JP2012171879A - Oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide an oral composition excellent in transparency, stability, taste and feeling in use, in which catechins are blended.SOLUTION: The oral composition contains catechins and a nonionic surfactant and has a pH of 2 to 6. Preferably the catechins are gallocatechin, epigallocatechin, catechin, epigallocatechin gallate, epicatechin, gallocatechin gallate, epicatechin gallate or catechin gallate.

Description

  The present invention relates to an oral composition.

  Patients who receive treatment in the intensive care unit are troubled with treatment once they have a respiratory infection, and the length of hospitalization is long. Among them, patients with tracheal intubation cause saliva, exudate, and exhalation to gradually flow into the lower airway through the cuff gap of the tracheal intubation tube and cause ventilator-associated pneumonia. One of the important infection sources of these ventilator-associated pneumonia is the oral cavity, and providing oral care is an important function in preventing the onset of ventilator-associated pneumonia and protecting the infection. Oral care is important not only for patients who receive treatment but also for elderly people and care recipients because of the increase in oral contamination and the causes of death due to pneumonia. By providing oral care to these elderly people and those who need care for the purpose of eating, talking, maintaining respiratory function, and improving their lives, it is also possible to support longevity, that is, to improve QOL (Quality Of Life). It is also an important role in oral care.

  However, oral compositions currently marketed, such as mouthwashes, are mainly highly irritating popidone iodine preparations and preparations containing a large amount of alcohol. On the other hand, it is also a factor that the oral mucosa becomes rough. Accordingly, there is a need for a mouthwash that can control bacteria against pathogenic bacteria, is less irritating, is harmless to the human body, and maintains moisture in the oral cavity.

  Therefore, the present inventors paid attention to catechins that are known to have various physiological activities such as anti-caries, anti-periodontal disease, anti-virus, antibacterial, and deodorant. Conventionally, oral compositions containing catechins have been proposed. However, since catechins have the property of being easily chemically altered, it is difficult to obtain a preparation that ensures stability. Specifically, oxidation / polymerization progresses during storage, and the physiological activity due to catechins decreases, and the problem of stability that turbidity and precipitation are likely to occur is raised. The mouthwash is a sanitary product used in the oral cavity, and is a dosage form that does not recognize foreign matter, that is, transparency is required. It is also advantageous that a transparent formulation is not noticeable when it remains in the oral cavity. In addition, oral compositions containing catechins have bitterness and astringency with respect to taste, and have a problem with usability.

  As a method of stabilizing catechins in oral compositions containing catechins or beverages containing catechins, organic acids such as ascorbic acid, oxalic acid, and glutamic acid are blended to suppress the effect on taste and stabilize Methods (for example, Patent Documents 1 to 3), polysaccharides such as dextrin and xanthan gum are blended to suppress the influence on taste and stabilize (for example, Patent Documents 4 and 5), and taurine is blended. And a method that suppresses the influence on the taste and stabilizes the taste (for example, Patent Document 6). Patent Documents 1, 2, and 6 describe that, in addition to each essential component, a known additive such as a fragrance, a sweetener, a colorant, and a surfactant can be added as desired. Also in this example, a composition containing a surfactant is not disclosed.

  As a composition containing catechins and a surfactant, an antibacterial detergent composition (patent document 7) containing catechins and a surfactant (cationic, amphoteric or nonionic), catechins and nonionics A cleaning composition containing a surfactant (Patent Document 8) and a tea extract-containing mouthwash (Patent Document 9) in which a surfactant and an organic acid are added to catechins are known. Patent Document 7 discloses that the pH of the antibacterial detergent composition is preferably from a neutral region to an alkaline region from the viewpoint of antibacterial properties, and specifically, pH 7.5 to 9.0 is preferable. (Paragraph [0023]). In Patent Document 8, the cleaning composition is applied to, for example, a pet shampoo for the purpose of cleaning pet skin or body hair, or a tableware cleaning agent for cleaning tableware or cooking utensils. Is preferred (paragraph [0019]) and is not intended for oral use.

Japanese Patent No. 4188326 JP 2009-215183 A JP 2008-11834 A JP 2008-118873 A JP 2010-64961 A JP 2008-22754 A JP 2008-195917 A JP 2007-112825 A Japanese Patent Laid-Open No. 7-258054

  An object of the present invention is to provide an oral composition containing catechins which eliminates the above-mentioned drawbacks of the prior art and is excellent in transparency, stability, taste, and feeling of use.

  As a result of intensive studies aimed at solving the above-mentioned problems, the present inventor has found that the catechins have a bitter taste, astringency by blending a predetermined amount of a nonionic surfactant even if a large amount of catechins is blended. It has been found that an oral composition having excellent stability for maintaining the transparency can be obtained even in long-term storage with reduced taste and astringent taste.

The present invention
[1] A composition for oral cavity comprising catechins and a nonionic surfactant and having a pH of 2 to 6.
[2] The oral composition of [1], wherein the catechins are epigallocatechin, catechin, epigallocatechin gallate, epicatechin, gallocatechin gallate, epicatechin gallate, or catechin gallate,
[3] The oral composition of [1] or [2], wherein the nonionic surfactant is polyoxyethylene hydrogenated castor oil.

  ADVANTAGE OF THE INVENTION According to this invention, although it contains catechins in high concentration, the composition for oral cavity excellent in storage stability and taste can be provided.

It is a graph which shows the result of the bacteriostatic effect test with respect to methicillin resistant Staphylococcus aureus (MRSA) of the composition for oral cavity by this invention. It is a graph which shows the result of the bacteriostatic effect test with respect to Pseudomonas aeruginosa of the composition for oral cavity by this invention.

  The catechins used in the present invention are not particularly limited as long as they have physiological activities useful for oral care, such as anti-caries, anti-periodontal disease, anti-virus, antibacterial, deodorant, etc. Catechins described in JP-A-2007-112825, for example, can be used.

  The catechins include monomeric catechins and low polymer catechins, and are contained in various plants such as tea, persimmons, and apples. Specific examples of plants include Camellia family plants such as tea, grape family plants such as grapes, Akane family plants such as coffee, Aogiri family plants such as cacao, Tade family plants such as buckwheat, Gooseberry, Blackcurrant, Akasuguri Plants, azaleas such as blueberries, white berries, black hackleberries, cranberries and bilberries, grasses such as red rice and purple corn, mulberry plants such as mulberry, honeysuckle such as elderberries and black mullet Rosaceae, plum, European Blackberry, Loganberry, Salmonberry, Ezo strawberry, Atlantic strawberry, White strawberry, Dutch strawberry, Black strawberry, Morello cherry, Yoshino cherry, Western cherry, Sakura, Apple, etc. ,soy Tamarind, Mimosa, include legumes such Peguasen'yaku, fruits depending on these plants, pericarp, flowers, leaves, stems, bark, roots, tubers, seeds, portions of the seed coat and the like are arbitrarily chosen.

  Catechins obtained by extraction from these are highly safe for human bodies and animals, and are therefore used in antioxidants, functional foods, health foods, processed foods, pharmaceuticals, feeds, cosmetics, and the like. Although it does not specifically limit, The catechin obtained by extracting from the tea which is a camellia is especially preferable. The catechins obtained by extraction from tea include (+)-gallocatechin, (−)-epigallocatechin, (+)-catechin, (−)-epigallocatechin gallate, (−)-epicatechin, (− ) -Gallocatechin gallate, (−)-epicatechin gallate, (−)-catechin gallate, and polymers thereof, one or a mixture of two or more selected from stereoisomers.

  The method for obtaining a purified product containing catechins from tea is not particularly limited. For example, a fraction obtained by pulverizing tea with water or hot water or an alcohol such as glycerin or ethanol, or It can be obtained from an ethyl acetate or acetone fraction obtained by adding ethyl acetate or acetone to a fraction extracted with water or hot water or an alcohol such as glycerin or ethanol. Or you may esterify with alcohol, saccharides, etc. by a conventional method.

Further, the purity of catechins in the extract is not particularly limited, and is preferably 20% by weight or more, more preferably 60% by weight or more, and further preferably 80% by weight or more. Its purity can be measured by high performance liquid chromatography.
In addition, Sanphenon (manufactured by Taiyo Kagaku Co., Ltd.), Theafranc (manufactured by ITO EN), Oolong tea extract M (manufactured by Maruzen Pharmaceutical Co., Ltd.), polyphenon (manufactured by Mitsui Norin Co., Ltd.), Theavigo (manufactured by Mitsui Norin Co., Ltd.), etc. Commercially available catechin-containing materials can also be used. In particular, Sanphenon EGCg (manufactured by Taiyo Kagaku Co., Ltd.) is preferable because it contains 90% or more of high-potency epigallocatechin gallate among catechins.

  The nonionic surfactant used in the present invention has no safety problem when used as a component of an oral composition, and preferably has excellent taste such as bitterness and astringency and a feeling of use. If it is, it will not specifically limit, Various nonionic surfactants, for example, the nonionic surfactant of Unexamined-Japanese-Patent No. 2008-195917 can be used.

Examples of nonionic surfactants include:
(Mono, di, tri) glycerin fatty acid esters such as glyceryl monostearate and glyceryl monooleate;
Polyglyceryl fatty acid esters such as polyglyceryl monostearate and polyglyceryl monolaurate;
Sorbitan fatty acid esters such as sorbitan monostearate and sorbitan tristearate;
Polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan trioleate;
Polyoxyethylene sorbit fatty acid esters such as tetraoleic acid polyoxyethylene sorbit, tetrastearic acid polyoxyethylene sorbit;
Polyoxyethylene hydrogenated castor oil;
Polyoxyethylene alkyl ethers such as polyoxyethylene lauryl ether and polyoxyethylene oleyl ether;
Polyoxyalkylene alkyl ethers;
Polyoxyethylene polyoxypropylene alkyl ethers such as polyoxyethylene polyoxypropylene cetyl ether and polyoxyethylene polyoxypropylene decyl tetradecyl ether;
Polyethylene glycol fatty acid esters such as polyethylene glycol monostearate and polyethylene glycol monolaurate;
Alkyl alkanolamides;
Etc. You may use these individually or in combination of 2 or more types.

  Among these nonionic surfactants, polyoxyethylene hydrogenated castor oil, which is preferably a highly safe oligomer type nonionic surfactant, is used. The polyoxyethylene hydrogenated castor oil is preferably a polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 5 to 100 mol, and a polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 40 to 80 mol. More preferably, for example, NIKKOL HCO-60 (Nikko Chemicals Co., Ltd./Nihon Surfactant Kogyo Co., Ltd.) is particularly preferred.

  The oral composition of the present invention has a pH of 2 to 6, preferably 3 to 5, and more preferably 4.0 to 4.9. When pH exceeds 6, when the composition for oral cavity of this invention is preserve | saved, stability of catechin will fall rapidly.

  The content of catechins contained in the oral composition of the present invention is not particularly limited as long as it is an amount that does not cause precipitation immediately after dissolution or during storage as an oral composition. However, it can be, for example, 0.01 to 3% by weight, preferably 0.05 to 2% by weight, more preferably 0.1 to 1% by weight, still more preferably 0.2 to 0.8% by weight, particularly preferably 0.4 to 0.6% by weight.

  The content of the nonionic surfactant contained in the oral composition of the present invention is not particularly limited as long as it is an amount that does not cause precipitation immediately after dissolution or during storage as an oral composition. For example, it may be 0.1 to 60% by weight, preferably 0.4 to 40% by weight, more preferably 0.5 to 30% by weight, and still more preferably It is 2 to 20% by weight, particularly preferably 3.2 to 12% by weight.

  In the oral composition of the present invention, the compounding ratio of the nonionic surfactant to the catechins can be, for example, 5 to 30 times, preferably 8 to 20 times, and more preferably 10 to 14 times. Is double. If it is less than 8 times, precipitation may occur, and if it exceeds 20 times, it is not preferable in terms of taste and cost.

  The composition for oral cavity of the present invention is not only a type that is used as it is, but also a type that is diluted at the time of use, a gel-type oral application, a spray-type spray, a mixture with a dentifrice Good. The oral composition of the present invention can be provided in various dosage forms such as mouthwash, mouthwash, oral gel, oral rinse, oral spray, dentifrice and the like.

  In addition to catechins and nonionic surfactants as essential components, the oral composition of the present invention includes additives that can be generally used in oral compositions, such as thickeners, humectants, and pH adjustments. Solvents, stabilizers, preservatives, fragrances, sweeteners, water, alcohols and other solvents can be added within a range that does not impair the stability of the preparation. Although a specific example is shown below, the component which can be mix | blended with the mouthwash of this invention is not restrict | limited to these. Examples of the thickener include gelatin, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, sodium carboxymethylcellulose, pullulan, cyclodextrin, xanthan gum, gum arabic, tragacanth gum, guar gum, locust bean gum, konjac mannan, dextrin, Examples thereof include carrageenan, agar, alginic acid, sodium alginate, polyvinyl alcohol, polyvinyl pyrrolidone, carboxyvinyl polymer, sodium polyacrylate and the like. Examples of the humectant include plant extract extracts such as glycerin, diglycerin, butylene glycol, propylene glycol, polyethylene glycol, sodium hyaluronate, sodium chondroitin sulfate, chitosan, collagen, betaine, and aloe extract. Examples of pH adjusters include citric acid or a salt thereof (such as sodium citrate), phosphoric acid or a salt thereof (such as sodium phosphate or sodium hydrogen phosphate), malic acid or a salt thereof, gluconic acid or a salt thereof, lactic acid or a salt thereof Examples thereof include salts, hydrochloric acid, acetic acid, nitric acid, sodium hydroxide, potassium hydroxide and the like. Examples of the stabilizer include gluconic acid, tartaric acid, edetic acid, sodium edetate, ascorbic acid, sodium ascorbate, erythorbic acid, sodium erythorbate and the like. Examples of the preservative include paraoxybenzoic acid ester, methylparaben, ethylparaben, propylparaben, butylparaben, benzoic acid, sodium benzoate, ethylenediaminetetraacetate, benzalkonium chloride, phenoxyethanol, cetylpyridinium chloride and the like. Examples of flavors include peppermint oil, rosemary oil, chamomile oil, zage oil, lavender oil, lemon oil, orange oil and other essential oils, l-menthol, carvone, eugenol, anethole, linalool, farnesol, limonene, citral, cineol. And perfume materials such as linalyl acetate, citronellol, vanillin, α-terpineol, methyl salicylate, and thymol. Examples of the sweetening agent include saccharin sodium, stevioside, dipotassium glycyrrhizinate, sorbitol, mannitol, xylitol, maltitol, erythritol and the like.

  EXAMPLES Hereinafter, the present invention will be specifically described by way of examples, but these do not limit the scope of the present invention.

<< Example 1: Bacteriostatic efficacy test >>
In this example, using methicillin-resistant Staphylococcus aureus (MRSA) IID 1677 and Pseudomonas aeruginosa NBRC 13275, which are important as infection-causing bacteria in intensive care patients, The bacteriostatic efficacy test of the oral composition of the present invention was performed according to the following procedure. The composition of the composition for oral cavity of the present invention used in this example (polyoxyethylene hydrogenated castor oil-containing catechin aqueous solution; Example A) and the comparative catechin aqueous solution (not including nonionic surfactant; comparison) The composition of Example a) is shown in Table 1. As catechins, a green tea extract containing 90% or more of epigallocatechin gallate (Sunphenon EGCg; manufactured by Taiyo Kagaku Co., Ltd.) is used, and polyoxyethylene hydrogenated castor oil has an average added mole number of ethylene oxide of 60. A certain thing (NIKKOL HCO-60; Nikko Chemicals Co., Ltd./Nihon Surfactant Kogyo Co., Ltd.) was used.

<Table 1>
Example A Comparative Example a
Catechins (epigallocatechin gallate) 0.5% 0.5%
Polyoxyethylene hydrogenated castor oil 60 6.0% −
Concentrated glycerin 15.0% −
Fragrance 0.2% −
Sodium edetate 0.2% −
Xylitol 0.5% −
Citric acid 0.05% −
Carrageenan 0.3% −
Methylparaben 0.3% −
Sodium benzoate 0.1% −
Purified water 76.85% 99.5%
Total 100.0% 100.0%

MRSA and Pseudomonas aeruginosa were prepared to about 10 ⁷ CFU (colony forming unit) / mL, respectively, and used as test bacterial solutions. Further, 5 w / v% of a commercially available powder medium (ordinary bouillon medium; Eiken Chemical) was added to each catechin aqueous solution shown in Table 1 to prepare a test solution. Each test bacterial solution 0.1 mL and each test solution 10 mL were mixed and then allowed to stand at 36 ± 2 ° C., and the number of bacteria was measured immediately after mixing, 8 hours later, and 24 hours later. For neutralization (inactivation) of the test bacterial solution for measuring the number of bacteria, SCDLP bouillon medium (Eiken Chemical Co., Ltd.) was used for 100-fold dilution. As a control, the same operation was performed using purified water added with 5% w / v of the normal bouillon medium.

  The results are shown in FIG. 1 (MRSA) and FIG. 2 (Pseudomonas aeruginosa). 1 and 2, the broken line A shows the results of Example A, the broken line B shows the results of Comparative Example a, and the broken line C shows the results of the control. The oral composition of the present invention has reduced bitterness, astringency, and astringency compared to a simple catechin aqueous solution (see Example 2 described later), and the transparency of the solution is maintained even during long-term storage. (See Example 3), the bacteriostatic efficacy against MRSA is not different from the catechin aqueous solution, and the bacteriostatic efficacy against Pseudomonas aeruginosa is superior to the catechin aqueous solution. Turned out to show.

<< Example 2: Taste test >>
In this example, the composition for oral cavity of the present invention comprising the composition shown in Table 2 (polyoxyethylene hydrogenated castor oil-containing catechin aqueous solution; Example B) and a comparative catechin aqueous solution (nonionic surfactant) Not included; Comparative Example b) was prepared and a taste test was conducted with 10 subjects. The results are shown in Table 2.

<Table 2>
Example B Comparative Example b
Catechins (epigallocatechin gallate) 0.5% 0.5%
Polyoxyethylene hydrogenated castor oil 60 6.0% −
Methylparaben 0.3% 0.3%
Purified water 93.2% 99.2%
Total 100.0% 100.0%

Bitter taste 0 people 10 people
There is astringency 0 people 10 people
Astringent taste 0 people 10 people

<< Example 3: Stability test >>
In this example, the composition for oral cavity of the present invention comprising the compositions shown in Table 1 and Examples 3 and 3 (polyoxyethylene hydrogenated castor oil-containing catechin aqueous solution; Examples C and D), catechin for comparison After preparing an aqueous solution (not containing a nonionic surfactant; Comparative Example c), each was transferred to a vial, sealed with a plastic lid, and allowed to stand at room temperature, 5 ° C, 40 ° C for 1 month, The state of the aqueous solution was observed. The results are shown in Table 4.

<< Table 3 >>
Example C Example D Comparative Example c
Catechin 0.5% 0.5% 0.5%
(Epigallocatechin gallate)
Polyoxyethylene hydrogenated castor oil 60 4.0% 5.0% −
Concentrated glycerin 15.0% 15.0% 15.0%
Perfume 0.2% 0.2% 0.2%
Sodium edetate 0.2% 0.2% 0.2%
Xylitol 0.5% 0.5% 0.5%
Citric acid 0.05% 0.05% 0.05%
Carrageenan 0.3% 0.3% 0.3%
Methylparaben 0.3% 0.3% 0.3%
Sodium benzoate 0.1% 0.1% 0.1%
Purified water 78.85% 77.85% 82.85%
Total 100.0% 100.0% 100.0%

<< Table 4 >>
Example A Example D Example C Comparative Example c
Catechin 0.5% 0.5% 0.5% 0.5%
(Epigallocatechin gallate)
Polyoxyethylene hydrogenated castor oil 60 6.0% 5.0% 4.0% −

Immediately after preparation Dissolved transparently Dissolved transparently Dissolved transparently Dissolved transparently 1 month (room temperature) As it was transparent As it was transparent As it was transparent As a transparent material 1 month later (5 ° C) Crystalline precipitation
1 month later (40 ° C) remains transparent, remains transparent, changes to opaque, changes to brown

<< Example 4: pH stability test >>
In this example, in order to evaluate the stability at different pH, the composition for oral cavity of the present invention (Examples A and E) having the composition shown in Table 5 and the composition for oral cavity for comparison (Comparative Example d). E) were prepared, transferred to vials, sealed with a plastic lid, allowed to stand at room temperature or 50 ° C. for 1 week, and the state of the aqueous solution was observed. The results are shown in Table 5.

<< Table 5 >>
Example E Example A Comparative Example d Comparative Example e
Catechin 0.5% 0.5% 0.5% 0.5%
(Epigallocatechin gallate)
Polyoxyethylene hydrogenated castor oil 60 6.0% 6.0% 6.0% 6.0%
Concentrated glycerin 15.0% 15.0% 15.0% 15.0%
Perfume 0.2% 0.2% 0.2% 0.2%
Sodium edetate 0.2% 0.2% 0.2% 0.2%
Xylitol 0.5% 0.5% 0.5% 0.5%
Citric acid 1.6% 0.05% 0.05% 0.05%
Sodium citrate-6.0% 18.0%
Carrageenan 0.3% 0.3% 0.3% 0.3%
Methylparaben 0.3% 0.3% 0.3% 0.3%
Sodium benzoate 0.1% 0.1% 0.1% 0.1%
Purified water 75.3% 76.85% 70.85% 58.85%
Total 100.0% 100.0% 100.0% 100.0%

pH 2.5 4.5 6.5 6.8
Immediately after preparation Dissolved transparently Dissolved transparently Dissolved transparently One week later (room temperature)
After 1 week (50 ° C)

  The oral composition of the present invention can be used for oral care applications.

Claims (3)

  An oral composition comprising catechins and a nonionic surfactant and having a pH of 2-6.   The oral composition according to claim 1, wherein the catechin is gallocatechin, epigallocatechin, catechin, epigallocatechin gallate, epicatechin, gallocatechin gallate, epicatechin gallate, or catechin gallate.   The composition for oral cavity of Claim 1 or 2 whose nonionic surfactant is polyoxyethylene hydrogenated castor oil.

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