JP2020055765A - Oral composition - Google Patents

Abstract

To provide an oral composition that has an improved effect of imparting a tightening feeling with an astringent compound, without giving gums discomfort irritation.SOLUTION: An oral composition contains (A) at least one allantoin selected from allantoin, aluminium chlorohydroxy allantoinate and allantoin dihydroxyaluminum or a derivative thereof and (B) menthyl glutarate, and the oral composition further contains (C) an ethanol.SELECTED DRAWING: None

Description

  The present invention relates to an oral composition having an improved astringent tightening effect of an astringent compound without giving unpleasant stimulation to the gums.

In order to realize the effect of improving the gums on the gums that have weakened due to an oral disease or the like, it is desirable to impart a moderate tightening feeling and a firm feeling instead of the pain and numbness reminiscent of stimulation of the gums.
The astringent compound exerts a gum tightening sensation when incorporated into the oral composition. Conventionally, complex phosphates such as sodium pyrophosphate and sodium tripolyphosphate, sodium chloride, allantoin and derivatives thereof have been known as astringent compounds (Patent Documents 1 and 2; JP-A-61-155315). And JP-A-11-21219). However, when the complex phosphate is used at a high concentration, there is a risk of exfoliation of the mucous membrane. At a low concentration, the complex phosphate has a stronger sensation of the teeth than the actual feeling of the gums, and thus has a poor effect on the gums. In addition, sodium chloride has a problem that the salty taste is strong and the feeling of use is impaired at a compounding amount that expresses a tightening feeling, and the feeling of use is particularly severely impaired in a liquid oral composition as compared with toothpaste.
On the other hand, allantoin and its derivatives are known as components that can be blended into oral compositions mainly as compounds that exert a firm feeling on gums, and are also applied to liquid oral compositions, It is susceptible to the effects of the ingredients and the pH of the preparation, and may cause a decrease in taste when the amount is increased, and there is room for improvement in the gum tightening effect.

  By the way, capsaicin, a pungent component, and monomenthyl succinate, a cooling agent, are known as components that enhance the tightening effect of the gums. This leads to a feeling of unpleasant irritation such as chattering, and there is a problem that a person with a gingival symptom such as gingivitis that is sensitive to a slight stimulus may lack the sensation of damaging the gums.

  Patent Literature 3 (Japanese Patent No. 5470837) discloses that isopropylmethylphenol, allantoin or a derivative thereof, polyoxyethylene hydrogenated castor oil, a specific acid and alkali agent, spiranthol, capsaicin, and the like are blended in a liquid oral composition. It is proposed that allantoin is excellent in stability and gum tightening effect and has no unpleasant taste. Patent Literature 4 (Japanese Patent Application Laid-Open No. 2006-222582) discloses that an oral composition obtained by blending a fatty acid or ester having a specific branched chain structure and a specific fragrance is excellent in retention and absorption of a water-soluble active ingredient in the oral cavity. Discloses that allantoin or a derivative thereof is blended as a water-soluble active ingredient having a refreshing feeling. Patent Document 5 (Japanese Patent No. 5251350) discloses a dentifrice composition containing sodium chloride, monomenthyl succinate, menthol and the like, and having an excellent effect of imparting a refreshing feeling and a medicinal effect (tightening of the gums, moderate irritation). Suggesting things. Oral compositions to which various cooling sensation agents and the like are applied are disclosed in Patent Documents 6 to 9 (Japanese Patent Application Laid-Open No. 2006-516429, Japanese Patent Application Laid-Open No. 2009-504651, Japanese Patent Application Laid-Open No. 2013-14521, Japanese Patent Application Laid-Open No. 2013-189623). No. 1).

JP-A-61-155315 JP-A-11-21219 Japanese Patent No. 5470837 JP-A-2006-222852 Japanese Patent No. 5251350 JP 2006-516429 A JP-T-2009-504651 JP 2013-14521 A JP 2013-189623 A

  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 an oral cavity in which an astringent compound has an improved tightening effect on gums without giving an unpleasant stimulus to the gums.

  The present inventors have conducted intensive studies to achieve the above object. As a result, when (B) menthyl glutarate is added to an oral composition containing (A) allantoin or a derivative thereof as an astringent compound, The present inventors have found that it is possible to enhance the gum tightening effect of the component (A) while suppressing the unpleasant stimulus of the present invention, and have accomplished the present invention.

According to the present invention, when the components (A) and (B) are used in combination, the two interact with each other, whereby the stimulus to the gums is moderately suppressed, and unpleasant stimuli such as chattering are not given. The tightening effect is enhanced, so that even with a liquid oral composition, unpleasant stimulation of the gums can be suppressed and a high tightening feeling can be effectively provided.
In this case, when the astringent compound allantoin or a derivative thereof is used in combination with the pungent component capsaicin or the cooling agent monomenthyl succinate to enhance the tightening effect of the gums, the tightening feeling is improved, but the unpleasant stimulus is strongly expressed. And is no longer suitable for use. On the other hand, mentil glutarate, which is known as a cooling agent and a refreshing agent, does not give any unpleasant irritation when used alone, but hardly has a gum tightening effect, and the astringent compound sodium pyrophosphate Even when used in combination with a complex phosphate or sodium chloride, the tightening effect of the gum was not improved, but rather an unpleasant stimulus was developed. However, in the present invention, when the component (B) is used in combination with the component (A), both of them surprisingly act specifically and suppress irritation without causing the above-mentioned unpleasant stimulus. As a result, the gum tightening effect of the component (A) was able to be enhanced, and a special action effect was exhibited.
In particular, when ethanol is added to the liquid oral composition, the refreshing feeling can be enhanced, but the irritation tends to be strong. However, in the present invention, the components (A) and (B) are used in combination. Even if ethanol was added, unpleasant stimulation was suppressed, the gum tightening effect was further improved, and an excellent action effect was able to be provided.
As a result, in the present invention, even for those suffering from periodontal disease having inflammation in the gums sensitive to slight stimuli, a tightening feeling can be effectively and satisfactorily given without feeling unpleasant stimuli in the gums. .
As shown in the comparative examples described below, the effect of the present invention was inferior when the component (A) or (B) was lacking. Comparative Example 1, in which only the component (B) was blended, showed no gum tightness (x), good irritability (感), and Comparative Example 2, in which only the component (A) was blended. Had poor gum tightness (△) and lacked sufficient irritation (△). And, even if sodium chloride or sodium pyrophosphate is blended with the component (B), Comparative Examples 3 and 4, in which the component (A) is not blended, have a low gum tightening feeling (△) and are not irritating. Was bad (△). Further, even when the component (A) and monomenthyl succinate or capsaicin were blended, in Comparative Examples 5 and 6 in which the component (B) was not blended, the tightening feeling of the gums was increased (）), but the irritating feeling was increased. Poorness (x). On the other hand, as shown in the Examples, the liquid oral composition containing the components (A) and (B) has an excellent firming feeling of the gums (又 は or ◎), and makes the test subject with the gum complaint uncomfortable. Little irritation was felt, and the lack of irritation was also excellent (○ or ◎).

Accordingly, the present invention provides the following oral composition.
[1]
(A) one or more allantoin selected from allantoin, allantoinchlorohydroxyaluminum and allantoindihydroxyaluminum, or a derivative thereof;
(B) A composition for oral cavity, comprising: menthyl glutarate.
[2]
(A) / (B) indicating the ratio between the content of the component (A) as allantoin and the content of the component (B) is 0.5 to 10,000 in terms of mass ratio. Oral composition.
[3]
The oral composition according to [1] or [2], wherein the component (A) contains 0.005 to 0.5% by mass as an allantoin and the component (B) contains 0.00001 to 2% by mass.
[4]
(B) The oral composition according to any one of [1] to [3], wherein the menthyl glutarate is a mixture of monomenthyl glutarate and dimenthyl glutarate.
[5]
The oral composition according to [4], wherein the mixing ratio of monomenthyl glutarate and dimenthyl glutarate is 1: 9 to 9: 1 as a mass ratio.
[6]
The oral composition according to any one of [1] to [5], further comprising (C) 2 to 20% by mass of ethanol.
[7]
The oral composition according to any one of [1] to [6], which is a liquid.

  According to the present invention, it is possible to provide an oral composition in which the effect of imparting a tightening feeling by the astringent compound (A) is improved without giving unpleasant stimulation to the gums. This oral composition can provide a high tightening feeling without giving any unpleasant irritation even when ethanol is further added, and also suffers from periodontal disease, the gums weaken, and even in a state sensitive to slight irritation It can effectively give a feeling of tightening of the gums under a sense of harm.

  Hereinafter, the present invention will be described in more detail. The oral composition of the present invention contains (A) allantoin or a derivative thereof, and (B) menthyl glutarate.

  (A) Allantoin or a derivative thereof has a gum tightening action and an anti-inflammatory action. Examples of the component (A) include allantoin and allantoin derivatives such as allantoinchlorohydroxyaluminum and allantoindihydroxyaluminum, and one or more selected from these can be used.

  The amount of the component (A) is not particularly limited, but is preferably 0.005 to 0.5% (mass%, hereinafter the same) as the allantoin, more preferably 0.01 to 0.5%. It is. When the content is 0.005% or more, a sufficient gum tightening effect can be obtained. When the content is 0.5% or less, off-taste such as bitterness of the component (A) itself is sufficiently suppressed, and the feeling of use can be maintained. In addition, in the composition for liquid oral cavity such as a mouthwash, it is particularly preferable that the amount of the component (A) is 0.1% or less of the whole composition, since an off-taste such as bitterness can be sufficiently suppressed.

(B) Menthyl glutarate is known as a cooling agent and a refreshing agent, but in the present invention, when used in combination with the component (A), it exerts an effect of enhancing the tightening effect of gums, and is unpleasant. A feeling of irritation can also be suppressed.
Menthyl glutarate includes, for example, monomenthyl glutarate and dimenthyl glutarate. These may be used alone, but it is more preferable to use a mixture of monomenthyl glutarate and dimenthyl glutarate.

  Here, when monomenthyl glutarate and dimenthyl glutarate are mixed, the mixing ratio of both (monomenthyl glutarate: dimenthyl glutarate) is preferably 1: 9 to 9: 1 as a mass ratio. , More preferably 1: 1 to 9: 1, and still more preferably 3: 2 to 3: 1. When the mixing ratio is within the above range, a sufficient tightening feeling of the gums can be provided, the effective feeling is excellent, and the irritating feeling can be sufficiently suppressed.

  The blending amount of (B) menthyl glutarate is preferably 0.00001 to 2%, more preferably 0.0001 to 1% of the whole composition. When it is 0.00001% or more, the effect of enhancing the tightening feeling of the gums is sufficiently exhibited. When it is 2% or less, the stimulus derived from the component (B) is suppressed, and the unpleasant stimulus is sufficiently suppressed. In particular, in a liquid oral cavity composition such as a mouthwash, from the viewpoint of suppressing irritation caused by the component (B), the blending amount of the component (B) is 0.2% or less, particularly 0.1% or less of the whole composition. Is more preferable.

  In the present invention, (A) / (B) indicating the ratio of the content of the component (A) as allantoin and the content of the component (B) is a point at which both the tightening effect of the gums and the suppression of the irritating feeling are compatible. Therefore, the mass ratio is preferably 0.5 to 10,000, more preferably 5 to 1,000. Within the above range, the tightening feeling of the gums is further improved, and the unpleasant stimulating feeling is further suppressed. If it is less than 0.5, the tightness of the gum may be inferior, and if it exceeds 10,000, unpleasant stimulus may not be suppressed.

It is preferable that the oral composition of the present invention further contains (C) ethanol. In the present invention, when ethanol is blended, the gum tightening effect of the components (A) and (B) is further enhanced, and even when ethanol is blended, unpleasant irritation is sufficiently suppressed, and the use is refreshing. Can give a feeling.
When blending ethanol, the blending amount is preferably 2 to 20%, particularly preferably 2 to 10% of the whole composition. If it is at least 2%, the effect of tightening the gums will be sufficiently enhanced, and if it is at most 20%, irritation derived from the component (C) will be sufficiently suppressed.
When ethanol is contained in the fragrance composition, the total amount of ethanol including the ethanol is preferably in the above range.

  The oral composition of the present invention can be in the form of a liquid, a paste, a gel, and the like. Examples of the dosage form include mouthwash, mouthwash, toothpaste, and dentifrices such as liquid dentifrice. It can be prepared by a conventional method according to the type. Particularly, a dentifrice or a mouthwash is preferable, and a liquid form is preferable, and a mouthwash is more preferable. In this case, other appropriate components other than the above-mentioned components may be added according to the purpose, dosage form and the like of the composition. For example, dentifrices include abrasives, wetting agents, binders, surfactants, sweeteners, preservatives, coloring agents, flavors other than the component (B), and active ingredients other than the component (A). It can be prepared by mixing each component with water. In mouthwashes, wetting agents, thickeners, surfactants, solvents such as water, sweeteners, preservatives, coloring agents, pH adjusters, fragrances other than component (B), and active ingredients other than component (A) And the like, and can be prepared by mixing these components.

  Abrasives include silica-based abrasives such as precipitated silica, aluminosilicate, zirconosilicate, and titanium-binding silica; dibasic calcium phosphate dihydrate or anhydrate; monobasic calcium phosphate, tribasic calcium phosphate, calcium pyrophosphate, etc. Calcium phosphate-based abrasives; calcium carbonate-based abrasives such as calcium carbonate, and calcium hydroxide, aluminum hydroxide, tertiary magnesium phosphate, magnesium carbonate, calcium sulfate, bentonite, and hydroxyapatite; Two or more can be blended. Among these, a silica-based abrasive containing the above silicate as a main component is particularly preferable. The compounding amount of these abrasives is preferably 8 to 70% of the whole composition. In addition, an abrasive is not usually added to a liquid oral composition such as a mouthwash.

  Examples of the wetting agent include glycerin, propylene glycol, polyhydric alcohols such as polyethylene glycol having an average molecular weight of 160 to 400 (average molecular weight described in quasi-drug raw material standards 2006), and sugar alcohols such as sorbit and xylit. The compounding amount of the thickener is preferably 5 to 50%, particularly preferably 20 to 45% of the whole composition. In addition, in a liquid oral composition such as a mouthwash, the compounding amount of the wetting agent is usually 5 to 50% of the whole composition.

As the binder, an organic binder or an inorganic binder can be used. For example, the organic binder includes xanthan gum, carrageenan, hydroxyethyl cellulose, sodium alginate, polyvinyl alcohol, carboxymethyl cellulose, and the like. Examples of the inorganic binder include thickening silica and aluminum silicate. These can be used alone or in combination of two or more. The amount of the binder is preferably 1.4 to 10%, particularly preferably 1.4 to 8% of the whole composition.
In a liquid oral cavity composition such as a mouthwash, the above substance is used as a thickener, and the compounding amount is usually 0 to 1%, particularly 0 to 0.5% of the whole composition.

Examples of the surfactant include an anionic surfactant, a nonionic surfactant, and an amphoteric surfactant.
Specifically, examples of the anionic surfactant include alkyl sulfates such as sodium lauryl sulfate, acyl sarcosine salts, acyl taurine salts, and acyl amino acid 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, polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene hydrogenated castor oil. Examples thereof include polyoxyethylene fatty acid esters, polyoxyethylene higher alcohol ethers, and fatty acid alkanolamides. In particular, polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 40 to 100 mol is preferable. Examples of the amphoteric surfactant include an alkyl betaine type, a betaine type and an imidazoline type.
The compounding amount of the surfactant is preferably 0 to 10%, particularly preferably 0.001 to 5% of the whole composition.

Sweetening agents include saccharin sodium and the like.
Preservatives include paraoxybenzoate, sodium benzoate and the like.
As a colorant, a highly safe water-soluble dye such as Blue No. 1, Green No. 3, Yellow No. 4, and Red No. 105 can be added.

As the fragrance, a general oral fragrance component can be used. For example, peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, lime oil , Lavender oil, rosemary oil, laurel oil, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, iris concrete, absolute peppermint, Natural fragrances such as absolute rose and orange flower, and fragrances processed with these natural fragrances (forehead cut, rear cut, fractionation, liquid-liquid extraction, essence, powdered fragrance, etc.), and menthol, Carvone, anethole, methyl salicylate, cinnamite Aldehydes, linalool, linalool acetate, limonene, menthone, pinene, octylaldehyde, citral, pulegone, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexanepropionate, methyl anthranilate, ethyl methyl phenyl glycylate Date, vanillin, undecalactone, hexanal, isoamyl alcohol, hexenol, dimethyl sulfide, cycloten, furfural, trimethylpyrazine, ethyl lactate, ethyl thioacetate, etc. Grape flavor, mango flavor, butter flavor, milk flavor, fruit mix Scan flavors, such as blended fragrance, such as tropical fruit flavors can be used a known fragrance materials used in the oral compositions, but are not limited to perfume embodiment.
The above-mentioned fragrance materials differ depending on the components, but are preferably used in the range of 0.000001 to 1% of the whole composition. It is preferable that the perfume for perfuming using the above perfume material is blended in the composition in an amount of 0.001 to 2%.

Examples of the pH adjuster include organic acids such as citric acid and malic acid, salts thereof, and inorganic acids such as phosphoric acid and hydrochloric acid.
The pH (25 ° C.) of the composition is not particularly limited, but is preferably from pH 4 to 6.5, and more preferably from pH 4 to 6.2.

  Optional active ingredients include, for example, enzymes such as dextranase, tranexamic acid, epsilon aminocaproic acid and cell activators such as various vitamins, bactericides such as isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, zeolites and the like. Examples of the agent include a tartar preventive and a fluorine-containing compound such as sodium fluoride. In addition, these compounding amounts are effective amounts as long as the effects of the present invention are not hindered.

  The oral composition of the present invention is preferably aqueous, and the balance (balance) of the total content of the various components can be water.

  Hereinafter, the present invention will be described specifically with reference to Examples, Comparative Examples, and Formulation Examples, but the present invention is not limited to the following Examples. In the following examples,% indicates mass% unless otherwise specified.

[Examples and Comparative Examples]
Using the menthyl glutarates 1 to 5 shown in Table 1, oral compositions (mouthwashes) having the compositions shown in Tables 2 to 4 were prepared by a conventional method, and these were used as samples and evaluated by the following method. The results are shown in Tables 2 to 4. The amount of the component (A) is the amount of allantoin.

Evaluation Method of Gum Tightening Feeling Ten test subjects (gulp symptomatic complainants) contained a 20 mL sample in their mouth, rinsed for 20 seconds, and rinsed. The tightening feeling of the gum immediately after use was evaluated according to the following four-point scale. The average score of 10 persons was calculated, and judged based on the following evaluation criteria.
Evaluation criteria 4 points: Very tight feeling of gums 3 points: Very good feeling of tightening gums 2 points: Somewhat feeling of tightening of gums 1 point: Not much feeling of tightening of gum Evaluation criteria ◎: Average score 3 0.5 or more ○: Average score of 3.0 or more and less than 3.5 Δ: Average score of 2.0 or more and less than 3.0 ×: Average score of less than 2.0

Evaluation method of irritability Ten test subjects (gulp symptomatic complainants) included a 20 mL sample in their mouth, rinsed for 20 seconds, rinsed, and evaluated the absence of irritation (unpleasant irritation) during use in the following four stages. The evaluation was based on a rating standard. The average score of 10 persons was calculated, and judged based on the following evaluation criteria.
Rating criteria 4 points: I do not feel any stimulus 3 points: I feel a little stimulus 2 points: I feel a little stimulus 1 point: I feel a lot of stimulus Evaluation criteria ◎: Average score 3.5 or more ○: Average score 3. 0 or more and less than 3.5 points Δ: Average point of 2.0 or more and less than 3.0 points ×: Average point of less than 2.0 points

Details of the used fragrance composition are as shown in Tables 5 to 12, and the component (B) is not contained in these fragrance compositions.
In addition, except that the fragrance composition B, C, D, E or F was used instead of the fragrance composition A, an oral composition having the same composition as in the above example was similarly prepared and evaluated. The same result as in the example was obtained.

＊；表中の部は、質量部である（以下同様）。

*: Parts in the table are parts by mass (the same applies hereinafter).

  An example of the formulation is shown below. Using the same raw materials as described above and preparing the oral composition of the formulation example in the same manner and evaluating the composition, it was found to be excellent in tightening of the gums and good in use without unpleasant irritation.

[Prescription Example 1] Toothpaste (A) Allantoin 0.1
(B) Mentyl glutarate 1 0.01
Silicic anhydride 20
Glycerin 35
Xanthan gum 0.6
Carrageenan 0.2
Sodium lauryl sulfate 1.5
Saccharin sodium 0.1
Fragrance composition A1
Purified water balance
100% in total
(A) / (B) = 10

[Prescription Example 2] Toothpaste (A) Allantoin 0.5
(B) Menthyl glutarate 1 2
Silicic anhydride 20
Glycerin 35
Xanthan gum 0.6
Carrageenan 0.2
Sodium lauryl sulfate 1.5
Saccharin sodium 0.1
Fragrance composition A1
Purified water balance 100%
(A) / (B) = 0.25

[Formulation Example 3] Mouthwash (A) Allantoin 0.03
(B) Mentyl glutarate 1 0.0002
Lauroyl sarcosine sodium 0.1
Polyoxyethylene (60) hydrogenated castor oil 0.2
Polyoxyethylene (15) cetyl ether 0.1
Glycerin 2.0
Propylene glycol 4.0
Polyethylene glycol 400 5.0
Citric acid 0.05
Sodium citrate 0.3
Perfume composition A 0.5
Purified water balance
100% in total
(A) / (B) = 150

Claims (7)

(A) one or more allantoin selected from allantoin, allantoinchlorohydroxyaluminum and allantoindihydroxyaluminum, or a derivative thereof;
(B) A composition for oral cavity, comprising: menthyl glutarate.   2. The oral cavity according to claim 1, wherein (A) / (B) indicating the ratio between the content of the component (A) as allantoin and the content of the component (B) is 0.5 to 10,000 as a mass ratio. Composition.   The oral composition according to claim 1 or 2, comprising (A) a component in an amount of 0.005 to 0.5% by mass as allantoin and (B) 0.00001 to 2% by mass.   (B) The oral composition according to any one of claims 1 to 3, wherein the menthyl glutarate is a mixture of monomenthyl glutarate and dimenthyl glutarate.   The oral composition according to claim 4, wherein the mixing ratio of monomenthyl glutarate and dimenthyl glutarate is 1: 9 to 9: 1 as a mass ratio.   The oral composition according to any one of claims 1 to 5, further comprising (C) 2 to 20% by mass of ethanol.   The oral composition according to any one of claims 1 to 6, which is a liquid.