JP2012056884A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a composition for oral cavity, which stably contains hesperidin and is excellent in usability.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 silicic anhydride, and enhances the dispersion stability in the composition for the oral cavity, usability and diffusivity of the hesperidin 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. In addition, there is provided the composition for the oral cavity, suitable for a tool for supplying a medicine.

Description

  The present invention relates to an oral composition containing hesperidin, and further relates to an oral composition for use in an oral drug supply device.

  The oral cavity has a complicated structure and a large number of narrow spaces such as hourglass-shaped gaps, so that food baskets and the like tend to stay. If daily cleaning is not performed properly, inflammation and caries occur at these sites, resulting in oral hygiene problems. Therefore, in these treatments and preventions, it is necessary to allow the cleaning liquid and the oral composition to reach every corner of the oral cavity.

  On the other hand, since hesperidin has excellent functions such as a remineralization promoting effect, it is desired to be applied to an oral composition. Since hesperidin has low solubility in water, the amount of hesperidin for obtaining a sufficient effect often exceeds the solubility of hesperidin in the oral composition. Become. In such a composition in which a solid is dispersed, it has been a problem to achieve good dispersion stability while ensuring diffusibility in the oral cavity. Furthermore, when using it in a chemical | medical agent supply tool, in order to make the discharge property from a chemical | medical agent supply device favorable, it is necessary to suppress the viscosity of an oral composition low, Therefore Problem solving also accompanies difficulty.

  Examples of the oral composition used in the medicine supply tool include, for example, an oral composition for use in a toothbrush having a built-in type container for storing a composition in Patent Document 1, and an electric toothbrush in Patent Document 2. A liquid dentifrice composition or the like for use in a small amount by using a lipstick has been proposed.

  However, these techniques cannot secure the dispersion stability of hesperidin or ensure the diffusibility of the oral composition in the oral cavity, and thus a new solution must be developed.

International Publication No. 04/032674 International Publication No. 04/032889

  This invention makes it a subject to provide the composition composition for oral cavity which can make hesperidin mix stably which can be reached to every corner in the oral cavity. Furthermore, an object of the present invention is to provide the composition for oral cavity that can be used even when a medicine supply tool is used.

  The present inventors have surprisingly found that the dispersion stability of hesperidin can be ensured by selecting a thickener, and further, by adjusting the viscosity of the composition for oral cavity, The oral cavity composition part can sufficiently reach the narrow space in the oral cavity while ensuring the discharge performance of the oral cavity, and can be provided with an oral composition having good dispersion stability of hesperidin. The present invention has been completed.

  That is, this invention concerns the composition for oral cavity of the following items 1-8, for example.

Item 1. An oral composition comprising one or more selected from the group consisting of xanthan gum and sodium alginate, silicic anhydride and hesperidin.
Item 2. Item 2. The oral composition according to Item 1, wherein the amount of hesperidin is 0.005 to 0.5 mass%.
Item 3. The oral cavity composition according to any one of Items 1 or 2, wherein the composition has a viscosity of 5000 to 25000 mPa · s at 30 ° C.
Item 4. Item 4. The composition for oral cavity according to any one of Items 1 to 3, wherein the amount of silicic anhydride is 0.2 to 2% by mass.
Item 5. Item 5. The composition for oral cavity according to any one of Items 1 to 4, which is applied to the oral cavity using a drug supply device.
Item 6. Item 5. A method for use wherein the composition for oral cavity according to any one of Items 1 to 4 is applied to the oral cavity using a drug supply tool.
Item 7. Item 7. The method according to Item 6, wherein the discharge part of the medicine supply tool is in the form of a brush.
Item 8. The medicine supply device includes an application unit, a delivery unit, a storage unit, and a delivery mechanism adjacent to the storage unit, and the oral composition is transported from the storage container to the application unit via the delivery unit. 8. The method according to any one of items 6 and 7.

  If it is the composition for oral cavity of this invention, the said composition can be reached to every corner in the oral cavity, without localization of hesperidin occurring. In particular, it is effective to use a medicine supply tool.

  Hereinafter, the present invention will be described in more detail.

  The composition for oral cavity of the present invention is preferably used for a drug supply device. The oral composition does not cause localization of hesperidin when used in a drug supply device, and can be applied to the oral cavity in a state in which the dispersion of hesperidin is stable every time it is used.

The composition for oral cavity of the present invention contains hesperidin. As for hesperidin used in the present invention, rutinose (L-rhamnosyl- (α1 → 6) -D-glucose) is β-bonded to the 7-position hydroxyl group of hesperetin (5,7,3′-trihydroxy-4′-methoxyflavanone). It is what you did. 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. Such hesperidin can usually be blended in an amount of 0.005 to 0.5 mass%, preferably 0.01 to 0.5 mass%, more preferably 0, based on the total amount of the oral composition of the present invention. 0.05 to 0.3% by mass can be blended.

  The oral composition of the present invention contains one or more selected from the group consisting of xanthan gum and sodium alginate. Such xanthan gum and sodium alginate are preferably blended in an amount of 0.3 to 3% by mass, more preferably 0.5 to 2% by mass, and most preferably 0.8 to 0.8%, based on the total amount of the oral composition of the present invention. 1.2 mass% can be mix | blended.

  The composition for oral cavity of the present invention contains silicic anhydride. Such silicic acid anhydride can be used as long as it can be used for a composition for oral cavity. Examples thereof include precipitated silica and gel silica. By blending silicic anhydride, hesperidin can be stably dispersed even if the viscosity of the composition is low, so that a composition suitable for a drug supply device can be provided. The silicic anhydride is preferably 0.2 to 2% by mass, more preferably 0.5 to 1.5% by mass, and most preferably 0.7 to 1.% by mass with respect to the total amount of the oral composition of the present invention. 3 mass% can be mix | blended.

  The viscosity of the composition for oral cavity of the present invention is preferably 5000 to 25000 mPa · s, and more preferably 5000 to 10,000 mPa · s. 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 but has an appearance in which some cloudiness is observed or a translucent appearance. In addition, since the solubility of hesperidin in water is 2 mg / 100 ml, usually when hesperidin of 0.002% by mass or more is blended, hesperidin that cannot be dissolved is present in the composition in a solid or liquid state. . Whether a solid or the like is floating can be easily confirmed by using a magnifying glass or a microscope. “Dispersion stability is good” as used in the present application 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 oral composition of the present invention is not particularly limited, but is a dentifrice (liquid dentifrice, liquid dentifrice, etc.), mouthwash, oral application, cream, oral gel, tooth application, oral cavity It can be used as a drying inhibitor. 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, a liquid dentifrice, a liquid mouthwash, an oral gel, an intraoral coating agent, an oral dry prevention agent and the like are preferable, and among them, a liquid dentifrice, a liquid mouthwash, and an oral coating agent are most preferable.

  In addition to xanthan gum, sodium alginate, silicic anhydride and hesperidin, the oral composition of the present invention is further blended with the following components that can be usually blended into the oral composition as long as the effects of the present invention are not impaired. May be.

  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, acylated methyl taurate salts, and the like. 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.

  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.

  Examples of the thickener include those other than carboxymethylcellulose, xanthan gum and sodium alginate. Natural polymers or natural rubbers such as Karaya gum, Arabia gum, carrageenan, dextrin, synthetic polymers such as polyvinyl alcohol and polyvinylpyrrolidone, cations such as O- [2-hydroxy-3- (trimethylammonio) propyl] hydroxyethylcellulose chloride Sexual thickeners may be mentioned. 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.

  In this invention, the method of applying the composition for oral cavity of this invention in an oral cavity using a chemical | medical agent supply tool is also disclosed.

  The drug supply device includes a storage unit for filling and storing the oral composition, and a drug discharge unit for allowing the oral composition to reach the oral region, and can be used with the main body in hand. A size is preferred. Moreover, the said storage part and a chemical | medical agent discharge part are connected as needed, and the channel | path part for transporting a composition for oral cavity is provided. Since the delivery path section needs to make the medicine ejection section reach the back of the oral cavity, it is preferably a thin tube. In the container, the storage unit may be detachable and can be repeatedly filled, or may be put on the market and disposed in a prefilled (prefilled) state. Specific examples of such a medicine supply tool include those having a medicine discharge nozzle as disclosed in Japanese Patent Application Laid-Open No. 2005-349134, and having a brush structure at the discharge portion as in Japanese translations 2010-526638 and 6-504924. Electric appliances, toothbrushes having a medicine discharge structure in a brush portion such as Japanese Patent Application Laid-Open No. 2005-65827 and 2002-503129, and those having a one-tuft type or brush-type brush structure such as Japanese Patent Application Laid-Open No. 2008-133099 Etc. Among these, those having a feeding path portion are preferable, those having a brush shape at the discharge portion are more preferable, and those having a brush one-tuft type or brush-type brush structure are most preferable.

  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 is dispersed Liquid oral compositions (Examples and Comparative Examples) are prepared according to the formulation shown in Table 1, hesperidin dispersion stability evaluation, usability evaluation using toothbrush and drug A discharge test using a supply tool was performed. 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. In the discharge test, the ease of discharge of the composition was evaluated using the container shown in Fig. 1 of JP-A-2008-13320. The evaluation of the composition for oral cavity was expressed as a comprehensive evaluation. General And the value of the criteria below. Or more of the 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 ×

Evaluation of discharge performance using chemical supply tool
Other than the above ×

Comprehensive evaluation When dispersion stability and dischargeability are ○ and usability evaluation is ◎
When dispersion stability and dischargeability are ○ 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 anhydrous silicic acid has superior dispersion stability of hesperidin and It has been found that the diffusibility of the oral composition in the oral cavity can be obtained.

Formulation Example 1
A liquid dentifrice was prepared according to a conventional method.
Component Blending amount (%)
Concentrated glycerin 18.0
Sorbit liquid (60%) 15.0
Reduced palatinose 10.0
Polyethylene glycol 3.0
Silica anhydride 2.0
Xanthan gum 1.5
Carboxymethylcellulose 0.5
Potassium nitrate 5.0
Zinc oxide 1.0
Hesperidin 0.5
Sodium fluoride 0.21
Cetylpyridinium chloride 0.05
Sodium monohydrogen phosphate 0.05
Sodium dihydrogen phosphate 0.2
Polyoxyethylene hydrogenated castor oil 0.2
Saccharin sodium 0.1
Methyl paraoxybenzoate 0.15
Perfume appropriate amount
Purified water balance
Total 100.0

Formulation Example 2
An intraoral coating agent was prepared according to a conventional method.
Component Blending amount (%)
Concentrated glycerin 20.0
Propylene glycol 1.0
Silica anhydride 1.2
Sodium alginate 1.8
Hesperidin 0.1
Cetylpyridinium chloride 0.05
Tranexamic acid 0.05
Trisodium citrate 0.1
Citric anhydride 0.01
Polyoxyethylene hydrogenated castor oil 0.2
Saccharin sodium 0.1
Methyl paraoxybenzoate 0.1
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 (%)
Concentrated glycerin 10.0
Propylene glycol 5.0
Silica anhydride 0.8
Xanthan gum 1.0
Sodium alginate 0.7
Xylitol 1.0
Cetylpyridinium chloride 0.3
Allantoin 0.33
Dipotassium glycyrrhizinate 0.46
Hesperidin 0.005
Sodium monohydrogen phosphate 0.05
Sodium dihydrogen phosphate 0.3
Perfume appropriate amount
Purified water balance
Total 100.0

Claims (7)

  An oral composition comprising one or more selected from the group consisting of xanthan gum and sodium alginate, silicic anhydride and hesperidin.   The composition for oral cavity according to claim 1, wherein the amount of hesperidin is 0.005 to 0.5 mass%.   The composition for oral cavity according to claim 1, wherein the viscosity of the composition at 30 ° C. is 5000 to 25000 mPa · s.   The composition for oral cavity according to any one of claims 1 to 3, wherein the amount of silicic anhydride is 0.2 to 2% by mass.   Item 5. The composition for oral cavity according to any one of Items 1 to 4, which is applied to the oral cavity using a drug supply device.   Item 5. A method for use wherein the composition for oral cavity according to any one of Items 1 to 4 is applied to the oral cavity using a drug supply tool.   The method according to claim 6, wherein the discharge part of the medicine supply tool is in the form of a brush.