JPH09110662A - Halitosis eliminating agent and composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a halitosis eliminating agent exhibiting antibacterial action specifically on Fusobacterium nucleatum which is a causative bacterium of halitosis and to obtain a composition compounded with the agent. SOLUTION: This halitosis aliminating agent contains one or more kinds of perfumes selected from 3-methyl-5-phenyl-1-pentanol, 11-dodecenoic acid and 4-methyl-4-decanolide.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to Fusobacterium nucleatum (Fusobacte), which is a bacteria causing halitosis.
The invention relates to a breath odor remover that specifically exhibits antibacterial activity against rium nucleatum) and a composition for oral cavity containing the same.

[0002]

2. Description of the Related Art Physiological halitosis is caused mainly by oral mucosa, exudates, food residues, and the like, Fusobacterium nucleatum (Fusobacte).
rium nucleatum; hereinafter abbreviated as Fn. )
It is caused by a volatile sulfur compound (VSC) such as methyl mercaptan which is generated by being decomposed by and causes a discomfort to humans. Therefore, in order to prevent or suppress the generation of bad breath, various attempts have been made to suppress VSC with a deodorant, mask VSC with a fragrance, and remove Fn with a bactericide.

However, when chlorhexidine, cetylpyridinium chloride or the like is used as an oral bactericidal agent, the bacterial flora in the oral cavity changes due to the strength of the antibacterial activity or the broad spectrum of the antibacterial effect, resulting in the occurrence of bacterial transmutation. The use of such a strong antibacterial agent for the removal of physiological odor which is expected to have harmful effects and is not pathological is not appropriate in terms of safety.

In this case, F, which is a bacterium causing physiological halitosis,
Since n has a stronger resistance to an antibacterial agent than other oral bacteria, there is a problem that a weak antibacterial agent cannot provide a sufficient halitosis removal effect.

On the other hand, various proposals have been made so far to use a fragrance as an antibacterial agent for the oral cavity, and particularly Streptococcus mutans (Streptococcus mu) is proposed.
There are many proposals relating to fragrances having antibacterial activity against tans (JP-A-59-29618 and 59-2).
9619, 59-175410, 63-881.
No. 23, etc.). Among them, JP-A-63-88123 proposes a compound using a fatty acid having 13 to 18 carbon atoms as an antibacterial agent.

However, a breath odor removing agent which is specific to Fn and is highly safe has not yet been obtained, and its development has been desired.

The present invention has been made in view of the above circumstances and has a highly safe halitosis remover having a specific antibacterial activity against Fn, which is a bacteria causing halitosis, and a composition for oral cavity using the same. The purpose is to provide things.

[0008]

Means for Solving the Problems and Modes for Carrying Out the Invention The inventors of the present invention have conducted extensive studies in order to achieve the above object, and as a result, 3-methyl-5-phenyl-1-pentanol, 11- It was discovered that dodecenoic acid and 4-methyl-4-decanolide surprisingly exhibit excellent antibacterial activity against Fn, which is a causative bacterium of physiological halitosis, and are effective in removing halitosis.

That is, by using one or more perfumes selected from 3-methyl-5-phenyl-1-pentanol, 11-dodecenoic acid and 4-methyl-4-decanolide as a breath freshener, It exhibits excellent antibacterial properties against Fn, which is the causative bacterium of physiological halitosis, and it can effectively prevent the development of halitosis by directly inhibiting the growth thereof, and its antibacterial properties against Fn. Porphyromonas gingival, a specific and other oral bacterium, Porphyromonas gingival
is), Actinomyces viscosus (Actinom)
yces viscosus), Streptococcus
Mutans (Streptococcus mutans)
Since it has no antibacterial property against the above, it has been found that the bacterial flora in the oral cavity does not change, and it is also excellent in terms of safety, and the present invention has been completed.

Therefore, the present invention comprises one or more perfume selected from 3-methyl-5-phenyl-1-pentanol, 11-dodecenoic acid and 4-methyl-4-decanolide as an active ingredient. Provided are a bad breath remover and a composition for oral cavity containing the above bad breath remover.

The present invention will be described in more detail below. The breath odor removing agent of the present invention comprises 3-methyl-5-phenyl-1-pentanol, 11-dodecenoic acid and 4-methyl-
One or two or more kinds of fragrances selected from 4-decanolide are used as active ingredients.

Here, 3-methyl-5-phenyl-1-
Pentanol, 11-dodecenoic acid, and 4-methyl-4-decanolide are all fragrances having 12 or less carbon atoms.

In this case, these fragrances have specific antibacterial properties against Fn, which is a physiological causative agent of halitosis, and other oral bacteria, Porphyromonas gingivali (Porphyromonas gingivali).
s), Actinomyces viscosus (Actinomy)
ces viscosus), Streptococcus mutans
However, since it has no antibacterial properties, it is highly safe and does not change the bacterial flora in the oral cavity and does not worry about transmutation, as compared with the conventional prevention of bad breath by sterilizing and antibacterial agents.
Further, the bad breath removing agent of the present invention does not act as a deodorant or a masking agent, but directly suppresses the growth of Fn, which causes bad breath, so that the bad breath removing effect is remarkable.

The breath odor removing agent of the present invention can be used by being blended with an oral composition, and the blending amount thereof is 0.0001 to 5% (% by weight, hereinafter the same) of the total amount of the oral composition. ,
In particular, it is preferably 0.001 to 3%. 0.00
If it is less than 01%, a satisfactory antibacterial effect may not be exhibited, and if it exceeds 5%, the stability or flavor of the composition may be impaired.

Further, the breath odor removing agent of the present invention is based on the existing VS.
When used in combination with a deodorant for C, such as a Lamiaceae plant extract, a Camelliaceae plant extract, or a masking agent, a stronger halitosis removing effect is exhibited.

In the oral composition of the present invention, it is possible to use the components other than the above-mentioned components which are usually used in oral compositions, and the addition amount of these components hinders the effect of the present invention. It can be a normal amount within the range not present.

In the case of toothpaste, for example, an abrasive, a binder,
Various active ingredients such as a thickener, a surfactant, a sweetener, a preservative, a coloring agent and the like can be added, and these ingredients can be mixed with water to produce the composition.

Here, as the abrasive, precipitated silica,
Silica-based abrasives such as silica gel, aluminosilicate, zirconosilicate, dibasic calcium phosphate dihydrate and anhydrate, calcium pyrophosphate, calcium carbonate,
Aluminum hydroxide, alumina, magnesium carbonate, tertiary magnesium phosphate, zeolite, zirconium silicate, synthetic resin-based abrasives and the like are preferably used.

Examples of the thickener include glycerin, sorbitol, propylene glycol, polyethylene glycol,
Xylit, maltit, lactit, and the like are preferably used.

As the binder, sodium carboxymethyl cellulose, hydroxyethyl cellulose, carrageenan, sodium alginate, xanthan gum, carbopol, guar gum, montmorillonite, gelatin and the like are preferably used.

As the surface active agent, an anionic surface active agent, a cationic surface active agent, a nonionic surface active agent and the like are used. Specifically, sodium lauryl sulfate,
α-Sodium olefin sulfonate, N-acyl sarcosinate, N-acyl glutamate, 2-alkyl-
N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, N-acyl taurate, sucrose fatty acid ester, alkylol amide, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester, pluronic, polyoxyethylene sorbitan monostearate Are preferably used.

As the sweetener, saccharin sodium,
Examples thereof include stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perillartine and the like.

Examples of preservatives include paraoxybenzoic acid ester and sodium benzoate.

Other various active ingredients include fluorides such as sodium fluoride, potassium fluoride, ammonium fluoride, stannous fluoride, sodium monofluorophosphate, potassium salts of orthophosphoric acid, sodium salts and the like. Water-soluble phosphate compounds, allantoin chlorohydroxyaluminum, hinokitiol, ascorbic acid, lysozyme chloride, glycyrrhizic acid and its salts, sodium chloride,
Tranexamic acid, epsilon aminocaproic acid, acetic acid d
Copper compounds such as 1-tocopherol, azulene, glycyrrhetinic acid, sodium copper chlorophyllin, and copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid and its derivatives, sodium tripolyphosphate, zeolite, dextranase, mutanase, amylase , Methoxyethylene, maleic anhydride copolymer, polyvinylpyrrolidone, epidihydrocholesterin, dihydrocholesterol, zinc citrate, touki, sorghum, clove, rosemary, sorghum, safflower and the like.

Suitable fragrances are terpenes such as 1-menthol, carvone, anethole and limonene, or their derivatives, and suitable colorants are Blue No. 1, Yellow No. 4 and titanium dioxide.

The oral composition containing the bad breath remover of the present invention includes toothpaste such as toothpaste, liquid toothpaste, powder toothpaste, mouthwash, mouthwash, oral pasta,
Examples include troches, chewing gum, mouth cooling agents, and the like include candy and the like.
It is not limited to these.

[0027]

EFFECTS OF THE INVENTION The breath odor-eliminating agent of the present invention shows a specific antibacterial activity against Fn, which is one of the bacteria causing halitosis, is highly safe and has an excellent breath odor removing effect on volatile sulfur compounds. And is preferably used for oral compositions.

[0028]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to Experimental Examples, Examples and Comparative Examples, but the present invention is not limited to the following Examples. In addition, all% in each example are weight%.

[Experimental Example] Using the following strains and liquid medium, 3-methyl-5-phenyl-1-pentanol, 11-dodecenoic acid, and 4-methyl-4- were used as test breath odor removers. An antibacterial activity test (measurement of MIC) was performed by the following method using decanolide.

Test tube (13 x 1) containing 4 ml of liquid medium
(00 mm) was mixed with 0.04 ml of the test breath odor remover solution having a stepwise changed concentration, and 0.04 ml of each bacterial solution precultured for one day was added and stirred. After anaerobic culture at 37 ° C. for 3 days, the amount of bacterial growth was measured by absorbance at 550 nm. An absorbance of less than 0.05 was regarded as effective, and a minimum growth inhibitory concentration (MIC) was determined. Table 1 shows the results. Strains and Liquid Medium Composition Fusobacterium nuclearatum 1436 (Fn) Medium: Todd Hewitt Broth (hereinafter abbreviated as THB) 3% L-cystine hydrochloride 0.05% Porphyromonas gingivalis 381 (Porphyromonas gin givalis 381 (Pg)) Medium: THB 3% Hemin 3 ppm Menadione 0.5 ppm Actinomyces viscosus cusus cus cus suc 15 s. Sm)) Medium: THB 3%

[0031]

[Table 1]

From the results shown in Table 1, the breath odor removing agent of the present invention is
It was confirmed that the antibacterial property was specifically shown only to Fn.

Next, examples will be shown. [Example 1] Toothpaste Calcium carbonate 50.00% Glycerin 20.00 Carrageenan 0.50 Carboxymethyl cellulose 1.00 Lauryl diethanolamide 1.00 Sucrose monolaurate 2.00 Fragrance 1.00 Saccharin 0.10 3- Methyl-5-phenyl-1-pentanol 0.10 Water Residual 100.0%

Example 2 Toothpaste Dicalcium Phosphate Dihydrate 50.00% Glycerin 20.00 Carboxymethyl Cellulose 2.00 Sodium Lauryl Sulfate 2.00 Fragrance 1.00 Sodium Saccharin 0.10 11-Dodecenoic Acid 0 10 Rosemary extract (deodorant) 0.10 water Residual 100.0%

Example 3 Toothpaste Aluminum hydroxide 45.00% Gelling silica 2.00 Solbit 25.00 Carboxymethyl cellulose 1.00 Sodium lauryl sulfate 2.00 Fragrance 1.00 Sodium saccharin 0.10 3-Methyl -5-Phenyl-1-pentanol 0.05 4-Methyl-4-decanolide 0.05 Water Residual 100.0%

Example 4 Toothpaste Precipitable silica 25.00% Glycerin 25.00 Sorbit 25.00 Lauroyl polyglycerin ester 1.00 Polyoxyethylene sorbitan monolaurate 2.00 Perfume 1.00 Sodium saccharin 0.20 4-Methyl-4-decanolide 0.10 Sage extract (deodorant) 0.05 Water Residual 100.0%

Example 5 Liquid Toothpaste Aluminum Hydroxide 25.00% Glycerin 40.00 Solbit 15.00 Carboxymethyl Cellulose 0.20 Propylene Glycol 2.00 Sodium Lauryl Sulfate 1.50 Decaglyceryl Monolaurate 1.00 Perfume 1 1.00 Sodium saccharin 0.10 11-dodecenoic acid 0.10 Water balance 100.0%

[Example 6] Liquid dentifrice Precipitable silica 20.00% Glycerin 25.00 Solbit 35.00 Xanthan gum 0.20 Propylene glycol 2.00 Sodium lauryl sulfate 1.50 Decaglyceryl monolaurate 2.00 Fragrance 1. 00 sodium saccharin 0.10 3-methyl-5-phenyl-1-pentanol 0.10 water balance 100.0%

[Example 7] Oral ointment Liquid paraffin 15.00% Cetanol 10.00 Glycerin 20.00 Polyoxyethylene sorbitan fatty acid ester 5.00 Perfume 0.50 Saccharin sodium 0.10 4-Methyl-4-decanolide 0 .20 Thyme extract (deodorant) 0.10 water Total balance 100.0%

[Example 8] Mouthwash Ethanol 20.00% Perfume 1.00 Polyoxyethylene hydrogenated castor oil 0.30 Sodium monofluorophosphate 0.10 Saccharin sodium 0.05 11-Dodecenoic acid 0.20 Water residue 100.0% in total

Example 9 Mouthwash Tablet Sodium Bicarbonate 54.00% Citric Acid 17.00 Anhydrous Sodium Sulfate 12.80 Sodium Dibasic Phosphate 10.00 Polyethylene Glycol 3.00 Sodium Monofluorophosphate 0.10 Fragrance 2.00 Oleic acid 0.10 3-Methyl-5-phenyl-1-pentanol 0.50 4-Methyl-4-decanolide 0.50 Total 100.0%

[Example 10] troche glucose 35.00% palatinose 35.00 gum arabic 6.00 fragrance 1.00 sardine extract (deodorant) 0.50 11-dodecenoic acid 1.00 water balance 100. 0%

[Example 11] Candy Sugar 50.00% Starch syrup 33.00 Organic acid 2.00 Fragrance 0.20 11-Dodecenoic acid 0.05 4-Methyl-4-decanolide 0.05 Water Residual 100.0 %

[Example 12] Chewing gum Sugar 53.00% Gum base 20.00 Glucose 10.00 Syrup 16.00 Fragrance 0.50 4-Methyl-4-decanolide 0.50 Total 100.0%

[Example 13] Chewing gum Sugar 55.00% Gum base 20.00 Corn syrup 12.00 Syrup 12.30 Fragrance 0.50 Thyme extract (deodorant) 0.10 3-Methyl-5-phenyl- 1-Pentanol 0.20 Total 100.0%

The MICs of the compositions of the above Examples were measured in the same manner as in the Experimental Examples, and all showed good antibacterial activity against Fn.

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Claims (2)

[Claims] 1. A breath freshener containing, as an active ingredient, one or more perfume selected from 3-methyl-5-phenyl-1-pentanol, 11-dodecenoic acid and 4-methyl-4-decanolide. 2. An oral composition containing the breath freshener according to claim 1.