KR20050046050A - Liquid-crystal tooth whitener - Google Patents

Abstract

The present invention relates to a liquid crystalline tooth whitening agent, which is applied to a tooth to obtain a tooth whitening effect, wherein the liquid crystalline tooth whitening agent of the present invention comprises glycerol monooleate, a polymer, a peroxide and a solvent. It is prepared by adding glycerol monooleate and optionally glycerol trioleate to make a basic medicine, and adding high molecular compound for the purpose of shape or adhesion control, and has the property of easy fluidity before application, and saliva after application The solidified by the moisture of the attached, fixed, and after being applied to the teeth, the peroxides such as hydrogen peroxide, sodium percarbonate, etc. for the tooth whitening may be released in a sustained release.

Description

Liquid crystalline tooth whitening agent {LIQUID-CRYSTAL TOOTH WHITENER}

The present invention relates to a liquid crystalline tooth whitening agent, which is easy to apply as a liquid when applied to the teeth, when the inflow of water such as oral saliva increases the viscosity of the formulation can be attached and fixed to the teeth, whitening while attached to the teeth Efficacy materials are associated with formulations that release slowly to the tooth surface to exert a tooth whitening effect.

The three major functions of the oral cavity in the human body include chewing function, pronunciation function, and aesthetic function. Oral health can be defined as the state of the oral tissues in which these three functions are properly exercised, and not only physical health but also obstacles to social activities and mental functions.

Oral health is mainly destroyed by oral diseases such as dental caries and periodontal tissue disease, but oral function may be impaired even without a specific oral disease, such as loss of cosmetic function due to pigmentation can be representative. That is, when teeth are colored by non-oral coloration factors, such as drugs, beverages such as coffee, diet and cosmetics, the cosmetic function of the teeth may be lost, which may cause social activities and mental disorders. In order to solve such mental disorders due to loss of beauty function, various domestic and foreign studies, such as blending a cosmetic effect material with toothpaste, coating agent, adhesive, etc. have been made.

As a result of this research, tooth whitening has been conventionally performed by using a rubber dam or a tray made in the shape of a tooth in order to secure sufficient reaction time between the gel and the tooth containing the whitening component. However, whether in professional dental whitening programs or in home or OTC programs, the repeated handling, cleaning, filling, installation, and wearing of rubber dams or trays inevitably leads to damage to oral soft tissues and loss of gel into the stomach. Occurred.

Recently, new formulations for overcoming such problems have been introduced or have been disclosed and disclosed as patents, and Korean Patent Application Nos. 1999-7011451 and 2001-7011679 are representative of them. Here, we present a formulation with a peroxide-containing gel on a polyethylene strip without the use of a rubber dam or tray, which can allow the peroxide to contact the teeth for a long time and is not intense when wearing a tooth whitening strip. It also presents the advantage that it is possible.

These formulations improve the feeling of use by attaching a peroxide-containing gel layer to the teeth on the strip, but the whitening component does not reach efficiently between the interdental, ie between teeth, as well as relatively less whitening efficacy. However, when saliva is introduced, there is a problem that the strip can easily fall due to movement of the tongue or lips. In addition, in these formulations, the strip form is fixed and not deformable, so that the efficiency is inferior or cumbersome when the whitening effect is selectively obtained for a specific desired tooth.

Liquid tooth whitening agent is present in order to improve the above disadvantages, but products sold in most liquid formulations tend to be easily diluted and lost by saliva after being applied to the teeth, and the effect thereof is insignificant.

In addition, US Patent No. 6,589,512 discloses a tooth whitening agent prepared in a semi-solid formulation using an organosiloxane resin. This formulation has fluidity without dilution or loss by saliva, which enables whitening between teeth and is designed to release the whitening component in a sustained release because it can be attached for a long time. However, when the organosiloxane resin is to be applied to the teeth, it is necessary to disperse the resin using an organic solvent having a high volatility in order to control fluidity, and when the organic solvent is volatilized, it becomes difficult to apply the formulation. In addition, when the organic solvent is excessively used, an irritating odor is induced, and there is an inconvenience of exposing the tooth until it is dried after the application.

The present invention is to solve various problems in the conventional tooth whitening formulation, and to develop a tooth whitening formulation having suitable properties that can be applied to the teeth to achieve the tooth whitening effect. In other words, it is a formulation that compensates for the shortcomings of the conventional strip form and organosiloxane resin formulation, and can be easily applied to a desired area in the oral cavity, and the applied drug is adhered to and fixed to the teeth to be released for a long time. It is an object of the present invention to provide.

In order to achieve the above object, the present invention provides a liquid crystalline tooth whitening agent comprising a glycerol monooleate, a polymer, a peroxide, and a solvent as a composition which is applied to a tooth to obtain a tooth whitening effect.

The tooth whitening agent according to the present invention is intended to complete a new type of tooth whitening system that can be easily applied when applying a medicament to a tooth to deliver a tooth whitening efficacy material to the tooth surface, and is easily fixed after being applied to the tooth. It is.

In order to achieve this object, in the present invention, glycerol monooleate was used as a basic medicine. In the case of glycerol monooleate, as is known, liquid crystals are formed depending on the temperature and the content of water, and their form and physical properties are different depending on their environment. In other words, in the phase change of the surfactant or the like, the lamellar phase, the reverse micelle phase, and the reverse phase hexagonal phase have fluidity and are easily applied or applied to the surface of the tooth, but the change of temperature and moisture As the content of is increased, the structure is solidified while changing into a cubic phase, and fluidity is lost. The present invention has developed such a change in the physical properties of the liquid crystal into the formulation. In addition, in the formulation of the present invention, while the drug is attached to the tooth, the substance having a whitening effect is gradually released to the surface of the tooth, and the viscosity increases after being absorbed by saliva, etc., thereby controlling the time for which the whitening component is in contact with the tooth. It was made possible.

That is, in the tooth whitening agent according to the present invention, glycerol monooleate was used as a basic drug, and the change in the cubic phase from the phase of the liquid crystal was induced and fixed to the tooth by the intraoral conditions. Specifically, the glycerol monooleate basic drug is solidified and the viscosity is increased by the body temperature in the oral cavity and the inflow of water such as oral saliva so that the drug applied to the tooth is attached and fixed. That is, when applied to the teeth, the fluidity is appropriate, so that it is easy to apply to the teeth, and after being applied to the teeth, the viscosity rises quickly by the inflow of saliva, so that it is fixed to the teeth and adheres well. It is not easily diluted or lost. It is also possible to optionally add glycerol trioleate.

In the liquid crystalline tooth whitening agent according to the present invention, glycerol monooleate may be added in the formulation in an amount of about 5 to 95%, and preferably in an amount of 30 to 90% in order to form the formulation.

Here, in order to effectively change the physical properties of the liquid crystalline tooth whitening agent, in particular, the viscosity change before and after tooth application, an appropriate amount of an organic solvent such as water or alcohol is required. That is, by adjusting the content of water or alcohol in the basic medicine it is possible to control the rate at which the viscosity rises.

In particular, in the tooth whitening agent of the present invention, when the fluorine component, phosphate, or the like is to be applied in the formulation, the moisture content may be easily adjusted to formulate it. The amount of water or alcohol used in the liquid crystal tooth whitening agent of the present invention is in the range of about 1 to 50%, preferably 2 to 20%.

In addition, in the liquid crystalline tooth whitening agent of the present invention, a polymer compound, that is, a polymer may be added to control the physical properties of the glycerol monooleate base agent. For example, the physical properties of the formulation can be changed by adding a polymer having excellent tooth adhesion, or by adding a polymer that exhibits different behavior with changes in temperature. In particular, even a small amount of the polymer compound is important because it can change the physical properties of the formulation. In addition, since the water content required for change in fluidity or solidification varies depending on the amount of the polymer compound added, the polymer used therein becomes important. In the liquid crystalline tooth whitening agent of the present invention, the polymer compound may be used in the range of 0.1 to 30%, and in order to maintain the formulation, it is preferably used in the range of 1 to 10%.

The polymers that can be used in the liquid crystalline tooth whitening agent of the present invention are as follows: Polyvinyl alcohol, poloxamer, polyvinyl pyrrolidone, polyvinyl pyrrole as nonionic polymers Don-vinyl acetate copolymer (polyvinyl pyrrolidone / vinyl acetate copolymer), hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropylethyl cellulose Anionic polymers, such as hydroxypropylethyl cellulose and polyox, are polymers of carboxymethyl cellulose, carboxypropyl cellulose and its salts, xanthan gum, and carrageenan gum ), Alginate gum, and other polymers, such as karayan gum, Arabic gum and salt derivatives thereof, and gelatin, synthetic polymers as polyacrylic acid, carbopol, polyquaternium-11, polyquaternium-39 polyquaternium-39) A polyalkyl vinyl ether-maleic acid copolymer (PVM / MA copolymer: Gantrez AN 119, AN 139, S-97) and the like, or a mixture of two or more thereof.

In the liquid crystalline tooth whitening agent according to the present invention, the tooth whitening component is hydrogen peroxide, percarbonate as percarbonate, percarbonate, and urea peroxide, pyrophosphate sodium phosphate, and polymers such as polyvinylpyrrolidone-hydrogen peroxide complex, and inorganic metal Examples of the solid peroxide salt include calcium peroxide (CaO ₂ ), barium peroxide (BaO ₂ ), magnesium peroxide (MgO ₂ ), sodium peroxide (Na ₂ O ₂ ), potassium peroxide (Ka ₂ O ₂ ), and the like. It is not limited only. These whitening agent components may be used alone or in combination of two or more to achieve superior effects. In the liquid crystalline tooth whitening agent according to the present invention, the tooth whitening component may be added at a concentration of 0.5 to 50%, preferably 0.75 to 30% of the composition. If the above peroxide is solid or powder, it can be made more uniform by dissolving or dispersing in water in advance.

While the liquid crystalline tooth whitening agent according to the present invention is advantageous in peroxide stability, it is preferable to set the pH to be suitable for oral care products, especially the tooth whitening agent, so that a stabilizer having a pH adjusting function can be added. These stabilizers are materials having a pH control function that can suppress pH changes during storage and keep them from irritating the oral cavity, and metal-complex agents having excellent compatibility with peroxides can be used. The stabilizers with good peroxide compatibility are polyphosphates, sodium pyrophosphate (TSPP), sodium pyrophosphate (SAPP), sodium hexametaphosphate (SHMP), and polyphosphate. Sodium tripolyphosphate (STP), sodium potassium tripolyphosphate (SKTP), potassium pyrophosphate (TKPP), ultraic phosphate (acidic sodium meta-polyphosphate), acidic sodium polyphosphate Or as a metal-chelating agent, ethylenediaminetetraacetate, aminotrimethylenephosphate and salts thereof, hydroxyethylenediphosphonate and salts thereof, ethylenediaminetetramethylenephosphonate and salts thereof, diethylenetriaminepentamethylenephosphonate and One or two or more kinds thereof may be used. It is preferable to use these stabilizers in ratio of 100: 1-1:10 with respect to a peroxide. In particular, condensed phosphates are known to be effective in inhibiting tartar formation and removing tartar, and therefore, it is thought that they can contribute to the improvement of the whitening effect. In fact, it can be seen that the surface of the teeth or between the teeth are clean if they contain them.

In addition to the above-mentioned components, the liquid crystal tooth whitening agent according to the present invention is added to the fragrance, bleach activator or dental caries suppressor, gum disease improving agent, without changing the shape maintenance and peroxide stability of the formulation It can be improved. The fragrance is typically peppermint, sparemint, menthol, citrus, herb, etc. Bleach activators include titanium oxide, transition metal complex, TAED (tetraacetyl ethylene diamine), and dental caries inhibitors such as sodium fluoride (NaF) and calcium fluoride ( CaF ₂ ) such as gum disease improver, bamboo salt, tocopherol acetate, vitamin D, allantoin chlorohydroxy aluminum, trilosan, xylitol, calcium glycerol phosphate, aminocaproic acid, tronicamine, KNO ₃ , monofluorophosphate, enzymes and the like can be used.

The use of the ingredients mentioned above completes the tooth whitening delivery system of the new formulation with improved usability and endowed with additional functionality.

The features of the tooth whitening agent according to the invention are summarized as follows:

Firstly, when the medicament is applied to the tooth to deliver the tooth whitening efficacy material to the tooth surface, it is attached to and fixed to the tooth. In other words, the viscosity of the drug is increased as the water, such as oral saliva is to be attached and fixed to the teeth. In the process of applying to the teeth, the fluidity is appropriate, so it is convenient to apply to the teeth. Accordingly, the whitening component is easily transferred between the teeth, that is, between the teeth, and after being applied to the teeth, the viscosity rises rapidly due to the inflow of saliva to the teeth. By fixing and adhering well, it can be prevented from being easily diluted or lost in oral conditions.

Secondly, while the medicament is attached to the tooth, a substance having a whitening effect is slowly released to the tooth surface. That is, after the viscosity of the saliva, etc. is introduced into the teeth as the viscosity increases, the tooth whitening ingredient inside the medicament is gradually released while attached to the tooth, thereby controlling the time for which the whitening ingredient is in contact with the tooth. Done.

Hereinafter, the present invention will be described in more detail with reference to preferred embodiments of the present invention. However, these Examples are only illustrative to aid the understanding of the present invention, and the scope of the present invention is not limited only to these examples.

Example 1

Hydrogen peroxide 6%

Glycerol Monooleate 77%

Poloxamer 5%

Sodium Pyrophosphate 3%

Flavor 0.5%

Purified Water 8%

Ethanol 0.5%

The remaining components were mixed while glycerol monooleate was liquefied at about 50 ° C., followed by homogenization of purified water and ethanol to prepare a liquid crystalline tooth whitening agent according to the present invention.

Example 2

20% sodium percarbonate

Glycerol Monooleate 67%

Glycerol Trioleate 5%

Polyvinylpyrrolidone 2%

Sodium Pyrophosphate 2%

Triclosan 0.1%

Sodium fluoride 2%

Purified water 2%

While glycerol monooleate was liquefied at about 50 ° C., the remaining components except for acidic pyrophosphate were mixed, and then purified water and ethanol were added at the end to homogenize to prepare a liquid crystalline tooth whitening agent according to the present invention.

Example 3

Urea Peroxide 20%

Glycerol Monooleate 70%

Hydroxypropyl 4%

Sodium pyrophosphate 2%

0.5% fragrance

Titanium Oxide 0.1%

Purified water 3%

Ethanol 0.4%

Comparative Example 1

Dental layer gel: Carbopol 12%, hydrogen peroxide 4.5%, acidic pyrophosphate 0.48%, glycerin 80%, purified water 100%

Backing layer: polyethylene strip

Strip form preparations of the above form

Comparative Example 2

Organosiloxane Resin 25%

Silicone gum 4.2%

Ethyl Acetate, Propyl Acetate Mixture 17%

Benton Clay 1%

Sodium percarbonate 17%

Semi-solid preparations using organosiloxane resins with the above

Effect Experimental Example 1 Viscosity Change Measurement

For the formulation prepared in Example 1, the viscosity change before and after the water inflow was measured by RVT method using a Brookfield Viscometer. The results are shown in Table 1 below.

Example 1 Viscosity (cps) Before water inflow 5000-11000 After water inflow (100% purified water compared to formulation) 70000 ~ 90000

As shown in Table 1, the formulation according to the present invention can be confirmed that the viscosity is increased by the inflow of moisture and cured.

Effect Experimental Example 2 Release Test

After the buffer was prepared using phosphate, the release test was carried out according to the release test in the US Pharmacopoeia. That is, the release test was carried out for the formulations of Example 2 and Comparative Example 1, respectively, with 500 ml buffer maintained at 35 ° C. and the paddle rotated at 25 rpm. Hydrogen peroxide in the buffer was measured and the release rate was calculated for each formulation. The results are shown in Table 2 below.

Measuring time 5 minutes 30 minutes 1 hours Example 2 30 ± 10% 50 ± 20% 70 ± 20% Comparative Example 1 80 ± 10% 100% 100%

As shown in Table 2, the formulation of the Example can be seen that the release rate is significantly lower compared to the formulation of the comparative example.

Effect Experimental Example 3 Usability Test

Samples of the formulations of Example 3 and Comparative Example 2 were distributed to 30 healthy adults in their 20s to 40s and scored for ease of use such as application and taste (rated out of 5). The results are shown in Table 3 below.

Example 3 (n = 30) Comparative Example 2 (n = 30) Ease of use 4.1 3.3

As shown in the results of Table 3, when the evaluation of the ease of use between the two groups statistically it can be seen that the formulation of the Example is excellent in terms of feeling (p <0.01).

As described above, the liquid crystalline tooth whitening agent of the present invention is prepared by adding glycerol monooleate, optionally glycerol trioleate, as a basic medicine, and adding a high molecular compound for the purpose of shape or adhesion control, before application. It has the property of fluidity and is easy to apply, and after being applied, it is solidified by water such as saliva and attached and fixed.After being applied to teeth, peroxides such as hydrogen peroxide and sodium percarbonate, which are teeth whitening components, can be released in a sustained release manner. have.

Claims (12)

A composition for applying a tooth whitening effect to a tooth, wherein the composition comprises a glycerol monooleate, a polymer, a peroxide, and a solvent. The method of claim 1, wherein the polymer is polyvinyl alcohol, poloxamer, polyvinyl pyrrolidone, polyvinylpyrrolidone-vinylacetate copolymer (polyvinyl pyrrolidone / vinyl acetate copolymer). ), Hydroxypropyl cellulose, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropylethyl cellulose, polyox, carboxymethyl cellulose (carboxymethyl cellulose, polymers of carboxypropyl cellulose and salts thereof, xanthan gum, carrageenan gum, alginate gum, Karayan gum, Arabian gum (arabic gum) and salt derivatives thereof, gelatin, polyacrylic acid, carbopol, polyquater Titanium -11 (polyquaternium-11), Polyquaternium nium -39 (polyquaternium-39), poly alkyl vinyl ether-maleic acid copolymer (PVM / MA copolymer) or a tooth whitening agent, characterized in that a mixture thereof. The method of claim 1, wherein the peroxide is hydrogen peroxide, percarbonate, perborate, urea peroxide, sodium pyrophosphate, polyvinylpyrrolidone-hydrogen peroxide complex, calcium peroxide (CaO ₂ ), barium peroxide (BaO ₂ ), magnesium peroxide (MgO ₂ ), sodium peroxide (Na ₂ O ₂ ), potassium peroxide (Ka ₂ O ₂ ), or a mixture thereof. A tooth whitening agent according to claim 1, wherein the amount of glycerol monooleate is 5 to 95% of the total composition. A tooth whitening agent according to claim 4, wherein the amount of glycerol monooleate is 30 to 90% of the total composition. A tooth whitening agent according to claim 1, wherein the solvent is water or an alcohol and 1 to 50% of the total composition. 7. A tooth whitening agent according to claim 6, wherein the solvent is 2 to 20% of the total composition. A tooth whitening agent according to claim 1, wherein the amount of polymer is 0.1 to 30% of the total composition. 9. A tooth whitening agent according to claim 8, wherein the amount of polymer is 1 to 10% of the total composition. A composition for applying a tooth whitening effect to a tooth, wherein the tooth whitening agent comprises glycerol monooleate, a polymer, a peroxide, a peroxide stabilizer, and a solvent. The method of claim 10, wherein the peroxide stabilizer has a pH control function, sodium pyrophosphate (TSPP), sodium pyrophosphate (SAPP), sodium hexametaphosphate (SHMP), poly Sodium tripolyphosphate (STP), sodium potassium tripolyphosphate (SKTP), potassium pyrophosphate (TKPP), ultraic phosphate (acidic sodium meta-polyphosphate), acidic sodium polyphosphate ), Ethylenediaminetetraacetate, aminotrimethylenephosphate and salts thereof, hydroxyethylenediphosphonate and salts thereof, ethylenediaminetetramethylenephosphonate and salts thereof, diethylenetriaminepentamethylenephosphonate and salts thereof, or A tooth whitening agent, characterized in that a mixture thereof. 12. The tooth whitening agent of claim 11, wherein the peroxide stabilizer is included in a ratio of 100: 1 to 1:10 relative to the peroxide.