JP5462476B2 - Oral composition - Google Patents

Description

  The present invention provides quick moisture supply to the dry oral cavity to ease dry symptoms in the oral cavity, dry in the oral cavity, quickly permeate moisture and dirt stuck to the mouth, making it easier to clean, The present invention relates to a composition for oral cavity having sufficient viscosity for increasing the retention of the composition in the inside to prevent drying and retaining active ingredients such as a humectant.

  In recent years, the number of patients who complain of dryness in the oral cavity is increasing with aging. This may be due to a decrease in the amount of saliva secreted into the oral cavity or an increase in breathing in the mouth. Patients who can take water and lick their wrinkles when they feel dry do not lead to severe dryness of the oral cavity, but patients who need to be moistened by themselves, such as those requiring care, especially tube feeding In patients whose life expectancy has been reduced and oral intake has stopped, symptoms such as excessive dryness of the oral cavity, wrinkles and dirt clinging to the oral cavity, and cracking of the oral mucosa appear.

  The treatment and prevention of these symptoms not only improves the patient's discomfort, but in recent years it has maintained the balance of oral resident bacteria, and oral infections such as oral Candida and aspiration pneumonia It is also regarded as important in terms of preventing the onset of the disease. Accordingly, there is a need for a product that can restore moisture in the patient's oral cavity, smoothly remove contaminants without burdening the patient, and prevent oral dryness after oral care.

  Currently, sprays containing moisturizers and gel-type moisturizing creams have been reported and are commercially available as products for moisturizing the oral cavity. The spray type is easy to use, but if the viscosity of the liquid is not low, it is not sprayed from the spray, so there is no sufficient viscosity to stay in the oral cavity and it is necessary to use it frequently. In order to improve such a defect, a composition imparted with thixotropy in the hope of extending the residence time of the contents on the oral mucosa has been reported (for example, see Patent Document 1). It only increases the water retention rate of itself, and it is not enough to supply moisture to the dry oral cavity to spread moisture, to soften dry dirt and to facilitate cleaning.

On the other hand, as a gel-type moisturizing cream, an oral care composition containing polyvinylpyrrolidone and an anionic mucoadhesive substance that can also be used as an oral lubricant (see, for example, Patent Document 2); used as an alternative to saliva A thermoreversible composition containing a thermoreversible polymer and a bioadhesive polymer (see, for example, Patent Document 3) has been reported. However, these compositions can retain a moisturizer in the oral cavity, but remain in the oral cavity with the moisture confined in the gel, thus supplying moisture to the dry oral cavity to spread moisture or drying. It takes time to clean the dirt and make it easier to clean.
JP 2005-200327 A JP 2008-508338 A JP 2005-526784 A

  The present invention provides quick moisture supply to the dry oral cavity to ease dry symptoms in the oral cavity, dry in the oral cavity, quickly permeate moisture and dirt stuck to the mouth, making it easier to clean, The present invention relates to a composition for oral cavity having sufficient viscosity for increasing the retention of the composition in the inside to prevent drying and retaining active ingredients such as a humectant.

  Aqueous compositions containing thickeners such as sodium carboxymethylcellulose, sodium alginate, and xanthan gum that are commonly used in the food and cosmetic field, exude moisture from the composition as its viscosity increases, i.e. from the composition The amount of moisture supplied to the oral cavity decreases, and the ability to give water before the viscosity exceeds 10,000 mPa · s (25 ° C.) is almost lost. In this way, <1> increasing the retention in the oral cavity to prevent drying, and imparting sufficient viscosity to the composition to retain active ingredients such as humectants, and <2> from the composition to the oral cavity It was difficult to achieve both of supplying water and quickly moistening the dried oral cavity.

  The inventors of the present invention have a constant water supply ability and a sufficient viscosity for retaining an active ingredient such as a humectant in the oral cavity so that the dried oral cavity can be quickly moistened. Intense study was conducted to provide the composition. As a result, a composition containing a thickener that can be generally used in the fields of pharmaceuticals, foods and cosmetics and agar, and having a viscosity at 25 ° C. of 10,000 to 50,000 mPa · s has such desired properties. The present invention has been completed.

  The composition of the present invention has a constant water supply ability despite its high viscosity at 25 ° C. of 10,000 to 50,000 mPa · s. Therefore, the dried oral cavity is quickly moistened, moisture is penetrated into the dried dirt, and the removal of the dirt is facilitated without giving a burden to the patient. On the other hand, since the viscosity of the composition of the present invention is as high as 10,000 to 50,000 mPa · s at 25 ° C., the residence time in the oral cavity is expected to be extended. Therefore, in addition to preventing dryness due to the composition itself covering the oral cavity, it is expected to have a therapeutic and preventive effect on the dryness of the oral cavity and associated diseases by retaining active ingredients such as a moisturizer incorporated in the composition. The

  The agar that can be used in the oral composition of the present invention may be in the form of powder, granules, or flakes that are commercially available as raw materials for pharmaceuticals, foods, and cosmetics. Examples of such agar include Ina Agar CS, Ina Agar CSG, Ultra Agar AX-100, and Ultra Agar Ena manufactured by Ina Food Industry Co., Ltd. The amount of agar blended is not particularly limited as long as the viscosity at 25 ° C. of the composition together with the thickener is 10,000 to 50,000 mPa · s. From this point, it is preferably in the range of 0.5% by mass or more and 5.0% by mass or less based on the weight of the composition, and more preferably in the range of 1.0% by mass or more and 2.0% by mass or less. Is preferred.

  The thickener that can be used in the composition for oral cavity of the present invention may be any one that is commercially available as a raw material for pharmaceuticals, foods and cosmetics, such as carrageenan, guar gum, pectin, sodium carboxymethylcellulose (CMC), sodium alginate. Examples include thickening polysaccharides such as (Na alginate) and xanthan gum. The thickener is preferably one or more selected from the group consisting of sodium carboxymethylcellulose, sodium alginate and xanthan gum. The blending amount of the thickener is not particularly limited as long as the viscosity at 25 ° C. of the composition together with agar is 10,000 to 50,000 mPa · s. From this point, it is preferable that it is in the range of 0.05% by mass or more and 10.0% by mass or less based on the weight of the composition, and further 0.1% by mass or more and 5.0% by mass or less. A range is preferred.

  In the composition of the present invention, additives such as a pH adjuster, a corrigent, a preservative, a fragrance, a pigment, a solubilizer, and a surfactant are further blended within a range that does not impair the water supply ability of the composition. May be. In addition, the composition of the present invention may contain active ingredients such as a moisturizer, an antibacterial agent and a vitamin agent in view of the dryness of the oral cavity and the treatment and prevention effects of the accompanying diseases.

  Since the composition of the present invention is used in the oral cavity, its pH is preferably in the range of 5.5 to 8.0. The pH adjuster that can be used in the composition of the present invention is not particularly limited as long as it can be used in foods. For example, phosphoric acid, sodium monohydrogen phosphate, sodium dihydrogen phosphate, potassium monohydrogen phosphate , Potassium dihydrogen phosphate, citric acid, malic acid, pyrophosphoric acid, tartaric acid, acetic acid, or salts thereof. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  Additives such as flavoring agents, preservatives, fragrances, coloring agents, solubilizers, surfactants and the like that can be used in the composition of the present invention are not particularly limited as long as they can be used in pharmaceuticals, foods, and cosmetics. . For example, as a flavoring agent, saccharin, sodium saccharin, disodium glycyrrhizinate, trisodium glycyrrhizinate, sucrose, glucose, fructose, lactose, honey, aspartame, stevia, sucralose, xylitol, inositol, trehalose, D-sorbitol, D- Examples include mannitol, raffinose, lactulose, lactitol, erythritol, reduced palatinose, palatinose, palatinit, acesulfame K, maltose, maltosyl trehalose or maltitol. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  Examples of the preservative include parabens (paraoxybenzoic acid esters) such as methylparaben, ethylparaben, isopropylparaben, propylparaben, butylparaben, isobutylparaben and benzylparaben, alcohols such as phenoxyethanol and ethanol, or sorbic acid and benzoic acid. Examples thereof include acids, dehydroacetic acid, propionic acid, and salts thereof. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  Examples of the fragrance include l-menthol, peppermint, spearmint, and fruit fragrance. The perfume also has the advantage of stimulating salivation. Examples of the colorant include natural or synthetic dyes such as edible tar dyes, caramel dyes, gardenia dyes, anthocyanin dyes, safflower dyes, and the like. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  Any solubilizing agent may be used as long as it can promote the dissolution of the additive and the active ingredient in water, which is the base of the composition of the present invention. Examples thereof include propylene glycol, dipropylene glycol, and butylene glycol. And polyhydric alcohols such as polyethylene glycol. Examples of the surfactant include polysorbate, lauryl sulfate, polyglyceryl laurate, lauroyl sarcosine salt, polyoxyethylene hydrogenated castor oil, and hydrogenated castor oil. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  The humectant as an active ingredient that can be further blended in the composition of the present invention is not particularly limited as long as it can be used in pharmaceuticals, foods, and cosmetics. For example, amino acids or salts thereof, pyrrolidone carboxylic acid; mucin, Examples include mucopolysaccharides such as hyaluronic acid or salts thereof, chondroitin sulfate; polyhydric alcohols such as glycerin, propylene glycol, butylene glycol, sorbitol, xylitol, and polyethylene glycol; natural extract components such as tea extract. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  Examples of the antibacterial agent include chlorhexidine, cetylpyridinium chloride, a zinc compound, and triclosan. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  Examples of vitamins include vitamin A such as retinoic acid and β-carotene, pantothenic acid or salts thereof, vitamin B such as niacin and biotin, vitamin C such as ascorbic acid or salts and derivatives thereof, α-tocopherol and the like Vitamin E, folic acid, etc. are mentioned. What is necessary is just to select these 1 type, or 2 or more types of combinations suitably.

  The composition of the present invention is obtained by blending agar and at least one thickener, and additives and / or active ingredients in water. In this case, the composition is agar and thickener so that the viscosity at 25 ° C. is 10,000 to 50,000 mPa · s, preferably 30,000 to 45,000 mPa · s. Adjust as appropriate. Here, the viscosity was measured at 25 ° C. with a B-type viscometer BL (manufactured by Tokyo Keiki Co., Ltd.).

  The oral composition of the present invention has a relatively high viscosity at 25 ° C. of 10,000 to 50,000 mPa · s. Therefore, it is generally preferred to be provided as a gel product for the oral cavity. The composition of the present invention may be used by applying an appropriate amount to the oral cavity by hand or with a brush or sponge by the patient himself or his / her caregiver.

[Experiment method of moisture supply measurement]
The water donating ability of the samples obtained in each of the following production examples was measured by the following method.
(1) A metal plate (diameter 22 mm, thickness 1.5 mm) having a hole with a diameter of 5 mm is placed in the center of a filter paper (manufactured by Tokyo Filter Paper Company, ADAVANTEC 5B (diameter 110 mm)).
(2) Put 25 μL of each sample into the hole and let stand at room temperature for 10 minutes.
(3) Gently remove the metal plate and measure the diameter of the part of the filter paper where the water is absorbed and discolored.

[Viscosity measurement method]
The viscosity was measured at 25 ° C. using a B-type viscometer BL (manufactured by Tokyo Keiki Co., Ltd.).

[Example 1]
0.5 wt. Of sodium carboxymethylcellulose (CMC: CMC Daicel, manufactured by Daicel Chemical Industries) is added to 1.0 wt%, 1.5 wt%, and 2.0 wt% aqueous solution of agar (Ultra Agar AX-100, manufactured by Ina Food Industry Co., Ltd.). %, 1.0 wt%, and 1.5 wt% were added, and the viscosity and water supply amount were measured.

  FIG. 1 shows the change in viscosity of each sample prepared in Example 1. In the graph, ■ indicates the change in viscosity in CMC 1.5 wt% and CMC 2.0 wt% aqueous solution, and ◆ indicates viscosity in agar 1.0 wt% + CMC 0.5 wt% aqueous solution; + CMC 1.0 wt% aqueous solution; + CMC 1.5 wt% aqueous solution ▲ indicates agar 1.5 wt% + CMC 0.5 wt% aqueous solution; + CMC 1.0 wt% aqueous solution; + CMC 1.5 wt% aqueous solution viscosity change, ● indicates agar 2.0 wt% + CMC 0.5 wt% aqueous solution + CMC 1.0 wt% aqueous solution; + CMC 1.5 wt% aqueous solution shows the change in viscosity. The viscosity increases with the increase in the amount of CMC added, and the water supply amount is clearly reduced. By using agar and CMC in combination, a high water supply amount can be obtained even at a viscosity exceeding 10,000 mPa · s. I was able to.

[Example 2]
Sodium alginate (Duck alginate NSPM, manufactured by Kibun Food Chemifa Co., Ltd.) in an aqueous solution of 1.0 wt%, 1.5 wt% and 2.0 wt% of agar (same as Example 1) The viscosity and the amount of water supply were measured by adding 0.0 wt%. As shown in FIG. 3, by using sodium alginate in combination with agar, a high water supply amount could be obtained even at a viscosity exceeding 10,000 mPa · s.

  FIG. 2 shows the change in viscosity of each sample prepared in Example 2. In the graph, ■ indicates changes in viscosity in aqueous solutions of 1.0 wt%, 2.0 wt%, and 4.0 wt% sodium alginate, and ◆ indicates an aqueous solution of 1.0 wt% agar + 0.5 wt% sodium alginate; + sodium alginate 1.0 wt% aqueous solution: + Viscosity change in sodium alginate 2.0 wt% aqueous solution, ▲ indicates agar 1.5 wt% + sodium alginate 0.5 wt% aqueous solution; + sodium alginate 1.0 wt% aqueous solution; + sodium alginate The change in viscosity in a 2.0 wt% aqueous solution is shown, and ● represents the change in viscosity in agar 2.0 wt% + sodium alginate 0.5 wt% aqueous solution; + sodium alginate 1.0 wt% aqueous solution; + sodium alginate 2.0 wt% aqueous solution Is shown. Viscosity increases with increasing amount of sodium alginate, and the amount of water supply is clearly reduced. By using agar and sodium alginate in combination, the amount of water supply is high even at a viscosity exceeding 10,000 mPa · s. Could get.

[Example 3]
Xanthan gum (San Ace NXG-S, Saneigen FFI Co., Ltd.) was added to 1.0 wt%, 1.5 wt%, and 2.0 wt% aqueous solutions of agar (same as Example 1). Viscosity and water supply were measured by adding 5 wt% and 1.0 wt%. As shown in FIG. 3, by using sodium alginate in combination with agar, a high water supply amount could be obtained even at a viscosity exceeding 10,000 mPa · s.

  FIG. 3 shows the change in viscosity of each sample prepared in Example 3. In the graph, ■ indicates changes in viscosity in xanthan gum 0.2 wt%, 0.5 wt%, 1.0 wt%, and 2.0 wt% aqueous solutions, and ◆ indicates agar 1.0 wt% + xanthan gum 0.2 wt% aqueous solution; + Xanthan gum 0.5 wt% aqueous solution; + Change in viscosity in xanthan gum 1.0 wt% aqueous solution, ▲ indicates agar 1.5 wt% + xanthan gum 0.2 wt% aqueous solution; + xanthan gum 0.5 wt% aqueous solution; The change in viscosity in a 0 wt% aqueous solution is shown, and the black circle shows the change in viscosity in an agar 2.0 wt% + xanthan gum 0.2 wt% aqueous solution; + xanthan gum 0.5 wt% aqueous solution; + xanthan gum 1.0 wt% aqueous solution. The viscosity increases with the increase in the amount of xanthan gum, and the water supply amount is clearly reduced. However, by using agar and xanthan gum in combination, a high water supply amount can be obtained even at a viscosity exceeding 10,000 mPa · s. I was able to.

[Example 4]
Preparation of oral gel composition

An oral gel composition of the above composition was prepared according to the following method:
(1) Agar was added to an appropriate amount of purified water, heated to 80 ° C. with dissolution and dissolved, and the resulting solution was cooled to 40 ° C. with stirring;
(2) Methylparaben and l-menthol were dissolved in propylene glycol and glycerin, and sodium alginate and xanthan gum were further dispersed therein;
(3) Other components were dissolved in the remaining purified water, and the resulting solution was added to the dispersion obtained in (2) above, stirred and dissolved;
(4) The solution of (3) was added to the solution of (1) maintained at 40 ° C. and cooled to room temperature while stirring.

[Example 5]
Preparation of oral gel composition

An oral gel composition of the above composition was prepared according to the following method:
(1) Agar was added to an appropriate amount of purified water, heated to 80 ° C. with dissolution and dissolved, and the resulting solution was cooled to 40 ° C. with stirring;
(2) methylparaben was dissolved in propylene glycol and glycerin, and CMC was further dispersed therein;
(3) Other components were dissolved in the remaining purified water, and the resulting solution was added to the dispersion obtained in (2) above, stirred and dissolved;
(4) The solution of (3) was added to the solution of (1) maintained at 40 ° C. and cooled to room temperature while stirring.

  The composition of the present invention has a constant water supply ability despite its high viscosity at 25 ° C. of 10,000 to 50,000 mPa · s. Therefore, the dried oral cavity is quickly moistened, moisture is penetrated into the dried dirt, and the removal of the dirt is facilitated without burdening the patient. On the other hand, since the viscosity of the composition of the present invention is as high as 10,000 to 50,000 mPa · s at 25 ° C., the residence time in the oral cavity is expected to be extended. Therefore, in addition to prevention of dryness due to the composition itself covering the oral cavity, the therapeutic and preventive effects of oral conditions and associated diseases are expected by retaining active ingredients such as a moisturizer blended in the composition.

It is the figure which showed the change of the viscosity of each sample (agar + CMC) adjusted in Example 1. FIG. It is the figure which showed the change of the viscosity of each sample (agar + sodium alginate) adjusted in Example 2. It is the figure which showed the change of the viscosity of each sample (agar + xanthan gum) adjusted in Example 3.

Claims (4)

  It includes at least one thickener selected from the group consisting of agar, sodium carboxymethylcellulose, sodium alginate and xanthan gum, and a humectant, and has a viscosity at 25 ° C. of 10,000 to 50,000 mPa · s. , Oral moisturizing composition (excluding silicic acid anhydride, calcium carbonate, sodium chloride and gadgets).   The composition for oral moisturizing according to claim 1, wherein the blending amount of the thickener is 0.5 to 1.5 mass% based on the weight of the composition.   The composition for oral moisturizing according to claim 1 or 2, wherein the blending amount of agar is 2.0 mass% or less based on the weight of the composition.   The composition for oral moisturization according to any one of claims 1 to 3, wherein the amount of agar is 1.0 to 2.0 mass% based on the weight of the composition.

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