KR20050073925A - Toothpaste composition - Google Patents

Abstract

The present invention relates to a dentifrice composition characterized in that it contains proline or glycine or a mixture of proline and glycine together with glutathione. According to the invention

And amino acids are used to prevent collagen, oral mucosa-induced collagen, to repair collagen damaged due to inflammation, to relieve symptoms, and to inhibit inflammation by the antioxidant glutathione to provide oral health. do.

Description

Toothpaste Composition

The present invention relates to a dentifrice composition, and more particularly, to a dentifrice composition which effectively alleviates and prevents oral inflammation such as gingivitis periodontitis by containing proline or glycine or a mixture of proline and glycine together with glutathione.

The most representative protein constituting the connective tissue of the living body is collagen, oral tissue is also composed of collagen protein. Collagen is a fibrous protein that contains more than 1000 amino acids to form collagen molecules. Collagen protein is mainly present in the human body's membranes, articular cartilage, cornea of the eye, bones and skin.In particular, it is a component of the dermal layer of the skin that causes the function of calcium adhesive and wrinkles. very important. Connective tissue is a tissue that connects or supports the entire body, skin, organs, or cells. All organs such as the liver and heart exist as connective tissue. In particular, the dermis, tendons, cartilage, bones, etc. are organs consisting only of connective tissue.

The components of the connective tissue are the most watery and occupy the drug. The other two are organic compounds, mainly proteins and polysaccharides. That is, the main component is a substance in which polysaccharide is bound to a collagen, elastin protein, and a protein called proteoglycan.

Collagen is a kind of protein. Like many proteins in cells or proteins in blood, collagen is hardly present in the water, but in the form of fibers. Collagen fiber has the most basic role of connective tissue, supporting the body or organs, binding, reinforcing, or creating an interface, and is the most protein in the body.

Collagen is widely found in the animal world, from mammals to birds, reptiles and fish to sea cucumbers, earthworms and sponges. Collagen, unlike other proteins in vivo, has a very high content of hydrophobic amino acids such as glycine and proline among its constituent amino acids.

Proline is a chemical formula of C ₅ H ₉ NO ₂ , having a structure of pyrrolidine-2-carboxylic acid. In 1901 E. Fischer first isolated during casein hydrolysis and named proline, and DL-proline was synthesized by R. Wilstedter in 1899. L-proline is contained in several proteins such as prolamin, protamine, casein, gelatin, and especially in collagen and its modified gelatin. Sweet, colorless crystals, the only amino acid that is soluble in ethanol and has the highest solubility in water.

Glycine is also called glycocoll or aminoacetic acid and the formula is represented by NH ₂ CH ₂ COOH. It is a non-essential amino acid first extracted from the hydrolyzate of a protein. It is a colorless columnar crystal, decomposed with foaming at 232 ~ 236 ℃. It is soluble in water but hardly soluble in organic solvents such as alcohol and ether. The only amino acid with no asymmetric carbon atom, no optical isomers. In 1820, H. Bracono (1780-1855) first extracted from collagen. Generally, vegetable protein is rarely contained, but animal protein is contained in large amounts. For example, silk yarn fibroin contains 40.7% and gelatin 25.5%. Moreover, it is also a component of proteins, such as hormones, such as oxytocin and vasopressin, and glutathione. In animals, it is synthesized by an interconversion reaction with serine, and glutamic acid or glutamine becomes a source of amino groups in glyoxylic acid to produce glutin. In addition, it plays an important role in metabolism in vivo, and is involved in the synthesis of hemoglobin, chlorophyll, and vitamin B porphyrin as well as purine, which is a base component of nucleic acid, and creatine involved in energy metabolism.

Glutathione is a peptide consisting of three amino acids

As the peptide, its constituent amino acids are glutamic acid, cysteine, glycine and the like. Glutathione is made in the liver and is a very powerful antioxidant that removes radicals or free radicals from the body. It also increases the titer of glutathione peroxidase along with cysteine in the body. This enzyme prevents free radicals from damaging parts of the body. Glutathione peroxidase has DNA repair, T lymphocyte activation, and various other cancer-causing effects. It also prevents the formation of free radicals and protects cellular tissues already damaged by free radicals.

 In the past, toothpaste and other oral products such as tranexamic acid, a kind of non-protein amino acid, have been used for the prevention and alleviation of gum disease, but biological amino acids such as glycine and proline and peptides such as glutathione No example was applied.

As a material for preventing or alleviating gum inflammation in the existing toothpaste, aminocaproic acid, vitamin E acetate (tocopherol acetate), allantoin and its derivatives, tranexamic acid, salt, pyridoxine hydrochloride (vitamin B6), and the like have been used. However, these materials were difficult to achieve the effect sufficiently, and some materials were difficult to apply a sufficient amount to cause the efficacy effect by causing a change in toothpaste stability.

The present invention is surprising that the dentifrice composition with proline or glycine or a mixture of proline and glycine together with glutathione for the prevention and treatment of gum disease such as periodontitis and gingivitis exhibits much improved efficacy and effect than conventional toothpaste. The facts have been discovered and the present invention has been completed.

 The present invention relates to a dentifrice composition characterized in that it contains proline or glycine or a mixture of proline and glycine together with glutathione.

The toothpaste composition of the present invention is a conventional ointment as a formulation and packaging form of the final product.

It can be applied to a tube (on paste). In the dentifrice composition of the present invention, glycine and proline in amino acids are each used as an amount of 0.001 to 1.0 grams in 100 grams of toothpaste as a weight in the dentifrice composition, and glutathione is used in an amount of 0.001 to 0.5 grams and below these concentration ranges. The effect is weak and above that, the cost is increased compared to the effect increase factor, and the fragrance and stability of the composition are not good.

The toothpaste composition according to the present invention can be proved through clinical experiments to reduce gum inflammation by amino acids and peptides, which is the antioxidant effect of the toothpaste composition according to the present invention amino acids and peptides It means that it is possible to prevent gum inflammation by inhibiting the generation of causative free radicals and to help relieve inflammation by aiding the biosynthesis of collagen, a constituent protein of gum tissue.

The type and the amount of abrasive used in the toothpaste composition of the present invention is precipitated silica, silica gel, zirconium silicate, calcium dihydrogen phosphate, anhydrous calcium monohydrogen phosphate, hydrous alumina, hard calcium carbonate, heavy calcium carbonate, calcium pyrophosphate, insoluble 5 to 60% by weight of at least one selected from metaphosphate and aluminum silicate is used, and although the particle size also varies depending on the type of abrasive, it is preferable to use an average particle diameter of 20 micro or less.

The use of humectants in toothpaste is an essential ingredient in the preparation of ointment formulations, which prevents the toothpaste from drying and solidifying when exposed to the air and gives the surface of the toothpaste a glow, as well as sweetening the toothpaste. In the present invention, concentrated glycerin (98%), glycerin (85%), sorbitol aqueous solution (70%), amorphous sorbitol aqueous solution (70

%), 20 to 70% by weight of one or more selected from ziitol, polyethylene glycols and propylene glycol.

In addition, a conventional dentifrice composition may use a suitable medicinal ingredient depending on the purpose of use. The use of a fluoride which forms a fluorine film on the teeth and makes it resistant to acid (lactic acid, etc.), which is a metabolite of caries, can be an essential ingredient in toothpaste compositions. . In addition, as a method for preventing periodontal disease, aminocapronic acid, allantoin and allantoin derivatives and vitamins may be used at the same time, and triclosan may be used simultaneously for the purpose of improving oral hygiene by inhibiting the reproduction of harmful microorganisms in the oral cavity.

The use of binders in toothpaste is essential to ointment toothpaste as it prevents the separation of solid powder and liquid components and can be used as long as it is a water-soluble polymer. Commonly used components include sodium carboxymethyl cellulose derived from cellulose, carrageenan extracted from seaweed, and xanthan gum obtained from metabolism of microorganisms.

Preservatives can help to prolong toothpaste preservation by preventing microbial contamination. Representatives include benzoic acid and parabens.

In addition, the use of foaming agent to enhance the feeling of use of the product, to help the cleaning action, and to act to easily remove foreign substances in the oral cavity by speeding up the dispersion and penetration of other active ingredients and reducing the interfacial tension. As the foaming agent, sodium lauryl sulfate, which is an anionic surfactant, is mainly used, and a copolymer of polyoxyethylene polyoxypropylene (poloxamer), polyoxyethylene-cured castor oil, and polyoxy, which is auxiliary nonionic surfactant depending on the characteristics of the formulation. Ethylene sorbitan fatty acid ester and the like are used.

In addition, in order to improve the feeling of use of the toothpaste composition according to the present invention can be used flavors, sweeteners and pigments, and for this purpose, the use of edible spices is essential, peppermint oil, spearmint oil, sage, eucalyptol, methylsalley Silates, fruit extracts, and the like. The most commonly used sweetener is sodium saccharin, and food coloring is mainly used.

The composition and composition of the present invention and the existing commercially available gum disease preventive toothpaste and tooth decay for preventing tooth decay and plaque in various aspects have been tested and evaluated in terms of effectiveness and stability. (See Tables 2, 3, 4 and 5), thus confirming that the inventors achieved the intended effect.

Hereinafter, the present invention will be described in more detail based on the following Examples and Comparative Examples. However, this is only to help the understanding of the present invention, the technical scope of the present invention in any sense is not limited thereto.

Examples 1-5 and Comparative Examples 1-3

Toothpaste composition according to the present invention (Examples 1 to 5) and the existing toothpaste composition (Comparative Examples 1 to 3) for comparison with the composition ratio as shown in Table 1 was prepared. The manufacturing method is as follows. The binder and other additives were previously dispersed in the humectant, and the active ingredients such as the abrasives and amino acids were added, followed by stirring for about 30 minutes. Finally, the foaming agent and the fragrance component were added, followed by stirring for 20 minutes in a vacuum state to obtain a final product.

Table 1

Experimental Example 1. Clinical oral inflammation mitigation effect evaluation

In order to clinically confirm the oral inflammation mitigation effect of the compositions of Examples and Comparative Examples, 400 male and female 20 to 40 year olds with oral inflammation were selected and divided into eight groups. After the primary oral examination of the marginal gingival and papillary gingival of the upper and lower anterior labial cavities according to the gingival index score of Silness, the test results were divided into the use groups of the Examples and Comparative Examples. The same toothbrush was provided and brushed in a customary manner, and the oral examination was performed in the same manner as the primary oral examination at the stage of 6 months. The measured results were t-tested to compare the differences with the comparative examples. The results are shown in Table 2 below.

TABLE 2

Significance *: gingival index t-test at the beginning of the experiment and at 6 months

Significance 1: t-test with Comparative Example 1,

Significance 2: t-test with Comparative Example 2,

Significance 3: t-test with Comparative Example 3

As shown in the results of Table 2, the gingival index of the group using the compositions of the examples was statistically significantly reduced, and also statistically significant differences with the comparative example. In the above results, the composition of the present invention was analyzed and evaluated to be superior to the oral inflammation mitigation effect compared to the conventional oral inflammation mitigation component.

Experimental Example 2 Inhibitory Effect of Laboratory Active Oxygen Generation

In order to compare the effect of preventing gum inflammation, the inhibitory effect of free radical generation, known as an inflammation-inducing substance, was compared and evaluated through a test. 1.0 g of the compositions of Examples and Comparative Examples containing glutathione were treated to macrophages and treated with pobolmystate acetate as a stimulus to generate active oxygen. In this case, chemiluminescence is caused by luminol treatment on the active oxygen generated, and the value thereof is measured, and the inhibition rate of inflammation is obtained by comparison with Comparative Example 3. The results are shown in Table 3.

% Inhibition = chemiluminescence of Comparative Example 1-chemiluminescence of Example x100

                        Chemiluminescence of Comparative Example 3

TABLE 3

Example 1 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 % Inhibition 51 83 71 96 36 32

As shown in Table 3, the composition containing glutathione in the examples showed a significantly higher active oxygen generation inhibitory effect compared to the comparative example was excellent in the anti-inflammatory effect.

Experimental Example 3. Evaluation of Antioxidant Effect of Laboratory Toothpaste

In order to compare the effects of gum inflammation, the antioxidant effect of toothpaste was evaluated. In order to evaluate the anti-oxidant effect, 1.0 g of the composition of Example and Comparative Example containing glutathione was treated with 3 mL of 10 mM linoleic acid solution (1 mM phosphate buffer solution pH 7.0) and then maintained at 37 ° C. for 18 hours. Then, 0.1 mL of the solution was added, followed by adding 9.1 mL of 70% Ethanol, 0.1 mL of 30% ammonium thiocyanate, and 0.1 mL of 20 mM Ferrous Chloride and maintained for 3 minutes. After centrifugation of the test solution, the absorbance was measured at 500 nm using a spectrophotometer, and the measured value was compared with the absorbance of Comparative Example 3 to obtain an antioxidant rate. The results are shown in Table 4.

% Antioxidant = absorbance of Comparative Example 3-absorbance of Example × 100

                       Absorbance of Comparative Example 3

Table 4

Example 1 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 Antioxidant Rate (%) 59 88 76 98 48 41

As shown in Table 4, the composition of the Example showed an excellent anti-oxidant effect compared to the comparative example was excellent in the inflammation inhibitory effect.

Experimental Example 4. Comparative evaluation of the stability of the toothpaste composition

The state stability of the toothpaste composition was evaluated at regular intervals according to the following criteria while the toothpaste compositions of Examples and Comparative Examples were stored at room temperature and 40 ° C.

<< evaluation criteria >>

◎ Very good: smooth surface, no phase separation, normal toothpaste

Relatively good: only the surface is slightly rough or the tube entrance is slightly bad

불량 relatively poor: phase separation and slight discoloration

 × Very poor: severe phase separation and gas generation or hardening

Table 5

The compositions of the examples were all evaluated as good in terms of state stability as compared to the compositions of the comparative examples.

The toothpaste composition according to the present invention prevents damage of collagen, which is an oral mucosa component protein, and repairs collagen damaged by inflammation, etc., effectively alleviating symptoms and inhibiting inflammation by the antioxidant glutathione, thereby protecting oral health. Function

Claims (3)

A dentifrice composition characterized in that it contains proline or glycine or a mixture of proline and glycine together with glutathione. The dentifrice composition according to claim 1, which contains 0.001 to 1.00 wt% of proline and 0.001 to 1.00 wt% of glycine. The dentifrice composition according to claim 1, which contains 0.001 to 0.50% by weight of glutathione.