JP2011073970A - Composition for oral cavity or throat - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a composition for oral cavity or throat, which masks peculiar bitterness of components and has a good taste even if mixed with cetylpyridinium chloride, benzethonium chloride and benzalkonium chloride. <P>SOLUTION: The composition for oral cavity or throat has reduced peculiar bitterness of cetylpyridinium chloride, etc., is obtained by mixing a composition comprising cetylpyridinium chloride, benzethonium chloride and benzalkonium chloride with hesperidin. The composition for oral cavity or throat has the enhanced effects of components by further mixing the composition with one or more kinds of polyhydric alcohols selected from glycerol, polyethylene glycol, propylene glycol and 1,3-butylene glycol. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  The present invention relates to a composition for oral cavity or throat with reduced bitterness peculiar to cationic fungicides such as cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride and the like.

  Conventionally, it is known that cationic bactericides such as cetylpyridinium chloride, benzethonium chloride, and benzalkonium chloride have strong bactericidal and antibacterial effects. For this reason, attempts have been made to blend the antibacterial agent into oral or throat compositions. When aiming at prevention of periodontal disease and dental caries disease, the composition for oral cavity has a sufficient effect even if the concentration of cetylpyridinium chloride or the like is low. However, for the purpose of advanced prevention and treatment for those who are at high risk of dental diseases and those suffering from diseases, higher plaque control power is required, and cetylpyridinium chloride and the like need to be blended at a high concentration.

  On the other hand, bacteria in the oral cavity, particularly those attached to the throat, are known to adversely affect the whole body. For example, it has been reported that when swallowing function and resistance decrease, bacteria in the oral cavity flow into the lungs from the trachea as a result of swallowing, causing opportunistic infections and pneumonia. In such a case, it is known that it is effective to sterilize the throat accurately, and for this purpose, a composition for the throat containing an antibacterial agent at a high concentration is required. However, cationic fungicides such as cetylpyridinium chloride have a unique bitter taste, and particularly when cetylpyridinium chloride is blended in a composition for oral cavity at a high concentration, the taste is very bad. Therefore, in order to improve the taste of oral compositions containing cationic fungicides such as cetylpyridinium chloride, attempts have been made to add various components.

  For example, a technique for reducing the bitter taste derived from a quaternary ammonium salt type cationic antibacterial agent containing cetylpyridinium chloride by blending tranexamic acid and / or ε-aminocaproic acid and a stevia sweetener (Patent Document 1), Technology to reduce bitterness derived from quaternary ammonium salt type cationic antibacterial agent by combining sodium chloride and magnesium chloride (Patent Document 2) Bitterness derived from cationic surfactant containing cetylpyridinium chloride The technique (patent document 3) etc. which reduce by mixing | blending is mentioned. However, even with these techniques, the bitter taste of cetylpyridinium chloride could not be reduced sufficiently.

JP 05-000931 A Japanese Patent Laid-Open No. 09-095457 JP 2001-072562 A

  The present invention provides an oral or throat composition having a good taste and masking the unique bitterness even when cetylpyridinium chloride, benzethonium chloride and benzalkonium chloride are blended. Objective.

  As a result of intensive studies to solve the above problems, the present inventors have found that the unique bitterness such as cetylpyridinium chloride is reduced by blending hesperidin which is surprisingly tasteless and odorless, and the present invention. It came to complete.

That is, the present invention includes the following aspects.
Item 1. An oral or pharyngeal composition comprising one or more cationic fungicides selected from cetylpyridinium chloride, benzethonium chloride, and benzalkonium chloride and hesperidin.
Item 2. Item 2. The composition for oral cavity or pharynx according to Item 1, wherein the compounding amount of the cationic fungicide is 0.01 to 0.3% by mass.
Item 3. Item 3. The composition for oral cavity or pharynx according to any one of Items 1 and 2, wherein the amount of hesperidin is 0.01 to 0.2% by mass.
Item 4. Item 4. The oral or pharyngeal composition according to any one of Items 1 to 3, wherein the cationic bactericidal agent is cetylpyridinium chloride.
Item 5. The composition for oral cavity or pharynx according to any one of Items 1 to 4, further comprising one or more polyhydric alcohols selected from glycerin, polyethylene glycol, propylene glycol, and 1,3-butylene glycol. .

  ADVANTAGE OF THE INVENTION According to this invention, the composition for oral cavity or throat with a good taste by which the bitterness peculiar to cationic type fungicides, such as cetyl pyridinium chloride, benzethonium chloride, and benzalkonium chloride was masked is provided.

  The present invention will be described in further detail.

  The cetylpyridinium chloride, benzethonium chloride, and benzalkonium chloride used in the present invention are not particularly limited as long as they can be used for pharmaceuticals and cosmetics. The effect is recognized when the blending amount is 0.3% by mass or less. In particular, cetylpyridinium chloride is preferable because it has a remarkable effect even at a high concentration of 0.05 to 0.3% by mass as compared with other cationic fungicides.

  Hesperidin used in the present invention may be any product obtained as a synthetic product or a natural product-derived product. Hesperidin is the one in which rutinose (L-rhamnosyl- (α1 → 6) -D-glucose) is β-bonded to the hydroxyl group at position 7 of hesperetin (5,7,3′-trihydroxy-4′-methoxyflavanone). It is. This hesperidin is a kind of flavanones among flavonoids, and those extracted and isolated from citrus peels such as Citrus unshiu and orange (Citrus aurantium L) can be used. In addition, hesperidin is considered to have little direct effect on the cell itself because hesperidin hardly suppresses degranulation of basophil cells and weakly affects colon cell function compared to other flavonoids. Therefore, there is no worry about side effects. Hesperidin used in the present invention is commercially available from Wako Pure Chemical Industries, Ltd. (trade name “Hesperidin”) and the like. The hesperidin used in the present invention is not limited to those comprising glycosides in which hesperetin is aglycone and sugar is bound to this, and hesperidin sugar adducts to which sugars such as glucose, maltose, fructose, rhamnose, and lactose are further bound. included. For example, the hesperidin sugar adduct is commercially available from Toyo Seika Co., Ltd. (trade name “αG-Hesperidin PA-T”). Although the compounding quantity of hesperidin is not specifically limited, it is 0.01-0.2 mass%, and 0.05-0.1 mass% is preferable from a viewpoint of an effect. If it is added more than 0.2% by mass, a large amount of insoluble hesperidin may cause discomfort in the oral cavity, which is not preferable. On the other hand, if it is less than 0.01% by mass, the desired effect may not be obtained, which is not preferable.

  In the present invention, one or more polyhydric alcohols selected from glycerin, polyethylene glycol, propylene glycol, and 1,3-butylene glycol can also be used. Of these, glycerin and polyethylene glycol are preferred because they can improve the flavor. As a compounding quantity of a polyhydric alcohol, it is 1-20 mass%, 1-15 mass% is preferable, and 3-10 mass% is more preferable.

  The composition for oral cavity or throat of the present invention is a toothpaste, liquid toothpaste, liquid toothpaste, mouthwash, mouse spray, coating agent, throat spray, prophy paste, pasta, drop, chewing gum, tablet, mouthwash, oral cavity It can be prepared in the form of an ointment for use. Among these forms, a liquid form is preferable, and a liquid dentifrice, a liquid dentifrice, a mouthwash, a mouth spray, a throat spray, and a mouthwash are particularly preferable. The composition of these forms can be prepared according to a conventional method by blending various known components according to each form in addition to the above-described components.

  In the composition for oral cavity or throat of the present invention, any components such as a surfactant, a binder, a wetting agent, an abrasive, a preservative, a sweetener, a flavoring agent, and an effective ingredient are used as long as the effects of the present invention are not impaired. Ingredients, pH adjusters and the like can be blended.

  Examples of the surfactant include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, acyl sarcosinates such as sodium lauroyl sarcosinate and sodium myristyl sarcosinate, acyl glutamate, palmitoyl glutamate, N-methyl- N-acyl taurine salts, acyl amino acid salts such as N-methyl-N-acylalanine salts, anionic surfactants such as coconut fatty acid monoglyceride monosulfate, lauryl sulfoacetate, α-olefin sulfonate, sucrose fatty acid Sugar fatty acid esters such as esters, maltose fatty acid esters and lactose fatty acid esters, sugar alcohol fatty acid esters such as maltitol fatty acid esters and lactitol fatty acid esters, polyoxyethylene sorbitan Laurate, polyoxyethylene sorbitan fatty acid ester such as polyoxyethylene sorbitan monostearate, polyoxyethylene fatty acid ester such as polyoxyethylene glycol laurate, mono- or di-ethanolamide of lauric acid, mono- or di of myristic acid -Nonionic surfactants such as fatty acid diethanolamide such as ethanolamide, polyoxyethylene polyoxypropylene copolymer, polyoxyethylene polyoxypropylene fatty acid ester, polyoxyethylene hydrogenated castor oil, alkylglycoside, polyglycerin fatty acid ester N-alkyldiaminoethylglycine such as N-lauryldiaminoethylglycine and N-myristyldiaminoethylglycine, fatty acid amidopropyl Examples include amphoteric surfactants such as betaine-type surfactants such as betaine, alkylbetaine imidazolinium betaine, and alkylsulfobetaine. These surfactants may be used alone or in combination of two or more. The compounding quantity is 0.01-20 mass% normally with respect to the whole composition.

  Examples of the binder include cellulose derivatives such as sodium carboxymethyl cellulose, hydroxyethyl cellulose, and hydroxypropyl methyl cellulose; gums such as propylene glycol alginate, tragacanth gum, caraya gum, gum arabic, and carrageenan; polyvinyl alcohol, sodium polyacrylate, carboxy Synthetic binders such as vinyl polymer and polyvinyl pyrrolidone are listed. These binders may be used alone or in combination of two or more. The compounding quantity is 0.3 to 10 mass% normally with respect to the whole composition.

  Examples of the wetting agent include sorbit, ethylene glycol, polypropylene glycol, xylite, maltite, lactit, and paratinite. These wetting agents may be used alone or in combination of two or more. The compounding quantity is 5 to 70 mass% normally with respect to the whole composition.

  Examples of the abrasive include calcium carbonate, calcium phosphate, dicalcium phosphate, calcium pyrophosphate, insoluble sodium metaphosphate, titanium oxide, amorphous silica, crystalline silica, abrasive silica, thickening silica, aluminosilicate, aluminum oxide, Examples thereof include titanium oxide, aluminum hydroxide, resin, and hydroxyapatite. These abrasives may be used alone or in combination of two or more. The compounding quantity is 0.01-30 mass% normally with respect to the whole composition.

  Examples of the preservative include parabens such as methylparaben, ethylparaben, propylparaben, and butylparaben, sodium benzoate, phenoxyethanol, and alkyldiaminoethylglycine hydrochloride. These preservatives may be used alone or in combination of two or more. The compounding quantity is 0.001-0.5 mass% normally with respect to the whole composition.

  Examples of the sweetening agent include saccharin sodium, acesulfame potassium, stevioside (stevia extract), neohesperidyl dihydrochalcone, glycyrrhizin, perilartin, thaumatin, α-L-aspartyl-L-phenylalanine methyl ester, methoxycinnamic aldehyde, xylit Etc. These sweeteners may be used alone or in combination of two or more. The amount is usually 0.01 to 1% by mass, preferably 0.05 to 0.5% by mass, based on the entire composition.

  As a flavoring agent, for example, menthol, carvone, eugenol, methyl salicylate, methyl eugenol, thymol, anethole, limonene, ocimene, n-decyl alcohol, citronell, α-terpineol, methyl acetate, citronenyl acetate, cineol, Linalool, ethyl linalool, crocodile, thyme, nutmeg, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, pimento oil, Tea tree oil, Davana oil, etc. are mentioned. These flavoring agents may be used alone or in combination of two or more. The compounding quantity is 0.1-5 mass% normally with respect to the whole composition, Preferably it is 0.5-2 mass%.

  Active ingredients include, for example, vitamin Es such as dl-α-tocopherol acetate, tocopherol succinate or tocopherol nicotinate, amphoteric fungicides such as dodecyldiaminoethylglycine, and nonionic fungicides such as triclosan and isopropylmethylphenol Enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme (lytechenzyme), alkali metal monofluorophosphates such as sodium monofluorophosphate and potassium monofluorophosphate, sodium fluoride, fluoride Fluorides such as stannous, tranexamic acid, epsilon aminocaproic acid, aluminum chlorohydroxy allantoin, dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, glycerophosphine Over DOO, chlorophyll, sodium chloride, Karopeputaido, like water-soluble inorganic phosphoric acid compounds. These medicinal components may be used alone or in combination of two or more. The blending amount of these components can be a normal amount within a range not impeding the effects of the present invention.

  Examples of the pH adjuster include citric acid, phosphoric acid, malic acid, pyrophosphoric acid, lactic acid, tartaric acid, glycerophosphoric acid, acetic acid, nitric acid, silicic acid, or a chemically possible salt or sodium hydroxide thereof. It is done. These may be used alone or in combination of two or more so that the pH of the composition is usually in the range of 5-9. The compounding quantity is 0.01 to 2 weight% normally with respect to the whole composition.

  EXAMPLES Hereinafter, although an Example and a comparative example are shown and this invention is demonstrated concretely, this invention is not limited to the following Example. In addition, the compounding quantity in each example shows the mass% unless there is special prescription | regulation.

<Bitter taste suppression evaluation>
Examples 1-4 and Comparative Examples 1-4 shown in Table 1 were used as samples for evaluation. Evaluation was performed by relative evaluation of Examples and Comparative Examples that differed only in the presence or absence of hesperidin. The scoring was performed according to the following five steps for the difference in how to feel bitterness. Moreover, about the evaluation order of an Example and a comparative example, random assignment was performed for every test subject, and it determined. For 5 specialist panels, put the first sample in the mouth in a blinded state, thoroughly spread the composition in the mouth, rinse the mouth with sufficient tap water, and then evaluated the remaining samples . Each scored score was calculated as a total, and the results were evaluated according to the following criteria.
Scoring
Example does not feel bitter +2
The example does not feel a bitter taste +1
I can't feel the difference 0
The comparative example does not feel a bitter taste.
The comparative example does not feel bitter -2
Evaluation criteria
Total value is 5 or more ◎
Total value is 1 or more and 4 or less ○
Total value is 0 or less ×
The obtained results are shown in Table 2.

Example 5: Coating agent
Ingredients Amount
Shellac 10.0
Ethyl alcohol 40.0
Hydroxyethyl cellulose 0.3
Benzalkonium chloride 0.01
Hesperidin 0.05
Sodium fluoride 0.2
Fragrance 2.0
Sodium hydroxide appropriate amount
Purified water balance
Total 100.0

Example 6: Toothpaste
Ingredients Amount
Dicalcium phosphate 30.0
Glycerin 10.0
Sorbitol 20.0
Sodium carboxymethylcellulose 1.0
Sodium lauryl sulfate 1.5
Carrageenan 0.5
Saccharin sodium 0.1
Fragrance 1.0
Sodium benzoate 0.3
Cetylpyridinium chloride 0.05
Hesperidin 0.05
Vitamin E 0.05
Oil-soluble licorice extract 0.05
Purified water balance
Total 100.0

Example 7: Liquid dentifrice
Ingredients Amount
Sorbit 10.0
Polyoxyethylene hydrogenated castor oil (60) 5.0
Cetylpyridinium chloride 0.05
Fragrance 0.5
Saccharin sodium 0.01
Sodium citrate 0.05
Hesperidin 0.01
Tocopherol acetate 0.02
Sodium fluoride 0.05
Purified water balance
Total 100.0

Example 8: Mouthwash
Ingredients Amount
Ethanol 10.0
Glycerin 5.0
Calcium gluconate 1.5
Cetylpyridinium chloride 0.05
Citric acid 0.01
Sodium citrate 0.1
Polyoxyethylene hydrogenated castor oil (60) 0.5
Methyl paraoxybenzoate 0.1
Fragrance 1.0
Hesperidin 0.1
Vitamin E 0.05
Vitamin C 0.01
Purified water balance
Total 100.0

Example 9: Gel for oral cavity
Ingredients Amount
Carboxymethylcellulose 0.3
Glycerin 10.0
Polyethylene glycol 10.0
Cetylpyridinium chloride 0.3
Hesperidin 0.2
Vitamin E 0.05
Purified water balance
Total 100.0

Example 10 Mouse Spray
Ingredients Amount
Glycerin 15.0
Ethanol 10.0
Trehalose 5.0
Stevia extract 0.1
Hesperidin 0.1
Benzethonium chloride 0.02
Citric acid 0.01
Sodium citrate 0.02
l-Menthol 1.0
Fragrance 0.2
Purified water balance
Total 100.0

Claims (5)

An oral or pharyngeal composition comprising one or more cationic fungicides selected from cetylpyridinium chloride, benzethonium chloride, and benzalkonium chloride and hesperidin. 2. The composition for oral cavity or pharynx according to claim 1, wherein the amount of the cationic fungicide is 0.01 to 0.3% by mass. The composition for oral cavity or pharynx according to claim 1 or 2, wherein the amount of hesperidin is 0.01 to 0.2 mass%. The composition for oral cavity or pharynx according to any one of claims 1 to 3, wherein the cationic bactericidal agent is cetylpyridinium chloride. Furthermore, 1 or more types of polyhydric alcohol chosen from glycerin, polyethyleneglycol, propylene glycol, and 1, 3- butylene glycol is mix | blended, The composition for oral cavity or pharynx in any one of Claims 1-4 characterized by the above-mentioned. object.