Oral components
The oral composition enhances astringency and stability while reducing unpleasant taste by using berberine with potassium nitrate, sodium chloride, and specific salts, addressing the limitations of existing formulations.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- LION CORP
- Filing Date
- 2024-12-16
- Publication Date
- 2026-06-26
Smart Images

Figure 2026105164000001 
Figure 2026105164000002 
Figure 2026105164000003
Abstract
Description
Technical Field
[0001] The present invention relates to an oral composition.
Background Art
[0002] For the purpose of preventing periodontal disease, there are oral compositions containing active ingredients having anti-inflammatory and antibacterial effects. In addition, for oral compositions aimed at preventing periodontal disease, a tightening feeling (astringent feeling) in the oral cavity is required. Users can actually feel the prevention of periodontal disease by the astringent feeling after cleaning the oral cavity. The astringent feeling can be imparted by blending a compound having astringency (astringent) into the oral composition. Patent Document 1 discloses an oral composition containing berberine as an astringent.
Prior Art Documents
Patent Documents
[0003]
Patent Document 1
Summary of the Invention
Problems to be Solved by the Invention
[0004] Patent Document 1 discloses an oral composition containing berberine as an astringent, but further improvement in the astringent feeling of the oral composition is required. In addition, for oral compositions, it is required that an unpleasant taste is suppressed and liquid separation due to storage does not occur (high storage stability). An object of the present invention is to provide an oral composition having a high astringent feeling, high storage stability, and suppressed unpleasant taste.
Means for Solving the Problems
[0005] The present invention has the following aspects. [1] Component (A): Berberine, and (B) Components: At least one selected from the group consisting of potassium nitrate and sodium chloride, (C) Ingredients: Contains at least one selected from lauroyl methyl taurate salt and lauroyl glutamate salt, The ratio of the total mass of components (A) and (B) to the mass of component (C), expressed as [component (A) + component (B)] / component (C), is between 0.5 and 13. Oral composition. [2] The content of component (A) is 0.001 to 0.005% by mass of the total mass of the oral composition. The oral composition described in [1]. [3] The content of component (B) is 0.1 to 8.0% by mass relative to the total mass of the oral composition. The oral composition described in [1] or [2]. [4] The content of component (C) is 0.4 to 2.0% by mass relative to the total mass of the oral composition. An oral composition as described in any one of [1] to [3]. [5] An oral composition according to any one of [1] to [4], which is a toothpaste. [Effects of the Invention]
[0006] According to the present invention, it is possible to provide an oral composition that has high astringency and storage stability, and suppresses unpleasant tastes. [Modes for carrying out the invention]
[0007] The embodiments of the present invention will be described in detail below, but the present invention is not limited to the embodiments described below and can be implemented with various modifications within the scope of its gist.
[0008] In this specification and in the claims, a numerical range represented by "~" means a numerical range that includes the numbers before and after "~" as the lower and upper limits, respectively. For example, A~B is synonymous with A or greater and B or less.
[0009] <Oral composition> The oral composition of this disclosure comprises the following components (A), (B), and (C).
[0010] [(A) component] (A) Component is berberine. By including component (A) in the oral composition, the astringent sensation of the oral composition can be enhanced. Berberine and berberine compounds can be used as the berberine. Examples of berberine compounds include berberine chloride and berberine sulfate. Commercially available berberine products may also be used. For example, berberine chloride hydrate manufactured by Alps Pharmaceutical Co., Ltd. can be used as the berberine.
[0011] (A) The component may be added to the oral composition as a solvent extract of a plant containing berberine (hereinafter sometimes referred to as "plant extract").
[0012] Examples of plants containing berberine include the bark of Phellodendron amurense Ruprecht or Phellodendron chinense Schneider (Rutaceae) or other plants of the same genus, with the periderm removed. Hydrophilic solvents can be used for extracting plants containing berberine, including lower monohydric alcohols such as water, ethanol, and propanol, as well as polyhydric alcohols such as 1,3-butylene glycol and propylene glycol. These hydrophilic solvents may be used individually or as a mixed solvent in combination of two or more. Water and ethanol are preferred, water is more preferred, and hot water is even more preferred. Conventional methods can be used for extraction conditions and post-treatment.
[0013] Furthermore, known plant extracts containing berberine can be used. These plant extracts may be used individually or in combination of two or more.
[0014] The state of the plant extract containing berberine is not particularly limited, and it may be, for example, in a liquid state, a dried solid state, a powdered extract, etc. Examples of the plant extract containing berberine include, for example, Coptis root extract listed in the Pharmaceutical Excipients Raw Material Standards 2021 and Coptis root powder listed in the 18th Revised Japanese Pharmacopoeia.
[0015] As the plant extract containing berberine, commercially available products may be used. Examples of the plant extract containing berberine include, for example, Coptis root extract manufactured by Kojima Pharmaceutical Co., Ltd., Coptis chinensis extract manufactured by Alps Pharmaceutical Industry Co., Ltd., Coptis root liquid B manufactured by Ichimaru Pharcos Co., Ltd., Coptis root extract BG-J manufactured by Maruzen Pharmaceutical Co., Ltd., and Coptis root extract BG manufactured by Koei Kogyo Co., Ltd., which can be obtained under these product names.
[0016] There is no particular limitation on the content of berberine contained in the oral composition. It is preferably 0.001 to 0.005% by mass, more preferably 0.002 to 0.004% by mass, and even more preferably 0.002 to 0.003% by mass, based on the total mass of the oral composition. When the content of berberine contained in the oral composition is not less than the above lower limit value, the astringency of the oral composition can be further enhanced. When the content of berberine contained in the oral composition is not more than the above upper limit value, the unpleasant taste of the oral composition can be more effectively suppressed. Here, the unpleasant taste refers to an unpleasant taste such as bitterness felt in the oral cavity caused by the salty taste of salts, etc.
[0017] When the component (A) contained in the oral composition is a plant extract containing berberine, there is no particular limitation on its content, as long as the content of berberine contained in the plant extract is within the above preferred range based on the total mass of the oral composition. In the oral composition, the content of the plant extract containing berberine is preferably, for example, 0.02 to 0.1% by mass, more preferably 0.04 to 0.08% by mass, and still more preferably 0.04 to 0.06% by mass based on the total mass of the oral composition. When the content of the plant extract containing berberine in the oral composition is not less than the above lower limit value, the astringent feeling of the oral composition can be further enhanced. When the content of the plant extract containing berberine in the oral composition is not more than the above upper limit value, the unpleasant taste of the oral composition can be more suppressed.
[0018] [Component (B)] Component (B) is at least one selected from the group consisting of potassium nitrate and sodium chloride. By including Component (B) in the oral composition, the astringent feeling of the oral composition can be enhanced.
[0019] There is no particular limitation on the content of Component (B) contained in the oral composition. It is preferably 0.1 to 8.0% by mass, more preferably 1.0 to 7.0% by mass, and still more preferably 1.0 to 6.0% by mass based on the total mass of the oral composition. When the content of Component (B) contained in the oral composition is not less than the above lower limit value, the astringent feeling of the oral composition can be further enhanced. When the content of Component (B) contained in the oral composition is not more than the above upper limit value, the storage stability can be further enhanced, the decrease in the astringent feeling can be suppressed, and the unpleasant taste can be more suppressed.
[0020] [Component (C)] Component (C) is at least one selected from the group consisting of lauroyl methyl taurine salt and lauroyl glutamate. By including Component (C) in the oral composition, the storage stability of the oral composition can be enhanced.
[0021] In the case of lauroyl methyl taurate salts, there are no particular limitations on the type of salt, and examples include alkali metal salts such as sodium salts. As for lauroyl methyl taurate salts, sodium lauroyl methyl taurate, in which the salt is sodium, is preferred. Commercially available products may be used as sodium lauroyl methyl taurate, for example, LMT-P (manufactured by Nikko Chemicals Co., Ltd.) can be used.
[0022] In the case of lauroyl glutamate, there are no particular limitations on the type of salt, and examples include alkali metal salts such as sodium salts. As for the lauroyl glutamate, sodium lauroyl glutamate, in which the salt is sodium, is preferred. As for sodium lauroyl glutamate, commercially available products may be used, for example, Amisoft® LS-11 (manufactured by Ajinomoto Co., Inc.) can be used.
[0023] There are no particular limitations on the amount of component (C) contained in the oral composition, but it is preferably 0.4 to 2.0% by mass, more preferably 0.4 to 1.0% by mass, and even more preferably 0.4 to 0.8% by mass, relative to the total mass of the oral composition. If the amount of component (C) contained in the oral composition is above the lower limit, the storage stability can be further improved. If the amount of component (C) contained in the oral composition is below the upper limit, unpleasant tastes can be further suppressed.
[0024] The ratio of the total mass of components (A) and (B) to the mass of component (C) contained in the oral composition (AB / C ratio), expressed as [(A) component + (B) component] / (C component), is 0.5 to 13, preferably 0.7 to 13, and more preferably 1 to 13. When the AB / C ratio is above the lower limit, the astringent feeling of the oral composition is enhanced and unpleasant tastes can be suppressed. When the AB / C ratio is below the upper limit, the astringent feeling and storage stability of the oral composition are enhanced, and unpleasant tastes can be suppressed.
[0025] [Optional ingredients] The oral composition may further contain components other than those described above (A), (B), and (C) (hereinafter sometimes referred to as "optional components"). The optional components can be appropriately selected from known components, taking into consideration the form and method of use of the oral composition. Examples of optional components include abrasives, surfactants other than component (C) (hereinafter sometimes referred to as "optional surfactants"), humectants, medicinal ingredients, fragrances, sweeteners, oily components, preservatives, binders, pH adjusters, colorants (pigments), and solvents. The total amount of component (A), component (B), component (C), and optional components mentioned above shall not exceed 100% by mass.
[0026] (Abrasive) The abrasive can be either an inorganic abrasive or an organic abrasive. Examples of inorganic abrasives include abrasive silica (e.g., anhydrous silicic acid, zeolite, precipitated silica, aluminosilicate, zirconosilicate, crystalline zirconium silicate, titanium-bonded silica, silica gel, etc.), calcium phosphate compounds (e.g., discalcium phosphate dihydrate or anhydrous, monocalcium phosphate, discalcium phosphate dihydrate or anhydrous, insoluble calcium metaphosphate, tricalcium phosphate, tetracalcium phosphate, octacalcium phosphate, calcium pyrophosphate, etc.), and calcium carbonate abrasives (e.g., calcium carbonate (light, heavy) Examples of abrasives include calcium-based abrasives (e.g., calcium hydroxide, calcium sulfate, calcium oxide, etc.), silicate-based abrasives (e.g., anhydrous silica, zeolite, zirconium silicate, etc.), magnesium-based abrasives (e.g., magnesium carbonate, trimagnesium phosphate, etc.), apatite-based abrasives (e.g., hydroxyapatite, fluoroapatite, calcium-deficient apatite, etc.), titanium-based materials (e.g., titanium dioxide, titanium mica, titanium oxide, etc.), aluminum-based materials (e.g., aluminum hydroxide, aluminum oxide), minerals (e.g., bentonite, etc.), etc.
[0027] Examples of organic abrasives include polymethyl methacrylate and synthetic resin-based abrasives. Inorganic abrasives are preferred as abrasives in oral compositions, and abrasive silica is more preferred.
[0028] The abrasive silica is preferably abrasive particles with an average particle size of 1 to 40 μm, and the BET specific surface area of the abrasive silica is preferably 80 to 250 square meters per gram. Here, the average particle size of the abrasive silica is the volume-based median diameter (D50) measured by laser diffraction-scattering.
[0029] There are no particular limitations on the RDA (Radioactive Dentine Abrasion Values) of the abrasive, but it is preferably between 50 and 200.
[0030] The abrasive may be in the form of granules. Examples of granules include particles obtained by granulating water-insoluble powders (e.g., silica gel, precipitated silica). Particles containing pigments such as Red No. 202, No. 205, Red No. 226, Orange No. 203, and Yellow No. 205 may be included. When granulating into granules, any suitable conventionally known binder may be used.
[0031] The abrasives described above may be used individually or in combination of two or more types. There are no particular limitations on the amount of abrasive contained in the oral composition, but it is preferably 50% by mass or less, more preferably 40% by mass or less, and even more preferably 30% by mass or less, relative to the total mass of the oral composition. Furthermore, in this invention, in terms of achieving the desired effect, abrasives may not be included (amount 0% by mass), and the composition may be abrasive-free.
[0032] (Optional surfactant) As optional surfactants, surfactants known in oral compositions can be used. Examples of optional surfactants include nonionic surfactants, anionic surfactants (excluding component (C)), amphoteric surfactants, cationic surfactants, and the like.
[0033] Examples of nonionic surfactants include polyoxyethylene alkyl ethers (e.g., polyoxyethylene stearyl ether), polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters (e.g., polyoxyethylene sorbitan monostearate), fatty acid alkylolamides (e.g., lauric acid mono or diethanolamide), polyoxyethylene fatty acid esters, polyoxyethylene alkenyl ethers, (poly)glycerin fatty acid esters (e.g., polyglyceryl monolaurate), sucrose fatty acid esters (e.g., sucrose stearate, sucrose palmitate), sugar alcohol fatty acid esters (e.g., maltitol fatty acid ester, lactitol fatty acid ester), alkyl glucosides, polyoxyethylene polyoxypropylene copolymers, and polyoxyethylene polyoxypropylene fatty acid esters.
[0034] The number of carbon atoms in the alkyl chain of polyoxyethylene alkyl ether is preferably 10 to 26, and the average number of moles of ethylene oxide added is preferably 2 to 50 moles. The average number of moles of ethylene oxide added to polyoxyethylene hydrogenated castor oil is preferably 5 to 100 moles, and more preferably 5 to 60 moles. The number of carbon atoms in the fatty acid of sorbitan fatty acid ester is preferably 10 to 18. The number of carbon atoms in the fatty acid of polyoxyethylene sorbitan fatty acid ester is preferably 12 to 18. The average number of moles of ethylene oxide added is preferably 10 to 40 moles. The number of carbon atoms in the alkyl chain of alkylolamide is preferably 12 to 14.
[0035] Preferred nonionic surfactants for oral compositions include polyoxyethylene hydrogenated castor oil, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene alkyl ethers. The inclusion of nonionic surfactants in oral compositions can further suppress liquid separation of the formulation.
[0036] In this disclosure, the anionic surfactant as an optional component refers to anionic surfactants other than lauroyl methyl taurate and lauroyl glutamate. Examples of anionic surfactants include alkyl sulfates, acyl amino acid salts, acyl taurine salts, α-olefin sulfonates, hydrogenated coconut fatty acid monoglyceride monosulfates, and lauryl sulfoacetates. The alkyl and acyl groups of the anionic surfactant may be linear or branched, saturated or unsaturated, and preferably have 10 to 20 carbon atoms.
[0037] The salt can be selected from pharmacologically acceptable salts. Examples of pharmacologically acceptable salts include base addition salts and amino acid salts. Specifically, examples include inorganic base salts (e.g., sodium salts, calcium salts, magnesium salts, ammonium salts, etc.), organic base salts (e.g., triethylammonium salts, triethanolammonium salts, pyridinium salts, diisopropylammonium salts, etc.), and basic amino acid salts (e.g., arginine salts, etc.). As anionic surfactants contained in oral compositions, inorganic base salts are preferred, alkali metal salts (e.g., sodium salts) or ammonium salts are more preferred, and sodium salts are even more preferred.
[0038] Examples of alkyl sulfates include lauryl sulfate (e.g., sodium lauryl sulfate) and myristoyl sulfate. Examples of acyl amino acid salts include acyl sarcosine salts (e.g., lauroyl sarcosine salt, myristoyl sarcosine salt), acyl glycine salts (e.g., N-lauroyl-N-methylglycine salt, cocoyl glycine salt), acyl alanine salts (e.g., N-lauroyl-β-alanine salt, N-myristyl-β-alanine salt, N-cocoyl-β-alanine salt, N-lauroyl-N-methyl-β-alanine salt, N-myristoyl-N-methyl-β-alanine salt, N-methyl-N-acyl alanine salt), and acyl aspartate salts (e.g., lauroyl aspartate salt). Examples of α-olefin sulfonates include α-olefin sulfonates with 12 to 18 carbon atoms, such as tetradecene sulfonate. Other examples of anionic surfactants include hydrogenated coconut fatty acid monoglyceride sodium monosulfate and sodium lauryl sulfoacetate.
[0039] When an oral composition contains an anionic surfactant, its foaming ability and foam quality are further improved.
[0040] Examples of amphoteric surfactants include betaine-type amphoteric surfactants (e.g., alkyldimethylaminoacetic acid betaine, fatty acid amidopropyldimethylaminoacetic acid betaine, etc.), imidazoline-type amphoteric surfactants (e.g., N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt, coconut oil fatty acid imidazolinium betaine, 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, etc.), and alkyl betaines (e.g., lauryldimethylaminoacetic acid betaine, etc.). When an oral composition contains an amphoteric surfactant, the foaming ability and foam quality are further improved.
[0041] Examples of cationic surfactants include alkylammonium salts and alkylbenzylammonium salts. When an oral composition contains a cationic surfactant, the preservative effect in the formulation can be further improved.
[0042] The surfactants used as optional components may be used individually or in combination of two or more types. There are no particular limitations on the amount of surfactant contained as an optional component in the oral composition, but it is preferably 0.2 to 15% by mass, more preferably 0.3 to 12% by mass, and even more preferably 0.5 to 10% by mass, relative to the total mass of the oral composition.
[0043] (Humectant) Preferred humectants are sugar alcohols and polyhydric alcohols other than sugar alcohols. Examples of sugar alcohols include sorbitol, erythritol, maltitol, lactitol, xylitol, reduced starch syrup, and glycerin. Examples of polyhydric alcohols other than sugar alcohols include ethylene glycol, propylene glycol, dipropylene glycol, butylene glycol, and polyethylene glycol. In oral compositions, sorbitol and glycerin are preferred as sugar alcohols, and propylene glycol is preferred as a polyhydric alcohol. These humectants may be used individually or in combination of two or more.
[0044] There are no particular limitations on the amount of humectant contained in the oral composition, but it is preferably 5 to 70% by mass, more preferably 10 to 65% by mass, and even more preferably 20 to 60% by mass, relative to the total mass of the oral composition. If the amount of humectant contained in the oral composition is above the lower limit, solidification of the composition due to drying can be further suppressed. If the amount of humectant contained in the oral composition is below the upper limit, the oral composition can be given an appropriate level of moisture, thereby improving the feel of use.
[0045] (Medicinal ingredients) Medicinal ingredients include, for example, bactericides or antibacterial agents (e.g., cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, isopropylmethylphenol, triclosan, thymol, hinokitiol, lysozyme chloride, etc.), enzymes (e.g., dextranase, mutanase, amylase, protease, Litec enzyme, papain, bromelain, etc.), fluorides (e.g., sodium fluoride, sodium monofluorophosphate, tin fluoride, etc.), anti-inflammatory agents (e.g., ε-aminocaproic acid, allantoin, tranexamic acid, etc.) Examples of medicinal ingredients include glycyrrhizinate, glycyrrhetinic acid, glycyrrhetinate, azulene, dihydrocholesterol, etc.), tartar preventive agents (e.g., condensed phosphate, ethane hydroxydiphosphonate, etc.), blood flow promoters (e.g., vitamin E, etc.), hypersensitivity inhibitors (e.g., aluminum lactate, etc.), coating agents (e.g., hydroxyethylcellulose dimethyldiallylammonium chloride, etc.), amino acids (e.g., alanine, glycine, proline, pyrrolidone carboxylic acid (salt), etc.), and astringents other than components (A) and (B). These medicinal ingredients may be used individually or in combination of two or more. The effective amount of the above medicinal ingredients can be appropriately determined according to conventional methods.
[0046] (fragrance) Fragrances include, for example, natural essential oils such as peppermint oil, spearmint oil, Japanese mint oil, anise oil, cassia oil, clove oil, eucalyptus oil, wintergreen oil, mastic oil, neroli oil (orange blossom oil), lemongrass oil, jasmine oil, rose oil, iris oil, thyme oil, sage oil, cardamom oil, coriander oil, rosemary oil, laurel oil, chamomile oil, caraway oil, basil oil, marjoram oil, lemon oil, orange oil, grapefruit oil, lime oil, mandarin oil, yuzu oil, nutmeg oil, lavender oil, paraclete oil, vanilla oil, cinnamon oil, pimento oil, cinnamon leaf oil, and perilla oil; menthol, menthofran, carvone, cinnamic aldehyde, anethole, 1,8-cineole, methyl salicylate Fragrance components contained in the above natural essential oils, such as phosphate, eugenol, thymol, linalool, limonene, menthone, menthyl acetate, citral, decanal, camphor, borneol, pinene, spiranthol, n-decyl alcohol, citronellol, α-terpineol, linalyl acetate, phenylethyl glycidate, phenylethyl alcohol, allyl hexanoate, octanol, octanal, octyl acetate, caryophyllene, germacrene, viridiflorol, methyl cinnamate, methylheptin carbonate, ionone, ethyl-β-methylthiopropionate, cis-6-nonenol, carone, methyl jasmonate, citronellyl acetate, ethyl linalool, etc.Ethyl acetate, ethyl butyrate, isoamyl acetate, hexanal, hexenal, methyl anthranilate, ethyl methylphenyl glycidate, benzaldehyde, vanillin, ethyl vanillin, furaneol, ethylcyclopentenolone, 3-hydroxy-4,5-dimethylfuran-2-one, cyclotene, 2-methylbutyric acid, acetate acid, propionic acid, cis-3-hexenol, trans-2-hexenal, undecalactone, decalactone, hexyl acetate, ethyl-2- Examples of fragrance components include methyl butyrate, benzyl alcohol, N-ethyl-p-menthane-3-carboxamide (N-ethyl-2-isopropyl-5-methylcyclohexanecarboxamide), menthyl lactate, ethylene glycol-l-menthyl carbonate, maltol, and ethyl maltol; plant extracts such as chili pepper extract, ginger extract, pepper extract, and Japanese pepper extract; cardamom extract; and various blended flavors such as mint, fruit, and herb, which are created by combining several fragrance components and natural essential oils.
[0047] Fragrances that can also function as cooling agents include, for example, N-ethyl-p-menthane-3-carboxamide (N-ethyl-2-isopropyl-5-methylcyclohexanecarboxamide), N-[(ethoxycarbonyl)methyl)-p-menthane-3-carboxamide, Np-benzeneacetonitrile menthanecarboxamide, N-(2-(pyridine-2-yl)ethyl)-3-p-menthanecarboxamide, N-(2-hydroxy-2-phenylethyl)-2-isopropyl-5,5-dimethylcyclohexane-1-carboxamide, 2-(4-methylphenoxy)-N-(1H-pyrazole-3-yl)-N-(thiophen-2-ylmethyl)acetamide, menthyl lactate, menthyl monosuccinate, vanillyl butyl ether, isopulegol, menthol glycoside ketal, N-(4-cyanomethylphenyl)-p Other examples include menthanecarboxamide, 3-l-menthoxypropane-1,2-diol, menthylglyceryl ether, menthyl succinate, linalool oxide, vanillyl butyl ether, 5-methyl-2-propane-2-yl-N-(2-pyridine-2-ylethyl)cyclohexane-1-carboxamide, 3-(p-menthane-3carboxamide)ethyl acetate, 2-isopropyl-N,2,3-trimethylbutylamide, N-ethyl-2,2-diisopropylbutanamide, N-(1,1-dimethyl-2-hydroxyethyl)-2,2-diethylbutanamide, N-(2-hydroxyethyl)-2,3-dimethyl-2-isopropylbutanamide, menthyl glutarate, 2-(4-methylphenoxy)-N-(1H-pyrazole-yl)-N-(thiophen-2-ylmethyl)acetamide, and isopulegol. As for the fragrance, one of the fragrances exemplified above may be used alone, or two or more may be used in combination.
[0048] When compounding the above fragrances, solvents may be used. Examples of solvents include ethanol, propylene glycol, glycerin fatty acid esters, and triacetin.
[0049] There are no particular limitations on the amount of fragrance contained in the oral composition, but it is preferably 0.0000001 to 5.0% by mass, more preferably 0.00001 to 3.0% by mass, and even more preferably 0.01 to 2.0% by mass, relative to the total mass of the oral composition. If the amount of fragrance contained in the oral composition is above the lower limit, it can better mask the unpleasant taste of other components. If the amount of fragrance contained in the oral composition is below the upper limit, the sensation of stimulation becomes moderately strong, and the user experience is further improved.
[0050] (Sweetener) Examples of sweeteners include saccharin, sodium saccharin, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidin dihydrochalcone, perillartin, glycyrrhizin, thaumatin, and aspartylphenylalanine methyl ester. Of these, sodium saccharin is preferred. These sweeteners may be used individually or in combination of two or more.
[0051] There are no particular limitations on the amount of sweetener contained in the oral composition, but it is preferably 0.001 to 10% by mass, more preferably 0.01 to 5% by mass, and even more preferably 0.05 to 3% by mass, relative to the total mass of the oral composition. If the amount of sweetener contained in the oral composition is above the lower limit above, it can better mask the unpleasant taste of other components.
[0052] (Oily components) Examples of oily components include hydrocarbons (e.g., squalane, liquid paraffin, petrolatum, microcrystalline wax, etc.), higher alcohols (e.g., alcohols with 8 to 22 carbon atoms such as lauryl alcohol, cetyl alcohol, cetostearyl alcohol, oleyl alcohol, isostearyl alcohol, etc.), higher fatty acids (e.g., fatty acids with 8 to 22 carbon atoms such as lauric acid, myristic acid, oleic acid, isostearic acid, etc.), vegetable oils (e.g., olive oil, castor oil, coconut oil, etc.), and fatty acid esters (e.g., isopropyl myristate, etc.). These oily components may be used individually or in combination of two or more.
[0053] There are no particular limitations on the amount of oily components contained in the oral composition, but it is preferably 50% by mass or less, more preferably 40% by mass or less, and even more preferably 30% by mass or less, relative to the total mass of the oral composition. When the amount of oily components contained in the oral composition is below the above upper limit, the feeling of use, such as moisturizing and mildness, is further improved. Furthermore, in this invention, in terms of achieving the desired effect, oily components do not need to be included (amount 0% by mass), and the composition may be free of oily components.
[0054] (Preservative) Examples of preservatives include parahydroxybenzoic acid esters (e.g., methyl parahydroxybenzoate, ethyl parahydroxybenzoate, butyl parahydroxybenzoate), sodium benzoate, etc. These preservatives may be used individually or in combination of two or more.
[0055] There are no particular limitations on the amount of preservative contained in the oral composition, but it is preferably 0.001 to 10% by mass, more preferably 0.01 to 5% by mass, and even more preferably 0.1 to 1% by mass, relative to the total mass of the oral composition. If the amount of preservative contained in the oral composition is above the lower limit mentioned above, the preservative power of the oral composition can be further improved.
[0056] (Binding agent) Examples of binders include polysaccharides, cellulosic binders (e.g., carboxymethylcellulose (CMC), hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, methylcellulose, cationized cellulose, etc., and pharmaceutically acceptable salts thereof such as their sodium salts), other polysaccharide thickeners (e.g., xanthan gum, guar gum, gellan gum, tragacanth gum, karaya gum, arabic gum, locust bean gum, carrageenan, sodium alginate, etc.), synthetic water-soluble polymers (e.g., sodium polyacrylate, carboxyvinyl polymer, polyvinylpyrrolidone, polyvinyl alcohol, propylene glycol alginate, etc.), and salts thereof. Furthermore, inorganic binders such as thickening silica, silicates, and anhydrous silicic acid may also be incorporated. These binders may be used individually or in combination of two or more.
[0057] There are no particular limitations on the amount of binder contained in the oral composition, but it is preferably 0.1 to 10% by mass, more preferably 0.3 to 7% by mass, and even more preferably 0.5 to 5% by mass, relative to the total mass of the oral composition. If the amount of binder contained in the oral composition is above the lower limit, the viscosity of the oral composition will be higher, and the shape retention and feel of use can be further improved. If the amount of binder contained in the oral composition is below the upper limit, the viscosity of the oral composition can be prevented from becoming excessively high, and the deterioration of shape retention and feel of use can be further suppressed.
[0058] (pH adjuster) Examples of pH adjusting agents include organic acids such as phthalic acid, citric acid, succinic acid, acetic acid, fumaric acid, malic acid, and lactic acid, or their salts (sodium citrate); inorganic acids such as phosphoric acid (orthophosphoric acid), or their salts (e.g., sodium salts and ammonium salts); and hydroxides such as sodium hydroxide. Examples of inorganic salts include disodium hydrogen phosphate and sodium dihydrogen phosphate. These pH adjusting agents may be used individually or in combination of two or more.
[0059] The amount of pH adjusting agent contained in the oral composition is not particularly limited, as long as the pH of the oral composition after the addition of the pH adjusting agent is at a value that exhibits buffering capacity. The amount of pH adjusting agent can be appropriately set, for example, so that the pH of the oral composition is preferably 5.0 to 9.0, more preferably 5.5 to 8.5. In this disclosure, the pH value usually refers to the value obtained 3 minutes after the start of measurement at 25°C. The pH value can be measured, for example, using a pH meter (model number Hm-30S) manufactured by Toa Denpa Kogyo Co., Ltd.
[0060] (Coloring agent) Examples of colorants include natural pigments such as safflower red pigment, gardenia yellow pigment, gardenia blue pigment, perilla pigment, red yeast rice pigment, red cabbage pigment, carrot pigment, hibiscus pigment, cocoa pigment, spirulina blue pigment, and tamarind pigment; legally approved colorants such as Red No. 2, Red No. 3, Red No. 104, Red No. 105, Red No. 106, Red No. 227, Yellow No. 4, Yellow No. 5, Green No. 3, and Blue No. 1; riboflavin; and titanium dioxide. These colorants may be used individually or in combination of two or more.
[0061] There are no particular limitations on the amount of coloring agent contained in the oral composition, but it is preferably 0.0000001 to 10% by mass, more preferably 0.000001 to 5% by mass, and even more preferably 0.00001 to 3% by mass, relative to the total mass of the oral composition. If the amount of coloring agent contained in the oral composition is above the lower limit of the above, discoloration over time can be masked more effectively.
[0062] (solvent) Preferred solvents include, for example, water (e.g., purified water) and ethanol. These solvents may be used individually or in combination of two or more.
[0063] When the oral composition of the present invention is in paste form, the water content is preferably 10 to 80% by mass, more preferably 15 to 70% by mass, and even more preferably 15 to 65% by mass.
[0064] When the oral composition of the present invention is a liquid oral composition, the water content is preferably 40% by mass or more of the total composition, more preferably 45 to 90% by mass, and even more preferably 50 to 90% by mass.
[0065] When the oral composition of the present invention is a liquid oral composition, the ethanol content is preferably 20% by mass or less of the total composition, and more preferably 8% by mass or less. Alternatively, it may be omitted and 0% by mass.
[0066] (Other optional components) Other optional components include, for example, inorganic compounds such as titanium mica, magnesium oxide, and zirconium oxide; natural polymer compounds such as agar, gelatin, starch, and glucomannan; synthetic polymer compounds or copolymers thereof such as polyvinyl acetate, acrylic resin, polyurethane, polyester, polyvinyl chloride, nylon powder, and polyethylene powder; waxes such as carnauba wax, rosin, rice wax, microcrystalline wax, beeswax, and paraffin wax; higher alcohols such as cetanol and stearyl alcohol; and polyisobutylene, polybutadiene, urethane, silicone, and natural rubber. The content of the above-mentioned other optional components in the oral composition can be appropriately set within a range that does not hinder the effects of the present invention.
[0067] Oral compositions can be adjusted to an appropriate viscosity depending on the dosage form, for example. For oral compositions in paste or gel form, the viscosity at 25°C measured with a BH viscometer is preferably 1 to 300 Pa·s, and more preferably 20 to 150 Pa·s. For oral compositions in liquid form, the viscosity at 25°C measured with a BL viscometer should be 1000 mPa·s or less, and particularly preferably 0.7 to 1000 mPa·s.
[0068] [Form, dosage form] There are no particular limitations on the form of the oral composition; for example, it can be prepared in various forms such as liquid, paste, or solid. There are no particular limitations on the dosage form of oral compositions. Examples include toothpastes (liquid toothpastes, liquid toothpastes, paste toothpastes, moistened toothpastes, powder toothpastes, etc.), mouthwashes, gargles, topical agents, mouth sprays, patches, sheets, oral sustained-release agents, chewing agents, oral dissolving agents, oral disintegrating agents, tongue care agents, mouth fresheners, denture care agents, etc. The dosage forms of the oral composition are preferably toothpaste and mouthwash.
[0069] [Manufacturing method] The oral compositions of this disclosure can be manufactured by known methods. For example, they can be manufactured by conventional methods by mixing components (A), (B), (C) and optional components as described above.
[0070] As described above, the oral composition of this disclosure contains components (A), (B), and (C) in specific proportions, resulting in high astringency, high storage stability, and suppression of unpleasant tastes. [Examples]
[0071] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to the following description. In these examples, "%" refers to "mass%" unless otherwise specified.
[0072] <Raw materials used> [(A) component] Phellodendron bark extract: Manufactured by Ogi Pharmaceutical Co., Ltd., product name "Phellodendron Bark Extract S" (berberine content: 5%) Berberine compound: Manufactured by Alps Pharmaceutical Co., Ltd., product name "Berberine Chloride Hydrate"
[0073] [(B) Component] Potassium nitrate: Manufactured by Wako Pure Chemical Industries, Ltd., product name "Potassium Nitrate" Sodium Chloride: Manufactured by Nippon Kaiyo Co., Ltd., product name "Sodium Chloride"
[0074] [(C) component] Sodium lauroyl methyl taurate: Manufactured by Nikko Chemicals Co., Ltd., product name "LMT-P" Sodium lauroyl glutamate: Manufactured by Ajinomoto Co., Inc., product name "Amisoft (registered trademark) LS-11"
[0075] [(C)´ component] The following surfactants were used as optional anionic surfactants. (Hereafter, these optional anionic surfactants may be referred to as "(C)' component.") Sodium lauryl sulfate: Manufactured by Shin-Nippon Rika Co., Ltd., product name "Sinolin 90TK-T"
[0076] [Optional ingredients] Abrasive silica: Manufactured by Evonik Industries, product name "Zeodent(registered trademark) 113" Thickening silica: DSL Japan Co., Ltd., product name "Carplex® #67" Xanthan gum: MP Gokyo Food & Chemical Co., Ltd., product name "Xanthan gum" Sodium polyacrylate: Manufactured by Toagosei Co., Ltd., product name "Leogic (registered trademark) 260H" Fragrance compositions A to S: The composition of each fragrance composition is shown in Tables 3 and 4 below, and the compositions of flavors 1 to 7 and solvents described in Tables 3 and 4 below are shown in Tables 5 to 12 below.
[0077] <Examples 1-13, Comparative Examples 1-6> Toothpaste compositions were prepared by conventional methods according to the compositions shown in Tables 1 and 2 to obtain the toothpaste compositions of Examples 1 to 13 and Comparative Examples 1 to 6. The values in Tables 1 and 2 represent the content (mass %) of each component relative to the total mass of the toothpaste composition for each example. In Tables 1 and 2, unless otherwise specified, mass percent indicates the purity, and if an ingredient is marked with "-", that ingredient is not included. Also, the "balance" indicated for purified water represents the amount at which the total volume of the toothpaste composition in each example becomes 100% by mass. In Tables 1 and 2, "Berberine (derived from Phellodendron bark extract)" indicates the amount of berberine contained in the Phellodendron bark extract relative to the total mass of the toothpaste composition (mass %).
[0078] <Evaluation Method> The toothpaste compositions of Examples 1-13 and Comparative Examples 1-6 were evaluated for astringency, storage stability, and taste according to the following evaluation method. The results are shown in Tables 1 and 2.
[0079] [Convergence] Each toothpaste composition, filled into an 8mm diameter laminate tube, was evaluated by a sensory test conducted by a panel of 10 experts. After applying 1g of the toothpaste composition to a toothbrush (Lion Corporation, Clinica toothbrush, 4-row head, medium) and brushing for approximately 3 minutes, each subject sensory evaluated the degree of astringency in the oral cavity using the following scoring and evaluation criteria. A score of B or higher was considered a passing grade.
[0080] Rating 4 points: Has a very strong sense of convergence. 3 points: There is a strong sense of convergence. 2 points: There is a slight feeling of astringency. 1 point: There is almost no feeling of astringency.
[0081] Evaluation Criteria A: Average score of 3.5 points or more and 4.0 points or less B: Average score between 3.0 and 3.5 points C: Average score below 3.0
[0082] [Storage stability] Each toothpaste composition, filled into an 8mm diameter laminate tube, was stored in a 50°C constant temperature bath for one month. The separation of the liquid when extruded from the tube onto paper was evaluated according to the following criteria. A result of B or higher was considered acceptable.
[0083] Evaluation Criteria A: No liquid separation was observed. B: Very slight liquid separation was observed (a glossy surface, indicative of separation, was visible), but it was at a level that did not affect the quality. C: Liquid separation was observed.
[0084] [taste] Each toothpaste composition, filled into an 8mm diameter laminate tube, was evaluated by a sensory test conducted by 10 expert panelists. Approximately 1g of toothpaste was placed on a toothbrush (Lion Corporation, Clinica toothbrush, 4-row head, medium), and brushed for 3 minutes. The perceived taste (absence of unpleasant taste) was evaluated sensorily using the following scoring and evaluation criteria. A score of B or higher was considered acceptable. Here, "unpleasant taste" refers to unpleasant tastes such as bitterness felt in the mouth, caused by the saltiness of salts, etc.
[0085] Rating 4 points: No unpleasant taste, just the right amount of sweetness. 3 points: Slightly unpleasant taste, or slightly too sweet, or slightly too sweet, but not to a level that would cause problems with toothpaste use. 2 points: The toothpaste has an unpleasant taste, or is too sweet, or too unsweet, making it unsuitable for use. 1 point: The toothpaste has a strong, unpleasant taste, or is either extremely sweet or extremely weak, making it unsuitable for use.
[0086] Evaluation Criteria A: Average score for bitterness: 3.5 to 4.0 points B: Average score for bitterness is between 3.0 and 3.5 points. C: Average bitterness score below 3.0
[0087] [Table 1]
[0088] [Table 2]
[0089] Tables 1 and 2 show that all of the oral compositions in the examples exhibited excellent evaluations in terms of astringency, storage stability, and taste.
[0090] In contrast, the oral compositions of Comparative Example 1, which did not contain component (A), and Comparative Example 2, which did not contain component (B), were shown to have impaired astringency. In Comparative Example 3, which does not contain component (C), it was shown that liquid separation occurs when the oral composition is stored. It was shown that liquid separation occurs when the oral composition of Comparative Example 4, which has a high AB / C ratio, is stored. Comparative Example 5, an oral composition with a low AB / C ratio, was shown to have a stronger unpleasant taste. In Comparative Example 6, which contains anionic surfactants other than component (C), it was shown that liquid separation occurs when the oral composition is stored.
[0091] <Example prescription> Examples of oral compositions to which the present invention is applied are shown below. In each example, the "%" indicating the content is "mass%". Furthermore, the "balance" indicated for purified water represents the amount that makes the total amount of the oral composition in each example 100% by mass. In the oral compositions of the following formulation examples 1 to 3, the evaluations of astringency, storage stability, and taste were all excellent.
[0092] [Prescription Example 1: Toothpaste] Phellodendron bark extract (berberine content 5%) 0.05% Potassium nitrate 5% Sodium lauroyl methyl taurate 1.0% Sorbitol solution (70%) 45.0% Propylene glycol 4.0% Sodium carboxymethylcellulose 1.5% Xanthan gum 0.6% Abrasive silica 10.0% Thickening silica 5.0% Polyoxyethylene (5) hydrogenated castor oil 1.5% Coconut oil fatty acid amidopropyl betaine solution 0.6% Sodium fluoride 0.32% Sodium saccharin 0.1% Titanium dioxide 0.4% Fragrance composition A 1.2% Purified water balance Total 100%
[0093] [Prescription Example 2: Toothpaste] Phellodendron bark extract (berberine content 5%) 0.05% Potassium nitrate 5% Sodium lauroyl methyl taurate 0.7% Glycerin (85%) 40.0% Propylene glycol 4.0% Sodium carboxymethylcellulose 1.0% Xanthan gum 0.7% Sodium polyacrylate 0.4% Abrasive silica 16.0% Thickening silica 6.0% Polyoxyethylene (5) hydrogenated castor oil 2.0% Coconut oil fatty acid amidopropyl betaine solution 1.0% Sodium lauryl sulfate 0.5% Sodium fluoride 0.32% Sodium saccharin 0.1% Titanium dioxide 0.1% Fragrance composition A 1.2% Purified water balance Total 100%
[0094] [Prescription Example 3: Mouthwash] Phellodendron bark extract (berberine content 5%) 0.05% Potassium nitrate 5% Sodium lauroyl methyl taurate 0.4% Ethanol 8% Sorbitol solution (70%) 7% Propylene glycol 4% Citric acid 0.05% Sodium citrate 0.3% Fragrance composition A 0.2% Purified water balance Total 100%
[0095] Furthermore, when toothpastes or mouthwashes with the same composition as those described in the above formulation examples 1 to 3 were prepared, except that fragrance compositions B to S listed in Tables 3 and 4 below were used instead of fragrance composition A, all of them showed excellent evaluations in terms of astringency, storage stability, and taste. The compositions of flavors 1-7 and solvents listed in Tables 3 and 4 below are shown in Tables 5-12. In the table, "a% cut from the forward distillation portion" means that the initial a% is removed during the fractional distillation of the essential oil, and "b% cut from the forward and backward distillation portions" means that the initial b% and the final b% are removed during the fractional distillation of the essential oil.
[0096] [Table 3]
[0097] [Table 4]
[0098] [Table 5]
[0099] [Table 6]
[0100] [Table 7]
[0101] [Table 8]
[0102] Table 9
[0103] Table 10
[0104] Table 11
[0105] Table 12
Claims
1. (A) Ingredients: Berberine and (B) Components: At least one selected from the group consisting of potassium nitrate and sodium chloride, (C) Components: Contains at least one selected from lauroyl methyl taurate salt and lauroyl glutamate salt, The ratio of the total mass of components (A) and (B) to the mass of component (C), as shown by [component (A) + component (B)] / component (C), is between 0.5 and 13. Oral composition.
2. The content of component (A) is 0.001 to 0.005% by mass relative to the total mass of the oral composition. The oral composition according to claim 1.
3. The content of component (B) is 0.1 to 8.0% by mass relative to the total mass of the oral composition. The oral composition according to claim 1.
4. The content of component (C) is 0.4 to 2.0% by mass relative to the total mass of the oral composition. The oral composition according to claim 1.
5. An oral composition according to any one of claims 1 to 4, which is a toothpaste.