JP2006306768A - Sterilization composition for oral cavity and throat - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a sterilization composition for oral cavity and throat, compounded with a cationic antibacterial agent, having good taste masking bitterness peculiar to the antibacterial agent and impairing no antibacterial activity of the antibacterial agent. <P>SOLUTION: The sterilization composition for oral cavity and throat comprises at least one selected from a group consisting of trehalose, erythritol and palatinit. That is, by adding trehalose, erythritol or palatinit to a cationic antibacterial agent (such as cetylpyridinium chloride), the sterilization composition for oral cavity and throat, masked bitterness to have good taste, and impaired no antibacterial activity of the antibacterial agent is obtained. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to a bactericidal composition for oral cavity or throat having a high antibacterial action, in which the bitterness peculiar to a cationic antibacterial agent is reduced.

  Conventionally, it is known that cationic antibacterial agents have strong bactericidal and antibacterial effects. For this reason, attempts have been made to blend the antibacterial agent into oral compositions. For the purpose of preventing periodontal disease and dental caries disease, the effect of the cationic antibacterial agent in the oral composition is sufficient even if the concentration 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 it is necessary to add a cationic antibacterial agent 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, accurate sterilization of the throat is effective, and for that purpose, a composition for the throat containing a high concentration of an antibacterial agent is required. However, this antibacterial agent has a unique bitter taste, and when this antibacterial agent is blended in the oral composition at a high concentration, the taste is very bad. Then, in order to improve the taste of the composition for oral cavity which mix | blended the cationic antibacterial agent, the mixing | blending of various components was tried.

For example, oral compositions containing a large amount of sweeteners such as saccharin and dipotassium glycyrrhizinate and sweet polyhydric alcohols such as glycerin and sorbit are known. Moreover, the composition for oral cavity which mix | blended tranexamic acid and / or (epsilon) -aminocaproic acid, and the stevia sweetener is known (refer patent document 1).
Japanese Patent Laid-Open No. 5-931

  However, saccharin tends to reduce the antimicrobial activity of cationic antimicrobial agents. Moreover, since the stevia sweetener itself has a peculiar bitter taste, there was a problem that a taste will deteriorate if the compounding quantity is increased.

  Therefore, even when the cationic antibacterial agent is blended at a high concentration, the present invention has good taste with its unique bitterness masked, and does not impair the antibacterial activity of the cationic antibacterial agent. An object is to provide a bactericidal composition for the oral cavity or throat.

  As a result of intensive studies in view of the above-mentioned problems of the prior art, the present inventor has masked the bitterness peculiar to cationic antibacterial agents in the bactericidal composition for oral cavity and throat containing either trehalose, erythritol, or palatinit. The present invention was completed by finding that it has good taste and does not impair the antibacterial activity of the cationic antibacterial agent.

That is, the present invention provides the following bactericidal composition for oral cavity or throat.
Item 1. A bactericidal composition for oral cavity or throat containing at least one selected from the group consisting of trehalose, erythritol and paratinite and a cationic antibacterial agent.
Item 2. Item 2. The bactericidal composition for oral cavity or throat according to item 1, wherein the cationic antibacterial agent is cetylpyridinium chloride.
Item 3. Item 3. The bactericidal composition for oral cavity or throat according to item 2, wherein the blending amount of cetylpyridinium chloride is 0.2 to 0.6% by weight relative to the whole composition.
Item 4. Furthermore, the bactericidal composition for oral cavity or throat according to any one of Items 1 to 3, containing a stevia sweetener.
Item 5. Item 5. The bactericidal composition for oral cavity or throat according to any one of Items 1 to 4, which is liquid or liquid.
Item 6. Item 6. The oral or throat bactericidal composition according to Item 5, which is any one of liquid dentifrice, liquid dentifrice, mouthwash, mouse spray, throat spray, and mouthwash.
Item 7. Item 6. The bactericidal composition for oral cavity or throat according to item 5, which is for spraying.

  The bactericidal composition for oral cavity or throat of the present invention contains a cationic antibacterial agent. Examples of the cationic antibacterial agent include quaternary ammonium salt type cationic antibacterial agents such as cetylpyridinium chloride, benzethonium chloride, benzalkonium chloride, and decalinium chloride; piguanide antibacterial agents such as chlorhexidine hydrochloride and chlorhexidine gluconate; hexetidine, Metallonidazole etc. are mentioned, These 1 type can be mix | blended individually or in combination of 2 or more types. A preferred antibacterial agent is a quaternary ammonium salt type cationic antibacterial agent, and a more preferred antibacterial agent is cetylpyridinium chloride. The amount of the antibacterial agent is usually 0.001 to 5% by weight, preferably 0.05 to 1% by weight, more preferably 0.2 to 0.6% by weight, based on the entire bactericidal composition for the oral cavity or throat. is there.

  The bactericidal composition for oral cavity or throat of the present invention contains at least one selected from the group consisting of trehalose, erythritol and paratinite in addition to the cationic antibacterial agent. By blending this sweetener, the bactericidal composition for the oral cavity or throat has a good taste in which the bitterness derived from the cationic antibacterial agent is masked. A preferred sweetening agent is trehalose. The compounding quantity of a sweetener is 1-20 weight% normally with respect to the whole composition for oral cavity, Preferably it is 5-15 weight%.

  Moreover, the masking effect can be further enhanced by blending the bactericidal composition for oral cavity or throat of the present invention with a stevia sweetener usually used for dentifrices and the like. Stevia sweeteners include stevia extract (including sweeteners contained in the extract that contain the most abundant stevioside, extracts that contain the most abundant rebaudioside, etc.), stevioside, Examples include baudioside, zulcoside, stevia powder, glycosylated stevia, enzyme-treated stevia, and the like. These can be used alone or in combination of two or more. Stevia extract is preferred. The amount of the stevia sweetener is usually 0 to 0.3% by weight, preferably 0.0005 to 0.3% by weight, more preferably 0.001 to 0.1%, based on the entire bactericidal composition for the oral cavity or throat. % By weight. If the amount of the stevia sweetener is within these ranges, the bitterness specific to the stevia sweetener will not be felt while masking the bitter taste of the antibacterial agent, and the taste of the bactericidal composition for the oral cavity or throat will be better. It will be a thing.

  The bactericidal composition for oral cavity or throat of the present invention is a toothpaste, powder dentifrice, liquid dentifrice, liquid dentifrice, mouthwash, mouth spray, throat spray, prophy paste, pasta, drop, chewing gum, tablet, mouthwash, oral cavity It can be prepared in the form of an ointment or the like. Among these forms, a liquid form is preferable, and a liquid dentifrice, liquid dentifrice, mouthwash, mouth spray, throat spray, and 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.

  The bactericidal composition for oral cavity or throat of the present invention may contain a surfactant, but an anionic surfactant may reduce the antibacterial properties of the cationic antibacterial agent. Even if it mix | blends a surfactant, it is preferable to make it a small quantity and not mix | blend. The compounding amount of the surfactant is usually 0 to 2.0% by weight, preferably 0 to 0.5% by weight, based on the whole composition. Examples of the surfactant include polyoxyethylene fatty acid esters such as polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monolaurate, polyoxyethylene hydrogenated castor oil, polyoxyethylene higher alcohol ether, polyoxyethylene polyoxypropylene Copolymer, polyoxyethylene polyoxypropylene fatty acid ester alkyl glycoside (for example, alkyl chain: about C8 to C16), polyglycerin fatty acid ester (for example, the fatty acid portion has about 8 to 16 carbon atoms), sucrose fatty acid ester (for example, fatty acid) Nonionic surfactants having a carbon number of about 8 to 16); N-alkyldiaminoethylglycine, alkylbetaine, alkylsulfobetaine, alkylbetaine, imidazoliumbetaine Examples of amphoteric surfactants include cationic surfactants such as alkyltrimethylammonium chloride, alkyltrimethylammonium bromide, and alkyldimethylammonium chloride. These may be used alone or in combination of two or more. be able to.

  Arbitrary or throat disinfecting composition of the present invention can be blended with arbitrary components within a range not impairing the effects of the present invention. For example, calcium salts such as calcium chloride, calcium lactate, calcium gluconate and calcium glycerylate, magnesium salts such as magnesium chloride and magnesium sulfate, menthol, carvone, anethole, eugenol, methyl salicylate, limonene, osimene, n-decyl alcohol, Citronell, α-terpineol, methyl acetate, citronenyl acetate, methyl eugenol, cineole, linalool, ethyl linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil Perfume such as perilla oil, winter green oil, clove oil, eucalyptus oil, pimento oil, saccharin, sodium saccharin, acesulfame potassium, neohesperidyl dihydrochalcone, glycyl Chin, perilartin, thaumatin, asparatylphenylalanyl methyl ester, ρ-methoxycinnamic aldehyde, xylitol, lactitol, maltitol and other sweeteners, sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene Wetting agents such as glycol and polypropylene glycol, vitamin Es such as dl-α-tocopherol acetate, tocopherol succinate or tocopherol nicotinate, amphoteric fungicides such as dodecyldiaminoethylglycine, nonionics such as triclosan and isopropylmethylphenol Bactericides, dextranases, amylases, proteases, mutanases, lysozymes, enzymes such as lytic enzymes (Litec Enzymes), monofluorolines Sodium, alkali metal monofluorophosphates such as potassium monofluorophosphate, fluorine compounds such as sodium fluoride and stannous fluoride, sodium carboxymethylcellulose, carrageenan, sodium alginate, veegum, hydroxyethylcellulose, xanthan gum, sodium polyacrylate Binders such as dibasic calcium phosphate, primary calcium phosphate, tertiary calcium phosphate, silica, insoluble sodium metaphosphate, aluminum chlorohydroxyl allantoin, dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, hinokitiol, glycerophosphate, chlorophyll, Azulene, polyphosphate, sodium chloride, caropeptide, water-soluble inorganic phosphate compounds, etc. These can be blended singly or in combination of two or more.

  According to the present invention, the bitterness peculiar to a cationic antibacterial agent is masked, and the taste is good, without impairing the effect of the cationic antibacterial agent, and suppression of plaque formation in the oral cavity, prevention of periodontal disease, whole body An antibacterial composition for the oral cavity or throat, which is useful for preventing infections that lead to diseases, is provided.

  EXAMPLES Hereinafter, although an Example demonstrates this invention in detail, this invention is not limited to these Examples.

Test Example 1: Bitterness and irritation suppression effect 1
Sprays were prepared by a conventional method with the compositions of Examples 1 to 3 and Comparative Examples 1 to 5 shown in Table 1. The prepared spray was sprayed to the throat and mouth several times on a total of 3 monitors, and the bitterness, irritation and sweetness were evaluated. In addition, the usage-amount of the sweetener (The stevia extract-erythritol in Table 1) was made into the quantity from which the sweetness degree of a sweetener will be about 4650 as much as possible. Sweetness = Σ (sweetness of sweetener × composition ratio of composition)
Bitterness evaluation 0: No bitterness
1: Almost no bitterness
2: Slightly bitter
3: Bitter taste
4: Very bitter and irritation evaluation 0: No irritation
1: Almost no irritation
2: Slightly irritating
3: Stimulated
4: Total evaluation with very irritation ◎: Total bitterness evaluation and irritation evaluation is less than 2
○: The sum of bitterness evaluation and stimulation evaluation is 2 or more and less than 4
Δ: The sum of bitterness evaluation and stimulation evaluation is 4 or more and less than 6
X: The sum of bitterness evaluation and irritation evaluation is 6 or more

  As a result of the test, trehalose was most excellent in bitterness evaluation, irritation evaluation and sweetness evaluation when the sweetness levels were equivalent. Erythritol and paratinite also had sufficient bitterness and irritation suppression effects.

Test Example 2: Bitterness and irritation suppression effect 2
As shown in Examples 4 to 6 and Comparative Examples 6 to 8 in Table 2, sprays were prepared by changing the cetylpyridinium chloride concentration, and bitterness evaluation and stimulation evaluation were performed. The evaluation criteria are the same as in Test Example 1.

As a result of the test, the masking effect of stevia extract decreases as the amount of cetylpyridinium chloride increases. In contrast, trehalose has an effect of sufficiently suppressing the bitter taste even in a region where the amount of cetylpyridinium chloride is high.

Test Example 3: Bitterness and irritation suppression effect 3
Sprays were prepared in Examples 7 to 16 in Table 3, and bitterness evaluation, stimulation evaluation, and sweetness were performed. The evaluation criteria are the same as in Test Example 1.

Test Example 4: Bactericidal effect, bitterness and irritation suppressing effect 4
Test solutions 1 to 6 in Table 4 were prepared, and the bactericidal effect was evaluated by the following test methods.
Test method: Streptococcus mutans cultured for 24 hours under anaerobic conditions at 37 ° C. in a brain heart infusion (BHI) liquid medium is adjusted to about 10 ⁹ cfu / mL, and 100 μL of the adjusted bacterial solution and 900 μL of the test solution are added, Touch for 30 seconds. This mixed test solution is diluted 10-fold with PBS, and 100 μL of each diluted solution is smeared on Trypticase Soy Agar (TSA) medium and cultured at 37 ° C. for 48 to 72 hours. It measured and evaluated the bactericidal effect by the following evaluation criteria. Further, bitterness and irritation were evaluated in the same manner as in Test Example 1.
Evaluation criteria: The bactericidal effect was expressed as follows according to the number of viable bacteria compared to the negative control (PBS aqueous solution).
-: Less than 1/10 +: 1/10 or more and less than 1/10 ⁶ +++: 1/10 ⁶ or more

Even if trehalose was added, the bactericidal effect of cetylpyridinium chloride was not impaired. Further, the smaller the amount of surfactant (polyoxyethylene hydrogenated castor oil) blended, the higher the bactericidal effect.

Formulation Example A bactericidal composition for the oral cavity or throat was produced by a conventional method using the following components. The unit is mass%.

<Throat spray>
Glycerin 35.0
Sorbit solution 10.0
Propylene glycol 5.0
Ethanol 2.0
Cetylpyridinium chloride 0.3
Trehalose 10.0
Stevia extract 0.1
Citric acid appropriate amount Sodium citrate appropriate amount l-menthol 0.2
Fragrance 0.1
Water balance
Total 100

<Toothpaste>
Calcium hydrogen phosphate 30.0
Silicic anhydride 5.0
Sorbit solution 10.0
Propylene glycol 5.0
Hydroxyethyl cellulose 2.0
Cetylpyridinium chloride 0.3
Tocopherol acetate 0.05
Trehalose 15.0
Stevia extract 0.1
Alkyl glucoside 0.5
Fragrance 1.0
Water balance
Total 100

<Liquid toothpaste>
Silicic anhydride 5.0
Glycerin 25.0
Propylene glycol 5.0
Hydroxyethyl cellulose 0.5
Chlorhexidine gluconate 0.2
Trehalose 10.0
Stevia extract 0.1
Polyoxyethylene hydrogenated castor oil 0.5
Fragrance 1.0
Water balance
Total 100

<Liquid toothpaste>
Glycerin 20.0
Benzethonium chloride 0.3
Triclosan 0.05
Trehalose 15.0
Citric acid appropriate amount Sodium citrate appropriate amount Stevia extract 0.02
Fragrance 1.0
Polyoxyethylene hydrogenated castor oil 0.1
Water balance
Total 100

<Liquid toothpaste>
Glycerin 15.0
Ethanol 5.0
Cetylpyridinium chloride 0.3
Tranexamic acid 0.05
Trehalose 10.0
Citric acid appropriate amount Sodium citrate appropriate amount Stevia extract 0.02
Fragrance 1.0
Water balance
Total 100

<Mouthwash>
Glycerin 20.0
Propylene glycol 5.0
Cetylpyridinium chloride 0.2
Trehalose 5.0
Stevia extract 0.05
Citric acid Appropriate amount Sodium citrate Appropriate amount Polyoxyethylene hydrogenated castor oil 0.2
Fragrance 1.0
Water balance
Total 100

<Mouthwash>
Glycerin 15.0
Ethanol 5.0
Propylene glycol 5.0
Cetylpyridinium chloride 0.2
Trehalose 10.0
Stevia extract 0.05
Citric acid appropriate amount Sodium citrate appropriate amount Fragrance 1.0
Water balance
Total 100

<Mouse spray>
Glycerin 15.0
Ethanol 10.0
Cetylpyridinium chloride 0.3
Trehalose 5.0
Stevia extract 0.10
Citric acid appropriate amount Sodium citrate appropriate amount 1-menthol 2.0
Fragrance 0.1
Water balance
Total 100

<Chewing gum>
Gum base 25.0
Calcium carbonate 2.5
Minamata 10.0
Powdered sugar 50.0
Cetylpyridinium chloride 0.3
Trehalose 10.0
Stevia extract 0.1
Anethole 0.1
l-Menthol 2.0
Total 100

<Drop>
Water candy 65.0
Trehalose 30.0
Copper chlorophyllin sodium 0.01
Cetylpyridinium chloride 0.3
Rebaudioside 0.1
l-Menthol 0.1
Sodium citrate 0.1
Water balance
Total 100

<An gargle (dilution type)>
Ethanol 50.0
Trehalose 5.0
Cetylpyridinium chloride 0.3
l-Menthol 2.0
Stevioside 0.05
Clove oil 0.05
Water balance
Total 100

<Oral pasta>
Glycerin 10.0
Trehalose 5.0
Hydroxyethyl cellulose 5.0
Cetylpyridinium chloride 0.3
Tocopherol acetate 0.05
Cetanol 5.0
White petrolatum 0.5
Polyoxyethylene hydrogenated castor oil 0.5
Glycerol monostearate 10.0
Stevia extract 0.1
Fragrance 0.5
Water balance
Total 100

  The bactericidal liquid composition for oral cavity or throat according to the present invention is masked with bitterness peculiar to a cationic antibacterial agent and has a good taste, so that it is a toothpaste, powder toothpaste, liquid toothpaste, liquid toothpaste, mouthwash, mouthwash, It is useful as a mouse spray, throat spray, profie paste, pasta, drop, chewing gum, tablet, gargle, oral ointment and the like.

Claims (7)

A bactericidal composition for oral cavity or throat containing at least one selected from the group consisting of trehalose, erythritol and paratinite and a cationic antibacterial agent. The bactericidal composition for oral cavity or throat according to claim 1, wherein the cationic antibacterial agent is cetylpyridinium chloride. The bactericidal composition for oral cavity or throat according to claim 2, wherein the blending amount of cetylpyridinium chloride with respect to the whole composition is 0.2 to 0.6% by weight. Furthermore, the bactericidal composition for oral cavity or throat according to any one of claims 1 to 3, further comprising a stevia sweetener. The bactericidal composition for oral cavity or throat according to any one of claims 1 to 4, which is liquid or liquid. The bactericidal composition for oral cavity or throat according to claim 5, which is any one of liquid dentifrice, liquid dentifrice, mouthwash, mouse spray, throat spray, and mouthwash. The bactericidal composition for oral cavity or throat according to claim 5, which is for spraying.