unheated mouth rinse of the same composition.  
         [0006]     The generation of heat in solutions for hair bleaching and dying using a combination of hydrogen peroxide and sulfites is well known, but there has been no disclosure of suggestion of such combinations in the oral cavity.  
       SUMMARY OF THE INVENTION  
       [0007]     The present invention provides a novel group of mouth rinses which enhance the activity of peroxide mouth rinses. This is achieved in two ways. The presence of orally acceptable inorganic cationic salts of sulfates, bisulfates or pyrosulfates in these rinses enhances the generation of saliva in the oral cavity and thus the level of peroxidase therein. This in turn causes a more rapid and efficient generation of active oxygen from the peroxide which in turn brings about greater whitening and microbial kill.  
         [0008]     A particularly preferred embodiment utilizes an in-situ formation of sulfate, bisulfate pyrosulfate or mixture thereof from the reaction between sulfites, bisulfites or metabisulfites and peroxide to form sulfates. This embodiment suitably utilizes a 2-phase system that is mixed just prior to use in the oral cavity. Part 1 of the system contains an orally acceptable inorganic cation salt of sulfite, bisulfite, metabisulfite or mixture thereof. Part 2 contains an orally acceptable peroxide in an amount that exceeds the stoichiometric amount required to convert the sulfite, bisulfite, metabisulfite or mixture thereof, by at least 0.5%. Other ingredients such as flavor, ethanol etc. may optionally be included when desired, as described below.  
         [0009]     During the reaction, not only is a sulfate and or a bisulfate formed but also the reaction is exothermic, which results in a temperature increase of about 3 to about 30 degrees centigrade depending on the concentrations employed. The resulting solution forms the mouth rinse, which if used substantially at once after formation, will provide not only increased salivary flow, but also increased temperature, both of which will increase the rate of peroxide decomposition, and result in greater antimicrobial efficacy and/or tooth whitening efficacy. 
     
    
     DESCRIPTION OF THE PREFERRED EMBODIMENTS  
       [0010]     In order for the peroxidase acceleration of peroxide decomposition to be effective, the saliva stimulation must be effective but taste acceptable. Clearly this is an individual matter. While operative, concentrations above 10 wt % in the rinse have a salty taste, it is thus preferred to provide somewhat less salt, suitably between about 1.5 and about 6 wt % of the solution in the oral cavity.  
         [0011]     For the reaction creating the oxidized salt to be sufficiently exothermic, sulfite, bisulfite or metabisulfite initial levels at the higher end of this range are preferred. Clearly there also needs to be not only the stoichiometric equivalent of peroxide to generate the exothermic reaction, but also sufficient excess peroxide to generate the active oxygen provided by the acceleration of decomposition caused by the rise in temperature. This excess should be at least 0.5 wt % of the solution used, but suitably may rise to about 5 wt %, though this should not be considered a limiting amount.  
         [0012]     Thus the oral mouth rinse composition which is utilized suitably consists essentially of: a) 1-20 wt % of an orally acceptable peroxide, b) 0.5-15 wt % of an orally acceptable sulfate, bisulfate, or pyrosulfate salt of an inorganic cation or mixtures thereof, and c) water to 100 wt %. For example this may be prepared by mixing equal amounts of i) an aqueous solution consisting essentially of 2-40 wt % of the peroxide, and ii) an aqueous solution consisting essentially of 1-30 wt % of the said inorganic cation salt of a sulfite, bisulfite, metabisulfite or mixture thereof, provided that the amount of peroxide in (i) exceeds the stoichiometric amount required to completely oxidize the salt of the sulfite, bisulfite, metabisulfite or mixture thereof, by at least 0.5 wt %. Similarly, the final mouthrinse can be prepared by mixing unequal amounts of i) and ii) in such quantities as needed to achieve a final solution within the ranges specified above. Desirably, the components i) and ii) are contained in a kit of containers each containing one of these components.  
         [0013]     Suitably, the peroxide is any orally acceptable peroxide, suitably hydrogen peroxide, urea peroxide or mixtures thereof and the cation is selected from the group consisting of sodium, potassium, ammonium, magnesium, calcium, aluminum, zinc, iron or mixture thereof.  
         [0014]     The rinse may contain other ingredients conventionally used in mouth rinses. These include but are not limited to ethanol, flavor oils, sweeteners, and surfactant in an amount to enable solubilization of flavor oils,  
         [0015]     While in no way to be considered as limiting favorable ranges in the present invention provide peroxide/bisulfate mouth rinses consisting essentially of from about 1.5 to about 6 wt %, preferably about 3 wt % peroxide and from about 3 to about 10 wt %, preferably about 5 wt % bisulfate. Additionally the rinses may contain ethanol, flavor oils, sweeteners and surfactant in an amount to enable solubilization of flavor oils, and water.  
       EXAMPLES  
     Example 1  
     Pre-Brushing Mouth Rinse  
       [0016]                                                                      Ingredient   % by Weight                                        Ethanol   5.00           Flavor Oil   0.10           Benzoic Acid   0.25           Poloxamer 407(10% Aq. Sol&#39;n)   0.25           Sucralose (1% Aq. Sol&#39;n)   15.00           Water   74.90           Sodium Bisulfate   3.00           Disodium Pyrophosphate   1.50           Total   100.00                        
 Combine Ethanol, Flavor and Benzoic Acid. Mix until clear. While mixing, slowly add the Poloxamer, Sucralose, and water. Continue mixing and add the Sodium Bisulfate and Disodium Pyrophosphate. Mix until a clear solution is obtained. 
 
       Example 2  
     Breath Freshening Mouth Rinse  
       [0017]                                                                      Ingredient   % by Weight                                        Ethanol   20.00           Flavor Oil   0.20           Benzoic Acid   0.25           Magnesium Lauryl Sulfate   0.20           Sorbitol   15.00           Water   61.85           Sodium Bisulfate   2.50           Total   100.00                        
 Combine Ethanol, Flavor and Benzoic Acid. Mix until clear. While mixing, slowly add the Magnesium Lauryl Sulfate, Sorbitol, water and Sodium Bisulfate. Mix until a clear solution is obtained 
 
       Example 3  
     Two Phase Tooth Whitening Mouth Rinse  
       [0018]    
       
         
               
               
               
             
               
             
               
               
               
             
               
             
               
               
               
             
           
               
                   
                   
               
               
                   
                   
               
               
                   
                 Ingredient 
                 % by Weight 
               
               
                   
                   
               
             
             
               
                   
               
             
          
           
               
                 Phase A: 
               
             
          
           
               
                   
                 Ethanol 
                 10.00 
               
               
                   
                 Flavor Oil 
                 0.20 
               
               
                   
                 Magnesium Lauryl Sulfate 
                 0.27 
               
               
                   
                 Sucralose (1% Aq. Sol&#39;n) 
                 15.00 
               
               
                   
                 Water 
                 61.53 
               
               
                   
                 Sodium Bisulfate 
                 8.00 
               
               
                   
                 Tromethamine 
                 5.00 
               
               
                   
                 Phase A Total 
                 100.00 
               
             
          
           
               
                 Phase B: 
               
             
          
           
               
                   
                 Hydrogen Peroxide(50% Aq. Sol&#39;n) 
                 6.00 
               
               
                   
                 Water 
                 94.00 
               
               
                   
                 Phase B Total 
                 100.00 
               
               
                   
                   
               
               
                   
                   Phase A: Combine Ethanol, Flavor Oil and Magnesium Lauryl Sulfate. Mix until clear. While mixing, add the Sucralose, Water, Sodium Bisulfate, and Tromethamine. Mix until a clear solution is obtained.    
               
               
                   
                   Phase B: Combine the Hydrogen Peroxide and water. Mix until uniform    
               
               
                   
                   Combine equal amounts of Phase A and Phase B, just prior to use, to form the final mouthrinse    
               
             
          
         
       
     
       Example 4  
     Two Phase Whitening Mouth Rinse (In-Situ Formation of Sodium Bisulfate)  
       [0019]    
       
         
               
               
               
             
               
             
               
               
               
             
               
             
               
               
               
             
           
               
                   
                   
               
               
                   
                   
               
               
                   
                 Ingredient 
                 % by Weight 
               
               
                   
                   
               
             
             
               
                   
               
             
          
           
               
                 Phase A: 
               
             
          
           
               
                   
                 Ethanol 
                 10.00 
               
               
                   
                 Flavor Oil 
                 0.20 
               
               
                   
                 Magnesium Lauryl Sulfate 
                 0.27 
               
               
                   
                 Sucralose (1% Aq. Sol&#39;n) 
                 15.00 
               
               
                   
                 Water 
                 61.53 
               
               
                   
                 Sodium Metabisulfite 
                 4.00 
               
               
                   
                 Sodium Sulfite 
                 4.00 
               
               
                   
                 Tromethamine 
                 5.00 
               
               
                   
                 Phase A Total 
                 100.00 
               
             
          
           
               
                 Phase B: 
               
             
          
           
               
                   
                 Hydrogen Peroxide(50% Aq. Sol&#39;n) 
                 12.00 
               
               
                   
                 Water 
                 88.00 
               
               
                   
                 Phase B Total 
                 100.00 
               
               
                   
                   
               
               
                   
                   Phase A: Combine Ethanol Flavor Oil and Magnesium Lauryl Sulfate. Mix until clear. While mixing, add the Sucralose, water, Sodium Metabisulfite, Sodium Sulfite and Tromethamine. Mix until a clear solution is obtained.    
               
               
                   
                   Phase B: Combine the Hydrogen Peroxide and water. Mix until uniform    
               
               
                   
                   Combine equal amounts of Phase A and Phase B, just prior to use, to form the final mouthrinse    
               
             
          
         
       
     
         [0020]     In accordance with the above formulation, but where in place of sulfite and/or the metabisulfite there is utilized only the metabisulfite, sulfite, or bisulfite, a similar solution is obtained.  
         [0021]     In accordance with the above formulation, but where in place of sodium the cation utilized is potassium, ammonium, magnesium, calcium, aluminum, zinc, iron or mixture thereof a similar formulation is obtained.  
         [0022]     Similarly in place of hydrogen peroxide, there may be utilized urea peroxide or mixtures thereof with hydrogen peroxide.  
         [0023]     The formulation is utilized by introducing a comfortable amount, suitably about 10 ml, into the mouth agitating it, and ejecting it.