JP6038563B2 - Oral composition - Google Patents

Description

  The present invention relates to an oral composition.

  Conventionally, in oral compositions, not only sugar alcohols such as xylitol, which are known to have growth-inhibiting action on caries-causing bacteria, but also sugar alcohols such as reduced palatinose are used. Attempts have been made to exert various effects by blending them together.

  For example, Patent Document 1 discloses a composition for oral cavity containing palatinit (Mitsui Sugar Co., Ltd.) and a fluorine compound, and attempts have been made to promote remineralization by the action of palatinit. Patent Document 2 discloses a composition for oral cavity in which a specific surfactant and paratinite are blended, and the bitterness is reduced by paratinit while suppressing coloring of teeth by such surfactant. Has brought a good feeling of use.

  On the other hand, Patent Document 3 discloses a composition for oral cavity in which palatinit and various bactericides are blended, and the bactericidal effect is improved by using these in combination. On the other hand, Patent Document 4 discloses a composition for oral cavity in which various sugar alcohols such as erythritol, xylitol, glucopyranosyl sorbitol, glucopyranosyl mannitol and amino acids are blended to inhibit the formation of biofilm. Or facilitates the removal of biofilms.

Japanese Patent Laid-Open No. 2000-247852 JP 2000-319148 A JP 2000-281545 A JP 2007-145876 A

  However, when various medicinal ingredients are used to prevent or improve periodontal diseases and oral diseases such as gingivitis, it is possible to quickly bring medicinal effects when reaching a local site (gingival sulcus or periodontal pocket). Although effective, the composition as described in the above literature has a problem that it is difficult to reach the local site because it dissolves and diffuses until the medicinal component is delivered locally. In addition, it is possible to take a method of increasing the viscosity of the composition by adding a large amount of a binder and extending the residence time in the oral cavity to increase the effect of the medicinal component, but local sites such as the gingival crevice are saliva and Since it is a narrow region filled with gingival crevicular fluid, it is still difficult to reach the medicinal component to the back of such region.

  Therefore, the present invention relates to a composition for oral cavity that can effectively bring the action of a medicinal component to a local region such as a gingival sulcus or periodontal pocket, which is a narrow region filled with saliva.

  Therefore, the present inventor immediately reduced the viscosity when reaching a local site such as a gingival sulcus or periodontal pocket, which is a narrow region filled with saliva or gingival crevicular fluid, while maintaining an appropriate viscosity. It has been noted that if a medicinal component can be released and acted quickly at such a site, it can effectively bring about a medicinal effect at the local site. And by containing specific sugar alcohol, oil-soluble medicinal ingredients, water and binder in specific amounts, and by making the mass ratio of sugar alcohol and water to specific values, local areas such as gingival crevice and periodontal pockets It has been found that an oral composition capable of effectively delivering a medicinal component to a site can be obtained.

That is, the present invention includes the following components (A) to (D):
(A) Sugar alcohol having a solubility in water at 20 ° C. of 30% by mass or less 25% by mass or more and 55% by mass or less,
(B) oil-soluble medicinal ingredients,
(C) Water 10 mass% or more and 35 mass% or less,
(D) Binder Contains 0.1% by mass or more and 1.5% by mass or less, and the mass ratio (A / C) between component (A) and component (C) is greater than 1 and 5.5 or less. The present invention relates to an oral composition.

  If the dentifrice composition of the present invention is used, the oil-soluble medicinal component efficiently reaches a local site such as a gingival crevice or a periodontal pocket, which is a narrow region, and effectively releases the medicinal component at the local site and The effect of the oil-soluble medicinal component can be exhibited efficiently.

It is a longitudinal cross-sectional view which shows the conceptual diagram of the model 1 for evaluating the delivery property of a medicinal ingredient to a gingival crevice. It is a perspective view which shows the conceptual diagram of the model 1 for evaluating the delivery property of a medicinal ingredient to a gingival crevice. It is a conceptual diagram which shows a mode that a flowing water is poured into the model 1 shown in FIG.

Hereinafter, the present invention will be described in detail.
The composition for oral cavity of the present invention contains 25% by mass or more and 55% by mass or less of a sugar alcohol having a solubility in water at 20 ° C. of 30% by mass or less (30 g or less dissolved in 100 g of a saturated aqueous solution) as the component (A). To do. This solubility imparts structural viscosity to the composition, improves the permeability of the oil-soluble medicinal component (B) in saliva, etc. that fills local sites such as the gingival sulcus and periodontal pocket, and ensures adequate fluidity. From the point to do, 5 mass% or more and 30 mass% or less are more preferable. Examples of such sugar alcohols include mannitol, glucopyranosyl sorbitol, glucopyranosyl mannitol, and reduced palatinose. More specifically, mannitol, α-D-glucopyranosyl-1,6-sorbitol, α-D- Examples include glucopyranosyl-1,6-mannitol, reduced palatinose, which is a mixture of α-D-glucopyranosyl-1,6-sorbitol and α-D-glucopyranosyl-1,6-mannitol, and has low solubility in water and is easy to handle. Mannitol is preferable from the standpoint of cooling and a cool feeling at the time of dissolution, and reduced palatinose is preferable from the viewpoint of moderate solubility and a moisturizing effect due to hygroscopicity.

  Mannitol is a kind of hexitol and is a sugar alcohol of mannose. Industrially, it is produced by electrolytic reduction of corn starch sugar and high-pressure reduction of sucrose. The mannitol used in the present invention is not particularly limited as long as it is at least one selected from D-mannitol, L-mannitol, and D, L-mannitol, but D-mannitol existing in nature is available. Easy and preferred. The solubility of mannitol in water at 20 ° C. is 18% by mass (18 g dissolved in 100 g of a saturated aqueous solution at 20 ° C.).

  Reduced palatinose is a disaccharide sugar alcohol and is an equimolar mixture of α-D-glucopyranosyl-1,6-mannitol and its isomer α-D-glucopyranosyl-1,6-sorbitol. Reduced palatinose is obtained by using sucrose as a raw material, converting sucrose to palatinose with a glycosyltransferase, and then carrying out a hydrogenation reaction. Palatinit, known as reduced palatinose, is a trade name of Mitsui Sugar Co., Ltd. and Suducker AG (Japanese name: South German Sugar Co., Ltd.), and there is another name called isomalt. The solubility of paratinite in water at 20 ° C. is 28% by mass (28 g dissolved in 100 g of a saturated aqueous solution at 20 ° C.).

These sugar alcohols (A) may contain 1 type (s) or 2 or more types, and as a sugar alcohol (A), you may mix | blend any of powder and a granule.
The content of the sugar alcohol (A) ensures fluidity of the component (A) while imparting structural viscosity to the composition, and is delivered to a local site such as a gingival sulcus or periodontal pocket, which will be described later. From the viewpoint of effectively exhibiting the action of the component (B), the composition for oral cavity of the present invention is 25% by mass or more, preferably 27% by mass or more, and more preferably 30% by mass or more. . The content of the sugar alcohol (A) is 55% by mass or less in the composition for oral cavity of the present invention from the viewpoint of imparting good structural viscosity and the dispersibility of the composition in the oral cavity, Preferably it is 50 mass% or less, More preferably, it is 45 mass% or less. Moreover, content of sugar alcohol (A) is 25-55 mass%, Preferably it is 27-50 mass%, More preferably, it is 30-45 mass%.

  The composition for oral cavity of this invention contains an oil-soluble medicinal ingredient as a component (B). The oil-soluble medicinal component (B) is not particularly limited, but the oral composition of the present invention efficiently reaches a local site such as a gingival sulcus or periodontal pocket, which is a narrow region, and at such a local site. It is preferable to use a medicinal component known to exhibit preventive and improving effects on periodontal disease because it is excellent in the effect of effectively releasing and acting the medicinal component. Examples of the oil-soluble medicinal component (B) include azulene, guaiazulene, tocopherols such as dl-α-tocopherol acetate and tocopherol nicotinate, α-glycyrrhetinic acid, β-glycyrrhetinic acid, glycyrrhizic acid, triclosan, isopropylmethylphenol, Hinokitiol, dihydrocholesterol, dihydroabietic acid and the like can be mentioned, and one or more selected from these can be contained. Of these, tocopherol, β-glycyrrhetinic acid, triclosan, and isopropylmethylphenol are preferable from the viewpoint of effectively providing medicinal effects at local sites such as gingival crevice and periodontal pocket.

  The content of the oil-soluble medicinal component (B) is preferably 0.001% by mass or more, more preferably 0.005% by mass in the composition for oral cavity of the present invention from the viewpoint of effectively exerting medicinal properties. % Or more, and more preferably 0.01% by mass or more. The content of the oil-soluble medicinal component (B) is preferably 10% by mass or less, and more preferably in the oral composition of the present invention, from the viewpoint of ensuring an appropriate range of application amount and good taste. Is 5% by mass or less, more preferably 1% by mass or less, and may be 0.5% by mass or less. Further, the content of the oil-soluble medicinal component (B) is preferably 0.001 to 10 mass in the oral composition of the present invention from the viewpoint of balancing the taste and the like while effectively acting the medicinal effect. %, More preferably 0.005 to 5% by mass, still more preferably 0.01 to 1% by mass, and still more preferably 0.01 to 0.5% by mass.

The oil-soluble medicinal component (B) may be used after being dissolved in a solvent (oil agent) that is liquid at room temperature (25 ° C.). Examples of such solvents include fatty acid ester oils such as isopropyl myristate and isopropyl palmitate, liquid triglycerides such as dicapric acid neopentyl glycol, fatty acid (C ₈ , C ₁₀ ) triglyceride, and the like.

  The composition for oral cavity of this invention contains 10 mass% or more and 35 mass% or less of water as a component (C). By containing water in such an amount, the composition has structural viscosity due to the presence of the undissolved sugar alcohol (A), and the flow of the oil-soluble medicinal component (B) dispersed in the contained water (C). While reducing the viscosity of the composition immediately upon reaching a local site such as a gingival sulcus or periodontal pocket, which is a narrow region filled with saliva, while releasing the medicinal component quickly at such site It is thought that it can act. In addition, since the amount of sugar alcohol (A) dissolved in water (C) is small, fluidity of water or the like present in the composition is secured, and the oil-soluble medicinal component (B) dispersed in water or the like is added. It becomes possible to flow at a high concentration, and the high-concentration oil-soluble medicinal component (B) flows and penetrates into saliva and the like, and the component (B) reaches the back of the local site such as the gingival crevice and periodontal pocket. It is thought that the action by can be brought about. Thus, it is considered that the composition for oral cavity of the present invention can effectively exert the action of a medicinal component to local sites such as gingival sulcus and periodontal pocket, which are narrow regions filled with saliva. In addition, the water (C) contains the water | moisture content contained in each component to mix | blend, for example, sorbitol liquid etc. other than the mix | blended purified water.

  The content of water (C) is the oral cavity of the present invention from the viewpoint of improving the deliverability of the oil-soluble medicinal component (B) to local sites such as the gingival crevice and periodontal pocket and the feeling of use of the oral composition. It is 10 mass% or more in the composition for use, Preferably it is 12 mass% or more, More preferably, it is 15 mass% or more. The content of water (C) is 35% by mass or less in the composition for oral cavity of the present invention, and preferably 30% by mass or less, from the viewpoint of ensuring good structural viscosity imparted to the composition. More preferably, it is 27 mass% or less. Moreover, content of water (C) is 10-35 mass%, Preferably it is 12-30 mass%, More preferably, it is 15-27 mass%.

  The composition for oral cavity of the present invention has a mass ratio (A / C) of sugar alcohol (A) to water (C) of more than 1 and 5.5 or less. By maintaining such a mass ratio between the component (A) and the component (C), the sugar alcohol (A) is contained in the oral composition beyond the saturated dissolved state, and the sugar alcohol (A) in the undissolved state (A ) To give the composition an appropriate structural viscosity, it is possible to improve the delivery of the oil-soluble medicinal component (B) to a local site such as the gingival sulcus. The mass ratio (A / C) between the sugar alcohol (A) and the water (C) is greater than 1 from the viewpoint that the undissolved sugar alcohol (A) is present and the composition has a good structural viscosity. Preferably, it is 1.2 or more, more preferably 1.5 or more. The mass ratio (A / C) between the sugar alcohol (A) and the water (C) is 5.5 or less from the viewpoint of ensuring the fluidity of the oil-soluble medicinal component (B) dispersed in the water (C). Thus, it is preferably 4 or less, more preferably 3 or less. Moreover, the mass ratio (A / C) of the sugar alcohol (A) and the water (C) is preferably more than 1 and not more than 5.5, more preferably 1.2 to 4, and still more preferably 1. .5-3.

  Even when the oil-soluble medicinal component (B) is blended in a small amount of 0.01 to 0.2% by mass, for example, the oral cavity composition of the present invention can be used for the gingival crevice by the blended sugar alcohol (A). The mass ratio (A / B) between the sugar alcohol (A) and the oil-soluble medicinal component (B) is preferably 220 to 3000, and is preferably 270 to 2700 from the viewpoint of improving the delivery to the local site. Is more preferable, and 300 to 2500 is even more preferable.

  The composition for oral cavity of this invention contains 0.1 to 1.5 mass% of binder as a component (D). Usually, a caking additive is mix | blended for the gelatinization of a gel-like dentifrice, or for paste-like dentifrice, the caking of a toothpaste, or caking of an application agent. In the present invention, a binder (D) is contained in order to ensure fluidity of the oil-soluble medicinal component (B) dispersed in water (C) while maintaining an appropriate viscosity. Examples of the binder (D) include sodium carboxymethyl cellulose, hydroxyethyl cellulose, carboxyvinyl polymer, xanthan gum, carrageenan, sodium alginate, hydroxypropyl cellulose, guar gum, sodium chondroitin sulfate, and the like. Sodium carboxymethyl cellulose, xanthan gum, carrageenan preferable. Component (D) can contain one or more selected from the above.

  Content of a component (D) is 0.1 mass% or more in the composition for oral cavity of this invention from an appropriate viscosity and a viewpoint of storage stability, Preferably it is 0.2 mass% or more. Content of a component (D) is 1.5 mass% or less in the composition for oral cavity of this invention from a viewpoint of ensuring the fluidity | liquidity of the oil-soluble medicinal component (B) disperse | distributed in water (C). And, it is preferably 1.3% by mass or less.

  Although the composition for oral cavity of this invention contains the sugar alcohol (A) which has fixed solubility, as a component (E), the solubility with respect to water in 20 degreeC exceeds 30 mass%, and is 40 mass% or less (saturated aqueous solution). You may contain the other sugar alcohol whose dissolution amount exceeds 30g and 40g or less with respect to 100g. When other sugar alcohol (E) is contained, the content of component (E) is used in combination with component (A) to deliver oil-soluble medicinal component (B) to a local site such as gingival crevice. From the viewpoint of improving the properties, the composition for oral cavity of the present invention is preferably 1% by mass or more, more preferably 2% by mass or more, and further preferably 5% by mass or more. The content of the component (E) is preferably 30% by mass or less in the oral composition of the present invention from the viewpoint of ensuring fluidity of the oil-soluble medicinal component (B) dispersed in water (C). More preferably, it is 20 mass% or less, More preferably, it is 15 mass% or less. Moreover, content of a component (E) becomes like this. Preferably it is 1-30 mass%, More preferably, it is 2-20 mass%, More preferably, it is 5-15 mass%.

  When the other sugar alcohol (E) is contained, the mass ratio (E / A) of the component (E) and the sugar alcohol (A) is preferably 1 or less, more preferably 0.7 or less. Yes, more preferably 0.5 or less, preferably 0.02 or more, more preferably 0.1 or more, more preferably 0.2 or more.

  Furthermore, other sugar alcohols (E) with respect to water (C) contained in the composition for oral cavity from the viewpoint of ensuring fluidity in the composition of component (B) while imparting good structural viscosity to the composition. ) And the sugar alcohol (A) total content mass ratio ((A + E) / C) is preferably greater than 1, more preferably 1.2 or more, even more preferably 1.5 or more, Is 5.5 or less, more preferably 4 or less, and still more preferably 3.5 or less. Further, the mass ratio ((A + E) / C) is preferably larger than 1 and not larger than 5.5, more preferably 1.2 to 4, and further preferably 1.5 to 3.5.

  Examples of the other sugar alcohol (E) include erythritol having a solubility in water at 20 ° C. of 33% by mass.

  The composition for oral cavity of this invention can contain the sugar alcohol with the high solubility which the solubility with respect to water in 20 degreeC exceeds 40 mass% as a component (F). The mass ratio (F / A) of the component (F) to the component (A) is preferably 1.5 or less from the viewpoint of not inhibiting the delivery of the oil-soluble medicinal component (B) to a local site such as a gingival sulcus. More preferably, it is 1 or less, More preferably, it is 0.8 or less. Moreover, the mass ratio (F / C) of the component (F) and the component (C) water contained in the oral cavity composition is preferably 1.5 or less.

  Examples of the sugar alcohol (F) include xylitol having a solubility in water at 20 ° C. of 66 mass%, 60 mass% maltitol, and 72 mass% sorbitol.

  The oral composition of the present invention includes, in addition to the above components, fluorine such as a foaming agent, a foaming aid, an abrasive, a wetting agent, a sweetening agent, a preservative, and sodium fluoride, as long as the effects of the present invention are not impaired. An ion supply compound, a pigment, a coloring matter, a fragrance and the like can be appropriately contained. In addition, the composition for oral cavity of the present invention is prepared in a dosage form such as a gel or paste, for example, a dentifrice such as a toothpaste or a gel dentifrice, or an oral application such as an oral ointment. It is possible to use a toothpaste.

  The composition for oral cavity of the present invention is glycerin, propylene glycol, 1, from the viewpoint of obtaining a good feeling of use while reducing the content of water of the component (C) of the present invention relative to the component (A). It is preferable to contain a wetting agent other than the above components (A), (E) and (F) selected from 3-butylene glycol, polyethylene glycol and dipropylene glycol, and the content of these wetting agents is In the composition for oral cavity, it is preferably 1 to 15% by mass, more preferably 2 to 10% by mass. Further, from the viewpoint of obtaining a good feeling of use while maintaining the shape-retaining property due to the structural viscosity of the component (A) of the present invention, it is measured by a method according to thickening silica (JIS K5101-13-2 (established in 2004)). It is preferable that the oil absorption amount to be contained is 200 to 400 mL / 100 g). The content of the thickening silica in the oral composition of the present invention is preferably 0.1% by mass in the oral composition of the present invention, from the viewpoint of good viscosity of the composition and dispersibility in the oral cavity. It is above, More preferably, it is 0.5 mass% or more, Preferably it is 15 mass% or less, More preferably, it is 10 mass% or less, More preferably, it is 8 mass% or less. The abrasive silica used as the abrasive has an oil absorption of 50 to 150 mL / 100 g measured by a method according to JIS K5101-13-2 (established in 2004).

  The composition for oral cavity of the present invention is effective in terms of retention in the oral cavity, adhesion to mucous membranes, shape retention when used as a coating agent or dentifrice, and saliva when reaching a local site. From the viewpoint of reducing the viscosity, the viscosity at 25 ° C. is preferably 1500 dPa · s or more, more preferably 2000 dPa · s or more, preferably 5000 dPa · s or less, more preferably 4000 dPa · s or less. is there. Further, the viscosity at 25 ° C. is preferably 1500 to 5000 dPa · s, more preferably 2000 to 4000 dPa · s. By setting the viscosity of the composition for oral cavity of the present invention within such a range, the sugar alcohol in an undissolved state is dispersed in the contained water (C) while having shape retention due to the structural viscosity of the composition. The fluidity of the oil-soluble medicinal component (B) can be ensured. Such a viscosity is packed in a container for viscosity measurement and stored for 24 hours in a thermostatic chamber at 25 ° C., and then a rotor TC with a rotation speed of 2.times. Using a helicus type viscometer (VISCOMETER TVB-10 Toki Sangyo). It can be measured at 5 rpm for 1 minute.

  The composition for oral cavity of the present invention preferably has a viscosity (25 ° C.) at a dilution of 1.2 times obtained by adding 20 parts by mass of water with respect to 100 parts by mass of the composition of 500 dPa · s or less. What becomes 20% or less with respect to the viscosity (25 degreeC) of the composition before adding is preferable, What becomes 17% or less is more preferable, What becomes 15% or less is further more preferable. In addition, it is preferable to set it as 3% or more with respect to the viscosity (25 degreeC) before dilution (25 degreeC) at the time of 1.2 time dilution with water, and it is more preferable to set it as 5% or more. Since the composition for oral cavity of the present invention imparts a structural viscosity to the composition by the undissolved sugar alcohol, the structural viscosity is destroyed by adding water, and the viscosity is greatly reduced. In a preferred embodiment, after dilution, according to a dilution model with saliva during toothpaste operation or application of a coating agent, similar to dilution with 20 parts by weight of water with respect to 100 parts by weight of the oral composition The viscosity of the composition of the present invention is reduced to 20% or less of the viscosity of the composition before dilution, so that the oil-soluble medicinal component (B) dispersed in water (C) has a high concentration and fluidity at a local site such as a gingival crevice The viscosity is quickly reduced by saliva etc. at such a site, and the component (B) can be released and acted on the local site. In the evaluation of the examples described later, in order to ensure the measurement accuracy of the viscosity, the viscosity (25 ° C.) when 20 parts by mass of water is added to 100 parts by mass of the composition is obtained by adding water, The viscosity is measured 24 hours after mixing.

In relation to the embodiment described above, the present invention further discloses the following dentifrice composition.
[1] The following components (A) to (D):
(A) Sugar alcohol having a solubility in water at 20 ° C. of 30% by mass or less 25% by mass or more and 55% by mass or less (B) Oil-soluble medicinal component (C) Water 10% by mass or more and 35% by mass or less (D) Binder The composition for oral cavity which contains 0.1 mass% or more and 1.5 mass% or less, and whose mass ratio (A / C) of a component (A) and a component (C) is larger than 1 and is 5.5 or less.
[2] Component (A) is one or more selected from mannitol, glucopyranosyl sorbitol, glucopyranosyl mannitol and reduced palatinose, preferably mannitol, α-D-glucopyranosyl-1,6 1 type selected from reduced palatinose which is a mixture of sorbitol, α-D-glucopyranosyl-1,6-mannitol, and α-D-glucopyranosyl-1,6-sorbitol and α-D-glucopyranosyl-1,6-mannitol Or it is 2 or more types, More preferably, the composition for oral cavity of said [1] which is 1 type or 2 types chosen from mannitol and reduced palatinose.
[3] The content of component (A) is 27% by mass or more, more preferably 30% by mass or more, 50% by mass or less, and more preferably 45% by mass or less [1] or [2] oral cavity composition.

[4] Component (B) is azulene, guaiazulene, dl-α-tocopherol acetate, tocopherol nicotinate, α-glycyrrhetinic acid, β-glycyrrhetinic acid, glycyrrhizic acid, triclosan, isopropylmethylphenol, hinokitiol, dihydrocholesterol, and dihydro Any one or two or more selected from abietic acid, preferably one or more selected from tocopherol, β-glycyrrhetinic acid, triclosan and isopropylmethylphenol The composition for oral cavity according to 1.
[5] The content of component (B) is preferably 0.001% by mass or more, more preferably 0.005% by mass or more, still more preferably 0.01% by mass or more, and preferably 10%. Any one of the above-mentioned [1] to [4], which is not more than 5% by mass, more preferably not more than 5% by mass, still more preferably not more than 1% by mass, and further preferably not more than 0.5% by mass. The composition for oral cavity of description.
[6] The mass ratio (A / B) between the component (A) and the component (B) is 220 to 3000, preferably 270 to 2700, more preferably 300 to 2500. The composition for oral cavity according to any one of [5].

[7] The content of the component (C) is 12% by mass or more, more preferably 15% by mass or more, 30% by mass or less, and more preferably 27% by mass or less. The composition for oral cavity according to any one of [6].
[8] The mass ratio (A / C) of the component (A) to the component (C) is 1.2 or more, preferably 1.5 or more, 4 or less, preferably 3 or less. The composition for oral cavity according to any one of [1] to [7].

[9] Component (D) is one or more selected from sodium carboxymethylcellulose, hydroxyethylcellulose, carboxyvinyl polymer, xanthan gum, carrageenan, sodium alginate, hydroxypropylcellulose, guar gum, and sodium chondroitin sulfate, preferably Is a composition for oral cavity according to the above [1] to [8], which is one or more selected from sodium carboxymethylcellulose, xanthan gum and carrageenan.
[10] The composition for oral cavity according to any one of [1] to [9], wherein the content of the component (D) is preferably 0.2% by mass or more, and preferably 1.3% by mass or less. object.

[11] The above [1], further comprising (E) another sugar alcohol having a solubility in water at 20 ° C. of more than 30% by mass and 40% by mass or less (solubility of more than 30g but not more than 40g with respect to 100g of a saturated aqueous solution). The composition for oral cavity of any one of-[10].
[12] The content of component (E) is 1% by mass or more, preferably 2% by mass or more, more preferably 5% by mass or more, and 30% by mass or less, preferably 20% by mass. It is below, More preferably, it is 15 mass% or less, The composition for oral cavity of said [11].

[13] The mass ratio ((A + E) / C) of the total content of the component (E) and the component (A) to the component (C) is greater than 1, preferably 1.2 or more, more preferably The composition for oral cavity according to the above [11] or [12], which is 1.5 or more, 5.5 or less, preferably 4 or less, more preferably 3.5 or less.
[14] The mass ratio (E / A) of the component (E) to the component (A) is 1 or less, preferably 0.7 or less, more preferably 0.5 or less, and preferably 0.8. It is 02 or more, More preferably, it is 0.1 or more, More preferably, it is 0.2 or more, The composition for oral cavity of said [11]-[13].
[15] The composition for oral cavity according to the above [11] to [14], wherein the component (E) is erythritol.

[16] The oral composition according to any one of the above [1] to [15], further comprising a sugar alcohol (F) having a solubility in water at 20 ° C. exceeding 40% by mass.
[17] The mass ratio (F / A) of the component (F) to the component (A) is 1.5 or less, preferably 1 or less, more preferably 0.8 or less. Oral composition.
[18] The composition for oral cavity according to the above [16] or [17], wherein the component (F) is one or more selected from xylitol, maltitol, and sorbitol.
[19] The viscosity at 25 ° C. is preferably 1500 dPa · s or more, more preferably 2000 dPa · s or more, preferably 5000 dPa · s or less, more preferably 4000 dPa · s or less. The composition for oral cavity of [18].
[20] The viscosity (25 ° C.) when 20 parts by mass of water is added to 100 parts by mass of the composition is 20% or less with respect to the viscosity (25 ° C.) of the composition before adding water. The composition for oral cavity according to any one of the above [1] to [19], wherein the composition is preferably 17% or less, more preferably 3% or more, and even more preferably 5% or more.
[21] 1-15% by mass, preferably 2-10% by mass, of one or more wetting agents selected from glycerin, propylene glycol, 1,3-butylene glycol, polyethylene glycol and dipropylene glycol The composition for oral cavity according to any one of [1] to [20] above.
[22] 0.1 to 15% by mass, preferably 0.5 to 10% by mass, more preferably 0.5 to 8% by mass of thickening silica having an oil absorption of 200 to 400 mL / 100 g The composition for oral cavity according to any one of [1] to [21] above.

[Examples 1-8, Comparative Examples 1-3]
According to the formulation shown in Table 1, each oral composition which is a toothpaste was prepared. Each oral composition was adjusted with thickening silica and a wetting agent so that the viscosity at 25 ° C. was 2600 to 3400 dPa · s. The initial viscosity of the obtained oral composition and the viscosity at the 1.2-fold dilution were measured by the following method, and then each oral composition was used and an oil-soluble medicinal component attached to the gingival crevice model 4 according to the following method The amount of (B) was compared. The results are shown in Table 1.

<Measurement of viscosity>
The obtained oral composition was packed in a container for viscosity measurement and stored for 24 hours in a thermostatic chamber at 25 ° C. to obtain an initial viscosity. Next, 20 parts by mass of water (25 ° C.) was added to 100 parts by mass of the oral composition, and the viscosity at the time of 1.2-fold dilution was measured 24 hours after the addition of water. Each viscosity was measured at 25 ° C. using a helipath type viscometer (VISCOMETER TVB-10 Toki Sangyo) under the conditions of rotor TC, rotation speed 2.5 rpm, and 1 minute.

<< Evaluation of deliverability to gingival crevice >>
The delivery property of the oil-soluble medicinal component to the gingival sulcus was evaluated using the following model 1. As shown in FIGS. 1 and 2, the model 1 uses a transparent acrylic plate 11 (length d80 mm, height h30 mm, thickness w2.5 mm) as a tooth model 2 and is a silicone rubber similar to the hardness of gingiva. (Colored transparent) 12 was used as the gingival model 3.

  The silicone rubber 12 of the gingival model 3 is 20 degrees thick with a thickness w of 2 mm and a hardness of A (measured with a rubber hardness meter A WR104A of Nishitokyo Seimitsu Co., Ltd .: Type A durometer in accordance with JIS K 6253). Then, an acrylic spacer 13 having a thickness w2 of 6.5 mm is folded between silicone rubbers, and the silicone rubber 12 is drawn in a U shape in a region above the upper end surface of the spacer 13. Folded to. Note that the highest position of the bent portion of the silicone rubber 12 and the upper end of the acrylic plate 11 have the same height, and the distance H from the upper end of the spacer 13 to the highest position of the bent portion of the silicone rubber 12 (the upper end of the acrylic plate 11). Was 15 mm. A groove between the acrylic plate 11 and the silicone rubber 12 was a gingival groove model 4. In addition, for the convenience of the test of the deliverability evaluation to the gingival crevice using the composition for oral cavity, the silicone rubber 12 is sandwiched between the two acrylic plates 11, and 2 between the two acrylic plates 11 and the silicone rubber 12. The delivery of the groove at the location was evaluated as a gingival sulcus model 4. Further, in order to improve the adhesion between the silicone rubber 12 and the acrylic plate 11, double clips from the outside at both ends in the longitudinal direction of the acrylic plate 11 (KOKUYO Co., Ltd., double-click extra-large frontage: mouth width 50 mm chestnut-31) Sandwiched between. The length d of the spacer 13, the acrylic plate 11, and the silicone rubber 12 is the same 80 mm, both ends of the length d are sandwiched between double clips, and the length of the intermediate region not sandwiched between the double clips is about 40 mm. It was. In addition, the double clip used was unused or used within about 20 times.

Pour 0.2 g of water into the two gingival crevice models 4 of model 1 and place 1.0 g of each oral composition on the two gingival crevice models 4, and use a toothbrush (Puola Compact hair hardness: normal) The composition for the oral cavity remaining on the silicone rubber 12 between the two acrylic plates 11 after brushing for 40 strokes so that the toothbrush bristles enter between the two acrylic plates 11 as shown in FIG. Run the running water 14 to wash things, brush with a toothbrush while running in running water for 2 minutes to remove the oral composition attached to the surface of the gingival crevice model 4 (the surface of the acrylic plate 11 and the silicone rubber 12). It was confirmed visually that the composition for oral cavity was not attached to the surface. Then, in order to collect the medicinal components of the gingival sulcus model 4, the double clip that is sandwiched and fixed from the outside of the acrylic plate 11 is removed, the acrylic plate 11 and the silicone rubber 12 are separated, and the two acrylic plates 11 The two areas between the silicone rubbers 12 were scraped with two cotton swabs to collect the deposits. Put a cotton swab with adsorbed components into a 50 ml centrifuge tube, add 5 ml of methanol, shake with a vortex mixer (Cute Mixer CM-1000, manufactured by Tokyo Rika Kikai Co., Ltd.) for 20 minutes, and then apply ultrasonic extraction for 15 minutes. The filtered liquid and the filter paper washed with methanol were used as the recovered liquid.
The concentration of the oil-soluble medicinal component (B) in the recovered liquid was calculated by comparing the recovered liquid with a standard curve using a liquid chromatograph method under the following conditions. The calculated concentration of the component (B) is converted to the concentration in 1.0 g of the composition for oral cavity to obtain the concentration of the component (B) of the recovered liquid, and the following component (B) into the gingival crevice model 4 The delivery rate was calculated.

  The delivery ratio of the oil-soluble medicinal component (B) in the recovered liquid to the gingival crevice is 10 minutes in the mobile phase of the oil-soluble medicinal component (B) in the same amount as the amount contained in the oral composition used for brushing. The oil-soluble medicinal component (B) in the filtered liquid was subjected to ultrasonic extraction, and the concentration of the oil-soluble medicinal component (B) was set to 100%. B) The delivery ratio of the oil-soluble medicinal component (B) to the gingival crevice model 4 was calculated with a concentration of 0%.

<< Conditions for liquid chromatography >>
High performance liquid chromatography (HPLC) was applied.
Apparatus: Hitachi High-Performance Liquid Chromatogram La chroma Elite
Column: LiChroCART 125-4 Supersphere100 RP-18 (e) (Merck)
Column temperature: 40 ° C
Mobile phase:
β-glycyrrhetinic acid, triclosan: 0.1 w / v% methanol containing phosphoric acid (methanol: water = 8: 2)
Tocopherol: 0.1 w / v% phosphoric acid-containing methanol (methanol: water = 98: 2)
Flow rate: 1.0 mL / min
Sample injection volume: 20 μL
Measurement wavelength:
β-glycyrrhetinic acid, triclosan: 250 nm
Tocopherol: 280 nm

Accurately take 20 μL each of the recovered solution and each standard solution of each oil-soluble medicinal component (B), conduct a liquid chromatographic test under the above conditions, and collect the collected liquid and the peak area of each measured wavelength of each oil-soluble medicinal component The content of the oil-soluble medicinal component (B) in the liquid was determined.
Oil-soluble medicinal component (B) content in recovered liquid = R × Q / P
P: Peak area of oil-soluble medicinal component (B) obtained by test of oil-soluble medicinal component (B) standard solution Q: Peak area of oil-soluble medicinal component (B) obtained by test of recovered solution R: Oil Concentration of soluble medicinal component (B) standard solution

  As shown in Table 1, the specific sugar alcohol (A) is contained in an amount of 25 to 55% by mass, the water (C) is contained in an amount of 10 to 30% by mass, and the mass ratio (A / C) is 1 or more and 5.5. In Examples 1 to 7 below, the viscosity at the time of 1.2-fold dilution is 460 dPa · s or less, and the viscosity after dilution is 16% or less with respect to that before dilution. The amount of oil-soluble medicinal component (B) adhering to No. 4 was larger than that of Comparative Examples 1 to 3, and was about twice as much. On the other hand, in Comparative Examples 1 to 3, the viscosity before dilution is the same as that of the example, but the viscosity at the time of 1.2-fold dilution is higher than that of the example, and all are 600 dPa · s or more. The viscosity after dilution was 20% or more than before, and the recovered amount of the oil-soluble medicinal component (B) adhering to the gingival crevice model 4 was also smaller than in the Examples.

4: Gingival sulcus model 11: Acrylic plate (2: Tooth model)
12: Silicone rubber (3: Gingival model)
13: Spacer 14: Running water H: Distance from the upper end of the spacer 13 to the highest position of the bent portion of the silicone rubber 12 (the upper end of the acrylic plate 11) d: Length of the acrylic plate 11 h: Height of the acrylic plate 11 : Thickness of acrylic plate 11 w2: Thickness of spacer 13

Claims (6)

The following components (A) to (D) and (F) :
(A) Sugar alcohol having a solubility in water at 20 ° C. of 30% by mass or less 25% by mass or more and 55% by mass or less (B) Oil-soluble medicinal component (C) Water 10% by mass or more and 35% by mass or less (D) Binder 0.1% to 1.5% by mass
(F) containing sorbitol <br/>, the weight ratio of the components (A) and (C) is (A / C), Ri der 5.5 greater than 1, and components (A) and component ( the weight ratio of B) (a / B) is from 220 to 3000 der Ru oral composition.   The composition for oral cavity according to claim 1, wherein the component (A) is one or more selected from mannitol, glucopyranosyl sorbitol, glucopyranosyl mannitol and reduced palatinose.   The oral composition according to claim 1 or 2, further comprising (E) 1 to 40% by mass of a sugar alcohol having a solubility in water at 20 ° C of greater than 30% by mass and 40% by mass or less.   The composition for oral cavity according to any one of claims 1 to 3, wherein the viscosity at 25 ° C is 1500 dPa · s or more and 5000 dPa · s or less.   The viscosity at 25 ° C when diluted by adding 20 parts by weight of water to 100 parts by weight of the composition is 20% or less of the viscosity at 25 ° C of the composition before dilution. The composition for oral cavity according to 1. The composition for oral cavity of any one of Claims 1-5 whose mass ratio (F / A) of a component (F) and a component (A) is 1.5 or less.