JP3065947B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention has a caries-preventing effect and a periodontal-disease-preventing effect obtained by blending a specific glycoside, and is excellent in flavor when used and changes flavor after use. The present invention relates to a composition for an oral cavity that expresses a new flavor by maintaining the flavor for a long time.

[0002]

2. Description of the Related Art Oral compositions such as dentifrices include Streptcoccus mutans, which is a cariogenic bacterium.
(Ccus mutatans) shows antibacterial properties, or suppresses glucosyltransferase produced by Streptococcus mutans, by inhibiting plaque formation by inhibiting glucosyltransferase, a plant extract having a caries preventive effect is included, There was a problem that the discoloration over time was caused by blending these extracts. In addition, against gram-negative anaerobic bacteria such as Porphyromonas gingivalis, which is a pathogen of periodontal disease such as alveolar pyorrhea, gingivitis, etc., against Kemponashi extract, Fennel extract, Licorice extract , L-menthol or l-carvone has been proposed (JP-A-6-131195). However, when a concentration for obtaining the effect is blended, coloring with time or disinfectant such as a bactericide is performed. There was a problem that the effect was not sustainable. On the other hand, many fragrances for dentifrices generally contain l-menthol or l-carvone, or a mixture of anises and spices, but have a drawback that they do not maintain a refreshing feeling.

[0003]

That is, an object of the present invention is to prevent caries and prevent periodontal disease, to be stable without discoloration over time, and to have little change in taste during use. An object of the present invention is to provide a composition for oral cavity which is excellent in the flavor of the present invention, changes the flavor after use, expresses a new flavor, and is excellent in persistence of the flavor after use.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies to achieve the above object, and as a result, the aglycone part of the glycoside has eugenol, raspberry ketone, isoeugenol, shogaol, capsaicin, vanillin By combining one or more glycosides, it shows higher antibacterial activity against cariogenic bacteria and pathogens of periodontal disease, is stable without discoloration over time, and changes in taste during use It has been found that an oral composition having a low flavor and excellent flavor at the time of use, changing the flavor after use to express a new flavor, and excellent persistence of the flavor after use can be obtained. completed.

That is, according to the present invention, the aglycone portion of the glycoside is a type of eugenol, raspberry ketone, isoeugenol, ginger, capsaicin, or vanillin,
Alternatively, there is provided an oral composition characterized by blending two or more glycosides.

[0006]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The configuration of the present invention will be described below. The glycosides are monosaccharides such as glucose, galactose, mantose, rhamnose, xylose, glusamine, and galactosamine; sugars such as disaccharides such as lactose, maltose and sucrose; and eugenol, raspberry ketone, isoeugenol, shogaol, and capsaicin. , A compound in which vanillin is D-glucoside-bonded.

[0007] Various perfume glycoside eugenol glycosides and the like phenylethyl glycosylase de used in the present invention, indigenous skin bacteria, by scalp flora is appropriately decomposed into aroma components portion and a sugar moiety The inventors of the present invention have previously found this and proposed a sustained-release fragrance composition for human body (JP-A-7-17-1).
No. 79328), the present inventors have found that, in particular, glycosides whose aglycon part is eugenol, raspberry ketone, isoeugenol, ginger, capsaicin, and vanillin are Streptcoccus mutans, which are cariogenic bacteria. And antimicrobial activity against Gram-negative anaerobic bacteria such as Porphyromonas gingivalis, which is a pathogen of periodontal disease such as alveolar pyorrhea and gingivitis, and sustained by oral bacteria It has been found that the composition has a high residual scent property and exhibits excellent properties as an oral composition.

In Japanese Patent Application Laid-Open No. 3-90016, one or more glycosides selected from thymol glycosides, cis-3-hexenol glycosides and methyl salicylate glycosides are blended into an oral composition, When an oral composition is used, a glycoside is hydrolyzed by the action of glucosidase in saliva, and thymol, cis-3-hexenol and salicylic acid are released to give an oral composition that expresses flavor. However, it is not described at all that the glycoside has a caries preventive effect and a periodontal disease preventive effect.

Glycosides used in the present invention are described in U.S. Pat. S. P.
No. 3201385, Flavor and Fragrance Journal [Flavour and Fragrance]
eJournal (Vol 4, 163-167, 198)
9)], and can be easily synthesized by a known method described in, for example. Among the glycosides used in the present invention, glucose glycosides are preferable in view of the degree of the effect .
In this case, the β-form is preferred, but there is no particular problem in the effect even if the α-form is contained.

The concentration of the specific glycoside in the present invention is from 0.005 to 5% based on the total amount of the oral composition.
It is 5.0% by weight (hereinafter abbreviated as wt%), more preferably 0.01 to 1.0% by weight. 0.0%
If it is less than 05 wt%, the effect may not be sufficiently obtained, and if it exceeds 5.0 wt%, the effect may not be improved in proportion to the increase.

Examples of the oral composition according to the present invention include dentifrices such as toothpaste, powdered toothpaste, and water toothpaste, mouthwash, mouth freshener, troche, pasta, paint and the like.
Other examples include chewing gum, candy, gummy candy, candy and the like.

Other ingredients that can be incorporated into the oral composition of the present invention are appropriately selected according to the type of the oral composition. For example, in the case of toothpaste, calcium carbonate, magnesium carbonate, dibasic calcium phosphate, tribasic calcium phosphate, magnesium phosphate, silica, zeolite, sodium metaphosphate, aluminum hydroxide, magnesium hydroxide, which are commonly used as abrasives, Examples include calcium pyrophosphate, red iron oxide, calcium sulfate, and silicic anhydride.

Also, a binder such as sodium carboxymethylcellulose, hydroxyethylcellulose, alginate, carrageenan, gum arabic, polyvinyl alcohol, methylcellulose, magnesium oxide, alumina sol, calcium silicate, pectin, guar gum, kaolin, sodium lauryl sulfate, dodecyl Sodium benzenesulfonate, sodium lauroylsulfoacetate,
Foaming agents such as sodium N-lauryl sulfonate, sodium N-lauroyl sarcosinate, sucrose fatty acid ester, polyoxyethylene sorbitan, and alkylolamide are used.

Further, sweeteners such as sodium saccharin, steviosite, glycyrrhizin, chalcone, dihydrochalcone, humectants such as glycerin, sorbitol, propylene glycol, polyethylene glycol, chylysitol, dipropylene glycol, sodium lactate, maltitol, paraoxybenzoate Preservatives such as acids, peppermint, spearmint essential oils and other fragrances, other aluminum lactate, edetate, dyes, BHT, etc. are used, and lysozyme chloride, dextranase, lytic enzyme, mutanase, and other active ingredients as necessary. Sorbic acid, alexidine, cetylpyridinium chloride, alkyl glycine, sodium chloride, allantoin, ε-aminocaproic acid, tranexamic acid, azulene, sodium fluoride, monofluorolyl Fluoride such as sodium, isopropyl methyl phenol, polyethylene glycol,
Plant-derived extracts such as polyvinylpyrrolidone, glycyrrhizin, glycyrrhizic acid, hinokitiol, vitamin E, and oil-soluble licorice extract can also be used.

The oral composition of the present invention, for example, in the case of toothpaste, is prepared by mixing these components with water and following a conventional method. In addition, in a mouthwash, a troche, a chewing gum and the like, components according to the properties of the product are appropriately compounded.

[0016]

The present invention will be described below in detail based on examples and comparative examples. The fragrance used below was menthol 10.0 wt%, carvone 15.0 wt%, peppermint oil 50.0 wt%, spearmint oil 20.0 wt%,
It has a composition of anethole 4.0 wt% and thymol 1.0 wt%. Prior to the description of the examples, a test method for antibacterial activity against periodontal disease pathogenic bacteria and cariogenic bacteria and storage stability will be described below.

(1) Porphyromonas gingivalis 3
81 (Porphyromonas gingivalis 381) Antibacterial test method against Porphyromonas gingivalis 381
gingivalis 381) is cultured in a liquid medium under anaerobic conditions at 37 ° C., and when the bacteria grow, they are collected by centrifugation. Further, this bacterium is suspended in physiological saline to obtain a bacterium solution. 0.01 wt% of the samples of Comparative Examples and Examples were added to this bacterial solution,
The cells were cultured at 37 ° C. under anaerobic conditions, and determined by visual observation. “+” Indicates “the bacterium has died and has antibacterial activity”, and “−” indicates “the bacterium has not died and has no antibacterial activity”.

(2) Test method for antibacterial activity against Streptococcus mutans 6715 (0.01% by weight of the samples of Comparative Examples and Examples) was added to a BHI medium containing 1.0% by weight of sucrose. Streptococcus mutans 6715 previously cultured
And cultured at 37 ° C. for 16 hours in an anaerobox gas-exchanged to N ₂ : CO ₂ : H ₂ = 80: 10: 10. After culturing, 0.01M phosphate buffer (pH 7.0)
Wash twice gently with, then add the same amount of the same buffer solution as the culture solution, stir vigorously, perform ultrasonic treatment for about 20 seconds to uniformly suspend plaque, and then use a photometer. 5
The absorbance (turbidity) is measured at 50 mm to determine the amount of attached plaque. As a result, the amount of adhered plaque of the example was represented by 100% when the amount of adhered plaque of the sample of the comparative example was 100%.

(3) Storage stability test method The degree of discoloration after storage at 40 ° C. for 3 months is examined. The samples of the examples and the comparative examples were stored at 40 ° C. for 3 months, and evaluated according to the following criteria. ×: “Discolored and impaired product value” ○: “Discolored”

(4) Practical evaluation test The sample after every meal was used for 20 panelists,
Five-point evaluation was performed on the persistence of flavor and aftertaste after use, and the total score was calculated. (Very good: 5 points, good: 4
Point, normal: 3 points, slightly bad: 2 points, bad: 1 point)

Examples and Comparative Example 1 Liquid dentifrice compositions shown in Table 1 containing eugenol glycosides (Example 1) and those containing no eugenol glycoside (Comparative Example 1) were prepared. The production method was based on a conventional method.

[0022]

[Table 1]

Table 2 shows the evaluation test results of the antibacterial property and the storage stability of Example 1 and Comparative Example 1. The liquid dentifrice of Example 1 exhibited high antibacterial activity against cariogenic bacteria and pathogens of periodontal disease, and was stable without discoloration over time.

[0024]

[Table 2]

Table 3 shows the results of the practical evaluation test performed on Example 1 and Comparative Example 1.

[0026]

[Table 3]

From the results shown in Table 3, Example 1 is Comparative Example 1
As compared with, the flavor was maintained 30 minutes after use, and the total score of the evaluation was high. That is, in Example 1, the change in taste during use was small, the flavor during use was excellent, the flavor after use was changed to develop a new flavor, and the persistence of the flavor after use was excellent.

Example 2 and Comparative Examples 2 and 3 Toothpastes of Example 2 and Comparative Examples 2 and 3 having the compositions shown in Table 4 were prepared and subjected to various tests.

[0029]

[Table 4]

In Example 2, compared to Comparative Examples 2 and 3, Porphyromonas gingivalis 381 (P. gingivalis 38) was used.
1), Streptococcus mutans 6715 (Stre
The antibacterial activity against ptcoccus mutans 6715) was strong, there was little coloration over time, and the flavor was excellent in terms of the flavor at the time of use in a practical test, the persistence of the flavor after use, and the aftertaste.

Example 3 A toothpaste was prepared based on the composition shown in Table 5 according to a conventional method.

[0032]

[Table 5]

Example 4 A toothpaste was prepared according to a conventional method based on the composition shown in Table 6.

[0034]

[Table 6]

Example 5 A toothpaste was prepared based on the composition shown in Table 7 according to a conventional method.

[0036]

[Table 7]

Example 6 An ointment preparation was prepared according to a conventional method based on the composition shown in Table 8.

[0038]

[Table 8]

Example 7 Based on the composition shown in Table 9, gel type oral pasta was prepared according to a conventional method.

[0040]

[Table 9]

Example 8 Based on the composition shown in Table 10, a troche was prepared according to a conventional method.

[0042]

[Table 10]

The composition for oral cavity obtained in Examples 3 to 8 above was used for Porphyromonas gingivalis 381 (P. gingiva).
lis 381), Streptococcus mutans 6715
(Streptcoccus mutans 6715)
The coloring due to the passage of time was small, and the flavor was good when used in a practical test of 20 persons, the persistence of the flavor after use, and the aftertaste.

[0044]

As described above, the present invention is excellent in the effect of preventing dental caries and periodontal disease, is stable without discoloration over time, has little change in taste during use, and has excellent flavor during use. It is clear that it is possible to provide a composition for the oral cavity in which the flavor after use is changed to develop a new flavor and the flavor is maintained for a long time.

Claims (1)

(57) [Claims] 1. An oral composition comprising a glycoside wherein the aglycone part of the glycoside is one or more of eugenol, raspberry ketone, isoeugenol, ginger, capsaicin and vanillin. .