KR20070102184A - Oral composition with improved antimicrobial property - Google Patents

Abstract

An oral composition is provided to improve antibacterial effects on harmful bacteria in oral cavity, thereby inhibiting plaque on the teeth and preventing oral disease and gingival ailments including gingivitis and periodontitis by adding the willow extract into a cationic sterilizer. An oral composition for preventing oral disease and gingival ailments comprises (i) 0.01-5 wt.% of a cationic sterilizer selected from cetyl pyridium chloride, hexal konium chloride, benzal konium chloride and chlorhexidine and (ii) 0.1-2 wt.% of the willow extract which is prepared by extracting willow branches in extraction solvent such as purified water and ethanol, and filtering, concentrating and drying the extract.

Description

Oral Composition with improved antimicrobial property

The present invention relates to a composition for oral cavity excellent in antimicrobial activity, and more particularly, containing a cationic fungicide and willow extract has excellent antimicrobial activity against oral bacteria, preventing oral diseases and gum disease, and excellent in removing dental plaque. It is about.

Oral diseases are generally caused by various bacteria living in the oral cavity. These bacteria can be divided into bacteria that cause tooth decay and gum disease. Examples of the bacteria that cause tooth decay include Streptococcus mutans and periodontal disease-derived Popyromonas jinbaris ( P. gingivalis ). Various fungicides have been used in oral products to remove such oral bacteria. Fungicides used in oral products include cetylpyridinium chloride, hexahalonium chloride, benzalkonium chloride, decarinium chloride, chlorohexidine, triclosan, thymol, isopropylmethylphenol and alkyldiaminoethylglycolic acid. Raw materials, polyphenols that are natural extraction components, and silver components. These fungicides follow a mechanism of cationic fungicides that are targeted to anionic phosphate or carboxyl groups on the surface of bacteria to inhibit enzymes on the cell wall and eventually destroy the cell wall of the bacteria to sterilize.

On the other hand, as interest in natural extracts has increased recently, studies on various plants have been actively conducted. As the effects on the oral cavity are known, many plant extracts have been applied to oral compositions related to oral disease prevention and bad breath control.

Korean Patent Publication No. 2005-0010082 is a harmless to the human body by adding a silver solution, silver powder or silver thin film known as a natural antibiotic substance has excellent sterilization and antibacterial effect, while whitening teeth and refreshing the mouth A composition is provided.

Korean Laid-open Patent No. 2005-0035954 contains lignan derivatives having high antimicrobial activity against S. mutans , a decay-causing bacteria, and P. gingivalis , a periodontal disease-causing bacterium. The present invention provides an effective antimicrobial agent for preventing tooth decay and gum disease, and uses it in a composition of various formulations such as toothpaste composition, mouthwash, gum and candy.

Korean Patent Laid-Open No. 2001-0001476 provides an oral composition containing oral fungicides, periodontal disease inhibitors and flavonoids to suppress bad breath by removing bacteria, periodontal disease and odor causing substances in the oral cavity. At this time, oral fungicides are used to provide a composition prepared using one or two or more selected from triclosan, cetylpyridinium chloride, sanguinarin, thymol and the like.

Korean Patent Application No. 2001-0026581 contains clove extract, which provides a refreshing feeling in the mouth, and has an excellent effect in preventing bad breath and gum disease due to antibacterial activity, and has an analgesic effect that conventional cleaning agents do not have. A clean composition is provided.

Korean Patent Application No. 1998-0014437 provides an oral composition effective for removing plaque, preventing bad breath and removing tooth coloring materials by preventing the degradation of the bactericidal activity of water-insoluble noncationic fungicides such as triclosan by adding porous calcium carbonate. .

Korean Patent Application No. 2001-0035980 discloses a toothpaste manufacturing method using green tea extract. The high antibacterial activity of the catechin component, the main ingredient of green tea extract, is excellent in antibacterial action and anti-cavities, and it is excellent in removing bad breath in the mouth.

Korean Patent Application No. 2001-0006218 discloses a composition for promoting oral hygiene containing a pomegranate extract. Pomegranate extract has an excellent effect of inhibiting the generation of free radicals and nitric oxide, indicating that it has a role in enhancing oral hygiene through this antioxidant effect.

In this way, various fungicides and plant extracts are used for the purpose of preventing tooth decay, preventing gum disease, and preventing bad breath. However, in most cases, the effect is insignificant and shows good effects. There is a difficulty.

Accordingly, the present inventors have steadily studied a stable composition showing a better effect on the prevention of various oral diseases, as a result of combining the willow extract that has been used for oral protection from the cationic fungicide used in the conventional oral composition from ancient times When it was found to exhibit an excellent effect on the removal of plaque as well as prevention of oral disease and gum disease, and completed the present invention.

Therefore, it is an object of the present invention to provide a composition for oral cavity having excellent antibacterial activity against oral bacteria and preventing gum disease and excellent plaque removal effect by containing a cationic fungicide and willow extract.

In order to achieve the above object, the present invention provides a composition for oral cavity containing the cationic fungicide and willow extract as an active ingredient.

Hereinafter, the present invention will be described in more detail.

Cationic disinfectants for use in the present invention is representative oral bacteria, Streptococcus mutans a result of an experiment on the (S. mutans), 4 quaternary ammonium salts, and biguanide-based disinfectant from the disinfectant has been used in conventional oral composition The antimicrobial activity of was found to be the best compared to other fungicides.

Specific examples of the cationic fungicides include cationic ammonium salt fungicides such as cetylpyridinium chloride, hexalconium chloride, and benzalkonium chloride, and bisguanide derivatives such as chlorohexidine. They sterilize harmful bacteria in the oral cavity to prevent plaque formation and prevent plaque and show excellent effects on various gum diseases including gingivitis and periodontitis. It has also been found to be safe when used at a suitable low concentration and is used predominantly in oral hygiene products such as mouse washes.

On the other hand, willow, also called yangji tree, has been widely used by Korean people since ancient times, and records of Korea and Japan have been found to keep the mouth clean by using willow branches for brushing after eating. In particular, a Japanese document states that fern is used as the best dental caries prevention method in Japan. (丹羽 源 男: When did the Japanese begin to brush teeth ?, Journal of the Korean Dental Association, 39: 2, pp 3 -6, 1982). In particular, it was confirmed that salicylic acid extracted from willows was used for oral inflammation (Schmid H, Kotter L, Heide I .: Pharmacokinetics of salicin after oral admistration of a standardized willow back extract.Eur J Clin Phamacol 57: 387-391, 2001).

The willow extract used in the present invention was extracted by dipping the willow branches in an extraction solvent, filtering, concentrating the extract, and drying the extract. As the extraction solvent used at this time, one or two or more solvents such as purified water and ethanol were mixed and used for extraction.

In the present invention, by combining the cationic fungicide and willow extract together, it is characterized by providing more excellent antimicrobial effect, oral disease prevention, gum disease prevention and plaque removal effect.

In the present invention, the cationic fungicide is contained in an amount of 0.01 to 5% by weight based on the total weight of the composition. This is because if less than 0.01% by weight, it is difficult to expect a large antibacterial effect, if it exceeds 5% by weight because of the bitter taste of the cationic fungicide raw material itself, there is a problem that the bitter taste of the composition is too strong and difficult to use.

In addition, the present invention contains willow extract in an amount of 0.1 to 2% by weight based on the total weight of the composition. This is because if less than 0.1% by weight it is difficult to obtain the desired effect, if it exceeds 2% by weight it is difficult to give a good feeling with the unique taste and aroma of the extract.

The composition for oral cavity of this invention is not specifically limited in the formulation, Specifically, it may have formulations, such as a toothpaste, a mouthwash, oral cleansing agent.

In particular, the toothpaste may contain abrasives, wetting agents, foaming agents, binders, sweeteners, pH adjusting agents, preservatives, active ingredients, fragrances, brighteners, pigments, solvents and the like.

Examples of the abrasive include calcium carbonate, precipitated silica, aluminum hydroxide, calcium dihydrogen phosphate, insoluble sodium metaphosphate, and 1 to 60% by weight, preferably 10 to 50% by weight, of these abrasives alone or in combination of two or more thereof. use.

Wetting agents include glycerin, sorbitol liquid, polyethylene glycol and propylene glycol, and are used alone or in combination of two or more.

Foaming agents include polyoxyethylene sorbitan fatty acid esters, polyoxyethylene (cured) castor oil, glycerin fatty acid esters, sorbitan fatty acid esters, sucrose fatty acid esters, alkylolamides, alkyls, to prevent deterioration of the activity of cationic fungicides. Nonionic surfactants, such as glucoside, and cationic surfactants, such as N-alkyldiamino ethylglycine, are used individually or in mixture of 2 or more types, and 0.5-10 weight%, Preferably 0.5-8 weight% is used.

As the binder, 0.1-5% by weight, preferably 0.1-2% by weight, of hydroxyethyl cellulose, hydroxypropyl cellulose, xanthan gum, 단독 carrageenan, sodium alginate, etc. alone or in combination of two or more thereof is used.

As a sweetener, saccharin sodium, aspartame, stevioside, xylitol, and licorice acid are used alone or in combination of two or more, and 0.05 to 5% by weight is used.

As the pH adjusting agent, sodium phosphate, disodium phosphate, trisodium phosphate, sodium pyrophosphate, sodium citrate, citric acid, tartaric acid, and the like are used, and as antiseptics, paraoxyanthine methyl acid, paraoxybenzoic acid propyl, sodium benzoate alone or 2 Mix more than one species.

Other active ingredients include sodium fluoride, sodium monofluorophosphate, tin fluoride, chlorohexidine, allantoin chlorohydroxy aluminate, aminocaproic acid, triclosan, cetylpyridium chloride, zinc chloride, pyridoxine hydrochloride, tocopherol acetate It is used alone or in mixture of two or more kinds, and mixed with a suitable amount of peppermint oil, spearmint oil, menthol, anetol, etc. as a fragrance, titanium oxide as a brightener, food coloring as a solvent, purified water as a solvent And ethanol to prepare a conventional toothpaste manufacturing method.

Hereinafter, although an Example and a comparative example are given and this invention is demonstrated further more concretely, the scope of the present invention is not limited to these.

Preparation Example Preparation of Toothpaste Composition

The toothpaste composition (Example 1) and the conventional toothpaste composition (Comparative Example 1 and Comparative Example 2) of the present invention were prepared using the components shown in Table 1 as main components.

division Ingredient Name Comparative Example 1 Comparative Example 2 Example 1 abrasive Calcium hydrogen phosphate 30 30 30 Active ingredient Sodium monofluorophosphate 0.76 0.76 0.76 Antibacterial / Anti-inflammatory Cetylpyridinium Chloride - 0.05 0.05 Antibacterial / Anti-inflammatory Willow Extract - - 0.5 Humectant Sorbitol solution 20 20 20 Thickener Hydroxyethyl Cellulose 2.0 2.0 2.0 antiseptic Methylparaben 0.2 0.2 0.2 Active ingredient Tocopherol Acetate 0.2 0.2 0.2 Spices Combination spices 1.0 1.0 1.0 Sweetener Zaccarin Sodium 0.3 0.3 0.3 pH regulator Sodium citrate 0.1 0.1 0.1 Brightener Titanium dioxide 0.3 0.3 0.3 Foam Lauryl Glusid 4 4 4 Purified water to 100 to 100 to 100

[Test Example 1] gingivitis index comparison experiment

An experiment for comparing the gingivitis index of the prepared Example 1 and Comparative Examples 1 and 2 was carried out. The experiment was conducted on 116 subjects (36 in Comparative Example 1, 40 in Comparative Example 2 and Example 1) in a relatively same environment. Baseline was obtained. A single blind method was applied and all subjects were given the same dentifrice and toothbrush of the same standard during the residual effect removal period of 4 weeks prior to the experiment.

The gingivitis index was measured for three months at three monthly intervals, and the experimental method was calculated as the mean value of the index calculated after dividing the gingiva per tooth into the buccal and lingual surfaces. Each gingivitis was evaluated from 0 to 3 points according to Loe & Silness's grading criteria, and the gingivitis index was calculated on average. The experimental results are shown in Table 2 below.

As can be seen in Table 2, in the case of Comparative Example 1, gingival inflammation temporarily appeared after 2 months of experiment, but there was no difference from the initial state after the last 3 months. However, in Comparative Example 2 and Example 1, the gingivitis mitigating effect appeared after one month, and it can be seen that the gingivitis mitigating effect continued to appear even after the last three months. In addition, two months later, the gingivitis mitigation effect was more significant than one month later (p <0.01).

Therefore, when comparing the results of the final experiment for 3 months, it can be seen that Comparative Example 2 and Example 1 is far superior to the gingivitis mitigation effect than Comparative Example 1. In addition, the gingivitis index of Example 1 was improved by 77.6%, Comparative Example 2 was improved by 71.7%, it can be seen that the gingivitis mitigation effect of Example 1 is more excellent.

[Test Example 2] Comparison of plaque index

In the test method of the plaque index, 20 ml of water is mixed with 10 drops of the coloring liquid when it is hit by the same subject as Test Example 1, sprinkled for 1 minute in the mouth, spited with water, and then applied with the Turesky modification standard of Quigley & Hein. Evaluated. The experimental results are shown in Table 3 below.

As can be seen in Table 3, Comparative Example 1 was found to have a plaque suppression effect after two months of experiment, but there was no difference from the initial state after the last three months. However, in Comparative Example 2 and Example 1, the plaque suppression effect appeared after 1 month, respectively, and it can be seen that the plaque suppression effect continued even after the last 3 months of the experiment. In particular, in the case of Example 1, it can be seen that after 3 months more excellent plaque suppression effect than after 2 months (p <0.01).

Therefore, when comparing the results of the final plaque suppression effect for three months, it can be seen that Comparative Example 2 and Example 1 is far superior to the plaque suppression effect than Comparative Example 1. In addition, the plaque index of Example 1 was improved by 47.8%, Comparative Example 2 was improved by 31.6%, it can be seen that the plaque suppression effect of Example 1 is more excellent.

Test Example 3 Snyder Experiment

The Snyder test was performed to directly measure the degree of destruction of acid bacteria in the oral cavity of cetylpyridinium chloride and willow extract. Based on the fact that bacteria contained in dental plaque or saliva produce acid, the activity of acid-producing bacteria is measured by colorimetric method. The basic chromaticity is as follows.

① Blue: Inactive (0 point)

② Green: Hardness activity (1 point)

③ Yellow-green: moderate activity (2 points)

④ Yellow: Highly active (3 points)

A total of 15 subjects were selected and assigned to each of 5 people in Comparative Example 1, 2 and 1, and then used for 2 months, and then the saliva of the subject was collected by 1 mm for each experimental group and dropped into a tube for activating bacteria. Observation was made for 3 days. At this time, the color change was photographed and recorded using a digital camera every 24 hours. The recorded photographs were checked for the activity of caries by looking at the determination table of the basic chromaticity. The production method of the medium used for the experiment is as follows.

① Prepare distilled water, agar, dextrose, BCG (indicator), beef extract, and lactic acid.

② Put beef extract in distilled water and boil.

③ Add BCG (indicator) to make the basic color blue.

④ Put agar, dextrose.

⑤ 40ml of the prepared medium in a 50ml tube by a fixed amount.

The experimental results measured after 2 months are shown in Table 4.

group Initial state 2 months later Comparative Example 1 2.4 1.8 Comparative Example 2 2.8 1.2 Example 1 2.8 0.2

Snyder test results conducted before the start of the experiment was 2.40 in Comparative Example 1 and 2.80 in Comparative Example 2 and Example 1, respectively, after 72 hours, which showed a high level of activity. However, the test conducted two months after the experiment was still moderate activity as 1.80 in Comparative Example 1, the hardness activity was 1.20 in Comparative Example 2, 0.20 in Example 1 was close to inactivity. In particular, in the case of Example 1, the improvement rate was 93.4%, showing an excellent antimicrobial effect compared to Comparative Example 1 and Comparative Example 2.

The Snyder test is based on the assumption that cetylpyridinium chloride, a quaternary ammonium compound, is a cationic surfactant that binds to the phosphates that make up the bacterial cell membrane and destroys the cell wall to increase permeability, thereby inhibiting or destroying the viability of bacteria. Becomes In addition, it will be seen that the willow extract acts as an ingredient that proceeds more effective on this antibacterial action.

As described above, the composition for oral cavity according to the present invention is a combination of a cationic fungicide and willow extract showed a more significant decrease in the gingival index and plaque index than the conventional combination of cationic fungicides, Snyder test results The bactericidal activity against oral bacteria is much increased, and thus, it shows an excellent effect on the prevention of gum disease such as gingivitis and periodontitis, removal of plaque and sterilization of oral bacteria.

Claims (4)

An oral composition comprising a cationic fungicide and willow extract. The composition of claim 1, wherein the cationic fungicide is selected from the group consisting of cetylpyridinium chloride, hexahalonium chloride, benzalkonium chloride and chlorohexidine. The composition according to claim 1, wherein the cationic fungicide is contained in the range of 0.01 to 5% by weight, and the willow extract is contained in the range of 0.1 to 2% by weight. According to claim 1, wherein the composition is characterized in that the composition for gingivitis relief, plaque suppression or antibacterial.