KR100333445B1 - Composition for enhancing oral hygiene - Google Patents

Abstract

PURPOSE: Provided is an oral cleaning composition which contains ursodeoxycholic acid or chenodeoxycholic acid as an active ingredient. Therefore, it is useful for prevention and treatment of tooth decay and periodontitis. CONSTITUTION: An oral cleaning composition is characterized by containing, as an active ingredient, 0.02-1.0 wt.% of at least one of ursodeoxycholic acid and chenodeoxycholic acid having excellent inhibition effect on collagenase known as a causing material of periodontitis.

Description

Composition for enhancing oral hygiene {Composition for enhancing oral hygiene}

The present invention relates to an oral hygiene-promoting composition that is excellent in preventing, treating and preventing tooth decay. More specifically, the present invention is an active ingredient of at least one selected from urodesoxycholine acid and chinodesoxycholine acid, which have an excellent effect of inhibiting the activity of collagenase known as the causative agent of periodontal inflammation. It relates to a composition for enhancing oral hygiene that can be effectively prevented and treated periodontal disease and tooth decay.

Various oral diseases in oral tissues are caused by plaques composed of numerous bacteria present in the oral cavity. The clinical and pathological significance of the oral tissues is widely studied and Alexander (Alex, A, G, J Periodent, 42, 21-28) , 1971), Ash (MM, J. Periodontol, 35, 424, 1964).

Acupuncture, on the other hand, is a unique mixture of electrolytes and other components that play a specific role in the maintenance and digestion of oral health, which contains various enzymes, some of which contain metalloproteinases. Since the increased enzyme activity of salivary enzymes is found in patients suffering from periodontal disease, salivary enzymes have become an important research subject in terms of prevention and treatment of periodontal disease. In general, salivary glands, serum, leukocytes, epithelial cells, oral bacteria And the like are known to be involved in the production of such enzymes.

Collagenase, a kind of metalloproteinase, plays an important role in decomposing connective tissues and is inactivated in healthy oral cavity and activated in periodontal disease patients. Therefore, there has been a need for the development of a substance having inhibitory ability of collagen enzymes in the recognition that inactivating the collagen enzyme will play an important role in treating periodontal disease.

As is well known, fel tauri (gallbladder of Bos taurus demesticus Gmelin) and ungdam (gallbladder of fel ursi, Selenarctos thibetanus G. Cuvier, etc.) are herbal remedies, which are used in Chinese medicine for pain relief, sedation, dysentery, chronic hepatitis, sore throat, Efficacy of lifespan and anti-inflammatory has been known and widely used. In Korean Patent Laid-Open Publication Nos. 93-11992 and 93-11993, bovine gallbladder and salt are mixed with calcined salt at high temperature and glycocholic acid. And by applying an oral hygiene prepared by mixing and firing mixed with walnut juice and salt containing taurocholic acid (taurocholic acid) and to provide plaque removal effect and periodontal disease prevention, treatment effect. However, Woodam and Woongdam have various components as animal herbal medicines, and thus have poor stability when applied to the product, and have a high possibility of deterioration of the raw materials themselves and storage of drug efficacy.

Therefore, the present inventors have made intensive studies to improve the problems and prevent the periodontal disease by fundamentally suppressing the cause of periodontal disease. As a result, ursodesoxycholic acid, which is the main component of ungdam, and A composition containing at least one selected from chenodesoxycholic acid as an active ingredient effectively inhibits the activity of collagen enzymes, which may be the causative agent of periodontal disease, and these compositions contain wodam or ungdam itself. Compared to the composition to be found that the storage stability and the like is significantly improved and also safe for the human body to complete the present invention. Hereinafter, the configuration of the present invention will be described in detail.

The present invention relates to a composition for enhancing oral hygiene, characterized in that it contains at least one selected from urodesoxycholic acid and chenodesoxycholic acid as an active ingredient. Suitable examples of such oral hygiene-promoting compositions include toothpaste compositions, mouthwash compositions, chewing gum, oral massage creams, and the like.

Ursodesoxycholic acid and chenodes oxycholic acid, which are the active ingredients of the composition according to the present invention, may be used alone or in combination, respectively. In the case of mixing, the preferred mixing ratio is slightly different depending on the type of the composition, but the weight ratio In the range of 100: 1 to 1: 100, the amount of 0.02 to 1.0% by weight, preferably 0.02 to 0.6% by weight based on the total composition is preferably used when less than 0.02% by weight of the gingivitis prevention effect is weak This is because it is difficult to achieve the desired purpose, and when used in excess of 1.00% by weight, there is no proportional increase in efficacy according to the increase in the amount used.

In addition, the composition containing urodesoxycholic acid and / or chenodesoxycholic acid according to the present invention, if necessary, a fluorine compound such as sodium fluoride, sodium phosphate fluoride, amine fluoride, tin fluoride, chlorhexidine, etc. 1 species selected from herbal extracts such as bamboo salt, chlorohexidine, tranexamic acid, allantoin, capronic acid, enzymes and yellowish white extract, cirrhosis extract, mold extract, gardenia extract, licorice acid and wild guinea extract The above materials may be contained, and the kind of materials to be used may be appropriately selected depending on the composition to be prepared. In particular, it is preferable to use a mixture of bamboo salt, yellow white extract, gilyeong extract, mold extract and fluorine compound in a certain ratio as an auxiliary pharmacist, wherein the content of each auxiliary component is 1.0 to 5.0% by weight based on the total composition In the case of three kinds of herbal extracts, the total amount is used in an amount of 0.01 to 5.0% by weight on the same basis, and in the case of a fluorine compound, an appropriate amount usually applied in the technical field to which the present invention belongs, specifically 1.0 based on the total composition To 1.0% by weight. If the auxiliary active ingredient is used in less than the preferred amount of use does not meet the expected effect is difficult to achieve the desired purpose, if used in excess, there is a problem that the state of the toothpaste is poor.

Hereinafter, the composition of each composition will be described in more detail.

In the preparation of the toothpaste composition according to the present invention, in addition to the active ingredient, conventional ingredients constituting the toothpaste, for example, abrasives, wetting agents, binders, foaming agents, sweeteners, flavoring agents, acidity regulators, brighteners and the like are contained.

Double abrasives include calcium dihydrogen phosphate, precipitated silica, calcium carbonate and hydrous alumina. At least one material selected from kaolin, sodium bicarbonate (NaHCO ₃ ) is used in an amount of 20 to 60% by weight, based on the total composition.

As the humectant, one or more substances selected from glycerin, sorbitol, amorphous sorbitol liquid, propylene glycol, polyethylene glycol, and xylitol are used in an amount of 20 to 60 wt% based on the total composition, preferably glycerin or amorphous The sorbitol solution and propylene glycol or polyethylene glycol are used in a weight ratio of 20 to 50% by weight in a ratio of 10: 1 to 1: 1.

As the binder, 0.1 to 3.0% by weight, preferably 0.5 to 2.0% by weight of at least one selected from carrageenan, xanthan gum, sodium carboxymethylcellulose, carboxyvinyl polymer, sodium alginate, gum, and laponite is used.

As the foaming agent, an anionic surfactant such as sodium lauryl sulfate and sodium lauryl sarcosinate, and at least one material selected from sorbitan fatty acid ester, polyoxyethylene hardened castor oil, and polyoxyethylene polyoxypropylene-based condensed polymer material are 0.5 to 5.0. % By weight, preferably 0.5 to 3.5% by weight.

As the sweetening agent, 0.05 to 0.5% by weight of at least one substance selected from sodium saccharin, aspartame and licorice acid is used, and at least one substance selected from paraoxybenzoic acid ester and sodium benzoate is used as preservative.

In addition, as a fragrance, a suitable amount of peppermint oil, spearmint oil, menthol, carbon, etc. may be mixed, and preferably, an appropriate amount of anise oil (ANISE OIL) is added to the fragrance mixed with a predetermined ratio, and the acidity is good. As the regulator, one or more substances selected from phosphoric acid, sodium phosphate, citric acid, sodium citrate, succinic acid, sodium succinate, tartaric acid, and sodium stannate can be used, and these are adjusted to a suitable acidity, that is, pH 5 to 8 range. As the brightener, titanium oxide is preferably used in the range of 0.1 to 2% by weight.

Preferred examples of the toothpaste composition according to the present invention is a mixture of bamboo salt, fluorine compound, yellow and white extract, gilyeong extract and mold extract extract with one or more components selected from urodesoxycholine acid and chinodesoxycholine acid. It is used to prevent and treat gingivitis and periodontal disease.

On the other hand, the mouthwash composition in the composition according to the present invention is prepared as follows.

The mouthwash composition can be generally divided into an alcohol portion and a purified water portion, and is prepared by mixing two phases formed by dissolving various components in easily dissolving portions. In this case, ethanol is used to give a refreshing feeling when used in oral cleaning products and to dissolve flavors and preservatives that are insoluble in water. Generally, the higher the ethanol content, the better the divergence of the perfume. It is used in the range of 1 to 30.0% by weight, preferably 2.0 to 20% by weight since it tastes and stimulates the oral mucosa.

Essential ingredients used in preparing the mouthwash composition may include solubilizers, wetting agents, flavoring agents, sweeteners, preservatives, and the like, in addition to fungicides such as fungicides, enzymes, and antiplasmin agents.

Antiseptics may include antibiotics, cationic surfactants, and quaternary ammonium compounds, but antibiotics need to be thoroughly reviewed due to problems such as hypersensitivity and bacterial resistance. Enzymes are anaerobically decomposed by glucoamylase, alpha amylase, beta amylase, and oral bacteria to decompose dextranase, starch in food waste and other sticky polysaccharides in oral food, and produce organic acids. It is 0.1 to 100,000 units / gram product by mixing at least one kind of glucose oxidase which makes hydrogen peroxide by dissolving the surface and oxidizing glucose which causes caries, and lysozyme which has a bactericidal effect by destroying the cell wall by directly acting on the bacterial cell wall. use. Anti-plasmin agent is used to prevent gum inflammation and bleeding to prevent periodontal disease, and at least one of tranexamic acid and aminocapronic acid is used at 0.05 to 0.30% by weight, respectively.

Solubilizers for solubilizing perfumes in water include anionic surfactants such as sodium lauryl sulfate and sodium lauryl sarcosinate, sorbitan fatty acid esters, polyoxyethylene-cured castor oil, polyoxyethylene polyoxypropylene-based condensed polymer materials, advanced 0.1 to 3.0% by weight of at least one selected from polyoxyethylene derivatives of alkyl acetates and sorbitan fatty acid esters, preferably sodium lauryl sulfate, polyoxyethylene hardened castor oil and polyoxyethylene polyoxypropylene-based condensed polymer material, Preferably it is used in the content of 0.5 to 3.0% by weight.

Wetting agents are used to give the product stability, sweetness and slight viscosity, and examples thereof include glycerin, sorbitol liquid, amorphous sorbitol liquid, propylene glycol, polyethylene glycol, and xylitol. Among them, glycerin is preferable. , Amorphous sorbitol liquid and xylitol. The amount of wetting agent used is generally 2.0 to 40.0% by weight, preferably 3.0 to 20% by weight.

In addition, flavors and sweeteners are used to improve the usability, and as the flavoring agent, peppermint, spearmint, L-menthol, eucalyptus or methylsalicylate may be used in an amount of 0.1 to 1.0% by weight, and as a sweetener, lactose, Sorbitol, aspartame, sodium saccharin and the like can be used, and among them, saccharin sodium is usually used in 0.001 to 0.1% by weight.

As a preservative, at least one substance selected from benzoic acid, sodium benzoate, paraoxybenzoic acid ester, cresol and formalin is used in an amount of 0.05 to 0.15% by weight, and preferred are benzoic acid, sodium benzoate, methyl paraoxybenzoate or propyl ester. .

In addition, the mouthwash composition according to the present invention may further contain a buffer, a pigment, sodium chloride and the like. Buffers for adjusting the acidity (pH) of the dual mouthwash composition are mainly sodium primary phosphate, dibasic sodium phosphate, sodium triphosphate, citric acid, sodium citrate, succinic acid, sodium succinate, tartaric acid and sodium stannate, preferably One or more substances selected from the first sodium phosphate and the third sodium phosphate may be used in combination, and pigments may be used to increase the commercial value of the oral cleanser composition and to meet the purpose of use, mainly using food coloring. Sodium chloride is generally used in the range of 3 to 35% by weight for the purpose of alleviating inflammation and sterilizing gums.

Hereinafter, the present invention will be described in more detail based on the following Examples and Experimental Examples. However, these examples are only for the understanding of the present invention, and the scope of the present invention in any sense is not limited to these examples.

Experimental Example 1:

In order to compare the collagenase activity inhibitory activity of various substances, including urodesoxycholic acid and chenodesoxycholic acid, which are the active ingredients of the composition for enhancing oral hygiene according to the present invention, the experiment was performed as described below.

1) Subject

Ursodesoxycholic acid. Chenodes oxycholine acid, cow encephalitis, bamboo salt, saline, thick, yellow white, gilyeong, hyungdae, licorice, donkey, chamomile, myrrh, green tea, pogongyoung, gold and silver, horse riding

2) Experiment Method

① 100 μl of azocol solution at 2% concentration was added to the test tube, and 190 μl of buffer solution (0.05M Tris-HCl, 1 mM CaCl ₂ , pH 7.8) was added.

② Each of the agonists was added to the solution at the following concentrations.

-Ursodesoxycholic acid (10% ethanol solution) and Chenodesoxycholic acid (10% ethanol solution) are added to a final concentration of 0.02%

-Milkitis, bamboo salt, and salt are dissolved in the buffer solution and added to a final concentration of 2.0%.

-Thickened, yellowish white, gilkyung, hyunggae, licorice, donkey, chamomile, myrrh, green tea, pogongyoung, gold and silver, horse riding are added to the final concentration of 0.1% to 30% ethanol extract

③ 100µl of 100ppm collagen was added and then left for 18 hours at 37 ° C incubator (addition of 10, 100, 200µl of collagenase was prepared for standard activity curve).

④ The test tube was centrifuged for 5 minutes.

⑤ The supernatant was taken from the test tube and added to the cell. The absorbance at 540 nm was measured using a spectrophotometer, and then the activity of the experimental group was confirmed using a standard activity curve.

3) results

TABLE 1

Inhibitory Effect of Raw Material on Collagen

TABLE 2

Inhibitory Effect of Collagen Enzyme Activity by Concentration and Mixing Ratio of Ursodesoxycholine Acid and Chenodesoxycholine Acid

As can be seen from the results of Tables 1 and 2, urodesoxycholine acid and chinodesoxycholine acid were superior to other herbal extracts in terms of inhibitory effect of collagen activity, and the efficacy began to appear from 0.01%. The maximum value was 0.6% and there was no increase in the content. In addition, in the case of mixing and applying urodesoxycholic acid and chinodesoxycholic acid, the efficacy according to the total content of the mixture was similar to that of each raw material.

Examples 1-6 and Comparative Examples 1-4:

Toothpaste compositions of Examples 1 to 6 and Toothpaste compositions of Comparative Examples 1 to 4 according to the present invention were prepared in the following composition ratios. The order of preparation of these toothpaste compositions was to disperse the powder components such as carboxymethyl cellulose sodium, saccharin sodium and paraoxybenzoic acid ester in wet sorbitol liquid and glycerin, dilute with purified water, and then mix in primary mixer. Toothpaste composition was prepared by adding an abrasive such as calcium dihydrogen phosphate and a medicinal agent to the mixed solution, mixing the mixture, and finally adding a foaming agent, sodium sulfate, stabilizers, and flavoring ingredients, and mixing in a vacuum.

TABLE 3

Note) Unit: weight%

Experimental Example 2:

In the toothpaste compositions of Examples 1 to 6 and Comparative Examples 1 to 4 of Table 3, the inhibitory effect of plaque formation and the gingival inflammation inhibitory effect were tested as follows, and the results are shown in Tables 4 and 5, respectively.

1) Experiment Method

① Screening the subject and explain the oral examination.

② Randomly dispense 10 subjects for each Example and Comparative Example composition, train the correct brushing method, and conduct oral examination to perform the Quigley-Hein Index modified by Turesky and Gingival Bleeding Index. , Loe-Silness Index).

③ Scale before the experimental group.

④ After using the control toothpaste for two weeks, oral examination is performed. At this time, the plaque index and the gingival index should be initial values.

⑤ Example and Comparative Example Toothpaste is distributed to each subject, and brushing is carried out three times a day for 4 weeks in the same manner as usual, and oral examination is performed at 2 and 4 weeks to score the plaque index and gingivitis index. .

⑥ Test the statistical significance by T-test by comparing the initial value of the experimental group with the score after 4 weeks.

TABLE 4

Plaque index

TABLE 5

Gingival index

As can be seen from the results of Table 4, the toothpaste compositions of Examples 1 to 6 and Comparative Examples 1 to 4 were used for 4 weeks, and then the plaque index was measured to perform statistically significant difference test. In the compositions of Examples 1 to 6 and Comparative Examples 1 to 3, it was confirmed that there is a significant effect after use compared to before use. However, no significant effect difference could be confirmed between the compositions of Examples 1 to 5 and Comparative Examples 1 and 2, and in Example 6 and Comparative Example 3, the significant difference was compared with Examples 1 to 5 and Comparative Examples 1 to 2 It was confirmed that no significant difference was found between Example 6 and Comparative Example 3. Therefore, urodesoxycholic acid and / or chinodesoxycholic acid do not seem to have a significant effect on suppression of plaque formation, and even when used in combination with herbal ingredients, there is no increase or inhibition effect. see.

On the other hand, as shown in Table 5 showing the results of statistically significant test by measuring the gingival index after using the toothpaste composition of Examples 1 to 6 and Comparative Examples 1 to 4 for 4 weeks, in the gingivitis relief effect The compositions of Examples 1 to 6 and Comparative Examples 2 to 3 showed a significant effect after use compared to before use, and Example 6 exhibited a better gingivitis relief effect compared to Comparative Example 3. In addition, looking at the basis of the urethanesoxy choline acid, the use of the gingival inflammatory effect began to appear from 0.01% by weight, and compared to Comparative Example 4 containing no urethanesoxy choline acid from 0.02% by weight or more On the other hand, when it was found to show a significant effect, when it exceeds 1.0% by weight (Comparative Example 2) there was no increase in efficacy proportional to the content used. Accordingly, urodesoxycholic acid and / or chenodesoxycholic acid are believed to exhibit good alleviation of gingival inflammation, and when used for this purpose they are in the range of 0.02 to 1.00% by weight, preferably 0.02 to 0.6% by weight. It was confirmed that it should be used, and it was confirmed that synergistic effect on gingivitis relief was applied by mixing with several herbal ingredients including bamboo salt.

Examples 7-12 and Comparative Examples 5-8:

The mouthwash composition of Examples 7 to 12 and Comparative Examples 5 to 8 according to the present invention was prepared according to a conventional method at the composition ratios shown in Table 6 below. That is, after completely dissolving the ethanol solubilizing agent as a solvent, the fragrance is added and stirred sufficiently, and this is added to the purified water part (liquid prepared by dissolving the humectant and other components in purified water) while stirring to completely solubilize the solution. The mouthwash composition was prepared by filtration in a conventional manner.

TABLE 6

Note) Unit: weight%

Experimental Example 3:

The oral cleaning composition of Examples 7 to 12 and Comparative Examples 5 to 8 of Table 6 was tested in the same manner as described in Experiment 2 to inhibit plaque formation and gingival inflammation formation, and the results are shown in Table 7 and 8 is shown respectively.

TABLE 7

Plaque index

TABLE 8

Gingival index

As can be seen from the results of Tables 7 and 8, the oral cleanser compositions of Examples 7 to 12 and Comparative Examples 5 to 8 were used for 4 weeks, and then the plaque index and the gingival index were measured and statistically significant. , The same phenomenon as in the case of toothpaste composition, urethanesoxycholine acid and / or chenodesoxycholine acid does not have a significant effect on the inhibition of plaque formation even when used as an active ingredient of the mouthwash composition On the other hand, it is considered to exhibit excellent gingivitis effect, and when used for this purpose, they should be used in the range of 0.02 to 1.00% by weight, preferably 0.02 to 0.6% by weight, and mixed with several herbal ingredients including bamboo salt. As a result, the synergistic effect of gingivitis was alleviated.

Example 13: Chewing Gum

Example 14 Oral Massage Cream (Ointment)

The chewing gum composition of Example 13 and the oral massage cream composition of Example 14 all showed an excellent effect in gingivitis inflammation relief.

Urodesoxycholine acid and chinodesoxycholine acid used as active ingredients in the present invention have excellent inactivation ability against collagen enzyme, which is a periodontitis-causing factor, and thus these compositions for enhancing oral hygiene, for example, toothpaste compositions, mouthwash compositions, When applied to chewing gum, oral massage creams, etc., these compositions were found to exhibit excellent gingival inflammation relieving effect.

In addition, the oral hygiene-promoting composition of the present invention exhibiting such an excellent effect does not use the raw herbal or woodam itself, which is an animal herbal medicine, so it is less likely to deteriorate the raw materials according to storage conditions, and thus has excellent storage stability and excellent safety for the human body. Has the advantage that it can be used.

Claims (10)

Oral hygiene composition for promoting oral hygiene, characterized in that it contains at least one selected from urodesoxycholine acid and chenodesoxycholine acid as an active ingredient. The composition according to claim 1, which contains 0.02 to 1.0% by weight of at least one selected from urodesoxycholic acid and chenodesoxycholic acid. The composition of claim 2 containing from 0.02 to 0.6% by weight. The composition according to claim 1, wherein the mixture is used in a weight ratio of 100: 1 to 1: 100 when urethanesoxycholine acid and chinodesoxycholine acid are mixed. The method according to claim 1, wherein the auxiliary medicament as sodium fluoride, sodium phosphate, fluoride amine, tin fluoride, chlorhexidine, bamboo salt, tranexamic acid, allantoin, capronic acid, enzymes, sulfur white extract, gilyeong extract, mold extract A composition containing at least one substance selected from gardenia extract, licorice acid and fresh guinea extract. The composition according to claim 5, wherein the composition contains 1.0 to 5.0 bamboo salts, the total content of sulfur white extract, gilpyeong extract and mold extract is 0.1 to 5.0% by weight, and contains 0.1 to 1.0% by weight of a fluorine compound. . The composition of claim 1 wherein the formulation is a toothpaste composition. The composition of claim 1 wherein the formulation is a mouthwash composition. The composition of claim 1 wherein the formulation is chewing gum. The composition of claim 1 wherein the formulation is an oral massage cream.