JPS5812251B2 - Oral composition - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an oral composition, and more particularly to an oral composition that effectively suppresses the formation of dental plaque that causes dental caries and alveolar pyorrhea.

Dental plaque is made up of oral bacteria and their metabolites, so to speak.
It is a home for oral bacteria, is produced as oral bacteria multiply, and forms a film that firmly adheres to teeth and gums.

Organic acids, proteolytic enzymes, and the like produced by oral bacteria in this dental plaque cause dental caries, and gingivitis and alveolar pyorrhea.

Therefore, suppression of dental plaque formation is an important means for preventing the occurrence of dental caries, gingivitis, and alveolar pyorrhea.

Conventionally, bactericidal agents such as chlorhexidine and enzymes such as dextranase have been used in various oral compositions to suppress the growth of oral bacteria and to decompose plaque constituent substances and suppress the formation of plaque. It is blended.

However, disinfectants have safety concerns such as impairing the taste of the composition or causing bacterial replacement, and enzymes have safety concerns such as taking time to act or having antigenicity. I have a problem with this, and I haven't found anything that satisfies me yet.

On the other hand, recently, Streplecochus mutans (S tr
2-deoxyglucose has been reported as a substance that has antibacterial activity against Eptococcus mutans [Journal of Dental Research,
Vol. 54, No. 3, p. 433 (1975)).

However, its antibacterial activity is still insufficient.

While carrying out various studies on inhibiting the formation of dental plaque, the present inventors unexpectedly discovered that when a certain sugar derivative, which itself exhibits almost no antibacterial properties, is used in combination with 2-deoxyglucose, its antibacterial activity is significantly improved. This led to the completion of the present invention.

That is, the present invention provides 2-deoxyglucose and 2-deoxyglucose.
An oral composition containing deoxygalactose is provided.

The oral composition of the present invention can effectively suppress the formation of dental plaque without problems such as bacterial replacement or antigenicity, and has extremely excellent effects in preventing dental caries, gingivitis, and alveolar pyorrhea. Demonstrate.

Next, the results of tests on the antibacterial activity of 2-deoxyglucose and various other sugar derivatives against Streptococcus mutans and the antibacterial activity of a combination of 2-deoxyglucose and other sugar derivatives are shown.

The test method is as follows.

Heart infusion broth medium with 1% glucose (
Difc porcelain) 2.2d and 2-deoxyglucose 2.
Add 0.1 ml of 0% (wt%) aqueous solution and/or 1.0% aqueous solution (klm) of various other sugar derivatives and stir well. 37 in 10ml
A 100-culture dilution of Streptococcus mutans (OM2 176 strain) cultured at ℃ for 18 hours was diluted with 0.1
ml and cultured at 37°C for 18 hours in a jar with N2-Co2 (95:5) gas exchange (concentration of 2-deoxyglucose in the medium 0.08%, concentration of other sugar derivatives 0.0)
4%).

After the culture is completed, stir well and measure the absorbance of the medium at 660 nm (specimen turbidity).

As a control, the same amount of water was used instead of the sugar derivative aqueous solution,
Measure the absorbance (control turbidity) using the same procedure.

From these measured values, the suppression rate is calculated according to the following formula.

The higher the inhibition rate, the stronger the antibacterial activity is judged to be.

The results are shown in Table 1 below.

As is clear from Table 1, sugar derivatives other than 2-deoxyglucose do not exhibit antibacterial activity at this concentration, and substances other than 2-deoxygalactose improve antibacterial activity even when used in combination with 2-deoxyglucose. do not.

However, 2-deoxygalactose specifically improves the antibacterial activity of 2-deoxyglucose.

Table 2 shows the results of testing the antibacterial activity by varying the concentration of 2-deoxygalactose in the medium in the same manner as in Table 1.

As shown in Table 2, as the concentration of 2-deoxygalactose increases, the antibacterial activity of 2-deoxyglucose improves.

Furthermore, the effect of using 2-deoxyglucose and 2-deoxygalactose in combination was clinically tested.

20 subjects with clinically healthy oral conditions
Divided into groups (5 people per group), the first group received a 2-deoxyglucose-containing mouthwash (containing only 0.001% 2-deoxyglucose according to the prescription in Example 3 below), and the second group received a −
A mouthwash containing deoxygalactose (contains only 0.001% 2-deoxygalactose according to the formulation in Example 3 below), and a third group contains a mouthwash containing 2-deoxyglucose and 2-deoxygalactose (example 3 below). ) and Group 4 were given a placebo mouthwash (prescribed in Example 3 below without the sugar derivative), and each was used five times daily for three days.

All subjects underwent scaling to completely remove stains from their teeth before starting the study, and were prohibited from performing oral cleaning other than mouthwash during the study period.

After 3 days, the plaque adhering to the teeth was stained with erythrosin revealing solution, and the state of the plaque adhering to the teeth was evaluated according to the scoring system according to the method of Suzuki et al. [Journal of the Oral Hygiene Society, Vol. 20, No. 9 (1971)]. evaluated.

The average degree of plaque adhesion in the fourth group (placebo mouthwash group) was set as 100, and the average degree of plaque adhesion for each group was calculated.

The results are shown in Table 3.

As shown in Table 3, it is clinically recognized that when 2-deoxyglucose and 2-deoxygalactose are used in combination, an excellent plaque formation inhibiting effect is exhibited.

During the test period, no side effects such as changes in the taste of food or peeling of the oral mucosa were observed.

Thus, the oral composition of the present invention contains 2-deoxyglucose and 2-deoxygalactose.

The amount of 2-deoxyglucose can be selected as appropriate depending on the properties of the oral composition, but usually 0.0001 to 1%, preferably 0.001 to 0.1%, of 2-deoxyglucose is added to the entire composition.
%, it is appropriate that the amount of 2-teoxygalactose is 0.1 to 10 times the amount of 2-deoxyglucose.

The oral composition of the present invention can be prepared using conventional methods such as toothpaste, powdered toothpaste,
It can be in the form of a toothpaste such as a liquid toothpaste, an oral cleansing agent such as a mouthwash, a pasta, a troche, and the like.

Other ingredients may be any commonly used ingredients, such as humectants such as glycerin and sorbitol for toothpaste,
Dicalcium phosphate, calcium carbonate, silicic anhydride,
Abrasive agents such as aluminum hydroxide, calcium pyrophosphate, and insoluble sodium metaphosphate, foaming agents such as sodium lauryl sulfate, sodium acylsarcosine, and sucrose fatty acid esters, binders such as sodium carboxymethyl cellulose, carrageenan, sodium alginate, and bentonite, and sweeteners. Agents, fragrances, sodium monofluorophosphate, anti-inflammatory agents, and other medicinal agents can be added.

Next, the present invention will be explained in more detail with reference to Examples.

Example 1 A toothpaste was manufactured according to a conventional method using the following formulation.

Ingredients % Dicalcium phosphate trihydrate 45 Glycerin 15 Nnorevit 10 Sodium carboxymethyl cellulose 0.5 Carrageenan 0.5 Sodium lauryl sulfate 1.5 Sodium saccharin
0.22-deoxyglucose 0.
012-deoxygalactose 0.001 Fragrance 1 Water Adjusted to 100% Example 2 A toothpaste was manufactured according to the conventional method using the following formulation.

Ingredients % Aluminum hydroxide 40 Glycerin 15 Nnolevit 10 Carboxymethyl cellulose 0.5 Thorium carrageenan 0.5 Sodium lauryl sulfate 1.5 Sodium saccharin
0.2 ingredients
% 2-deoxyglucose 0.01 2-deoxygalactose 0.01 Flavor
1 Adjustment to 100% water Example 3 A mouthwash was manufactured according to a conventional method using the following formulation.

Ingredients % Sodium saccharin 0.05 Ethanol 25 Glycerin
5 Polyoxyethylene hardened castor 2 Oil fragrance 1 Ingredients % 2-deoxyglucose o-ooi2-deoxygalactose 0.001 water
Adjustment to 100% Example 4 A troche was manufactured according to the conventional method using the following recipe.

Ingredients % Gum arabic 6 glucose
72 2-deoxyglucose 0.0012-deoxygalactose 0.1 sucrose monostearate ester 0.5

Claims (1)

[Claims] 1 0.0001 to 1% by weight of 2-deoxyglucose
and 2-deoxygalactose in an amount of 0.1 to 10 times the amount of 2-deoxyglucose.