KR20110133573A - Composition for oral cavity - Google Patents

Abstract

(A) at least one copper compound selected from copper gluconate, copper sulfate and its hydrate, (B) betaine-type amphoteric surfactant, and (C) at least one sugar alcohol selected from erythritol, xylitol and mannitol To the composition for oral cavity. ADVANTAGE OF THE INVENTION According to this invention, it has the effect of providing sufficient convergence to the gum which is an effective feeling of periodontal disease improvement effect, and also exhibits the unpleasant bitterness improvement effect peculiar to a copper compound, and the inhibitory effect of oral mucosal irritation, and is excellent in a feeling. Can be provided.

Description

Composition for oral cavity {COMPOSITION FOR ORAL CAVITY}

This invention has the effect of providing sufficient convergence to the gum which is an effective feeling of the periodontal disease improvement effect, and exhibits the unpleasant bitterness improvement effect peculiar to a copper compound, and the inhibitory effect of oral mucosal irritation, and is excellent in a feeling of use. It relates to a composition for oral cavity containing a copper compound.

Background Art Conventionally, various oral compositions containing copper compounds have been proposed since copper compounds such as copper gluconate, copper citrate and copper sulfate have antibacterial effects, bad breath removal effects, and plaque formation inhibiting effects, and are derived from copper compounds. A variety of techniques have been proposed for improving or preventing discoloration (Patent Documents 1 to 5; Japanese Patent Laid-Open No. 2-212413, Japanese Patent Laid-Open No. 8-310928, Japanese Patent No. 2882017 and Japanese Patent Laid-Open No. 10-). 505831, Japanese Patent Laid-Open No. 2003-231621).

Generally in dentifrice, periodontal disease treatment drug, etc., a feeling of convergence of a gum is effective as an effect of a periodontal disease improvement effect, and a copper compound is used suitably as a component which has a convergence effect.

However, since the copper compound has an unpleasant taste such as bitterness or metal taste, and has oral mucosal irritation, the copper compound can be satisfactorily exhibited in effect. there is a problem. Many solutions have been proposed so far, and the applicant has proposed in Patent Document 6 (Japanese Patent Laid-Open No. 2003-137755) that a metal taste can be improved by incorporating a menthol derivative or the like into a metal ion-releasing compound such as copper. .

However, according to the studies of the present inventors, if the unpleasant taste such as bitterness derived from the copper compound is improved, the effect of imparting convergence is also impaired, and thus the effectiveness is insufficient, and the conventional feeling improvement technique is still improved in this respect. There was room. On the other hand, when the oral mucosa stimulation derived from a copper compound is suppressed, the effect of converging feeling is suppressed. Therefore, it is also difficult to suppress the oral mucosa stimulation without impairing the satisfactory convergence feeling derived from the copper compound.

Therefore, the development of the technique which can simultaneously have the unpleasant bitterness improvement effect derived from a copper compound, the inhibitory effect of oral mucosal irritation, and the effect of providing sufficient convergence to a gum is desired.

Patent Document 1: Japanese Patent Laid-Open No. 2-212413 Patent Document 2: Japanese Patent Application Laid-Open No. 8-310928 Patent Document 3: Japanese Patent No. 2882017 Patent Document 4: Japanese Patent Application Laid-Open No. 10-505831 Patent Document 5: Japanese Patent Application Laid-Open No. 2003-231621 Patent Document 6: Japanese Patent Application Laid-Open No. 2003-137755 Patent Document 7: Japanese Patent Application Laid-Open No. 2000-297022 Patent Document 8: Japanese Patent Application Laid-Open No. 2008-150335 Patent Document 9: Japanese Patent Application Laid-Open No. 2007-320894

This invention has the effect of providing sufficient convergence to the gum which is an effective feeling of the periodontal disease improvement effect, and exhibits the unpleasant bitterness improvement effect peculiar to a copper compound, and the inhibitory effect of oral mucosal irritation, and contains the copper compound excellent in usability. It is an object to provide a composition for oral cavity.

MEANS TO SOLVE THE PROBLEM The present inventors earnestly researched in order to achieve the said objective, As a result, (A) 1 or more types of copper compounds chosen from copper gluconate, copper sulfate, and its hydrate, (B) a betaine type amphoteric surfactant, ( C) By combining at least one sugar alcohol selected from erythritol, xylitol and mannitol in combination with the composition for oral cavity, an unpleasant bitterness improvement effect derived from a copper compound and an inhibitory effect on oral mucosal irritation and sufficient convergence to the gums It has been found that the effect can be combined.

In the composition for oral cavity containing a copper compound, the bitterness, oral mucosa irritation, and convergence feeling derived from a copper compound arise as a result of the copper compound interacting with the mucous membrane in an oral cavity. That is, as mentioned above, in the composition for oral cavity containing a copper compound, if unpleasant taste, such as bitterness derived from a copper compound, and oral mucosal irritation are suppressed, the effect of converging feeling will also be impaired at the same time. I think it's because I changed the interaction with. On the other hand, in this invention, a betaine type amphoteric surfactant and a sugar alcohol cooperate cooperatively with copper gluconate, copper sulfate, or its hydrate, and the interaction of a copper compound and the mucous membrane in an oral cavity differs from the above. By doing so, the bitterness derived from a copper compound improves, oral mucosal irritation is suppressed, and it is guessed that the effect of providing sufficient convergence to a gum can be maintained.

Such effects of the present invention are also apparent from the examples described later. When the present invention lacks any one of its constituent requirements, or when an amino acid type amphoteric surfactant is used in place of a betaine amphoteric surfactant, and saccharide or sorbitol is used in place of the component (C), It cannot be achieved and can be achieved by satisfying all of the structural requirements of the present invention.

Moreover, sugar alcohol is well-known as a compounding component to the composition for oral cavity, and is mix | blended normally as a moisturizing agent or the like. In addition, by combining sugar alcohols, a technique for improving discoloration of the preparation by a polyphenol-containing plant extract (Patent Document 7; Japanese Patent Application Laid-Open No. 2000-297022), to a composition containing a fluorine compound, sodium lauryl sulfate and trimethylglycine By combining erythritol, a composition showing an oral disease improvement effect can be obtained by combining a technique (Patent Document 8; Japanese Patent Application Laid-Open No. 2008-150335) with erythritol or copper bisglycinate and xylitol (Patent Document 4). ) And the like have been proposed. Moreover, as a technique which mix | blends an amphoteric surfactant with a composition for oral cavity, the fluorine compound containing sodium lauryl sulfate, a cationic polymer, and a betaine type amphoteric surfactant are mix | blended with the skirt composition containing fluorine compound, and the oral retention property of a fluorine compound, a feeling, etc. (Patent Document 9; Japanese Patent Application Laid-Open No. 2007-320894) and the like have been proposed. Moreover, the applicant has the technique (patent document 1) which mix | blends sugar alcohol whose reducing sugar content is 0.2 mass% or less as a moisturizing agent to the composition for oral cavity containing a copper compound, and the technique which mix | blends an amphoteric surfactant (patent document 3). ) Is proposed. These techniques enable the prevention of discoloration over time derived from a copper compound and the maintenance of bad breath removal effects, and the problems are different from the present invention. And no effect is shown.

Thus, various proposals have been made regarding the composition for oral cavity containing a copper compound, and sugar alcohol and an amphoteric surfactant are known as a compounding component of an oral composition. However, by combining a betaine type amphoteric surfactant and sugar alcohol erythritol, xylitol, or mannitol in combination with a composition for oral cavity containing copper gluconate, copper sulfate, or a hydrate thereof, an excellent convergence feeling derived from a copper compound It is a new study result of the present inventors that the unpleasant bitterness and oral mucosal irritation derived from a copper compound can be satisfactorily improved without impairing the imparting effect.

Therefore,

(A) at least one copper compound selected from copper gluconate, copper sulfate and hydrates thereof,

(B) a betaine amphoteric surfactant,

(C) at least one sugar alcohol selected from erythritol, xylitol and mannitol

It provides a composition for oral cavity comprising the.

The copper compound-containing composition for oral cavity of the present invention has a sufficient astringent imparting effect to the gum which is a feeling of effectiveness of the periodontal disease improving effect, and also exhibits an unpleasant bitterness improvement effect peculiar to the copper compound and an inhibitory effect on oral mucosal irritation. Excellent in feeling.

Hereinafter, the present invention will be described in more detail. The composition for oral cavity of this invention is chosen from (A) copper gluconate, a copper compound chosen from copper sulfate, and its hydrate, (B) a betaine type amphoteric surfactant, (C) erythritol, xylitol, and mannitol. It is characterized by containing one or more sugar alcohols.

As a copper compound which is (A) component, copper gluconate and copper sulfate may be used and may be used individually by 1 type or in combination of 2 types. Copper gluconate and copper sulfate may be anhydrides or hydrates, respectively. As a hydrate, the hydrate containing crystal water, such as copper sulfate pentahydrate, a trihydrate, and a monohydrate, can be used, for example.

As for the compounding quantity of a copper compound, 0.0026 to 0.51% (mass% or less) of the whole composition as copper in a compound is especially 0.013 to 0.26%, Especially 0.026 to 0.26% is preferable. If the blending amount is less than 0.0026%, the convergence feeling-derived effect derived from the copper compound may not be sufficiently exhibited. If the blending amount exceeds 0.51%, it may be difficult to sufficiently exhibit the bitterness improving effect, and the usability may not be satisfactorily improved.

As a betaine type amphoteric surfactant which is (B) component, a lauryl betaine, a stearyl betaine, a lauryl dimethylamino acetic acid betaine, a stearyl dimethyl amino acetic acid betaine, 2-alkyl-N-carboxymethyl-N-hydride Oxyethyl imidazolinium betaine, N-lauroyl-N'-carboxymethyl-N'-hydroxyethylethylenediamine sodium, lauric acid amide propyl betaine, palm oil fatty acid amide propyl betaine, lauryl hydroxy And syruppobetaine. Among them, lauryl dimethylamino acetic acid betaine, palm oil fatty acid amide propyl betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, N-lauroyl-N'-carboxymethyl It is preferably selected from -N'-hydroxyethylethylenediamine sodium. These betaine type amphoteric surfactants can be used individually by 1 type or in combination of 2 or more types.

A commercially available product can be used for a betaine type amphoteric surfactant, For example, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine (brand name Levon 105) and N-laux manufactured by Sanyo Kasei Co., Ltd. Loyl-N'-carboxymethyl-N'-hydroxyethylethylenediamine sodium (brand name Levon 101-H), palm oil fatty acid amide propyl betaine liquid (brand name Levon 2000), lauryl dimethylamino by Nikko Chemicals Betaine acetate aqueous solution (brand name NIKKOL AM-301) etc. are mentioned. As 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, 2-palm oil alkyl-N-carboxymethyl-N-hydroxy sold by Lion Co., Ltd. as brand name Enazol C-40H Aqueous sodium imidazolinium betaine solution may also be used.

As for the compounding quantity of a betaine type amphoteric surfactant, 0.01-5%, especially 0.05-2%, especially 0.1-1% of the whole composition are preferable. If the blending amount is less than 0.01%, the inhibitory effect of oral mucosal irritation may not be sufficiently exhibited. If the amount exceeds 5%, the problem of oral mucosal irritation caused by the surfactant may occur, and the bitter taste improvement effect may not be sufficiently exhibited. have.

(C) component is sugar alcohol chosen from erythritol, xylitol, and mannitol. These sugar alcohols may be used individually by 1 type, or may use 2 or 3 types together. When using two types together, combination of erythritol and xylitol is preferable.

As for the compounding quantity of the sugar alcohol which is (C) component, 2-50%, especially 5-30% of the whole composition are preferable, and 10-30% are the most preferable especially. If the blending amount is less than 2%, the bitterness improving effect may not be sufficiently exhibited. If the blending amount exceeds 50%, the effect of imparting convergence by the copper compound is inhibited, and the effect of suppressing oral mucosal irritation is not sufficiently exhibited. have.

The composition for oral cavity of the present invention can be prepared in various formulations, such as a skirt, a mouthwash, a gel, an ointment, a mouthwash, a toothbrush, a toothpaste, a mouthwash, a gum such as a toothpaste, a polished skirt and a liquid skirt. It is particularly preferably formulated as a dentifrice and a gel, in particular a gel. When prepared with such a formulation, the effects of the present invention can be more effectively expressed. In addition to the above essential ingredients, these preparations may be blended with other ingredients in accordance with the formulation, if necessary, within a range that does not impair the effects of the present invention, and may be prepared by conventional methods.

As other components, for example, in the case of a dentifrice, various abrasives, wetting agents, caking additives, surfactants, and sweeteners, colorants, coloring agents, preservatives, pH adjusters, other active ingredients, etc. can be mix | blended as needed. In the case of a gel agent, a wetting agent, a caking additive, surfactant, and a sweetener, a coloring agent, a coloring agent, a preservative, a pH adjuster, an alcohol, an oily component, other active ingredients, etc. can be mix | blended as needed.

As the abrasive, precipitated silica, silica gel, aluminosilicate, zeolite, zirconosilicate, dicalcium phosphate dihydrate and anhydride, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, alumina, magnesium carbonate, magnesium triphosphate, insoluble meta Sodium phosphate, insoluble potassium metaphosphate, titanium oxide, hydroxyapatite, synthetic resin-based abrasives, and the like (mixture amount; usually 5 to 50% based on the total composition).

Examples of the humectant include polyhydric alcohols such as sugar alcohols other than the (C) component, for example, sorbitol, glycerin, propylene glycol, polyethylene glycol, and 1,3-butylene glycol. When mix | blending a humectant, the compounding quantity is 10 to 50% normally.

Examples of the caking agent include cellulose derivatives such as sodium carboxymethyl cellulose and hydroxyethyl cellulose, alginic acid derivatives such as sodium alginate and propylene glycol esters, guar rubber, xanthan rubber, gum arabic, carrageenan, gelatin, and polyvinyl alcohol. And synthetic caking additives such as sodium polyacrylate, carboxyvinyl polymer, and polyvinylpyrrolidone (compound amount usually 0.5 to 10%).

As surfactant, things other than the betaine type amphoteric surfactant which is (B) component, for example, a nonionic surfactant, anionic surfactant, and cationic surfactant can be mix | blended.

Examples of nonionic surfactants include sugar alcohol fatty acid esters such as sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, and sucrose fatty acid esters, glycerin fatty acid esters, polyglycerol fatty acid esters, polyoxyethylene glycerin fatty acid esters, and polyethylene glycol fatty acid esters. Ether type or ester type surfactant, such as polyhydric alcohol fatty acid ester, polyoxyethylene alkyl ether, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene alkyl phenyl ether, polyoxyethylene hardened castor oil, lauric acid di Fatty acid alkanolamides, such as ethanolamide, are mentioned.

Examples of the anionic surfactants include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, sodium N-acyl salcosine, sodium dodecylbenzene sulfonate, such as sodium N-lauroyl salcosine, and sodium N-myristoyl sarcosine, N-acyl glutamate, such as hydrogenated coconut fatty acid sodium monoglyceride monosulfate, sodium lauryl sulfoacetate, sodium N-palmitoyl glutamate, sodium N-methyl-N-acyltaurine, sodium N-methyl-N-acylalanine, sodium α-olefin sulfonate; and the like. Examples of cationic surfactants include alkyl ammonium and alkylbenzyl ammonium salts.

When mix | blending these surfactant as an arbitrary component, the compounding quantity is 0.01 to 2% normally.

In addition, in this invention, since anionic surfactant, especially alkyl sulfates, such as sodium lauryl sulfate, tends to reduce usability, it is more preferable not to mix | blend. When mix | blending anionic surfactant, the compounding quantity is 0.5% or less, Especially 0 to 0.1% are preferable, but 0% may be sufficient. It is especially preferable that it is no compound.

Examples of sweeteners include sodium saccharin, stevioside, stevia extract, paramethoxycinnamicaldehyde, neohespyridylhydrochalcone, peraryllatin, and the like.

As a coloring agent, Blue No. 1 (FD & C Blue No. 1 (42090)), Yellow No. 4 (FD & C Yellow No. 5 (19140)), titanium dioxide, etc. are mentioned. As a preservative, benzoic acid, such as a palaoxybenzoic acid ester and sodium benzoate, or its salt, etc. are mentioned. Examples of the drug include terpenes such as l-menthol, carbon, anetol, and limonene, derivatives thereof, peppermint oil, and the like.

Citric acid, fumaric acid, malic acid, tartaric acid, lactic acid, etc. are mentioned as a pH adjuster.

Examples of the alcohol include lower alcohols having 3 or less carbon atoms such as ethanol. When mix | blending an alcohol, the compounding quantity is 1 to 20% normally.

As the oily component, hydrocarbon oils such as liquid paraffin, hard liquid paraffin, paraffin wax, ceresin, microcrystalline wax, squalane and squalene, lauric acid, myristic acid, parmitic acid, stearic acid, lauloric acid, oleic acid, Fatty acids such as arachidonic acid, linoleic acid, linolenic acid, and ricinolic acid, linseed oil, sesame oil, soybean oil, soybean oil, corn oil, rapeseed oil, cottonseed oil, olive oil, camellia oil, castor oil, cacao oil, palm oil and palm oil And animal oils such as beef tallow, pork tallow, marzipan and yangji. Among these, hydrocarbon oil is preferable at the point of retention in the oral cavity of a preparation, More preferably, they are liquid paraffin and hard fluid paraffin. When mix | blending an oil-based component, the compounding quantity is 0.1 to 10% normally.

As an active ingredient, things other than the copper compound which is (A) component, For example, vitamins, such as ascorbate and tocopherol ester, enzymes, such as dextranase, mutanase, and lysozyme, sulfur white extract, golden extract, and sperm Herbicides such as extracts, fungicides such as cetylpyridinium chloride, benzetonium chloride, benzalkonium chloride, decuanium chloride, chlorhexidine hydrochloride, gluconate chlorhexidine, triclosan, isopropylmethylphenol, and hygithiol And inorganic salts and organic salts such as sodium chloride, sodium polyphosphate, sodium metaphosphate, sodium oleate, sodium tripolyphosphate, aluminum lactate and chitosan. In addition, the compounding quantity of these active ingredients can be made an effective amount in the range which does not prevent the effect of this invention.

Example

Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not limited to a following example. In addition, in the following example, all compounding quantities are the mass%. In addition, about the component of aqueous solution, the form showed the compounding quantity of pure part conversion including the inside of a table | surface.

[Example, Comparative Example]

The composition for oral cavity (gel) of the composition shown to Tables 1-4 was prepared, and about 0.5 g of the composition for oral cavity was apply | coated to the gums of five expert panels with the finger. After the sensory evaluation by the four-step evaluation criteria shown below, the convergence feeling effect, the oral mucosal irritation effect, and the bitter taste improvement effect with respect to the gum immediately after, were evaluated according to the following evaluation criteria. The results are shown in Tables 1-5. In addition, the detail of a compounding component is shown in Table 6.

Convergence effect;

grade

4 points | pieces: A feeling of convergence is felt.

3 points | pieces: A feeling of convergence is felt a little.

2 points | pieces: A feeling of convergence is hardly felt

1 point: It does not feel a convergence

Criterion for evaluation of convergence effect;

◎: 3.5 points or more and 4.0 points or less

○: 3.0 points or more and less than 3.5 points

△: 2.0 points or more and less than 3.0 points

×: less than 2.0 points on average of convergence

Inhibitory effect of oral mucosal irritation;

grade

4 points | pieces: It does not feel a stimulus at all.

3 points | pieces: I hardly feel a stimulus.

2 points | pieces: I feel a little stimulation.

1 point | piece: I feel a stimulus

Evaluation criteria for the inhibitory effect of oral mucosal stimulation;

◎: 3.5 points or more and 4.0 points or less of the average point of the inhibitory effect of oral mucosa stimulation

(Circle): Average point 3.0 or more and less than 3.5 points of the inhibitory effect of oral mucosal irritation

(Triangle | delta): 2.0 points or more and less than 3.0 points of average points of the inhibitory effect of oral mucosal irritation

×: less than 2.0 points on average of the inhibitory effect of oral mucosa stimulation

Bitterness improvement effect;

grade

4 points: It does not feel bitter at all.

3 points: hardly feel bitter taste

2 points | pieces: A little bitter taste

1 point | piece: Feel bitterness, or strong irritation

Evaluation criteria of bitterness improvement effect;

◎: 3.5 points or more and 4.0 points or less

(Circle): Average point 3.0 or more and less than 3.5 points of bitterness improvement effect

(Triangle | delta): 2.0 points or more and less than 3.0 points of average points of the bitterness improvement effect

X: Less than 2.0 points on average of bitterness improvement effect

Claims (4)

(A) at least one copper compound selected from copper gluconate, copper sulfate and hydrates thereof,
(B) a betaine amphoteric surfactant,
(C) Oral composition containing at least 1 type of sugar alcohol selected from erythritol, xylitol, and mannitol. The method of claim 1,
Betaine-type amphoteric surfactants include lauryldimethylaminoacetic acid betaine, palm oil fatty acid amidepropylbetaine, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazoliniumbetaine and N-lauroyl-N Oral composition characterized by the 1 type (s) or 2 or more types chosen from sodium "-carboxymethyl-N" -hydroxyethylethylenediamine. 3. The method according to claim 1 or 2,
(A) Component contains 0.013-0.26 mass% as copper, 0.05-2 mass% of (B) component, and 5-30 mass% of (C) component, The composition for oral cavity characterized by the above-mentioned. 4. The method according to any one of claims 1 to 3,
A composition for oral cavity, which is prepared as a gel agent.