JP2012056870A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for oral cavity, which contains a hesperidin compound and is excellent in dispersion stability and diffusivity in the oral cavity of the hesperidin compound.SOLUTION: There is provided the composition for the oral cavity, which is prepared by adding the hesperidin compound to a composition comprising one or more kinds selected from xanthan gum and sodium alginate and a cellulosic thickener, and enhances the dispersion stability, usability and diffusivity of the hesperidin in the composition for the oral cavity in the oral cavity, and enables that the hesperidin reaches every corner in the oral cavity, such as embrasure and boundary lines between teeth and gums.

Description

  The present invention relates to an oral composition containing hesperidins and excellent in usability. More specifically, the present invention relates to an oral composition containing at least one selected from the group consisting of xanthan gum and sodium alginate and a cellulose-based thickener.

  Since hesperidin has excellent functions such as a remineralization promoting effect, it is desired to blend and apply it to an oral composition. Since hesperidin has low solubility in water, when hesperidin is added to the oral composition in an amount sufficient to obtain the effect, it can hardly be dissolved in the composition, so hesperidin is blended in a dispersed state. It will be. When developing such a dispersion composition, it is necessary to satisfy the usability and stability in use and distribution in consideration of the Japanese climate where the temperature changes greatly. In addition, hesperidin particles are quickly and sufficiently diffused in the oral cavity to adhere to and remain in the target site in order to leave hesperidin in the hourglass space (tooth gap between teeth) and the tooth gums, where caries tend to occur. It is necessary to let

  Conventionally, in order to increase the dispersion stability of a composition, a thickener such as a water-soluble polymer has been added to increase the viscosity of the composition, or to reduce the specific gravity difference between the dispersoid and the dispersion medium. ing. For example, a method of obtaining a composition having good dispersion stability by adding a crosslinking agent to an aqueous solution of polysaccharides such as agar and gellan gum and shearing while gelling (Patent Document 1), an abrasive having a specific specific volume A method of obtaining a composition having good dispersion stability (Patent Document 2) by blending a specific amount and setting the blending amount of the dispersant and the viscosity of the composition within a specific range has been proposed. However, even with these contrivances, the above conditions cannot be satisfied, and no satisfactory solution has yet been found.

JP 2005-104966 A Japanese Patent Laid-Open No. 10-167940

  An object of the present invention is to provide an oral composition having high dispersion stability of hesperidins, easy to use, and good diffusibility and persistence in the oral cavity.

  As a result of intensive studies in view of such circumstances, the present inventors have formulated hesperidin in a composition containing at least one selected from xanthan gum and sodium alginate and a cellulose-based thickener, whereby the dispersion stability of hesperidin is improved. The present invention has been completed by finding that an oral composition that is high and easy to use and has good diffusibility and persistence in the oral cavity can be obtained.

That is, this invention provides the composition for oral cavity of the following items 1-4 especially.
Item 1. An oral composition comprising one or more selected from the group consisting of xanthan gum and sodium alginate, a cellulose-based thickener, and hesperidins.
Item 2. The oral cavity composition according to Item 1, wherein the viscosity at 30 ° C is 10,000 to 65,000 mPa · s.
Item 3. Item 3. The oral composition according to any one of Items 1 and 2, wherein 0.2 to 2% by mass of one or more selected from the group consisting of xanthan gum and sodium alginate is blended.
Item 4. Item 4. The composition for oral cavity according to any one of Items 1 to 3, wherein 0.5 to 3% by mass of a cellulosic thickener is blended.

  The composition for oral cavity of the present invention improves the dispersion stability of hesperidin in the composition for oral cavity by blending hesperidin into a composition blended with one or more selected from xanthan gum and sodium alginate and a cellulose-based thickener. It is easy to use and has good diffusibility and persistence in the oral cavity, allowing hesperidin to reach the corners of the oral cavity, such as the hourglass space (tooth gap) and the gum boundary It becomes possible.

The hesperidins used in the present invention mean hesperidin and its sugar adduct. Hesperidin is the one in which rutinose (L-rhamnosyl- (α1 → 6) -D-glucose) is β-bonded to the hydroxyl group at position 7 of hesperetin (5,7,3′-trihydroxy-4′-methoxyflavanone). It is. This hesperidin is a kind of flavanones, and those extracted and isolated by a known method from citrus peels such as Citrus unshiu and orange ( Citrus aurantium L ) can be used. It can also be purchased from Wako Pure Chemical Industries, Ltd., Hamari Pharmaceutical Co., Ltd., Alps Pharmaceutical Co., Ltd., etc. In addition, it is possible to use a crude product that is being purified from raw materials such as citrus peels without using purified hesperidin, or to use raw materials such as citrus peels by grinding or freeze-drying and grinding. May be. Examples of hesperidin sugar adducts include hesperidin sugar adducts in which sugars such as glucose, maltose, fructose, rhamnose, and lactose are bound to hesperidin. These hesperidin sugar adducts can be purchased as Toyo Seika Co., Ltd. (trade name “αG-Hesperidin PA-T”). Such hesperidins can usually be blended in an amount of 0.005 to 0.5% by weight, preferably 0.01 to 0.5% by weight, more preferably, based on the total amount of the oral composition of the present invention. 0.05-0.3 mass% can be mix | blended.

  Any one of xanthan gum and sodium alginate used in the present invention may be used alone or in combination. Such xanthan gum and sodium alginate can be blended in an amount of 0.2 to 5% by mass, preferably 0.2 to 3% by mass, more preferably 0.2 to 2%, based on the total amount of the oral composition of the present invention. % By mass, most preferably 0.5 to 2% by mass can be blended.

  The cellulosic thickener used in the present invention is not particularly limited as long as it is used in an oral composition. Specific examples include methylcellulose, hydroxyethylcellulose, carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, chlorinated O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethylcellulose, and crystalline cellulose. Among these, carboxymethyl cellulose, hydroxyethyl cellulose, and O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethyl cellulose are preferable, carboxymethyl cellulose and hydroxyethyl cellulose are more preferable, and carboxymethyl cellulose is most preferable. In addition, carboxymethyl cellulose is not particularly limited as long as it is usually used in an oral composition, but the degree of etherification is 0.45 to 2.0, and among these, 0.6 to 1 .8 is preferable, 0.8 to 1.6 is more preferable, and 1.0 to 1.4 is most preferable. Such a cellulosic thickener can be blended in an amount of 0.1 to 5% by mass, preferably 0.2 to 3% by mass, and more preferably 0.5 to 0.5% by mass with respect to the total amount of the oral composition of the present invention. 2 mass%, most preferably 1-2 mass% can be blended.

  Although the viscosity of the composition for oral cavity of this invention is not specifically limited, 10000-65000 mPa * s is preferable, 10000-35000 mPa * s is more preferable, and 12000-25000 mPa * s is the spreading | diffusion of the composition in an oral cavity. Is more preferable because it becomes even better. In addition, the viscosity value in this specification is a value in 30 degreeC. A B-type rotary viscometer is used as the measuring apparatus, and a combination in which the indicated value of the viscometer falls within the range of about 20 to about 80 is adopted for the spindle and the measurement rotational speed. The viscosity value can be obtained by multiplying the indicated value of the viscometer by a coefficient corresponding to each condition.

  The pH of the composition for oral cavity of the present invention is usually pH 3 to 10, preferably pH 4 to 9, and more preferably pH 5 to 8. The measurement is performed based on a known method, and the pH value in this specification is a value at 25 ° C.

  In the present application, “dispersion” means a state in which a solid floats in a solution. “Hesperidin dispersed” refers to a state in which a hesperidin solid is suspended in the composition, and the appearance of the composition in which hesperidin is dispersed is translucent or slightly cloudy. Therefore, the composition for oral cavity according to the present application is not clear and has an appearance or a translucent appearance in which some cloudiness is recognized. Since the solubility of hesperidin in water is 2 mg / 100 ml, normally, when hesperidin of 0.002% by mass or more is blended, hesperidin that cannot be dissolved is present in the composition in a solid state. The presence or absence of solids can be easily confirmed by using a magnifying glass or a microscope. As used herein, “dispersion stability is good” means that floating solid particles are not unevenly distributed in the composition. The presence or absence of uneven distribution can be easily determined by visually observing the appearance.

  The composition for oral cavity of the present invention is not particularly limited, but is a dentifrice (liquid dentifrice, liquid dentifrice, etc.), mouthwash, mouth spray, oral application, foam, cream, oral gel. It can be used as an agent, a tooth coating agent, an oral dry prevention agent, and the like. Among these, liquid and gel-like dosage forms that allow hesperidin to sufficiently reach and remain in every corner of the oral cavity are preferable. For example, liquid dentifrices, liquid dentifrices, mouthwashes, mouth sprays, oral gels, oral coatings, dry mouth prevention agents, etc. are preferred, among which liquid dentifrices, mouthwashes, oral coatings are the most preferable.

  If the composition for oral cavity of this invention is a range which does not impair the effect of this invention other than a cellulose thickener, a xanthan gum, sodium alginate, and hesperidin, the following component which can be normally mix | blended with an oral composition is included. Furthermore, you may mix | blend.

  As the surfactant, a nonionic surfactant, an anionic surfactant or an amphoteric surfactant can be blended. Specifically, as a nonionic surfactant, glycerin fatty acid ester, sugar fatty acid ester, sorbitan fatty acid ester, polyoxyethylene fatty acid ester, fatty acid diethanolamide, fatty acid monoglyceride, polyoxyethylene alkyl ether, polyoxyethylene hydrogenated castor oil, Examples thereof include alkyl glucoside and polyoxyethylene polyoxypropylene block copolymer. Examples of the anionic surfactant include sulfate ester salts, α-olefin sulfonates, sulfosuccinates, N-acyl amino acid salts, and acylated methyl taurate salts. Examples of amphoteric surfactants include betaine acetate type activator and imidazoline type activator. These surfactants can be blended alone or in combination of two or more.

  As the wetting agent, for example, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, sorbit, ethylene glycol, polyethylene glycol, polypropylene glycol ethanol and the like can be used alone or in combination of two or more.

  Examples of the abrasive include dicalcium phosphate dihydrate and anhydrous, calcium phosphate, tricalcium phosphate, calcium carbonate, calcium pyrophosphate, aluminum hydroxide, aluminum oxide, anhydrous silicic acid, silica gel, aluminum silicate, insoluble Sodium metaphosphate, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, polymethyl methacrylate, bentonite, zirconium silicate, hydroxyapatite, synthetic resin, and the like can be used. These abrasive | polishing agents can be mix | blended individually or in combination of 2 or more types.

  As a flavoring agent, for example, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronell, α-terpineol, methyl acetate, citronenyl acetate, methyl eugenol, cineol, linalool, ethyl 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, pimento oil alone or 2 More than one species can be used in combination.

  Sweetening agents include, for example, saccharin, saccharin sodium, acesulfame potassium, stevia extract, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perilartin, saumatine, aspartylphenylalanine methyl ester, methoxycinnamic aldehyde, palatinose, palatinit, erythritol, multi Tall, xylitol, lactitol and the like. These sweeteners can be used alone or in combination of two or more.

  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 components can be contained in the oral composition of the present invention alone or in combination of two or more. These pH adjusters can be used alone or in combination of two or more.

  Examples of the preservative include parabens such as methylparaben and propylparaben, and benzoates such as sodium benzoate. These preservatives can be used alone or in combination of two or more.

  Thickeners are those other than cellulosic thickeners, xanthan gum and sodium alginate, for example, microbially produced polymers such as gellan gum, natural polymers or natural rubbers such as tragacanth gum, karaya gum, arabiya gum, carrageenan and dextrin And synthetic polymers such as polyvinyl alcohol and polyvinyl pyrrolidone. These thickeners can be used alone or in combination of two or more.

  Medicinal properties include bactericides, anti-inflammatory agents, blood circulation promoters, antiplasmin agents, bleeding remedies, tissue repair agents, remineralizing agents, and other plant extracts extracted with water-soluble solvents, chlorophyll, sodium chloride , Caropeptides, zinc compounds, hinokitiol, and the like. These can be used alone or in combination of two or more.

  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.

Evaluation of oral composition in which hesperidin was dispersed Liquid oral compositions (Examples and Comparative Examples) were prepared according to the formulation shown in Table 1, and hesperidin dispersion stability evaluation and usability evaluation using an applicator were conducted. went. Evaluation of the dispersion stability of hesperidin was carried out by visually observing the appearance when a composition of about 120 ml was filled in a cylindrical bottle of about 120 ml and left standing at 55 ° C. for 1 week. Evaluation was in accordance with the criteria shown below. Usability evaluation using an applicator was performed by filling each oral composition in a tube (φ about 21 mm, length about 12 cm, discharge port diameter φ about 4.5 mm) and commercially available toothbrush (brush part 35 mm × 9 mm). Then, the composition for oral cavity is squeezed from the tube at a length of about 3 cm onto the brush surface of the hair transplantation pattern (3 rows of toothbrush major axis direction, 9 rows of vertical direction), and applied to the lower jaw model by the bath method. The application was performed once for each part, and the application time was 60 seconds.After the application, the adhesion state of hesperidin in the vicinity of each hourglass space and tooth gum of the lower jaw model was evaluated by visual observation. The evaluation of the composition for oral cavity was expressed as a comprehensive evaluation.The standard of the comprehensive evaluation is as follows.The above evaluation results are shown in Table 1.

Evaluation criteria for evaluation of dispersion stability of hesperidin Uniform appearance ○
Other than the above ×

Evaluation criteria for usability evaluation using brush body The composition for oral cavity spreads uniformly,
And penetration can be confirmed in the hourglass-shaped gap ◎
Spreads almost without leaving a lump of composition for the oral cavity.
Other than the above ×

Comprehensive evaluation When dispersion stability is ○ and usability evaluation is ◎
When dispersion stability is ○ and usability evaluation is ○ ○
Other than the above ×

As shown in Table 1, the oral composition containing one or more selected from the group consisting of xanthan gum and sodium alginate and carboxymethyl cellulose or hydroxyethyl cellulose gave excellent evaluation results. Moreover, when the viscosity of the composition in the composition for oral cavity of this invention is 40000 mPa * s or more, it turned out that usability evaluation is inferior to the thing of the viscosity below it.

Formulation Example 1
A liquid dentifrice was prepared according to a conventional method.
Component Blending amount (%)
Sorbit liquid (60%) 20.0
Concentrated glycerin 15.0
Polyethylene glycol 4.0
Hydroxypropyl methylcellulose 1.8
Xanthan gum 0.3
Sodium fluoride 0.21
Potassium nitrate 5.0
Reduced palatinose 10.0
Hesperidin 0.1
Anhydrous citric acid 0.05
Trisodium citrate 0.2
Glycerin fatty acid ester 2.0
Polyoxyethylene hydrogenated castor oil 0.3
Methyl paraoxybenzoate 0.2
Saccharin sodium 0.1
Perfume appropriate amount
Purified water balance
Total 100.0

Formulation Example 2
An oral gel was prepared according to a conventional method.
Component Blending amount (%)
Sorbit liquid (60%) 20.0
Concentrated glycerin 8.0
Xylitol 10.0
Carboxymethyl cellulose
(Degree of etherification: 1.00 to 1.06) 2.0
Xanthan gum 0.2
Sodium alginate 0.2
Propylene glycol 2.0
Cetylpyridinium chloride 0.05
Pyridoxine hydrochloride 0.12
Sodium ascorbate 0.1
Hesperidin 0.1
Anhydrous citric acid 0.05
Trisodium citrate 0.2
Methyl paraoxybenzoate 0.15
Polyoxyethylene hydrogenated castor oil 0.4
Perfume appropriate amount
Purified water balance
Total 100.0

Formulation Example 3
An intraoral coating agent was prepared according to a conventional method.
Component Blending amount (%)
Sorbit liquid (60%) 20.0
Concentrated glycerin 15.0
Reduced palatinose 10.0
Propylene glycol 3.0
O- [2-hydroxy-3-chloride]
(Trimethylammonio) propyl]
Hydroxyethyl cellulose 2.0
Sodium alginate 0.5
Cetylpyridinium chloride 0.05
Dipotassium glycyrrhizinate 0.15
Sodium monohydrogen phosphate 0.1
Sodium dihydrogen phosphate 0.25
Polyoxyethylene hydrogenated castor oil 0.2
Methyl paraoxybenzoate 0.15
Saccharin sodium 0.1
Perfume appropriate amount
Purified water balance
Total 100.0

Claims (4)

  An oral composition comprising one or more selected from the group consisting of xanthan gum and sodium alginate, a cellulose-based thickener and hesperidins.   The composition for oral cavity according to claim 1, wherein the viscosity at 30 ° C. is 10,000 to 65000 mPa · s.   The oral composition according to any one of claims 1 and 2, wherein 0.2 to 2% by mass of one or more selected from the group consisting of xanthan gum and sodium alginate is blended.   The composition for oral cavity according to any one of claims 1 to 3, wherein 0.5 to 3% by mass of a cellulosic thickener is blended.