Method for improving adsorption of active ingredient to oral mucosa and agent for improving adsorption of active ingredient

Abstract

To provide a method for improving the adsorption of an active ingredient to the oral mucosa.SOLUTION: The present invention relates to a method for improving the adsorption of an active ingredient to the oral mucosa by using an oral composition containing the active ingredient and shellac.SELECTED DRAWING: Figure 1

Description

[Technical field]

[0001] The present invention relates to a method for improving the adsorption of an active ingredient to the oral mucosa and an agent for improving the adsorption of an active ingredient. [Background technology]

[0002] Oral compositions that are applied to the oral cavity are blended with various active ingredients depending on the purpose. For example, oral compositions such as dentifrices and mouthwashes may contain active ingredients for preventing or improving oral diseases such as periodontal disease, gingivitis, caries, hypersensitivity, and bad breath, and active ingredients for moisturizing the oral cavity. For example, Patent Document 1 discloses a liquid oral composition containing dipotassium glycyrrhizinate as an anti-inflammatory agent. [Prior art documents] [Patent documents]

[0003] [Patent Document 1] JP 2000-16927 A Summary of the Invention [Problem to be solved by the invention]

[0004] In order to enhance the effect of an active ingredient in an oral composition, for example, it is possible to increase the amount of the active ingredient, but this approach often leads to new problems such as an unpleasant taste, an unpleasant odor, and a decrease in the stability of the composition due to the increase in the amount of the active ingredient.

[0005] Therefore, the present inventors have focused on lengthening the retention time of the active ingredient in the oral cavity as another means for enhancing the effect of the active ingredient. Usually, even if an oral composition containing an active ingredient is applied to the oral cavity, the active ingredient is unlikely to remain on the oral mucosa, and in particular, when the oral composition is spit out, the active ingredient is discharged from the oral cavity, so that the effect of the active ingredient in the oral cavity may not be fully exerted. The present inventors have conducted extensive research to lengthen the retention time of the active ingredient in the oral cavity. As a result, they have found that the adsorption of the active ingredient to the oral mucosa can be improved by using an oral composition containing shellac together with the active ingredient. This allows the retention time of the active ingredient in the oral cavity to be lengthened, and the effect of the active ingredient on the oral mucosa to be fully exerted. [Means for solving the problem]

[0006] That is, the present invention is characterized by the following (1) to (4). (1) A method for improving adsorption of an active ingredient to the oral mucosa by using an oral composition containing the active ingredient and shellac. (2) The method according to (1) above, wherein the oral composition further contains a cationic bactericidal component. (3) The method according to (1) or (2) above, which improves adsorption of the active ingredient to keratin in the oral mucosa. (4) An active ingredient adsorption enhancer containing shellac for improving the adsorption of active ingredients to the oral mucosa. Effect of the Invention

[0007] According to the present invention, it is possible to improve the adsorption of an active ingredient to the oral mucosa, and to fully exert the effect of the active ingredient on the oral mucosa. [Brief description of the drawings]

[0008] [Figure 1] FIG. 1 is a graph showing the results of the adsorption test in the examples. [Diagram 2] FIG. 2 is a graph showing the results of the adsorption test in the examples. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0009] Hereinafter, the embodiments of the present invention will be described in further detail.

[0010] <Method for improving the adsorption of active ingredients to the oral mucosa> One embodiment of the present invention relates to a method (hereinafter also referred to as this method) for improving adsorption of an active ingredient to the oral mucosa by using an oral composition (hereinafter also referred to simply as an oral composition) containing the active ingredient and shellac.

[0011] As described above, this method focuses on lengthening the residence time of the active ingredient in the oral cavity as a means for enhancing the effect of the active ingredient in the oral cavity composition, and is based on the discovery that the adsorption of the active ingredient to the oral mucosa can be improved by applying the active ingredient together with shellac to the oral mucosa. The details of the above mechanism are not clear, but it is speculated as follows. That is, the active ingredient in the oral cavity composition is unlikely to remain on the oral mucosa and is often gradually expelled, but when the active ingredient is applied to the oral mucosa together with shellac, the resin component and wax component contained in the shellac interact with the active ingredient and form a film or adhere to the mucosal surface, mediating the adsorption of the active ingredient to the oral mucosa, and as a result, it is considered that the adsorption of the active ingredient to the oral mucosa is improved. It is to be noted that the present invention is not limited to the above mechanism.

[0012] In this method, the adsorption of the active ingredient to the oral mucosa can be evaluated by measuring the adsorption rate of the active ingredient to keratin (keratin powder), a type of protein contained in the oral mucosa, using the following method. (i) First, 5 mL of the oral composition is added to 200 mg of keratin powder to obtain a treated sample. Separately, 5 mL of the oral composition is prepared as a sample without treating the keratin powder (untreated sample). If the oral composition is not liquid, instead, add 5 mL of a solution in which the oral composition is dissolved in water so that the active ingredient concentration is 0.001 to 0.1 w / v% to 200 mg of keratin powder to obtain a treated sample. Separately, prepare 5 mL of a solution in which the oral composition is dissolved in water so that the active ingredient concentration is the same as that of the treated sample (untreated sample) as a sample in which the keratin powder is not treated. (ii) Next, the treated sample obtained in (i) above is mixed in a shaker at 200 rpm for 5 minutes, the resulting mixture is centrifuged at 3,000 rpm for 10 minutes, and the supernatant is collected. (iii) Furthermore, the concentration of the active ingredient in the supernatant obtained in (ii) above and the concentration of the active ingredient in the oral composition that has not been subjected to treatment with keratin powder (untreated sample) are quantitatively analyzed by a quantitative method. (iv) Based on the concentration of the active ingredient in the supernatant, the adsorption rate of the active ingredient to the keratin powder is calculated using the following formula.

[0013]

number

[0014] In the present method, the adsorption rate of the active ingredient to the keratin powder is preferably 20% or more, more preferably 25% or more, and even more preferably 30% or more. With the adsorption rate of 20% or more, the active ingredient can be sufficiently maintained on the oral mucosa, so that the effect of the active ingredient can be fully exerted in the oral cavity.

[0015] The oral composition containing shellac used in this method has an improved adsorption rate of the active ingredient to the keratin powder compared to the composition not containing shellac. The adsorption rate in the oral composition containing shellac used in this method is preferably 1.5 times or more, more preferably 1.7 times or more, and even more preferably 1.9 times or more, of the adsorption rate in the oral composition not containing shellac.

[0016] The oral composition used in the present method will be described in detail below. The oral composition used in the present method (hereinafter, also simply referred to as the oral composition) contains an active ingredient and shellac.

[0017] [Active ingredients] The active ingredient in the oral composition is generally used as an active ingredient or medicinal ingredient that can be applied to the oral cavity. For example, as described above, it can be mentioned that it forms a film or adheres to the surface of the oral mucosa in a state of interacting with the resin component or wax component contained in shellac. Specifically, it can be mentioned the conventionally known anti-inflammatory ingredient, anti-allergic ingredient, moisturizing ingredient, bitterness masking ingredient, etc. Note that the active ingredient in the present invention does not include the cationic bactericidal ingredient described later.

[0018] Specific examples of the active ingredient in the oral cavity composition include glycyrrhizinic acid or a salt thereof. Glycyrrhizinic acid or a salt thereof has anti-inflammatory effect, anti-allergic effect, moisturizing effect, bitterness masking effect, etc., and can be used as an active ingredient in the oral cavity composition having these effects.

[0019] For example, in the case of an anti-inflammatory effect, one possible mode of use is to apply the oral composition as a liquid into the oral cavity and use it as a mouthwash, thereby causing glycyrrhizinic acid or a salt thereof to be adsorbed onto keratin present near cells of the oral mucosa where inflammation is occurring, thereby obtaining an anti-inflammatory effect. In addition, in the case of anti-allergic effects, one possible mode of use is to apply the oral composition as a liquid into the oral cavity and use it as a mouthwash, thereby causing glycyrrhizinic acid or a salt thereof to be adsorbed onto keratin present in the vicinity of cells experiencing an allergic reaction, thereby obtaining an anti-allergic effect. In addition, in the case of a moisturizing effect, one possible mode of use is to apply the oral composition as a liquid into the oral cavity and use it as a mouthwash, thereby causing glycyrrhizinic acid or a salt thereof to be adsorbed onto keratin on the oral mucosa, thereby maintaining the moisture content of the oral mucosa and achieving a moisturizing effect. In addition, in the case of the bitterness masking effect, one possible mode of use is to apply the oral composition as a liquid into the oral cavity and use it as a mouthwash, thereby causing glycyrrhizinic acid or a salt thereof to be adsorbed onto keratin, thereby sustaining the lingering bitterness masking effect after use. The above-mentioned usage patterns include personal use by general consumers.

[0020] Glycyrrhizic acid or its salt is an ingredient contained in the root or stem of licorice, a kind of herbal medicine. The type of glycyrrhizic acid or its salt that can be used as an active ingredient contained in the oral composition is not particularly limited, and can be appropriately selected according to the purpose. For example, glycyrrhizic acid, dipotassium glycyrrhizinate (GK2), trisodium glycyrrhizinate, monoammonium glycyrrhizinate, diammonium glycyrrhizinate, disodium glycyrrhizinate, etc. can be mentioned. These may be used alone or in combination of two or more. Among these, dipotassium glycyrrhizinate is preferred from the viewpoint of stability of the oral composition. Glycyrrhizic acid or a salt thereof can be obtained by extraction from licorice using a conventionally known method, or a commercially available product such as dipotassium glycyrrhizinate or monoammonium glycyrrhizinate manufactured by Alps Pharmaceutical Co., Ltd. or Maruzen Pharmaceutical Co., Ltd. can be used.

[0021] Other active ingredients include, for example, fluorides such as sodium fluoride and sodium monofluorophosphate; anti-inflammatory agents such as azulene, azulene sulfonate, β-glycyrrhetinic acid, dihydrocholesterol, epidihydrocholesterol, dl-α-tocopherol acetate, dl-α-tocopherol nicotinate, ε-aminocaproic acid, tranexamic acid, allantoin, and ascorbic acid; tartar prevention agents such as phosphates, polyphosphates, methoxyethylene maleic anhydride copolymer, zinc chloride, and zinc organic acids; astringents such as hinokitiol, allantoin chlorohydroxyaluminum, allantoin dihydroxyaluminum, and sodium chloride; and dentin hypersensitivity suppressants such as potassium nitrate and aluminum lactate. The above-mentioned effects include those obtained through personal use by general consumers.

[0022] The content of the active ingredient in the entire oral composition is not particularly limited, but is preferably, for example, 0.001 to 10% by mass (hereinafter also referred to as w / v%) in terms of mass-to-volume concentration. If it is 10 w / v% or less, the flavor of the composition is maintained and the occurrence of bitterness and irritation can be suppressed. Also, if it is 0.001 w / v% or more, the effect of the active ingredient can be sufficiently obtained. The content of the active ingredient is more preferably 0.005 w / v% or more, even more preferably 0.01 w / v% or more, more preferably 5 w / v% or less, and even more preferably 1 w / v% or less.

[0023] In particular, when glycyrrhizic acid or a salt thereof is used as an active ingredient, the content of glycyrrhizic acid or a salt thereof in the entire oral composition is preferably 0.001 to 0.3 w / v%. If it is 0.3 w / v% or less, the sweetness is not too strong, and it is easy to adjust the taste. If it is 0.001 w / v% or more, effects such as anti-inflammatory effect, anti-allergic effect, moisturizing effect, and bitterness masking effect can be obtained. The content of glycyrrhizic acid or a salt thereof is more preferably 0.005 w / v% or more, more preferably 0.01 w / v% or more, more preferably 0.1 w / v% or less, and even more preferably 0.05 w / v% or less.

[0024] [Shellac] It is important that the oral composition contains shellac. Shellac is a resinous substance obtained by purifying the secretions that cover the body of lac scale insects, as described in the Japanese Pharmacopoeia, and refined shellac or bleached white shellac can be used. As described above, when the oral composition contains shellac, the resin components and wax components contained in the shellac interact with the active ingredient, forming a film or adhering to the mucosal surface, thereby mediating the adsorption of the active ingredient to the oral mucosa, and as a result, it is considered that the adsorption of the active ingredient to the oral mucosa is improved.

[0025] The content of shellac in the entire oral composition is not particularly limited, but is preferably, for example, 0.01 to 1% by mass (w / v%) in terms of mass-to-volume concentration. If it is 1 w / v% or less, the characteristic odor is less noticeable and the feeling of use is less likely to be impaired. Also, if it is 0.01 w / v% or more, the effects expected from shellac can be obtained. The content of shellac is more preferably 0.05 w / v% or more, even more preferably 0.1 w / v% or more, more preferably 0.5 w / v% or less, and even more preferably 0.25 w / v% or less.

[0026] [Cationic antibacterial ingredient] The oral composition preferably contains a cationic bactericidal component. By applying the cationic bactericidal component in addition to shellac together with the active ingredient to the oral mucosa, the adsorption of the active ingredient to the oral mucosa can be further improved. Although the details of the above mechanism are not clear, it is considered that the function of the cationic bactericidal component, which strongly binds to keratin and interacts with shellac, promotes the adsorption of shellac interacting with the active ingredient to the oral mucosa, and as a result, the adsorption of the active ingredient to the mucosa is further improved. This is also inferred from the fact that, as shown in the examples below, when the oral composition does not contain shellac, the effect of improving the adsorption of the active ingredient is not obtained even if the cationic bactericidal component is contained, but when the oral composition contains both shellac and a cationic bactericidal component, the effect of improving the adsorption of the active ingredient is more remarkable than when the oral composition contains shellac alone. It should be noted that the present invention is not limited to the above mechanism.

[0027] Cationic bactericidal components include, for example, those that strongly bind to keratin as described above and interact with shellac, thereby promoting the adsorption of shellac interacting with the active ingredient to the oral mucosa.Cationic bactericidal components include, for example, quaternary ammonium salts, and specific examples of quaternary ammonium salts include cetylpyridinium chloride, benzethonium chloride, dodecylpyridinium chloride, benzalkonium chloride, chlorhexidine hydrochloride, and chlorhexidine gluconate.These may be used alone or in combination of two or more.Among these, cetylpyridinium chloride is preferred from the viewpoint of being easily dissolved in water and having good stability.

[0028] When the oral composition contains a cationic bactericidal component, the content of the cationic bactericidal component in the entire oral composition is, for example, preferably 0.001 to 1% by mass (w / v%) in terms of a mass-to-volume ratio concentration. If it is 1 w / v% or less, the bitterness derived from the bactericidal component is not too strong, and the palatability is not likely to decrease. Also, if it is 0.001 w / v% or more, a desired bactericidal effect against bacteria in the oral cavity is obtained. The content of the cationic bactericidal component is more preferably 0.005 w / v% or more, even more preferably 0.01 w / v% or more, and more preferably 0.5 w / v% or less, and even more preferably 0.1 w / v% or less.

[0029] In the oral cavity composition, the content ratio of the active ingredient to the shellac (active ingredient content / shellac content) is preferably 0.001 to 1000 by mass. The content ratio of the active ingredient to the shellac is more preferably 0.01 or more, even more preferably 0.05 or more, and more preferably 100 or less, even more preferably 10 or less, and particularly preferably 1 or less. By setting the content within the above range, the active ingredient can be adsorbed to the oral mucosa without impairing the flavor.

[0030] When the oral cavity composition contains a cationic bactericidal component, the content ratio of the active ingredient to the cationic bactericidal component (active ingredient content / cationic bactericidal component content) is preferably 0.001 to 1000 by mass. The content ratio of the active ingredient to the cationic bactericidal component is more preferably 0.01 or more, even more preferably 0.1 or more, and more preferably 100 or less, even more preferably 10 or less, and particularly preferably 5 or less, by setting it within the above range, the active ingredient can be efficiently adsorbed to the oral mucosa.

[0031] When the oral cavity composition contains a cationic bactericidal component, the content ratio of the cationic bactericidal component to the shellac (content of cationic bactericidal component / content of shellac) is preferably 0.001 to 10 by mass. By setting the content within the above range, the cationic bactericidal component can more effectively improve the adsorption of the active ingredient of the shellac. If the content is 10 or less, precipitation due to aggregation of the cationic bactericidal component and shellac is less likely to occur. The content ratio of the cationic bactericidal component to the shellac is more preferably 0.01 or more by mass, even more preferably 0.05 or more, and more preferably 5 or less, even more preferably 1 or less by mass.

[0032] When the oral cavity composition contains a cationic bactericidal component, the content ratio of the active ingredient to the shellac and the cationic bactericidal component (content of active ingredient / total content of shellac and cationic bactericidal component) is preferably 0.001 to 1000 by mass. The content ratio of the active ingredient to the shellac and the cationic bactericidal component is more preferably 0.005 or more, even more preferably 0.01 or more, and more preferably 500 or less, even more preferably 100 or less, and particularly preferably 1 or less. By setting it within the above range, the active ingredient can be effectively adsorbed to the oral mucosa.

[0033] The oral composition can be made into any application and dosage form depending on the type of active ingredient, and examples include mouthwashes, toothpastes such as liquid toothpastes and toothpastes, mouth fresheners, mouthwashes, lozenges, chewing gums, and the like. Among them, in order to ensure that the entire oral composition is sufficiently distributed throughout the oral cavity, a liquid oral composition that is used by placing an appropriate amount in the oral cavity is preferred, specifically, mouthwash and liquid toothpaste are included. To prepare mouthwash and liquid toothpaste, for example, they may be prepared by a conventional method using water, ethanol, or the like as a solvent. Liquid toothpastes can also be used that contain abrasives such as calcium phosphate, calcium hydrogen phosphate, calcium pyrophosphate, calcium carbonate, aluminum oxide, aluminum hydroxide, anhydrous silicic acid, titanium oxide-coated mica, crystalline cellulose, and charcoal grains as necessary.

[0034] Furthermore, the oral composition may contain other optional components as long as they do not impair the effects of the present invention. For example, humectants such as glycerin, sorbitol, polyethylene glycol, etc.; foaming agents such as sodium lauryl sulfate, etc.; fragrances such as pinene, peppermint oil, cinnamon oil, clove oil, eugenol, lemon oil, vanillin, cineole, eucalyptus oil, etc.; sweeteners such as saccharin, saccharin sodium, sucralose, xylitol, erythritol, sorbitol, maltitol, stevia, etc.; colorants such as Blue No. 1, Yellow No. 5, Yellow No. 4, Yellow No. 203, Green No. 3, Green No. 201, Red No. 102, etc.; preservatives such as parabens and sodium benzoate, etc.; pH adjusters such as monosodium phosphate, disodium phosphate, citric acid, sodium citrate, etc.; POE hydrogenated castor oil, POE-POP block polymer, POE-POP alkyl ether, POE alkyl ether, POE alkyl phenyl ether, POE fatty acid ester, POE higher alcohol ether, POE-POP fat nonionic surfactants such as POE sorbitan fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, propylene glycol fatty acid esters, and POE alkylamine / fatty acid amides; anionic surfactants such as sodium lauryl sulfate, sodium myristyl sulfate, POE alkyl ether sulfate, sodium lauroyl sarcosine, sodium myristoyl sarcosine, alkyl ether carboxylates, alkyl phosphates, N-acyltaurine salts, POE alkyl ether phosphoric acid / phosphate salts, and sulfonates; cationic surfactants such as alkyl ammonium salts and alkyl benzyl ammonium salts; and amphoteric surfactants such as 2-alkyl-N-carboxymethyl-N-hydroxyethyl imidazolinium betaine, coconut oil fatty acid amidopropyl betaine, and sodium lauryl diaminoethyl glycine.

[0035] In this method, the method of applying the above-mentioned oral composition to the oral cavity is not particularly limited, and a conventionally known method can be appropriately selected depending on, for example, the dosage form of the above-mentioned oral composition and the type of active ingredient of the oral composition. The method includes a method for self-use by non-physician consumers.

[0036] <Active ingredient adsorption enhancer> One embodiment of the present invention relates to an active ingredient adsorption enhancer (hereinafter, also referred to as the present agent) containing shellac for adsorbing an active ingredient to the oral mucosa. By using the present agent containing shellac, the adsorption of the active ingredient to the oral mucosa can be improved.

[0037] As a method of using this agent, for example, the agent may be applied to the oral cavity together with the active ingredient to improve adsorption of the active ingredient to the oral mucosa, the agent may be applied to the oral cavity and then the active ingredient may be applied to the oral cavity to improve adsorption of the active ingredient to the oral mucosa, or the active ingredient may be applied to the oral cavity and then the agent may be applied to the oral cavity to improve adsorption of the active ingredient to the oral mucosa. Among them, it is preferable to apply the agent together with the active ingredient to the oral cavity. For example, the agent and the active ingredient are mixed, and the mixture obtained is applied to the oral cavity. That is, the agent and the active ingredient are mixed to obtain the composition for oral cavity in the above-mentioned method, and the composition may be applied to the oral cavity.

[0038] The content of shellac in the present agent is not particularly limited, but in order to make the adsorption of the active ingredient to the oral mucosa more effective, for example, a mass-to-volume ratio concentration of 0.01 to 1% by mass (w / v%) is preferable. If it is 1 w / v% or less, the characteristic odor is less likely to be felt and the feeling of use is less likely to be impaired. The content of the above active ingredient is more preferably 0.05 w / v% or more, even more preferably 0.1 w / v% or more, and more preferably 0.5 w / v% or less, and even more preferably 0.25 w / v% or less.

[0039] The agent may contain a cationic bactericidal component that may be contained in the oral composition in the method described above. When applying this agent to the active ingredient for which adsorption is to be improved, it is preferable to apply the agent so that the ratio of shellac to active ingredient contained in the agent is in the same range as the content ratio of shellac to active ingredient in the oral composition in the method described above. Furthermore, when the agent contains a cationic bactericidal component, when it is applied to the active ingredient for which adsorption is to be improved, it is preferable that the ratio of the cationic bactericidal component to the active ingredient contained in the agent is in the same range as the content ratio of the cationic bactericidal component to the active ingredient in the oral composition in the above-mentioned method. Furthermore, when the agent contains a cationic bactericidal component, it is preferable that the ratio of shellac to the cationic bactericidal component contained in the agent is in the same range as the content ratio of shellac to the cationic bactericidal component in the oral composition in the method described above. Furthermore, when the agent contains a cationic bactericidal component, it is preferable that when applied to an active ingredient whose adsorption is to be improved, the ratio of the shellac and cationic bactericidal component contained in the agent to the active ingredient whose adsorption is to be improved is applied in a range similar to the content ratio of the shellac and cationic bactericidal component to the active ingredient in the oral composition in the above-mentioned method.

[0040] As with the oral composition described above, this agent can be used for any purpose and in any dosage form depending on the type of active ingredient to be improved adsorption, and examples include mouthwash, mouth freshener, gargling agent, troche, chewing gum, etc. Among them, in order to ensure that the entire composition is sufficiently distributed in the oral cavity, a liquid oral composition that is used by placing an appropriate amount in the oral cavity is preferable, specifically, mouthwash and liquid toothpaste are mentioned. To prepare mouthwash and liquid toothpaste, for example, they may be prepared by a conventional method using water, ethanol, or the like as a solvent. Liquid toothpastes can also be used that contain abrasives such as calcium phosphate, calcium hydrogen phosphate, calcium pyrophosphate, calcium carbonate, aluminum oxide, aluminum hydroxide, anhydrous silicic acid, titanium oxide-coated mica, crystalline cellulose, and charcoal grains as necessary.

[0041] The agent may contain any other ingredients as long as they do not impair the effects of the present invention, and the types of ingredients may be the same as those of the oral composition in the method described above. EXAMPLES

[0042] The present invention will be further described below with reference to examples, but the present invention is not limited to the following examples.

[0043] <Preparation of oral composition> Example 1 Ethanol was mixed with POE cetyl ether to prepare solution 1. In a separate container, sodium hydroxide, shellac (manufactured by Nippon Shellac Kogyo Co., Ltd.) and purified water were mixed to prepare solution 2. In a separate container, dipotassium glycyrrhizinate (hereinafter also referred to as GK2) and purified water were added and mixed to prepare solution 3. After mixing solution 1 and solution 2, solution 3 was further added and stirred to prepare the oral composition of Example 1 with the blending ratio shown in Table 1.

[0044] Example 2 Solution 1 was prepared by mixing ethanol with POE cetyl ether. In a separate container, solution 2 was prepared by mixing sodium hydroxide, shellac (manufactured by Nippon Shellac Kogyo Co., Ltd.), and purified water. In yet another container, dipotassium glycyrrhizinate, cetylpyridinium chloride (hereinafter also referred to as CPC), and purified water were mixed to prepare solution 3. After mixing solution 1 and solution 2, solution 3 was added and stirred to prepare the oral composition of Example 2 so as to have the blending ratio shown in Table 1.

[0045] Comparative Example 1 Comparative Example 1 was prepared in the same manner as Example 1, except that shellac was not added, so as to have the blending ratio shown in Table 1.

[0046] Comparative Example 2 Comparative Example 2 was prepared in the same manner as Example 2, except that shellac was not added, so as to have the blending ratio shown in Table 1. The formulations of the oral compositions of the Examples and Comparative Examples are shown in Table 1. In Table 1, "-" means that the corresponding component is not included.

[0047] [Table 1]

[0048] (Examples 3 to 9) In the same manner as in Example 2, Examples 3 to 9 were prepared so as to have the blending ratios shown in Table 2.

[0049] (Examples 10 and 11) Examples 10 and 11 were prepared in the same manner as in Example 2, except that benzalkonium chloride or benzethonium chloride was used instead of CPC, so as to have the blending ratios shown in Table 2.

[0050] [Table 2]

[0051] <Adsorption test> The adsorption rate of the active ingredient GK2 to keratin (keratin powder), a type of protein contained in the oral mucosa, was determined using the following method. (i) First, 5 mL of the oral composition of each Example and Comparative Example was added to 200 mg of keratin powder (manufactured by Tokyo Chemical Industry Co., Ltd.) to obtain a treated sample. Separately, 5 mL of the oral composition was also prepared as a sample without treating the keratin powder (untreated sample). (ii) Next, the treated specimen obtained in (i) above was mixed in a shaker (manufactured by Yamato Scientific Co., Ltd.) at 200 rpm for 5 minutes, and the resulting mixture was centrifuged at 3,000 rpm for 10 minutes, and the supernatant was collected. (iii) Furthermore, the GK2 concentration in the supernatant obtained in (ii) above and the GK2 concentration in the oral composition in which the keratin powder had not been treated (untreated sample) were quantitatively analyzed by a quantitative method. (iv) Based on the GK2 concentration in the supernatant, the adsorption rate of GK2 to keratin powder was calculated using the following formula.

[0052]

number

[0053] The above test was carried out three times, and the average adsorption rate of GK2 to the keratin powder was calculated.

[0054] The results of the adsorption tests for Examples 1 and 2 and Comparative Examples 1 and 2 are shown in Table 3 and FIG.

[0055] [Table 3]

[0056] As can be seen from the results in Table 3, in the oral composition containing the active ingredients GK2 and shellac (Example 1), the adsorption rate of GK2 to keratin was approximately 1.5 times higher than in the oral composition containing only GK2 (Comparative Example 1). In addition, in the oral composition (Example 2) containing a cationic bactericidal component (CPC) in addition to the active ingredients GK2 and shellac, the adsorption rate of GK2 to keratin was found to be about 1.3 times higher than that of Example 1. In addition, the adsorption rate in Example 2 was found to be about 1.9 times higher than that in Comparative Examples 1 and 2. Considering that the adsorption rate of GK2 in the oral composition (Comparative Example 2) containing only the active ingredients GK2 and CPC was as low as that of the oral composition (Comparative Example 1) containing only GK2, it is considered that shellac and CPC act synergistically to improve the adsorption rate of GK2 to keratin.

[0057] The results of the adsorption tests for Examples 3 to 11 are shown in Table 4 and FIG.

[0058] [Table 4]

[0059] As can be seen from the results in Table 4, in Examples 3 to 9, which contain the cationic bactericidal component cetylpyridinium chloride in addition to the active ingredients GK2 and shellac, the adsorption rate of GK2 to keratin was found to be high even when the amount of each component was changed. In Example 10, which used benzalkonium chloride as a cationic bactericidal component, and Example 11, which used benzethonium chloride, the adsorption rate of GK2 to keratin was also high.

Claims

1. A method for improving adsorption of an active ingredient to the oral mucosa by using an oral composition containing the active ingredient and shellac.

2. The method of claim 1 , wherein the oral composition further comprises a cationic antiseptic component.

3. 3. The method of claim 1 or 2, which enhances adsorption of the active ingredient to keratin in the oral mucosa.

4. An active ingredient adsorption enhancer containing shellac for improving the adsorption of an active ingredient to the oral mucosa.

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