JPS5812250B2 - 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, and is produced as oral bacteria multiply and forms a film that firmly adheres to teeth and gums.

The organic acids and proteolytic enzymes 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 issues such as impairing the taste of the composition or causing bacterial replacement, and enzymes have safety issues such as taking time to act or having antigenic properties. However, I haven't found anything that satisfies me yet.

In view of these circumstances, the present inventors have conducted intensive research to find a highly safe substance that exhibits an excellent effect on inhibiting plaque formation and is suitable for inclusion in oral compositions. , 4,6-dideoxyglucose and 110-methyl-4,6-dideoxyglucose have high antibacterial activity against Streptococcus mutans, a major oral bacterium in dental plaque. It was found that these substances have excellent effects in inhibiting dental plaque formation, and that they are derivatives of glucose and have high safety, leading to the completion of the present invention.

That is, the present invention provides an oral composition containing 4,6-dideoxyglucose and/or 1-0-methyl-4,6-dideoxyglucose.

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 an extremely excellent effect on preventing dental caries, gingivitis, and alveolar pyorrhea. Demonstrate.

Next, we selected various sugar derivatives and tested their antibacterial activity against Streptococcus mutans. The results are shown below.

The test method is as follows.

Heart Infusion Broth Medium C with 1% Cucumber Course
Difc) 2.3 mA' and 2.0 of various sugar derivatives
% (weight %, the same applies hereinafter) aqueous solution, and to this, brain-heart infusion medium (Di
Streptococcus mutans (OM2176 strain) cultured for 18 hours at 37°C in 10 m/ml of N2-CO2 (95
:5) Cultivate at 37°C for 18 hours in a gas-exchanged jar (concentration of each sugar derivative in the medium is 0.08%).

After culturing, 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.

It is clear from Table 1 that amine sugars and methylated sugars do not have antibacterial activity, and even deoxysugars such as glucose and deoxylation in specific positions have antibacterial activity. In particular, it was found that the antibacterial activity of 4,6-dideoxyglucose and 1-0-methyl-4,6-dideoxyglucose was sufficiently satisfactory.

Furthermore, the effects of 4,6-dideoxyglucose and 110-methyl-4,6-dideoxyglucose were clinically tested.

15 subjects with clinically healthy oral conditions
Divided into groups (5 people per group), the first group received a 4,6-dideoxyglucose-containing mouthwash (contains 0.001% of 4,6-dideoxyglucose, see Example 3 below), and the second group received 1
-0-Methyl-4,6-dideoxyglucose combination mouthwash (according to the recipe in Example 3 below)
- dideoxyglucose o. ooi% combination) and the third group were given a placebo mouthwash (prescription of Example 3 described later, except for the sugar derivative), and each group was allowed to use it five times a month for three days.

All subjects underwent scaling to completely remove stains from their teeth before the start of 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 an erythrosin revealing solution, and the status of the plaque adhering to the teeth was evaluated according to the scoring system according to Suzuki et al.'s method [Journal of the Oral Hygiene Society, Vol. evaluated.

The average degree of plaque adhesion of the third group (placebo mouth rinse group) was set as 100, and the average degree of plaque adhesion for each group was calculated.

The results are shown in Table 2. As shown in Table 2, 4,6-dideoxyglucose, and 10-methyl-4,6-dideoxyglucose all exhibit excellent plaque formation inhibiting effects.

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 4,6-dideoxyglucose or 1-Q-methyl-4,6-dideoxyglucose alone or in combination.

The amount to be blended can be appropriately selected depending on the properties of the oral composition, but it is usually o. oooi~1%, preferably 0.001~0.1% is suitable.

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, monofluorinated sodium phosphate, 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 Sorbitol 10 Carboxymethyl cellulose sodium O. 5 Um carrageenan 0.5 Sodium lauryl sulfate 1.5 Sodium saccharin 0.24.6-dideoxyglucose 0.005 Flavor
1 water
100% Preparation Example 2 A toothpaste was manufactured according to a conventional method using the following formulation.

Ingredients % Aluminum hydroxide 40 Glycerin
15 Sorbitol 10 Carboxymethyl cellulose O. 5 um carrageenan 0.5 sodium lauryl sulfate 1.5 saccharin sodium 0.2■-0-methyl-4.6
- Dideoxy 0.001 Siglucose Flavor 1 Water
100% Preparation Example 3 A mouthwash was manufactured according to the conventional method using the following formulation.

Satucalin sodium 0.05 ethanol
25 Glycerin 5 Polyoxyethylene hydrogenated castor oil 2 Fragrance
14,6-dideoxyglucose 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 ingredients
% 1-0-methyl-4,6-dideoxy 0.1 Glucose sucrose monostearate 0.5 Ingredients % Water Adjusted to 100%

Claims (1)

[Claims] 1 4,6-dideoxyglucose i and/or 1-
0-methyl-4,6-dideoxyglucose 0.00
An oral cavity composition characterized by containing 0.01 to 1% by weight.