JPS5812254B2 - 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 composed of oral bacteria and their metabolites, and is produced when oral bacteria adhere firmly to teeth and gums in the form of a film and multiply.

Organic substances 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, various types of disinfectants such as chlorhexidine, enzymes such as dextranase, or sugars such as xylitol have been used to suppress the growth of oral bacteria and to decompose plaque constituent substances and suppress the formation of plaque. It is blended into oral compositions.

However, bactericidal agents have problems in terms of safety, such as impairing the taste of the composition or bacterial replacement phenomenon, and enzymes and sugars have problems in terms of effectiveness, such as low plaque formation inhibiting effect.
I haven't found anything that satisfies me yet.

On the other hand, in recent years, Streptococcus mutans, a major oral bacterium in dental plaque, has been
It has been reported that mutanase, an enzyme that decomposes the insoluble sticky glucan that is produced by dental cartilage, effectively suppresses the formation of dental plaque [Journal of Dental Research, Vol. 51, Suppl, p. 394] (1972)
].

However, the effects of mutanase are not completely satisfactory.

The present inventors have conducted various studies on inhibiting dental plaque formation, and have unexpectedly discovered that the combined use of mutanase and dextran or certain dextran derivatives exhibits an extremely excellent inhibitory effect on dental plaque formation. heading,
This led to the completion of the present invention.

That is, the present invention provides an oral composition comprising mutanase and dextran or diethylaminoethyldextran.

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

Next, the results of testing mutanase, dextranase, dextran, various dextran derivatives, and various saccharides alone or in combination to inhibit plaque formation are shown.

The test method is as follows.

Pour 2.3 ml of heart infusion broth medium containing 5% sucrose (manufactured by Difco) into a test tube.
d, and add 0.1 ml of each sample aqueous solution).

To this, Streptococcus mutans (OMz17) was cultured in advance at 37°C for 18 hours in 10 ml of Brain-Heart Infusion Medium (manufactured by Difco).
Add 0.1 d of the 100 times diluted solution of 6) and hold the test tube at an angle of 8.
Maintain at 5°C and culture at 37°C for 18 hours.

After culturing, the culture medium was discarded, the bacterial cells adhering to the tube wall (possibly similar to dental plaque) were washed once with physiological saline, and 2.5 d of 0.5N sodium hydroxide solution was added. Disperse and suspend the bacterial cells.

After standing for 30 minutes, the solution is stirred and the absorbance at 550 nm (specimen turbidity) is measured.

As a control, absorbance (control turbidity) is measured in the same manner using the same amount of water instead of the sample aqueous solution.

From these values, the plaque generation inhibition rate is calculated according to the following formula.

Specimen aqueous solution (1) Mutanase (50,000 units/P) 0.05% (wt%, same hereinafter) aqueous solution.

(2) Dextranase (1 million units/t) 0. 0
0 0 5% aqueous solution.

(3) Diethylaminoethyldextranase 0.25
% aqueous solution (concentration in medium 0.01%).

(4) Dextran, other dextran derivatives, or various saccharide 0.5% aqueous solution (concentration in medium: 0.02%).

The results are shown in Table 1 below.

As is clear from Table 1, among substances other than mutanase and dextranase, dextran, diethylamine ethyl dextran, and aluminum carboxymethyl dextran exhibit an inhibitory effect on plaque formation, but even when these substances are used in combination with dextranase, Its effectiveness does not improve.

However, unexpectedly, it has been found that when dextran or diethylaminoethyl dextran is used in combination with mutanase, the effect of inhibiting dental plaque formation is mutually improved.

Additionally, the effects of mutanase, dextran and diethylaminodextran were tested clinically.

Thirty subjects (24 men, 6 women) with clinically considered healthy oral conditions were divided into 6 groups (5 people per group).
The group received a mouthwash containing 1% mutanase (50,000 units/1) (a mouthwash based on the formulation of Example 3 below, the same applies hereinafter), and the second group received 0.1% dextran (molecular weight 2 x 105). % combination mouthwash. The third group contained diethylaminoethyl dextran (molecular weight 2 x 105, number of moles added 1.2/AGU) 0.
1% mouthwash, Group 4 had 1% mutanase and 0.1% dextran, Group 5 had 1% mutanase and 0.1% diethylaminoethyldextran.
The combined mouthwash and the 6th group received a placebo mouthwash (without mutanase, dextran, and diethylamine ethyldextran), and each was used 5 times daily for 3 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 erythrosine 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 Oral Hygiene, Vol. 20, No. 9, (1971)]. was evaluated.

Group 6 (placebo mouth rinse group) The average degree of plaque adhesion was calculated.

The results are shown in Table 2.

As shown in Table 2, it is clear that when mutanase and dextran or diethylamine ethyldextran are used in combination, the plaque formation inhibiting effect is mutually improved.

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 mutanase and dextran or diethylaminoethyldextran.

The dextran and diethylaminoethyl dextran used may be any commonly available ones, but the dextran has an average molecular weight of 103 to 107, the diethylaminoethyl dextran has an average molecular weight of 103 to 107, and the average number of added moles of diethylamine ethyl groups is 0.1/AGU to 2.
．． 9/AGU (AGU: Anhydrous Gluc
ose Unit) is preferred.

In addition, the amount of these compounds can be appropriately selected depending on the properties of the desired composition, but usually (1000
1-5%, preferably 0.001-1% is suitable.

The blending amount of mutanase is 5,000 to 5,000 to the entire composition.
0.1 to 2.0% is suitable for 1 million units/g.

Note that 1 unit of mutanase is 0. 2 M acetate buffer (
It refers to the amount of enzyme that decomposes mutan at 40°C in pH 5.5) and liberates 1 μg of reducing sugar per minute in terms of glucose.

The oral composition of the present invention can be prepared using conventional methods such as toothpaste, powdered toothpaste,
It can be in the usual dosage forms such as toothpastes such as liquid toothpastes, mouthwashes such as mouthwashes, pasta, pastilles, etc.

Other ingredients may be any commonly used ingredients; for example, in the case of toothpaste, wetting agents such as glycerin and sorbitol, dicalcium phosphate, calcium carbonate, silicic anhydride, aluminum hydroxide, calcium pyrophosphate, insoluble sodium metaphosphate, etc. abrasives, foaming agents such as sodium lauryl sulfate, sodium acylsarcosinate,
Binder such as sodium carboxymethylcellulose, carrageenan, sodium alginate, bentonite,
Sweeteners, flavoring agents, monofluorous 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 Ingredients % Glycerin 15 Sorbitol 10 Carboxymethyl cellulose nat 0.5 Lium casiginan 0.5 Sodium lauryl sulfate 1.5 Sodium saccharin
0.2 Mutanase (50,000 units/f!)
0. 1 dextran (molecular weight 9400)
1 Fragrance 1 Water Adjusted to 100% 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 0.5 Lium carrageenan 0.5 Sodium lauryl sulfate 1.5 Sodium saccharin
0.2 Mutanase (500,000 units/t)
0.1 diethylaminoethyl dextran (molecular weight 5 x 104, added mole 0.01 number 1.0
/AGU) Fragrance 1 Water Adjusted to 100% 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 hydrogenated castor oil 2 Flavor 1 Mutanase (50,000 units/1) 1 Dextran (molecular weight 2XIQ') 0.1 Water
Example of adjustment to 100%
4. A troche was manufactured according to the conventional method using the following recipe.

Ingredients % Gum arabic 6 glucose
72 Mutanase (500,000 units/g) 1 Diethylaminoethyldextran (molecular weight 2 x 105, added mole 0.001 number 1.
0/AGU)

Claims (1)

[Claims] 1 Mutanase (5000-1 million units/g) at 0.
1 to 20% by weight and dextran with an average molecular weight of 103 to 107 or 0.0001 to 5 of diethylaminoethyl dextran with an average molecular weight of 103 to 107 and an average number of added moles of diethylaminoethyl groups of 0.1 to 2-9/AGU.
An oral composition characterized by containing % by weight.