Oral composition

The oral composition with camphor, isopropylmethylphenol, and cocamidopropyl betaine in specific ratios addresses the inadequacy of conventional oral compositions by improving biofilm penetration and sterilization efficacy.

JP7601374B2Active Publication Date: 2024-12-17NIPPON ZETTOC CO LTD
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Patent Information

Application Number
JP2020216090
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2020-12-25
Publication Date
2024-12-17
Estimated Expiration
2040-12-25

AI Technical Summary

Technical Problem

Conventional oral compositions lack sufficient osmotic bactericidal effects against biofilms, making it difficult to penetrate and sterilize bacteria within biofilms effectively.

Method used

An oral composition comprising camphor, a phenolic antibacterial agent (preferably isopropylmethylphenol), and a betaine surfactant (preferably cocamidopropyl betaine) in specific mass ratios, enhancing permeability and bactericidal properties against biofilms.

Benefits of technology

The composition achieves a high penetrating bactericidal effect against biofilms, effectively sterilizing and removing them.

✦ Generated by Eureka AI based on patent content.

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Abstract

To provide a composition for oral cavity having a high penetrating bactericidal action to a biofilm.SOLUTION: There is provided a composition for oral cavity comprising camphor, a phenolic antimicrobial agent and a betaine-based surfactant, wherein the content of the camphor is 0.05 to 5 mass%, the content of the phenolic antimicrobial agent is 0.0005 to 2 mass% and the content of the betaine-based surfactant is 0.01 to 20 mass%. In addition, in the composition for oral cavity, the content of the phenolic antimicrobial agent preferably is 1 / 10000 pts.mass or more and 40 pts.mass or less when the content of the camphor is defined as 1 pt.mass. Further, in the composition for oral cavity, the content of the betaine-based surfactant preferably is 1 / 500 pts.mass or more and 400 pts.mass or less when the content of the camphor is defined as 1 pt.mass.SELECTED DRAWING: None
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Description

[Technical field]

[0001] The present invention relates to an oral composition. [Background technology]

[0002] Biofilms are one of the causes of dental caries and periodontal disease. Biofilms, also known as bacterial membranes, are structures formed by microorganisms such as bacteria. A biofilm is generally a film formed by bacterial aggregates covered with glycocalyx, which is made of exopolysaccharides, attached to the surface of a material. Since biofilms have a barrier function on their surface, it is difficult for antibacterial agents to penetrate deep into the biofilm, and it has been difficult to kill the bacteria inside the biofilm using only conventional antibacterial agents.

[0003] Accordingly, various oral compositions that exhibit a high penetrating effect into biofilms have been developed (see, for example, Patent Documents 1 to 3). Patent Documents 1 to 3 describe preparations that use isopropylmethylphenol as one of the biofilm bactericidal components. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP 2011-098919 A [Patent Document 2] JP 2012-131769 A [Patent Document 3] JP 2013-245187 A Summary of the Invention [Problem to be solved by the invention]

[0005] However, conventional oral compositions have yet to provide a sufficient improvement in their penetrating bactericidal activity against biofilms, and there is a demand for oral compositions with high penetrating bactericidal activity.

[0006] Therefore, an object of the present invention is to provide an oral composition that has a high penetrating bactericidal effect against biofilms. [Means for solving the problem]

[0007] The oral composition according to the present invention comprises camphor and A phenolic antibacterial agent, A betaine surfactant, The camphor content is 0.05 to 5% by mass, The content of the phenol-based antibacterial agent is 0.0005 to 2% by mass, The content of the betaine surfactant is 0.01 to 20% by mass. the law of nature, The phenolic antibacterial agent is isopropyl methylphenol. do.

[0008] In the oral composition according to the present invention, the content of the phenol-based antibacterial agent is preferably 1 / 10,000 to 40 parts by mass when the content of the camphor is 1 part by mass. In the oral composition according to the present invention, the content of the betaine surfactant is preferably 1 / 500 to 400 parts by mass when the content of the camphor is 1 part by mass.

[0009] In the oral composition according to the present invention, the betaine surfactant is preferably cocamidopropyl betaine. In addition, the oral composition according to the present invention is preferably a biofilm inhibitor. Effect of the Invention

[0010] According to the present invention, it is possible to provide an oral composition that has a high penetrating bactericidal effect against biofilms. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0011] Preferred embodiments of the oral composition of the present invention will be described in detail below. The oral composition according to the present invention comprises camphor, a phenol-based antibacterial agent, and a betaine-based surfactant. The oral composition according to the present invention is characterized in that the camphor content is 0.05 to 5 mass %, the phenol-based antibacterial agent content is 0.0005 to 2 mass %, and the betaine surfactant content is 0.01 to 20 mass %. By containing each of the above components in the above-mentioned specified amounts, the permeability into the biofilm is improved, and the biofilm can be effectively sterilized and removed.

[0012] In addition, the oral compositions in this specification include dentifrices such as toothpaste, powdered toothpaste, liquid toothpaste, and liquid toothpaste, as well as lozenges, tablets, creams, ointments, patches, mouthwashes, and chewing gum.

[0013] <Camphor> The oral composition of the present invention contains camphor. Camphor is an ingredient that has effects such as promoting blood circulation, relieving pain, and anti-inflammatory properties. Examples of camphor include d-camphor and dl-camphor, and these can be used alone or in mixtures.

[0014] The camphor content is 0.05 to 5% by mass, preferably 0.1 to 2% by mass, and more preferably 0.3 to 1% by mass, which allows the penetrating bactericidal effect on biofilms to be exerted more effectively.

[0015] <Phenol-based antibacterial agent> The oral composition of the present invention contains a phenolic antibacterial agent. Phenolic antibacterial agents are components that have antibacterial and bactericidal effects against biofilms. Examples of phenol-based antibacterial agents include isopropylmethylphenol, triclosan, hinokitiol, thymol, etc., and these can be used alone or in combination of two or more. Among these, isopropylmethylphenol is preferably used because it has particularly high bactericidal activity against biofilms.

[0016] The content of the phenol-based antibacterial agent is 0.0005 to 2 mass%, preferably 0.01 to 1 mass%, and more preferably 0.02 to 0.1 mass%, which allows the agent to more effectively exert its penetrating bactericidal effect on biofilms.

[0017] When the above-mentioned camphor content is taken as 1 part by mass, the content of the phenol-based antibacterial agent is preferably 1 / 10000 parts by mass or more and 40 parts by mass or less, more preferably 1 / 200 parts by mass or more and 10 parts by mass or less, and even more preferably 1 / 50 parts by mass or more and 1 / 3 parts by mass or less. When the camphor content ratio is within the above range, the permeability of the phenol-based antibacterial agent (particularly isopropyl methylphenol) into the biofilm is increased, and the bactericidal properties against the biofilm can be further improved.

[0018] <Betaine surfactant> The oral composition according to the present invention further contains a betaine surfactant. Betaine surfactants are a type of amphoteric surfactant. Examples of betaine surfactants include cocamidopropyl betaine, lauryl dimethylaminoacetate betaine, lauryl dimethylamine oxide, 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolium betaine, N-lauryl diaminoethyl glycine, N-myristyl diaminoethyl glycine, and N-alkyl-1-hydroxyethyl imidazoline sodium betaine, and one or more of these surfactants can be used in combination. Among these surfactants, it is preferable to use cocamidopropyl betaine. This can further improve the bactericidal activity against biofilms.

[0019] The content of the betaine surfactant is 0.01 to 20% by mass, preferably 0.1 to 10% by mass, and more preferably 0.4 to 5% by mass, which allows the penetrating bactericidal effect on biofilms to be exerted more effectively.

[0020] When the content of camphor is 1 part by mass, the content of the betaine surfactant is preferably 1 / 500 parts by mass or more and 400 parts by mass or less, more preferably 1 / 20 parts by mass or more and 100 parts by mass or less, and even more preferably 2 / 5 parts by mass or more and 50 / 3 parts by mass or less. When the content ratio to camphor is within the above range, the bactericidal property against biofilms can be further improved.

[0021] <Other ingredients> The oral cavity composition of the present invention may contain various ingredients depending on its dosage form, etc. For example, when the oral cavity composition of the present invention is applied to a toothpaste, it may contain abrasives, humectants, binders, foaming agents, sweeteners, preservatives, flavoring ingredients, medicinal ingredients, etc. Examples of the abrasive include silica-based abrasives such as silica gel, precipitated silica, pyrogenic silica, hydrous silicic acid, anhydrous silicic acid, zeolite, aluminosilicate, and zirconosilicate, crystalline cellulose, dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrate, calcium pyrophosphate, tribasic magnesium phosphate, tribasic calcium phosphate, aluminum hydroxide, alumina, light calcium carbonate, heavy calcium carbonate, magnesium carbonate, zirconium silicate, and synthetic resin abrasives, and these can be used alone or in combination of two or more kinds. The amount of the abrasive blended is not particularly limited, but is preferably 3 to 60 mass %, and more preferably 10 to 45 mass %.

[0022] Examples of humectants include polyhydric alcohols such as glycerin, diglycerin, polyglycerin, 1,3-butylene glycol, polyethylene glycol, 1,2-pentanediol, 1,3-hexanediol, propylene glycol, dipropylene glycol, isopropylene glycol, polypropylene glycol, ethylene glycol, diethylene glycol, triethylene glycol, maltitol, reduced starch syrup, lactitol, palatinite, erythritol, sorbitol, mannitol, xylitol, xylose, trehalose, glucose, lactose, mannose, maltose, fructose, inositol, pentaerythritol, maltotriose, starch hydrolyzed sugar, and starch hydrolyzed sugar reduced alcohol, and these can be used alone or in combination of two or more kinds. The blending amount of the wetting agent is not particularly limited, but is preferably from 1 to 60% by mass, and more preferably from 5 to 50% by mass.

[0023] Examples of binders include alginic acid and its derivatives such as carrageenan (ι, λ, κ), alginic acid, sodium alginate, propylene glycol alginate, calcium-containing sodium alginate, potassium alginate, calcium alginate, and ammonium alginate, xanthan gum, guar gum, gelatin, agar, sodium carboxymethylcellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, and sodium polyacrylate, and these can be used alone or in combination of two or more kinds. The blending amount of the binder is not particularly limited, but is preferably 0.1 to 5.0 mass %, and more preferably 0.5 to 3.0 mass %.

[0024] Examples of foaming agents include sodium lauryl sulfate, sodium lauroyl sarcosine, sodium alkyl sulfosuccinate, sodium coconut oil fatty acid monoglycerin sulfonate, sodium α-olefin sulfonate, N-acylamino acid salts such as N-acyl glutamate, maltitol fatty acid esters, sucrose fatty acid esters, glycerin fatty acid esters, fatty acid diethanolamides, polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, polyoxyethylene fatty acid esters, and the like, and one or more of these can be used in combination. The blending amount of the foaming agent is not particularly limited, but is preferably 0.1 to 10.0% by mass, and more preferably 0.5 to 5.0% by mass.

[0025] Examples of sweeteners include saccharin sodium, aspartame, trehalose, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perillartine, and the like, and one or more of these can be used in combination. The amount of the sweetener to be added is not particularly limited, but is preferably 0.005 to 5.0% by mass, and more preferably 0.01 to 3.0% by mass.

[0026] Examples of preservatives include parabens such as methylparaben, ethylparaben, propylparaben, and butylparaben, sodium benzoate, phenoxyethanol, and alkyldiaminoethylglycine hydrochloride, and these can be used alone or in combination of two or more kinds. The amount of the preservative to be added varies depending on the type, etc., but is preferably 0.005 to 5.0% by mass, and more preferably 0.01 to 3.0% by mass.

[0027] As the fragrance component, one or more of 1-menthol, anethole, menthone, cineol, limonene, carvone, methyl salicylate, ethyl butyrate, eugenol, cinnamic aldehyde, trans-2-hexenal, etc. may be used in combination. These components may be blended alone, or essential oils containing them may be used. In addition to the above-mentioned fragrance components, fragrance components such as aliphatic alcohols and their esters, terpene hydrocarbons, phenol ethers, aldehydes, ketones, lactones, and essential oils may be blended within a range that does not impair the effects of the present invention. The blending amount of the above-mentioned fragrances is generally in the range of 0.02 to 2% by mass.

[0028] In addition to the above, the oral cavity composition of the present invention may contain other active ingredients.Such active ingredients include lysozyme chloride, sodium fluoride, potassium fluoride, sodium monofluorophosphate, polyethylene glycol, polyvinylpyrrolidone, zeolite, ascorbic acid, ascorbic acid salts, chlorhexidine salts, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, dequalinium chloride, bisabolol, ascorbic acid and / or its derivatives, tocopherol acetate, ε-aminocaproic acid, tranexamic acid, aluminum hydroxyl allantoin, aluminum lactate, potassium nitrate, dihydrocholesterol, glycyrrhetinic acid, glycyrrhizinate salts, copper chlorophyllin salt, sodium chloride, guaiazulene sulfonate, dextranase, pyridoxine hydrochloride, etc., and one or more of these can be contained.

[0029] In addition to the above-mentioned components, the composition may contain, for example, colorants such as Blue No. 1, pigments such as titanium oxide, antioxidants such as dibutylhydroxytoluene, chelating agents such as edetate, and flavoring agents such as tea extract and tea distillate.

[0030] In addition to the above, the oral composition of the present invention may also contain herbal extracts. Examples of herbal extracts include chamomile extract, valerian extract, jujube extract, hop extract, lamenda extract, linden extract, quince extract, goldenrod extract, kumazasa extract, oleander extract, clove extract, ginseng extract, salvia extract, soapberry extract, platycodon extract, rehmannia extract, peony extract, hawthorn extract, angelica extract, tea extract, oak salicylate extract, bark extract, white birch extract, carrot extract, acacia extract, turmeric extract, and rosemary extract, and one or more of these may be used in combination. In addition to the above-mentioned ingredients, the product may contain, for example, coloring matter such as Blue No. 1, pigments such as titanium oxide, tea dry distillate, flavoring agents such as monosodium glutamate, and the like.

[0031] The oral composition of the present invention can be produced in accordance with a conventional method, and the production method is not particularly limited. The resulting toothpaste or other composition can be filled into an aluminum tube, a laminate tube, a glass-deposited tube, a plastic tube, a plastic bottle, an aerosol container, or the like for use.

[0032] Although the oral composition of the present invention has been described above, the present invention is not limited thereto. For example, in addition to the above-mentioned components, components having any desired functions can be blended into the oral composition of the present invention. EXAMPLES

[0033] Next, specific examples of the present invention will be described. 1. Preparation of oral composition (Examples 1 to 4, Comparative Examples 1 to 8) The components shown in Table 1 were mixed in the amounts shown in Table 1, and liquid oral compositions were produced in the usual manner.

[0034] Table 1 shows the ingredients and amounts thereof for each of the examples and comparative examples. In the table, isopropylmethylphenol is abbreviated as IMP, cetylpyridinium chloride as CPC, and cocamidopropyl betaine as CPB.

[0035] [Table 1]

[0036] 2. Biofilm Penetration Bactericidal Test [Creation of biofilm] Streptococcus mutans JCM5705 was pre-cultured in SCD medium at 32.5°C for 24 hours to obtain a pre-culture solution. The pre-culture solution was diluted to 10 7 The cultured bacteria solution was obtained by adding the bacteria to a 1% sucrose-containing SCD medium so that the concentration was CFU / mL, and 2 mL of the cultured bacteria solution was seeded on a 24-well plate. The seeded cultured bacteria was cultured anaerobically at 37°C for 48 hours to obtain a biofilm.

[0037] [Biofilm penetrating bactericidal test] The prepared biofilm was washed twice with 0.01 mL / L phosphate buffered saline (PBS) to remove floating bacteria. 2 mL of the oral composition of each Example and Comparative Example was added to the biofilm on a 24-well plate, left for 10 minutes, and all the supernatant was removed by sucking. 2 mL of LP dilution was added to the residue and the biofilm was peeled off from the well plate by using an ultrasonic homogenizer. 1 mL of the bacterial liquid containing the peeled biofilm was serially diluted with 9 mL of LP dilution, and 1 mL of the diluted solution of the obtained bacterial liquid was smeared on a TSA medium, and the viable bacterial count was determined by the pour culture method. Here, in the pour culture method, the sample liquid and the agar medium were mixed and solidified in a petri dish, and cultured under aerobic conditions at 32.5 ° C., and the number of colonies generated after culture was measured visually and multiplied by a multiplier to obtain the viable bacterial count.

[0038] The test results are shown in Table 1. As can be seen from the test results of Comparative Examples 1 to 4 in Table 1, no penetrating germicidal effect was observed in the case of cocamidopropyl betaine alone, or in the case of cocamidopropyl betaine combined with dl-camphor or isopropyl methylphenol. On the other hand, as can be seen from the test results of Examples 1 to 4 and Comparative Examples 5 to 8, it was confirmed that the addition of three types of ingredients, dl-camphor, isopropyl methylphenol, and cocamidopropyl betaine, in the amounts specified in the present application exerted a penetrating bactericidal effect. Moreover, as can be seen from the test results of Comparative Example 8, when cetylpyridinium chloride, a cationic bactericide, was used instead of isopropylmethylphenol, no penetrative bactericidal effect was observed.

Claims

1. Camphor and A phenolic antibacterial agent, A betaine surfactant, The camphor content is 0.05 to 5% by mass, The content of the phenol-based antibacterial agent is 0.0005 to 2% by mass, The content of the betaine surfactant is 0.01 to 20% by mass, The oral composition wherein the phenolic antibacterial agent is isopropyl methylphenol.

2. 2. The oral composition according to claim 1, wherein the content of the phenol-based antibacterial agent is 1 / 10,000 part by mass or more and 40 parts by mass or less when the content of the camphor is 1 part by mass.

3. 3. The oral composition according to claim 1, wherein the content of the betaine surfactant is 1 / 500 part by mass or more and 400 parts by mass or less when the content of the camphor is 1 part by mass.

4. 4. The oral composition according to claim 1, wherein the betaine surfactant is cocamidopropyl betaine.

5. The oral composition according to any one of claims 1 to 4, which is a biofilm inhibitor.

Citation Information

Patent Citations

  • Skin care preparation for external use

    JP2005343834A

  • Isopropylmethylphenol-containing liquid oral composition

    JP2011098919A

  • Composition for oral cavity

    JP2012131769A

  • Biofilm inhibitor

    JP2013245187A

  • Oral antiseptic composition for treating oral mucositis

    JP2016507534A