Abstract:
The invention concerns a topical oral composition comprising taurine, propanediol and xylitol and its use for alleviating or eliminating symptoms of dry mouth and/or preventing or treating mouth ulcers.

Description:
FIELD OF THE INVENTION 
       [0001]    The invention concerns a topical oral composition comprising taurine, propanediol and xylitol and its use for alleviating or eliminating symptoms of dry mouth and/or preventing or treating mouth ulcers. 
       TECHNOLOGICAL BACKGROUND 
       [0002]    Dry mouth or xerostomia is caused by a decrease in the activity of salivary glands. The reduction of the salivary flow can result in discomfort, interfere with speech and swallowing, make wearing dentures difficult, cause halitosis, and impair oral hygiene by causing a decrease in oral pH and an increase in bacterial growth. Longstanding dry mouth can result in severe tooth decay and oral candidiasis. Dry mouth is a common complaint among older adults, affecting about 20% of the elderly. 
         [0003]    The causes of dry mouth are different and involve many factors such as stress, infection of salivary glands or the use of drugs such as anticholinergics, antiparkinsonians, antineoplastics, radiation to the head and neck (for cancer treatment) or it may be also associated to certain diseases such as Sjögren&#39;s syndrome and HIV/AIDS, uncontrolled diabetes, and other disorders. 
         [0004]    Dry mouth is currently treated with mouth rinses, topical applications, salivary substitutes, or salivary stimulants such as sugarless candies and chewing gum. Some saliva stimulants are commercially available. The current treatments focus on relieving the symptoms and preventing dental cavities. Artificial saliva products are often the treatment of choice for xerostomia patients. 
         [0005]    Dry mouth can make oral soft tissues such as oral mucous membrane, gingival tissue and taste buds on tongue more vulnerable to damage physically, physicochemically and biologically. However existing treatments/products does not solve the problem of soft tissue trouble. The present compositions solve this problem due to the effect of protection and repair promotion of the oral soft tissues. 
         [0006]    Mouth ulcers and oral lesions are inflammatory forms which occur on the oral mucosa with erythematous lesions similar to burns and injuries, such painful ulcers making it difficult chewing and swallowing, compromising the quality of life of the patient. They are painful because a layer of the oral mucosa has been removed, exposing the nerve endings beneath. 
         [0007]    There are a number of various causes, including poor-fitting braces and dentures, physical or chemical trauma, dry mouth, taking immuno-suppressive medications, burns, allergies, infection from microorganisms or viruses. Once formed, the ulcer may be maintained by inflammation and/or secondary infection. Two common oral ulcer types are aphthous ulcers (canker sores) and cold sores. Cold sores can be caused by the herpes simplex virus. 
         [0008]    Mouth ulcers are managed with topical rinses, topical gels and liquids, behavioural modifications, analgesics and preventive measures. 
       DESCRIPTION OF THE INVENTION 
       [0009]    In accord with the present invention it has been found that compositions containing taurine, xylitol and propane-1,3-diol, topically applied to the mucous membrane of the mouth, exert beneficial effects on dry mouth and promote regeneration of oral mucous membrane. 
         [0010]    The present invention provides topical oral compositions comprising taurine or a salt thereof, xylitol and propane-1,3-diol. 
         [0011]    Taurine (2-aminoethanesulfonic acid) is an organic acid widely distributed in animal tissues. Taurine is present in high concentration in mammalian plasma and cells and plays an important role in a number of biological processes. Taurine has been shown to have osmoregulatory, antioxidative, antiapoptopic, anti-inflammatory and antilipidic activity. 
         [0012]    Xylitol is classified as a polyol and it is considered a “sugar-free” sweetener. Xylitol is known to reduce the risk of tooth decay. 
         [0013]    Propane-1,3-diol is commercialized under the trademark Zemea® and it is known to be an emollient, humectant, hand-feel modifier or solvent. 
         [0014]    The composition of the present invention are able to protect oral soft tissues and promote their repair, to relieve inflammation of oral soft tissues, to prevent taste disorder due to protection of taste buds and to protect from dryness damage due to humectant function. 
         [0015]    The concentration of taurine in the composition varies from 0.01 to 5.0% by weight, preferably the concentration is 0.1 to 1.0% by weight. 
         [0016]    The concentration of xylitol in the composition varies from 0.1 to 10.0% by weight, preferably the concentration is 0.5 to 5.0% by weight. 
         [0017]    The concentration of propone-1,3-diol in the composition varies from 0.1 to 30.0% by weight, preferably the concentration is 2.0 to 20.0% by weight. 
         [0018]    The composition may further comprise sodium hyaluronate. 
         [0019]    Sodium hyaluronate is present in a concentration of 0.01 to 1.0% by weight, preferably the concentration is 0.05 to 0.3% by weight. Sodium hyaluronate has preferably a Molecular Weight (MW) of 1.0-1.5×10 6 . 
         [0020]    The compositions of the invention may comprise further components such as remineralizing agents, osmoprotectant agents, lubricating agents, compounds for stimulating saliva flow. 
         [0021]    Remineralising agents preferably are chosen among fluoride anions, phosphate anions, sodium cations and potassium cations such as potassium fluoride, sodium fluoride, sodium monofluorophosphate, tin fluoride, amine fluorides (hexadecylamine hydrofluoride, bis-(hydroxyethyl)aminopropyl-N-hydroxyethyl-octadecylamine dihydrofluoride, N-N′,N′-tri(polyoxyethylene)-N-hexadecyl-propylenediamine dihydrofluoride or octadecenylamine hydrofluoride), potassium phosphate, potassium pyrophosphate, tripotassium citrate, calcium lactate, calcium pantothenate and calcium carbonate. 
         [0022]    Preferred remineralizing agent is sodium monofluorophosphate which is preferably present in concentrations of 0.10 to 1.14% by weight. 
         [0023]    The osmoprotectant agent is preferably betaine, which is preferably present in concentrations of 0.5 to 5.0% by weight. 
         [0024]    The preferred lubricating agent is polyvinylpyrrolidone, which is preferably is present in concentrations of 0.01 to 5.0% by weight. 
         [0025]    The compound for stimulating saliva flow may be a citrate salt or citric acid. The preferred compound for stimulating saliva flow is citrate sodium/citric acid which is preferably present in concentrations of 0.5 to 5.0% by weight. The composition of the invention can include at each time all the necessary ingredients known to the skilled in the art in order to obtain the necessary organoleptic and rheologic properties. 
         [0026]    The topical oral composition according to claims may be in the form of gel, spray, toothpaste, mouthwash, oral patch, chewing gum and tablet. 
     
    
     EXAMPLES 
     Example 1 
       [0027]      
         [0000]    
       
         
               
             
               
               
               
             
               
               
               
             
           
               
                   
               
               
                 Dry mouth gel 
               
             
          
           
               
                   
                 INCI-EU NAMES 
                 % 
               
               
                   
                   
               
             
          
           
               
                   
                 AQUA 
                 49.583969 
               
               
                   
                 SORBITOL, AQUA 
                 25.000000 
               
               
                   
                 PROPANEDIOL 
                 15.000000 
               
               
                   
                 PVP 
                 3.000000 
               
               
                   
                 SODIUM CITRATE 
                 2.400000 
               
               
                   
                 BETAINE 
                 1.000000 
               
               
                   
                 GLUCONOLACTONE, SODIUM BENZOATE, 
                 1.000000 
               
               
                   
                 CALCIUM GLUCONATE 
               
               
                   
                 CARRAGEENAN 
                 0.700000 
               
               
                   
                 XANTHAN GUM 
                 0.700000 
               
               
                   
                 XYLITOL 
                 0.500000 
               
               
                   
                 PEG-40 HYDROGENATED CASTOR OIL 
                 0.400000 
               
               
                   
                 TAURINE 
                 0.300000 
               
               
                   
                 CITRIC ACID 
                 0.240000 
               
               
                   
                 SODIUM HYDROXIDE 
                 0.076000 
               
               
                   
                 SODIUM HYALURONATE 
                 0.050000 
               
               
                   
                 SUCRALOSE 
                 0.030000 
               
               
                   
                 STEVIA REBAUDIANA EXTRACT 
                 0.010000 
               
               
                   
                 CI 19140 
                 0.000026 
               
               
                   
                 CI 42090 
                 0.000005 
               
               
                   
                 total 
                 100.000000 
               
               
                   
                   
               
             
          
         
       
     
       Example 2 
       [0028]      
         [0000]    
       
         
               
             
               
               
               
             
               
               
               
             
           
               
                   
               
               
                 Dry mouth toothpaste 
               
             
          
           
               
                   
                 INCI-EU NAMES 
                 % 
               
               
                   
                   
               
             
          
           
               
                   
                 SORBITOL, AQUA 
                 43.000000 
               
               
                   
                 AQUA 
                 15.843000 
               
               
                   
                 PROPANEDIOL 
                 10.000000 
               
               
                   
                 SILICA 
                 13.500000 
               
               
                   
                 BETAINE 
                 4.000000 
               
               
                   
                 LAURYL GLUCOSIDE 
                 3.000000 
               
               
                   
                 COCAMIDOPROPYL BETAINE, AQUA 
                 2.000000 
               
               
                   
                 XANTHUM GUM 
                 1.500000 
               
               
                   
                 POLYSORBATE 20 
                 1.500000 
               
               
                   
                 SODIUM CITRATE 
                 1.200000 
               
               
                   
                 SODIUM MONOFLUOROPHOSPHATE 
                 1.097000 
               
               
                   
                 XYLITOL 
                 1.000000 
               
               
                   
                 GLUCONOLACTONE, SODIUM BENZOATE, 
                 0.800000 
               
               
                   
                 CALCIUM GLUCONATE 
               
               
                   
                 AROMA 
                 0.500000 
               
               
                   
                 CI77891 
                 0.400000 
               
               
                   
                 TAURINE 
                 0.300000 
               
               
                   
                 STEVIA REBAUDIANA EXTRACT 
                 0.100000 
               
               
                   
                 SUCRALOSE 
                 0.100000 
               
               
                   
                 CITRIC ACID 
                 0.100000 
               
               
                   
                 SODIUM HYALURONATE 
                 0.050000 
               
               
                   
                 PVP 
                 0.010000 
               
               
                   
                 total 
                 100.000000 
               
               
                   
                   
               
             
          
         
       
     
       Example 3 
       [0029]      
         [0000]    
       
         
               
             
               
               
               
             
               
               
               
             
           
               
                   
               
               
                 Dry mouth mouthwash 
               
             
          
           
               
                   
                 INCI-EU NAMES 
                 % 
               
               
                   
                   
               
             
          
           
               
                   
                 AQUA 
                 79.480000 
               
               
                   
                 SORBITOL, AQUA 
                 10.000000 
               
               
                   
                 SODIUM CITRATE 
                 2.400000 
               
               
                   
                 PVP 
                 2.000000 
               
               
                   
                 PROPANEDIOL 
                 2.000000 
               
               
                   
                 BETAINE 
                 1.000000 
               
               
                   
                 GLUCONOLACTONE, SODIUM BENZOATE, 
                 1.000000 
               
               
                   
                 CALCIUM GLUCONATE 
               
               
                   
                 PEG-40 HYDROGENATED CASTOR OIL 
                 0.600000 
               
               
                   
                 XYLITOL 
                 0.500000 
               
               
                   
                 TAURINE 
                 0.300000 
               
               
                   
                 CITRIC ACID 
                 0.240000 
               
               
                   
                 SODIUM MONOFLUOROPHOSPHATE 
                 0.190000 
               
               
                   
                 SODIUM HYDROXIDE 
                 0.100000 
               
               
                   
                 AROMA 
                 0.090000 
               
               
                   
                 SODIUM HYALURONATE 
                 0.050000 
               
               
                   
                 HYDROXYETHYLCELLULOSE 
                 0.020000 
               
               
                   
                 SUCRALOSE 
                 0.020000 
               
               
                   
                 STEVIA REBAUDIANA EXTRACT 
                 0.010000 
               
               
                   
                 total 
                 100.000000 
               
               
                   
                   
               
             
          
         
       
     
       Example 4 
       [0030]      
         [0000]    
       
         
               
             
               
               
               
             
               
               
               
             
           
               
                   
               
               
                 Dry mouth spray 
               
             
          
           
               
                   
                 INCI-EU NAMES 
                 % 
               
               
                   
                   
               
             
          
           
               
                   
                 AQUA 
                 79.560000 
               
               
                   
                 SORBITOL, AQUA 
                 10.000000 
               
               
                   
                 SODIUM CITRATE 
                 2.300000 
               
               
                   
                 PVP 
                 2.000000 
               
               
                   
                 PROPANEDIOL 
                 2.000000 
               
               
                   
                 BETAINE 
                 1.000000 
               
               
                   
                 GLUCONOLACTONE, SODIUM BENZOATE, 
                 1.000000 
               
               
                   
                 CALCIUM GLUCONATE 
               
               
                   
                 PEG-40 HYDROGENATED CASTOR OIL 
                 1.000000 
               
               
                   
                 XYLITOL 
                 0.500000 
               
               
                   
                 TAURINE 
                 0.300000 
               
               
                   
                 CITRIC ACID 
                 0.240000 
               
               
                   
                 SODIUM HYALURONATE 
                 0.050000 
               
               
                   
                 SUCRALOSE 
                 0.030000 
               
               
                   
                 STEVIA REBAUDIANA EXTRACT 
                 0.010000 
               
               
                   
                 AROMA 
                 0.010000 
               
               
                   
                 total 
                 100.000000