JP4681269B2 - Liquid oral composition - Google Patents

Description

  The present invention relates to a composition for liquid oral cavity with good usability that suppresses the formation of plaque and improves bitterness derived from a bactericidal agent.

It is widely known that dental plaque is a cause of caries and periodontal disease. Plaque formation begins when proteins contained in saliva or the like are adsorbed on the tooth surface to form a film called a pellicle, and bacteria are adsorbed on the pellicle. Therefore, compositions that inhibit the adsorption of bacteria to the tooth surface have been proposed, but the effect of suppressing the plaque formation of these compositions has not been sufficient (Patent Documents 1 and 2).
In addition, compositions that inhibit the adsorption of salivary proteins to the tooth surface by a polymer composed of a phosphorus acid and consequently inhibit the adsorption of bacteria to the tooth surface have been reported (Patent Documents 3 and 4). However, since these components are polymers having a large molecular weight, the aqueous solution has viscosity, and cannot be applied to a liquid composition such as a mouthwash.
JP-A-57-135817 JP-A-9-175965 JP 2003-48842 A JP 2003-105031 A

  An object of the present invention is to provide a component that can be blended in a liquid composition such as a mouthwash and suppresses the formation of a pellicle on the tooth surface, and a liquid oral composition containing the component.

  Therefore, as a result of searching for low molecular weight compounds that inhibit protein adsorption to the tooth surface, the present inventor has found that erythritol, xylitol, and palatinit have an excellent pellicle formation inhibitory action. Furthermore, when these sugar alcohols are blended with a combination of maltitol and / or lactitol and a cationic bactericidal agent, a liquid oral composition having an excellent plaque formation inhibitory effect, a good feeling of use and excellent continuous use is obtained. I found out that

That is, the present invention includes the following components (A), (B) and (C):
(A) one or more selected from the group consisting of erythritol, xylitol and paratinite,
(B) a cationic fungicide,
(C) A liquid oral composition containing maltitol and / or lactitol is provided.
Moreover, this invention provides the pellicle formation inhibitor in the tooth surface which uses an erythritol, a xylitol, and / or a palatinit as an active ingredient.

  According to the present invention, the pellicle formation on the tooth surface, which is the first stage of plaque formation, is suppressed, the antibacterial agent is effective in suppressing plaque formation, and the bitterness of the antibacterial agent is improved. Since it is favorable, a liquid oral composition excellent in continuous use is provided.

  The (A) erythritol, xylitol and / or palatinit used in the present invention has pellicle formation inhibition on the tooth surface. The pellicle formation is the first stage of plaque formation that causes caries and periodontal disease as described above, and the pellicle formation inhibitor containing these components (A) is a plaque formation inhibitor, Furthermore, it is useful as a preventive agent for caries and periodontal disease. It was first discovered by the present inventor that these components (A) have a pellicle formation inhibitory action. A component (A) can be used individually or in combination of 2 or more types.

  The said component (A) is 3-30 mass% in this invention liquid oral composition from the point of the pellicle formation inhibitory effect, Furthermore, it is preferable to contain 5-20 mass%, especially 6-15 mass%.

  (B) Cationic fungicides adsorb on oral tissue surfaces such as tooth surfaces, oral mucosa (including gums), etc., and have a bactericidal action against bacteria that cause caries, periodontal disease, bad breath, etc. And quaternary ammonium compounds and biguanide compounds. Examples of the bactericides belonging to the quaternary ammonium compounds include cetylpyridinium chloride, decalinium chloride, benzethonium chloride, benzalkonium chloride, alkyldimethylammonium chloride, alkyltrimethylammonium chloride, methylbenzethonium chloride, lauroylcoraminoformylmethylpyridinium chloride, and the like. Is mentioned. Examples of the bactericides belonging to the biguanide compounds include chlorhexidine and salts thereof, preferably chlorhexidine gluconate and chlorhexidine hydrochloride. Component (B) is preferably contained in the composition for liquid oral cavity of the present invention in an amount of 0.001 to 0.5 mass%, more preferably 0.005 to 0.2 mass%, from the viewpoint of bactericidal action and taste.

(C) Maltitol and / or lactitol have the effect | action which masks the bitter taste of the said (B) cationic disinfectant, improves the taste of this invention liquid oral composition, and improves a usability | use_condition. The bitterness masking effect of the component (C) is remarkably excellent when combined with the component (A). Component (C) is preferably contained in the composition for liquid oral cavity of the present invention in an amount of 0.1 to 30% by mass, more preferably 0.5 to 20% by mass, and particularly preferably 1 to 15% by mass from the viewpoint of the bitterness improving effect. .
Moreover, it is preferable that a component (C) contains 10-3000 mass parts with respect to 1 mass part of a component (B) from the point of a bitterness improvement effect, Furthermore, 50-2000 mass parts, Especially 75-1500 mass parts is contained.

  It is preferable to mix | blend ethanol with the liquid oral cavity composition of this invention from the point of a bactericidal effect and a refreshing feeling further. The content of ethanol is preferably 0.5 to 30% by mass, more preferably 1 to 20% by mass, and particularly preferably 4 to 15% by mass in the liquid oral composition.

  In the liquid oral composition of the present invention, an oil-soluble fragrance can be blended in order to improve the bitterness of the cationic fungicide. Examples of the oil-soluble fragrances include menthol, carvone, anethole, eugenol, cineol, thymol, methyl salicylate, pulegone, menthone, pinene, limonene, menthyl acetate, as well as peppermint oil, spearmint oil, mint oil, etc. Citrus oil such as mint oil, lemon, orange, grapefruit, lime, eucalyptus, sage, rosemary, thyme, laurel, basil, perilla, bay, estragon, parsley, celery, coriander, herb oil, cinnamon, pepper, nutmeg, Natural essential oils such as spice oil such as mace, clove, ginger, cardamom, anise, apple, banana, melon, grape, peach, strawberry, blueberry, raspberry, blackcurrant, lychee, star fruit, Tsu Deployment fruit, can be used plum, pineapple, and fruit flavors, such as Muscat. Among these oil-soluble fragrances, menthol, carvone, peppermint oil, spearmint oil, peppermint oil, methyl salicylate, cineol, limonene, and pinene are particularly preferable from the viewpoint of imparting a refreshing feeling and refreshingness to the oral cavity. These oil-soluble fragrances are used alone or in combination of two or more. These oil-soluble fragrances are from 0.1 to 1% by mass, more preferably from 0.2 to 0.6% by mass, particularly from 0.2 to 0.6% by mass in the liquid oral composition of the present invention from the viewpoint of obtaining the masking effect of the cationic fungicide. It is preferable to contain 0.3-0.5 mass%.

  Furthermore, nonionic surfactants, anionic surfactants, binders, polyhydric alcohols, buffers, other medicinal agents, sweeteners, water, and the like can be blended in the liquid oral cavity composition of the present invention.

  Nonionic surfactants include sugar fatty acid ester, polyglycerin fatty acid ester, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid ester, polyoxyethylene polyoxypropylene block copolymer type nonionic surfactant, fatty acid alkanolamides, polyoxyethylene fatty acid Examples include esters, fatty acid monoglycerides, polyoxyethylene alkyl ethers, and the like. Among these, from the viewpoint of suppression of plaque formation, it is preferable that polyglycerin fatty acid ester, sucrose fatty acid ester, maltose fatty acid ester or lactose fatty acid ester is contained. These nonionic surfactants are preferably contained in the liquid oral composition of the present invention in an amount of 0.01 to 2% by mass, more preferably 0.05 to 1% by mass, and particularly preferably 0.1 to 0.8% by mass.

  Examples of the anionic surfactant include alkyl sulfate salts such as sodium lauryl sulfate and sodium myristyl sulfate; N-acyl amino acid salts such as sodium lauroyl sarcosine; acyl taurine salts such as sodium lauroylmethyl taurine; sodium coconut oil fatty acid ethyl ester sulfonate And fatty acid ester sulfonates such as salts.

  The content of these anionic surfactants is 0.01% by mass or less (0 to 0.01% by mass) in the liquid oral composition from the viewpoint of stimulation and adsorption of the cationic bactericidal agent to the teeth and the like. preferable.

  As a binder, cellulose derivatives such as sodium carboxymethyl cellulose and hydroxyethyl cellulose, alginic acid derivatives such as sodium alginate and propylene glycol alginate, gums such as carrageenan, xanthan gum, duran gum, tragacanth gum and karaya gum, polyvinyl alcohol, sodium polyacrylate, Examples thereof include synthetic binders such as carboxyvinyl polymer, inorganic binders such as silica gel, bee gum and laponite, and starch degradation products such as dextrin and reduced dextrin. One or more of these can be mixed and used.

  Examples of the polyhydric alcohol include propylene glycol, glycerin, and polyethylene glycol. Examples of the buffer include citric acid and its salt, malic acid and its salt, phosphoric acid and its salt, and the like. Examples of the sweetener include saccharin sodium, acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perilartine, saumatine, asparatylphenylalanyl methyl ester, sucralose and the like. Other medicinal agents include anti-plasmin agents such as tranexamic acid and epsilon aminocaproic acid, vitamins such as ascorbic acid and tocopherol ester, glycyrrhizin salts, allantoins, plant extracts such as buckwheat, oxon, chamomile, latania and myrrh. Enzymes such as stranase, mutanase, lysozyme chloride, alkali metal monofluorophosphates such as sodium monofluorophosphate, fluorides such as sodium fluoride, stannous fluoride, sodium chloride, potassium nitrate, carbonate, bicarbonate , Salts such as sesquicarbonate, copper chlorophyllin sodium, copper gluconate, zinc chloride, zeolite, water-soluble inorganic phosphate compound, aluminum lactate, etc.

  The liquid oral composition of the present invention can be applied as liquid dentifrice, water dentifrice, mouthwash, mouth spray, mouthwash, and the like.

Of the compositions shown below, Examples 2 and 3 and Formulation Example 1 in Example 1 are reference examples and are not included in the scope of the claims. Comparative products 3 and 4 in the second embodiment are comparative products in the invention according to claim 2, and correspond to the embodiment of the invention according to claim 1.
Example 1
Mouthwash solutions shown in Table 1 were prepared, and a pellicle formation inhibition test on a tooth surface model was performed. That is, using hydroxyapatite powder (Taipei Chemical Industry; hereinafter abbreviated as HA), which is the main component of enamel, as a tooth model, and adding bovine serum albumin as a protein source while being dispersed in the mouthwash. After adsorbing the pellicle to the HA powder, the protein was quantified by (fluorescamine method).
The time until the protein amount is almost saturated is shown in FIG. 1 as the pellicle formation time.
In comparison products 1 and 2 containing glycerin or maltitol, a pellicle was formed in 30 minutes, whereas in products 1 to 3 containing erythritol, xylitol, or palatinit, it took 70 to 80 minutes to form a pellicle. It can be seen that pellicle formation was suppressed.

Example 2
The mouthwashes shown in Table 2 were prepared, and the bitterness remaining in the mouth when 10 mL of each mouthwash was sprinkled and exhaled for 30 seconds was determined according to the criteria shown below.
Judgment criteria ◎: not bitter ○: slightly bitter △: slightly bitter ×: quite bitter

Example 3 Artificial Biofilm Formation Inhibition Test A pellet plate (hereinafter abbreviated as HAP) obtained by compressing hydroxyapatite powder, which is a main component of enamel, into a flat plate having a diameter of about 8 mm was used as a tooth model. After preparing the mouthwash shown in Table 3, saliva collected from a human was added to 10 mL of each mouthwash, and HAP was immersed at 37 ° C. for 90 minutes to form a pellicle. HAP was washed with 10 mL of ion-exchanged water, then immersed in a culture solution obtained by adding sucrose to saliva collected from humans, and cultured at 37 ° C. for 4 days under anaerobic conditions. After culturing, the biofilm on the HAP surface is stained with plaque stain solution, and the stained area is image-processed (average value of R after color separation by RBG: measuring instrument VH-7000 (manufactured by Keyence): analysis software WIN ROOF (Mitani)). The amount of biofilm formed was calculated based on the amount of biofilm formed on the HAP surface when treated with ion-exchanged water instead of the mouthwash, and is shown in FIG. Comparative products 7 and 8 formed 90% or more of biofilms of HAP treated with ion-exchanged water, whereas example product 9 formed only 60% of biofilms.

Formulation Example 1

Formulation Example 2

It is a figure which shows time (minute) until pellicle formation to the tooth surface model of each mouthwash. It is a figure which shows the artificial plaque formation amount (%) of each mouthwash.

Claims (5)

As an active ingredient, (A) 3-15 mass% of erythritol , ( B) 0.001-0.5 mass% of cationic bactericides, and 0.5-15 mass% of ethanol are contained, and an anionic surfactant is contained. A tooth surface pellicle formation inhibitor not contained .   The pellicle formation inhibitor according to claim 1, further comprising (C) 1 to 15% by mass of maltitol and / or lactitol. Furthermore, the pellicle formation inhibitor of Claim 1 or 2 containing 0.1-0.8 mass% of nonionic surfactant . Furthermore, the pellicle formation inhibitor of any one of Claims 1-3 which contains 0.1-1 mass% of oil-soluble fragrance | flavors. As an active ingredient, (A) 3-15 mass% of erythritol , ( B) 0.001-0.5 mass% of cationic bactericides, and 0.5-15 mass% of ethanol are contained, and an anionic surfactant is contained. A method for inhibiting pellicle formation, which comprises applying a liquid oral composition not contained on a tooth surface.

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