KR20210008828A - Oral composition - Google Patents

Abstract

It provides an oral composition stably blending tranexamic acid or ε-aminocaproic acid, which is an anti-inflammatory component, and imparting an excellent halitosis inhibitory effect. Oral composition containing (A) tranexamic acid or ε-aminocaproic acid, (B) copper ions or zinc ions, and (C) sodium monofluorophosphate, and (C) having a component content of 0.8 to 3% by mass .

Description

Oral composition

The present invention relates to a composition for oral cavity in which tranexamic acid or ε-aminocaproic acid as an anti-inflammatory component is stably blended, and provides an excellent halitosis inhibitory effect.

Periodontal disease is often accompanied by bad breath, and the anti-inflammatory component and a medicinal ingredient effective for suppressing bad breath are added to an oral composition for the purpose of gum care to impart both effects to prevent periodontal disease or It is effective and desirable for inhibition.

Tranexamic acid and ε-aminocaproic acid, which have anti-inflammatory effects, are anti-inflammatory components used in oral compositions such as dentifrice for preventing periodontal disease, which is an inflammatory disease, but depending on the composition of the oral composition, The stability may deteriorate and discoloration of the formulation may be caused over time, and other ingredients cannot be easily added, making it difficult to use other bad breath suppressing ingredients in combination.

In Patent Document 1 (Japanese Patent No. 5842565), tranexamic acid or ε-aminocaproic acid, cinnamic aldehyde and an alkyl sulfate are blended to suppress discoloration of a liquid oral composition.

By the way, copper or zinc has an action of inhibiting volatile sulfur compounds (VSC) generated from periodontal disease causative bacteria, and water-soluble copper or zinc compounds that supply copper or zinc ions are known as components having a bad breath inhibiting action. The lasting effect of halitosis suppression was not sufficient.

In Patent Documents 2 and 3 (Japanese Patent No. 2580657, Japanese Patent No. 2738021), a polybasic acid or modified aluminum hydroxide can be used in combination with a water-soluble copper compound such as copper gluconate and copper citrate to improve the effect of preventing bad breath. Is proposed.

Japanese Patent No. 5842565 Japanese Patent No. 2580657 Japanese Patent No. 2738021 Japanese Patent No. 3922329

The present invention has been made in view of the above circumstances, and an object of the present invention is to provide a composition for oral cavity stably blending tranexamic acid or ε-aminocaproic acid as an anti-inflammatory component and providing an excellent lasting effect of suppressing bad breath.

The inventors of the present invention conducted a thorough study in order to achieve the above object, and as a result of the anti-inflammatory component (A) tranexamic acid or ε-aminocaproic acid, and (B) copper ions or zinc ions as the halitosis suppressing component, preferably the above When a water-soluble copper compound or zinc compound is used in combination as a source of ions, and (C) sodium monofluorophosphate is combined in a specific amount and blended into an oral composition, discoloration of the formulation derived from (A) component is suppressed even after storage. In addition, it was discovered that the halitosis suppressing effect persisted even after several hours from immediately after use, and that the component (A) could be stably blended and an excellent halitosis suppressing effect could be imparted, and the present invention was accomplished.

In more detail, even if the component (B) which has anti-inflammatory action and component (B) which has an anti-inflammatory action are used in combination in an oral composition, the anti-odor effect does not persist, and it is almost confirmed after several hours of use. (See Comparative Example 6 described later). Further, when the (B) component is increased in order to improve the lasting effect of halitosis, there has been a problem in the formulation stability that discoloration of the formulation derived from the component (A) is caused (described later). See Comparative Example 5). Therefore, in order to solve the problem related to the suppression of bad breath and discoloration of the formulation, the present inventors further studied.When the component (C) is further added in a specific amount, the above problem is solved and discoloration of the formulation is suppressed even after storage. In addition, even if the component (B) was not mixed in a relatively large amount, the effect of suppressing bad breath could be sustained. And by this, in addition to the anti-inflammatory effect of the component (A), it became possible to impart an excellent halitosis suppressing effect lasting several hours even after use. In this case, even if the (C) component was used in combination with the (A) and (B) components, discoloration of the formulation was confirmed when the (C) component amount was relatively small and an inappropriate amount (refer to Comparative Examples 1 and 2 described later), (C) component When the addition amount of is not less than a specific value, unexpectedly, discoloration of the formulation was suppressed by the component (C), and discoloration of the formulation was hardly observed even after long-term storage (see Examples to be described later). Therefore, according to the present invention, the above-described special effects can be provided by simultaneously blending the component (A) and the component (B).

The effect of the present invention is, for example, as shown in Comparative Example 4 described later, if disodium hydrogen phosphate is used instead of the component (C), the lasting effect of suppressing bad breath is inferior, and, in place of the component (C), When a fluorine-containing compound is used, or when copper citrate which is poorly soluble in water is used instead of the component (B), the effect of the present invention is inferior. On the other hand, the composition for oral cavity containing the components (A), (B) and (C) of the present invention shown in the examples, and the content of the component (C) is within a specific range, discoloration of the formulation is suppressed even after storage It was excellent in the absence of a bad breath, and the effect of suppressing bad breath (immediately after) and its persistence (after 3 hours) were excellent.

In addition, Patent Document 4 (Japanese Patent No. 3922329) is an invention in which the astringent and metallic taste of a dentifrice composition containing a condensed phosphate or the like and a water-soluble transition metal compound is improved while preventing discoloration by amino acids. It does not focus on and does not mention any.

Therefore, the present invention provides the following oral composition.

〔One〕

(A) tranexamic acid or ε-aminocaproic acid,

(B) copper ions or zinc ions, and

(C) sodium monofluorophosphate

A composition for oral cavity containing, and the content of (C) component is 0.8-3 mass %.

〔2〕

(B) The oral composition according to [1], wherein the source of the copper ion or zinc ion is a water-soluble copper compound or zinc compound having a water solubility at 25°C of 5 g/100 mL or more.

(3)

(B) [1] or [2] wherein the source of the copper ion or zinc ion is one or two or more water-soluble copper compounds or zinc compounds selected from copper gluconate, sodium copper chlorophyllin, zinc chloride and zinc gluconate. The oral composition according to [].

〔4〕

(B) The oral composition according to [1], wherein the supply source of copper ions or zinc ions is an acidic aqueous solution of a poorly water-soluble or water-insoluble copper compound or zinc compound having a water solubility at 25°C of less than 5 g/100 mL.

(5)

The oral composition according to any one of [1] to [4], containing 0.006 to 0.5 mass% of the component (A) and 0.001 to 0.1 mass% of the component (B).

(6)

The oral composition according to any one of [1] to [5], wherein (C)/(B) is 10 to 1,500 as a mass ratio.

(7)

The oral composition according to any one of [1] to [6] which is a dentifrice composition.

According to the present invention, there is provided a composition for oral cavity that stably blends tranexamic acid or ε-aminocaproic acid as an anti-inflammatory component, and provides an excellent halitosis suppressing effect lasting several hours from immediately after use. can do. The oral composition can be effectively used for preventing or inhibiting periodontal disease.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention contains (A) tranexamic acid or ε-aminocaproic acid, (B) copper ions or zinc ions, and (C) sodium monofluorophosphate. The ``copper ions or zinc ions'' refer to copper ions or zinc ions of a copper compound or zinc compound dissolved in a liquid medium (water, etc.) of the composition, and an insoluble copper compound or zinc present in a solid form in the composition Not a compound.

(A) Tranexamic acid or ε-aminocaproic acid is an active ingredient having anti-inflammatory action. Tranexamic acid and ε-aminocapronic acid can be used as the component (A), but tranexamic acid and ε-aminocaproic acid can also be used in combination.

The blending amount of the component (A) is preferably 0.006 to 0.5% (mass%, hereinafter the same) of the whole composition, more preferably 0.03 to 0.2%. The larger the blending amount, the higher the anti-inflammatory effect, and if it is 0.006% or more, a sufficient anti-inflammatory effect is obtained. If it is 0.5% or less, discoloration of the formulation is sufficiently suppressed, and the expression of irritation caused by the component (A) itself can be sufficiently prevented.

(B) The component is a copper ion or a zinc ion.

Copper ions or zinc ions dissolved in the oral composition of the present invention are components having a bad breath suppressing effect. As (B) component, the said copper ion or zinc ion can be used individually, or both ions can be used together.

The component (B) can be said to be derived from a water-soluble compound, and can be blended using a water-soluble copper compound or a zinc compound as the source of the ion. The water-soluble compound herein is a compound having a water solubility of 5 g/100 mL or more at 25°C. Examples of such a water-soluble copper compound include copper gluconate, copper sulfate, copper chloride, sodium copper chlorophyllin, and copper acetate. The water-soluble zinc compound includes zinc chloride, zinc sulfate, zinc nitrate, and zinc gluconate. These can be used alone or in combination of two or more, but among them, copper gluconate, copper chlorophyllin sodium, zinc chloride, zinc gluconate are preferable, more preferably copper gluconate of a water-soluble copper compound, It is copper chlorophyllin sodium.

As for the component (B), as another form, a poorly water-soluble or insoluble copper compound, copper ions and zinc ions derived from a solution obtained by dissolving a zinc compound in another solvent may be used, or the above solution may be used as a source of ions and blended. For example, copper ions and zinc ions obtained by dissolving water-insoluble copper oxide or zinc oxide in an acidic aqueous solution such as dilute hydrochloric acid can also be used. Further, a metal complex may be formed and dissolved in the system. Here, "poorly water soluble or insoluble" means that the water solubility at 25°C is less than 5 g/100 mL.

The blending amount of the component (B) is the amount of copper ions and zinc ions, preferably 0.001 to 0.1% of the total composition, and more preferably 0.005 to 0.05%. When the blending amount is 0.001% or more, the halitosis suppressing effect and its persistence are sufficiently obtained, and when it is 0.1% or less, discoloration of the formulation is sufficiently suppressed.

As the component (B), it is preferable to blend the copper compound and the zinc compound in an amount satisfying the range of the blending amount of the component (B). In this case, the blending amount of the copper compound and the zinc compound is It is preferably 0.01 to 0.5%, particularly 0.05 to 0.3%.

(C) Sodium monofluorophosphate is already known as an active ingredient for preventing tooth decay, but in the present invention, by blending at a predetermined concentration or more, it has an action of suppressing discoloration of the formulation due to the combination system of the components (A) and (B), In addition, it serves to improve the persistence of the halitosis inhibitory effect. Further, when a fluorine-containing compound other than the component (C), for example sodium fluoride, is used, discoloration of the formulation is not suppressed, and the effect of the present invention is inferior.

The blending amount of the component (C) is 0.8 to 3% of the total composition, preferably 1 to 2%, particularly 1 to 1.5%. If the blending amount is not satisfied at 0.8%, the inhibitory effect of discoloration of the formulation is inferior. The higher the blending amount, the more the discoloration of the formulation is suppressed, and the persistence of the halitosis suppressing effect increases, but if it exceeds 3%, the astringent taste and bitter taste due to the component (C) itself are expressed, making it unsuitable for use.

In the present invention, (C)/(B) representing the ratio of the (B) component amount (the amount of copper ions and zinc ions) and (C) the component amount is not particularly limited, but the mass ratio is preferably 10 to 1,500, more preferably. It is preferably 35 to 1,100, more preferably 35 to 150. If it is within the above range, the discoloration inhibitory effect of the formulation is more excellent, and the halitosis inhibitory effect and its persistence are also excellent. When the mass ratio of (C)/(B) is less than 10, the effect of suppressing discoloration of the formulation may not be sufficiently obtained, and when it exceeds 1,500, the persistence of the halitosis suppressing effect may not be sufficiently obtained.

The composition for oral cavity of the present invention can be prepared in various formulations such as dentifrice, liquid toothpaste, etc., mouthwash, coating agent, spray, patch, chewing gum, gummi, but preferably dentifrice, mouthwash, coating agent , In particular, it is prepared with a dentifrice, especially a toothpaste, and is more preferably a dentifrice composition. In addition, the oral composition can be prepared by employing a commercial method according to the formulation. In this case, in addition to the above components, other known components may be optionally blended depending on the purpose of the composition, formulation, and the like. For example, in the case of toothpaste, active ingredients other than abrasives, viscous agents, binders, surfactants, sweeteners, preservatives, coloring agents, flavoring agents, and (A), (B) and (C) components as needed Can be blended, and can be prepared by mixing these components and water.

Abrasives include silica-based abrasives such as precipitated silica, aluminosilicate, and zirconosilicate, calcium phosphate abrasives such as dicalcium phosphate, dihydrate or anhydride, calcium phosphate, calcium phosphate, calcium carbonate, and aluminum hydroxide. Can be mentioned. The blending amount of the abrasive is preferably 0 to 50%, particularly 5 to 30% of the total composition.

Examples of the viscosity aid include sugar alcohols such as sorbitol, xylitol, and erythritol, and polyhydric alcohols such as glycerin and propylene glycol. The blending amount of the viscous agent is preferably 5 to 60%, particularly 20 to 50% of the total composition.

The binder may contain an organic or inorganic binder. Specifically, organic binders include cellulose derivatives such as sodium carboxymethylcellulose and methylcellulose, gums such as xanthan gum and gum arabic, alginic acid derivatives, carrageenan, and inorganic binders: gelatinous silica, gelatinous aluminum silica, bigum, rapo There is a knight. The blending amount of the binder can be adjusted according to the formulation, and in the case of toothpaste, the organic binder is preferably 0.1 to 5%, particularly 0.5 to 3% of the composition, and the inorganic binder is 1 to 10%, particularly 2 ∼8% is good. In the oral detergent of a liquid formulation, 0-5% of the whole composition is good for both an organic caking agent and an inorganic caking agent.

As surfactants, anionic surfactants, nonionic surfactants, cationic surfactants, and amphoteric surfactants can be blended.

Examples of the anionic surfactant include alkyl sulfates such as sodium lauryl sulfate, acylamino acid salts, and acyltaurine salts.

Nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters, sugar alcohol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerol fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene hydrogenated castor oil, and the like. Oxyethylene fatty acid ester and polyoxyethylene higher alcohol ether.

Cationic surfactants include alkyl ammonium salts, and amphoteric surfactants include alkyl betaine, fatty acid amide alkyl betaine, and fatty acid amide propyldimethylaminoacetic acid betaine.

The blending amount of the surfactant is preferably 0 to 10%, particularly 0.1 to 5% of the total composition.

The sweetening agent is sodium saccharin, and the preservative is paraoxybenzoic acid ester, benzoic acid, or its salt.

The colorants include Blue No. 1, Yellow No. 4, and titanium dioxide.

Flavors are peppermint oil, spearmint oil, anise oil, eucalyptus oil, wonter green oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, mentha oil, cardamom oil, coriander oil, mandarin oil, lime oil, Lavender oil, rosemary oil, laurel milk, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, duckweed oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweetie oil, Natural fragrances such as citron oil, iris concrete, absolute peppermint, absolute rose, and orange flower, and processing treatment of these natural fragrances (current part cut, tail part cut, fractionation, liquid extraction, essence, powder fragrance Hwa, etc.), and menthol, carbon, anetol, cineol, methyl salicylate, cinnamic aldehyde, eugenol, 3-1-mentoxypropane-1,2-diol, thymol, linalool, linalyl Acetate, limonene, menthone, menthyl acetate, N-substituted-paramentane-3-carboxamide, pinene, octylaldehyde, citral, fullegon, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allylcyclohexane Propionate, methylanthranylate, ethylmethylphenylglycidate, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethylsulfide, cycloten, furfural, trimethylpyrazine, ethyl lactate, ethyl A la carte flavors such as thioacetate, strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor, and other combination flavors can be mentioned. Although known fragrance materials used in the composition may be used in combination, it is not limited to the fragrances described in Examples. In addition, the blending amount is not particularly limited, but it is preferable to use 0.000001 to 1% of the perfume material in the composition, and 0.1 to 2% of the fragrance perfume using the perfume material in the formulation composition.

Active ingredients include medicinal ingredients related to periodontal disease, such as isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetylpyridinium chloride, sodium lauroylsarcosine, and other fungicides, vitamins such as vitamin E, allantoin, And herbal medicines such as hinokitiol, glycyrrhetinic acid, dipotassium glycyrrhizinate, sodium chloride, potassium nitrate, and barley. These optional active ingredients can be blended in an effective amount within a range that does not interfere with the effects of the present invention.

(Example)

Hereinafter, examples and comparative examples are shown, and the present invention is specifically described, but the present invention is not limited to the following examples. In addition, in the following examples, all represent% by mass unless otherwise specified.

[Examples, Comparative Examples]

The dentifrice composition (toothpaste) of the composition shown in Tables 1-3 was prepared by a conventional method, and evaluated by the following method. The results are also listed in Tables 1-3. The numerical value indicating the amount of the component (B) in the table is the amount of copper or zinc ions derived from the compound used.

Moreover, all of the dentifrice compositions of Examples had an anti-inflammatory effect.

<Evaluation method of formulation discoloration (no discoloration)>

The dentifrice composition was filled in a laminate tube container having a diameter of 8 mm for filling 100 g, and stored at 60°C for 1 month. Further, the dentifrice composition of the same composition was filled in the same container and stored at -5°C for 1 month to obtain a standard product for comparison. The discoloration state when each was extruded from a tube container after storage was observed, and evaluated by the following evaluation criteria by comparing with a standard product.

Evaluation standard

◎: No discoloration is observed compared to -5℃ preserved products (standard products)

○: Almost no discoloration is observed compared to the -5°C storage product (standard product).

×: Discoloration is confirmed compared with the -5°C preservation product (standard product).

<Bad breath suppression effect and evaluation method of its persistence>

A feeling of use was evaluated by a test subject consisting of five expert panelists. A toothbrush (Clinica Advantage toothbrush, 4-row compact, normal type) was moistened with 1 g of the chima composition and brushed for 3 minutes. The mouth was rinsed with water, and a questionnaire was conducted on the feeling of bad breath immediately after rinsing and after 3 hours of rinsing, and the halitosis suppressing effect (immediately after) and the persistence of the halitosis suppressing effect (after 3 hours) were respectively determined based on the following score criteria. The average score of 5 people was calculated|required, and it evaluated by the following evaluation criteria. In addition, food was prohibited during the evaluation of the halitosis inhibitory effect.

Rating criteria

5: do not feel bad breath

4: I hardly feel bad breath

3: A level with a little bad breath but no problem

2: I feel bad breath considerably

1: I feel bad breath very much

Evaluation standard

◎: Average score of 5 persons is 4 or more

○: Average score of 5 persons is 3 or more and less than 4 points

×: average score of 5 people is less than 3

Mass number

Copper gluconate: 453.84

Zinc chloride: 136.29

Zinc oxide: 81.408

Copper Ion: 63.546

Zinc Ion: 65.38

Claims (7)

(A) tranexamic acid or ε-aminocaproic acid,
(B) copper ions or zinc ions, and
(C) sodium monofluorophosphate
A composition for oral cavity containing, and the content of (C) component is 0.8-3 mass %. The method of claim 1,
(B) An oral composition wherein the source of the copper ion or zinc ion is a water-soluble copper compound or zinc compound having a water solubility at 25°C of 5 g/100 mL or more. The method according to claim 1 or 2,
(B) An oral composition wherein the source of copper ions or zinc ions is one or two or more water-soluble copper compounds or zinc compounds selected from copper gluconate, sodium copper chlorophyllin, zinc chloride and zinc gluconate. The method of claim 1,
(B) An oral composition wherein the source of copper ions or zinc ions is an acidic aqueous solution of a poorly water-soluble or water-insoluble copper compound or zinc compound having a water solubility at 25°C of less than 5 g/100 mL. The method according to any one of claims 1 to 4,
The composition for oral cavity containing 0.006 to 0.5 mass% of (A) component and 0.001 to 0.1 mass% of (B) component. The method according to any one of claims 1 to 5,
(C) / (B) is a composition for oral cavity of 10 to 1,500 as a mass ratio. The method according to any one of claims 1 to 6,
Oral composition, which is a dentifrice composition.