KR980008209A - Toothpaste composition - Google Patents

Abstract

The present invention relates to a toothpaste composition having an effect of preventing and treating periodontal disease, preventing tooth decay, and removing bad breath by containing grapefruit seed extract and / or green tea extract.

Description

Toothpaste composition

Since this is a trivial issue, I did not include the contents of the text.

The present invention relates to a dentifrice composition having an effect of preventing and treating periodontal disease, preventing tooth decay, and removing bad breath, and more particularly, to a dentifrice composition having an excellent periodontal disease prevention and bad breath removing effect by containing grapefruit seed extract or green tea extract will be.

Various oral diseases in oral tissues are caused by plaque and numerous bacteria in oral cavity, and the clinical pathological significance thereof has been widely studied.

The plaque is a sticky film adhered to the surface of teeth. The composition is composed of a dental floss that is trapped in a mesh of dextran, which is a glucose polymer. When it is left without being removed, It progresses to gum disease.

Dextran in the plaque is the sugar in the food by the enzyme glucosyl trans-flops and at the same time raise secretion decomposed to glucose and fructose synthesis α ^1-3, and the outside of the cell membrane of the cell or binding straps sat mutans in the oral cavity It is adherent to the teeth with adhesive properties to glucose polymers of α ^1-6 bonds.

In this process, Streptococcus mutans continue to proliferate, and during the intracellular metabolism, glucose acts as a substrate to produce pyruvic acid. The resulting pyruvic acid produces lactic acid by lactate dehydrogenase and releases it to the outside of the cell, thereby lowering the pH of the pyruvate to an acidity of about 4.0 to 4.5 to dissociate hydroxyapatite, which is a component of the tooth, into phosphoric acid and calcium components A decay process occurs and tooth decay occurs.

In addition, the acidic environment in the prage promotes the proliferation of periodontal disease bacteria and causes inflammation of the gums, and progression to periodontal disease continues.

More specifically, periodontal disease refers to the loss of teeth due to clinically gingivitis and hemorrhage, formation of periodontal pockets, and destruction of alveolar bone.

This periodontal disease progresses to bacterial colonization, bacterial infiltration of periodontal tissue, and destruction of periodontal tissue. First, saliva protein in the oral saliva is adsorbed on the dentin and cementum surfaces to form a film, Bacteria such as caucus and actinomycis grow to form plaque.

As the time passed, the plaque migrated in the apical direction, and anaerobic gram-negative bacteria such as bacteriophage and actinobacillus grew, and these bacteria, bacterial components, and bacterial products penetrated into the connective tissue through the gingival salivary epithelium, The result of metabolism of this bacterium is that it releases toxins such as ammonia hydrogen sulfide and toxic amines toxic to the periodontal tissues, and destroys the upright tissues by toxins such as cell wall constituents lipopolysaccharide, Collagen is secreted by enzymes such as collagen AIDS, which breaks down the collagen, which is an early periodontal substrate, and causes gingival recession. At the same time, it activates the vital immune system and stimulates the immune system. By the action of the humoral and cellular immune system, Rocotrien, histamine, etc. When the body cause inflammation and continuing advances in periodontal disease.

In addition, bad breath is generally caused by acquired systemic diseases, proteins in the saliva, food residues, etc. are broken down by microorganisms in the oral cavity, and the fish amino acids are decomposed by deacidifying enzymes or amino enzymes, Lt; / RTI >

Examples of substances that cause bad breath include volatile sulfides such as hydrogen sulfide and methyl mercaptan, and other bad breath inducing substances include aldehyde, fatty acid, ammonia, amines, and pyridine.

Ancient people can see records using various herbal medicines for the prevention and treatment of oral diseases. In ancient China, it was used as a treatment for gingival inflammation and gingival bleeding, the herb Hinhong (Inhin Tong) The poinsey of the poet used honey. In the Middle Ages, opium and rose oil were used. In the 14th and 15th centuries, white pimples and roasted salt were used. In oriental countries, Chinese medicines were used for prevention and treatment of oral diseases.

In order to prevent the occurrence of periodontal disease and tooth decay and bad breath, antibacterial agents such as chlorohexidine, quaternary ammonium compounds such as cetylpyridinium chloride, triclosan and sanguinarine, and penicillin Such as sodium fluoride and sodium monofluorophosphate, which inhibit tooth decay or accelerate remineralization to prevent tooth decay, and dextrinases of enzyme preparations have been used variously. As is known, herbal medicine extracts Are also studied in various ways and applied to products.

In Japanese Patent Application Laid-Open Nos. 55-120 and 509, herbal medicine extracts such as herbal extracts, papaya leaves, herbaceous oils, rootstocks and lobes are disclosed in Japanese Patent Publication Nos. 57-5641 and 57-85319, Japanese Patent Laid-open No. 87-268613 discloses a method for obtaining a bacterium-containing seed oil, and Japanese Patent Application Laid-open No. 60-75418 discloses a method for obtaining an oral cavity bacterial inhibitory effect by blending sage or rosemary.

However, all of the above-mentioned prior art components have a problem that the oral bacteria-suppressing effect is insufficient, and when applied to a product, there is a problem that periodontal disease prevention and treatment, tooth decay prevention, bad breath removal effect are weak and usability is poor. Therefore, in order to solve such problems, the present invention has been made to overcome the above problems and to provide a pharmaceutical composition which is excellent in the inactivation of the collagen enzyme and the germicidal effect of the cavitating bacteria, which are causative factors of periodontitis, and the preparation using the grapefruit seed extract, It has been found out that the formulation using a certain proportion of the mixture is applied to the dentifrice composition to excellently inhibit bacteria in the oral cavity, to prevent periodontal disease, to prevent tooth decay, to remove bad breath, and to complete the present invention. The present invention relates to a toothpaste composition characterized by containing a grapefruit extract and / or a green tea extract. Grapefruit seed extract contains a large amount of natural ascorbic acid, naringin, and tocopherol. It has excellent antimicrobial and antioxidant properties. It is a natural extract that inhibits the production of toxic and degenerated products. It is completely decomposed when it is absorbed into the body It is a safe material for the human body without any risk of toxicity due to accumulation in the body.

The grapefruit seed extract contains 45% ascorbic acid, which is a reducing agent for metal ions, which produces oxygen radicals, particularly hydrogen radicals, which inhibit the enzyme activity distributed in the cell membrane and weaken the cell membrane function It inhibits the cell respiration of microorganisms and inhibits the normal growth of microorganisms. In other words, sterilization of microorganisms can be achieved by inhibiting cell membrane weakening and cell respiration.

Antioxidant Functional Auto-Oxidation Process of the Small Oil During the process of forming the hydro-paroxyside, which is a careful part, the antioxidant molecule itself gives active hydrogen atoms to various active maintenance radicals participating in or participating in the chain reaction It makes sulfur free radicals a safe, non-active compound and causes itself to become an antioxidant mechanism that is stabilized by resonance, that is, a radical with low activity. The mechanism of action of antioxidants is shown in the following reaction scheme.

The major antimicrobial substances of grapefruit seed extract are Naringin and Citral. Naringin is a component of flavanoid known as vitamin P, and this substance is mainly present in the seeds and peels of ripe grapefruit. Naringin has a bitter taste, and its molecular formula is C ₂₇ H ₃₂ 0 ₁₄ .2H ₂ O, and its chemical structure is as follows.

Citral is present in many citrus fruits and naturally exists in two isomers, geranial and neral, and its chemical structure is as follows.

Geranium (Citral α) Neral (Citral b)

And green tea extract is a natural compound containing mainly tannin and polyphenol derivatives as camellia and plant.

The Japanese Society of Textile Engineers (Vol. 40 No. 3, 1987) describes that a polyphenol derivative or the like having a three-dimensional structure covers odor molecules or atoms to remove odors.

Green tea extract mainly contains components such as caffeine, organic acid, amino acid, (+) - catechin and saccharides. Among these components, (+) - catechin having a three- Which is the most common cause of halitosis.

Generally, the green tea extract is excellent in anti-inflammatory action and anti-bacterial action against various bacterium that inhibits swelling in the inflammation site, and also has excellent cell protection effect, so that the anti-aging effect of the skin is excellent, It is known to have an antimutagenic effect.

In addition, it inhibits angiotensin-converting enzyme that induces hypertension and acts to lower blood pressure by relaxing platelets. It is also known that it has an effect of inhibiting atherosclerosis by decreasing the concentration of blood cholesterol.

In the dentifrice composition according to the present invention, the grapefruit seed extract contains 0.005 to 1.0% by weight, preferably 0.01 to 0.5% by weight.

In the dentifrice composition according to the present invention, the green tea extract contains 0.01 to 5.0% by weight, preferably 0.05 to 1.0% by weight. When the grapefruit seed extract and the green tea extract are mixed, it is preferable to use the ratio of 1: 5 to 1: 100.

In the dentifrice composition according to the present invention, the grapefruit seed extract contains not more than 0.005% by weight of green tea extract and not more than 0.01% by weight. When the blending ratio of grapefruit seed extract and green tea extract is not more than 1: 5 to 1: 100, , And 1.0% by weight or more of grapefruit seed extract and 1.0% by weight or more of green tea extract, it is very difficult to apply to grapefruit seed extract and green tea extract because of their unpleasant taste such as strong smell when used.

In addition, the dentifrice composition of the present invention can be used as a dentifrice preventive agent such as sodium fluoride, sodium fluorophosphate, fluoride amine, tin fluoride, xylitol, fungicide chlorhexidine, cetylpyridium chloride, triclosan, Allantoin, aminocaproic acid, tranexamic acid, tocopherol acetate, enzyme dextrinase, glucosoxidase, anti-inflammatory agent, anti-inflammatory agent, Glucoamylase,?,? -Amylase, lactoperoxidase, lysozyme, and the like may be used alone or in combination of two or more.

The dentifrice composition of the present invention may further contain an abrasive, a wetting agent, a binder, a foaming agent, a sweetener, an antiseptic agent, a pH adjuster, a perfume, and the like in addition to the above components.

Examples of the abrasive include calcium carbonate, calcium monohydrogenphosphate, precipitated silica, hydrous alumina, silica gel, insoluble sodium metaphosphate, and zirconium silicate. These abrasives may be used alone or in admixture of two or more, Is used in an amount of 35 to 55% by weight.

The wetting agent is used in an amount of 20 to 60% by weight, preferably 20 to 50% by weight, of glycerin, sorbitol, amorphous sorbitol, glycerin, polyethylene glycol or the like alone or in admixture of two or more.

As the binding agent, carrageenan, dipeptide, carboxymethylcellulose sodium, carboxyvinylforryl, sodium alginate and the like are usually suitable. The amount of the binder to be used is suitably from 0.1 to 3.0% by weight, preferably from 0.5 to 2.0% by weight.

As the foaming agent, anionic surfactants such as sodium lauryl sulfate and sodium lauroyl sarcosinate and nonionic surfactants such as sorbitan fatty acid ester, polyoxyethylene hydrogenated castor oil, and polyoxyethylene polyoxypropylene copolymer are used. The foaming agent is used in an amount of 0.5 to 5.0% by weight, preferably 0.5 to 2.5% by weight, of an anionic surfactant and a nonionic surfactant alone or in admixture of two or more.

Examples of the sweetening agent include sodium saccharin, aspartame, acesulfame, stevioside, licorice acid, etc. These are preferably used alone or in combination of two or more thereof in an amount of 0.05 to 0.5% by weight.

The antiseptic agent is preferably used in an amount of 0.05 to 0.25% by weight, based on a mixture of two or more of p-oxybenzoic acid esters, benzoic acid and sodium benzoate.

It is possible to use softened sodium which has a disinfection and sterilization effect with a high osmotic action and suppresses edema and hemorrhage by using 0.05 to 3.0% by weight, preferably 0.05 to 2.0% by weight, of calcium glycerophosphate excellent in re-painting effect in toothpaste have.

As the pH adjusting agent, phosphoric acid, sodium phosphate, citric acid, sodium citrate, succinic acid, sodium succinate, tartaric acid, sodium tartrate and the like are used, and phosphoric acid, sodium phosphate, citric acid and sodium citrate are used singly or in combination of two or more, %.

Examples of the material constituting the flavor include a flavor oil, menthol, spearmint oil, carbo, anise oil, anisole, eucalyptus oil, , Cinnamol oil, cinnamic aldehyde and other perfume ingredients are used, and the material constituting the flavor is selected from the group consisting of: 0.1 to 2.0% by weight, preferably 0.5 to 1.5% by weight, of one kind or a mixture of two or more kinds is used.

As a refreshing agent, methyl lactate, menthyl glycol carbonate, menthyl propylene glycol carbonate, menthone glycerin acetal and the like are used for promoting exhilaration and persistence. The content of one or more kinds Is 0.01 to 10.0% by weight.

Hereinafter, the present invention will be described in detail with reference to the following examples and comparative examples, but the technical scope of the present invention is not limited in any way by these examples.

Examples 1-14 and Comparative Examples 1-3

A dentifrice composition was prepared according to a conventional method at a ratio of the composition components shown in the following table.

[Experimental Example 1]

The plaque formation and the organic acid generation inhibitory effect of the toothpaste of the present invention (Examples 1 to 14) and the comparative toothpaste (Comparative Examples 1 to 3)

1) Experimental method

Experimental results on the formation of plaque and the inhibition of organic acid production with the toothpaste of the present invention are as follows.

This test method was developed based on the fact that plaque and organic acid produced by Streptococcus mutans, the causative organism of tooth decay, play the most important role in the process of tooth decay and periodontal disease.

First, Streptococcus mutans 10449 was subcultured on a Brain Heart Infusion agar medium, platinum was inoculated on Todd Hewitt Broth, cultured at 37 ° C for one day, 20 mm and 70 mm long was prepared and sterilized at 180 ° C for 2 hours. After the first glass rod weight was measured to five decimal places, the glass rod was immersed in a 10 ml THB medium containing 1% The slurry of Comparative Examples 1 to 3 and Examples 1 to 14 was made into a slurry of 1: 2 (product: distilled water), and the mixture was completely homogenized. After centrifugation at 1000 g for 10 minutes, 1 ml of the supernatant was added, 100 μl of Tanz 10449 was added and cultured in a thermostat at 37 ° C. for 24 hours. When the glass rods were not added, the degree of plaque formation was calculated by the following equation,

In addition, the degree of organic acid production was measured by measuring the pH of the cultured medium using a pH meter, and the following results were obtained.

2) Experimental results

As a result of the above test, Comparative Example 1, which did not contain the grapefruit extract, did not exhibit the effect of inhibiting plaque formation and organic acid production. In Comparative Example 2 containing 0.001% by weight of the grapefruit extract, In Comparative Example 3 containing 10% by weight, the effect of inhibiting plaque formation and organic acid formation was 100%. In Example 1 containing 0.005% by weight of the grapefruit extract, 50% of the grapefruit formation inhibitory effect was shown. %, The effect of inhibiting plaque formation and organic acid production was 100%, indicating that the grapefruit extract had a potent effect on the formation of plaque and the inhibition of organic acid production.

[Experimental Example 2]

The inhibitory effect of the toothpaste of the present invention (Examples 1 to 14) and the comparative toothpaste (Comparative Examples 1 to 3) on collagen AIDS,

1) Experimental method

Experimental results on the inhibitory effect on collagen AIDS, a periodontal tissue degrading enzyme, with the toothpaste of the present invention are as follows. This test is performed in the saliva and gingival crevicular fluid of periodontal disease patients secreted from Bact eriods gingivalis, Polymorphonuclear leukocytes and Neutrophil during periodontal disease. It is an experimental method that imitates the oral environment of the living organism in which collagen, which is a matrix of periodontal manipulation, is degraded by the action of collagen Azease enzyme contained therein and gum recession occurs.

100 μl of a 2% red collagen substrate, Azpcoll solution, was added to each of 25 25 ml Eppendorf tubes, one Eppendorf tube was used as a blank and three tubes were purchased from Sigma One collagen AIDS type I standard enzyme solution (collagen decomposition activity: 315 units / mg) was added at 10, 100 and 200 ppm, and each of the remaining tubes was subjected to Sephacryl S-200 chromatography 100 μl of the collagen Azease purified through the addition of 100 μl of the purified collagenase enzyme was used as a control. One tube was used as a control group, and the remaining tubes were subjected to the procedures of Comparative Examples 1 to 3 and Examples 1 to 14 in a ratio of 1: 2 Slurry, and centrifuged at 10000 g for 5 minutes to precipitate undegraded collagen and take a supernatant containing the degraded collagen to measure the absorbance at 540 nm Create a standard activity curve over and in terms of the activity concentration of the enzyme from the standard curve to the experimental structure The results were as follows to evaluate the comparative enzyme activity of the control group.

2) Experimental results

(Unit:% = enzyme activity of the test group × 100 ÷ enzyme activity of the control group)

In the above test results, no inhibitory effect on collagen Azease activity was observed in the test groups of Comparative Examples 1 to 3 containing no green tea extract and in the experimental groups of Examples 1 to 5. However, In Examples 6 to 14 containing weight%, excellent inhibition of enzyme activity was shown. Thus, it was found that only green tea extract had an excellent effect in inhibiting enzyme activity of collagenase which decomposes periodontal tissue.

[Experimental Example 3]

The clinical efficacy and efficacy of the toothpaste of the present invention (Examples 1 to 14) and the comparative toothpaste (Comparative Examples 1 to 3)

1) Subjects to be tested

Subjects were divided into 10 groups of 30 to 50 years of age. The subjects were divided into 30 groups according to their gender, and 120 subjects were selected. The clinical tests on the therapeutic effects of the gingival inflammation of the present invention products (Examples 1 to 14) and the comparative products (Comparative Examples 1 to 10) were performed in the following manner.

2) Experimental method

The subjects were divided into two groups: the experimental group and the comparative group. The subjects were instructed to use 2 hours after the meal and 3 times a day before sleep, and then the dental calculus was performed to score the initial gingival index. After 1 week, 1 month, 3 months, and 6 months, oral examinations were performed to check gingival index. To measure gingival sulcus size, the periodontal probe was inserted into the gingival sulcus and the force was not applied. After the probe was continuously probed around each tooth, the appearance of the gingivitis was measured after 30 seconds. The scores were recorded and the results were obtained.

3) Experimental results

The results of the clinical tests for treating gingival inflammation with the product of the present invention are as follows.

4) Review

As a result of the above clinical test, Comparative Example 1, which did not contain any active ingredient, had no gingival inflammation inhibitory effect, and Comparative Example 2 containing 0.001% by weight of grapefruit extract had no gingival inflammation inhibitory effect In Comparative Example 3 containing 1% grapefruit extract, the gingival inflammation inhibitory effect was excellent. In Examples 1 to 5, which contained the grapefruit extract alone in an amount of 0.005 to 0.50% by weight, The grapefruit extract inhibited the formation of plaque and inhibited the activity of collagen Azease by inhibiting plaque formation and inhibiting the activity of collagen Azease by inhibiting plaque formation and inhibiting the enzyme activity of Examples 6 to 14 in which the grapefruit extract and green tea extract were combined. The efficacy of the inventive product for treating gingival inflammation was excellent from 1 week to 6 months.

[Experimental Example 4]

Clinical comparison experiments on the odor suppressing effect of the toothpaste of the present invention (Examples 1 to 14) and the comparative toothpaste (Comparative Examples 1 to 3)

1) Subjects to be tested

Eighty-five male and female dentists who do not have dental caries are selected.

2) Experimental method

After a certain amount of garlic (0.5 g) was masticated for 2 minutes, the oral malodor was generated and then the sample was used for 1 minute. After 1 minute, 5 minutes, 10 minutes and 15 minutes, methylmercaptan .

Keep the mouth shut except when using the product to prevent mixing of the subject's breath with the outside air.

The volume is measured by gas chromatography (detector: FPD) after taking 100 ml of a gas tighter sy- ringe.

At this time, 1 ml Sampling Loop is attached to analyze only 1 ml of the sample.

Chromosil 330 column, Teflon tube with a filling length of 61xm and outer diameter of 1/8 inch is used. The column temperature is adjusted to 70 ° C and helium is used as carrier gas at 20ml / min.

3) Experimental result: Decrease rate (%) of methyl mercaptan

According to the above-mentioned method, the dentifrice products of Examples and Comparative Examples were measured by gas chromatography three times, and the amount of methylbercaptan generated during the time of garlic chewing was shown as follows.

The dentifrice composition using the dentifrice composition containing 63.3 to 65.5% of the dentifrice composition using 0.001% by weight of grapefruit seed extract and the 1.0% by weight of the grapefruit seed extract using 87.5 to 88.6% appear.

As described above, dentifrice compositions using grapefruit seed extracts are excellent, and particularly, dentifrice compositions using 1.0% by weight of grapefruit seed extracts are very difficult to apply to products due to their unpleasant feeling, such as strong tastes.

Therefore, it is considered that the deodorizing effect of the toothpaste products using the grapefruit seed extract and the nongap extract is very good.

Claims (8)

Grapefruit seed extract and / or green tea extract. 2. The dentifrice composition according to claim 1, which contains 0.005 to 1.0% by weight of grapefruit seed extract. 3. The dentifrice composition according to claim 2, which contains from 0.01 to 0.5% by weight of grapefruit seed extract. The dentifrice composition according to claim 1, which contains 0.01 to 5.0% by weight of green tea extract. 2. The dentifrice composition according to claim 1, which contains 0.05 to 1.0% by weight of green tea extract. The dentifrice composition according to claim 1, wherein the grapefruit seed extract and green tea extract are contained at a ratio of 1: 5 to 1: 100. The pharmaceutical composition according to any one of claims 1 to 6, wherein the medicinal active agent is sodium fluoride, sodium fluoride, fluoroamine, tin fluoride, xylitol, chlorhexidine, cetylpyridinium chloride, triclosan, Allantoin, aminocaproic acid, tranexamic acid, tocopheryl acetate, dextranase, which is an enzymatic agent, glucose, is an effective antioxidant, which is an antiinflammatory agent, Wherein the dentifrice composition further comprises one or more of an oxidase, a glucoamylase, an?,? -Amylase, a lactoperoxidase, and a lysozyme. The dentifrice composition according to claim 1, further comprising an abrasive, a wetting agent, a binder, a foaming agent, a gamma-suppressant, an antiseptic and a fragrance. ※ Note: It is disclosed by the contents of the first application.