JP2022072785A - Oral composition - Google Patents

Abstract

To provide an oral composition that exhibits anti-inflammatory action inside the oral cavity and that is capable of maintaining continuous moisturizing effect on the oral mucosa.SOLUTION: An oral composition contains (A) an azulene sulfonic acid and/or a salt thereof, and (B) hypromellose.SELECTED DRAWING: None

Description

The present invention relates to an oral composition capable of extinguishing inflammation in the oral cavity and continuously exerting a moisturizing effect on the oral mucosa.

In recent years, the number of people affected by dry mouth has been increasing. Dry mouth is also called xerostomia, which is a symptom that the amount of saliva secreted decreases and the oral cavity becomes dry. Dry mouth can have various causes such as aging, stress, muscle weakness, diabetes, renal failure, menopausal disorders, side effects of medication, etc., and these causes cannot be completely eliminated, so it is often used for the treatment of dry mouth. , Oral sprays, mouthwashes, mouthwashes, artificial saliva, troches and other oral compositions are used to moisturize the oral cavity.

Conventionally, various oral compositions effective for the prevention or improvement of dry mouth have been reported. For example, Patent Document 1 discloses that an oral composition containing a hydrophobically modified polyether urethane and a wetting agent is effective for the prevention or treatment of dry mouth. Further, Patent Document 2 describes polyglutamate as 0.05 to 5% by mass, an organic acid such as citric acid and a salt thereof, 2 to 6% by mass, l-menthol, glycerin as 10 to 50% by mass, and a surfactant. And a composition for oral spray containing 0.01-0.3% by mass of monomentyl succinate is disclosed to be effective in the prevention or treatment of dry mice.

Japanese Unexamined Patent Publication No. 2012-153677 Japanese Unexamined Patent Publication No. 2011-105651

For the prevention or treatment of dry mouth, it is important not only to temporarily impart a moisturizing effect to the oral mucosa but also to maintain the effect. In addition, since the barrier function against bacteria of dry mouth is lowered due to the drying of the oral mucosa, bacterial infection and inflammation are likely to occur in the oral cavity. Therefore, it can be said that it is desirable that the oral composition effective for the prevention or treatment of dry mouth not only imparts a moisturizing effect to the oral cavity but also has an anti-inflammatory effect.

Therefore, an object of the present invention is to provide an oral composition capable of extinguishing inflammation in the oral cavity and continuously exerting a moisturizing effect on the oral mucosa.

The present inventor has made diligent studies to solve the above problems, and found that by using azulene sulfonic acid and / or a salt thereof in combination with hypromellose in the oral composition, the anti-inflammatory effect is exhibited. It was found that the synergistic action of the ingredients dramatically improves the sustainability of the moisturizing effect on the oral mucosa. The present invention has been completed by further studies based on such findings.

That is, the present invention provides the inventions of the following aspects.
Item 1. An oral composition comprising (A) azulene sulfonic acid and / or a salt thereof, and (B) hypromellose.
Item 2. Item 2. The oral composition according to Item 1, which is used for the prevention or treatment of dry mouth.

The oral composition of the present invention is effective for oral care because it can continuously exert a moisturizing effect on the oral mucosa while exhibiting an anti-inflammatory effect, and can be suitably used for applications such as prevention or treatment of dry mouth.

The oral composition of the present invention is characterized by containing (A) azulene sulfonic acid and / or a salt thereof, and (B) hypromellose. Hereinafter, the oral composition of the present invention will be described.

[(A) Azulene sulfonic acid and / or a salt thereof]
The oral composition of the present invention contains azulene sulfonic acid and / or a salt thereof (sometimes referred to as component (A)). By containing azulene sulfonic acid and / or a salt thereof in the external composition of the present invention, it becomes possible to exert an anti-inflammatory effect in the oral cavity.

Azulene sulfonic acid is a known anti-inflammatory component also referred to as 1,4-dimethyl-7-isopropylazulene-3-sulfonic acid.

The type of salt of azulene sulfonic acid is not particularly limited as long as it is pharmaceutically acceptable, but for example, alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt. Other metal salts such as aluminum salts; Ammonium salts; Acetate, trifluoroacetate, butyrate, palmitate, stearate, fumarate, maleate, succinate, malonate, lactate , Tartrate, citrate and other carboxylates; methanesulfonate, toluenesulfonate, tosylate and other organic sulfonates; methylamine salt, triethylamine salt, triethanolamine salt, morpholine salt, piperazine salt , Pyrrolidine salt, tripyridine salt, picolin salt and other organic amine salts; examples thereof include hydrochlorides, sulfates, nitrates, hydrobromide salts, and inorganic acid salts such as phosphates. Among these salts, an alkali metal salt is preferable, and a sodium salt is more preferable.

Among the components (A), a salt of azulene sulfonic acid is preferable, and sodium azulene sulfonic acid is more preferable, from the viewpoint of further improving the sustainability of the moisturizing effect on the oral mucosa.

As the component (A), one component from azulene sulfonic acid and a salt thereof may be used alone, or two or more components may be used in combination.

The content of the component (A) in the oral composition of the present invention may be appropriately set according to the type of the component (A) to be used, the formulation form of the oral composition, etc., and may be appropriately set, for example, 0.0001. It is about 5% by weight, preferably 0.001 to 1% by weight, and more preferably 0.01 to 0.5% by weight.

[(B) Hypromellose]
The oral composition of the present invention contains hypromellose (sometimes referred to as component (B)) in addition to the component (A). By using the component (A) in combination with hypromellose, it becomes possible to dramatically improve the sustainability of the moisturizing effect on the oral mucosa by these synergistic actions.

Hypromellose is a known cellulose derivative also called hydroxypropylmethyl cellulose.

The content of the component (B) in the oral composition of the present invention may be appropriately set according to the formulation form of the oral composition and the like, and is, for example, 0.01 to 1.5% by weight, preferably 0.01 to 1.5% by weight. 0.1 to 1.5% by weight, more preferably 0.2 to 1.5% by weight, still more preferably 0.5 to 1.5% by weight. When the content of the component (B) satisfies the above range, the sustainability of the moisturizing effect on the oral mucosa can be dramatically improved without causing a decrease in usability due to an increase in viscosity.

In the oral composition of the present invention, the ratio of the component (A) to the component (B) is determined according to the content of each of these components. For example, (B) per part by weight of the component (A). ) The component is 1 to 300 parts by weight, preferably 5 to 80 parts by weight, more preferably 10 to 80 parts by weight, still more preferably 30 to 80 parts by weight.

[(C) Monohydric lower alcohol]
The oral composition of the present invention may contain a monohydric lower alcohol (sometimes referred to as a component (C)) in addition to the above-mentioned components (A) and (B). In the present invention, the monohydric lower alcohol refers to a monohydric alcohol having 1 to 5 carbon atoms.

The type of monohydric lower alcohol is not particularly limited as long as it is pharmaceutically acceptable, but for example, ethanol, n-propanol, isopropanol, n-butanol, sec-butanol, tert-butanol, n-amyl alcohol. , Se-amyl alcohol, isoamyl alcohol, tert-amyl alcohol, neopentyl alcohol and the like. These monohydric lower alcohols may be used alone or in combination of two or more.

Among these monohydric lower alcohols, ethanol is preferable.

When the component (C) is contained in the oral composition of the present invention, the content thereof is not particularly limited, but is, for example, 0.01 to 10% by weight, preferably 0.1 to 5% by weight, more preferably. Is 0.5 to 3% by weight.

[(D) Multivalent alcohol]
The oral composition of the present invention may contain a polyhydric alcohol (sometimes referred to as a component (D)) in addition to the above-mentioned components (A) and (B).

The type of polyhydric alcohol is not particularly limited as long as it is pharmaceutically acceptable, but for example, 1,3-butylene glycol, ethylene glycol, propylene glycol, isoprene glycol, diethylene glycol, dipropylene glycol, polyethylene glycol and the like. Dihydric alcohol; glycerin and the like. These polyhydric alcohols may be used alone or in combination of two or more.

Among these polyhydric alcohols, a dihydric alcohol is preferable, and propylene glycol is more preferable.

When the component (D) is contained in the oral composition of the present invention, the content thereof is not particularly limited, but is, for example, 1 to 80% by weight, preferably 10 to 75% by weight, and more preferably 30 to 70% by weight. Weight% is mentioned.

[water]
The oral composition of the present invention may contain water as part of the base. When the oral composition of the present invention contains water, the content thereof may be appropriately set according to the form of the formulation and the like, but is, for example, 1 to 90% by weight, preferably 10 to 70% by weight. It is preferably 25 to 60% by weight.

[Other ingredients]
The oral composition of the present invention may contain other medicinal ingredients in addition to the above-mentioned ingredients, if necessary. Such medicinal ingredients are not particularly limited as long as they can be blended in pharmaceutical products, oral care products, etc., but for example, iodine-based bactericidal ingredients (for example, iodine, povidone iodine, nonoxinol iodine and phenoxy iodine). Etc.), bronchial dilators, antitussives, expectorants, anti-inflammatory agents (other than azulene sulfonic acid and its salts), glucosyltransferase inhibitors, plaque inhibitors, hypersensitivity inhibitors, tooth stone preventives, antipyretic analgesics, antihistamines Examples include medicines, bactericides (other than quaternary ammonium salts), gastromucosal protective medicines, caffeines, vitamin medicines, Chinese herbs, and raw medicine ingredients.

In addition, the oral composition of the present invention may contain a base or an additive in order to obtain a desired pharmaceutical form. Such bases and additives are not particularly limited as long as they can be blended in pharmaceuticals, oral care products, etc., but for example, oily components, surfactants, preservatives, thickeners (other than hypromerose). ), Fragrances, flavoring agents, cooling agents, pigments, deodorants, pigments, buffers, pH adjusters and the like.

[Shape / formulation form]
The shape of the oral composition of the present invention is not particularly limited and may be liquid, solid, semi-solid (gel, ointment, paste) or the like, but liquid is preferable. Be done.

The formulation form of the oral composition of the present invention is not limited as long as it is applied to the oral cavity and can stay in the oral cavity for a certain period of time, but for example, an oral spray (including a throat spray agent), a mouse. Oral care products such as wash, mouthwash, liquid dentifrice, kneaded dentin, mouth refresher, oral pasta, gingival massage cream and the like can be mentioned. Among these, an oral spray, a mouthwash, a mouthwash, and more preferably an oral spray are preferable.

[how to use]
When applied to the oral cavity, the oral composition of the present invention can extinguish and / or sterilize the oral cavity and can continuously exert a moisturizing effect on the oral mucosa. Therefore, for example, prevention of dry mouth or Suitable for therapeutic use.

The usage and volume of the oral composition of the present invention are appropriately set according to the content of each compounding component, the pharmaceutical form of the oral composition, the expected effect, etc., and are, for example, 1 to 1 per day. An appropriate amount may be applied intraorally at a frequency of 6 times.

Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited thereto.

Test Example 1
An oral composition (oral spray) having the composition shown in Table 1 was prepared. The obtained oral composition was evaluated for its long-lasting moisturizing effect on the oral mucosa by the following method. First, the edible pig tongue (unsliced) excised as a pseudo-mucosa is lightly moistened with running water and then lightly wiped off. It was allowed to stand until the measured value at Yoshida Co., Ltd.) reached the drying index value (25 or less). Next, the obtained oral composition was placed in a spray container, and about 0.3 ml of the oral composition was spray-applied to a portion slightly from the center of the pig tongue to a portion slightly from the tip, and the temperature was 30 ° C. and the relative humidity was 30%. It was allowed to stand for 6 hours in the atmosphere of RH. Immediately after application of the oral composition and 6 hours after application, the moisture value of the pig tongue part to which the oral composition was applied was measured using an oral moisture meter (Oral Moisture Meter Mucus, Yoshida Co., Ltd.) and calculated as follows. According to the formula, the water retention rate (%) 6 hours after application was calculated, and the value rounded off to the first digit was taken as the water retention rate (%) 6 hours after application.

The results are shown in Table 1. With sodium azulene sulfonate alone, the water retention rate after 6 hours of application was low, and the moisturizing effect could not be maintained (Comparative Example 1). In addition, hypromellose, hydroxyethyl cellulose, and carboxyvinyl polymer alone had a slightly higher water retention rate after 6 hours of application, but were still insufficient (Comparative Examples 6 to 8). Furthermore, even when hydroxyethyl cellulose or carboxyvinyl polymer was used in combination with sodium azulene sulfonate, the water retention rate after 6 hours of application was only additively improved (Comparative Examples 2 to 5). On the other hand, when sodium azulene sulfonate and hypromellose were used in combination, the water retention rate after 6 hours of application was synergistically improved, and the sustainability of the moisturizing effect was significantly enhanced (Example 1). ~ 3). Since the oral compositions of Examples 1 to 3 contain sodium azulene sulfonate, they have a composition capable of exhibiting an anti-inflammatory effect.

An oral composition (oral spray) having the composition shown in Table 2 of the formulation example was prepared. For comparison, a comparative oral composition in which the hypromellose of Formulation Examples 5 and 6 was changed to purified water was also prepared. The sustainability of the moisturizing effect of these oral compositions was evaluated by the same method as in Test Example 1. In each of Formulation Examples 1 to 4, the water retention rate after 6 hours of application was significantly higher than that of Comparative Examples 1 to 8. Further, even in Formulation Examples 5 and 6 in which cetylpyridinium chloride was replaced with benzalkonium chloride or benzethonium chloride, the water retention rate after 6 hours of application was the comparative oral composition of Formulation Examples 5 and 6, and Comparative Examples 1 to 18. Compared with, the sustainability of the moisturizing effect was significantly increased.

Claims (2)

An oral composition containing (A) azulene sulfonic acid and / or a salt thereof, and (B) hypromellose. The oral composition according to claim 1, which is used for the prevention or treatment of dry mouth.