WO2020115974A1

WO2020115974A1 - Composition for oral cavity

Info

Publication number: WO2020115974A1
Application number: PCT/JP2019/034920
Authority: WO
Inventors: 陽介内野; 綾荻原
Original assignee: 花王株式会社
Priority date: 2018-12-04
Filing date: 2019-09-05
Publication date: 2020-06-11
Also published as: CN113164353A; TW202031240A; JP2020094030A; JP7337610B2; CN113164353B

Abstract

The present invention relates to a composition for oral cavity, which exhibits an excellent oral biofilm removing effect by means of erythritol, while having an excellent dentin hyperesthesia suppressing effect. The present invention relates to a composition for oral cavity, which contains the components (A), (B), (C) and (D) described below, and which is configured such that the mass ratio of the component (D) to the component (A), namely (D)/(A) is from 1 to 10 (inclusive). Component (A): from 3% by mass to 33% by mass (inclusive) of erythritol Component (B): a potassium compound Component (C): an N-acyl amino acid having a hydrocarbon group with 14-18 carbon atoms, or an alkali metal salt thereof Component (D): water

Description

Oral composition

The present invention relates to a composition for oral cavity.

Conventionally, in order to prevent oral diseases such as dental caries, periodontal disease and halitosis, it is effective to inhibit the formation of biofilm in the oral cavity and to remove the already formed biofilm. Oral compositions using various components such as a foaming agent, a bactericide, and the like have been developed. Among these components, erythritol, as contained in the oral composition described in Patent Document 1, is an effective component for suppressing or dissociating the agglutination reaction between bacteria in the oral cavity, and is a biofilm. It is known to be excellent not only in the effect of inhibiting the formation but also in the effect of removing the biofilm formed in the spaces between the teeth and the periodontal pockets.

On the other hand, potassium compounds such as potassium nitrate exert a nerve blunting action by the released potassium ions, and are known to be excellent in alleviating hypersensitivity symptoms. For example, Patent Literature 2 discloses an oral composition containing an acylamino anionic surfactant, a nonionic surfactant, and isopropylmethylphenol at a specific blending ratio together with such potassium nitrate. By enhancing the dissolution property, the nerve blunting effect is sufficiently expressed, and the pain caused by hypersensitivity of dentin is reduced.

(Patent Document 1) Japanese Patent Laid-Open No. 2005-29484 (Patent Document 2) Japanese Patent Laid-Open No. 2016-222579

The present invention comprises the following components (A), (B), (C) and (D):
(A) Erythritol 3% by mass or more and 33% by mass or less (B) Potassium compound (C) N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms or an alkali metal salt thereof (D) Water, and a component ( The present invention relates to a composition for oral cavity in which the mass ratio ((D)/(A)) between the content of D) and the content of component (A) is 1 or more and 10 or less.

While using erythritol which is excellent in inhibiting biofilm formation and removing effect in the oral cavity as in Patent Document 1, pain caused by hypersensitivity of dentin is enhanced by osmotic stimulation caused by dissolution of erythritol in water. Therefore, even if an attempt is made to give a palliative effect of hypersensitivity symptoms by using a potassium compound such as potassium nitrate by taking the description of Patent Document 2 into consideration, reduction of pain caused by sufficient hypersensitivity of dentin It has been found by the present inventor that it is difficult to achieve the above.
Thus, while enjoying the effect of removing the biofilm in the oral cavity by erythritol, an oral composition that can effectively prevent the pain caused by dentin hypersensitivity can not yet exist, its realization Is in a desirable situation.

That is, the present invention relates to a composition for oral cavity which has an excellent effect of removing an oral biofilm by erythritol and an excellent effect of suppressing hypersensitivity of dentin.

Therefore, the present inventor has conducted various studies and, while containing a specific amount of erythritol and containing a potassium compound such as potassium nitrate, further uses an N-acylamino acid having a specific hydrocarbon group or a salt thereof, and By adjusting erythritol and water to a specific mass ratio, it is possible to effectively block the oral biofilm removal effect of erythritol and block the opening of dentinal tubules on the surface of exposed dentin. In addition, it was found that an oral composition capable of effectively preventing pain caused by hypersensitivity of dentin can be obtained.

According to the composition for oral cavity of the present invention, the opening of the dentin tubule on the surface of the exposed dentin can be effectively blocked while erythritol sufficiently exerts the effect of dispersing the oral biofilm. That is, the composition for oral cavity of the present invention is a highly useful composition having both the effect of removing the biofilm in the oral cavity and the effect of suppressing pain caused by hypersensitivity of dentin.

FIG. 1 is an electron micrograph of the surface of dentin when the oral composition of Example 1 was used. FIG. 2 is an electron micrograph of the surface of dentin when the oral composition of Comparative Example 2 was used.

Detailed Description of the Invention

Hereinafter, the present invention will be described in detail.
In the present invention, "dentin tubule" is also referred to as "dentin tubule". In addition, "blocking dentinal tubules" means physically blocking dentin tubules, not only covering the opening of the dentin tubule on the surface of the dentin, but also in the tubule near the surface of the dentin tubule. It is also meant to include the state of filling and covering (closing).

The oral composition of the present invention contains 3% by mass or more and 33% by mass or less of erythritol as the component (A). Thereby, together with the coexistence of the component (C) described later, by suppressing the agglutination reaction between the bacteria or by dissociating the agglutination between the bacteria, the formation of the biofilm is inhibited and the teeth and teeth or teeth A biofilm that has already formed can be removed to a narrow area such as a gap such as a peripheral pocket, and a sufficient oral biofilm can be obtained while having a pain suppressing effect due to excellent dentin hyperesthesia. It is possible to exert a dispersion effect.

The content of the component (A) is 3% by mass or more, and preferably 5% by mass or more, in the composition for oral cavity of the present invention, from the viewpoint of sufficiently exerting the biofilm removal effect. It is preferably 8% by mass or more, more preferably 10% by mass or more, still more preferably 20% by mass or more. The content of the component (A) depends on the component (B) so as to effectively prevent the pain caused by hypersensitivity of dentin from being enhanced by osmotic stimulation caused by dissolution in water. From the viewpoint of ensuring a good effect of suppressing pain caused by dentin hypersensitivity, it is 33% by mass or less, preferably 32% by mass or less, more preferably in the oral composition of the present invention. Is 31% by mass or less, more preferably 30% by mass or less. The content of the component (A) in the oral composition of the present invention is 3% by mass or more and 33% by mass or less, preferably 5 to 32% by mass, more preferably 8 to 31% by mass. %, more preferably 10 to 30% by mass, still more preferably 20 to 30% by mass.

The oral composition of the present invention contains a potassium compound as the component (B). With this, while ensuring the effect of removing the biofilm by the above component (A), after applying the oral composition of the present invention to the oral cavity, it rapidly releases potassium ions to form a composition with the component (C) described below. It quickly forms a potassium salt of N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms, which is stably dissolved in a substance, and the salt acts on the surface of dentin to effectively block the dentinal tubule. However, it is possible to exert an effect of suppressing an increase in pain caused by hypersensitivity of dentin due to osmotic stimulation caused by dissolution of the component (A) in water. Among these components (B), not only the nerve blunt action by the released potassium ions, but also the effect of blocking the dentinal tubule in combination with the above component (C) is enhanced to suppress pain caused by dentin hypersensitivity. From the viewpoint of improving the effect, one or more potassium compounds selected from potassium nitrate, tripotassium citrate, potassium acetate and potassium hydroxide are preferable, and among them, one or two selected from potassium nitrate and potassium hydroxide. The seeds are more preferable, and it is preferable to use these in combination. The component (B) means a potassium compound other than the component (C) described later.

The content of the component (B) is preferably 0.001% by mass or more in the oral composition of the present invention from the viewpoint of promoting rapid release of potassium ions after application of the composition to the oral cavity. %, more preferably 0.01% by mass or more, further preferably 0.05% by mass or more, even more preferably 2% by mass or more, still more preferably 3% by mass or more, and It is preferably 4% by mass or more. In addition, the content of the component (B) is preferably 10% by mass or less, more preferably 8% by mass or less in the oral composition of the present invention from the viewpoint of preventing off-taste. , And more preferably 7% by mass or less. The content of the component (B) in the oral composition of the present invention is preferably 0.001% by mass or more and 10% by mass or less, more preferably 0.01 to 10% by mass, and further The amount is preferably 0.05 to 10% by mass, more preferably 2% by mass or more and 10% by mass or less, still more preferably 3 to 8% by mass, and further preferably 4 to 7% by mass. ..

The mass ratio ((B)/(A)) between the content of the component (A) and the content of the component (B) is due to the removal effect of the intraoral biofilm and the dissolution of the component (A) in water. Is preferably 0.1 or more, and more preferably 0.13 or more, from the viewpoint of satisfactorily combining the effect of suppressing the increase in pain caused by dentin hypersensitivity by the osmotic stimulation. Yes, more preferably 0.15 or more, still more preferably 0.18 or more, even more preferably 0.2 or more, preferably 1.5 or less, more preferably 1.25 or less. And more preferably 1 or less, and even more preferably 0.8 or less.

The oral composition of the present invention contains, as the component (C), an N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms or an alkali metal salt thereof. By containing the component (C), when the oral composition of the present invention is applied to the oral cavity, it has a hydrocarbon group having 14 to 18 carbon atoms together with the potassium ion released by the component (B). An N-acyl amino acid potassium salt which forms a N-acyl amino acid potassium salt promptly or has a potassium ion abundantly present in the oral composition by the component (B) and has a hydrocarbon group having 14 to 18 carbon atoms. The salt of the present invention can be stabilized and the salt of the present invention can be sufficiently spread throughout the oral cavity in the composition of the present invention to easily reach the desired dentin surface. Furthermore, when such a salt reaches the surface of dentin, the substitution of the potassium salt of the N-acyl amino acid with the calcium salt of the N-acyl amino acid proceeds rapidly, and the hydrocarbon group having 14 to 18 carbon atoms is replaced. Since the precipitate of the calcium salt of the N-acyl amino acid has firmly adhered to the surface of the dentin, the dentinal tubule can be effectively blocked and the pain suppressing effect can be effectively enhanced. Further, the above component (A There is no fear of impeding the biofilm removal effect of ).

As the amino acid portion of the N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms in the component (C), one selected from glutamic acid, glycine and alanine from the viewpoint of exerting an excellent dentinal tubule blocking effect, or Two or more types are preferable, and one or two types selected from glutamic acid and glycine are more preferable, and glycine is even more preferable, from the viewpoint of blocking dentinal tubules more effectively and quickly. Further, these amino acid moieties may be any of D-form, L-form or a mixture of D-form and L-form, and preferably L-form.

The acyl group of the N-acyl amino acid in the component (C) has a hydrocarbon group having 14 to 18 carbon atoms from the viewpoint of exhibiting an excellent dentinal tubule blocking effect. The N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms or its alkali metal salt is derived from a saturated or unsaturated linear or branched fatty acid or a mixed fatty acid thereof. More preferably, it has a hydrocarbon group having 14 to 16 carbon atoms. That is, as the acyl group having a hydrocarbon group having such a carbon number, a plurality of types of the hydrocarbon group having the above-mentioned carbon number may be mixed, but from the viewpoint of sufficiently exhibiting the excellent effect of blocking the opening of the dentinal tubule. One or more selected from a myristoyl group, a palmitoyl group and a stearoyl group are preferable, and a myristoyl group is more preferable.

Examples of the salt of the alkali metal salt of the N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms in the component (C) include sodium and potassium, and potassium is preferable.

The content of the component (C) is effective by forming a potassium salt which dissolves rapidly and stably in the composition together with the potassium ion released by the component (B), and the salt acts on the surface of the dentin. From the viewpoint of effectively blocking pain by effectively blocking dentinal tubules, it is preferably 0.01% by mass or more, more preferably 0.05% by acid equivalent in the oral composition of the present invention. It is at least mass%, more preferably at least 0.1 mass%. Moreover, the content of the component (C) is preferably 2% by mass or less, more preferably 1.5% by acid equivalent in the oral composition of the present invention from the viewpoint of ensuring a good flavor. It is not more than 1% by mass, preferably not more than 1% by mass. The content of the component (C) in the oral composition of the present invention is, in terms of acid, preferably 0.01% by mass or more and 2% by mass or less, more preferably 0.05 to 1. It is 5% by mass, more preferably 0.1 to 1% by mass.
Here, the “acid conversion amount” means that the content of the component (C) is expressed as a content converted into an N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms.
It should be noted that an N-acyl amino acid or an alkali metal salt thereof having an acyl group capable of containing a hydrocarbon group having a carbon number other than the above-mentioned number of carbon atoms, such as a cocoyl group, mixed with a plurality of hydrocarbon groups having the above-mentioned carbon number, is used. When used in the composition for oral cavity of the present invention, if the content of the N-acyl amino acid having a hydrocarbon group of the above carbon number or its alkali metal salt is the content of the above component (C). Good.

The mass ratio ((C)/(A)) between the acid equivalent amount of the component (C) and the content of the component (A) is due to the removal effect of the oral biofilm and the dissolution of the component (A) in water. From the viewpoint of satisfactorily having the effect of effectively suppressing the increase in pain due to dentin hypersensitivity by the osmotic stimulus, it is preferably 0.001 or more, and more preferably 0. It is 0.004 or more, more preferably 0.008 or more, preferably 0.035 or less, more preferably 0.03 or less, and further preferably 0.02 or less.

The oral composition of the present invention contains water as a component (D). By adjusting the water content, it is possible to effectively prevent the pain caused by dentin hypersensitivity from being enhanced by the osmotic stimulation caused by the dissolution of the component (A) into the component (D). To do. Further, the potassium ion released from the component (B) is allowed to be present in the composition, and the potassium salt of the N-acyl amino acid having the above-mentioned specific carbon number, which shows stable solubility by the components (B) and (C), is obtained. It becomes possible to effectively block the dentinal tubules while allowing the dentin tubules to exist and fully spread to every corner of the oral cavity, and the biofilm removing effect can be sufficiently exerted.

The content of the component (D) is such that the osmotic stimulation caused by the dissolution of the component (A) in the component (D) is suppressed, and the stable solubility is obtained by the components (B) and (C). From the viewpoint of efficiently forming the N-acyl amino acid potassium salt having the specific carbon number shown above to improve the blocking effect of dentinal tubules, and from the viewpoint of effectively exhibiting the biofilm removal effect by the component (A), In the composition for oral cavity, it is preferably 8% by mass or more, more preferably 10% by mass or more, further preferably 12% by mass or more, even more preferably 15% by mass or more, still more preferably Is 33% by mass or more, more preferably 34% by mass or more, even more preferably 40% by mass or more, still more preferably 45% by mass or more, preferably less than 60% by mass, It is more preferably 55% by mass or less, and further preferably 50% by mass or less.

The mass ratio ((D)/(A)) between the content of the component (D) and the content of the component (A) ensures that the component (A) has an excellent biofilm removal effect. From the viewpoint of appropriately controlling the osmotic stimulus due to the dissolution in the component (D) of (1) to improve the blocking effect of the dentinal tubule, it is 1 or more, preferably 2 or more, and more preferably 3 Or more, more preferably 3.5 or more, 10 or less, preferably 9 or less, and more preferably 5 or less.

The oral composition of the present invention may further contain a fatty acid divalent metal salt (E) having a hydrocarbon group having 12 to 18 carbon atoms. This can further enhance the effect of suppressing pain caused by hypersensitivity of dentin. The component (E) is derived from a saturated fatty acid having 12 to 18 carbon atoms and is composed of two saturated fatty acids and a divalent metal. Specific examples of the derived saturated fatty acid include lauric acid, myristic acid, pentadecyl acid, palmitic acid, margaric acid, and stearic acid. Among them, lauric acid, myristic acid, palmitic acid and stearic acid are preferable, and lauric acid, myristic acid and stearic acid are more preferable. The two saturated fatty acids constituting the component (E) are preferably the same. Specific examples of the divalent metal include zinc, calcium, magnesium, strontium and barium. Among them, zinc, calcium and magnesium are preferable, and zinc and calcium are more preferable, from the viewpoints of effectively enhancing the pain suppressing effect caused by dentin hypersensitivity and the applicability in the oral cavity.
More specifically, zinc stearate is preferable as the component (E).

The content of the component (E) is preferably 0.1 to 3 in the oral composition of the present invention, from the viewpoint of enhancing the sealing property of the opening of the dentin tubule and maintaining a good flavor. %, more preferably 0.2 to 2% by mass, further preferably 0.4 to 1.8% by mass.

The oral composition of the present invention may further contain maltitol (F). As a result, unnecessary crystal growth of the component (A) can be effectively suppressed, an excellent biofilm removal effect can be ensured, and the dissolution of the component (A) into the component (D) is a factor. The osmotic stimulus effectively suppresses the enhancement of pain due to dentin hypersensitivity, while maintaining high stability of the composition to ensure a good appearance, and also good. It is possible to secure the perfect flavor.

The content of the component (F) is preferably 1 in the oral composition of the present invention from the viewpoint of effectively ensuring the excellent biofilm removal effect of the component (A) and ensuring a good appearance. To 30% by mass, more preferably 3 to 20% by mass, and further preferably 5 to 15% by mass.

When the oral composition of the present invention is a toothpaste composition, it may contain 10% by mass or less of an abrasive, or does not contain an abrasive. Examples of such abrasives include abrasive silica, dibasic calcium phosphate dihydrate and anhydride, calcium pyrophosphate, calcium carbonate, alumina, aluminum hydroxide, magnesium acetate, dibasic magnesium phosphate, magnesium acetate, and triphosphoric acid. One or more selected from abrasives such as magnesium and zeolite may be used. Among them, from the viewpoint of suppressing an excessive increase in pH of the composition, an abrasive containing at least abrasive silica is preferable, and an abrasive consisting only of abrasive silica is more preferable.
Here, the abrasive silica is one having an oil absorption of 50 to 150 mL/100 g, and the oil absorption is the amount of oil that can be supported by silica. The measuring method is JIS K5101-13-2 (2004). Established), specify by the amount of boiled linseed oil absorbed.

The content of the abrasive is preferably in the oral composition of the present invention from the viewpoint of the effect of blocking dentinal tubules, from the viewpoint of suppressing the further hypersensitivity of the user of the present invention due to the composition of the present invention. It is 10% by mass or less, more preferably 8% by mass or less, still more preferably 4% by mass or less, and imparts a good flavor while achieving both an excellent biofilm removal effect and a dentinal tubule sealing effect. From the viewpoint of ensuring also the above, it is preferably more than 0 mass%, more preferably 2 mass% or more.

The oral composition of the present invention may further contain a wetting agent in addition to the above components. Examples of such a wetting agent include one or more selected from glycerin, propylene glycol, polyethylene glycol, sorbitol, xylitol and lactol, and one or more selected from sorbitol, glycerin, xylitol and propylene glycol. Is preferred, and one or two selected from sorbitol and propylene glycol is more preferred. The total content of the wetting agent is preferably in the oral composition of the present invention, from the viewpoint of ensuring good storage stability and flavor of the composition while exhibiting a quick and excellent blocking effect for dentin tubules. 5 mass% or more, more preferably 8 mass% or more, preferably 60 mass% or less, more preferably 45 mass% or less, further preferably 40 mass% or less, and even more preferably It is 35 mass% or less.

The oral composition of the present invention may further contain a binder. As such a binder, one or more selected from sodium alginate, sodium carboxymethyl cellulose, carrageenan, xanthan gum, sodium polyacrylate, hydroxyethyl cellulose, hydroxypropyl cellulose, pectin, tragacanth gum, gum arabic, and guar gum. Can be mentioned. Among them, one or more selected from sodium alginate, sodium carboxymethyl cellulose, carrageenan, xanthan gum, and hydroxyethyl cellulose is preferable, and one or more selected from sodium carboxymethyl cellulose and carrageenan is particularly preferable.
When the oral composition of the present invention is a toothpaste composition, the content of such a binder in the oral composition of the present invention is preferably 0.2% by mass or more, more preferably 0%. It is 0.4% by mass or more, preferably 3% by mass or less, more preferably 2.5% by mass or less, and further preferably 1.8% by mass or less.

The oral composition of the present invention may further contain an amphoteric surfactant as the component (G). Examples of such amphoteric surfactants include one or more selected from alkylamidopropyl betaine such as coconut oil fatty acid amide propyl betaine and alkyl hydroxysulfobetaine such as lauryl hydroxysulfobetaine.
The content of the amphoteric surfactant as the component (G) is preferably 0.05 mass in the oral composition of the present invention from the viewpoint of appropriately controlling the osmotic pressure stimulation of the component (A) by its foaming property. % Or more, more preferably 0.1% by mass or more, further preferably 0.25% by mass or more, preferably 3% by mass or less, more preferably 2% by mass or less, and further preferably Is 0.8 mass% or less.

The mass ratio ((G)/(A)) between the content of the component (G) and the content of the component (A) is such that the component (A) can maintain an excellent biofilm removal effect. From the viewpoint of appropriately controlling the osmotic pressure stimulation of (1) to improve the blocking effect of dentinal tubules, it is preferably 0.001 or more, more preferably 0.5 or more, and further preferably 0.1 or more. , Preferably 0.05 or less.

When the oral composition of the present invention is a toothpaste composition, it is preferable to use a thickening silica together with the above binder. Thickening silica is silica having an oil absorption of 200 to 400 mL/100 g. Here, the oil absorption indicates the amount of oil that can be supported by silica, and the measuring method is specified by JIS K5101-13-2 (established in 2004) by the amount of boiled linseed oil absorbed. The content of the thickening silica in the oral composition of the present invention is preferably 0.1 to 20% by mass, more preferably 1 to 10% by mass, and further preferably 2 to 8% by mass. is there.

The composition for oral cavity of the present invention, in addition to the above components, within a range that does not impair the effects of the present invention, anionic surfactants such as sodium lauryl sulfate and sodium lauroylmethyl taurine, cationic surfactants, coconut oil fatty acid amide propyl betaine. And other amphoteric surfactants, polyoxyethylene hydrogenated castor oil, nonionic surfactants such as sucrose fatty acid esters, sorbitan fatty acid esters, and other surfactants; sweeteners such as saccharin sodium; perfumes; dyes; Can be included.

Still further, as long as the effects of the present invention are not impaired, tin fluoride, sodium fluoride, a fluoride ion supply compound such as ammonium fluoride, a fluoride such as sodium monofluorophosphate, titanium oxide, aluminum lactate, calcium phosphate, hydroxy. Other components such as apatite and arginine-calcium carbonate may also be included.

The potassium contained in the oral composition of the present invention exists in the ionic form or the salt form in the oral composition of the present invention. For example, such potassium is present as potassium ions released from component (B), when component (C) is a potassium salt, as potassium forming such salt.
Present in ionic or salt form in the oral composition of the present invention, the total amount of potassium present, from the viewpoint of promoting rapid release of potassium ions after application of the composition into the oral cavity, the oral cavity of the present invention In the composition for use, it is preferably 0.05 mass% or more, more preferably 0.1 mass% or more, and further preferably 0.5 mass% or more. Further, the total amount of potassium present in the composition for oral cavity of the present invention is preferably 6% by mass or less, more preferably 4% by mass or less, and further preferably from the viewpoint of preventing off-taste. It is 2 mass% or less. The total amount of potassium present in the composition for oral cavity of the present invention is preferably 0.05% by mass or more and 6% by mass or less, more preferably 0.1 to 4% by mass, and further preferably 0.1. It is 5 to 2 mass %.
The total amount of potassium present in the oral composition can be measured by ion chromatography, ICP emission spectroscopy, or the like.

Further, the mass ratio ((C)/potassium) between the content of the component (C) and the total amount of potassium present is such that the rapid release of potassium ions after application of the composition into the oral cavity and the taste From the viewpoint of preventing the feeling of being felt, it is preferably 0.01 or more, more preferably 0.05 or more, still more preferably 0.08 or more, preferably 1 or less, more preferably 0. It is 0.5 or less, more preferably 0.3 or less.

The pH of the composition for oral cavity of the present invention at 25° C. is preferably 6.5 or more, more preferably 7 or more, from the viewpoint of promoting the formation of a salt by the components (B) and (C). More preferably, it is 7.5 or more, preferably 9.5 or less, more preferably 9 or less, and further preferably from the viewpoint of ensuring good flavor while preventing discoloration of the composition and modulation of the fragrance. Is 8.5 or less.
The pH of the oral composition of the present invention is a value measured at 25° C. using a pH electrode, and when the oral composition of the present invention is a liquid toothpaste composition, the composition should be diluted. When the oral composition of the present invention is a toothpaste composition, it is measured without adjusting to an aqueous solution having a concentration of 10% by mass with purified water composed of ion-exchanged water or distilled water. Means the value

The oral composition of the present invention exhibits an excellent biofilm removal effect, and can effectively prevent pain caused by dentin hypersensitivity, and therefore, an oral composition for dentin hypersensitivity. That is, it can be widely used as a dentin hypersensitivity reducing agent or a preventive agent.

The method for producing the oral cavity composition of the present invention is not particularly limited, and the above components may be appropriately mixed by a conventional method.
Specifically, for example, it is obtained in the step (I) and the step (I) in which a mixture containing the component (B) and at least a part of the component (D) and having a pH at 25° C. of 9 or more is obtained and heated. It is preferable to include a step (II) of mixing the component (C) with the mixture, and a step (III) of adding the component (A) to the mixture obtained in the step (II). The heating temperature of the mixture in step (I) is preferably 40° C. or higher, more preferably 50° C. or higher, even more preferably 55° C. or higher, preferably 100° C. or lower, more preferably 80° C. It is below.
In this step (II), it is preferable to mix other water-soluble components with the mixture obtained in step (I). Examples of the other water-soluble component include a water-soluble component such as a fluoride ion supplying compound and saccharin sodium. Further, a binder may be added and mixed.

Further, in the step (III), it is preferable to add the component (A) and powders such as a surfactant and an abrasive. In this step (II) or step (III), the rest of the component (D) may be added and mixed.
Further, after the step (III), a step (IV) of adding a fragrance to the mixture obtained in the step (III) and mixing at room temperature of 15 to 30° C. may be provided.

Regarding the above-described embodiment, the present invention further discloses the following oral compositions.
[1] The following components (A), (B), (C) and (D):
(A) Erythritol 3% by mass or more and 33% by mass or less (B) Potassium compound (C) N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms or an alkali metal salt thereof (D) Water, and a component ( A composition for oral cavity in which the mass ratio ((D)/(A)) between the content of D) and the content of component (A) is 1 or more and 10 or less.
[2] The content of the component (A) is preferably 5% by mass or more, more preferably 8% by mass or more, further preferably 10% by mass or more, still more preferably 20% by mass or more. Yes, preferably 32% by mass or less, more preferably 31% by mass or less, and further preferably 30% by mass or less, the oral composition according to the above [1].
[3] The mass ratio ((B)/(A)) of the content of the component (A) to the content of the component (B) is preferably 0.1 or more, more preferably 0.13 or more. Yes, more preferably 0.15 or more, still more preferably 0.18 or more, even more preferably 0.2 or more, preferably 1.5 or less, more preferably 1.25 or less. And more preferably 1 or less, and even more preferably 0.8 or less, [1] or [2].

[4] The amino acid portion of the N-acyl amino acid in the component (C) is preferably one or more selected from glutamic acid, glycine and alanine, and more preferably one or two selected from glutamic acid and glycine. And more preferably glycine, the composition for oral cavity according to any one of the above [1] to [3].
[5] The acyl group of the N-acyl amino acid in the component (C) is preferably one or more selected from myristoyl group, palmitoyl group and stearoyl group, and more preferably myristoyl group. [4] The composition for oral cavity of any one of [4].
[6] The content of the component (C) in terms of acid is preferably 0.01% by mass or more, more preferably 0.05% by mass or more, and further preferably 0.1% by mass or more. It is preferably 2% by mass or less, more preferably 1.5% by mass or less, still more preferably 1% by mass or less, and the oral composition according to any one of the above [1] to [5].
[7] The mass ratio ((C)/(A)) between the acid equivalent amount of the component (C) and the content of the component (A) is preferably 0.001 or more, more preferably 0.004 or more. And more preferably 0.008 or more, preferably 0.035 or less, more preferably 0.03 or less, still more preferably 0.02 or less. [1] to [6] No. 1 oral composition.

[8] The content of the component (D) is preferably 8% by mass or more, more preferably 10% by mass or more, further preferably 12% by mass or more, still more preferably 15% by mass or more. Yes, even more preferably 33 mass% or more, even more preferably 34 mass% or more, even more preferably 40 mass% or more, even more preferably 45 mass% or more, preferably 60 mass% %, more preferably 55% by mass or less, and further preferably 50% by mass or less, the oral composition according to any one of the above [1] to [7].
[9] The mass ratio ((D)/(A)) of the content of the component (D) and the content of the component (A) is preferably 2 or more, more preferably 3 or more, and further preferably Is 3.5 or more, preferably 9 or less, more preferably 5 or less, the oral composition according to any one of the above [1] to [8].
[10] Any of the above-mentioned [1] to [9], which further contains a fatty acid divalent metal salt (E) having a hydrocarbon group having 12 to 18 carbon atoms, and is preferably zinc stearate as the component (E). The composition for oral cavity of 1.
[11] The content of the component (E) is preferably 0.1 to 3% by mass, more preferably 0.2 to 2% by mass, and still more preferably 0.4 to 1.8% by mass. The composition for oral cavity according to any one of [1] to [10] above.

[12] Maltitol (F) is further contained, and the content of the component (F) is preferably 1 to 30% by mass, more preferably 3 to 20% by mass, and further preferably 5 to 15% by mass. %, The oral composition according to any one of the above [1] to [11].
[13] The content of the component (B) is preferably 0.001% by mass or more, more preferably 0.01% by mass or more, still more preferably 0.05% by mass or more, even more preferably Is 2% by mass or more, more preferably 3% by mass or more, even more preferably 4% by mass or more, preferably 10% by mass or less, more preferably 8% by mass or less, and The oral composition according to any one of the above [1] to [12], which is preferably 7% by mass or less.
[14] It further contains an amphoteric surfactant (G), and the content of the component (G) is preferably 0.05% by mass or more, more preferably 0.1% by mass or more, and further preferably 0.25% by mass or more, preferably 3% by mass or less, more preferably 2% by mass or less, and further preferably 0.8% by mass or less, [1] to [13]. Composition for oral cavity.
[15] The mass ratio ((G)/(A)) of the content of the component (G) and the content of the component (A) is preferably 0.001 or more, more preferably 0.5 or more. Yes, more preferably 0.1 or more, preferably 0.05 or less, the oral composition according to the above [14].
[16] Component (B) and step (I) containing at least a part of component (D) and having a pH at 25° C. of 9 or more and heating the mixture, and the mixture obtained in step (I) The method includes a step (II) of mixing (C) and a step (III) of adding the component (A) to the mixture obtained in the step (II), preferably 15 to 30° C. after the step (III). The method for producing an oral composition according to any one of [1] to [15] above, which comprises the step (IV) of adding a fragrance to the mixture obtained in the step (III) and mixing the mixture at room temperature.

Hereinafter, the present invention will be specifically described based on Examples. Unless otherwise specified in the table, the content of each component is% by mass.

[Examples 1 to 11, Comparative Examples 1 to 6]
The oral compositions shown in Tables 1 and 2 were produced by mixing the respective components by the above production method. The contents of the component (C) in Tables 1 and 2 are shown in terms of acid.
Each of the obtained compositions was evaluated according to the methods and criteria shown below.

<<Evaluation of closed state of opening of dentinal tubule>>
Approximately 1 cm of each piece of bovine dentin (thickness: about 500 μm) was mirror-polished with a sandpaper with an abrasive grain size of 40 μm and a sandpaper with an abrasive grain size of 3 μm, and then ultrasonically treated for 10 minutes. did. Then, the smear layer is completely removed by performing an etching treatment with a 1% citric acid aqueous solution for 20 seconds and then performing an ultrasonic treatment for 10 minutes again to expose the opening of the dentinal tubule of bovine dentin, It was used as a dentin sample.
Next, 1 g of each composition was placed on a toothbrush (Deep Clean Ultra Compact Ordinary, manufactured by Kao Corporation), the dentin sample was brushed for 1 minute, and then the sample was washed with distilled water for 10 seconds. Platinum was vapor-deposited on the surface of the sample after washing, and the dentin surface was photographed at a magnification of 2000 using an electron microscope (VE-7800, manufactured by KEYENCE, accelerating voltage 2 kV). The condition was evaluated.
Electron micrographs of Example 1 and Comparative Example 2 are shown in FIGS. 1 and 2, respectively.
As shown in FIG. 1, in Example 1, the openings of the dentinal tubules were sufficiently covered, whereas in Comparative Example 2 shown in FIG. 2, only a slight amount of deposits could be confirmed on the surface of the dentin. It can be seen that the ivory tubules are almost exposed.

《Sensory sensory evaluation》
For each composition shown in Tables 1 and 2, the degree of pain prevention due to hypersensitivity of dentin immediately after use was evaluated. The panelists were those who had teeth bleeding every day in the last month, or those who had more than 2 or 3 times a week. The evaluation method was as follows: 3 panelists took 1 g of each oral composition on a toothbrush (Deep Clean Super Compact Ordinary, manufactured by Kao Co., Ltd.), brushed for 1 minute, spit out and rinse the mouth with cold water, and immediately after use. The pain caused by hypersensitivity of dentin was evaluated by holding the mouth in the mouth.
The evaluation was obtained from four factors: 4: no stains, 3: almost no stains, 2: slight stains, 1: stains, and the average value of the panelists' responses was due to dentin hypersensitivity. The effect of suppressing pain was evaluated.
The results are shown in Tables 1 and 2.
In addition, the larger the number, the more the suppression or reduction of the pain caused by the hypersensitivity of dentin.

<<Evaluation method of plaque removing property>>
1) Collection of stimulated saliva Targeting healthy men in their twenties to thirties, the gum pellets contained in Dent Buff Strip (Oral Care Inc. OralCare Inc.) were chewed, and saliva accumulated in the mouth each time. Saliva was collected in such a Falcon tube by having the Falcon tube exhale. Since the bacteria in saliva differ from person to person, the plaque-removing properties of all the examples and comparative examples were evaluated using saliva of one healthy male.
2) Preparation of dental plaque model Saliva collected in a falcon tube was centrifuged at 3000 rpm/rt (25°C)/10 min (cooling centrifuge CF15RN, manufactured by HITACHI). Using the separated supernatant saliva, sucrose was added so as to be a 5 mass% solution, and then stirred using a stirring device (voltex, manufactured by Nippon Genetics Co., Ltd.) to prepare a plaque model test solution.
Next, one side of the HAp substrate (manufactured by Cosmo Bio, 1 cm square) was mirror-polished using 40 μm, 12 μm, and 3 μm polishing paper, and then immersed in 1N HCl for 1 minute for acid deashing treatment. The treated HAp plate is washed with ion-exchanged water, dried, put in a 24-well plate, and 1 mL of each of the above-prepared plaque model test solutions is added, and then stored in a plastic case together with a CO ₂ pack to anaerobically Under the conditions, the cells were cultured at 37° C. for 48 hours.

3) Evaluation of Plaque Removal Property Using a vacuum pump, saliva in the plate was absorbed, 1 mL of ion-exchanged water was added, and the plate was shaken for 5 minutes. Next, water was absorbed using a pump, 1 mL of each composition obtained in Examples and Comparative Examples was added, and the mixture was shaken for 5 to 20 minutes. Shaking was performed using a shaker (BioShake iQ (Waken Betech Co., Ltd.)) at room temperature (25° C.) and 500 rpm.
Then, each composition was absorbed, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, and this was repeated twice. Next, water was absorbed, 750 μL of a 0.1 mass% crystal violet (CV) solution was added, and the mixture was shaken for 15 minutes.
Further, the CV staining solution was sucked up with a pump, 1 mL of ion-exchanged water was added, and the mixture was shaken for 5 minutes, and this was repeated twice. Then, absorb the water with a pump, add 500 μL of ethanol and pipette, dilute the extract 10 times with ion-exchanged water, and use a microplate recorder (TECAN wavelength tunable absorption microplate reader Sunrise Rainbow Thermo). Absorbance OD _{595 nm} was measured.
Further, without using the composition obtained above, the plaque residual rate (%) was calculated according to the following formula, using the absorbance OD _{595 nm} (initial value) just washed with ion-exchanged water as a reference.
Plaque residual ratio (%) = × 100 {OD 595nm only washed with OD _{595 nm} / ion-exchanged water at the time of using the resulting composition}
Based on the obtained plaque residual rate (%), the plaque removability was evaluated according to the following criteria. It should be noted that the smaller the obtained plaque residual rate value, the higher the plaque removability.
The results are shown in Tables 1-2.
AA: Plaque removability is sufficiently high (remaining plaque rate less than 40%)
A: Highly removable plaque (plaque plaque remaining rate of 40% or more and less than 60%)
B: Slightly high plaque removability (remaining plaque rate 60% or more and less than 80%)
C: Low plaque removability (remaining plaque rate of 80% or more)

Claims

The following components (A), (B), (C) and (D):
(A) Erythritol 3% by mass or more and 33% by mass or less (B) Potassium compound (C) N-acyl amino acid having a hydrocarbon group having 14 to 18 carbon atoms or an alkali metal salt thereof (D) Water, and a component ( A composition for oral cavity in which the mass ratio ((D)/(A)) between the content of D) and the content of component (A) is 1 or more and 10 or less.
The oral composition according to claim 1, wherein the amino acid portion of the N-acyl amino acid in the component (C) is one or more selected from glutamic acid, glycine and alanine.
The oral composition according to claim 1 or 2, further comprising a fatty acid divalent metal salt (E) having a hydrocarbon group having 12 to 18 carbon atoms.
The oral composition according to claim 3, wherein the component (E) is zinc stearate.
The oral composition according to any one of claims 1 to 4, which is an oral composition for dentin hypersensitivity.