KR19990041922A - Enzyme-containing toothpaste composition - Google Patents

Abstract

The present invention relates to a toothpaste composition that is safe for the human body and has an aesthetic function. Specifically, the present invention provides a toothpaste composition that is stable and effective in storage of a product by using a water-soluble condensate phosphate and hydroxyapatite and hydroxyapatite in a toothpaste composition having a whitening effect, and generating a peroxide when the double enzyme system is used. It is about.

The toothpaste composition of the present invention contains dextranase or glucanase and glucose oxidase, and at the same time, water-soluble condensate phosphate and hydroxyapatite.

Description

Enzyme-containing toothpaste composition

The present invention relates to a toothpaste composition that is safe for the human body and has an aesthetic function. Specifically, the present invention provides a toothpaste composition that is stable and effective in storage of a product by using a water-soluble condensate phosphate and hydroxyapatite and hydroxyapatite in a toothpaste composition having a whitening effect, and generating a peroxide when the double enzyme system is used. It is about.

In general, tooth discoloration factors can be classified into exogenous discoloration and endogenous discoloration. Exogenous tooth discoloration may be caused by food waste, nicotine and tar components of tobacco or coffee, tea, etc. deposited on the tooth surface, or soft deposits on the tooth surface by staining with pigment components. Loss or overdose of tetracycline antibiotics or fluorides, or aging. In addition, toothpaste compositions with excessive amounts of cationic surfactants have also been shown as tooth discoloration factors.

Toothpaste for whitening has been commercialized and used for a long time in order to suppress or prevent tooth discoloration caused by these various causes. Looking at the teeth whitening technology commercialized to date, the most classic method is the method of strong polishing and the method of corrosive tooth surface by adjusting the pH of the product to strong acidity.

However, the method by the strong degree of polishing simply polishes the surface of the tooth to make the surface smooth and expect the whitening effect, but the tooth and the gum where the enamel area is the thinnest area due to excessive wear of the tooth itself when used for a long time It is obvious that abrasion can occur first and cause cervical abrasion. The method of adjusting the pH of the product to strong acidity to corrode the tooth surface also presupposes the corrosion of the tooth surface, so that the damage of the tooth caused by this corrosion will reduce the hardness of the tooth and increase the rate of tooth decay and cause irritable teeth. There is a problem that can be.

Recently, commercially available technologies are used to make the surface of teeth roughened with hydroxyapatite or titanium dioxide to smooth the surface of the teeth or bleach using peroxide-based materials.

However, it is difficult to expect the actual whitening effect with only the smoothing of the tooth surface. The bleaching effect by peroxide is expected to be effective. However, when the peroxide is used in toothpaste, it is compatible with common ingredients used in toothpaste. In addition to poor performance, the peroxide itself is very unstable, so the concentration of active oxygen decreases rapidly over time.

In order to overcome this problem, US Pat. Nos. 4,687,663 and 5,020,694, etc., use a double container system to separate peroxides to stabilize peroxides over time, and US Pat. No. 5,122,365 uses three separate packages to In the step 2, the tooth surface is treated with acid, the step 2 is bleached with peroxide, and in step 3, the surface of the tooth is smoothed with titanium oxide. If this is not considered and commercialized on this principle, the inconvenience of use and the increase of the packaging cost of the manufacturer are expected to be a problem.

On the other hand, US Patent No. 4,986,981 attempts to whiten teeth using papain, a plant proteolytic enzyme, without peroxide as another approach to tooth whitening effect. The effect was also evaluated to be very weak. In addition, the use of enzymes in toothpaste compositions has been used for many years, not for the purpose of whitening, but for the purpose of biochemical plaque decomposition and sterilization, and Japanese Patent Application No. 87-4221 discloses the use of dextranase to stabilize carbon sources. The higher fatty acid alcohols of embroidery 18 to 28 were used and US Patent No. 4,537,764 claims that hydrogen peroxide occurs when used simultaneously with glucose and glucose oxidase in the toothpaste composition, resulting in a bactericidal effect. However, the composition has a problem in that the enzyme and the substrate of the enzyme are used at the same time, the enzyme reaction proceeds in the composition to lose gas generation and effects.

Therefore, the present inventors do not have excessive wear and corrosion of teeth and when the peroxide is generated by using the biochemical reaction with the plaque in the oral cavity when used without using the peroxide, it is safer to the human body, and it can maximize the whitening effect as well as the whitening effect. A study on the prescription of toothpaste, which used dextrane or glucanase, used glucose oxidase, which oxidizes the final breakdown product of glucose to form peroxides, and at the same time, a source of tooth discoloration. The present invention has been accomplished by using a water-soluble condensate phosphate capable of radically removing hydroxyapatite which is coated on a rough or damaged tooth surface to impart gloss on the surface.

Toothpaste composition of the present invention is dextranase or glukenase that can biochemically decompose the dextran or glucan of the prag, glucose oxidase which oxidizes the final decomposition product glucose to form peroxides, sources of tooth discoloration One or two or more water-soluble condensate phosphates represented by the following chemical formula which can be essentially removed, and hydroxyapatite which gives the surface gloss by coating on rough or damaged tooth surfaces:

M _{n + 2} P _n O _{3n + 1}

Wherein M is sodium or potassium and n is an integer of 2 or greater.

The toothpaste composition of the present invention can be applied to the tube of the existing ointment (paste) as a formulation and packaging form of the final product.

Dextranase and glucanase used in the toothpaste composition of the present invention are used in an amount of 250 units / gram toothpaste to 25000 units / gram toothpaste in the toothpaste composition, and glucose oxidase is 10 units / gram toothpaste to 150 in the toothpaste composition. Used in units / grams of toothpaste. Below these concentration ranges, the effect is insignificant, and above that, the cost rises compared with the effect increase factor, and the time-lapse stability of a composition is not good.

As the water-soluble condensed phosphate used in the toothpaste composition of the present invention, one or two or more thereof may be specifically selected from sodium pyrophosphate, potassium pyrophosphate, sodium pyrophosphate, sodium tripolyphosphate or potassium salt. Their content is 0.5 to 7% by weight. Hydroxyapatite contains 0.1 to 10% by weight. Water-soluble condensate phosphate and hydroxyapatite have a weak effect below the lower limit of the amount used, and use above the upper limit of the condensate phosphate may cause intraoral irritation when brushing teeth. .

Experimental experiments show that the toothpaste composition according to the present invention has the effect of degrading plaque by biochemical enzyme action, inhibiting tartar formation by soluble condensate phosphate, and relieving hypersensitivity by hydroxyapatite in addition to tooth whitening function. And clinical experiments (see Experimental Example 3), which indicates that the toothpaste composition according to the present invention is not a cosmetic whitening toothpaste with a simple whitening function but fundamentally removes the causative agent of all diseases in the oral cavity. This means that you can relieve tooth decay and gum disease at the same time.

Particularly, the degrading effect of dextranase is caused by biochemical enzymatic reaction, and it is a poor brushing or wrong brushing method that can dissolve and dissolve even plaque between teeth and teeth that are hard to brush when brushing teeth. It is thought that better plaque removal effect can be expected for those who do.

The type and the amount of abrasive used in the present invention are precipitated silica, silica gel, zirconium silicate, calcium dihydrogen phosphate, calcium dihydrogen phosphate, hydrous alumina, hard calcium carbonate, heavy calcium carbonate, calcium pyrophosphate, insoluble metaphosphate, And 5 to 60% by weight of at least one of the aluminum silicates to give a final value of 50 to 100, the particle size is also dependent on the type of abrasive, but the average particle size is preferably 20 micro or less Do.

There is no standard standard for toothpaste polishing, but when comparing the degree of polishing of commercially available toothpaste, the roughness of less than about 50, the less than 50 to 100 medium polishing, and the more than 100 are classified as high polishing. Long-term brushing with high-polishing toothpaste is very likely to cause cervical abrasion as mentioned above. The degree of polishing of the toothpaste may be determined by the type and amount of the abrasive among the components of the toothpaste.

The use of humectants in toothpaste is an essential base ingredient for making ointment formulations. It prevents dry solidification when toothpaste is exposed to the air, gives shine to the surface of the toothpaste, and gives a sweetening effect when brushing depending on the type. . In the present invention, 20 to 70 using concentrated glycerin (98%), glycerin (85%), aqueous sorbitol solution (70%), aqueous solution of amorphous sorbitol (70%), xyitol, polyethylene glycol, and propylene glycol Use by weight.

In addition, in conventional toothpaste compositions, suitable medicinal ingredients can be used depending on the purpose of use. The use of fluoride, which forms a fluorine film on the teeth and makes it strong for acid (lactic acid, etc.), a metabolite of caries, has recently been recognized as an essential ingredient in oral toothpaste compositions. It is becoming. In addition, in order to prevent periodontal disease, water-soluble salts such as sodium chloride or sodium bicarbonate having high osmotic pressure, aminocapronic acid, allantoin and allantoin derivatives having hemostatic action, and various vitamins may be used simultaneously.

In particular, the hydroxyapatite used in the present invention has been known to be effective for hypersensitive teeth by filling the crown of dentin exposed from damaged teeth in the past, but these techniques have recently been applied as a whitening effect. In other words, hydroxyapatite is the main component of the bones and teeth of the human body, and especially in the enamel layer, which is the outer surface of the tooth, hydroxyapatite occupies about 97%. Therefore, when the fine powder of hydroxyapatite is used, the tooth surface can be whitened by filling the tooth surface by adsorption to the damaged and rough tooth surface.

On the other hand, the use of the binder in the toothpaste is a role that prevents the separation of the solid powder component and the liquid component is essential in the ointment, and any water soluble polymer can be used. In general, many of the components used include sodium carboxymethylcellulose synthesized from cellulose of wood, carrageenan oil extracted from seaweed, and xanthan gum obtained from metabolism of microorganisms.

The use of foaming agent enhances the feeling of use of the product, helps cleansing action, facilitates the dispersal and penetration of other active ingredients, and reduces the interfacial tension, thereby easily removing foreign substances in the oral cavity. As the foaming agent, sodium lauryl sulfate, an anionic surfactant, is mainly used, and a copolymer of a polyoxyethylene polyoxypropylene (poloxamer), a polyoxyethylene-cured castor oil, poly Oxyethylene sorbitan fatty acid ester etc. 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, etc. The fragrance used for this purpose is necessary to use edible edible flavors, peppermint oil, spearmint oil, Sage, eucalyptol, methyl salicylate and fruit extract can be used. Sodium saccharin is the most commonly used sweetener, and food coloring is mainly used.

As a result of comparing and evaluating the effect and stability of the toothpaste composition of the present invention composed of the above components and the existing whitening toothpaste in various aspects, the toothpaste composition according to the present invention was found to be much superior (Tables 2 and 3). , 4, 5 and 6) Thus, the inventors could achieve the intended effect.

Hereinafter, the present invention will be described in more detail with reference to Examples and Comparative Examples. However, these examples are only for the understanding of the present invention, and do not limit the scope of the present invention in any sense.

<Examples 1 to 5 and Comparative Examples 1 to 2>

Toothpaste compositions according to the present invention (Examples 1 to 5) and conventional toothpaste compositions (Comparative Examples 1 to 2) for comparison thereto were prepared in the following composition ratios.

division Ingredient Name Example Comparative example One 2 3 4 5 One 2 abrasive Precipitated silica 20.0 - 5.0 - - - - Calcium dihydrogen phosphate - 35.0 - - 5.0 - 40.0 Hydrous alumina - 5.0 - 30.0 - 30.0 - Hard calcium carbonate - - 30.0 5.0 - 5.0 - Calcium Pyrophosphate - - - 5.0 - 5.0 - Silica gel 3.0 - - - 10.0 - - Humectant Concentrated glycerin (98%) - 50.0 20.0 - 2.0 - 35.0 Sorbitol aqueous solution (70%) 35.0 - - 33.0 60.0 33.0 - Zyritol - - 5.0 1.0 - 1.0 - Foam Sodium Lauryl Sulfate 2.0 2.0 1.5 2.0 2.0 2.0 2.0 Poloxamer - - 0.5 - - - - Binder Carboxymethyl Cellulose Sodium 0.2 - - - 0.1 - - Xanthan Gum 0.5 - 0.7 0.3 0.3 0.3 - Carrageenan - 0.7 - 0.6 0.2 0.6 1.0 Whitening Agents and Drugs Dextranase (500,000 units / g) 0.1 0.2 1.0 2.0 5.0 - - Glucose oxidase (5,000 units / g) 0.2 0.5 0.5 3.0 0.2 - - Sodium pyrophosphate 2.0 0.5 - 1.5 3.0 1.5 - Potassium pyrophosphate - - 2.5 1.5 - 1.5 2.0 Sodium Pyrophosphate - 1.5 1.0 2.0 2.5 2.0 - Sodium tripolyphosphate - 0.5 - - 1.5 - - Hydroxyapatite 10.0 7.5 5.0 3.0 0.5 - 5.0 Sodium Fluoride 0.76 - 0.76 - 0.38 - 0.76 Hydrogen peroxide (30%) - - - - - 5.0 - Titanium dioxide - - - - - 1.0 - Papain - - - - - - 1.0 Sodium bicarbonate - - - - - 5.0 - additive Spices 1.0 1.0 1.0 1.0 1.0 1.0 1.0 Saccharin 0.1 0.1 0.1 0.1 0.1 0.1 0.1 Purified water 25.14 10.50 25.44 9.00 6.22 6.00 12.14

The manufacturing method is as follows.

1) The binder and other additives were previously dispersed in the humectant, and the abrasive and the whitening agent were added, followed by stirring for about 30 minutes.

2) Finally, a foaming agent and an enzyme component were added thereto, followed by stirring for 20 minutes in a vacuum state to obtain a final product.

Experimental Example 1: Evaluation of the whitening effect of the toothpaste composition

1) Evaluation test of whitening effect using human teeth

The stain removal effect of the dentifrice compositions according to Examples 1 to 5 and Comparative Examples 1 to 2 was evaluated by the following method. Tobacco, coffee, tea, sugar and calcium are mixed into a gel, which is then transferred to the bottom container of a motorized device for rotation, and tooth specimens extracted from healthy people in their 20s to 30s are epoxy resins. After the specimens were manufactured to have an exposed area of width × length = 2 mm × 2 mm by fixing to, the plates were attached to a rotating plate and operated for 3 days to force attachment.

At this time, an incandescent lamp was installed at the center of the rotating plate to dry the stains attached to the specimens, thereby promoting the adhesion of the stains. On the last day, remove the stained specimen and measure the whiteness using a color difference meter (Model: SZ, Nippon Denshoku). To rub against the specimen. At this time, each of the Example and Comparative Example composition on the tip of the bristles 0.5g equally put and operated for 30 minutes to reciprocate 180 times per minute, and then take out the specimen again using a colorimeter to improve the whiteness of the specimen After calculating the calculated as a percentage and the results are shown in Table 2 below.

division Example 1 Example 2 Example 3 Example 4 Example 5 Comparative Example 1 Comparative Example 2 Whiteness Improvement Rate (%) 85.6 83.2 87.7 93.8 90.2 67.5 76.0

As shown in Table 2, the toothpaste composition according to the present invention was evaluated to have a better whitening effect (increase in whiteness) than the composition of Comparative Example.

2) Whitening effect test through clinical trial

In order to see the more obvious whitening effect of the toothpaste composition according to the present invention, the whitening effect of the toothpaste composition of Examples 1 and 3 and Comparative Examples 1 and 2 was directly evaluated for two months.

Select 40 people who had relatively strong teeth, and measure the color tone of the incisoral cotton surface before starting the experiment by measuring the color tone using a Trubyte Bioform colorimeter in a room with constant lighting. Each grouping toothpaste composition was divided into 4 groups (10 people each), and the toothbrushing was performed as usual.

In order to confirm the increase of the brightness of teeth, 10 kinds of sensory identifications were easily selected among 24 standard standards of brightness of the Tourbite Bioform colorimeter, and each of them was evaluated from 1 to 10 points in order of increasing brightness. The score was added.

Prior to using the experimental toothpaste, the tooth brightness value of each group was evaluated to the first digit below the decimal point based on the above criteria, and the brightness value after the brushing for 2 months was evaluated, and then the increase rate of the average brightness value was calculated from the brightness value before the experiment. The results are shown in Table 3 below.

division Example 1 Example 4 Comparative Example 1 Comparative Example 2 Average brightness value (before experiment) 3.6 4.3 3.8 4.0 Average brightness value (after 2 months use) 6.9 7.3 4.8 6.0 % Increase in brightness 91.7 69.8 26.3 50.0

As can be seen from the results, the toothpaste composition according to the present invention when evaluated clinically was evaluated to have a better whitening effect (increase effect of brightness) than the composition of Comparative Example.

Experimental Example 2: Comparative evaluation of the stability of the toothpaste composition

The toothpaste compositions of Examples 1 to 5 and Comparative Examples 1 and 2 were stored at room temperature and 40 ° C., and the state stability of the toothpaste compositions was evaluated at regular intervals according to the following criteria. The results are shown in Table 4 below.

≪Evaluation Criteria≫

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

○ relatively good: only slightly rough surface or slightly poor tube entrance

▽ relatively poor: phase separation and slight discoloration

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

Time lapse Example Comparative example One 2 3 4 5 One 2 1 month Room temperature ◎ ◎ ◎ ◎ ◎ ◎ ○ 40 degrees ◎ ◎ ◎ ◎ ◎ ◎ ○ 3 months Room temperature ◎ ◎ ◎ ◎ ◎ ○ ▽ 40 degrees ○ ◎ ◎ ◎ ○ ○ ▽ 6 months Room temperature ◎ ◎ ◎ ◎ ◎ ○ ▽ 40 degrees ▽ ○ ○ ▽ ▽ ▽ × 12 months Room temperature ○ ○ ○ ○ ○ ▽ × 40 degrees ▽ ▽ ▽ ▽ × × ×

As shown in the above results, the toothpaste composition according to the present invention may be advantageous in terms of commercial value because it is superior in aging stability than the toothpaste composition containing peroxide as a conventional whitening agent and papain, which is a vegetable enzyme, and the like. It became more severe as time passed.

Experimental Example 3: Effect experiment on the oral hygiene of the toothpaste composition

In addition to tooth whitening function, the toothpaste composition according to the present invention has the effect of degrading plaque by biochemical enzymatic action, depressing tartar formation by soluble condensate phosphate, and relieving hypersensitivity by hydroxyapatite. It was confirmed through experiments and clinical experiments.

1) Plasma decomposition effect experiment by laboratory experiment

10 ml of Heart Infusion medium inoculated with Streptococcus mutanz bacteria were incubated anaerobicly (95% nitrogen, 5% carbon dioxide) for 24 hours at 37 ° C, and then the medium solution was removed. The solution was diluted with 1% aqueous solution, 10 ml of the diluted solution was added to the medium, and left at 37 ° C. for 10 hours. The amount of prag in the medium without adding a sample was measured and used as a control test. At this time, the amount of plaque decomposition was expressed as follows using the amount of plaque (Yo) of the control test and the amount of plaque (Y) remaining in the test tube wall for each sample. The results are shown in Table 5 below. Indicated.

Plaque Degradation Amount (mg) = Yo-Y

division Example Comparative example One 2 3 4 5 One 2 Plaque decomposition amount (mg) 23.5 42.1 57.4 63.3 67.4 10.1 1.4

As shown in Table 5, the degree of decomposition of the plaque was increased in proportion to the content of dextranase in the composition, and the degree of decomposition was weak in more than 1% of the liquid. The composition of Comparative Example showed a small amount of decomposition of plaque, and in Comparative Example 1, it was determined that the bactericidal action of hydrogen peroxide contained inhibited the growth of Streptococcus mutanz bacteria.

2) Clinical evaluation of tartar formation inhibitory effect and alleviation of perceptual hypersensitivity

In order to clinically confirm the inhibitory effect of tartar formation and alleviation of perceptual hypersensitivity of the composition, 60 men and women aged 20 to 40 years old who have a lot of tartar and feel perceptual hypersensitivity to food and the like were divided in half. After the scale for all the personnel was used as a commercially available simple fluoride toothpaste for 1 week, at this time, after recording the tartar index, the plague index and the perceptual hypersensitivity by the electric dimensional tester of Example 1 and Comparative Example 1 After providing the composition, training the same oral hygiene management method, and using it for 3 months, assessing the perceptual hypersensitivity by calculus index, prag index and electric dimensional tester, and evaluating the index value before and after 3 months By comparing the index values, the degree of increase or decrease is expressed as the inhibition rate and the relaxation rate. The results are shown in Table 6 below.

Example 4 Comparative Example 1 Tartar formation inhibition rate (%) 50.5 11.3 % Of plaque formation inhibition 43.6 23.6 Perceptual hypersensitivity relief rate (%) 56.3 3.1

The group using the composition of Example 4 was analyzed and evaluated to be statistically significantly more effective than the group using the composition of Comparative Example 1 in the plaque formation inhibitory effect, plaque formation inhibitory effect, and hypersensitivity relieving effect (P <0.01).

In addition to tooth whitening, the toothpaste composition according to the present invention has the effect of degrading plaque by biochemical enzyme action, inhibiting tartar formation by soluble condensate phosphate, and relieving hypersensitivity by hydroxyapatite. Therefore, the toothpaste composition of the present invention is not simply a cosmetic toothpaste of a whitening function, but can fundamentally remove the causative agent of all diseases in the oral cavity to simultaneously treat and alleviate tooth decay and gum disease, which are two major oral diseases.

Claims (4)

Toothpaste composition with safe and aesthetic function to human body containing dextranase or glucanase and glucose oxidase and at the same time containing water-soluble condensate phosphate and hydroxyapatite represented by the following formula: [Formula 1] M _{n + 2} P _n O _{3n + 1} Wherein M is sodium or potassium and n is an integer of at least 2. The method of claim 1, wherein the condensed phosphate is selected from one or two or more selected from sodium pyrophosphate, potassium pyrophosphate, acidic pyrophosphate, and sodium tripolyphosphate or potassium salt, the content of which is 0.5 to 7 relative to the entire toothpaste composition. Toothpaste composition by weight. The dentifrice composition of Claim 1 containing 0.1-10 weight% of hydroxyapatite with respect to the whole dentifrice composition. The method of claim 1, wherein the abrasive used in the dentifrice composition 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 methphosphate. And 5 to 60% by weight of one or more of aluminum silicate.