KR100450391B1 - Toothpaste Composition - Google Patents

Abstract

The present invention relates to a toothpaste composition having an excellent periodontal disease prevention and treatment, caries prevention, and bad breath removal effect by containing grapefruit seed extract and / or green tea extract.

Description

Toothpaste composition

The present invention relates to a toothpaste composition having excellent periodontal disease prevention and treatment, tooth decay prevention, and bad breath removal effect, and more particularly, to a toothpaste composition having excellent periodontal disease prevention and bad breath removal effect by containing grapefruit seed extract and green tea extract. .

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

The plaque is a sticky membrane attached to the tooth surface, and its composition is composed of the dental plaque that is oral bacteria trapped in the mesh of dextran, a glucose polymer. Proceeds to gum disease.

Dextran in the prag is bound to the cell membranes of the straptococcus mutans in the oral cavity, or by the enzyme glucosyltransferase secreted extracellularly, sugars in food are decomposed into glucose and fructose, and α ^1-3 and Glucose polymer of α ^1-6 bond, which has stickiness and adheres to teeth.

The growth of the Straptococcus mutans continues, and glucose is used as a substrate during intracellular metabolism to produce pyruvic acid. The pyruvate produced is lactic acid produced by lactate dehydrogen AIDS and released to the outside of the cell, lowering the pH in the peg to an acid of 4.0-4.5 and dissociating hydroxyapatite, a component of the tooth, into phosphoric acid and calcium. The demineralization process occurs, and tooth decay occurs.

In addition, the acidic environment in the plaque promotes the growth of periodontal disease bacteria, causing gum inflammation and progressing to periodontal disease.

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

The periodontal disease proceeds as a process of colonization of bacteria, infiltration of periodontal tissues of bacteria, and destruction of periodontal tissues. First, saliva proteins in oral saliva are adsorbed to dentin and chalky surfaces, forming a film, and mainly streptoco Bacteria, such as the caucus and actinomysis, grow and form plaques.

As time passes, these plaques move toward the root canal, and anaerobic gram-negative bacteria such as bacteroids and actinobacillus grow, and these bacteria, bacterial components, and bacterial products penetrate into the connective tissue through the gingival epithelium. The metabolism of these bacteria resulted in the release of toxins such as toxic hydrogen sulfide ammonia and toxic amines into the periodontal tissue, and at the same time, the upright tissues were destroyed by toxins such as lipopoly saccharide, a cell wall component, or from bacteria and leukocytes. Collagen, which is a substrate of periodontal tissue, is degraded by enzymes such as secreted collagenase, and gum retraction occurs, and at the same time, stimulating the biological immune system, free radicals secreted extracellularly by various actions of humoral and cellular immune systems, prostaglandins, By rucotrienne, 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., which are decomposed by microorganisms in the oral cavity, and the resulting amino acids are decomposed by dehydrating enzymes or amino enzymes. Is generated.

Examples of bad breath causing substances include volatile sulfides such as hydrogen sulfide and methyl mercaptan, and other bad breath causing substances include aldehydes, fatty acids, ammonia, amines or pyridine.

Ancient people can see the record using various herbal medicines for the prevention or treatment of oral disease, and ancient Chinese used the medicine Inhin Tong to treat gingivitis, bleeding bleeding, etc. The Poeniches used honey and so on. In the Middle Ages, opium, rose oil, etc., in the 14th and 15th centuries, white wine, roasted salt, etc., oriental medicines were used especially for the prevention and treatment of oral diseases.

In an effort to prevent the occurrence of periodontal disease, tooth decay and bad breath, chlorohexidine, a quaternary ammonium compound, cetyl pyridium crawlide, triclosan, and sanguinarin, and penicillin Antibiotics such as fluoride and dextranase such as sodium fluoride and enzymatic preparations, such as sodium fluoride and sodium fluoride phosphate, which prevent tooth decay or promote remineralization and prevent tooth decay, are widely used. Extracts are also studied and applied to products in a variety of ways.

Japanese Unexamined Patent Application Publication Nos. 55-120,509 discloses herbal extracts such as bone extracts, white locusts, fat milk, lotus root, and young leaves, and Japanese Unexamined Patent Publications No. 57-5641 and 57-85319 disclose yellow extracts. In Japanese Patent Application Laid-Open No. 87-268613, the seed oil of Moondogchoe was mixed with Sage or Rothmari in Japanese Patent Laid-Open No. 60-75418 to obtain oral bacterial suppression effect.

However, all of the above-described components of the prior art have a problem that the periodontal disease prevention and treatment, caries prevention, bad breath removal effect is weak, and the usability is poor when applied to the product because the continuous oral bacterial inhibitory effect is weak.

Therefore, in order to solve these problems, the present invention has excellent inactivation of collagen enzyme, which is a trigger factor of periodontitis, and bactericidal effect of caries bacteria, and green tea extract using safe grapefruit seed extract. By applying the formulation to the dentifrice composition using a certain ratio of the mixture is excellent in the oral bacteria inhibitory effect, periodontal disease prevention, caries prevention, bad breath removal effect was found to complete the present invention.

The present invention relates to a toothpaste composition, characterized in that it contains grapefruit seed extract and green tea extract. Grapefruit seed extract and green tea extract in the present invention uses those extracted by conventional methods well known in the art.

Grapefruit Seed Extract contains a large amount of natural ascrobinic acid, naringin and tocopherol, which is excellent in antibacterial and antioxidant activity. It is a natural extract that inhibits the production of toxic products and septic products. It is a safe substance to human body without any risk of toxicity due to accumulation in the body.

45% of ascorbic acid is present in the grapefruit seed extract, which is a reducing agent of metal ions, which produces oxygen-based, especially hydrogen radical, which inhibits the enzymatic activity distributed in the cell membranes, weakening cell membrane functions. Inhibit microbial cell respiration and inhibit normal growth of microorganisms. That is, microorganisms can be sterilized by suppressing cell membrane weakness and cell respiration.

The mechanism of action of antioxidants is the formation of active hydrogen atoms for the various active-retaining radicals that can participate in or participate in the chain reaction in the fats and oils in the formation of hydro parosides, which are part of the automatic oxidation of fats and oils. This gives active free radicals a stable compound that is inactive and induces an antioxidant mechanism that is stabilized by resonance, ie, becomes a less active radical. The mechanism of action of antioxidants is shown in the following scheme.

The main antimicrobials of grapefruit seed extract are naringin and citral. Naringin is a flavonoid known as vitamin P. It is found in the skin and seeds of ripe grapefruit. Naringin has a bitter taste, and the molecular formula is C ₂₇ H ₃₂ O ₁₄ · 2H ₂ O. The chemical structure is as follows.

Citral is present in many citrus fruits, and naturally there are two isomers of geranial and neral. The chemical structure is as follows.

Green tea extract is a natural complex containing camellia and tannins and polyphenol derivatives. The Japanese Society for Textile Machinery (Vol. 40 No. 3, 1987) describes that polyphenol derivatives having a three-dimensional structure and the like contain a molecule or an atom of an odor component to remove odors.

Green tea extract contains mainly caffeine and other organic acids, amino acids, (+)-catechin, sugars, etc. Among them, the (+)-catechin having a three-dimensional structure of a polyphenol derivative is included. By continually suppressing bad breath.

In general, the green tea extract has excellent anti-inflammatory action and antimicrobial action against swelling at the inflamed area, and it has excellent cell protection effect, so it is excellent in anti-aging effect of skin and also works on animal cancer cells to inhibit cancer development and It is known to have antimutagenic effects.

In addition, it inhibits angiotensin transfer enzymes that cause high blood pressure and relaxes platelets to lower blood pressure. In addition, it is known to have an effect of inhibiting arteriosclerosis by reducing the concentration of cholesterol in the blood.

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

Green tea extract in the toothpaste composition according to the present invention contains 0.01 to 5.0% by weight, preferably 0.05 to 1.0% by weight. In addition, when using the grapefruit seed extract and green tea extract is preferably used in a ratio of 1 to 5 to 1 to 100.

In the toothpaste composition of the present invention, if the grapefruit seed extract 0.005% by weight or less and the green tea extract 0.01% by weight or less, when the combination ratio of grapefruit seed extract and green tea extract is used other than 1 to 5 to 1 to 100, sufficient effects cannot be expected. When used in more than 1.0% by weight of the seed extract, 1.0% by weight or more of green tea extract, it is very difficult to apply to the product due to the unpleasant taste such as strong astringent taste when used as the unique smell and taste of grapefruit seed extract and green tea extract.

In addition, the dentifrice composition of the present invention is a medicinal ingredient as sodium fluoride, sodium phosphate, amine fluoride, tin fluoride, xylitol, chlorohexidine as a fungicide, cetylpyridium chloride, triclosan, medicinal herbs as bamboo salt, yellowish white , Gilyeong, hyunggeung, gardenia, myrrh, baekryepi, horseback riding, gold and silver, gold, pore dinosaur, propolis, allantoin, aminocapronic acid, tranexamic acid, tocopherol acetate, dextranase, enzyme glucosidase, You may use 1 type, or 2 or more types of glucoamylase, (alpha), (beta) -amylase, lactoperoxidase, and lysozyme.

In addition to the above components, the toothpaste composition of the present invention may further contain an abrasive, a humectant, a binder, a foaming agent, a sweetener, a preservative, a pH adjuster, a perfume, and the like.

Abrasives include calcium carbonate, calcium dihydrogen phosphate, precipitated silica, hydrous alumina, silica gel, insoluble sodium metaphosphate, zirconium silicate, and the like, which are used alone or in combination of two or more thereof, preferably 20 to 70% by weight. 35 to 55% by weight is used.

The humectant is 20 to 60% by weight, preferably 20 to 50% by weight of glycerin, sorbitol liquid, amorphous sorbitol liquid, glycerin, polyethylene glycol, or the like, alone or in combination of two or more thereof.

As the binder, carrageenan, xantham gum, carboxymethyl cellulose sodium, carboxy vinyl polymer, sodium alginate and the like are usually suitable. The amount of the binder used is appropriately 0.1 to 3.0% by weight, preferably 0.5 to 2.0% by weight.

As the foaming agent, anionic surfactants such as sodium lauryl sulfate and sodium lauroyl sarcosinate, nonionic surfactants such as sorbitan fatty acid esters, polyoxyethylene hardened castor oil, and polyoxyethylene polyoxypropylene copolymers 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, either alone or in combination of two or more kinds of the anionic surfactant and the nonionic surfactant.

Examples of the sweetening agent include sodium saccharin, aspartame, acesulfame, stevioside, and licorice acid, and these are preferably used alone or in a mixture of two or more of 0.05 to 0.5% by weight.

It is preferable to use 0.05-0.25 weight% of preservatives individually or in mixture of 2 or more types of paraoxy benzoic acid ester, benzoic acid, and sodium benzoate.

Calcium glycerol phosphate having excellent remineralization effect in toothpaste is used in the range of 0.05 to 3.0% by weight, preferably 0.05 to 2.0% by weight, and sodium chloride which has a disinfection and sterilization effect by high osmotic action and suppresses edema and bleeding can be used. have.

As the pH adjuster, phosphoric acid, sodium phosphate, citric acid, sodium citrate, succinic acid, sodium succinate, tartaric acid, sodium tartarate and the like are used, and phosphoric acid, sodium phosphate, citric acid, sodium citrate alone or by mixing two or more kinds 0.02 to 1.5 weight It is preferable to use%.

Flavoring materials include aromatic substances used in conventional toothpaste and substances used in food flavoring, such as peppermint oil, menthol, spearmint oil, carbon, anise oil, anitol, and eucalyptus oil. Eucalyptol (1,8-cineol), clove oil, eugenol, winter green oil, methyl salicylate, cinnamon oil, cinnamic aldehyde and other flavoring ingredients are used to make up the flavor The substance is used in an amount 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.

Cooling agents are used to enhance freshness and durability.Methyl lactate, menthyl glycol carbonate, menthyl propylene glycol carbonate, menthyl glycerine acetal, etc. are used as the refreshing agent. Is 0.01 to 10.0% by weight.

Hereinafter, the present invention will be described in detail with Examples and Comparative Examples, but the technical scope of the present invention is not limited in any way by these Examples.

Example 1-14 and Comparative Example 1-3

Toothpaste compositions were prepared according to a conventional method at the ratio of the composition components shown in the following table.

Experimental Example 1 Inhibition Effect of Plaque Formation and Organic Acid Production between Toothpaste of the Invention (Examples 1 to 14) and Comparative Toothpaste (Comparative Examples 1 to 3)

1) Experiment Method

Experimental results of the plaque formation and organic acid production inhibitory effect with the present invention is as follows.

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

First, the Straptococcus mutans 10449 was passaged on Brain Heart Infusion agar medium, inoculated with Todd Hewitt Broth with platinum, and incubated at 37 ° C. for one day. , Prepare a glass rod of 70mm length and sterilize at 180 ℃ for 2 hours, measure the weight of the first glass rod to 5 decimal places, and then test the glass rod containing 10ml THB medium containing 1% by weight sugar solution. Into a slurry of Comparative Example 1 to 3 and Examples 1 to 14 (product: distilled water), completely homogenized, centrifuged at 1000 g for 10 minutes, and then added 1 ml of a supernatant, followed by Straptococcus mutans. 100 μl of 10449 was added thereto and incubated for 24 hours at 37 ° C. in a thermostat. The glass rod was not added to the group.

In addition, the degree of organic acid generation was measured by measuring the pH of the culture medium using a pH meter to obtain the following results.

2) Experiment result

In the above test results, Comparative Example 1 containing no grapefruit extract showed no inhibitory effect on plaque formation and organic acid formation, and Comparative Example 2 containing 0.001% by weight of grapefruit extract did not show any effect or effect, but the grapefruit extract contained 1 In Comparative Example 3 containing 100% by weight, the inhibitory effect of plaque formation and organic acid production was 100%, and in Example 1, which contained 0.005% by weight of grapefruit extract, 50% of gram formation was inhibited, and 0.01% by weight of grapefruit extract was shown. In Examples 2 to 14 containing more than%, all of the inhibitory effect of plaque formation and organic acid production was 100%, and the grapefruit extract was found to have excellent efficacy in inhibiting plaque formation and organic acid production.

Experimental Example 2: Inhibitory effect of the present invention toothpaste (Examples 1 to 14) and comparative toothpaste (Comparative Examples 1 to 3) against collagenase, which is a periodontal tissue degrading enzyme

1) Experiment Method

Experimental results of the present invention with the toothpaste inhibitory effect on collagen, a periodontal tissue degrading enzyme is as follows.

This test method is included in the salivary and gingival fluid of periodontal patients secreted from the bacteriopathogens Bacteriods gingivalis, Polymorphonuclear leukocytes, and Neutrophil. It is an experimental method that mimics the bio-oral environment where the collagen, which is the substrate of periodontal tissue, is degraded by the action of collagenase enzyme.

Add 100 μl of 2% red collagen-based Azpcoll solution to 25 1.5 ml Eppendorf tubes and use one Eppendorf tube as blank and three tubes from Sigma Add the purchased collagenase type I standard enzyme solution (collagen degrading activity: 315 units / mg) to 10, 100, 200ppm and separate the remaining tubes from the saliva and gingival sac of patients with periodontal disease. Another tube was used as a control by adding 100 µl of purely purified Klazenase enzyme separated through -200 chromatography, and Comparative Examples 1 to 3 and Examples 1 to 14 were added to each of the remaining tubes. After fully homogenizing with slurry of distilled water, centrifugation at 1000g for 10 minutes, and processing 100µl of supernatant, and adding 500µl of buffer solution (0.05M Tris-Hcl, 1nM CaCl ₂ , 7.8). 37 ℃ thermostat After reacting for 18 hours at 10000g, centrifuged at 10000g for 5 minutes, precipitated undigested collagen and taking a supernatant containing the decomposed collagen. The enzyme concentration of the enzyme was converted and the enzyme activity of the experimental group and the control group were evaluated.

2) Result of experiment

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

In the test results of Comparative Examples 1 to 3 and Examples 1 to 5 containing no green tea extract showed no inhibitory effect on collagenase enzyme activity that degrades the periodontal tissue, but the green tea extract 0.1 wt% to 1 Examples 6 to 14 containing the weight% showed excellent inhibition of enzyme activity, only green tea extract was found to have an excellent effect on the inhibition of collagenase enzyme activity that degrades periodontal tissue.

Experimental Example 3 Clinical Experiments on the Efficacy and Effect of the Toothpaste of the Invention (Examples 1 to 14) and Comparative Toothpaste (Comparative Examples 1 to 3)

1) Subject

Subjects were selected with 120 orthodontic examinations by selecting 30 oral subjects from 30 to 50 years of age by age from 30 to 50 years old. The clinical experiments on the gingival inflammation treatment effect of the present invention (Examples 1 to 14) and comparative products (Comparative Examples 1 to 10) were performed by the following method.

2) experimental method

After dividing the test group into the test group and the comparison group, after 2 hours after meals and after training three times a day before going to sleep, the toothpaste was performed to score the initial gingivitis index and to supply the present invention and the comparative product to use. After 1 week, 1 month, 3 months, 6 months, oral examination was performed to check the gingivitis index. To measure the gingivitis dimension, insert a periodental probe into the gingival sulcus and continuously probe each tooth without applying force and measure the bleeding state after 30 seconds. Record the results.

3) Experiment result

Results of conducting clinical trials for the treatment of gingivitis with the present invention are as follows.

4) Discussion

In the above clinical test results, Comparative Example 1 containing no medicinal active ingredient had no inhibitory effect on gingival inflammation, and Comparative Example 2 containing 0.001% by weight of grapefruit extract also had no inhibitory effect on gingival inflammation after 6 months. In Comparative Example 3 containing 1% of grapefruit extract, gingival inflammation inhibitory effect was found to be excellent, and Examples 1 to 5 containing 0.005 to 0.50% by weight of grapefruit extract alone showed gingival inflammation inhibitory effect. However, it was lower than the gingival inflammation inhibitory effect of Examples 6 to 14, which was prescribed in combination with grapefruit extract and green tea extract, containing grapefruit extract to inhibit plaque formation and green tea extract to inhibit the enzyme activity of collagenase. It can be seen that the gingivitis effect of the present invention is excellent in efficacy from one week to six months.

Experimental Example 4: Clinical comparison of bad breath inhibitory effect of the present invention toothpaste (Examples 1 to 14) and comparative toothpaste (Comparative Examples 1 to 3)

1) Subject

85 males and females in their 20s with no dental caries were selected and 5 subjects per product were tested.

2) experimental method

After chewing a certain amount of garlic (0.5g) for 2 minutes to induce oral bad breath, and then use it as a target product for 1 minute and after 1 minute, 5 minutes, 10 minutes, 15 minutes, the amount of methyl mercaptan, a bad breath product, is measured. .

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

The exhalation is 100 ml taken using a gas suction injection machine (Gas Tighter Syringe), and then measured by gas chromatography (detector: FPD).

At this time, a 1 ml sample loop is attached to analyze only 1 ml of exhalation.

The column uses a Chromosil 330, a filling length of 6 feet and an outer diameter of 1/8 inch, a Teflon tube. The column temperature is controlled at 70 ° C and helium is used as a carrier gas at 20 ml / min.

3) Experimental Result: Methyl Mecaptan Reduction (%)

According to the test results of measuring the toothpaste products of the Examples and Comparative Examples three times by the above method, the amount of methylmercaptan produced during garlic mastication over time is as follows.

63.3% to 65.5% of the toothpaste composition which does not use the medicament as in the comparative example, 71.2 to 72.4% of the toothpaste composition using 0.001% by weight of grapefruit seed extract, and 87.5% to 88.6 of the toothpaste composition using 1.0% by weight of grapefruit seed extract. Appeared.

Toothpaste composition using grapefruit seed extract as described above is excellent, in particular, toothpaste composition using 1.0% by weight of grapefruit seed extract is very difficult to apply to the product, such as a strong astringent taste when used.

Therefore, the bad breath removal effect of the toothpaste product using the grapefruit seed extract and green tea extract is considered to be very excellent.

Claims (5)

Toothpaste composition characterized in that it contains 0.005 to 1.0% by weight grapefruit seed extract and 0.01 to 5.0% by weight green tea extract. According to claim 1, Toothpaste composition containing 0.01 to 0.5% by weight of grapefruit seed extract. According to claim 1, Toothpaste composition containing green tea extract 0.05 to 1.0% by weight. The method of claim 1, wherein the medicament preventive of sodium fluoride, sodium fluorophosphate, amine fluoride, tin fluoride, xylitol, bactericidal chlorohexidine, cetylpyridium chloride or triclosan as a drug, bamboo salt, yellowish white, gilkyung , Mold, gardenia, licorice, sterling silver, gold, pore dinosaur or propolis, allantoin, aminocaproic acid, tranexamic acid or tocopherol as an anti-inflammatory agent, dextranase, glucose oxidase, glucoamylase, α, β as enzyme Toothpaste composition containing amylase, lactoperoxidase or lysozyme. The toothpaste composition of claim 1 comprising an abrasive, a humectant, a binder, a foaming agent, a sweetening agent, a preservative, and a fragrance.