KR102275877B1 - Removable tooth-attached patch by brushing - Google Patents

Abstract

The present invention relates to a tooth attachment patch, comprising: a drug layer that delivers a drug to the tooth; and a support layer that is located opposite to the tooth attachment surface of the drug layer, and contains a water-soluble polymer and a water-insoluble polymer at the same time. The patch of the present invention can be easily removed only by brushing without removing the supporting layer.

Description

Removable tooth-attached patch by brushing

The present invention relates to a tooth attachment patch that can be removed by brushing, and more particularly, to a tooth attachment patch that can be simply removed by brushing without removing the support layer supporting the drug layer.

Treatments such as teeth whitening have been mainly performed in dentistry in the past, but since dental procedures are cumbersome and expensive in terms of cost, there have been many developments of products that can be used conveniently in recent years.

There are products such as toothpaste, mouthrinse, chewing gum, oral tray, tooth application gel, and oral patch as options for teeth whitening, but in terms of ease of use, patch-type products are the most used. is becoming

A tooth attachment patch generally includes a drug layer containing a drug for its intended use, such as a drug for teeth whitening, a drug for preventing or improving sore throat, and a support layer to allow the drug component to be selectively delivered to the tooth. have

Patent Registration 10-0458337 proposes to make the support layer insoluble in water so that the drug component contained in the patch can be selectively delivered only to the teeth. However, the patch including such a water-insoluble support layer is inconvenient to remove the remaining support layer after using the product. On the other hand, when removing only by brushing without a peeling process, the non-decomposable film mass was agglomerated on the toothbrush, which caused a difficult situation to remove from the toothbrush. As an improved product, a product that dissolves in the oral cavity after attaching a patch was developed, but there was a problem that the drug component was not selectively delivered to the teeth and mixed with saliva so that the intended drug effect was not expressed.

Accordingly, the present invention solves the above problems, and provides a patch for attaching teeth, which can be easily removed from the tooth surface only by brushing, and the film mass that does not decompose does not stick between the toothbrushes.

The present invention provides a simple tooth attachment patch that can be removed simply by brushing without generating a separate waste after use.

In order to solve the above problems, the present invention provides a support layer for a tooth attachment patch that serves to allow the drug of the drug layer to selectively move only to the tooth surface in the tooth or tooth peripheral attachment patch, and to maintain the shape of the patch uniformly. The present invention was completed after discovering that the water-soluble polymer and the water-insoluble polymer can be easily decomposed and removed only by pressure such as brushing after use by simultaneously including the water-soluble polymer and the water-insoluble polymer.

Drug delivery systems of most patch formulations, particularly patches for attaching teeth, have a support layer to enable specific delivery of drugs to a target site. A polymer that does not dissolve in water or saliva is used to maintain its shape even if it is attached to the tooth. In addition, when the active ingredient is eluted when attached to the tooth and delivered to the tooth, dissolution is possible only in the tooth direction. That is, in order to selectively deliver the drug in the direction of the tooth, and prevent the drug from being diluted with saliva or water, it was common to be prepared in a water-impermeable or water-insoluble form.

This water impermeable or water insoluble backing layer had to be removed from the tooth surface after application of the patch and discarded.

After use, after removing the support layer, you need to brush your teeth to remove the residue remaining on the tooth surface. The inventors of the present invention are looking for a way to deliver drugs to the tooth surface and achieve a perfect finish with only brushing without removing the support layer. As a result, the present invention was completed.

That is, the drug support layer, which has been produced and used only in water-insoluble in the industry, has come to be produced in a form that can be dissolved by saliva.

Specifically, the inventors of the present invention provide a tooth or tooth peripheral attachment patch comprising a drug layer that delivers a drug to the tooth, and a support layer that is located on the opposite side of the tooth attachment surface of the drug layer, and contains a water-soluble polymer and a water-insoluble polymer at the same time do.

The drug layer may include a drug delivered to the tooth. The drug may preferably be delivered to the tooth surface, and examples of the drug include a tooth whitening component, a component for preventing or improving sore throat, a component for preventing or improving periodontal disease such as periodontitis and gingivitis, or a component for preventing caries can do.

Examples of the tooth whitening component include peroxides, polyphosphates, enzymes, and chlorine-based bleach. Peroxide is hydrogen peroxide, carbamide peroxide, calcium peroxide, sodium percarbonate, sodium perborate, tetrasodiumpyrophosphate peroxidate, and mixtures thereof. It can be used by selecting from the group consisting of. Phosphates and enzymes are effective in removing major stains contained in the enamel adhesion layer. As polyphosphate, for example, sodium pyrophosphate (tetrasodium pyrophosphate, TSPP), acid sodium pyrophosphate (SAPP), sodium metaphosphate (sodium hexametaphosphate, SHMP), sodium polyphosphate (sodium tripolyphosphate, STP), One or two of sodium potassium tripolyphosphate (SKTP), tetrapotassium pyrophosphate (TKPP), and ultra phosphates, acidic sodium meta-polyphosphate and acidic sodium polyphosphate More than one species can be used. In general, polyphosphate is known as a tartar control agent in toothpaste to inhibit calculus formation or to remove tartar. In addition, these are good metal chelating agents, which can effectively remove tooth stains generated by metals such as iron, calcium, and magnesium in food or work environment among tooth stains, thereby contributing to the improvement of the whitening effect. When these polyphosphates are used in the formulation according to the present invention, it is effective not only to improve the whitening effect by removing light extrinsic stains, but also to extend the contact time between the teeth and the condensed phosphate to inhibit the formation of calculus or remove calculus. is expected to Chlorine-based whitening agents include sodium chlorite and sodium hypochlorite. In addition, papain, vitamin E and sodium bicarbonate can also be used as whitening agents.

In another embodiment, strontium chloride, calcium carbonate, sodium citrate, sodium fluoride, silica, hydroxyapatite, potassium nitrate, potassium phosphate, and the like may be used as a component for preventing or improving tooth decay or tooth decay.

In another embodiment, the active ingredient may include a component for preventing periodontal disease, and periodontal disease clinically refers to tooth loss due to periodontitis, gingivitis and bleeding, formation of periodontal pockets and destruction of alveolar bone. In order to prevent the occurrence of periodontal disease, the drug layer is bamboo salt, corn saponification quantitative extract, polycrezulene, tetracycline, chlorhexidine gluconate, cetylpyridium chloride ), Sanguinarine and Triclosan, and the like, such as peppermint, centella asiatica, chamomile, ratania, myrrh, sagebrush, horseradish, green tea, licorice, gold, pogongyeong, gold and silver coins, etc. It may also contain herbal extracts.

The drug layer has no adhesive strength or weak strength in the dry state, but is hydrated by a small amount of water in the area where the whitening agent wants to act. However, it can be used in a gel state that can be attached to teeth due to its own viscosity. The polymer used herein must be hydrophilic or at least partially hydrophilic. Polyalkyl vinyl ether-maleic acid copolymer (PVM/MA copolymer; Gantrez AN 119, AN 139, S-97), polyvinyl alcohol, polyacrylic acid, poloxamer 407 (Poloxamer 407; Pluronic, poly( ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymer), polyethylene oxide (Polyox), polyvinylpyrrolidone-vinyl acetate copolymer (PVP/VA copolymer; Luviskol VA, Plasdone S PVP/VA) , polyvinylpyrrolidone (PVP; K-15~K-120), polyquaternium-11 (polyquaternium-11, Gafquat 755N), polyquaternium-39 (polyquaternium-39, Merquat plus 3330), carboxypolymethylene (Carbomer, Carbopol), hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, gelatin, sodium alginate alone or a mixture thereof may be used. As a solvent for these polymers, mainly water, ethanol alone or a mixture thereof, and other organic solvents such as ethyl acetate, methylene chloride, isopropyl alcohol, acetonitrile alone or mixtures thereof may be used in a controlled ratio. .

The tooth attachment must be flexible enough because it must be attached directly to the tooth and can be easily shaped according to the curvature of the tooth. Since some polymers have poor flexibility, an appropriate plasticizer may be added. Suitable plasticizers are polypropylene glycol, glycerin, or polyethylene glycol, which are generally used although there are differences depending on the type of polymer and its formulation, and all of them may be used.

In addition, it is also possible to add a chelating agent such as EDTA or sodium citrate to the drug layer for the purpose of improving the temporal stability of the peroxide.

As used herein, the term “drug layer” refers to a layer containing an active ingredient capable of achieving the purpose of a tooth attachment patch. For example, a tooth whitening patch means a layer containing a tooth whitening component (preferably hydrogen peroxide, sodium peroxide, etc.), and an anti-shrink patch means a layer containing potassium nitrate, potassium chloride, etc. do.

The support layer used to protect the drug layer from physical and chemical contact such as saliva and oral contact, or to maintain the shape of the product, it is generally preferable to use a water-insoluble polymer in order to perform the role of the support layer, and the support layer It has been recognized in the industry as being removed after use. However, the inventors of the present invention have devised a method for easily removing and using the support layer by simply brushing, without removing the water-soluble polymer in the support layer, contrary to common sense in the industry.

As used herein, "support layer" means a layer that serves to prevent contact with other skin in the oral cavity other than teeth.

In one embodiment of the present invention, the support layer may include a water-insoluble polymer generally used for oral film, for example, cellulose acetate phthalate, shellac, polyvinyl acetate, ethyl cellulose, polymethylmethacrylic Late, methacryloyl ethyl betaine/methacrylate copolymer (Yukaformer: manufactured by Mitsubishi, methacryloylethyl betain/ methacrylate copolymer), methacrylic acid copolymer; Eudragit L 100, Eudragit L 12,5, Eudragit L 100-55, Eudragit L 30D-55), an aminoalkyl methacrylate copolymer (Eudragit E 100, Eudragit E 12,5, Eudragit RL 100, Eudragit RL 30D) may be used. In addition, the support layer of the tooth or tooth periphery attachment patch of the present invention includes a water-soluble polymer. As used herein, a water-soluble polymer refers to a polymer that can be dissolved in water, swelled, or dispersed into small particles. The hydrophilic polymer may also be used in the same sense as the water-soluble polymer of the present invention.

The water-soluble polymer may include a water-soluble polymer that can be used in the drug layer, polyalkylvinyl ether-maleic acid copolymer (PVM/MA copolymer; Gantrez AN 119, AN 139, S-97), polyvinyl alcohol, polyacrylic acid , Poloxamer 407; Pluronic, poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) triblock copolymer), polyethylene oxide (Polyox), polyvinylpyrrolidone-vinyl acetate copolymer (PVP/ VA copolymer; Luviskol VA, Plasdone S PVP/VA), polyvinylpyrrolidone (PVP; K-15~K-120), polyquaternium-11 (polyquaternium-11, Gafquat 755N), polyquaternium-39 ( polyquaternium-39, Merquat plus 3330), carboxypolymethylene (Carbomer, Carbopol), hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, gelatin, alginic acid (sodium alginate), etc. may be used. , preferably hydroxypropylmethyl cellulose, polyvinylpyrrolidone, or a mixture thereof.

According to an embodiment of the present invention, the content of the water-soluble polymer and the water-insoluble polymer included in the support layer may be in a weight ratio of the water-soluble polymer: the water-insoluble polymer included in the support layer: 1:4 to 4:1, preferably 1.5:4 to 3.5: may be included in a weight ratio of 4.

When the water-soluble polymer and the water-insoluble polymer have the same weight ratio as described above, the patch may be well decomposed when removed after use while stably maintaining the structure of the patch.

The support layer can be used by adding various plasticizers for the same reason as the drug layer. In addition to the above-mentioned plasticizers propylene glycol, glycerin, and polyethylene glycol, more types of plasticizers can be used depending on the solvent used, and castor oil and hydrogenated castor oil can also be used.

As the solvent, mainly water, ethanol alone or a mixture thereof, and other organic solvents such as ethyl acetate, methylene chloride, isopropyl alcohol, acetonitrile alone or a mixture thereof may be used in a controlled ratio.

In addition to the drug layer and the support layer, the patch for attachment to the tooth or the tooth periphery of the present invention may optionally include an additional layer between the drug layer and the support layer or at the outside of each according to the purpose.

According to an embodiment of the present invention, the patch for attaching to a tooth or a tooth periphery of the present invention can be easily removed from the tooth only by brushing, without separately removing the support layer after use.

The patch according to an embodiment of the present invention was brushed for 3 minutes per minute at a load of 250 g and washed with distilled water while collecting the washing solution. As a result, after filtering through a mesh having a sieve size of 1 mm, the weight checked by drying the residue is the total weight less than 2% by weight. The tooth attachment patch of the present invention can be easily removed only by brushing after use.

The patch comprising the drug layer and the support layer of the present invention can be used by attaching to the tooth. In another embodiment, the patch may be used by being attached to the tooth and tissue surrounding the tooth according to the purpose of use. As used herein, the term “peripheral or surrounding tissue” may include both the portion of the gum in contact with the tooth and the portion of the oral cavity that may be in contact with the toothbrush during brushing even if it is somewhat distant from the tooth.

The term "decomposition" means that one large piece is divided or split into smaller pieces. The decomposed pieces of the present invention may have a certain size, but may be divided into various sizes according to external force or pressure. If the word has the meaning of being split into several parts, it may be included in the scope of decomposition and identity of the present invention.

As used herein, the term "patch" refers to an adhesive formulation containing a specific component, and the form or structure of the patch is not particularly limited.

In addition, the tooth attachment patch according to the present invention may be manufactured according to the methods described in Korean Patent No. 10-0816250, US Patent No. 6,689,344, 6,682,721, 6,780,401, and the like.

The tooth attachment patch of the present invention is a tooth attachment patch of a convenient use form that does not need to remove the support layer while selectively releasing the drug to the tooth surface.

The patch of the present invention can be disassembled and removed with only light brushing.

The patch of the present invention may contain various drugs depending on the purpose.

The following drawings attached to this specification illustrate preferred embodiments of the present invention, and serve to further understand the technical spirit of the present invention together with the above-described content of the present invention, so the present invention is limited to the matters described in those drawings It should not be construed as being limited.
1 shows the results of a questionnaire on the convenience of removal of a patch having a support layer containing starch (Example) and a patch having a water-insoluble support layer (Comparative Example) of the present invention. As can be seen in FIG. 1 , higher scores were obtained from users who used the patch of Example.
Figure 2 is a view showing the tooth attachment patch (1) of the present invention by way of example. As exemplarily shown in FIG. 2 ( a ), it may be a patch including a drug layer 10 and a support layer 20 , and as shown in FIG. 2 ( b ), between the drug layer 10 and the support layer 20 . According to the purpose, another layer 30 may be provided separately.

Hereinafter, in order to explain the present invention in more detail, the following examples and the like will be described. However, the embodiments according to the present invention may be modified in various other forms, and the scope of the present invention should not be construed as being limited to the embodiments described below. The embodiments of the present invention are provided by way of example to help the specific understanding of the present invention. Unless otherwise specified, percentages in this specification may be understood to mean weight percent.

<Manufacturing patch for teeth whitening>

The tooth whitening patch of Comparative Example having the composition of Table 1 and the tooth whitening patch of Example having the composition of Table 2 below were prepared. It was manufactured according to the method of manufacturing the backing layer and the drug reservoir layer of Preparation Example 1 of Korean Patent Registration No. 10-0816250.

Comparative Example 1 Comparative Example 2 drug layer Hydrogen peroxide 2.9%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% Hydrogen peroxide 2.9%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% support layer Ethyl Cellulose 15.0%
Castor oil 10.0%
Ethanol etc to 100% Povidone 15.0%
Glycerin 3.0%
Pullulan 1.0%
water, etc. to 100%

Example 1 Example 2 Example 3 Example 4 drug layer Hydrogen peroxide 2.9%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% Hydrogen peroxide 2.9%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% Hydrogen peroxide 2.9%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% Hydrogen peroxide 2.9%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% support layer Ethyl Cellulose
12.0%
Hydroxypropylmethyl cellulose 3.0%
Castor oil 15.0%
SPAN80 5.0%
Ethanol etc to 100% Ethyl Cellulose
3.0%
Hydroxypropylmethyl cellulose 12.0%
Castor oil 5.0%
SPAN80 15.0%
Ethanol etc to 100% Ethyl Cellulose 12.0%
Povidone 3.0%

Castor oil 15.0%
SPAN80 5.0%
Ethanol etc to 100% Ethyl Cellulose 3.0%
Povidone 12.0%

Castor oil 5.0%
SPAN80 15.0%
Ethanol etc to 100%

Example 5 Example 6 drug layer Monobasic potassium phosphate 2.0%
Dibasic Potassium Phosphate 3.0%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% Bamboo salt 3.0%
Corn unsaponifiable quantitative extract 0.5%
Povidone 19.0%
Glycerin 3.0%
Pullulan 1.0%
SPAN80 5.0%
water, etc. to 100% support layer Ethyl Cellulose 6.0%
Hydroxypropylmethyl cellulose 8.0%
Castor oil 15.0%
SPAN80 5.0%
Ethanol etc to 100% Ethyl Cellulose 7.0%
Hydroxypropylmethyl cellulose 8.0%
Castor oil 5.0%
SPAN80 15.0%
Ethanol etc to 100%

<Removal Power Survey>

Except for Comparative Example 2, which melts away during use A questionnaire on the convenience of removal was conducted for Comparative Example 1 and Examples 1 to 6, which require a removal process after use. Thirty respondents applied each patch of Comparative Example 1 and Examples 1 to 6 for 15 minutes for each group, and then removed Comparative Example 1 or Examples 1 to 6 through brushing. Then, each group responded to a questionnaire about the ease of removal after changing the product.

- Based on survey responses -

5: It is very convenient to remove and there is no clumping on the toothbrush

4: It is convenient to remove, but a little residue remains on the toothbrush.

3: Removal is not convenient, and residues on the toothbrush remain inconvenient.

2: Removal is inconvenient and there are many residues on the toothbrush.

1: It is very inconvenient to remove and there is a lot of residue on the toothbrush.

As can be seen in FIG. 1 , in the case of Comparative Example 1, the majority of investigators evaluated that a large amount of lumpy residue remained on the toothbrush and the removal was very inconvenient. However, the majority of investigators using the examples of the present invention rated that removal by brushing was convenient and left very little residue.

It was confirmed that the tooth patch of the present invention is conveniently removed when removed through brushing after use, and is clean without agglomeration and agglomeration on the toothbrush.

<Evaluation of degradation by brushing>

Two sets of Comparative Example 1 and Examples 1 to 6 were prepared, and one set was shaken in distilled water for 30 minutes so that only the support layer remained, dried and weighed, and the other set was attached to a slide glass and attached to a slide glass at 37°C, 85% humidity. After holding in the environment for 30 minutes, brushing was carried out for 3 minutes using a brushing machine at a load of 250 g at a speed of 90 reciprocations per minute. After that, the slide glass, brushing chamber and toothbrush were removed and washed with distilled water to collect the cleaning solution. The washing solution collected in this way was filtered through a mesh with a sieve size of 1 mm, and the residue was dried and weighed to determine the ratio of the residue to the total weight of the support layer.

Comparative Example 1 Example 1 Example 2 Example 3 Example 4 Example 5 Example 6 Residual rate (wt%) 98.6 1.6 0.8 1.9 0.6 0.5 0.4

As can be seen in Table 4, it was confirmed that the patch of Comparative Example had a residue ratio of 98% or more, and was hardly decomposed by brushing. However, in the case of the patch having the support layer mixed with the water-soluble polymer of the present invention, the residual ratio was less than 2%, and it was confirmed that most of the patches were decomposed by brushing.

1: patch
10: drug layer
20: support layer

Claims (9)

a drug layer that delivers the drug to the tooth; and
It includes a support layer located on the opposite side of the tooth attachment surface of the drug layer,
The support layer includes both a water-soluble polymer and a water-insoluble polymer, and the water-insoluble polymer is cellulose acetate phthalate, shellac, polyvinyl acetate, ethyl cellulose, polymethylmethacrylate, methacryloyl ethyl betaine/methacryloyl A patch for attaching teeth or surrounding teeth removed by brushing, characterized in that at least one selected from the group consisting of acrylate copolymers, methacrylic acid copolymers, and aminoalkyl methacrylate copolymers. The method of claim 1, wherein the water-soluble polymer is polyalkylvinylether-maleic acid copolymer, polyvinyl alcohol, polyacrylic acid, poloxamer 407, polyethylene oxide, polyvinylpyrrolidone-vinylacetate copolymer, polyvinylpyrrolidone, Polyquaternium-11, polyquaternium-39, carboxypolymethylene, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, gelatin, and characterized in that it contains any one or more selected from the group consisting of alginic acid A patch for attachment to or around teeth that is removed by brushing. [Claim 3] The patch according to claim 2, wherein the water-soluble polymer is hydroxypropylmethyl cellulose, polyvinylpyrrolidone, or a mixture thereof. The tooth removed by brushing according to claim 1, wherein the water-soluble polymer and the water-insoluble polymer contained in the support layer have a weight ratio of the water-soluble polymer: the water-insoluble polymer contained in the support layer of 1:4 to 4:1. or a patch for attachment to the periphery of the tooth. The method of claim 1, wherein the drug layer is removed by brushing, characterized in that it contains any one or more selected from the group consisting of a tooth whitening component, a component for preventing or improving sore throat, a component for preventing tooth decay, and a component for preventing periodontal disease. Patches for attachment to teeth or periphery of teeth. According to claim 5, wherein the tooth whitening component is hydrogen peroxide, urea peroxide, calcium peroxide, sodium percarbonate, sodium perborate, sodium peroxide, and any one or more peroxides selected from the group consisting of pyrophosphate and mixtures thereof;
Sodium pyrophosphate, acid sodium pyrophosphate, sodium metaphosphate, sodium polyphosphate, potassium sodium pyrophosphate, potassium pyrophosphate, any one or more polyphosphates selected from the group consisting of ultra metaphosphates and acid polyphosphates that are ultra phosphates; Or a patch for attachment to a tooth or a tooth periphery removed by brushing, characterized in that it is a mixture thereof. The method of claim 5, wherein the ingredient for preventing or improving tooth decay or tooth decay is at least one selected from the group consisting of strontium chloride, calcium carbonate, sodium citrate, sodium fluoride, silica, hydroxyapatite, potassium nitrate, and potassium phosphate. A patch for attachment to or around teeth that is removed by brushing. The method of claim 5, wherein the periodontal disease prevention component is bamboo salt, corn unsaponifiable quantitative extract, polycrezulene, tetracycline, chlorhexidine gluconate, cetylpyridium chloride, sangguinarin, tricrosan, hubark, sen Tela asiatica, chamomile, latania, myrrh, sangbaekpi, horseback riding, green tea, licorice, gold, pogongyeong, and a patch for attachment to a tooth or surrounding tooth removed by brushing, characterized in that at least one selected from the group consisting of gold and silver coins. The brushing according to claim 1, wherein the patch is brushed for 3 minutes at a speed of 90 reciprocations per minute under a load of 250 g, and the dry weight of the residue filtered through a 1 mm mesh is less than 2% by weight based on the total weight of the patch before brushing. A patch for attachment to or around a tooth that is removed with a

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