KR102520101B1 - Oral composition for relieving sensitive teeth - Google Patents

Abstract

The present invention is a first agent containing a metal chloride; And it relates to an oral composition for relieving or improving ache, including a second agent containing an insoluble calcium salt-forming substance. The composition for oral cavity of the present invention can effectively exhibit the effect of preventing ache in a short time.

Description

Oral composition for relieving sensitive teeth {Oral composition for relieving sensitive teeth}

The present invention relates to a composition for oral cavity, and more particularly, to a composition for oral cavity for preventing and relieving ache.

Tooth tissue is composed of enamel, cement, and dentin. The outside of exposed teeth is covered with enamel, and dentin exists on the inside. In dentin, fine tubes called dental tubules are distributed throughout the dentin.

A symptom called tooth sensitivity or tooth hypersensitivity refers to a symptom of tooth sensitivity when eating sour fruits or drinking cold drinks. It occurs when the protected dentinal tubules are exposed.

Treatments for these symptoms include dentinal tubule sealing and pulpal nerve desensitization. The dentinal tubule sealing method is a treatment that fills the exposed dentinal tubules with resin, etc., and the pulpal nerve desensitization method is a treatment that increases the content of potassium ions so that the nerve does not feel pain. However, these professional treatment procedures have the inconvenience of having to go to the dentist.

On the other hand, there are toothpastes and gargles as toothpastes and gargles, which are purchased and used by patients directly without a doctor's prescription, but these products have a limitation in exerting an effect in a short brushing time in the mouth and must be used for several weeks or months to be effective There was a difficulty that appeared.

In addition, among the symptomatic treatment of Shirin, the toothpaste containing dibasic potassium phosphate and the like to exhibit the pulpal nerve desensitization effect has an effect by the dentinal tubule sealing method, which is relatively fast because the effect appears as long as 15 days. Toothpaste is preferred. However, in the case of a toothpaste using a conventional method of sealing the dentinal tubules, the ingredients for sealing the dentinal tubules are diluted in the process of brushing the teeth, and most of them are washed out during the process of rinsing with water, so the dentinal tubules are not sealed and exposed again.

Therefore, the present invention is to solve the above problems, and to provide a composition for relieving ache, which can be applied to the tooth surface and exert an effect within a short time.

The pain reliever composition of the present invention can effectively relieve pain through the action of suppressing the flow of a stimulus transmission medium in the dentinal tubule, along with the action of reducing pain through conventional dentinal tubule blockade.

In order to solve the above problems, the present invention provides an oral composition for relieving or improving ache, including a first agent containing a metal chloride, and a second agent containing an insoluble calcium salt-forming substance.

Dentin (dentin) is a hard tissue that constitutes most of the tooth tissue, and fine tubes, dentinal tubules, are distributed throughout the dentin.

Cell projections in the dental pulp are distributed from the dental pulp to enamel to form dentinal tubules, and the space between the dentinal tubules and cell projections is filled with dentin fluid.

The term "cold tooth" refers to a case in which a tooth exhibits symptoms of aching in an external stimulus such as a temperature stimulus, or the symptom lasts for a long time and develops into pain in severe cases.

Exposure of the entrance of the dentinal tubules can be considered as the cause of these symptoms.

When the enamel or cementum is destroyed and the entrance of the dentinal tubule is exposed to the outside, stimulation is transmitted to the dental pulp by the cell protrusions, nerves, and dentin fluid of the dentinal tubule, so that pain can be felt.

As used herein, "relieving" means that the above symptoms of cold, sensitive teeth, etc. are reduced or mitigated, and can be understood as a broad concept including improvement, prevention, treatment, and the like.

In addition, "improvement" as used herein may be understood as a broad concept that means restoring symptoms to an original state by treating symptoms of syrin, sensitive teeth, and the like.

The metal chloride coagulates proteins in the dentinal tubules to inhibit the flow of dentinal tubular fluid, and the insoluble calcium salt-forming substance can block the dentinal tubules. The composition may act to block the surface of pores after proteins in the dentinal tubules are coagulated so that stimulation transmitters are not delivered to the dentinal tubules.

The metal chloride has an excellent protein coagulation action compared to other metal salts. The metal chloride is a water-soluble chloride and may include zinc chloride, magnesium chloride, strontium chloride, iron chloride, aluminum chloride, manganese chloride, or a mixture thereof. For the purpose of suppressing the flow of the present invention, preferably, zinc chloride, magnesium chloride or a mixture thereof may be used.

In order to block the dentinal tubules after treating the metal chloride according to an embodiment of the present invention, the composition may further include a component capable of forming an insoluble precipitate.

The insoluble calcium salt may form an insoluble precipitate by the calcium component contained in saliva. The insoluble calcium salt-forming material may be used without limitation as long as it is a component capable of forming an insoluble precipitate by calcium, preferably i) calcium chloride and oxalic acid, ii) potassium phosphate monobasic and calcium chloride, iii) potassium oxalate, and/or iv) Sodium succinate may be used, and any one or more mixtures selected from i) to iv) may be used.

The insoluble calcium salt forming material may form insoluble calcium salts such as calcium oxalate, calcium phosphate, and calcium carbonate.

The oral composition may be applied to the second agent after the first agent is applied to the tooth surface. In the oral composition of the present invention, the first agent included in the composition can block the flow of dentinal tubular fluid contained in the dentinal tubule, and the second agent blocks the entrance of the dentinal tubule. can

The present inventors have confirmed that the effect does not last because the conventional active agent does not stay on the tooth surface for a long time, and also, in the method of forming insoluble salts to fill the dentinal tubules, the adhesive strength of the insoluble salt is insignificant and the dentinal tubules are insignificant. Since the particles that filled the gap come out again, we confirmed the disadvantage that the effect is low and conducted research to improve it.

Therefore, the composition for oral cavity of the present invention has excellent dentinal tubule blockade ability, and can effectively prevent or alleviate ache symptoms in a short period of time.

The composition for oral cavity according to the present invention is suitable for formulation and formulation stability, enhancement of desired effects, enhancement of use preference, etc., for example, wetting agents, abrasives, medicinal agents, sweeteners, pH adjusters, preservatives, binders, flavoring agents, It may further contain additives such as a brightener, a foaming agent, or purified water, but is not limited thereto.

The humectant may be used, for example, but not limited to, concentrated glycerin, glycerin, sorbitol aqueous solution or amorphous sorbitol aqueous solution alone or in combination, and the amount used may be 1 to 60% by weight relative to the total weight of the oral composition. , but not limited thereto.

Examples of the abrasive include, but are not limited to, precipitated silica, silica gel, zirconium silicate, calcium monohydrogen phosphate, anhydrous calcium monohydrogen phosphate, hydrous alumina, light calcium carbonate, heavy calcium carbonate, calcium pyrophosphate, and insoluble metaphosphate. Alternatively, aluminum silicate may be used. The amount of the abrasive used may generally be 1 to 60% by weight based on the total weight of the oral composition, but is not limited thereto.

Examples of the sweetener include, but are not limited to, sucralose, sodium saccharin, xylitol, erythritol, or aspartame. The amount of the sweetener is generally 0.02 to 1.00% by weight relative to the total weight of the oral composition. However, it is not limited thereto.

Examples of the pH adjusting agent include, but are not limited to, sodium phosphate, disodium phosphate, citric acid, sodium citrate, succinic acid, sodium succinate, tartaric acid or sodium tartrate, and the like, and a preferred pH is 5 to 10.

Examples of the preservative include, but are not limited to, benzoic acid, methylparaben, propylparaben, or sodium benzoate alone or in combination.

Examples of the binder include, but are not limited to, guar gum, pectin, carboxyvinyl polymer, sodium alginate, laponite, carbomer, carrageenan, xanthan gum, or alginate. The amount of the binder is generally 0.1 to 3% by weight based on the total weight of the oral composition, and preferably 0.5 to 2% by weight, but is not limited thereto.

As the fragrance, for example, but not limited thereto, peppermint oil, spearmint oil, carvone, menthol, etc. may be used alone or in combination, and preferably anise oil is added to the fragrance mixed in a certain ratio can be mixed in an appropriate amount.

Titanium oxide may be used as the brightener, and preferably 0.1 to 2% by weight may be used.

Examples of the foaming agent include, but are not limited to, anionic surfactants such as sodium alkyl sulfate and sodium lauryl sulfate, nonionic surfactants such as polyoxyethylene polyoxypropylene copolymer (poloxamer), polyoxyethylene hydrogenated castor oil , or polyoxyethylene sorbitan fatty acid ester and the like can be used. The amount of these foaming agents is generally 0.5 to 5% by weight based on the total weight of the oral composition, and may be preferably 0.5 to 3.5% by weight, but is not limited thereto.

As the sweetener, for example, sodium saccharin, aspartame, licorice acid, etc. may be used alone or in combination, and may be used in an amount of 0.05 to 0.5% by weight.

The oral composition of the present invention may also use enzymes such as dextranase as other additives.

The oral composition of the present invention may contain the remaining amount of water, preferably purified water, in addition to active ingredients and additives.

The composition for oral cavity according to the present invention may have formulations such as, for example, toothpaste, mouthwash, spray, mouthwash, gum, candy, oral rinse, tooth whitening agent, etc. in its formulation, but is not limited thereto. Any formulation that is likely to come into contact with oral tissue after intravenous administration may be included without limitation, and may be formulated by conventional means known to those skilled in the art.

In another embodiment of the present invention, the composition for oral cavity of the present invention can be provided in the form of a tooth attachment patch having a multi-layer structure consisting of one or more layers.

In one embodiment of the present invention, the patch for attaching the teeth includes a first layer comprising a metal chloride; and a second layer including an insoluble calcium salt forming material.

That is, another embodiment of the present invention is a first layer containing a metal chloride; and a second layer comprising an insoluble calcium salt-forming material, providing a tooth attachment patch for alleviating or improving pain.

The present inventors have confirmed that it is important to block external stimuli by preventing the flow of dentin fluid as well as filling the dentinal tubules of exposed dentin in order to alleviate the symptoms of sensitive teeth or teeth showing cold symptoms.

The first layer may further include a caries preventing component, a phosphate, an abrasive, and the like in addition to the metal chloride. Ingredients other than the metal chloride may be included in an appropriate range for the purpose of the present invention.

The cavity preventing component may include any one selected from sodium fluoride, sodium fluorophosphate monobasic, tartaric acid fluoride, or mixtures thereof, preferably sodium fluoride.

The phosphate may be any one selected from sodium phosphate, potassium phosphate, calcium phosphate, or mixtures thereof, and preferably, potassium phosphate or a mixture of potassium phosphate and sodium phosphate may be used.

In particular, the potassium phosphate can also be expected to have a neuroleptic action by potassium ions, has excellent reactivity with calcium ions, and can stably generate an insoluble calcium compound.

The abrasive is any one selected from precipitated silica, silica gel, zirconium silicate, calcium monohydrogen phosphate, anhydrous calcium monohydrogen phosphate, hydrous alumina, light calcium carbonate, heavy calcium carbonate, calcium pyrophosphate, insoluble metaphosphate, aluminum silicate, or mixtures thereof. One abrasive may be included, and preferably, silica such as precipitated silica or silica gel may be used.

The abrasive plays a role of smoothing the tooth surface after removing the patch from the tooth surface after a certain period of time has elapsed after attaching the patch of the present invention.

The first layer of the present invention is attached to the tooth surface by saliva, releases metal chloride, and uses a water-soluble polymer as a main base to release the components included in the second layer slowly, and further contains a plasticizer. can do.

Since the polymer serving as a tooth adhesive property of the present invention should have a property of being hydrated by water, it should be a hydrophilic polymer or a polymer showing at least a little hydrophilicity. Commonly used polymers include polyalkyl vinyl ether-maleic acid copolymer (PVM/MA copolymer, Gantrez AN 119, AN 139, S-97), polyvinyl alcohol, polyacrylic acid, poloxamer (Poloxamer 407 (Pluronic)), Polyvinylpyrrolidone-vinyl acetate copolymer (PVP/VA copolymer; Luviskol VA, Plasdone S PVP/VA), polyvinylpyrrolidone (PVP, K-30 ~ K-120), polyquaterium- 11 (Gafquat 755N), polyquaternium-39 (Merquat plus 3330), Carbomer (Carbopol), hydroxypropylmethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, gelatin, alginic acid ( Sodium Alginate), polymethyl methacrylate, methacryloyl ethyl betaine/methacrylate copolymer (Yukaformer: Methacryloyl Ethyl Betain/Methacylates Copolymer), aminoalkyl methacrylate copolymers (Eudragit E 100, Eudragit E 12,5, Eudragit RL 100, Eudragit RL 30D) or mixtures thereof may be used. As the 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 a mixture thereof may be used by adjusting the ratio. .

In order to quickly release the metal chloride and other components included in the first layer of the present invention, a hydrophilic and water-soluble polymer may be further included. As the polymer, carboxymethyl cellulose, xanthan, hydroxypropylmethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose, pullulan, or mixtures thereof may be used.

In order for the patch of the present invention to flexibly bend along the curved surface of the tooth, polypropylene glycol, glycerin or polyethylene glycol, castor oil, hydrogenated castor oil castor oil) or any one plasticizer selected from mixtures thereof may be added.

The patch of the present invention includes a second layer on the opposite side of the first layer in contact with the teeth.

The second layer may further include a component capable of forming insoluble precipitates. Components capable of forming the insoluble precipitate may include potassium oxalate, calcium chloride and oxalic acid, potassium monophosphate and calcium chloride, potassium oxalate, or sodium succinate, as mentioned herein, or may include mixtures thereof .

Like the first layer, the second layer may further include an abrasive.

The second layer uses a water-soluble polymer as a main base so that the components included in the first layer are released and the components included in the first layer coagulate proteins in the dentinal tubules and then release after a certain period of time, , It may further include a plasticizer.

Components included in the first layer may be equally used as the water-soluble polymer and plasticizer.

According to still other embodiments of the present invention, the patch of the present invention serves to support the first and second layers, and prevents the layer included in the patch from contacting other skin in the oral cavity other than the teeth. A support layer may be further included to prevent it.

Such a support layer may be mainly composed of insoluble materials such as polyethylene and ethyl cellulose for the purpose of the support layer, and may further include components such as plasticizers and oils.

The dental patch according to the present invention may further include a peeling layer attached to the first layer to be removed before use.

The tooth attachment patch according to the present invention may be manufactured by a method disclosed in, for example, U.S. Patent Nos. 6,682,721, 6,689,344, 6,780,401, 6,946,142, etc., but the present invention relates to the components and manufacturing method of such a patch. is not limited to

The term "patch" used herein refers to an adhesive formulation containing specific components, and the shape or structure of the patch is not particularly limited.

The oral composition of the present invention can improve symptoms of ache by filling and wrapping fine gaps on the tooth surface.

The composition for oral cavity of the present invention not only has the effect of filling the dentinal tubules, but also prevents the flow of dentinal fluid contained in the dentinal tubules, thereby minimizing the degree of transmission of stimulation to the pulp nerve.

The composition for oral cavity of the present invention provides a pain relief and relief effect.

The following drawings attached to this specification illustrate preferred embodiments of the present invention, and serve to further understand the technical idea of the present invention together with the contents of the above-described invention, so the present invention is limited to those described in the drawings. It should not be construed as limiting.
1 is a diagram showing a cross-section of exposed dentin where cold symptoms may appear. Shirin ear symptoms are caused by stimulation of the inner nerves of the dentinal tubules exposed to the outside.
2-5 show the result of observing the degree of blockade of dentinal tubules with a scanning electron microscope after treating human teeth with exposed dentinal tubules with the compositions of Comparative Examples and Examples. 2 shows the case of processing Example 1, FIG. 3 shows the case of processing Example 2, FIG. 4 shows the case of processing Example 3, and FIG. 5 shows the case of processing Comparative Example 1.

Hereinafter, the following examples and the like will be described in order to explain the present invention in more detail. However, embodiments according to the present invention can be modified in many different forms, and the scope of the present invention should not be construed as being limited to the embodiments described below. Embodiments of the present invention are provided by way of example to help a detailed understanding of the present invention.

[Preparation of Examples 1-3 and Comparative Examples]

Oral preparations were prepared according to Table 1 below.

Example 1 prepared a dry type patch, Example 2 prepared a dry type patch after applying a primer, and Example 3 prepared a double toothpaste. The following contents are expressed in weight %.

Example 1
Dry patch or adhesive toothpaste Example 2
Primer + Dry patch Example 3
Double toothpaste formulation
(double container or two stripes, etc.) 1st layer: zinc chloride 0.5%
2nd layer: calcium chloride 3.0%
Oxalic acid 1.0% Primer: 2% magnesium chloride solution
Dry patch: Potassium oxalate 3% Agent 1: Zinc chloride 1.0%
Agent 2: 4% monobasic potassium phosphate
Calcium Chloride 2%

Comparative Example 1: Potassium oxalate 3.0% patch product (P&G Crest Sensystop)

Comparative Example 2: Potassium nitrate 5.0% toothpaste formulation

Comparative Example 3: Zinc Chloride 1.0% Adhesive Toothpaste

[Electron microscopy observation of dentinal tubule blocking effect]

A dentin specimen of a bovine tooth (cortex) was prepared with the compositions of Examples and Comparative Examples, and was immersed in a solution diluted with bovine serum protein in physiological saline to be similar to the situation in the living body. After treatment with the composition for about 10 minutes, washing with running water and drying at room temperature, electron microscopic observation was performed. (Comparative Example 2 was excluded from the photo experiment because it was a prescription for a sensitive neuroleptic, not a blocking action of the dentinal tubule.

1) Experiment method

Using a dentin specimen, an appropriate amount of artificial saliva was applied to the dentin surface, and the adhesive patch was attached for 30 minutes. In the comparative example, a slurry solution in which artificial saliva and the composition of the comparative example were mixed at a ratio of 2: 1 was added to a shaker for 30 minutes. , washed in flowing distilled water for 30 minutes, dried at room temperature, and sputtered with an Ion Beam Coater (GATAN) for 5 minutes to coat the sample surface with Iridium particles. Using SEM/EDS (Scanning Electron Microscope / Energy Dispersive Spectrometer: Hitachi S-4800), the acceleration voltage was set to 15 kV and the emission current was set to 15 μA, and observation and analysis were performed at 2,000 times.

2) Experimental results

The degree of dentinal tubule blockage through Examples and Comparative Examples is shown in FIGS. 2 to 5.

As can be seen in Figure 5, in the comparative example, the dentinal tubules were exposed as they were, and no precipitate was observed. From these results, it is thought that the preparation of Comparative Example 1 has room to stimulate internal nerves because the dentinal tubules are exposed as they are even after application.

In contrast, in the case of the embodiments, it was found to completely block the dentinal tubules, and through this, the embodiments of the present invention are thought to be able to fill the fine gaps in the dentinal tubules and block nerve stimulation.

Therefore, it is thought that the patch for tooth attachment of the present invention can improve symptoms of tooth hypersensitivity or ache.

[Clinical questionnaire evaluation for humans]

1) Test subjects and usage: Example 1 group, Comparative Example 1 group, and Comparative Example 3 group were attached to the ache site for 10 minutes once a day and then removed (Comparative Example 3 group removed by brushing) Example 3 Group and Comparative Example 2 were used as a substitute for toothpaste for 3 minutes 3 times a day.

2) 15 volunteers from each group who felt the pain were evaluated on a 3-point Likert scale after using it for 1 week.

3) Scale standard

1 point: Compared to before use, ache symptoms were similar or worsened

2 points: A little less numbness than before use

3 points: The soreness symptoms were alleviated compared to before use

4) Survey results

Example 1 Example 3 Comparative Example 1 Comparative Example 2 Comparative Example 3 Sirin ear symptom questionnaire score 2.8 2.4 1.7 1.9 1.8

As can be seen in Table 2, in the case of the comparative example in which the dentinal tubules were confirmed to be exposed as they were in the micrograph, the result was obtained that there was no significant difference in the symptoms of ache from before use. However, in the case of Examples 1 and 3, it was found that the ache symptoms were alleviated than before use.

Claims (10)

An oral preparation comprising the first agent and the second agent,
The second agent is applied after the first agent is applied to the tooth surface,
The first agent contains a metal chloride,
The second agent includes an insoluble calcium salt-forming substance,
The metal chloride coagulates proteins in the dentinal tubules to inhibit the flow of dentinal tubular fluid, and the insoluble calcium salt-forming substance blocks the dentinal tubules so that the oral formulation blocks the dentinal tubules after the proteins in the dentinal tubules are coagulated. characterized in that,
The metal chloride is zinc chloride, magnesium chloride, strontium chloride, iron chloride, aluminum chloride, manganese chloride or a mixture thereof, oral formulation for relieving or improving ache. delete delete The oral cavity of claim 1, wherein the insoluble calcium salt-forming substance is i) calcium chloride and oxalic acid, ii) potassium phosphate monobasic and calcium chloride, iii) potassium oxalate, iv) sodium succinate, or v) mixtures thereof. formulation. delete A tooth attachment patch having a multilayer structure of two or more layers,
The patch for attaching the tooth includes a first layer that includes a metal chloride and is attached to the tooth; and
A second layer comprising an insoluble calcium salt forming material;
The metal chloride coagulates proteins in the dentinal tubules to inhibit the flow of dentinal tubular fluid, and the insoluble calcium salt-forming material blocks the dentinal tubules so that the patch for tooth attachment blocks the dentinal tubules after the proteins in the dentinal tubules are coagulated. characterized in that,
The metal chloride is characterized in that it comprises zinc chloride, magnesium chloride, strontium chloride, iron chloride, aluminum chloride, manganese chloride or a mixture thereof, the tooth attachment patch. The method of claim 6, wherein the first layer or the second layer of the tooth attachment patch
Polyalkyl vinyl ether-maleic acid copolymer, polyvinyl alcohol, polyacrylic acid, poloxamer, polyvinyl pyrrolidone-vinylacetate copolymer, polyvinylpyrrolidone, polyquaternium, polyquaternium-39, carbomer, hydroxy Roxypropylmethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, gelatin, alginic acid, polymethylmethacrylate, methacryloylethylbetaine/methacrylate copolymer, aminoalkylmethacrylate copolymer or any of these Characterized in that it comprises any one polymer selected from the mixture, the patch. delete 7. The patch of claim 6, wherein the insoluble calcium salt-forming substance is i) calcium chloride and oxalic acid, ii) potassium phosphate monobasic and calcium chloride, iii) potassium oxalate, iv) sodium succinate, or v) mixtures thereof. . 7. The patch according to claim 6, wherein the first layer or the second layer comprises a plasticizer selected from polypropylene glycol, glycerin, polyethylene glycol, castor oil, hydrogenated castor oil, or mixtures thereof.

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