JP6479526B2 - Aqueous oral composition - Google Patents

Description

  The present invention relates to an aqueous oral composition containing pantenol stably. More specifically, the present invention relates to an aqueous oral composition in which pantenol stability is maintained by combining panthenol with cetylpyridinium chloride and dipotassium glycyrrhizinate in combination.

  Panthenol is thought to activate cells and increase metabolism, and in daily necessities, it is used in the fields of hair care and skin care for the purpose of preventing itching, sunburn skin care and scalp care, etc., and improving metabolism in oral tissues It can be used for the purpose of On the other hand, panthenol is generally known to have poor stability when dissolved in water. For this reason, even if panthenol is incorporated into an aqueous preparation as a useful ingredient, it is difficult to maintain the desired effect, and in particular, when it is incorporated into an quasi-drug or pharmaceutical as an active ingredient, it has been a major issue. .

  As a past attempt to stabilize panthenol in an aqueous solution, a method using in combination with boric acid (Patent Document 1), a method using in combination with a compound having 3 or more hydroxyl groups in one molecule in addition to boric acid (Patent Document 2) ), A method of using allantoin and diphenhydramine in combination (Patent Document 3), and a method of using in combination with ibuprofenpiconol (Patent Document 4). All of these methods have been solved by the combined use of a pharmaceutical ingredient that cannot be used in a composition for oral use, and there has been no method for stably blending panthenol into an aqueous oral composition.

Japanese Patent Laid-Open No. 05-017355 JP 2002-265357 A JP 2006-335676 A Japanese Patent Laying-Open No. 2015-010060

  An object of the present invention is to provide an aqueous oral composition having extremely high panthenol stability.

  As a result of intensive studies in view of such circumstances, the present inventors have surprisingly found that cetylpyridinium chloride and dipotassium glycyrrhizinate are used together with panthenol, so that the stability of panthenol is extremely high even in an aqueous composition. As a result, the present invention has been completed.

That is, this invention provides the aqueous oral cavity composition of the following claim | item 1 -7.
Item 1.
An aqueous oral composition comprising 0.1 to 0.3% by mass of cetylpyridinium chloride, 0.4% by mass of dipotassium glycyrrhizinate, and 0.3 to 0.5% by mass of panthenol.
Item 2.
Item 2. The aqueous oral composition according to Item 1, wherein the composition is a quasi-drug or a pharmaceutical product.
Item 3.
Item 3. The aqueous oral composition according to any one of Items 1 or 2, wherein cetylpyridinium chloride is 0.2 to 0.3 mass% and panthenol is 0.3 to 0.4 mass%.
Item 4.
Item 4. The aqueous oral composition according to any one of Items 1 to 3, which contains 15% by mass or more of water based on the total amount of the composition.
Item 5.
Any of Items 1-4, wherein the composition is any one of a toothpaste, a liquid toothpaste, a mouthwash, an intraoral coating agent, a mouthwash, an oral bactericidal agent, a throat sterilizing agent, an oral throat drug, and a periodontal disease therapeutic agent. The aqueous oral composition of Claim 1.
Item 6.
Item 5. The aqueous oral composition according to any one of Items 1 to 4, wherein the composition is any one of a mouthwash, a bactericidal agent, a throat bactericidal agent, a buccal throat drug, and a periodontal disease therapeutic agent.
Item 7.
Item 3. The aqueous oral composition according to Item 2, wherein the composition is a pharmaceutical product.

  Since the aqueous oral composition of the present invention can realize the extremely high stability of panthenol, it is utilized particularly in quasi-drugs and pharmaceuticals used in the oral cavity and throat region containing panthenol as an active ingredient. Is optimal.

  The aqueous oral composition referred to in the present invention means a composition existing in a state where panthenol is completely dissolved, and specifically contains 15% by mass or more of water with respect to the total amount of the composition. Refers to the composition. Therefore, it includes not only liquid and liquid forms but also non-flowing forms such as paste and gel.

  In the present invention, panthenol is usually 0.3 to 0.5% by mass, most preferably 0.4% by mass, based on the total amount of the aqueous oral composition.

  In the present invention, cetylpyridinium chloride is usually 0.1 to 0.3% by mass, preferably 0.2 to 0.3% by mass, and most preferably 0.3% by mass based on the total amount of the aqueous oral composition. is there. If the amount is less than 0.1% by mass, a sufficient panthenol stabilizing effect may not be obtained, which is not preferable. If the amount exceeds 0.3% by mass, it may not be possible to obtain only the effect of blending. This is not preferred for economic reasons.

  In the present invention, glycyrrhizic acid dipotassium salt is blended in an amount of 0.4% by mass based on the total amount of the aqueous oral composition.

    The aqueous oral composition of the present invention includes toothpaste, gel toothpaste, liquid toothpaste, mouthwash, mouthwash, mouth spray, bad breath prevention agent, gum massage agent, oral moisturizer, tongue coating remover (auxiliary) agent Oral coating agents, oral germicides, throat germicides, oral throat drugs, periodontal disease therapeutic agents, and the like.

  As long as the composition for oral cavity is a range which does not impair the effect of this invention in addition to the said component, normally the arbitrary components mix | blended in an oral composition and a pharmaceutical can be mix | blended. Specific examples include surfactants, wetting agents, sweetening agents, flavoring agents, medicinal agents, pH adjusting agents, and thickeners.

  Examples of the surfactant include a nonionic surfactant and a zwitterionic surfactant, and a nonionic surfactant is more preferable. Examples of zwitterionic surfactants include N-alkyldiaminoethylglycine such as N-lauryldiaminoethylglycine and N-myristyldiethylglycine, N-alkyl-N-carboxymethylammonium betaine, 2-alkyl-1hydroxyethylimidazoline betaine Sodium etc. are mentioned. Nonionic surfactants include sugar fatty acid esters such as sucrose fatty acid esters and maltose fatty acid esters; sugar alcohol fatty acid esters such as maltitol fatty acid esters; sorbitan fatty acid esters such as sorbitan monolaurate; polyoxyethylene sorbitan mono Polyoxyethylene sorbitan fatty acid esters such as laurate and polyoxyethylene sorbitan monostearate; Fatty acid alkanolamides such as lauric acid diethanolamide; Polyoxyethylene alkyl ethers such as polyoxyethylene stearyl ether and polyoxyethylene oleyl ether; Mono Polyethylene glycol fatty acid esters such as polyethylene glycol oleate and polyethylene glycol monolaurate; lauryl glucosi , Alkyl glucosides such as decyl glucoside; polyglycerin fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene fatty acid esters, alkyl glucosides, polyoxyethylene hydrogenated castor oil, glycerin fatty acid esters, polyoxyethylene propylene block copolymers, etc. It is done. Among these nonionic surfactants, polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 2 to 150 is preferable, and among them, the average addition mole number of ethylene oxide is 40 to 100, and more preferably 40 to 40. 80 polyoxyethylene hydrogenated castor oil is particularly preferred. These nonionic surfactants and zwitterionic surfactants may be used alone or in combination of two or more, and may be blended in an amount of 0.01 to 0.5% by mass based on the total amount of the composition. It is preferable to set it as 0.01-0.3 mass%.

    As the wetting agent, a polyhydric alcohol other than a dihydric alcohol having 3 or 4 carbon atoms or ethyl alcohol can be blended. Examples of such polyhydric alcohols include sugar alcohols such as sorbitol, xylitol, maltitol, lactitol, erythritol, mannitol, and palatinit, ethylene glycol, polyethylene glycol, and the like. These wetting agents can be blended alone or in combination of two or more.

  Examples of the sweetener include saccharin sodium, stevioside, glycyrrhizin, xylit, sucralose, xylitol, palatinose, palatinit, erythritol, maltitol and the like. These sweeteners can be blended alone or in combination of two or more.

  As a flavoring agent, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, osimene, n-decyl alcohol, citronell, α-terpineol, methyl acetate, citronenyl acetate, methyl eugenol, cineol, linalool, ethyl Examples include perfume such as linalool, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil, and pimento oil. These flavoring agents may be used alone or in combination of two or more, and may be blended in an amount of 0.01 to 5% by weight, preferably about 0.05 to 1% by weight, based on the total amount of the composition.

  Examples of medicinal agents include enzymes such as dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme (Litec Enzyme); Agents: Thiamines, riboflavins, pyridoxines, vitamin B12, folic acid, niacin, biotin, vitamin C, vitamin A, vitamin D, vitamin E, vitamin K and other vitamins; other, glycerophosphate, chlorophyll, Examples include sodium chloride, caropeptide dodecyl diaminoethyl glycine, triclosan, and isopropylmethylphenol. These medicinal agents can be blended alone or in combination of two or more.

  Examples of thickeners include cationized hydroxyethyl cellulose; alkali metal alginates such as sodium alginate; gums such as propylene glycol alginate, xanthan gum, tragacanth gum, karaya gum, arabic gum, carrageenan; polyvinyl alcohol, sodium polyacrylate, carboxyvinyl polymer, Examples include polyvinyl pyrrolidone, carboxymethyl cellulose, and hydroxyethyl cellulose. These thickeners can be used alone or in combination of two or more, and can be blended in an amount of about 0.001 to 1% by mass based on the total amount of the composition.

  Examples of pH adjusters include citric acid, phosphoric acid, malic acid, gluconic acid, maleic acid, aspartic acid, succinic acid, glucuronic acid, fumaric acid, glutamic acid, adipic acid, and salts thereof, hydrochloric acid, sodium hydroxide, Examples thereof include potassium hydroxide and sodium silicate. These pH adjusters can be blended alone or in combination of two or more. The pH in the aqueous oral composition of the present invention is not particularly limited, but is usually pH 6 to 7, preferably pH 6.3 to 7.0, and more preferably pH 6.4 to 7.0. If the pH is lower than 6, it is not preferable because demineralization of enamel may occur, and if it exceeds 7, the intended effect of the present application may not be obtained.

  Hereinafter, the present invention will be specifically described, but the present invention is not limited to the following examples. In the following, “%” means “mass%” unless otherwise specified.

According to the composition described in Table 1, panthenol, cetylpyridinium chloride, and dipotassium glycyrrhizinate were dissolved in purified water to prepare a specimen. The amount of panthenol was measured for the specimen immediately after the adjustment. Next, 50 mL of these specimens were filled into a PET container (about 60 ml), left at 55 ° C. for 1 month, and the amount of panthenol after being left was measured. The “pantenol residual rate (%)” was calculated by the following calculation formula using the obtained two measured values. The obtained results are shown in Table 1. In addition, “-” in the table means that the operation is not performed. Further, panthenol was quantified according to the following method.

(Calculation formula)
(Panthenol residual ratio) = 100 * [(quantitative value at 55 ° C., 1M) / (quantitative value immediately after production)]

(Quantitative test method for panthenol)
1 g of a sample was accurately weighed and water was added to make 50 mL to obtain a sample solution. Separately, a standard panthenol was precisely weighed, and water was added to accurately measure up and used as a standard solution. Note that the amount of the sample weighed and the amount of the measured up amount are appropriately adjusted according to the amount of panthenol contained in the subject.

(Measurement conditions for liquid chromatography)
Detector: UV-visible spectrophotometer (measurement wavelength: 208 nm)
Column: Octadecylsilylated silica gel for liquid chromatography Column temperature: Constant temperature around 40 ° C. Mobile phase: 0.01 mol / L pH2.5 phosphate buffer / acetonitrile mixture for liquid chromatography (19: 1)

  As shown in Table 1, in the range of 0.3 to 0.5% by mass of panthenol, in the range of 0.4% by mass of dipotassium glycyrrhizinate and 0.1 to 0.3% by mass of cetylpyridinium chloride It was found that very high panthenol stability over time can be realized. In particular, it was found that the panthenol blending amount was 0.3 to 0.4% by mass and the cetylpyridinium chloride blending amount was 0.2 to 0.3% by mass.

  Hereinafter, formulation examples of the aqueous oral composition of the present invention will be shown. In the following, “%” means “mass%” unless otherwise specified.

Formulation Example 1 Toothpaste

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.4
Dipotassium glycyrrhizinate 0.4
Sorbit liquid (70%) 30
Dentifrice Calcium Hydrogen Phosphate 15
Anhydrous calcium hydrogen phosphate 10
Propylene glycol 2
Polyoxyethylene hydrogenated castor oil (60E.O.) 2
Polyethylene glycol monooleate (10E.O.) 2
Hydroxyethyl cellulose 1.2
Titanium oxide 0.8
Sodium monofluorophosphate 0.7
Hydroxypropyl methylcellulose 0.2
Tocopherol acetate 0.1
Triclosan 0.02
Isopropyl methylphenol 0.05
Saccharin sodium 0.3
Paraben 0.3
Fragrance 1
Purified water balance
Total 100

Formulation Example 2 Toothpaste

Component content <br/> Cetylpyridinium chloride 0.2
Panthenol 0.4
Dipotassium glycyrrhizinate 0.4
Sorbit liquid (70%) 30
Silicic anhydride 20
Hydroxyapatite 5
Sodium carboxymethylcellulose 1.2
Sucrose fatty acid ester 1
Polyethylene glycol monooleate (10E.O.) 0.8
Aluminum lactate 0.2
Mica titanium 0.2
Methylparaben 0.2
Pyridoxine hydrochloride 0.05
Hinokitiol 0.04
Sucralose 0.02
Purified water balance
Total 100

Formulation Example 3 Toothpaste

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.3
Dipotassium glycyrrhizinate 0.4
Erythritol 40
Silicic anhydride 15
Reduced palatinose 2
Xanthan gum 1.5
Light anhydrous silicic acid 1
Crystalline cellulose 1
Polyoxyethylene stearyl ether (7E.O.) 1
Sodium fluoride 0.2
Dextranase 0.2
Methylparaben 0.2
Gunjo Pink 0.2
Polyoxyethylene lauryl ether (5E.O.) 0.1
Polyethylene glycol monooleate (10E.O.) 0.1
Purified water balance
Total 100

Formulation Example 4 Toothpaste

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.5
Dipotassium glycyrrhizinate 0.4
Concentrated glycerin 40
Polyethylene glycol 600 10
Silicic anhydride 10
Sodium chloride 5
Zeolite 3
Sodium alginate 1.5
Palm oil fatty acid amidopropyl betaine 0.6
Crystalline cellulose / Carmellose sodium 0.3
Lysozyme chloride 0.2
Sodium ascorbate 0.05
Copper chlorophyllin sodium 0.05
Green No. 3 0.002
Yellow No. 4 0.002
Purified water balance
Total 100

Formulation Example 5 Liquid dentifrice

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.4
Dipotassium glycyrrhizinate 0.4
Sorbit liquid (60%) 20
Concentrated glycerin 15
Reduced palatinose 10
Potassium nitrate 5
Polyethylene glycol 400 4
Glycerin fatty acid ester 2
Hydroxypropyl methylcellulose 1.8
Xanthan gum 0.3
Polyoxyethylene hydrogenated castor oil (60E.O.) 0.3
Trisodium citrate 0.2
Hesperidin 0.1
Anhydrous citric acid 0.05
Saccharin sodium 0.1
Perfume appropriate amount
Purified water balance
Total 100

Formulation Example 6 Oral Gel

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.3
Dipotassium glycyrrhizinate 0.4
Sorbit liquid (60%) 20
Xylitol 10
Concentrated glycerin 8
Carboxymethyl cellulose
(Degree of etherification: 1.00 to 1.06) 2
Propylene glycol 2
Polyoxyethylene hydrogenated castor oil (60E.O.) 0.4
Xanthan gum 0.2
Sodium alginate 0.2
Trisodium citrate 0.2
Pyridoxine hydrochloride 0.12
Sodium ascorbate 0.1
Anhydrous citric acid 0.05
Perfume appropriate amount
Purified water balance
Total 100

Formulation Example 7 Oral coating agent

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.4
Dipotassium glycyrrhizinate 0.4
Sorbit liquid (60%) 20
Concentrated glycerin 15
Reduced palatinose 10
Propylene glycol 3
O- [2-hydroxy-3-chloride]
(Trimethylammonio) propyl]
Hydroxyethyl cellulose 2
Sodium alginate 0.5
Sodium dihydrogen phosphate 0.25
Polyoxyethylene hydrogenated castor oil (60E.O.) 0.2
Dipotassium glycyrrhizinate 0.15
Sodium monohydrogen phosphate 0.1
Saccharin sodium 0.1
Perfume appropriate amount
Purified water balance
Total 100

Formulation Example 10 Mouse Spray

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.4
Dipotassium glycyrrhizinate 0.4
Ethanol 30
Glycerin 15
Polyoxyethylene hydrogenated castor oil (60E.O.) 1.5
Menthol 1
Saccharin 0.1
Sodium citrate 0.2
Purified water balance
Total 100

Formulation Example 11 Mouthwash

Component content <br/> Cetylpyridinium chloride 0.3
Panthenol 0.5
Dipotassium glycyrrhizinate 0.4
Glycerin 5
Propylene glycol 2
Sodium azulene sulfonate 1
Polyoxyethylene hydrogenated castor oil (60E.O.) 0.5
Palm oil fatty acid amidopropyldimethylaminoacetic acid betaine 0.2
L-Menthol 0.5
Sodium benzoate 0.2
Sodium citrate 0.07
Citric anhydride 0.01
Saccharin sodium 0.01
Fragrance 0.1
Purified water balance
Total 100

Claims (3)

An aqueous oral composition comprising 0.1 to 0.3% by mass of cetylpyridinium chloride, 0.4% by mass of dipotassium glycyrrhizinate, and 0.3 to 0.5% by mass of panthenol (however, Allantoin, allantoin chlorohydroxyaluminum, or oral compositions containing allantoin hydroxyaluminum are excluded) .   The aqueous oral composition according to claim 1, wherein the composition is a quasi-drug or a pharmaceutical product.   The aqueous oral composition according to any one of claims 1 and 2, wherein cetylpyridinium chloride is 0.2 to 0.3 mass% and panthenol is 0.3 to 0.4 mass%.