JPS5812253B2 - 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 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 menichlorhexidine and enzymes such as dextranase have been used in various oral compositions to inhibit the growth of oral bacteria and decompose plaque constituent substances to 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 various studies on the inhibition of plaque formation, and have found that certain highly safe dextran derivatives have been found to be effective against Streptococcus mutans (Streptococcus mutans), a major oral bacterium in dental plaque. S treptoc
occus mutans) from adhering to the hard surface of teeth and effectively suppressing the formation of dental plaque.
This led to the completion of the present invention.

That is, the present invention provides an oral composition containing diethylaminoethyldextran.

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 testing the plaque formation inhibiting effects of dextran derivatives in each food are shown.

The test method is as follows.

2.3 ml of heart infusion broth medium supplemented with 5% sucrose (manufactured by Difco) is placed in a test tube, and 0.1 ml of a 0.5% (wt%, same hereinafter) aqueous solution of various dextran derivatives is added thereto.

To this, Streptococcus mutans (OMZ176) was cultured in advance at 37°C for 18 hours in 10 ml of plain heart infusion medium (manufactured by Difco).
), add 0.1 ml of 100 times diluted solution, and hold the test tube at an angle of 8.
The cells are maintained at 5° and cultured at 37° C. for 18 hours (the concentration of dextran derivative in the medium is 0.02%).

After culturing, the culture medium was discarded, and the bacterial cells (which are thought to be similar to dental plaque) adhering to the tube wall were washed once with raw saline solution, and 0.5N sodium hydroxide solution 2. Add 5 ml to 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 dextran derivative aqueous solution.

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

As shown in Table 1, the results are shown in Table 1. Among various dextran derivatives, diethylaminoethyl dextran was found to have a remarkable effect of inhibiting dental plaque formation.

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

Three groups (1
The first group received dextran (molecular weight 2X
105) 0.1% compounded mouthwash (mouthwash according to the formulation of Example 3 described later, the same applies hereinafter), and the second group contained diethylaminoethyldetrane (molecular weight 2 x 105, number of added moles 1. 2/AGU) 0.1% combination washirrhea, and the third
The groups were given a placebo mouthwash (without dextran and diethylaminoethyldextran), and each was given 5 times daily.
It was used 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 fungi was stained with erythrosine revealing solution, and the plaque adhesion to the teeth was determined according to the scoring system according to the method of Suzuki et al. [Journal of the Oral Hygiene Society, Vol. 20, No. 9, (1971)]. Assessed the condition.

The average degree of plaque adhesion for the third group (placebo mouthwash group) was calculated.

The results are shown in Table 2. As shown in Table 2, it is clear that diethylamine ethyl dextran exhibits an excellent effect of inhibiting tooth formation.

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

Thus, diethylaminoethyl dextran is incorporated into the oral composition of the present invention.

The molecular weight of the diethylamine ethyldextran used and the number of added moles of diethylaminoethyl groups are not particularly limited, but generally, the average molecular weight is lO3 to 107, and the average number of added moles of diethylaminoethyl groups is 0.1/AGU to
2.9/AGU (AGU: Anhydrous Glu
0.0001 to 1% of the total composition, preferably 0.0001% to 1%, preferably 0.0001% to 1% based on the total composition.
0.001 to 0.1% is appropriate.

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 birophosphate, insoluble sodium metaphosphate, etc. abrasives, foaming agents such as sodium lauryl sulfate, sodium acylsarcosinate, and sucrose fatty acid esters, binding agents such as sodium carboxymethylcellulose, carrageenan, sodium alginate, and bentonite, sweeteners, fragrances, sodium monofluorophosphate, and 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 % dibasic calcium phosphate di-aqueous phase 45 glycerin 15 sorbitol 10 carboxymethyl cellulose 0.5 thorium carrageenan 0.5 sodium lauryl sulfate 1.5 saccharin sodium
0.2 Diethylamine ethyl dext 0.005 run (molecular weight 5 x 104, number of moles added 1.0/AGU) Flavor and fragrance 1 Water Adjusted to 100% Example 2 A toothpaste was produced according to the conventional method using the following formulation.

Ingredients % Aluminum hydroxide 40 Glycerin 15 Sorbitol 10 Carboxymethylsenorelosena 0.5 Thorium carrageenan 0.5 Sodium lauryl sulfate 1.5 Sodium saccharin
0.2 diethylaminoethyldex}
0.001 run (molecular weight 2 x 105, number of added moles 1.0/AGU) Fragrance 1 Water Adjusted to 100% Example 3 A mouthwash was manufactured according to the conventional method using the following formulation.

Ingredients % Sodium saccharin 0.05 Ethanol 25 Glycerin
5 Polyoxyethylene hardened castor 2 Oil fragrance 1 Diethylaminoethyl dext 0.001 run (
Molecular weight: 2 x 106, number of moles added: 1.2/AGU) Water Adjusted to 100% Example 4 A troche was produced according to a conventional method using the following recipe.

Ingredients % Gum arabic 6 glucose
72 Diethylaminoethyl dext 0.1 run (molecular weight 1 x 105, number of moles added 0.6/AGU) Sucrose monostearate ester 0.5 l

Claims (1)

[Claims] 1. An oral composition comprising 0.0001 to 1% by weight of diethylaminoethyl dextran having 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.