JP6783555B2 - Oral composition - Google Patents

Description

The present invention relates to an oral composition.

Conventionally, glycyrrhetinic acid, tocopherol, and the like, which can impart various pharmacological actions to oral compositions, have been widely used as medicinal ingredients. However, since these components have low solubility in water, some measures are required to ensure good storage stability. For example, in the liquid oral composition described in Patent Document 1, the dispersibility and long-term storage stability of β-glycyrrhetinic acids are enhanced by using a specific amount of allantoin or the like in combination. Further, in Patent Document 2, by using a specific polyoxyethylene hydrogenated castor oil and an anionic surfactant to prepare a dentifrice composition filled in a specific container, glycyrrhetinic acid and the like are stabilized after long-term storage. We are trying to formulate it.

On the other hand, Patent Document 3 exhibits excellent medicinal effects and sustains them by containing an active ingredient such as tocopherol and an oily ingredient, and a sucrose fatty acid ester and an anionic surfactant in specific mass ratios. Toothpaste compositions with enhanced properties are disclosed. Further, in the dentifrice composition described in Patent Document 4, by using a specific amount of a specific peppermint oil together with the above active ingredient and a surfactant, an attempt is made to develop a good flavor in addition to an excellent medicinal effect.

Japanese Unexamined Patent Publication No. 2011-168557 Japanese Unexamined Patent Publication No. 2004-250381 Japanese Unexamined Patent Publication No. 2005-289917 Japanese Unexamined Patent Publication No. 2007-45786

However, oil-soluble medicinal ingredients such as glycyrrhetinic acid and tocopherol are likely to bring about an offensive taste, and the amount used thereof is limited because of the provisions of the Pharmaceutical Affairs Law in Japan. In order to fully exert the effect of the medicinal ingredient under such circumstances, it is effective to enhance the adsorptivity to the gums and the oral mucosa, but sufficient studies have not yet been made.

Therefore, the present invention relates to an oral composition having enhanced adsorption performance of oil-soluble medicinal ingredients such as glycyrrhetinic acid and tocopherol on the gums and oral mucosa.

Therefore, as a result of various studies, the present inventors have conducted various studies and found that a specific higher alcohol, a fatty acid or a salt thereof, and a surfactant are used in a specific amount together with an oil-soluble medicinal ingredient such as glycyrrhetinic acid and water. On the other hand, the content of oil-soluble medicinal ingredients and oils other than higher alcohols and fragrances is restricted, and the content of abrasive powders containing a certain amount or more of higher alcohols with respect to fatty acids or salts thereof and containing polyvalent metals is contained. It was also found that if the composition for the oral cavity is restricted, the amount of the oil-soluble medicinal ingredient adsorbed on the gums and the oral mucosa can be effectively increased.

That is, the present invention describes the following components (A), (B), (C), (D) and (E):
(A) One or more oil-soluble medicinal ingredients selected from glycyrrhetinic acid, tocopherol, and tocopherol derivatives 0.02% by mass or more and 2.5% by mass or less,
(B) Higher alcohol having 12 or more and 22 or less carbon atoms containing cetanol (b1) and stearyl alcohol (b2) 4% by mass or more and 30% by mass or less,
(C) Nonionic surfactant selected from sorbitan fatty acid ester and polyoxyethylene sorbitan fatty acid ester,
(D) One or more fatty acids selected from stearic acid, palmitic acid, and myristic acid or salts thereof In terms of fatty acid equivalent, 0.2% by mass or more and 5% by mass or less,
(E) Contains water, and the mass ratio of the content of the oil (F) other than the components (A), (B), (C), (D) and the fragrance to the content of the component (B) (((E) F) / (B)) is less than 1, the mass ratio ((B) / (D)) of the content of the component (B) to the content of the component (D) is larger than 1, and the polyvalent metal The present invention relates to an oral composition having a content of abrasive powder (G) containing 5% by mass or less.

According to the oral composition of the present invention, an α-gel having a lamellar structure is formed, the adsorption performance is enhanced while effectively embedding the oil-soluble medicinal ingredient, and the amount of adsorption to the gums and the oral mucosa is increased. It can be effectively increased. Therefore, it is possible to sufficiently exert the medicinal effect of the oil-soluble medicinal ingredient, and also to have excellent storage stability, so that the excellent medicinal effect can be exhibited even after storage.
The oral composition of the present invention is also extremely useful as an adsorbent-promoting agent for oil-soluble medicinal ingredients on the gums and oral mucosa.

It is a figure which shows the diffracted X-ray intensity distribution by wide-angle X-ray diffraction of the α-gel formed in the dentifrice obtained in Example 1. FIG.

Hereinafter, the present invention will be described in detail.
The oral composition of the present invention contains one or more oil-soluble medicinal ingredients selected from glycyrrhetinic acid, tocopherol, and tocopherol derivative as the component (A) of 0.02% by mass or more and 2.5% by mass or less. contains. This can bring about an anti-inflammatory action, an alveolar bone resorption suppressing action, a histamine release suppressing action, a blood circulation promoting action and the like, and can also bring about a preventive and improving action such as periodontitis and periodontal disease.

Examples of glycyrrhetinic acid include α-glycyrrhetinic acid, β-glycyrrhetinic acid, glycyrrhizic acid and the like. Of these, β-glycyrrhetinic acid is preferable. Examples of tocopherol and its derivatives include tocopherol acetate, tocopherol succinate, tocopherol nicotinate and the like. Of these, tocopherol acetate is preferable, and -DL-α-tocopherol acetate is more preferable. In the present invention, one or more selected from these glycyrrhetinic acid, tocopherol, and tocopherol derivatives can be used.

The content of the component (A) is 0.02% by mass or more, preferably 0.05% by mass or more in the oral composition of the present invention from the viewpoint of effectively exerting a desired pharmacological action. Yes, more preferably 0.08% by mass or more. Further, the content of the component (A) is 2.5% by mass or less, preferably 1.5% by mass or less in the oral composition of the present invention from the viewpoint of ensuring a good flavor and the like. It is more preferably 1% by mass or less, and further preferably 0.5% by mass or less. The content of the component (A) in the oral composition of the present invention is 0.02% by mass or more and 2.5% by mass or less, preferably 0.05 to 1.5% by mass. , More preferably 0.08 to 1% by mass, and even more preferably 0.08 to 0.5% by mass or less.
Further, the component (A) preferably contains glycyrrhetinic acid, and the content of glycyrrhetinic acid is preferably 0.01% by mass or more, more preferably 0 in the oral composition of the present invention. It is 0.02% by mass or more, more preferably 0.05% by mass or more, still more preferably 0.08% by mass or more, preferably 0.5% by mass or less, and more preferably 0.3. It is mass% or less.

The oral composition of the present invention contains 4% by mass or more and 30% by mass or less of a higher alcohol having 12 or more and 22 or less carbon atoms containing cetanol (b1) and stearyl alcohol (b2) as the component (B). That is, the component (B) is a higher alcohol having 12 or more and 22 or less carbon atoms, which contains cetanol of the component (b1) and stearyl alcohol of the component (b2) as essential components. By containing such a component (B), an α-gel having a structure in which lamellar layers are overlapped is formed together with the above component (A) and the component (C) described later, and the component (A) is satisfactorily embedded. At the same time, the adsorption performance on the gums and oral mucosa can be effectively enhanced.

The higher alcohol of the component (B) contains cetanol of the component (b1) and stearyl alcohol of the component (b2) from the viewpoint of maintaining an appropriate viscosity as an oral composition while satisfactorily forming an α-gel. A mass ratio of the total amount of the content of the component (b1) and the content of the component (b2) to the content of the component (B), which is a higher alcohol containing 12 or more and 22 or less carbon atoms (((). (B1) + (b2)) / (B)) is preferably 0.85 or more, more preferably 0.9 or more, still more preferably 0.92 or more, and 1 or less.

The component (B) other than the component (b1) and the component (b2) is preferably one or more selected from lauryl alcohol, myristyl alcohol, and behenyl alcohol.

The mass ratio ((b1) / (b2)) of the content of the component (b1) to the content of the component (b2) provides good storage stability as an oral composition while forming an α-gel well. From the viewpoint of improvement, it is preferably 0.5 or more, more preferably 0.7 or more, preferably 5 or less, more preferably 3 or less, still more preferably 2 or less, and even more preferably. Is 1.7 or less.
Lauryl alcohol and myristyl alcohol, which are higher alcohols having 12 or more and 22 or less carbon atoms other than the component (b1) and the component (b2), are the sum of the lauryl alcohol content and the myristyl alcohol content from the viewpoint of taste. The mass ratio of the amount to the content of the component (B) ((lauryl alcohol + myristyl alcohol) / (B)) is preferably 0.05 or less, more preferably 0.03 or less, still more preferable. Is 0.01 or less.

Behenyl alcohol, which is a higher alcohol having 12 or more and 22 or less carbon atoms other than the component (b1) and the component (b2), has the content of the behenyl alcohol and the component (B) from the viewpoint of suppressing the precipitation and separation of the component (B). The mass ratio to the content (behenyl alcohol / (B)) is preferably 0.1 or less, more preferably 0.05 or less.

From the viewpoint of storage stability, the higher alcohol having 10 or less carbon atoms has a mass ratio of the content of the higher alcohol having 10 or less carbon atoms to the content of the component (B) (higher alcohol having 10 or less carbon atoms / ( B)) is preferably 0.1 or less, more preferably 0.01 or less, still more preferably 0.005 or less, or the oral composition of the present invention has a higher carbon number of 10 or less. It is even more preferable that it does not contain alcohol.
Further, the higher alcohol having 24 or more carbon atoms has a mass ratio of the content of the higher alcohol having 24 or more carbon atoms to the content of the component (B) from the viewpoint of storage stability (higher alcohol having 24 or more carbon atoms / ( B)) is preferably 0.1 or less, more preferably 0.01 or less, still more preferably 0.005 or less, or the oral composition of the present invention has a higher carbon number of 24 or more. It is even more preferable that it does not contain alcohol.

The content of the component (B) is 4% by mass or more, preferably 4.5% by mass or more, more preferably, in the oral composition of the present invention, from the viewpoint of forming an α-gel satisfactorily. It is preferably 5% by mass or more. Further, the content of the component (B) is 30% by mass or less in the oral composition of the present invention from the viewpoint of making the viscosity appropriate and ensuring the dispersibility of each component in the composition. It is preferably 25% by mass or less, more preferably 20% by mass or less, and further preferably 18% by mass or less. The content of the component (B) in the oral composition of the present invention is 4% by mass or more and 30% by mass or less, preferably 4.5 to 25% by mass, and more preferably 4. It is 5 to 20% by mass, more preferably 5 to 18% by mass.

The mass ratio ((A) / (B)) of the content of the component (A) to the content of the component (B) is determined by the α-gel formed while ensuring the pharmacological action of the component (A). From the viewpoint of satisfactorily embedding (A), it is preferably 0.002 or more, more preferably 0.004 or more, and even more preferably 0.005 or more. Further, the mass ratio ((A) / (B)) of the content of the component (A) to the content of the component (B) is such that the dispersibility of each component is ensured and the gum and oral cavity of the component (A) are secured. From the viewpoint of enhancing the adsorption performance to the inner mucosa, it is preferably 0.2 or less, more preferably 0.15 or less, further preferably 0.1 or less, and containing glycyrrhetinic acid as the component (A). The mass ratio of the content of glycyrrhetinic acid to the content of component (B) (glycyrrhetinic acid / (B)) is preferably 0.1 or less, more preferably 0.05 or less. The mass ratio ((A) / (B)) of the content of the component (A) to the content of the component (B) is preferably 0.002 to 0.2, more preferably 0.004 to 0.2. It is 0.15, more preferably 0.005 to 0.1, and when glycyrrhetinic acid is contained as the component (A), the mass ratio of the content of glycyrrhetinic acid to the content of the component (B) (glycyrrhetinic acid). / (B)) is preferably 0.002 to 0.1, more preferably 0.004 to 0.1, and even more preferably 0.005 to 0.05.

The oral composition of the present invention contains, as the component (C), a nonionic surfactant selected from a sorbitan fatty acid ester and a polyoxyethylene sorbitan fatty acid ester. In this way, by containing the nonionic surfactant of the component (C), the component (B) is further ensured while ensuring the stability of the component (A) in combination with the fatty acid of the component (D) described later or a salt thereof. ) And α-gel can be formed to satisfactorily embed the component (A), and the adsorption performance to the gums and the oral mucosa can be effectively enhanced.

The sorbitan fatty acid ester of the component (C) is preferably derived from a fatty acid having 10 or more carbon atoms, and more preferably 12 or more carbon atoms, from the viewpoint of the adsorption performance of the component (A) on the gums and oral mucosa. It is derived from the fatty acid of the above, preferably derived from a fatty acid having 20 or less carbon atoms, and more preferably one or more selected from those derived from a fatty acid having 18 or less carbon atoms. Specifically, for example, sorbitan monocaprate, sorbitan monoundecylate, sorbitan monolaurate, sorbitan monotridecylate, sorbitan monomyristate, sorbitan monopalmitate, sorbitan monooleate, sorbitan trioleate, sorbitan tetraoleate, sesqui One or more selected from sorbitan oleate, sorbitan monostearate, sorbitan tristearate and the like can be mentioned. Among them, one or more selected from sorbitan monooleate, sorbitan sesquioleate, and sorbitan monostearate are preferable.

The polyoxyethylene sorbitan fatty acid ester of the component (C) is preferably derived from a fatty acid having 6 or more carbon atoms, and more preferably carbon, from the viewpoint of the adsorption performance of the component (A) on the gums and the oral mucosa. One or more selected from those derived from fatty acids having a number of 12 or more, preferably those derived from fatty acids having 22 or less carbon atoms, and more preferably those derived from fatty acids having 20 or less carbon atoms can be mentioned. From the same viewpoint, the average number of moles of ethyleneoxy groups added to the polyoxyethylene sorbitan fatty acid ester is preferably 5 to 40 mol, more preferably 10 to 25 mol, and further preferably 10 to 20 mol. Is. Examples of such polyoxyethylene sorbitan fatty acid esters include polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monomyristate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene monooleate. One kind or two or more kinds selected from sorbitan and the like can be mentioned. Among them, one or two selected from polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate from the viewpoint of enhancing low temperature stability while exhibiting excellent foaming properties. More than seeds are preferred.

The content of the component (C), in combination with the fatty acid of the component (D) described later or a salt thereof, further forms an α-gel together with the component (B) while ensuring the stability of the component (A), and the component ( From the viewpoint of satisfactorily embedding A) and effectively enhancing the adsorption performance on the gums and oral mucosa, the content in the oral composition of the present invention is preferably 1% by mass or more, more preferably 1. It is 5% by mass or more, more preferably 2% by mass or more, and preferably 10% by mass or less from the viewpoint of ensuring the storage stability of the composition and from the viewpoint of the balance with an appropriate viscosity and flavor. It is more preferably 7% by mass or less, and further preferably 5% by mass or less.

In the oral composition of the present invention, the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) satisfactorily forms an α-gel. From the viewpoint of enhancing the adsorption performance of (A) on the gums and oral mucosa, it is preferably 1 or more, more preferably 1.2 or more, still more preferably 1.4 or more, still more preferably 2. That is all. Further, the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is the storage stability from the viewpoint of maintaining an appropriate viscosity as an oral composition. From the viewpoint of the above, it is preferably 15 or less, more preferably 10 or less, still more preferably 8 or less, and even more preferably 5 or less. The mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is preferably 1 to 15, and more preferably 1.2 to 10. Yes, more preferably 1.4 to 8, and even more preferably 2 to 5.

The oral composition of the present invention contains one or more fatty acids selected from stearic acid, palmitic acid, and myristic acid or salts thereof as the component (D) in an amount of 0.2% by mass or more in terms of fatty acid. Contains less than% by mass. In this way, by using the fatty acid of the component (D) or a salt thereof at a specific content, the stability of the component (A) is ensured in combination with the component (C), and further together with the component (B). The α-gel can be formed to satisfactorily embed the component (A), and the adsorption performance to the gums and the oral mucosa can be effectively enhanced. In addition, it can exhibit high storage stability and maintain a good flavor.

Examples of the salt constituting the component (D) include alkali metals selected from sodium and potassium, and among them, sodium is preferable from the viewpoint of storage stability of the composition. The component (D) is one or two selected from stearic acid and palmitic acid from the viewpoint of the adsorption performance of the component (A) on the gums and the oral mucosa and the viewpoint of ensuring a good flavor. It preferably contains a fatty acid or a salt thereof, and preferably contains at least stearic acid or a salt thereof.

The content of the component (D), in combination with the above component (C), ensures the stability of the component (A) and further forms an α-gel together with the component (B) to satisfactorily enclose the component (A). From the viewpoint of burying and effectively enhancing the adsorption performance to the gums and oral mucosa, and from the viewpoint of imparting an appropriate viscosity, the amount of fatty acid in the oral composition of the present invention is 0.2% by mass or more. It is preferably 0.4% by mass or more, more preferably 0.8% by mass or more, and further preferably 1.5% by mass or more. The content of the component (D) is the oral cavity of the present invention from the viewpoint of ensuring the storage stability of the composition, the appropriate viscosity, the balance with the flavor, and the reduction of harmfulness to the oral mucosa. In the composition for use, the amount in terms of fatty acid is 5% by mass or less, more preferably 4.5% by mass or less, still more preferably 4% by mass or less, still more preferably 3% by mass or less. is there.

The total amount of the content of the component (C) and the converted amount of the fatty acid of the component (D), in combination with these components, further forms an α-gel together with the component (B) while ensuring the stability of the component (A). From the viewpoint of satisfactorily embedding the component (A) and effectively enhancing the adsorption performance to the gums and the oral mucosa, the content is preferably 1.5% by mass or more in the oral composition of the present invention. , More preferably 2% by mass or more, still more preferably 3% by mass or more, and preferably 12% by mass from the viewpoint of ensuring the storage stability of the composition and from the viewpoint of balancing with an appropriate viscosity and flavor. It is less than or equal to, more preferably 8% by mass or less, still more preferably 7% by mass or less.

In the oral composition of the present invention, the mass ratio ((B) / (D)) of the content of the component (B) to the content of the component (D) satisfactorily forms an α-gel and the component ( From the viewpoint of enhancing the adsorption performance of A) on the gums and oral mucosa, it is larger than 1, preferably 1.5 or more, more preferably 2 or more, still more preferably 2.5 or more, and even more. It is preferably 3 or more. Further, the mass ratio ((B) / (D)) of the content of the component (B) to the content of the component (D) ensures storage stability while maintaining an appropriate viscosity as an oral composition. From the viewpoint of providing a good feeling of use, it is preferably 25 or less, more preferably 20 or less, still more preferably 18 or less, and even more preferably 12 or less. The mass ratio ((B) / (D)) of the content of the component (B) to the content of the component (D) is larger than 1, preferably 1.5 to 25, and more preferably 2. It is ~ 20, more preferably 2.5-18, and even more preferably 3-12.

The oral composition of the present invention contains the component (E) water. The water of the component (E) in the present invention is not only purified water or the like blended in the oral composition, but also, for example, a 70% sorbitol solution (aqueous solution) or a 48% potassium hydroxide solution (aqueous solution) used for prescribing. As described above, it means the total water contained in the oral composition, which also includes the water contained in each of the blended components. By containing the water of the component (E), each α-gel formed is well retained in the composition while ensuring an appropriate viscosity and good shape retention as an oral composition. The component can be well dispersed or dissolved, and the good feeling of use and the gum of the component (A) can improve the adsorptivity to the oral mucosa. The content of the component (E) is preferably 50% by mass or more, more preferably 55% by mass or more, still more preferably 60% by mass or more, and preferably 60% by mass or more in the oral composition of the present invention. It is 95% by mass or less, more preferably 92% by mass or less, and further preferably 80% by mass or less. The content of the component (E) is preferably 50 to 95% by mass, more preferably 55 to 92% by mass, still more preferably 60 to 80% by mass in the oral composition of the present invention. Is.

The content of the component (E) of the oral composition of the present invention, that is, the water content, can be calculated from the blended water content and the water content in the blended component. For example, Karl Fischer titer Can be measured with. As the Karl Fischer titer, for example, a trace moisture measuring device (Hiranuma Sangyo) can be used. In this device, 5 g of the oral composition is taken, suspended in 25 g of anhydrous methanol, and 0.02 g of this suspension can be separated to measure the water content.

In the oral composition of the present invention, the mass ratio of the content of the oil agent (F) other than the above components (A), (B), (C), (D) and the fragrance to the content of the component (B). ((F) / (B)) is less than 1. By limiting the content of the oil agent (F) with respect to the content of the component (B) in the oral composition of the present invention, the range of the surfactant that can be blended in the oral composition is limited. The storage stability of the composition can be improved, the inhibition of α-gel formation can be effectively suppressed, and the flavor can be improved. Examples of such component (F) include hydrocarbon oils such as liquid paraffin, vaseline, mineral oil, light liquid paraffin, paraffin wax, selecin, microcrystallin wax, carnauba wax, beeswax, squalane, and squalane; isopropyl myristate and palmitin. Ester oils such as isopropyl acid, propyl adipate, diethyl sebacate, glycerin fatty acid ester; triglyceride and olive oil containing it, rapeseed oil, shea butter, vegetable oil of rice bran oil; silicone oil; methyl paraoxybenzoate, ethyl paraoxybenzoate, etc. Preservatives; oil-soluble bactericides and the like.

The mass ratio ((F) / (B)) of the content of the component (F) to the content of the component (B) is less than 1, preferably 0.5 or less, and more preferably 0. It is 0.3 or less.

The content of the component (F) in the oral composition of the present invention is preferably 5% by mass or less, more preferably 2% by mass or less, still more preferably 1% by mass or less. Even more preferably, it is 0.5% by mass or less. When the component (F) is a liquid oil at 25 ° C., the content of the component (F) is preferably 5% by mass or less in the oral composition of the present invention, which is more preferable. Is 3% by mass or less, more preferably 2% by mass or less.

The oral composition of the present invention contains 5% by mass or less of the abrasive (G) (abrasive powder) containing a polyvalent metal. As a result, the α-gel formed by the above components can be suppressed from collapsing, and the polyvalent metal of the component (D) and the component (G) can be prevented from binding to precipitate a metal salt. It is also possible to ensure excellent adsorption performance of the component (A) on the gums or the oral mucosa. Examples of the polyvalent metal include aluminum, calcium, zirconium, iron, copper, zinc, and manganese, and the component (G) containing these includes a water-insoluble calcium compound such as calcium carbonate, calcium hydrogen phosphate, and insoluble metallin. Examples thereof include potassium acid, aluminum silicate, zirconium silicate, aluminum oxide, aluminum hydroxide and zinc oxide. The content of the component (G) in the oral composition of the present invention is 5% by mass or less, more preferably 3% by mass or less, still more preferably 1% by mass or less, or unavoidable. It is preferable that the oral composition of the present invention does not contain the component (G) except when it is mixed with.
Further, from the same viewpoint, the oral composition of the present invention has a polyvalent metal content selected from strontium, magnesium, aluminum, calcium, zirconium, iron, copper, zinc, and manganese in terms of metal atom equivalent. In the oral composition of the present invention, it is preferably 2% by mass or less, more preferably 1% by mass or less, still more preferably 0.5% by mass or less, still more preferably 0.1% by mass. % Or less.

The oral composition of the present invention maintains an appropriate viscosity and shape retention as an oral composition by the formed α-gel, and has excellent adsorption performance of the component (A) to the gingiva or the oral mucosa. From the viewpoint of ensuring, it is preferable to limit the content of the cellulosic binder. Specific examples of the cellulosic binder include one or two selected from hydroxyalkyl cellulose (for example, hydroxyethyl cellulose and hydrokipropyl cellulose) and sodium carboxymethyl cellulose. The content of the cellulosic binder in the oral composition of the present invention is preferably 0.3% by mass or less, more preferably 0.25% by mass or less, still more preferably 0.2. The oral composition of the present invention preferably does not contain a cellulosic binder, except in the case of mass% or less, more preferably 0.1% by mass or less, or unavoidably mixed.

The oral composition of the present invention can contain a binder other than the cellulosic binder. Blotting agents other than cellulose-based binders include sodium alginate, carrageenan, xanthan gum, sodium polyacrylate, pectin, agar, tragant gum, gum arabic, guar gum, karaya gum, locust bean gum, gela gum, tamalido gum, and psyllium seed gum. One or more kinds selected from the above, and one kind or two kinds of binders selected from carrageenan and xanthan gum are preferable. The content of the binder other than these cellulosic binders is preferably 0.5% by mass or less, more preferably 0.5% by mass or less, from the viewpoint of improving the adsorptivity of the component (A) to the gums or the oral mucosa. Is 0.3% by mass or less.

The oral composition of the present invention preferably further contains a thickener from the viewpoint of enhancing the viscoelasticity of the binder. As the thickener, one or two kinds selected from thickening silica having an oil absorption of 180 to 350 mL / 100 g and fatty acid dextrin are preferable. The content of the thickening silica is preferably 5% by mass or less in the oral composition of the present invention from the viewpoint of improving the adsorptivity of the component (A) to the gingiva or the oral mucosa, which is more preferable. Is 3% by mass or less. The content of the fatty acid dextrin is preferably 3% by mass in the oral composition of the present invention from the viewpoint of improving the adsorptivity of the component (A) to the gingiva or the oral mucosa and the balance with the flavor. It is less than or equal to, more preferably 1.5% by mass or less. As the fatty acid dextrin, dextrin palmitate is preferable.

The oral composition of the present invention can contain abrasive silica having an oil absorption of 50 to 150 mL / 100 g. The abrasive silica is an abrasive other than the above-mentioned abrasive containing a polyvalent metal (abrasive powder). The content of the abrasive silica is preferably 7% by mass or less, more preferably 7% by mass or less, in the oral composition of the present invention from the viewpoint of improving the adsorptivity of the component (A) to the gingiva or the oral mucosa. It is 5% by mass or less, more preferably 3% by mass or less, even more preferably 2% by mass or less, still more preferably 1% by mass or less, or the oral composition of the present invention absorbs oil. It may not contain abrasive silica in an amount of 50 to 150 mL / 100 g.
The amount of oil absorbed indicates the amount of oil that silica can support, and the measuring method is specified by the amount of oil absorbed in the boiled sardine by the method of JIS K5101-13-2 (established in 2004). Means the value.

The oral composition of the present invention effectively suppresses the disintegration of the α-gel formed by the above components, and maintains the excellent adsorption performance of the component (A) on the gingiva or the oral mucosa. It is preferable to limit the content of ethanol from the viewpoint of ensuring an appropriate viscosity and suppressing irritation. Specifically, the content of ethanol in the oral composition of the present invention is preferably 8% by mass or less, more preferably 5% by mass or less, still more preferably 2% by mass or less. Alternatively, the oral composition of the present invention preferably does not contain ethanol.

From the viewpoint of flavor, the oral composition of the present invention preferably further contains a sugar alcohol. The content of the sugar alcohol is preferably 30% by mass or less, more preferably 20% by mass or less, still more preferably 20% by mass or less, from the viewpoint of improving the adsorption performance of the component (A) on the gums or the oral mucosa. It is 15% by mass or less, preferably 1% by mass or more, more preferably 2% by mass or more, and further preferably 5% by mass or more from the viewpoint of flavor. As the sugar alcohol, one or more selected from sorbitol, xylitol, erythritol, reduced palatinose, and mannitol are preferable, and sorbitol, from the viewpoint of high solubility in water and a smooth feel of the composition, And one or two selected from xylitol are more preferable, and at least sorbitol is preferably contained as the sugar alcohol.

The oral composition of the present invention may further contain a nonionic surfactant selected from polyoxyethylene hydrogenated castor oil, sucrose fatty acid ester, and polyglycerin fatty acid ester as a nonionic surfactant other than the above component (C). Good. The average number of moles of ethyleneoxy groups added in such polyoxyethylene-hardened castor oil is from the viewpoint of ensuring the storage stability of the composition while maintaining good adsorption performance of the component (A) on the gums and oral mucosa. , It is preferably 20 to 100 mol, more preferably 40 to 80 mol. The content of the polyoxyethylene hydrogenated castor oil is preferably 0.5 in the oral composition of the present invention from the viewpoint of maintaining good adsorption of the component (A) to the gums or the oral mucosa. By mass or less, more preferably 0.3% by mass or less, still more preferably 0.1% by mass or less, even more preferably 0.01% by mass or less, or the oral composition of the present invention The product may be one that does not contain polyoxyethylene hydrogenated castor oil.

Examples of the polyglycerin fatty acid ester include those in which 1 to 4 fatty acids having 8 to 24 carbon atoms are ester-bonded to polyglycerin in which 2 to 20 glycerins are condensed. The fatty acid portion constituting the polyglycerin fatty acid ester has 12 to 12 carbon atoms from the viewpoint of ensuring the storage stability of the composition while maintaining good adsorption performance of the component (A) on the gums and oral mucosa. Those derived from 20 fatty acids are preferable, those derived from fatty acids having 12 to 18 carbon atoms are more preferable, those derived from fatty acids having 12 to 14 carbon atoms are more preferable, and the polyglycerin fatty acid ester is composed of these fatty acid portions. It is preferably a monoester. From the same viewpoint, the average degree of condensation of glycerin in the polyglycerin fatty acid ester is preferably 2 to 20, and more preferably 5 to 12.

Examples of the sucrose fatty acid ester include sucrose fatty acid esters composed of fatty acid portions derived from fatty acids having 6 to 20 carbon atoms. Among them, the fatty acid portion constituting the sucrose fatty acid ester is good from the viewpoint of ensuring the storage stability of the composition while maintaining good adsorption performance of the component (A) on the gums and oral mucosa. From the viewpoint of imparting a good feeling of use, those derived from fatty acids having 10 to 18 carbon atoms are preferable, and those derived from fatty acids having 12 to 14 carbon atoms are more preferable.

The content of the nonionic surfactant selected from these polyoxyethylene hydrogenated castor oil, sucrose fatty acid ester, and polyglycerin fatty acid ester is from the viewpoint of improving the adsorption performance of the component (A) on the gums and oral mucosa, and From the viewpoint of ensuring a balance between the adsorption performance of the component (A) on the gums and the oral mucosa and the flavor, it is preferably 0.5% by mass or less, more preferably 0 in the oral composition of the present invention. It is .25% by mass or less, more preferably 0.2% by mass or less, still more preferably 0.1% by mass or less, and even more preferably 0.05% by mass or less.

The oral composition of the present invention may contain an anionic surfactant selected from sodium alkyl sulfate, acyl methyl taurine salt, and acyl sarcosine salt as a surfactant other than the nonionic surfactant. Examples of such anionic surfactants include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate; N-lauroyl sarcosine, N-myristoyl sarcosine, N-palmitoyl sarcosine, N-stearoyl sarcosine, N-isostearoyl sarcosine, N-ole. Sodium salt or potassium salt of acyl sarcosine such as oil sarcosine; one selected from sodium salt or potassium salt of acyl methyl taurine such as capryl methyl taurine, lauryl methyl taurine, myristyl methyl taurine, palmityl methyl taurine, stearyl methyl taurine, etc. Two or more types can be mentioned. Among them, one or more selected from sodium lauryl sulfate, N-lauroyl sarcosine salt, N-myristoyl sarcosine salt, lauryl methyl taurine salt, and myristyl methyl taurine salt are preferable, and sodium lauryl sulfate is more preferable.

The content of the anionic surfactant selected from these sodium alkylsulfate, acylmethyltaurine salt, and acylsarcosine salt is in the oral composition of the present invention from the viewpoint of harmfulness to the gums and oral mucosa and flavor. In addition, 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 even more preferably 0.7% by mass or less.

The oral composition of the present invention preferably limits the content of a cationic surfactant other than the cationic bactericide from the viewpoint of preventing harmful effects on the oral mucosa. The content of the cationic surfactant other than the cationic bactericide is preferably 0.1% by mass or less, more preferably 0.05% by mass or less in the oral composition of the present invention. More preferably, it is 0.01% by mass or less, or the oral composition of the present invention preferably does not contain a cationic surfactant other than a cationic bactericide. Examples of the cationic bactericide include one or more selected from a quaternary ammonium compound and a biguanide compound. Examples of the quaternary ammonium compound include cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, stearyldimethylammonium chloride, stearyltrimethylammonium chloride, cetyltrimethylammonium chloride, methylbenzethonium chloride, lauryltrimethylammonium chloride, and lauroylcolamino chloride. Examples thereof include formylmethylpyridinium. Examples of the biguanide compound include chlorhexidine and a salt thereof, and examples of such salts include chlorhexidine gluconate and chlorhexidine hydrochloride.

The oral composition of the present invention may contain polyhydric alcohols, sweeteners, wetting agents, preservatives, fluorides, enzymes, pigments and the like in addition to the above components as long as the effects of the present invention are not impaired. ..

The viscosity of the oral composition of the present invention at 25 ° C. is from the viewpoint of maintaining an appropriate viscosity and exhibiting excellent adsorption performance of the component (A) to the gingiva or the oral mucosa, and good shape retention. From the viewpoint of ensuring a feeling of use, it is preferably 5000 dPa · s or less, more preferably 4000 dPa · s or less, further preferably 3800 dPa · s or less, preferably 1000 dPa · s or more, and more preferably 1100 dPa · s. It is s or more, more preferably 1200 dPa · s or more, and even more preferably 1400 dPa · s or more. The viscosity of the oral composition of the present invention at 25 ° C. is preferably 1000 dPa · s or more and 5000 dPa · s or less, more preferably 1100 to 4000 dPa · s, and further preferably 1200 to 3800 dPa · s. , Even more preferably 1400 to 3800 dPa · s. Such viscosity is determined by packing in a container for measuring viscosity, storing in a thermostat at 25 ° C for 24 hours, and then using a helipas type viscometer (VISCOMETER TVB-10 Toki Sangyo) in an environment of 25 ° C to rotate the rotor T-. It can be measured under the conditions of C, rotation speed 2.5 rpm, and 1 minute.

Examples of the form of the oral composition of the present invention include dentifrices, coating agents, mouthwashes, liquid dentifrices and the like. Among them, liquid dentifrices and dentifrices are preferable from the viewpoint of sufficiently spreading the oral composition of the present invention to the gums or the oral mucosa and effectively adsorbing the component (A). The oral composition of the present invention is preferably applied into the oral cavity, and after application, water is contained in the oral cavity and gargled. Even if water is contained in the oral cavity after application, the component (A) can be effectively adsorbed on the gums or the oral mucosa. The method of application to the oral cavity may be application, brushing with a toothbrush, or gargle, and application or brushing with a toothbrush is preferable.

The method for producing an oral composition of the present invention includes a step of mixing a mixed solution containing the components (B) to (D) at a temperature equal to or higher than the melting point of the component (B) and 90 ° C. or lower. Specifically, from the viewpoint of effectively enhancing the adsorption performance of the component (A) on the gingiva or the oral mucosa, a production method including the following step (X) is preferable, or the gingiva or the component (A) From the viewpoint of effectively enhancing the adsorption performance to the oral mucosa and the simplification of the manufacturing equipment, the manufacturing method including the following step (Y) is preferable.

The production method including the step (X) was obtained after mixing the mixed solution 1-1 containing the components (B) to the component (D) at a temperature of 90 ° C. or higher than the melting point of the component (B). This is a production method comprising a step (X) of adding and mixing the component (E) to the mixed solution 1-1 to obtain the mixed solution 1-2. In such a production method, the component (A) is preferably contained in the mixed solution 1-1 and mixed, but may be added and mixed in the mixed solution 1-2 obtained after the step (X). It may be added and mixed together with the component (E). Further, it is preferable to include a part of the component (E) in the mixed solution 1-1 and mix them. In this case, it is preferable that the component (A) is added to the remaining component (E) and added to and mixed with the mixed solution 1-1 to obtain the mixed solution 1-2. The temperature at which the mixed solution 1-1 is mixed and the temperature at the step of obtaining the mixed solution 1-2 may be a temperature equal to or higher than the melting point of the component (B) and 90 ° C. or lower, which is the highest among the components (B). It is a temperature of a high melting point or higher, more preferably a temperature of the melting point of the component (B) or higher and 85 ° C. or lower, and further preferably a temperature of 80 ° C. or higher and 85 ° C. or lower. Further, the mixing order of the components (A) to (D) is not particularly limited. The temperature above the melting point of the component (B) is preferably 65 ° C. or higher, more preferably 75 ° C. or higher, and even more preferably 80 ° C. or higher.

The manufacturing method including the step (Y) is a manufacturing method including the step (Y) of mixing the mixed liquid 2 containing the components (B) to (E). In such a production method, the component (A) is preferably contained in the mixed solution 2 and mixed, but the component (A) may be added to the mixed solution 2 obtained after obtaining the step (Y) and mixed, or the component (A) may be mixed. It may be added in advance to E).

Since the oral composition of the present invention can effectively adsorb the component (A) to the gingiva or the oral mucosa, it is also very useful as an adsorption accelerator for the component (A) to the gingiva or the oral mucosa. Is.

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

[Examples 1 to 9, Comparative Examples 1 to 5]
Each oral composition was produced according to the formulation shown in Table 1. Specifically, the component (A), the component (B), the component (C), and the component (D), and if necessary, the component (F) are heated to 80 ° C. (80 to 82 ° C.) and mixed. And stirred for about 10 minutes. Then, the component (E) was added and mixed, and then the other components were added and mixed for 10 minutes to obtain an oral composition.
Using each of the obtained oral compositions, the viscosity and the amount of β-glycyrrhetinic acid adsorbed were measured according to the following methods, and the formation of α-gel was observed.
The results are shown in Table 1.

<< Observation of α-gel formation >>
Using each of the obtained oral compositions, it was confirmed whether or not α-gel was formed by wide-angle X-ray diffraction. Specifically, the presence or absence of α-gel formation was determined by whether or not one sharp diffraction peak appeared in the vicinity of Bragg angle = 21 to 22 ° in wide-angle X-ray diffraction.
Specifically, as shown in FIG. 1, one sharp diffraction peak was observed near the Bragg angle = 21 to 23 °, and it was confirmed that the composition was formed with an α-gel structure. The case was evaluated as "yes", and the case where such a peak was not confirmed was evaluated as "none". FIG. 1 shows the diffraction X-ray intensity distribution of the α-gel formed in the dentifrice of Example 1 by wide-angle X-ray diffraction, while Comparative Example 2 in which separation was confirmed was confirmed by wide-angle X-ray diffraction. Did not do.

<< Evaluation of storage stability at 50 ° C >>
Each of the obtained oral compositions was stored at 50 ° C. for 1 month (30 days), and then the appearance change was observed with the naked eye. When separation was not confirmed, it was "good" and separation was observed. The case was evaluated as "separation".

<< Measurement of adsorption amount of β-glycyrrhetinic acid >>
5.0 g of each oral composition after preparation and storage at room temperature (25 ° C.) for 1 month is placed inside a glass cylinder having a diameter of 25 mm of a silicone sheet (30 mm × 30 mm, thickness 0.1 mm). After adding and contacting for 30 seconds, 5 mL of purified water was added and pipetteed with purified water, and then 5 mL of purified water was added again and pipetteed with purified water. Further, it was washed 10 times with 5 mL of purified water. Then, the silicone sheet is immersed in 2 mL of methanol, shaken with a vortex mixer (EYELA CUTE MIXER CM-1000, manufactured by Tokyo Rikaki) for 5 minutes, and then ultrasonically cleaned (ASU CLEANER ASU-3 (manufactured by AS ONE)). Was treated for 30 minutes. The amount of β-glycyrrhetinic acid in methanol was measured by HPLC (High Performance Liquid Chromatography) under the following conditions.

The standard solution of glycyrrhetinic acid was prepared by adding 0.1 g of β-glycyrrhetinic acid to a mobile phase (0.1 w / v% phosphoric acid-containing methanol (methanol: water = 8: 2)) to make 100 mL, and further using the mobile phase. The one diluted 200 times by volume was used. The content of β-glycyrrhetinic acid is determined by the peak area (X) of the absorbance of β-glycyrrhetinic acid measured by HPLC, the ratio (X / Y) to the peak area (Y) of the standard solution, and β-glycyrrhetin in the standard solution. ((Z) × (X) / (Y)) was determined by the product of the acid concentration (Z).

(HPLC measurement conditions)
Equipment: SHIMADZU Prominence (LC-20AD) (Shimadzu Corporation)
Column: LiChrCART 125-4.0 Superspher100 RP-18 (e) (Kanto Chemical Co., Inc.)
Column temperature: 40 ° C
Mobile phase: Methanol containing 0.1 w / v% phosphoric acid (methanol: water = 8: 2)
Flow rate: 1.0 mL / min
Sample injection volume: 20 μL
Measurement wavelength: 250 nm

《Evaluation of flavor》
Approximately 1 g of each oral composition obtained is brushed with a toothbrush (Deep Clean Ultra Compact Ordinary, manufactured by Kao Corporation) for 2 minutes, then spit out, rinse the oral cavity with water, and evaluate the flavor according to the following criteria. Was done.
3: There was no oily odor and the flavor was good.
2: A slight oily odor was felt, and a slight offensive taste was also felt.
1: An oily odor was felt, and a strange taste was also felt.
0: A strong taste was felt.

《Measurement of viscosity》
Each of the obtained oral compositions was packed in a container for measuring viscosity and stored in an incubator at 25 ° C. for 24 hours before measurement. The viscosity was measured at 25 ° C. using a helipas type viscometer (VISCOMETER TVB-10 Toki Sangyo) under the conditions of rotor TC, rotation speed 2.5 rpm, and 1 minute.

<< Evaluation of manufacturability >>
It was confirmed whether or not a problem such as separation of some components occurred during the production of each oral composition according to the above method.
When there was no particular problem, it was evaluated as "no problem", and when separation was observed, it was evaluated as "separation". In addition, the case where the composition could not be produced due to an extremely high viscosity of the composition during stirring was evaluated as "unmanufacturable".

From the results in Table 1, in the dentifrice of the example, α-gel was effectively formed, and the adsorption performance of the component (A) on the gingiva or the oral mucosa could be effectively enhanced even after storage. Understand. In addition, it is found that it retains a good flavor, exhibits excellent storage stability even when exposed to a high temperature environment, and is also excellent in manufacturability.

Claims (6)

The following components (A), (B), (C), (D) and (E):
(A) Glycyrrhetinic acid 0.02 % by mass or more and 0.5 % by mass or less,
(B) Cetanol (b1) and higher alcohol which is stearyl alcohol (b2) 4% by mass or more and 30% by mass or less,
(C) Nonionic surfactant selected from sorbitan fatty acid ester and polyoxyethylene sorbitan fatty acid ester,
(D) One or more fatty acids selected from stearic acid, palmitic acid, and myristic acid or salts thereof In terms of fatty acid equivalent, 0.2% by mass or more and 5% by mass or less,
(E) Contains water, and the mass ratio of the content of the oil (F) other than the components (A), (B), (C), (D) and the fragrance to the content of the component (B) (((E) F) / (B)) is less than 1, and the mass ratio ((B) / (D)) of the content of the component (B) to the content of the component (D) is 2 or more and 25 or less , and Ri der content of 5 mass% of abrasive powder (G) containing a polyvalent metal, the oral composition content of Ru der than 0.3 wt% cellulosic binder. The oral composition according to claim 1, wherein the mass ratio ((B) / (C)) of the content of the component (B) to the content of the component (C) is 1 or more and 20 or less. The oral composition according to claim 1 or 2 , wherein the cellulosic binder is one or two selected from hydroxyalkyl cellulose and sodium carboxymethyl cellulose. The oral composition according to any one of claims 1 to 3 , wherein the content of abrasive silica is 7% by mass or less. The oral composition according to any one of claims 1 to 4 , wherein the content of the component (E) is 50% by mass or more and 95% by mass or less. The oral composition according to any one of claims 1 to 5 , wherein the content of the polyoxyethylene cured castor oil is 0.5% by mass or less.