JPS6040405B2 - anti-dental plaque agent - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to an oral preparation for use on teeth, specifically an anti-dental plaque agent that can effectively suppress the formation of dental plaque that causes cavities and other oral diseases. be.

Certain groups of bacteria in the oral cavity produce sticky polysaccharides such as glucan, forming so-called dental plaque.

The organic acids and toxins produced by the caries-causing bacteria that live in dental plaques can cause oral diseases such as cavities and pyorrhea. Dental plaque is removed by mechanical methods such as the following. However, the use of antibacterial substances often has side effects, and there are restrictions on the usage method and dosage for daily use, and mechanical methods can always clean the entire tooth surface, which has a complex shape and is full of irregularities. It is quite difficult to keep it that way. Therefore, there has been a strong desire to develop oral preparations that are safe, easy to use, and effective in preventing dental caries. As a result of intensive research, the present inventors have found that an oral composition containing water-soluble glucomannan as its main ingredient inhibits the development of dental plaque, which is the initial stage of caries and other oral diseases, and prevents cavities and gums. The present invention was completed by discovering that the present invention is extremely effective in preventing various oral diseases such as inflammation and gingivitis, and has no side effects.

To prevent the development of dental plaque, it is necessary to prevent caries bacteria from attaching to the teeth or suppress their proliferation.
It is known that substances that inhibit the activity of polysaccharide synthase of cariogenic bacteria can be used, but water-soluble glucomannan has an excellent anti-inflammatory effect, as is clear from the experimental results described later. It has dental plaque activity.

Glucomannan is konjac (Amorphophal)
lusKonSagicC. It is a polysaccharide that exists in the tubers or viscous substances of Koch), and its molecules contain a small amount of acetyl groups, carboxyl groups, phosphate groups, and proteins [Nihon Kagaku Zasshi, 73, 533-53
8 (1952)].

Glucomannan itself is commercially available as a health food (trade name: ``Imannan Hamannan Foods Co., Ltd.''), and is also used as a food casing material, food additive (mainly thickener), and as a sustained release agent in pharmaceuticals. However, it has never been used for oral hygiene purposes, and its anti-dental plaque effect was completely unknown. There is a cylindrical type [Industrial Chemistry Magazine 36, 320, 324, 1586 (1933)] and usually both types are mixed.

Water-insoluble glucomannan has almost no anti-dental plaque activity, whereas water-soluble glucomannan has strong anti-dental plaque activity. The anti-dental plaque agent of the present invention has water-soluble glucomannan as its main component, and its amount is 0.1% by weight or more irrespective of the dosage form, but the preferred amount depends on the dosage form. It depends.

Water-soluble glucomannan can be obtained, for example, by washing konjac powder with an organic solvent such as alcohol, removing water-insoluble glucomannan, and then drying. The water-soluble glucomannan used in the present invention is preferably of high purity. Next, the present invention will be explained in detail using experimental examples.

Experimental Method A portion of the preserved mother liquor of Streptococcus mutans is taken and added to a freshly prepared liquid tower of Tryptocase soy broth and cultured for 2 hours.

After culturing, centrifuge for 15 minutes (300 pm) and prepare a bacterial suspension (1 to 18 cells) using isotonic phosphate buffer. On the other hand, a bovine incisor tooth of 1 to 3 years old was cleaned and polished and soaked in a glucomannan sample solution at 370° C. for 30 seconds. After a brief rinse with isotonic phosphate buffer,
The bovine incisors are immediately transferred to the cocoon suspension prepared in advance and shaken gently at 370 for 3 minutes. Thereafter, the incisors were cultured in Tryptocase soy flose containing 2% sucrose, and the medium was replaced with fresh medium every 4 hours.
After 86 Terama culture at 370°C, rinse with isotonic phosphate buffer, then incubate in 9.3% formalin-containing phosphate buffer for 2 hours.
Let it soak for a day.

After thoroughly washing with water and drying, the specimen is stained with U) ffler's methylene fluoride solution and examined under a microscope.

Anti-dental plaque activity was determined by the number of colony-forming unit bacteria in a unit area of the sample. Anti-Dental Black Activity The anti-dental plaque agent of the present invention can be used in various forms.

In liquid form, in addition to those in a solution state in which the components are clearly dissolved, those in which an emulsifier or suspending agent is added as necessary to form an emulsion or suspension are used. In solid form, in addition to tablets such as gargling tablets, sublingual tablets, chewable tablets, and troches, it is also used as a powder for chewing gum, bonbons, and powdered toothpaste. In semi-solid form, it can be used as toothpaste, oral cream, or oral paste. Among these, preferred are toothpastes, mouthwashes (mouthwash and gargle types), oral pastes, chewing gum, chewable tablets,
These include bonbons for shiyaburome. Furthermore, the anti-dental plaque agent of the present invention may contain substances having various medicinal effects, such as aluminum alanthinate, common salt, fluoride, glycyrrhizinate, hinokitiol, azureso, and dextrose. Stranase,
z-aminocaproic acid, lysozyme, tranexamic acid,
Examples include substances having antibacterial effects such as 1,6-bis-diguanidohexanes (for example, chlorohexidine), sodium N-lauroyl sarcosinate, sucrose fatty acid esters, alkylamines, and sodium ricinoleate. Next, typical forms of use will be explained. (All percentages hereinafter indicate weight percentages.) Toothpaste: The blending ratio of glucomannan can be selected as appropriate depending on the prescription, but is usually 0.1 to 5.0%.
, preferably from 0.1 to 0.1, which can be dissolved or uniformly dispersed in the base material.
It is 1.0%.

The abrasive is blended in a proportion of about 0.5 to about 95%, preferably about 6 to about 60% for toothpastes, and about 20 to about 95% for powdered toothpastes. The diameter of the abrasive is 0.1
~20 types of calcium carbonate, dicalcium orthophosphate dihydrate, calcium pyrophosphate, calcium polymetaphosphate,
Polysodium metaphosphate and the like are used. A binder can be added to toothpaste and liquid toothpaste at a rate of 0.5 to 5.0%. Examples of binders include polyvinyl alcohol, methylcellulose, ethylcellulose, hydroxyethylcellulose, hydroxymethylcellulose, water-soluble salts of cellulose ethers (for example, sodium carboxymethylcellulose, sodium hydroxyethylcellulose, etc.), natural rubber (for example, karaya gum, gum arabic, gum tragacanth), carrageenan, colloidal magnesium aluminum silicate, or fine silica. Glycerin, sorbitol, and other edible polyhydric alcohols up to 36% may be added as heat insulating agents. When adding a foaming agent, add a small amount of sodium lauryl sulfate, sodium lauroyl sarcosinate, etc. In addition, commonly used flavoring agents, sweeteners, and other non-ionic substances such as polyoxyethylene fatty acid esters, polyoxyethylene higher alcohol ethers, polyoxyethylene sorbitan fatty acid esters, and glycerin monofatty acid esters are also available. A suitable amount of surfactant can be added. Gargle: The ratio of glucomannan to the gargle can be selected as appropriate depending on the prescription, but is usually preferably about 0.1% to about 0.2%.

As the solvent, water, an aqueous glycerin solution, an aqueous glycerin/ethanol solution, and an aqueous propylene glycol solution are preferred, but in addition to these, an aqueous ethanol solution, an aqueous isopropanol solution, an aqueous n-propanol solution, an aqueous solpitol solution, and the like can be used. Furthermore, flavoring agents, sweeteners, and surfactants can be added in the same way as toothpastes. Oral paste: The ratio of glucomannan to the oral paste can be selected as appropriate depending on the prescription, but is usually about 0.1 to about 1.0.
% is preferred.

Base materials include Vaseline and Plastibase.
(manufactured by Squibb), polyethylene glycol, a mixture of vegetable oil and beeswax, etc. are used. In addition, flavoring agents, sweeteners, heat-retaining agents, surfactants, and the like can be added as necessary, similar to dentifrices. Bonbon: The blending ratio of glucomannan in the bonbon to make it soft can be selected as appropriate depending on the prescription, but it is usually about 1.0%.
The above is preferable.

Sorbitol, mannitol, cocoa butter, or a mixture of two or more of these may be used as the base material. In addition, flavoring agents, sweeteners, heat retaining agents, surfactants, etc. can be added as necessary, similar to toothpastes. The usage form of the anti-dental plaque agent of the present invention will be specifically explained below with reference to Examples, but the present invention is not limited thereto. Reference Example Extraction method of water-soluble glucomannan Thoroughly stir commercially available konjac flour in methanol and discard the supernatant liquid immediately after cooling.

Repeat the same operation until the toplight liquid becomes clear. The precipitate is taken out of the oven, washed with ether, and air-dried at room temperature. Example 1 Glucomannan was first added to distilled water according to the following recipe,
After mixing well, make toothpaste according to the usual method.

(%) Glucomannan
0.5 dicalcium phosphate dihydrate 44
．． 7-hydroxymethyl cellulose sodium 0.
5 power raginan 0
．． 5 Glycerin 10 Sorbitol 10 Sodium saccharin 0.2 Flavoring
1.0 Sodium lauryl sulfate 1.0 Distilled water
31.6 Example According to the second prescription,
A toothpaste is made according to a method similar to Example 1.

(%) Glucomannan 0.
3 Calcium carbonate 40 Ruboxymethyl cellulose 0.5 Laginan 0.
5 Glycerin 15 Sorbitol 10 Light silicic anhydride 1.5 Distilled water
32.2 Example 3 A toothpaste is prepared according to the following recipe according to a conventional method.

(%) Dicalcium phosphate 5
0 Calcium carbonate 26 Sorbitol 15 Sodium lauryl sulfate 1 Saccharin
0.1 fragrance
0.9 glucoma nnan
1.0 distilled water
6 Example 4 A toothpaste is prepared according to the following recipe according to a conventional method.

(%) Glycerin
30 Sodium polyacrylate 55 Saccharin 0.1
Fragrance 09 lauryl ethanolamide 0.5 alcohol
Le 1.0 Glucomannan 1.0 Distilled water
11.5 Example 5 A gargle is prepared according to the following recipe.

(%) Glucomannan
0.2 Glycene (Japanese Pharmacopoeia) 8.
5 dye solution (Blue No. 3), 0.4% 0.
01 Hatsuka oil 0.
15 ethanol
3.0 Distilled water 8
8.14 Example 6 Chewable tablets are manufactured according to the following formulation.

<%) Mannitol 9
2 glucomannan 2
．． 0 Macrogol 6000 (Japanese Pharmacopoeia) 3
．． 5 Methylcellulose (Product name: Metrose SM400
) 0.7 Light silicic anhydride 1.0 Magnesium stearate 0.5 Tulk
0.3 Example 7
Make chewing gum according to the following recipe.

(%) Gum base
65.5 mannitol
28.0 Glucomannan
5.0 glycerin
0.5 fragrance
1.0 Example 8 An oral paste is prepared according to the following recipe.

(%) Macrogol 4000 (Japanese Pharmacopoeia)
48 Macrogol 400 (Japanese Pharmacopoeia) 4
8 Glucomannan 3 Carpopol 934 (product name) 0.5 Flavor
0.5 Example 9 An oral paste is prepared according to the following recipe.

(%) White petrolatum 90
Liquid paraffin 7.5 Glucomannan 2.0 Flavor 0.5 Example 10 A bonbon for Shiyabu is made according to the following recipe.

Claims (1)

[Claims] 1. An anti-dental plaque agent containing water-soluble glucomannan as a main component. 2. The anti-dental plaque agent according to claim 1, which is in liquid form. 3. The anti-dental plaque agent according to claim 1 in solid form. 4. The anti-dental plaque agent according to claim 1, which is in semi-solid form.