JP7167713B2 - oral composition - Google Patents

Description

TECHNICAL FIELD The present invention relates to an oral composition that contains a polyvalent metal salt, has an excellent astringent feeling and persistence thereof, suppresses the metallic taste derived from polyvalent metal ions, and has a good feeling in use.

Oral compositions such as dentifrices contain compounds containing polyvalent metal ions such as zinc, copper, tin, strontium and aluminum. These polyvalent metal ions have pharmacological effects such as sterilizing bacteria that lead to caries, periodontal disease, and bad breath, and provide astringent effects due to the denaturation effect of oral mucosal proteins of metal ions. It is known to have significant effects on the surface.

However, since these polyvalent metal ions have a strong metallic taste such as bitterness and astringency and adversely affect the taste of the formulation, a technique for masking the metallic taste has been desired in order to improve the feeling of use. For example, in Patent Document 1 (Japanese Patent Application Laid-Open No. 2010-235557), an oral composition has two perfume-containing portions having different scent notes, and a specific perfume component is blended therein to obtain a polyvalent metal Methods have been proposed to improve the palatability and taste of ions. In addition, Patent Document 2 (Japanese Unexamined Patent Application Publication No. 2002-302450) proposes a method of suppressing bitterness caused by metal ions, tea extract, etc. by blending sodium bicarbonate.

JP 2010-235557 A Japanese Patent Application Laid-Open No. 2002-302450

However, in the method of Patent Document 1, it is considered that the variation of flavor is limited due to the use of a flavor component, and it cannot be adopted for oral preparations such as general dentifrices. In method 2, the taste derived from baking soda appears, so there is still room for improvement in taste.

The present invention has been made in view of the above circumstances, and is an oral composition that contains a polyvalent metal salt, has excellent astringent feeling and its persistence, suppresses the metallic taste derived from polyvalent metal ions, and has a good feeling in use. intended to provide

The inventors of the present invention have made intensive studies to achieve the above object, and found that a divalent or trivalent metal salt of a specific organic acid or inorganic acid as a polyvalent metal salt has a linear structure or a branched chain structure with a specific number of carbon atoms. When a fatty acid or fatty acid ester having a structure is used in combination with an oral composition, the astringent action of the polyvalent metal ion is sufficiently and persistently expressed in the oral cavity, giving an excellent astringent feeling and its persistence, and It was found that the metallic taste derived from polyvalent metal ions is masked and the feeling of use is improved. That is, according to the present invention,
(a) one or more polyvalent metal salts selected from divalent metal salts and trivalent metal salts of organic acids having 2 to 12 carbon atoms and divalent metal salts and trivalent metal salts of inorganic acids;
(b) an oral composition comprising at least one selected from fatty acids and fatty acid esters having a straight chain structure with 8 to 22 carbon atoms and fatty acids and fatty acid esters having a branched chain structure with 8 to 22 carbon atoms; When blended in products, the astringent feeling and its persistence are excellent, the metallic taste derived from polyvalent metal ions is suppressed, and the oily odor derived from fatty acids or fatty acid esters is also suppressed, and a good feeling of use can be maintained. This finding led to the present invention.
In the present invention, when component (a) is used in combination with component (b), component (b) unexpectedly acts as a masking agent for the metallic taste of component (a). It provides the above-mentioned special effect that cannot be achieved when using an inappropriate fatty acid or its ester.

Accordingly, the present invention provides the following oral compositions.
[1]
(a) one or more polyvalent metal salts selected from divalent metal salts and trivalent metal salts of organic acids having 2 to 12 carbon atoms and divalent metal salts and trivalent metal salts of inorganic acids;
(b) containing one or more selected from fatty acids and fatty acid esters having a straight chain structure with 8 to 22 carbon atoms and fatty acids and fatty acid esters having a branched chain structure with 8 to 22 carbon atoms; An oral composition characterized by:
[2]
The oral composition according to [1], wherein component (b) is one or more selected from fatty acids having a branched chain structure with 8 to 22 carbon atoms and fatty acid esters having the branched chain structure.
[3]
The oral composition according to [2], wherein component (b) is one or more selected from branched chain fatty acids having 8 to 22 carbon atoms and sterol esters thereof.
[4]
The oral cavity composition according to [3], wherein the component (b) is one or two selected from isostearic acid and phytosteryl isostearate.
[5]
The oral composition according to [1], wherein the component (b) is one or more selected from linear fatty acids having 8 to 22 carbon atoms and esters thereof.
[6]
The component (a) is a water-soluble polyvalent metal salt, the divalent metal salt is selected from copper salts, zinc salts, tin salts, strontium salts, calcium salts and magnesium salts, and the trivalent metal salt is an aluminum salt and The oral composition according to any one of [1] to [5], which is selected from aluminum potassium salts.
[7]
(a) component is one or more water-soluble polyvalent metals selected from copper gluconate, zinc gluconate, calcium glycerophosphate, aluminum lactate, magnesium sulfate, magnesium chloride, zinc chloride, strontium chloride and potassium aluminum sulfate The oral composition according to any one of [1] to [6], which is a salt.
[8]
The oral cavity composition according to any one of [1] to [7], wherein (a)/(b), which indicates the content ratio of component (a) and component (b), is 0.1 to 15 as a mass ratio. thing.
[9]
The oral cavity composition according to any one of [1] to [8], containing 0.08 to 2.5% by mass of component (a) and 0.05 to 1% by mass of component (b).
[10]
The oral composition according to any one of [1] to [9], which is a dentifrice composition.

According to the present invention, it is possible to provide an oral composition that contains a polyvalent metal salt, has excellent astringency and excellent persistence, suppresses the metallic taste derived from polyvalent metal ions, and has a good feeling when used. This composition for oral cavity can provide a high feeling of use, and is useful for preventing or suppressing oral diseases such as dental caries, periodontal disease, and halitosis.

The present invention will be described in further detail below. The oral composition of the present invention includes (a) 1 selected from divalent metal salts and trivalent metal salts of organic acids having 2 to 12 carbon atoms, and divalent metal salts and trivalent metal salts of inorganic acids and (b) fatty acids and fatty acid esters having a straight chain structure with 8 to 22 carbon atoms and fatty acids and fatty acid esters having a branched chain structure with 8 to 22 carbon atoms. contains one or more

(a) The polyvalent metal salt is a water-soluble polyvalent metal ion-containing compound having an astringent action, and is a divalent or trivalent metal salt of an organic acid having 2 to 12 carbon atoms, or a divalent or trivalent inorganic acid. Trivalent metal salts can be used. These can be used individually by 1 type or in combination of 2 or more types.

Here, the organic acid has 2 to 12 carbon atoms, preferably 2 to 8 carbon atoms, and may contain a phosphoric acid group. Examples include citric acid, lactic acid, gluconic acid, glycerophosphoric acid and the like. Examples of inorganic acids include sulfuric acid, hydrochloric acid, nitric acid and phosphoric acid.

Examples of divalent or trivalent metal salts include, for example, divalent metal salts such as copper salts, zinc salts, tin salts, strontium salts, calcium salts, and magnesium salts. Salts and magnesium salts are preferred in view of their astringent action on the oral mucosa. Trivalent metal salts include aluminum salts and the like, and aluminum potassium salts containing monovalent metals can also be used.

Specific examples of divalent or trivalent metal salts of organic acids include copper gluconate, zinc gluconate, calcium glycerophosphate, and aluminum lactate.
Specific examples of divalent or trivalent metal salts of inorganic acids include magnesium sulfate, magnesium chloride, zinc chloride, strontium chloride, and potassium aluminum sulfate. Among them, magnesium sulfate, magnesium chloride, zinc chloride, and strontium chloride are preferred. Magnesium sulfate, magnesium chloride, and zinc chloride are particularly preferred.

The blending amount of component (a) is preferably 0.08 to 2.5% (% by mass, hereinafter the same) of the entire composition, more preferably 0.1 to 0.5%, and still more preferably 0.2 to 0.5%. When it is 0.08% or more, the astringent feeling and its persistence are sufficiently excellent, and when it is 2.5% or less, it is suitable for sufficiently masking the metallic taste.
Furthermore, within the range of the blending amount of the component (a), when blending a divalent or trivalent metal salt of an organic acid, or when blending a divalent or trivalent metal salt of an inorganic acid, each preferred blend The amount ranges are the same as above. In addition, each preferred compounding amount of the polyvalent metal salt of the component (a) is also within the above range.

Component (b) is one or more selected from fatty acids and fatty acid esters having a straight chain structure with 8 to 22 carbon atoms and fatty acids and fatty acid esters having a branched chain structure with 8 to 22 carbon atoms. . When these are used together with the component (a), they act as an astringent persistence improving agent and a metallic taste masking agent.
As component (b), a fatty acid having a straight chain structure of 8 to 22 carbon atoms or an ester thereof, a fatty acid having a branched chain structure of 8 to 22 carbon atoms, or a fatty acid ester having the branched chain structure can be used. These can be used singly or in combination of two or more in terms of exhibiting effects. From the viewpoints of persistence of astringent feeling and masking effect of metallic taste, the number of carbon atoms is preferably 12 to 20, particularly 16 to 18.

Here, the fatty acid having a linear or branched structure with 8 to 22 carbon atoms is a linear or branched higher fatty acid, and may be either a saturated fatty acid or an unsaturated fatty acid. Branched chain higher fatty acids, particularly saturated fatty acids, having high affinity for oral mucosa are preferable from the viewpoint of the longevity of flavor and the effect of masking the metallic taste.
Specifically, decanoic acid (C10), lauric acid (C12), myristic acid (C14), palmitic acid (C16), stearic acid (C18), oleic acid (C18), isodecanoic acid (C10), isomyristic acid (C14), isopalmitic acid (C16), isostearic acid (C18), etc., and one or more of these can be used (C in parentheses is an abbreviation for the number of carbon atoms). Among them, palmitic acid, stearic acid, oleic acid, and isostearic acid are preferable, and isostearic acid is more preferable, from the viewpoint of the persistence of astringent feeling and the effect of masking the metallic taste.

In addition, as the fatty acid ester having a linear or branched structure with 8 to 22 carbon atoms, in particular, from the viewpoint of the persistence of astringency and the effect of masking the metallic taste, the number of carbon atoms in the branched chain is as described above. Within the range, fatty acid esters having such a branched structure in acid or alcohol residues, or acid and alcohol residues are preferred, and sterol esters of branched chain fatty acids are more preferred. Examples of sterol esters having a sterol skeleton include phytosterol esters and cholesterol esters, with phytosterol esters being particularly preferred.
The fatty acid ester may contain an amino acid structure or a hydroxy group, and such a fatty acid ester may also be used.
Specifically, fatty acid sterol esters such as cholesteryl butyrate, cholesteryl stearate, cholesteryl isostearate, phytosteryl isostearate, cholesteryl hydroxystearate, cholesteryl oleate, macadamia nut oil fatty acid cholesteryl, N-lauroyl-L-glutamic acid di(cholesteryl octyldodecyl), N-acyl amino acid sterol esters such as N-lauroyl-L-glutamic acid di(cholesteryl/behenyl/octyldodecyl). Among them, phytosteryl isostearate is preferable from the viewpoint of persistence of astringent feeling and masking effect of metallic taste.

The blending amount of component (b) is preferably 0.05 to 1%, more preferably 0.06 to 1%, and particularly preferably 0.08 to 0.6% of the total composition. If it is 0.05% or more, the feeling of astringency is sufficiently maintained, and the metallic taste is masked. When it is 1% or less, it is possible to sufficiently prevent the appearance of the oily smell of itself.
When a fatty acid and a fatty acid ester are used together as the component (b), the blending amount of the fatty acid is preferably 0.05 to 1% of the total composition within the range of the blending amount of the component (b). , More preferably 0.06 to 1%, particularly preferably 0.08 to 0.6%. % is more preferred, and 0.08 to 0.6% is particularly preferred. The blending ratio of the fatty acid and the fatty acid ester is preferably 1:5 to 5:1 in terms of the mass ratio of fatty acid/fatty acid ester. Being within this range is more preferable in terms of effect expression.

In the present invention, (a)/(b), which indicates the ratio of the blending amount of component (a) and component (b), is preferably 0.1 to 15 as a mass ratio, and more preferably 0.3 to 12.5. It is preferably 0.5 to 4, more preferably 1.0 to 2.5. Within this range, the feeling of astringency and its persistence, and the effect of masking the metallic taste are excellent, and the oily smell can be further suppressed. If it is less than 0.1, the persistence of the astringent feeling may be poor and the oily smell may not be suppressed, and if it exceeds 15, the effect of masking the metallic taste may be poor.

The dosage form and shape of the oral composition of the present invention are not particularly limited. Formulations, capsules, films, kneaded substances, molten solids, waxy solids, elastic solids, etc.) can be prepared into any dosage form.
In addition, the preparations prepared above include, for example, dentifrices (toothpaste, liquid toothpaste, toothpaste, etc.), mouthwashes, coatings, patches, mouth fresheners, foods (e.g., chewing gums, tablets, candies, gummies, films, lozenges, etc.), but dentifrices, especially toothpastes, are preferred within the range of oral uses.

In addition to the components described above, the composition for oral cavity of the present invention can contain various components that can be used in the composition for oral cavity within a range that does not impair the effects of the present invention. Examples of such additive components in the case of dentifrices include abrasives, thickeners, binders, surfactants, sweeteners, preservatives, fragrances, coloring agents, pH adjusters, solvents, active ingredients, and the like. can be appropriately selected depending on the dosage form. Specific examples of additive components are shown below, but components that can be blended in the oral composition of the present invention are not limited to these.

Examples of abrasives include silica-based abrasives such as silicic anhydride, crystalline silica, amorphous silica, silica gel and aluminosilicate, zeolite, calcium hydrogen phosphate anhydrate, calcium hydrogen phosphate dihydrate, Calcium pyrophosphate, calcium carbonate, sodium hydrogen carbonate, aluminum hydroxide, alumina, magnesium carbonate, magnesium phosphate tertiary, zirconium silicate, calcium tertiary phosphate, hydroxyapatite, calcium tetraphosphate, synthetic resin abrasives. Among them, silica-based abrasives such as silicic anhydride are preferable from the viewpoint of oral mucosa irritation and usability. The amount of abrasive compounded is usually 0-20%, especially 3-20%, especially 5-15%.

Examples of thickening agents include sugar alcohols and polyhydric alcohols such as sorbitol, propylene glycol, butylene glycol, glycerin and polyethylene glycol. The blending amount of the thickening agent is usually 1 to 60%.

Binders include, for example, pullulan, gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, carrageenan, sodium alginate, xanthan gum, sodium polyacrylate, gum arabic, guar gum, locust bean gum, polyvinyl alcohol, polyvinyl Examples include organic binders such as pyrrolidone and carboxyvinyl polymer, and inorganic binders such as thickening silicic anhydride and bentonite. When an organic binder is used, its blending amount is usually 0.1 to 3%, and when an inorganic binder is used, its blending amount is usually 1 to 10%, particularly 1 to 7%. be.

As surfactants, anionic surfactants, nonionic surfactants and amphoteric surfactants can be blended.
Examples of anionic surfactants include N-acylamino acid salts, α-olefin sulfonates, N-acyl sulfonates, alkyl sulfates, and polyoxyethylene alkyl ether sulfates. Among them, N-acylamino acid salts, α-olefin sulfonates, alkyl sulfates, and particularly alkyl sulfates such as sodium lauryl sulfate are preferred from the viewpoint of versatility.
Examples of nonionic surfactants include polyoxyethylene alkyl ethers, polyoxyethylene-polyoxypropylene block copolymers, polyoxyethylene hydrogenated castor oil, polyoxyethylene ethers of glycerin esters, sucrose fatty acid esters, alkylolamides. , glycerin fatty acid ester, sorbitan fatty acid ester, and polyoxyethylene sorbitan fatty acid ester. Among these, polyoxyethylene alkyl ethers, polyoxyethylene hydrogenated castor oils, alkylolamides, and sorbitan fatty acid esters are preferably used in terms of versatility. The polyoxyethylene alkyl ether preferably has 14 to 30 carbon atoms in the alkyl chain. Polyoxyethylene alkyl ether preferably has an average number of moles of ethylene oxide added of 3 to 30. The polyoxyethylene hydrogenated castor oil preferably has an average number of moles of ethylene oxide added of 10 to 100. The alkylolamide preferably has an alkyl chain of 12 to 14 carbon atoms. Moreover, the sorbitan fatty acid ester preferably has a fatty acid having 12 to 18 carbon atoms. The polyoxyethylene sorbitan fatty acid ester preferably has 16 to 18 carbon atoms in the fatty acid and 10 to 40 average moles of ethylene oxide added. The above ester is different from the fatty acid ester of component (b).
Examples of amphoteric surfactants include alkylbetaine-based, amine oxide-based, and imidazolinium betaine-based surfactants, specifically 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, coconut oil. Fatty acid amide alkyl betaines can be mentioned.
One or two or more surfactants can be used, and the blending amount is usually 0 to 10%, particularly 0.01 to 10%.

Sweetening agents include, for example, saccharin sodium, stevioside, neohesperidin dihydrochalcone, glycyrrhizin.
Examples of antiseptics include paraoxybenzoic acid esters such as sodium benzoate, methylparaben, ethylparaben and butylparaben.

Flavors include peppermint oil, spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cassia oil, clove oil, thyme oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, Lime oil, lavender oil, rosemary oil, laurel oil, chamomile oil, caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil, neroli oil, rose oil, jasmine oil, grapefruit oil, sweetie Natural flavors such as oil, yuzu oil, iris concrete, absolute peppermint, absolute rose, orange flower, etc., and processing of these natural flavors perfumed, etc.), and menthol, carvone, anethole, cineole, methyl salicylate, cinnamic aldehyde, eugenol, 3-l-menthoxypropane-1,2-diol, thymol, linalool, linalyl acetate, limonene, Menthone, menthyl acetate, N-substituted-paramenthane-3-carboxamide, pinene, octylaldehyde, citral, pulegone, carbyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexane propionate, methyl anthranilate, ethyl Single fragrances such as methyl phenylglycidate, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, cyclotene, furfural, trimethylpyrazine, ethyl lactate, ethyl thioacetate, strawberry flavor, apple flavor, banana Flavors, pineapple flavors, grape flavors, mango flavors, butter flavors, milk flavors, mixed flavors such as fruit mix flavors, tropical fruit flavors, and other known flavor materials used in oral compositions can be used in combination. , but not limited to the fragrances described in the examples.
In addition, the blending amount is not particularly limited, but it is preferable to use 0.000001 to 1% of the above perfume material in the composition. It is preferable to use 0.1 to 2% for

Examples of coloring agents include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, monascus pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cacao pigment, spirulina blue pigment, and coumarind pigment. , Red No. 3, Red No. 104, Red No. 105, Red No. 106, Yellow No. 4, Yellow No. 5, Green No. 3, Blue No. 1, riboflavin, sodium copper chlorophine, and titanium dioxide. The amount of the coloring agent is usually 0.00001 to 3%.

Examples of solvents include water and lower alcohols having 3 or less carbon atoms such as ethanol and propanol. Solvents are commonly included in liquid oral compositions. When water is blended as the solvent, the blending amount is preferably 20 to 95%. When a lower alcohol is blended as a solvent, the blending amount is preferably 1 to 20%.

Examples of active ingredients include fluorine-containing compounds such as sodium fluoride and sodium monofluorophosphate, bactericides, anti-inflammatory agents, tissue activators, and vitamins.

EXAMPLES Hereinafter, the present invention will be specifically described by showing examples and comparative examples, but the present invention is not limited to the following examples. In the following examples, % indicates % by mass unless otherwise specified.

[Examples, Comparative Examples]
Dentifrice compositions (toothpaste) having compositions shown in Tables 1 to 5 were prepared by conventional methods and evaluated by the following methods. The results are also shown in the table.

Evaluation method of feeling of astringency and its persistence Ten subjects (specialized panelists) placed the dentifrice composition on a toothbrush, brushed the oral cavity for 3 minutes, and then rinsed. After) was evaluated according to the following rating criteria. The scores of 10 people were averaged, and the feeling of astringency immediately after rinsing and the feeling of astringency after 5 minutes were evaluated according to the following evaluation criteria.
Rating criteria 4 points: sense of convergence.
3 points: A sense of astringency is slightly felt.
2 points: The feeling of convergence is not very felt.
1 point: Virtually no astringency is felt.
Evaluation Criteria ◎: Average score of 3.5 to 4.0 ○: Average score of 3.0 to 3.5 △: Average score of 2.0 to 3.0 x: Average score of 2.0. Less than 0 points

Evaluation method for lack of metallic taste and oily smell (during and after brushing) Ten expert panelists put the dentifrice composition on the toothbrush, brushed the oral cavity for 3 minutes, rinsed, and then rinsed. , the metallic taste and oily smell felt after rinsing were evaluated according to the following rating criteria. The scores of 10 people were averaged, and the metallic taste during brushing or after rinsing and the oily smell during brushing or after rinsing were evaluated according to the following evaluation criteria.
Rating criteria for absence of metallic taste 4 points: No metallic taste is felt.
3 points: Almost no metallic taste is felt.
2 points: A slight metallic taste is felt.
1 point: Very strong metallic taste.
Evaluation criteria for lack of metallic taste ◎: Average score of 3.5 to 4.0 points ○: Average score of 3.0 to 3.5 points △: Average score of 2.0 to 3.0 points × : Less than 2.0 points on average Rating criteria for absence of oily smell 4 points: No oily smell is felt.
3 points: Almost no oily smell is felt.
2 points: A little oily smell is sensed.
1 point: Very strong oily smell.
Evaluation criteria for lack of oily odor ◎: Average score 3.5 to 4.0 points ○: Average score 3.0 to 3.5 points △: Average score 2.0 to 3.0 points ×: Average score less than 2.0 points

*；Reference example

Claims (6)

(a) one or more polyvalent metal salts selected from divalent metal salts and trivalent metal salts of organic acids having 2 to 12 carbon atoms, and divalent metal salts and trivalent metal salts of inorganic acids;
(b) contains one or more selected from branched chain fatty acids having 16 to 18 carbon atoms and sterol esters thereof, and the polyvalent metal salt of component (a) is a water-soluble polyvalent metal salt; The valent metal salt is selected from copper salts, zinc salts, tin salts, strontium salts, calcium salts and magnesium salts, and the trivalent metal salt is selected from aluminum salts and aluminum potassium salts . Oral composition. 2. The oral cavity composition according to claim 1, wherein component (b) is one or two selected from isostearic acid and phytosteryl isostearate. (a) component is one or more water-soluble polyvalent metals selected from copper gluconate, zinc gluconate, calcium glycerophosphate, aluminum lactate, magnesium sulfate, magnesium chloride, zinc chloride, strontium chloride and potassium aluminum sulfate The oral composition according to claim 1 or 2 , which is a salt. The oral composition according to any one of claims 1 to 3 , wherein (a)/(b), which indicates the content ratio of component (a) and component (b), is 0.1 to 15 as a mass ratio. . The oral cavity composition according to any one of claims 1 to 4 , containing 0.08 to 2.5% by mass of component (a) and 0.05 to 1% by mass of component (b). The oral composition according to any one of claims 1 to 5 , which is a dentifrice composition.