Oral composition

Abstract

To provide a composition for oral cavity comprising an inorganic basic compound which suppresses reduction in viscosity with time.SOLUTION: There is provided a composition for oral cavity which comprises liquid paraffin, a polyhydric alcohol, at least two polyglycerol fatty acid esters and at least one inorganic basic compound selected from the group consisting of an alkali metal hydroxide, an alkaline earth metal hydroxide, an alkali metal carbonate, an alkali metal hydrogen carbonate, an alkali metal monohydrogen phosphate and an alkali metal silicate, wherein the content mass ratio of the polyhydric alcohol to the liquid paraffin in the composition is 0.21 to 0.71.SELECTED DRAWING: None

Description

Technical Field

[0001] The present disclosure relates to oral compositions and the like.

Background Art

[0002] Among the components that can be contained in oral compositions, there are quite a few compounds that are unstable under acidic conditions. In order to formulate such compounds into a preparation, it is necessary to increase the pH.

Prior Art Documents

Patent Documents

[0003]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0004] An object of the present disclosure is to provide an oral composition containing an inorganic basic compound, in which a decrease in viscosity over time is suppressed.

Means for Solving the Problems

[0005] When the inventors prepared an oral composition containing sodium hydroxide to increase the pH, they found that the viscosity of the oral composition decreased over time.

[0006] As a result of intensive studies, the inventors found that by adding at least two types of polyglycerol fatty acid esters to an oral composition containing sodium hydroxide, it is possible to suppress a decrease in viscosity over time of the composition, and further improvements were made.

[0007] The present disclosure includes, for example, the subject matters described in the following items. Item 1. Liquid paraffin, Polyhydric alcohol, At least two kinds of polyglycerol fatty acid esters, and at least one or more inorganic basic compounds selected from the group consisting of alkali metal hydroxides, alkaline earth metal hydroxides, alkali metal carbonates, alkali metal hydrogen carbonates, alkali metal monohydrogen phosphates, and alkali metal silicates An oral composition containing In the composition, the mass ratio of the polyhydric alcohol to liquid paraffin is 0.21 to 0.71. An oral composition Item 2. The oral composition according to Item 1, wherein the polyglycerol fatty acid ester is an ester of a saturated or unsaturated fatty acid having 8 to 24 carbon atoms and polyglycerol Item 3. The oral composition according to Item 1 or 2, wherein the at least two kinds of polyglycerol fatty acid esters are at least two kinds of polyglycerol fatty acid esters selected from the group consisting of polyglyceryl-10 laurate, polyglyceryl-10 myristate, and polyglyceryl-10 stearate Item 4. The oral composition according to any one of Items 1 to 3, wherein the pH of the composition diluted 4-fold with water is 6 to 11 Item 5. The oral composition according to any one of Items 1 to 4, wherein the polyhydric alcohol is glycerin Item 6. The oral composition according to any one of Items 1 to 5, wherein the water content in the composition is 5% by mass or less Item 7. The oral composition according to any one of Items 1 to 6, which is a non-aqueous composition [Effect of the Invention]

[0008] An oral composition containing an inorganic basic compound, in which a decrease in viscosity over time is suppressed, is provided [Modes for Carrying Out the Invention]

[0009] The present disclosure includes an oral composition containing liquid paraffin, a polyhydric alcohol, at least two kinds of polyglycerol fatty acid esters, and an inorganic basic compound. In this specification, the oral composition may be referred to as "the oral composition of the present disclosure".

[0010] As the liquid paraffin, light liquid paraffin is preferred. In this specification, light liquid paraffin refers to those having a specific gravity of 0.830 to 0.870 and a viscosity of less than 37 mm 2 / s. The viscosity is calculated by the capillary viscometer method according to the description in the seventeenth revised Japanese Pharmacopoeia. As the kinematic viscosity of light liquid paraffin, for example, it can be less than about 45 mm 2 / s.

[0011] In the oral composition of the present disclosure, the content of liquid paraffin is not particularly limited, but can be, for example, about 57 to 78% by mass based on the total mass of liquid paraffin, polyhydric alcohol, and polyglycerol fatty acid ester. The upper or lower limit of this range can be, for example, about 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75, 76, or 77% by mass. More specifically, for example, it can be about 58 to 77% by mass.

[0012] Examples of the polyhydric alcohol include glycerin, propanediol, butylene glycol, polyethylene glycol, and the like. As propanediol, both propylene glycol (1,2-propanediol) and 1,3-propanediol can be preferably used. As butylene glycol, 1,3-butylene glycol is preferred. As polyethylene glycol, the average number of added moles of ethylene oxide units (EO) is preferably 4 to 20 (4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20). Among them, glycerin is preferred as the polyhydric alcohol. The polyhydric alcohol can be used alone or in combination of two or more kinds.

[0013] In the oral composition of the present disclosure, the content of the polyhydric alcohol is not particularly limited, but can be, for example, about 17 to 38% by mass based on the total mass of liquid paraffin, polyhydric alcohol, and polyglycerol fatty acid ester. The upper limit or lower limit of this range may be, for example, about 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, or 37% by mass. More specifically, it may be, for example, about 18 to 37% by mass.

[0014] In the oral composition of the present disclosure, the mass ratio of the polyhydric alcohol to the liquid paraffin can be, for example, about 0.21 to 0.71. The upper limit or lower limit of this range may be, for example, about 0.22, 0.23, 0.24, 0.25, 0.3, 0.35, 0.4, 0.45, 0.5, 0.55, 0.6, 0.65, or 0.7. More specifically, it may be, for example, about 0.25 to 0.65.

[0015] Examples of the polyglycerol fatty acid ester include esters of saturated or unsaturated fatty acids having 8 to 24 carbon atoms and polyglycerol. The upper limit or lower limit of the number of carbon atoms may be, for example, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, or 23. More specifically, it may be, for example, 10 to 20. The fatty acid may be a saturated fatty acid or an unsaturated fatty acid. More preferably, it is a saturated fatty acid. Also, the fatty acid may be a straight-chain fatty acid or a branched fatty acid. More preferably, it is a straight-chain fatty acid. Examples of the fatty acid include capric acid, lauric acid, myristic acid, stearic acid, palmitic acid, palmitoleic acid, margaric acid, oleic acid, linoleic acid, behenic acid, isocapric acid, isolauric acid, isomyristic acid, isostearic acid, isopalmitic acid, isopalmitoleic acid, isomargaric acid, isooletic acid, isolinoleic acid, isobehenic acid, etc. Among them, capric acid, lauric acid, myristic acid, stearic acid, oleic acid, and isostearic acid are preferred, and lauric acid, myristic acid, and stearic acid are more preferred. Also, natural fatty acids such as coconut oil fatty acid and palm oil fatty acid containing these fatty acids may be used. Also, the polyglycerol fatty acid ester is preferably a mono, di, tri, tetra, penta, or cycloester compound of the fatty acid and polyglycerol, and more preferably a mono, di, or triester compound. Polyglycerol preferably contains an average of 4 to 12 glycerol units. The upper or lower limit of the glycerol units may be, for example, 5, 6, 7, 8, 9, 10, or 11. More specifically, for example, it may be 5 to 11. Examples of preferred polyglycerol fatty acid esters include polyglyceryl-n caprate, polyglyceryl-n laurate, polyglyceryl-n myristate, polyglyceryl-n stearate, polyglyceryl-n oleate, polyglyceryl-n dimyristate, polyglyceryl-n distearate, polyglyceryl-n diisostearate, polyglyceryl-n trilaurate, polyglyceryl-n trimyristate (n represents the number of glycerol units), etc. More preferably, they are polyglyceryl-n laurate, polyglyceryl-n myristate, and polyglyceryl-n stearate, and polyglyceryl-10 laurate, polyglyceryl-10 myristate, and polyglyceryl-10 stearate can be particularly preferably used. It is preferable to use at least two or more polyglycerol fatty acid esters in combination. Preferred combinations of polyglycerol fatty acid esters include polyglyceryl-n myristate (more preferably polyglyceryl-10 myristate) and polyglyceryl-n stearate (more preferably polyglyceryl-10 stearate), polyglyceryl-n laurate (more preferably polyglyceryl-10 laurate) and polyglyceryl-n myristate (more preferably polyglyceryl-10 myristate), and polyglyceryl-n laurate (more preferably polyglyceryl-10 laurate) and polyglyceryl-n stearate (more preferably polyglyceryl-10 stearate).

[0016] In the oral composition of the present disclosure, the content of the polyglycerol fatty acid ester is not particularly limited, but can be, for example, about 0.3 to 7% by mass as the total amount of the polyglycerol fatty acid ester with respect to the total mass of liquid paraffin, polyhydric alcohol, and polyglycerol fatty acid ester. The upper or lower limit of this range may be, for example, about 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1, 2, 3, 4, 5, or 6% by mass. More specifically, for example, it may be about 0.4 to 6% by mass.

[0017] When two polyglycerol fatty acid esters are contained in the oral composition of the present disclosure, the mass ratio of the contained polyglycerol fatty acid esters can be, for example, about 5:1 to 1:5. The upper or lower limit of this range may be, for example, about 4:1, 3:1, 2:1, 1:1, 1:2, 1:3, or 1:4. More specifically, for example, it may be about 4:1 to 1:4.

[0018] Examples of the inorganic basic compound include alkali metal hydroxides such as sodium hydroxide and potassium hydroxide; alkaline earth metal hydroxides such as calcium hydroxide; alkali metal carbonates such as sodium carbonate and potassium carbonate; alkali metal hydrogen carbonates such as sodium hydrogen carbonate and potassium hydrogen carbonate; alkali metal monohydrogen phosphates such as sodium monohydrogen phosphate; and alkali metal silicates such as sodium silicate. Among them, alkali metal hydroxides such as sodium hydroxide and potassium hydroxide are preferred, and sodium hydroxide is more preferred. The inorganic basic compound can be used alone or in combination of two or more.

[0019] In the oral composition of the present disclosure, the content of the inorganic basic compound can be appropriately set according to the type of the inorganic basic compound. For example, it can be about 0.005 to 0.3% by mass. The upper limit or the lower limit of the range may be, for example, about 0.006, 0.007, 0.008, 0.009, 0.01, 0.02, 0.03, 0.04, 0.05, 0.06, 0.07, 0.08, 0.09, 0.1, or 0.2% by mass. More specifically, for example, it may be about 0.006 to 0.2% by mass.

[0020] The oral composition of the present disclosure can have a pH of about 6 to 11 at room temperature (25°C) of the composition obtained by diluting the oral composition 4-fold with water. The upper limit or the lower limit of the range may be, for example, about 6.1, 6.2, 6.3, 6.4, 6.5, 7.0, 7.5, 8.0, 8.5, 9.0, 9.5, 10.0, or 10.5. More specifically, for example, it may be about 6.1 to 10.5.

[0021] The oral composition of the present disclosure may contain water as long as a decrease in viscosity over time is suppressed. Specifically, for example, the water content is preferably about 5% by mass or less. The upper limit of the range of the water content may be about 4, 3, 2, 1, or 0.5% by mass. Further, the oral composition of the present disclosure is more preferably a composition that does not contain water (i.e., a non-aqueous composition). However, in the case where the composition contains an amount of water that is difficult to remove as inevitable impurities, it is included in the "non-aqueous composition" in this specification.

[0022] The oral composition of the present disclosure contains the above-described components and may further contain known components that can be incorporated into the oral composition. Examples of such known components include surfactants other than polyglycerol fatty acid esters, abrasives, humectants, foaming agents, fragrances, activators, sweeteners, preservatives, colorants, stabilizers, flavoring agents, astringents, thickeners, other medicinal agents, and the like. Such known components can be used individually or in combination of two or more.

[0023] As a method for preparing the oral composition of the present disclosure, for example, there is a method in which a polyhydric alcohol, a polyglycerol fatty acid ester, and an inorganic basic compound are first stirred and mixed, and then while continuing stirring, liquid paraffin is gradually added to the mixture and mixed. The mixing can be carried out by a known stirrer (for example, a disperser, etc.). Since it may not be uniformly mixed when a large amount of liquid paraffin is added at once, it is preferable to add it little by little.

[0024] The oral composition of the present disclosure preferably has a viscosity of about 20 to 480 Pa·s as measured under the following conditions. The upper or lower limit of this range may be, for example, about 25, 30, 35, 40, 45, 50, 100, 150, 200, 250, 300, 350, 400, 450, 460, or 470 Pa·s. More specifically, for example, it may be about 25 to 470 Pa·s. The viscosity measurement was carried out using a B-type viscometer (manufactured by Brookfield, spindle T-F, rotation speed: 10 rpm / 1 minute) on the oral composition filled in a 70 mL glass beaker after keeping it at 30°C for 30 minutes in a constant temperature bath at 30°C to bring the composition to 30°C.

[0025] The oral composition of the present disclosure preferably has a "two-week viscosity reduction rate (%) = (initial viscosity - viscosity after two weeks) / initial viscosity × 100" of 50% or less when left standing at room temperature (25°C) for two weeks after preparation. The upper or lower limit of this range may be, for example, about 40, 30, 20, 10, 0, -5, -10, -15, -20, -25, -30, -40, -50, -60, -70, -80, -90, -100, -120%. More specifically, for example, it may be about -120 to 40%.

[0026] The oral composition of the present disclosure is preferably an oral composition in which the decrease in viscosity over time is suppressed. Further, the oral composition of the present disclosure is more preferably an oral composition having good viscosity stability.

[0027] The oral composition of the present disclosure is preferably an emulsion composition. Further, the oral composition of the present disclosure preferably does not cause phase separation when left standing at room temperature (25°C) for two weeks after preparation. The shape of the oral composition of the present disclosure is not particularly limited, but for example, it is preferably in the form of a gel or a cream.

[0028] The form of the oral composition of the present disclosure is not particularly limited, but for example, it can be in the form (dosage form) of an ointment, a paste, a pasta, a gel, a liquid, a spray, a mouthwash, a liquid dentifrice, a toothpaste, a coating agent, etc. The oral composition of the present disclosure can be used, for example, as pharmaceuticals and quasi-drugs. Further, the oral composition of the present disclosure can be used, for example, as a carrier for an oral composition.

[0029] In addition, in this specification, the term "comprising" includes "consisting essentially of" and "consisting of". Further, the present disclosure includes all arbitrary combinations of the constituent elements described in this specification.

[0030] Moreover, the various characteristics (properties, structures, functions, etc.) described for each embodiment of the present disclosure above may be combined in any manner in identifying the subject matter encompassed by the present disclosure. That is, the present disclosure encompasses all subject matters consisting of any combination of the combinable characteristics described in this specification.

Examples

[0031] The content of the present disclosure will be specifically described using the following examples. However, the present disclosure is not limited to these in any way. In the following, unless otherwise specified, the experiments are carried out under atmospheric pressure and normal temperature conditions. Also, unless otherwise specified, "%" means "% by mass". Further, the blending amount values of each component described in each table indicate "% by mass" unless otherwise specified.

[0032] Composition Preparation According to the formulation shown in Table 1 below, a composition was prepared. More specifically, glycerin, various polyglycerol fatty acid esters, and sodium hydroxide were added to a container (beaker) and stirred and mixed with a disperser. Then, while continuing stirring, light liquid paraffin was added little by little. The light liquid paraffin used had a kinematic viscosity of 12.56 mm 2 / s (40°C) and a density (specific gravity) of 0.843. The viscosity of the light liquid paraffin calculated from the kinematic viscosity and density was 10.59 mm 2It was / s.

[0033] Physical Property Measurement The pH of the composition itself at room temperature (25 °C) and the pH of the slurry obtained by diluting the composition 4-fold with distilled water were measured. Also, the freshly prepared composition was filled into a 70 mL glass beaker and visually observed to confirm the presence or absence of phase separation. Those that maintained a gel-like (emulsified state) without phase separation were evaluated as ○, and those in which the oil phase had separated were evaluated as × (preparation feasibility). Further, after keeping the 70 mL glass beaker in a constant temperature bath at 30 °C for 30 minutes to bring the composition to 30 °C, the viscosity of the composition was measured using a B-type viscometer (manufactured by Brookfield, spindle T-F, rotation speed: 10 rpm / 1 minute) (initial viscosity). After further standing at room temperature (25 °C) for 2 weeks, the preparation feasibility and viscosity were evaluated again in the same manner. Regarding the viscosity, the "viscosity reduction rate after 2 weeks (%) = (initial viscosity - viscosity after 2 weeks) / initial viscosity × 100" was calculated. The results are shown in Table 1.

[0034]

Table 1

[0035] As shown in Table 1, it was confirmed that the compositions of Examples 1 to 9 did not undergo phase separation and maintained a gel-like (emulsified state) both immediately after preparation and after standing at room temperature (25 °C) for 2 weeks. Also, it was found that the compositions of Examples 1 to 9 had a viscosity reduction rate after 2 weeks (%) of 50% or less, and the decrease in viscosity over time was suppressed.

Claims

1. Liquid paraffin, at least one polyhydric alcohol selected from the group consisting of glycerin, propylene glycol, and 1,3 - propanediol, at least two polyglycerol fatty acid esters, and at least one inorganic basic compound selected from the group consisting of alkali metal hydroxides, alkaline earth metal hydroxides, alkali metal carbonates, alkali metal hydrogen carbonates, alkali metal monohydrogen phosphates, and alkali metal silicates An oral composition containing The polyglycerol fatty acid ester is an ester of a saturated or unsaturated fatty acid having 8 to 18 carbon atoms and a polyglycerol containing 4 to 12 glycerol units, In the composition, the mass ratio of the polyhydric alcohol to the liquid paraffin is 0.21 to 0.

71. An oral composition.

2. The at least two polyglycerol fatty acid esters are at least two selected from the group consisting of polyglyceryl - n caprate, polyglyceryl - n laurate, polyglyceryl - n myristate, polyglyceryl - n stearate, polyglyceryl - n oleate, polyglyceryl - n dimyristate, polyglyceryl - n distearate, polyglyceryl - n diisostearate, polyglyceryl - n trilaurate, and polyglyceryl - n trimyristate (n represents the number of glycerol units and is 4 to 12), The oral composition according to Claim 1.

3. The at least two polyglycerol fatty acid esters are at least two selected from the group consisting of polyglyceryl - n laurate, polyglyceryl - n myristate, polyglyceryl - n stearate, and polyglyceryl - n oleate (n represents the number of glycerol units and is 4 to 12), The oral composition according to Claim 1.

4. The oral composition according to any one of claims 1 to 3, wherein the at least two polyglycerol fatty acid esters are at least two polyglycerol fatty acid esters selected from the group consisting of polyglyceryl-10 laurate, polyglyceryl-5 myristate, polyglyceryl-10 myristate, polyglyceryl-10 stearate, and polyglyceryl-5 oleate.

5. The oral composition according to any one of claims 1 to 4, wherein the pH of the composition obtained by diluting the oral composition four-fold with water is 6 to 11.

6. The oral composition according to any one of claims 1 to 5, wherein the polyhydric alcohol is glycerin.

7. The oral composition according to any one of claims 1 to 6, wherein the water content in the composition is 5% by mass or less.

8. The oral composition according to any one of claims 1 to 7, which is a non-aqueous composition.

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