Composition for intraoral application

Abstract

To provide a composition for intraoral application that can express excellent applicability and retentivity to an intraoral affected area.SOLUTION: A composition for intraoral application contains following components (A)-(C): (A) at least one nonionic polymer selected from pullulan, polyvinylpyrrolidone, and hydroxypropyl methylcellulose of 0.01 mass% or more and 10 mass% or less, (B) at least one anionic polymer selected from a carboxyvinyl polymer, sodium carboxymethylcellulose, xanthan gum, and sodium polyacrylate of less than 0.5 mass%, and (C) water of 30 mass% or more and 95 mass% or less, with a viscosity at 25°C of 500 dPa s or more and 10000 dPa s or less.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to a composition for application in the oral cavity. [Background technology]

[0002] There is a high demand for compositions that can be applied directly to affected areas in the oral cavity, such as the gums and oral mucosa, and various compositions have been developed.

[0003] For example, Patent Document 1 discloses an oral ointment composition containing a cationic antibacterial agent, azulene, a lower monohydric alcohol, and a water-soluble vinyl polymer, which exerts an oral biofilm bactericidal effect. Patent Document 2 discloses an oral composition containing carbazochrome or a derivative thereof and a water-soluble polymer, which attempts to improve adhesion to the oral mucosa. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP 2013-43869 A [Patent Document 2] JP 2018-90585 A Summary of the Invention [Problem to be solved by the invention]

[0005] However, since the affected area in the oral cavity is constantly moistened by saliva, none of the compositions described in the above documents exhibit sufficient spreadability or adhesion to such moist affected areas, and further improvement is required.

[0006] That is, the present invention relates to a composition for application in the oral cavity that can exhibit excellent application properties and retention properties on affected areas in the oral cavity. [Means for solving the problem]

[0007] The inventors therefore conducted various studies and discovered that by containing a specific amount of water and adjusting the viscosity to a specific range, while containing a specific amount of a specific nonionic polymer, and limiting the content of a specific anionic polymer, it is possible to obtain a composition for application within the oral cavity that can exhibit excellent application and retention properties on saliva-wetted surfaces in the oral cavity.

[0008] Therefore, the present invention provides the following components (A) to (C): (A) One or more nonionic polymers selected from pullulan, polyvinylpyrrolidone, and hydroxypropyl methylcellulose, 0.01% by mass or more and 10% by mass or less (B) One or more anionic polymers selected from carboxyvinyl polymers, sodium carboxymethylcellulose, xanthan gum, and sodium polyacrylate: less than 0.5% by mass (C) Water: 30% by mass or more and 95% by mass or less and The present invention provides a composition for intraoral application having a viscosity at 25°C of 500 dPa·s or more and 10,000 dPa·s or less. Effect of the Invention

[0009] The composition for intraoral application of the present invention exhibits good spreadability and high adhesion to affected areas such as gums and oral mucosa that are constantly moistened by saliva, and exhibits excellent applicability, allowing the user to feel ease of application. Furthermore, even after the composition for intraoral application of the present invention is applied to affected areas such as gums and oral mucosa, it exhibits high retention, allowing the action of the composition to be sustained for a long period of time.

[0010] In addition, "spreadability" means the property of the composition spreading evenly over the surface of the affected area along the direction of application without forming lumps, i.e., when the composition is applied to the affected area, part of the composition is unevenly distributed. "Adhesiveness" means the property of the composition adhering to and remaining on the affected area when applied to a moist affected area such as the gums or oral mucosa. "Applicability" means a property that combines these "spreadability" and "adhesiveness". Furthermore, the term "retentiveness" refers to the property of a composition applied to an affected area to remain stably on the affected area over time. Furthermore, a "composition for application inside the mouth" is a composition that is intended to be applied directly to moist affected areas such as the gums or oral mucosa, as opposed to a composition for brushing the tooth surface, such as a toothpaste composition, and does not necessarily require rinsing after application. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0011] The present invention will be described in detail below. The composition for intraoral application of the present invention contains, as component (A), 0.01% by mass to 10% by mass of one or more nonionic polymers selected from pullulan, polyvinylpyrrolidone, and hydroxypropylmethylcellulose. By containing a specific amount of a specific nonionic polymer in this way, in the presence of a specific amount of water (C), coupled with the limited content of an anionic polymer (B) described below, it is possible to effectively prevent the composition from clumping on the application surface of a finger, a cotton swab, a finger cot, or other application implement when the composition is applied to a moist affected area such as the gums or oral mucosa while exhibiting an appropriate viscosity. Therefore, the composition does not form lumps on the application surface of the finger or applicator, and the composition spreads evenly over the moist affected area, exhibiting good applicability, and also exhibits high retention, remaining stably on the affected area for a long period of time even after application.

[0012] The nonionic polymer of component (A) is one or more selected from pullulan, polyvinylpyrrolidone, and hydroxypropyl methylcellulose. From the viewpoint of improving the applicability to the affected area in the oral cavity, polyvinylpyrrolidone is preferred. From the viewpoint of improving the adhesion and retention on the affected area in the oral cavity, one or two selected from pullulan and polyvinylpyrrolidone are preferred, or both pullulan and polyvinylpyrrolidone may be contained.

[0013] The content of component (A) in the composition for application in the oral cavity of the present invention is 0.01% by mass or more, preferably 0.1% by mass or more, more preferably 0.5% by mass or more, even more preferably 0.7% by mass or more, even more preferably 1% by mass or more, and even more preferably 1.1% by mass or more, from the viewpoint of enhancing adhesion and retention to the affected area in the oral cavity. The content of component (A) in the composition for application in the oral cavity of the present invention is 10% by mass or less, preferably 7% by mass or less, more preferably 5% by mass or less, and even more preferably 2% by mass or less, from the viewpoint of suppressing the occurrence of lumps when applied to the affected area and exhibiting excellent spreadability. The content of component (A) in the composition for application in the oral cavity of the present invention is 0.01% by mass or more and 10% by mass or less, preferably 0.1 to 7% by mass, more preferably 0.5 to 5% by mass, even more preferably 0.7 to 4% by mass, even more preferably 1 to 3.5% by mass, and even more preferably 1.1 to 2% by mass.

[0014] The composition for intraoral application of the present invention contains, as component (B), less than 0.5 mass% of one or more anionic polymers selected from carboxyvinyl polymer, sodium carboxymethylcellulose, xanthan gum, and sodium polyacrylate. That is, the content of component (B) in the composition for intraoral application of the present invention is more than 0 mass% and less than 0.5 mass%, or the composition for intraoral application of the present invention does not contain component (B). In this way, limiting the content of a specific anionic polymer can greatly contribute to achieving both good application property and high retention property without inhibiting the development of excellent spreadability and adhesiveness due to the above-mentioned component (A).

[0015] From the viewpoint of combining excellent application properties and good retention properties, the content of component (B) in the composition for application in the oral cavity of the present invention is less than 0.5% by mass, preferably 0.4% by mass or less, more preferably 0.27% by mass or less, even more preferably 0.2% by mass or less, still more preferably 0.08% by mass or less, even more preferably 0.01% by mass or less, and particularly preferably essentially 0% by mass, i.e., the composition for application in the oral cavity of the present invention does not contain component (B).

[0016] From the viewpoint of achieving both excellent application property and retention property, the mass ratio of the content of component (B) to the content of component (A) ((B) / (A)) is preferably 0.8 or less, more preferably 0.4 or less, even more preferably 0.25 or less, even more preferably 0.22 or less, and even more preferably the case where the composition for application within the oral cavity of the present invention does not contain component (B), i.e., the mass ratio of the content of component (B) to the content of component (A) ((B) / (A)) is 0.

[0017] The composition for intraoral application of the present invention contains 30% by mass or more and 95% by mass or less of water as component (C), which allows the above-mentioned components to be dispersed or dissolved well while also increasing the compatibility of the composition for intraoral application with saliva after application in the oral cavity, thereby contributing to the realization of excellent application property and retention.

[0018] The content of component (C) in the composition for intraoral application of the present invention is 30% by mass or more, preferably 40% by mass or more, more preferably 45% by mass or more, even more preferably 50% by mass or more, and is 95% by mass or less, preferably 90% by mass or less, more preferably 80% by mass or less, even more preferably 75% by mass or less, and even more preferably 60% by mass or less. In addition, the water of component (C) in the present invention means the total water contained in the composition to be applied intraoral, including not only the purified water etc. directly blended into the composition to be applied intraoral, but also the water contained in each of the blended components.

[0019] The composition for intraoral application of the present invention may further contain a medicinal component (D). By containing such component (D), the composition for intraoral application of the present invention exhibits excellent applicability and retention, and thus can provide the desired medicinal effect continuously over a wide area of ​​the affected area.

[0020] Specific examples of such component (D) include one or more selected from glycyrrhetinic acid, tocopherol acetate, hinokitiol, isopropylmethylphenol, copper chlorophyllin sodium, and carbazochrome. Among them, one or more selected from glycyrrhetinic acid and tocopherol acetate are preferred, and it is preferred to contain at least glycyrrhetinic acid, or it is preferred to contain both.

[0021] From the viewpoint of the effect of alleviating various symptoms in affected areas in the oral cavity, the content of component (D) in the composition for application in the oral cavity of the present invention is preferably 0.01 mass% or more, more preferably 0.02 mass% or more, even more preferably 0.1 mass% or more, and preferably 3.5 mass% or less, more preferably 3 mass% or less, even more preferably 2.5 mass% or less.

[0022] The composition for intraoral application of the present invention may further contain a nonionic surfactant (E). By containing such component (E), high adhesion of the composition for intraoral application to the affected area can be ensured.

[0023] Specific examples of such component (E) include one or more selected from sorbitan fatty acid esters such as sorbitan monocaprate, sorbitan monoundecylate, sorbitan monolaurate, sorbitan monotridecylate, sorbitan monomyristate, sorbitan monopalmitate, sorbitan monooleate, sorbitan trioleate, sorbitan tetraoleate, sorbitan sesquioleate, sorbitan monostearate, and sorbitan tristearate; and polyoxyethylene sorbitan fatty acid esters such as polyoxyethylene sorbitan monolaurate, polyoxyethylene sorbitan monomyristate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate. Of these, from the viewpoint of ensuring high adhesion, one or more selected from sorbitan monooleate, sorbitan sesquioleate, sorbitan monostearate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monostearate, and polyoxyethylene sorbitan monooleate are preferred.

[0024] From the viewpoint of ensuring a good usability, the content of component (E) in the composition for application in the oral cavity of the present invention is preferably 0.1% by mass or more, more preferably 0.5% by mass or more, even more preferably 1% by mass or more, preferably 10% by mass or less, more preferably 5% by mass or less, and even more preferably 3% by mass or less.

[0025] The composition for application in the oral cavity of the present invention may further contain a higher alcohol (F) having a carbon number of 12 to 22. By containing such component (F), the spreadability of the composition for application in the oral cavity of the present invention can be further improved.

[0026] Examples of such component (F) include one or more selected from cetanol, stearyl alcohol, lauryl alcohol, myristyl alcohol, and behenyl alcohol. Among them, from the viewpoint of effectively suppressing the generation of unwanted lumps of the composition during application, higher alcohols having 14 to 20 carbon atoms are preferred, and one or two selected from cetanol and stearyl alcohol are more preferred.

[0027] The content of component (F) in the oral composition of the present invention is preferably 0.5% by mass or more, more preferably 1% by mass or more, even more preferably 3% by mass or more, preferably 20% by mass or less, more preferably 15% by mass or less, and even more preferably 10% by mass or less, from the viewpoint of contributing to the provision of an appropriate viscosity and effectively suppressing the unwanted transfer and occurrence of lumps of the composition during application. The content of component (F) in the oral composition of the present invention is preferably 0.5 to 20% by mass, more preferably 1 to 15% by mass, and even more preferably 3 to 10% by mass.

[0028] In order to effectively suppress the generation of unnecessary lumps of the composition during application and to avoid the occurrence of unnecessary irritation, it is preferable that the content of ethanol in the composition for application in the oral cavity of the present invention is limited. Specifically, the content of ethanol in the composition for application in the oral cavity of the present invention is preferably less than 3% by mass, more preferably 2% by mass or less, and even more preferably 1% by mass or less, or the composition for application in the oral cavity of the present invention does not contain ethanol.

[0029] The composition for application in the oral cavity of the present invention may contain a polyhydric alcohol such as 1,3-butylene glycol, propylene glycol, polyethylene glycol, glycerin, sorbitol, xylitol, erythritol, reduced palatinose, and mannitol, in order to effectively suppress the formation of unnecessary lumps of the composition during application. The content of the polyhydric alcohol in the oral composition of the present invention is preferably 5 to 50% by mass, more preferably 10 to 40% by mass, and even more preferably 15 to 30% by mass, from the viewpoints of contributing to imparting an appropriate viscosity and effectively suppressing the occurrence of unnecessary lumps of the composition during application.

[0030] The composition for application within the oral cavity of the present invention may contain a saturated fatty acid having 14 to 18 carbon atoms, such as myristic acid, palmitic acid, or stearic acid, in order to effectively suppress the formation of unwanted lumps of the composition during application. The content of the saturated fat having 14 to 18 carbon atoms in the oral composition of the present invention is preferably 0.2 to 5 mass%, more preferably 0.4 to 3 mass%, and even more preferably 0.8 to 2 mass%, from the viewpoints of contributing to imparting appropriate viscosity and effectively suppressing the occurrence of unnecessary lumps of the composition when applied.

[0031] The composition for application within the oral cavity of the present invention may contain, in addition to the above-mentioned components, oily components such as hydrocarbon oils, ester oils, vegetable oils, silicone oils, etc.; pH adjusters such as sodium hydroxide; flavorings; sweeteners; colorants, etc., within the scope of not impairing the effects of the present invention.

[0032] From the viewpoint of facilitating long-term use of the composition for application in the oral cavity of the present invention, the pH of the composition for oral cavity use at 25° C. of the present invention is preferably 5 or more, more preferably 5.5 or more, even more preferably 6.2 or more, and preferably 10.5 or less, more preferably 10 or less, even more preferably 9.5 or less. The pH of the composition for oral cavity use at 25° C. of the present invention is preferably 5 to 10.5, more preferably 5.5 to 10, even more preferably 6.2 to 9.5.

[0033] The viscosity at 25°C of the composition for intraoral application of the present invention, from the viewpoint of exhibiting good spreadability and adhesion and thus providing excellent application properties, is preferably 500 dPa·s or more, more preferably 800 dPa·s or more, even more preferably 1500 dPa·s or more, even more preferably 1750 dPa·s or more, preferably 10000 dPa·s or less, more preferably 7000 dPa·s or less, even more preferably 5000 dPa·s or less, and even more preferably 3000 dPa·s or less. The viscosity can be measured by filling a viscosity measurement container, storing the mixture in an incubator at 25°C for 24 hours, and then using a Helipath viscometer (VISCOMETER TVB-10, manufactured by Toki Sangyo Co., Ltd.) at a measurement temperature of 25°C, using a rotor TC and a rotation speed of 2.5 r / min for 1 minute.

[0034] When using the composition for application in the oral cavity of the present invention, the composition may be placed directly on a fingertip or an application tool such as a cotton swab or a finger cot, and then applied to the desired affected area in the oral cavity. In order to fully enjoy the effects of the composition for application in the oral cavity of the present invention, it is preferable not to rinse after application to the affected area. In particular, when the composition for application in the oral cavity of the present invention contains a medicinal ingredient (D), this is a suitable mode of use for providing sufficient medicinal effects. EXAMPLES

[0035] The present invention will now be described in detail with reference to the following examples. In the tables, the content of each component is expressed as mass % unless otherwise specified.

[0036] [Examples 1 to 17, Comparative Examples 1 to 6] According to the formulations shown in Tables 1, 2 and 3, compositions for application in the oral cavity were prepared. The obtained compositions for intraoral application were used to carry out measurements and evaluations according to the following methods. The results are shown in Tables 1 to 3. All of the compositions for intraoral application had a pH of 9.

[0037] <pH Measurement> 45 mL of purified water was added to 5 g of each composition, and the solution was shaken well (25° C.). The pH of the solution was measured using a pH meter (HORIBA LAQUA pH / ION METER F53; 9615S JF15 (manufactured by Horiba, Ltd.)).

[0038] <Evaluation of malleability> 0.3 g of the composition for intraoral application was placed on a finger and applied to artificial leather (model gums) that had been evenly moistened with 100 μL of artificial saliva with a pressure of approximately 30 g, moving back and forth 10 times. The condition of the composition was visually inspected and the spreadability was evaluated according to the following criteria. A: Spreads evenly without lumps B: No lumps, spread fairly evenly C: Slight clumps observed and not uniform D: Small lumps were observed instead of uniformity. E: Large, uneven lumps were observed.

[0039] <Evaluation of adhesion to gums> 0.3 g of the composition for intraoral application was taken on a finger, and immediately after application to the gums, the entire amount of the composition attached to the finger was collected and the weight of the composition was measured.Then, the difference from before application was calculated to calculate the adhesion rate (%) to the gums, which was used as an index for evaluating the adhesion to the gums according to the following criteria. The adhesion rate was calculated as the average value of five expert panelists. A:Average 85% or more B: Average 75% to less than 85% C: Average 65% to less than 75% D: Average 55% to less than 65% E: Less than 55% average

[0040] <Evaluation of retention> 0.3 g of the composition for intraoral application was applied to a finger, and 15 minutes later, five expert panelists sensorily evaluated the retention (residual feeling) of the composition on the gums and scored according to the following criteria. The five panelists then calculated the average score and rated it on a five-level scale from A to E according to the following criteria. <Score> 5 points: The composition is strongly felt to be retained in the gums 4 points: Strong feeling of the composition remaining on the gums 3 points: Feeling the composition remaining on the gums 2 points: Somewhat felt like the composition was stuck to the gums 1 point: No feeling of retention in gums <Evaluation criteria> A: Average of 3.0 points or more B: Average score between 2.5 and 3.0 C: Average score between 2.0 and 2.5 D: Average 1.5 points or more and less than 2.0 points E: Average score below 1.5

[0041] [Table 1]

[0042] [Table 2]

[0043] [Table 3]

Claims

1. The following components (A), (C) and (F): (A) One or more nonionic polymers selected from pullulan, polyvinylpyrrolidone, and hydroxypropyl methylcellulose: 0.01% by mass or more and 10% by mass or less (C) Water 50% by mass or more and 95% by mass or less (F) higher alcohol having 12 to 22 carbon atoms, 3% by mass or more and 20% by mass or less and the content of one or more anionic polymers (B) selected from a carboxyvinyl polymer, sodium carboxymethylcellulose, xanthan gum, and sodium polyacrylate is more than 0 mass% and less than 0.5 mass%, or the component (B) is not contained, Does not contain ethanol and A composition for application inside the oral cavity, having a viscosity at 25°C of 800 dPa·s or more and 10,000 dPa·s or less.

2. A composition for application within the oral cavity as described in claim 1, wherein component (F) is cetanol and stearyl alcohol.

3. 3. A composition for application within the oral cavity according to claim 1 or 2, wherein the mass ratio ((B) / (A)) of the content of component (B) to the content of component (A) is 0.8 or less.

4. The composition for application in the oral cavity according to any one of claims 1 to 3, further comprising a medicinal ingredient (D) in an amount of 0.01% by mass or more and 3.5% by mass or less.

5. 5. A composition for application within the oral cavity according to claim 4, wherein component (D) is one or more selected from the group consisting of glycyrrhetinic acid, tocopherol acetate, hinokitiol, isopropylmethylphenol, sodium copper chlorophyllin, and carbazochrome.

6. A composition for application in the oral cavity according to any one of claims 1 to 5, which is used in a manner that does not require rinsing after application in the oral cavity.

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