TW201725030A - Tooth whitening composition having improved stability - Google Patents

Abstract

One embodiment of the present invention provides a tooth whitener composition comprising peroxide as an active ingredient, the tooth whitener composition comprising 0.1-10 wt% of phytic acid or a salt thereof, based on the total weight of the tooth whitener composition.

Description

Improved whitening agent composition for stability

The present invention relates to a tooth whitening agent composition, and more particularly to the inhibition of decomposition of a peroxide as a whitening functional active ingredient by phytic acid and to improve the pH stability of the composition, thereby maintaining long-term storage. A tooth whitening composition that can also continue to exert a whitening effect.

The teeth are composed of internal dentin and enamel as the exterior of the protective wall of the teeth. The color of the enamel is originally opaque white or yellow. The enamel has a natural space or pores into which some coloring matter and a color changing agent permeate.

A variety of materials in contact with people may cause tooth coloring or reduce tooth whitening. In particular, food and tobacco accumulate in the enamel of the teeth to form a film on the teeth, and such coloring and discoloring substances can pass through the enamel. If these phenomena occur repeatedly, it may cause discoloration of the teeth.

Moreover, certain diseases or environmental factors may also affect the discoloration of the teeth. Even if the discoloration of the above teeth does not pose a health risk in a short period of time, the demand for tooth whitening has continued to increase as people's interest in aesthetics has increased recently.

The peroxide-based tooth whitening agents currently used are believed to move free radicals generated by peroxides through the enamel layer and dentin of the teeth to oxidize pigments or stains present inside the teeth, and the dosage forms are divided. It is used for liquid, gel type, paste type, patch type, and the like.

The cream type tooth whitening agent is easy to use and inexpensive, and is used by many people, but the whitening effect is insufficient due to the short contact time, and in the case of the liquid tooth whitening agent, the whitening ingredient is stabilized in the liquid. The product is easy to use, but is diluted by saliva in the mouth, so that the whitening effect is reduced.

In addition, in the case of a patch type tooth whitening product which is currently on the market, although it is simple to use and its effect is better than a cream type tooth whitening agent or a liquid tooth whitening agent, it may wrinkle or fold during storage and cannot be used. The situation is very frequent, and in order to whiten a part of the discolored teeth, it is necessary to stick the product on the entire tooth, and an additional patch deformation process is required, which has a complicated preparation method.

It is known that the peroxide has excellent tooth whitening effect, but there is a problem that compatibility with a generally used tooth whitening agent is poor and stability of long-term storage is lowered. Further, the generally used tooth whitening agent contains a large amount of metal ions including iron (III) ions as impurities, and this metal ion acts as a catalyst for decomposing peroxide, and therefore, it causes peroxide during storage and circulation. It is rapidly decomposed to generate gas in the product, thereby causing problems such as expansion of the container or separation of the dosage form.

In order to remedy the above problem, Korean Patent No. 10-0870232 and the like disclose a tooth whitening agent which can stabilize a material which is a peroxide functional active ingredient, but it is difficult to ensure long-term stability. The problem of maintaining the stability of the peroxide.

Technical Problem to be Solved: The present invention has been made to solve the above problems of the prior art, and the present invention is directed to providing a peroxide by inhibiting metal ions released during storage due to other components in the composition during storage. The decomposition of the composition and the unnecessary pH change of the composition, the tooth whitening agent composition which has good stability during long-term storage and can continuously exert a whitening effect.

Technical Solution: One object of the present invention is to provide a tooth whitening composition comprising a peroxide as an active ingredient and comprising 0.1 to 10% by weight relative to the total weight of the tooth whitening composition. Phytic acid or a salt thereof.

In one embodiment, the peroxide may be present in an amount from 0.5 to 50% by weight relative to the total weight of the tooth whitener composition.

In one embodiment, the peroxide may be selected from the group consisting of hydrogen peroxide, percarbonate, perborate, urea peroxide, sodium pyrophosphate perphosphate, calcium peroxide, barium peroxide, magnesium peroxide, and potassium peroxide. At least one of the group consisting of.

In one embodiment, the tooth whitening composition may further comprise from 1 to 10% by weight of a chelating agent, relative to the total weight of the tooth whitening composition.

In one embodiment, the chelating agent may be at least one selected from the group consisting of ethylenediaminetetraacetic acid and salts thereof, sodium stannate, potassium stannate, and pyrophosphate.

In one embodiment, the tooth whitening composition may further comprise from 1 to 10% by weight of a pH adjusting agent relative to the total weight of the tooth whitening composition.

In one embodiment, the pH adjusting agent may be selected from the group consisting of disodium phosphate, trisodium phosphate, sodium carbonate, sodium hydrogencarbonate, sodium hydroxide, potassium hydroxide, potassium carbonate, ammonium hydroxide, triethanolamine, tri ( At least one of the group consisting of hydroxymethyl)aminomethane, citric acid, and sodium citrate.

In one embodiment, the tooth whitening composition may further comprise from 5 to 80% by weight of the adhesive polymer relative to the total weight of the tooth whitening composition.

In one embodiment, the adhesive polymer may be selected from the group consisting of hydroxyethyl cellulose, hydroxypropyl methyl cellulose, polyacrylic acid, polyvinyl alcohol, polyvinyl pyrrolidone, carboxymethyl cellulose, carboxyethyl fiber. At least one of the group consisting of a carboxypropyl cellulose.

In an embodiment, the adhesive polymer may be polyvinylpyrrolidone having a K value of 12 to 120.

In one embodiment, the tooth whitening composition may further comprise from 1 to 10% by weight of surfactant relative to the total weight of the tooth whitening composition.

In one embodiment, the surfactant may be at least one selected from the group consisting of polyethylene glycol, propylene glycol, glycerin, triethyl citrate, and polysorbate.

Efficacy: A tooth whitening composition according to an embodiment of the present invention inhibits decomposition of a peroxide as a whitening functional active ingredient and unnecessary pH change of a composition by phytic acid, thereby stabilizing during long-term storage Good, and can continue to play the whitening effect.

The effects of the present invention are not limited to the above effects, and it should be understood that all the effects deduced from the structure of the invention described in the specification of the present invention or the scope of the patent application are included.

Hereinafter, the present invention will be described with reference to the drawings. However, the invention may be embodied in many different forms and should not be construed as being limited to the embodiments set forth herein.

Throughout the text, the term "comprising" means that the presence or addition of one or more other constituent elements is not excluded, and may include other constituent elements, unless the context dictates otherwise.

One aspect of the present invention provides a tooth whitening composition comprising a peroxide as an active ingredient and comprising 0.1 to 10% by weight relative to the total weight of the tooth whitening composition Acid or its salt.

As used herein, the term "active ingredient" means an ingredient having a direct whitening function in the ingredients of the tooth whitening composition. That is, the radical generated by the peroxide moves through the enamel and the dentin of the tooth, and the pigment or stain existing inside the tooth is oxidized, so that the whitening effect on the discolored tooth can be achieved.

The peroxide may be present in an amount of from 0.5 to 50% by weight, based on the total weight of the tooth whitener composition, preferably from 3 to 35% by weight. If the content of the peroxide is less than 0.5% by weight, the desired level of whitening effect cannot be achieved, and if the content of the peroxide is more than 50% by weight, the surface of the tooth may be corroded or the oral mucosa may be damaged. .

The peroxide may be selected from the group consisting of hydrogen peroxide, percarbonate, perborate, urea peroxide, sodium pyrophosphate pyrophosphate, calcium peroxide, barium peroxide, magnesium peroxide and potassium peroxide. At least one of them, preferably, may be hydrogen peroxide, but is not limited thereto.

Also, the tooth whitening composition may include phytic acid or a salt thereof (hereinafter collectively referred to as "phytic acid"). The phytic acid is one of the organic phosphoric acid compounds represented by the following Chemical Formula 1, also known as phytate, and is a natural antibiotic extracted from the outer skin of cereals, beans, and fruits such as rice, wheat, barley, and corn. Oxidizer. It is mainly present in the form of a salt combined with a metal ion such as phosphorus, calcium, magnesium, zinc, iron, copper or the like.

Examples of the salt of the phytic acid which may be used include sodium phytate such as monosodium phytate and disodium phytate, potassium phytate such as potassium phytate, potassium phytate, phytic acid, etc., but are not limited thereto. this. <Chemical Formula 1>:

The phytic acid is bonded to a metal ion to form a complex compound, thereby producing a "metal sealing effect" by preventing various side effects which may occur due to contact between the metal ion and other components.

The tooth whitening agent contains a large amount of metal ions including iron (III) ions as impurities, and the metal ions generate a catalyst for decomposing peroxide, so that the peroxide is rapidly decomposed during storage and circulation. It is difficult to maintain the whitening effect for a long period of time, and there are problems such as swelling of the container or separation of the dosage form due to generation of gas in the product.

In this regard, the phytic acid can substantially deactivate the metal ions by adsorbing the metal ions. That is, by preventing the peroxide from being directly exposed to the metal ions, delaying or suppressing decomposition of the peroxide due to the reaction between the peroxide and the metal ion, and making the composition The pH is stabilized so that the chemical stability and storage stability of the tooth whitening composition can be improved.

The phytic acid may be present in an amount of from 0.1 to 10% by weight relative to the total weight of the tooth whitening composition. If the content of the phytic acid is less than 0.1% by weight, the metal sealing effect is weak, and if the content of the phytic acid is more than 10% by weight, the activity of the peroxide may be excessively lowered, thereby failing to achieve the desired The standard whitening effect.

In addition, depending on the kind of metal ion present in the tooth whitening composition, the affinity between the metal ion and the phytic acid may be relatively different, and therefore, the phytic acid may not have a metal ion for all kinds of metal ions. Metal sealing effect.

Accordingly, the tooth whitening composition can further adsorb and seal metal ions that are not sealed by the phytic acid through at least one chelating agent other than the phytic acid, and the content of the chelating agent The total weight of the tooth whitening composition may range from 1 to 10% by weight. If the content of the chelating agent is less than 1% by weight, the stabilizing effect is weak, and if the content of the chelating agent is more than 10% by weight, the usability is lowered.

The chelating agent may be at least one selected from the group consisting of ethylenediaminetetraacetic acid and salts thereof, sodium stannate, potassium stannate, and pyrophosphate. Preferably, it may be ethylenediaminetetraacetic acid or tin. At least one of sodium and pyrophosphate, more preferably, may be a combination of ethylenediaminetetraacetic acid, sodium stannate, and pyrophosphate.

In particular, the pyrophosphate has a tar removal effect in addition to the metal sealing effect possessed by phytic acid and other chelating agents, and thus can be used for preventing tartar. The pyrophosphate salt may be at least one selected from the group consisting of Na ₄ P ₂ O ₇ , K ₄ P ₂ O ₇ , Na ₂ H ₂ P ₂ O ₇ and K ₂ H ₂ P ₂ O ₇ , Preferably, it may be K ₂ H ₂ P ₂ O ₇ , Na ₂ H ₂ P ₂ O ₇ or a combination thereof, but is not limited thereto.

Also, the tooth whitening composition may further include a pH adjusting agent. The pH adjusting agent serves to increase the long-term storage stability of the tooth whitening composition, and can further enhance the storage stability imparted to the composition by the phytic acid. The pH adjusting agent may be included in an amount of from 1 to 10% by weight based on the total weight of the tooth whitening composition.

The pH adjusting agent may be selected from the group consisting of disodium phosphate, trisodium phosphate, sodium carbonate, sodium hydrogencarbonate, sodium hydroxide, potassium hydroxide, potassium carbonate, ammonium hydroxide, triethanolamine, tris(hydroxymethyl)amino group. At least one of the group consisting of methane, citric acid and sodium citrate, preferably, may be sodium hydrogencarbonate, sodium citrate or a combination thereof, but is not limited thereto.

Also, the tooth whitening composition may further comprise an adhesive polymer. The adhesive polymer can be used by being applied to the surface of the tooth to form a film, or for formulating the tooth whitening agent into a gel form.

The binder polymer may be present in an amount of from 5 to 80% by weight, based on the total weight of the tooth whitener composition, preferably from 5 to 60% by weight. If the content of the adhesive polymer is less than 5% by weight, the viscosity of the whitening component layer is too low, so the applicability is lowered when the operation is performed, and the content of the adhesive polymer is more than 80% by weight. The viscosity is excessively increased, so that the operability is lowered.

The adhesive polymer may be selected from the group consisting of hydroxyethyl cellulose, hydroxypropyl methyl cellulose, polyacrylic acid, polyvinyl alcohol, polyvinyl pyrrolidone, carboxymethyl cellulose, carboxyethyl cellulose, and carboxypropyl group. At least one of the groups consisting of cellulose, preferably, may be polyvinylpyrrolidone.

In particular, the polyvinylpyrrolidone may have a K value of from 12 to 120, preferably from 80 to 100, and more preferably from 90. The K value is a value proportional to the molecular weight (degree of polymerization), and as the molecular weight increases, the viscosity increases, and the K value increases. As for the K value, there is a description of this in the United States Pharmacopoeia, and as for its physicochemical properties, see the United States Pharmacopoeia and Handbook of Pharmaceutical Excipients.

When the K value of the polyvinylpyrrolidone is less than 12, the adhesiveness is low, which may cause inconvenience in use, and if the K value is more than 120, the peroxide which is an active ingredient of the whitening functional ingredient cannot be smoothly released.

The adhesive polymer may have a weight average molecular weight (Mw) of from 100,000 to 4,000,000, preferably from 100,000 to 2,000,000. If the molecular weight of the adhesive polymer is less than 100,000, it is difficult to achieve a viscosity suitable for coating in a usual use amount, and if the molecular weight of the adhesive polymer is more than 4,000,000, the viscosity is also high at a low concentration. Therefore, it is difficult to apply.

Also, the tooth whitening composition may further include a surfactant, and the content of the surfactant may be 1 to 10% by weight relative to the total weight of the tooth whitening composition. If the content of the surfactant is less than 1% by weight, the flexibility is lowered, so that it may cause foreign body sensation when used, and if the content of the surfactant is more than 10% by weight, the tooth whitening composition The stability will be reduced.

The surfactant may be at least one selected from the group consisting of polyethylene glycol, propylene glycol, glycerin, triethyl citrate, and polysorbate. Preferably, it may be polyethylene glycol or glycerin. More preferably, it may be glycerin, but is not limited thereto.

The tooth whitening composition may include, in addition to the above components, additives such as caries inhibitors, gum disease improving agents, sweeteners, hypersensitivity preventing agents, perfumes and the like.

The caries inhibitor may be sodium fluoride, calcium fluoride, sodium monofluorophosphate, etc., and the gum disease improving agent may be bamboo salt, vitamin E acetate, vitamin D, hydroxychloroacyl sulphonate ester, and the like. Chlorogenic, xylitol, calcium glycerophosphate, aminocaproic acid, sodium monofluorophosphate, etc., the sweetener may be sorbitol, mannitol, aspartame, stevioside, saccharin, etc., the perception The allergy preventing agent may be potassium nitrate, tin fluoride, sodium monofluorophosphate, chlorine fluoride, sodium citrate, calcium hydroxide or the like, and the flavor may be menthol, peppermint oil, L-menthol, cinnamic acid or the like.

Further, as the solvent for dissolving the above components, a mixed solvent of at least one volatile organic solvent selected from the group consisting of methanol, ethanol and butanol and water may be used. Preferably, ethanol and water may be used as 1 respectively. A mixed solvent of a volume ratio of 1 to 1:10.

Hereinafter, embodiments of the invention will be described in detail.

Examples 1 to 4: Dissolve hydrogen peroxide, phytic acid, sodium hydrogencarbonate, sodium citrate, sodium acid pyrophosphate, and glycerin in a mixed solvent composed of distilled water and ethanol, and then add polyvinylpyrrolidone and stir for 1 hour or more. Thereby, a gel type tooth whitening composition is prepared.

Comparative Example 1: A gel-type tooth whitening composition was prepared in the same manner as in the above examples except that phytic acid was replaced with ethylenediaminetetraacetic acid.

Comparative Example 2: A gel-type tooth whitening composition was prepared in the same manner as in the above examples except that sodium stannate was used in place of phytic acid.

Comparative Example 3: A gel-type tooth whitening composition was prepared in the same manner as in the above examples except that phytic acid was omitted.

Comparative Example 4: A gel-type tooth whitening composition was prepared in the same manner as in the above examples except that the content of phytic acid was increased.

The compositions of the tooth whitening compositions prepared in the above examples and comparative examples are shown in Table 1 below. The numerical units in Table 1 below are percentages by weight (%) unless otherwise stated. 【Table 1】

Experimental Example 1: Evaluation of pH stability The tooth whitening compositions prepared in Examples 1, 2 and Comparative Examples 1 to 3 were filled in a 15 ml syringe and then sealed for the first time using a sealing film. Use a pouch for a second seal. The sealed tooth whitening composition was stored in a constant temperature and humidity chamber (high temperature, 40 ° C), and the change in pH was periodically measured within 12 weeks. The results are shown in Fig. 1.

Referring to Figure 1, it can be seen that a tooth whitening composition comprising a certain amount of phytic acid (Examples 1, 2) has a smaller change in pH compared to Comparative Examples 1 to 3 which does not include phytic acid, thereby providing a more stable pH value. good.

In particular, if the pH change of Comparative Example 3 and Example 1 at week 12 is compared, it can be confirmed that in the case of Comparative Example 3, it is increased by about 1.2, and in the case of Embodiment 1, it is increased by about 0.3. That is, the pH stability is remarkably improved.

Experimental Example 2: Evaluation of Hydrogen Peroxide Residual Rate The tooth whitening composition prepared in Examples 1, 2 and Comparative Examples 1 to 3 was filled in a 15 ml syringe, and then sealed for the first time using a sealing film, and a small bag was used. Perform a second seal. The sealed tooth whitening composition was stored in a constant temperature and humidity chamber (high temperature, 40 ° C), and the residual amount of hydrogen peroxide was periodically measured within 12 weeks. The results are shown in Fig. 2 .

Referring to Figure 2, it can be seen that the tooth whitening composition comprising a certain amount of phytic acid (Examples 1, 2) has a smaller amount of decomposition of hydrogen peroxide than the comparative examples 1 to 3 which do not include phytic acid, i.e., combination The hydrogen peroxide which is a whitening functional active ingredient contained in the substance is more excellent in stability.

In particular, if the change in the residual ratio of hydrogen peroxide at the 12th week in Comparative Example 3 and Example 1 is compared, it can be confirmed that in the case of Comparative Example 3, about 60% of the hydrogen peroxide is decomposed and is being carried out. In the case of Example 1, only about 2% of hydrogen peroxide was decomposed. According to the analysis, the above result is because the phytic acid added to the composition effectively adsorbs metal ions in the composition, thereby delaying and blocking the decomposition of hydrogen peroxide due to the metal ions.

The above description of the present invention has been described by way of example only, and it will be understood by those of ordinary skill in the art that the present invention can be easily modified to other specific forms without departing from the spirit and scope of the invention. Therefore, the embodiments described above are merely illustrative in all aspects, but are not limited thereto. For example, each structural member described as a single form can also be dispersed and implemented, and similarly, the structural member described using the dispersed form can be implemented in a combined form.

The scope of the present invention is to be construed as being limited by the scope of the appended claims, and all modifications and variations of the scope of the invention are intended to be included within the scope of the invention.

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Fig. 1 is a view schematically showing the results of pH stability evaluation of a tooth whitening composition according to Examples and Comparative Examples of the present invention. Fig. 2 is a view schematically showing the results of evaluation of peroxide stability of the tooth whitening composition according to Examples and Comparative Examples of the present invention.

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Claims (12)

A tooth whitening composition comprising a peroxide as an active ingredient and comprising 0.1 to 10% by weight of phytic acid or a salt thereof relative to the total weight of the tooth whitening composition. The tooth whitening composition of claim 1, wherein the peroxide is present in an amount of from 0.5 to 50% by weight relative to the total weight of the tooth whitening composition. The tooth whitening composition of claim 1, wherein the peroxide is selected from the group consisting of hydrogen peroxide, percarbonate, perborate, urea peroxide, sodium pyrophosphate pyrophosphate, calcium peroxide, and barium peroxide. At least one of the group consisting of magnesium peroxide and potassium peroxide. The tooth whitening composition of claim 1, wherein the chelating agent is further included in an amount of from 1 to 10% by weight based on the total weight of the tooth whitening composition. The tooth whitening composition according to claim 4, wherein the chelating agent is at least one selected from the group consisting of ethylenediaminetetraacetic acid and salts thereof, sodium stannate, potassium stannate, and pyrophosphate. The tooth whitening composition of claim 1, wherein the pH adjuster is further included in an amount of from 1 to 10% by weight based on the total weight of the tooth whitening composition. The tooth whitening composition according to claim 6, wherein the pH adjusting agent is selected from the group consisting of disodium phosphate, trisodium phosphate, sodium carbonate, sodium hydrogencarbonate, sodium hydroxide, potassium hydroxide, potassium carbonate, ammonium hydroxide. At least one of the group consisting of triethanolamine, tris(hydroxymethyl)aminomethane, citric acid, and sodium citrate. The tooth whitening composition of claim 1, wherein the adhesive polymer is further included in an amount of from 5 to 80% by weight based on the total weight of the tooth whitening composition. The tooth whitening composition of claim 8, wherein the adhesive polymer is selected from the group consisting of hydroxyethyl cellulose, hydroxypropyl methyl cellulose, polyacrylic acid, polyvinyl alcohol, polyvinyl pyrrolidone, carboxymethyl At least one of the group consisting of cellulose, carboxyethyl cellulose, and carboxypropyl cellulose. The tooth whitening composition of claim 8, wherein the adhesive polymer is polyvinylpyrrolidone having a K value of 12 to 120. The tooth whitening composition of claim 1, wherein the surfactant is further included in an amount of from 1 to 10% by weight based on the total weight of the tooth whitening composition. The tooth whitening composition according to claim 11, wherein the surfactant is at least one selected from the group consisting of polyethylene glycol, propylene glycol, glycerin, triethyl citrate, and polysorbate.