Oral composition

Abstract

To provide a formulation technique for producing a hinokitiol-containing oral composition in which the hinokitiol has enhanced solubility and can be inhibited from forming a precipitate or an insoluble.SOLUTION: An oral composition includes a water-soluble copper compound together with hinokitiol. Due to the inclusion of the water-soluble copper compound, the solubility of the hinokitiol is improved and the hinokitiol can be inhibited from forming a precipitate or an insoluble.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to an oral composition containing hinokitiol, in which the solubility of hinokitiol is improved. [Background technology]

[0002] In recent years, oral diseases such as dental caries and periodontal disease have become widespread due to factors such as diversification of dietary habits. Dental caries and periodontal disease are bacterial infections whose onset is largely due to oral bacteria present in dental plaque formed in hard tissues or periodontal pockets. Streptococcus species such as Streptococcus mutans (S. mutans) are known to cause dental caries, while Porphyromonas gingivalis (P. gingivalis) and other bacteria are known to cause periodontal disease. Therefore, in order to maintain a healthy oral cavity, it is important to keep the number of these pathogenic bacteria in the oral cavity at a low level.

[0003] Conventionally, bactericides have been incorporated into oral compositions such as dentifrices and mouthwashes to reduce the number of pathogenic bacteria that cause dental caries and periodontal disease. Various bactericides are known for incorporation into oral compositions, but hinokitiol is widely used in oral compositions due to its low toxicity and broad antibacterial spectrum. Various formulations of oral compositions containing hinokitiol have been proposed. For example, Patent Document 1 discloses that the bactericidal effect can be synergistically improved by incorporating lemongrass citral together with hinokitiol into an oral composition.

[0004] However, hinokitiol has low solubility in water, and when incorporated into oral compositions, it is difficult to solubilize and precipitates tend to form. Therefore, there is a need to develop formulation techniques that can increase the solubility of hinokitiol in oral compositions containing hinokitiol. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] Japanese Patent Application Laid-Open No. 2007-63166 Summary of the Invention [Problem to be solved by the invention]

[0006] An object of the present invention is to provide a formulation technique that can increase the solubility of hinokitiol in an oral composition containing hinokitiol and inhibit the formation of precipitates or insoluble matter due to hinokitiol. [Means for solving the problem]

[0007] The present inventors have conducted extensive research to solve the above problems and have found that by incorporating a water-soluble copper compound together with hinokitiol in an oral composition, the solubility of hinokitiol can be improved and the formation of precipitates and insoluble matter caused by hinokitiol can be suppressed.The present invention was completed through further research based on this finding.

[0008] That is, the present invention provides the following aspects. Item 1. An oral composition containing hinokitiol and a water-soluble copper compound. Item 2. The oral composition according to Item 1, wherein the water-soluble copper compound is copper chlorophyllin sodium or copper gluconate. Item 3. A method for improving the solubility of hinokitiol in an oral composition containing hinokitiol, comprising: A method for improving solubility by blending hinokitiol and a water-soluble copper compound into an oral composition. [Effects of the Invention]

[0009] According to the present invention, in an oral composition containing hinokitiol, the solubility of hinokitiol can be increased and the formation of precipitates or insoluble matter due to hinokitiol can be suppressed. DETAILED DESCRIPTION OF THE INVENTION

[0010] 1.Oral composition The oral composition of the present invention is characterized by containing hinokitiol and a water-soluble copper compound. The oral composition of the present invention will be described in detail below.

[0011] [Hinokitiol] The oral composition of the present invention contains hinokitiol, a known compound having antiseptic and other properties.

[0012] In the present invention, hinokitiol may be derived from natural products or may be chemically synthesized. Furthermore, the hinokitiol used in the present invention may be a purified or crude product, and for example, a hinokitiol-containing essential oil obtained from trees may also be used.

[0013] The content of hinokitiol in the oral composition of the present invention may be set appropriately depending on the type of oral composition, the degree of bactericidal effect to be imparted, etc., and may be, for example, 0.0005 to 1% by weight, preferably 0.005 to 0.8% by weight, and more preferably 0.01 to 0.5% by weight.

[0014] [Water-soluble copper compound] The oral composition of the present invention contains, in addition to hinokitiol, a water-soluble copper compound, which increases the solubility of hinokitiol and inhibits the formation of precipitates or insoluble matter due to hinokitiol.

[0015] The water-soluble copper compounds are water-soluble copper complexes and copper salts. The type of water-soluble copper complex is not particularly limited as long as it is suitable for oral administration, and examples thereof include alkali metal salts of copper chlorophyllin (such as sodium copper chlorophyllin). The type of water-soluble copper salt is not particularly limited as long as it is suitable for oral administration, and examples thereof include copper gluconate, copper sulfate, copper chloride, copper nitrate, copper acetate, copper lactate, copper butyrate, copper formate, copper phosphate, copper malate, copper succinate, copper malonate, and copper maleate.

[0016] These water-soluble copper compounds may be used alone or in combination of two or more. Among these water-soluble copper compounds, from the viewpoint of further improving the solubility of hinokitiol, alkali metal salts of copper chlorophyllin and copper gluconate are preferred, alkali metal salts of copper chlorophyllin are more preferred, and sodium copper chlorophyllin is even more preferred.

[0017] The content of the water-soluble copper compound in the oral composition of the present invention may be set appropriately depending on the type of oral composition, the content of hinokitiol, etc., but may be, for example, 0.00005 to 5 wt % of the total amount of water-soluble copper compound, preferably 0.0001 to 1 wt %, more preferably 0.005 to 0.5 wt %, and even more preferably 0.01 to 0.2 wt %.

[0018] In the oral composition of the present invention, the ratio of hinokitiol to water-soluble copper compound is determined according to the respective contents of these two components, but for example, the total amount of water-soluble copper compound per 1 part by weight of hinokitiol is 0.001 to 100 parts by weight, preferably 0.01 to 10 parts by weight, and more preferably 0.05 to 5 parts by weight.

[0019] [Dimethyl sulfoxide] The oral composition of the present invention may contain dimethyl sulfoxide in addition to the above-mentioned components.

[0020] When dimethyl sulfoxide is contained in the oral composition of the present invention, the content is not particularly limited, but may be, for example, 0.01 to 15% by weight, preferably 0.1 to 10% by weight, and more preferably 1 to 8% by weight.

[0021] [Monohydric lower alcohol] The oral composition of the present invention may contain a monohydric lower alcohol, if necessary. In the present invention, the monohydric lower alcohol refers to a monohydric alcohol having 1 to 5 carbon atoms.

[0022] The type of monohydric lower alcohol is not particularly limited as long as it is applicable to the oral cavity, and examples thereof include ethanol, n-propanol, isopropanol, n-butanol, sec-butanol, tert-butanol, n-amyl alcohol, sec-amyl alcohol, isoamyl alcohol, tert-amyl alcohol, neopentyl alcohol, etc. These monohydric lower alcohols may be used alone or in combination of two or more.

[0023] Among these monohydric lower alcohols, ethanol is preferred.

[0024] When a monohydric lower alcohol is contained in the oral composition of the present invention, the content is not particularly limited, but may be, for example, 0.001 to 5% by weight, preferably 0.01 to 2% by weight, and more preferably 0.05 to 1% by weight.

[0025] [water] The oral composition of the present invention contains water as a solvent. The content of water in the oral composition of the present invention may be the remainder excluding the added components, and may be, for example, 30 to 99 wt %, preferably 40 to 99 wt %, or 50 to 98 wt %.

[0026] [Other ingredients] The oral composition of the present invention may contain other medicinal ingredients, if necessary, in addition to the above-mentioned ingredients. Such medicinal ingredients are not particularly limited as long as they can be incorporated into pharmaceuticals, oral care products, etc. Examples of such medicinal ingredients include iodine-based antibacterial ingredients, bronchodilators, antitussives, expectorants, anti-inflammatory agents, glucosyltransferase inhibitors, plaque inhibitors, hypersensitivity inhibitors, anti-tartar agents, antipyretics, analgesics, antihistamines, disinfectants, gastric mucosa protectants, caffeines, vitamins, herbal medicines, and herbal ingredients.

[0027] The oral composition of the present invention may contain bases and additives to obtain a desired formulation. Such bases and additives are not particularly limited as long as they can be incorporated into pharmaceuticals, oral care products, etc. Examples of such bases and additives include oily components, polyhydric alcohols, surfactants, freshening agents, preservatives, thickeners, fragrances, flavoring agents, colorants, deodorizing components (other than water-soluble copper compounds), pigments, buffers, pH adjusters, etc.

[0028] [Shape / dosage form] The form of the oral composition of the present invention is not particularly limited, and may be either liquid or semi-solid (gel, ointment, paste).

[0029] The formulation form of the oral composition of the present invention is not limited as long as it can be applied to the oral cavity and remain there for a certain period of time, and examples thereof include oral care products such as liquid dentifrices, toothpastes, mouthwashes, oral sprays (including throat sprays), mouthwashes, mouth fresheners, oral pastes, and gum massage creams. Of these, preferred are liquid dentifrices, toothpastes, mouthwashes, and mouthwashes, and more preferred are liquid dentifrices and toothpastes.

[0030] 2. Method for improving the solubility of hinokitiol The method for improving solubility of the present invention is a method for improving the solubility of hinokitiol in an oral composition containing hinokitiol, and is characterized by blending hinokitiol and a water-soluble copper compound into the oral composition.

[0031] In the solubility improving method of the present invention, the types and amounts of ingredients used, the shape and formulation of the oral composition, etc. are as shown in the section "1. Oral composition" above. [Example]

[0032] The present invention will be explained in more detail below by showing examples, but the present invention is not limited to these examples.

[0033] Test Example 1 The oral compositions (liquid) shown in Table 1 were prepared. Specifically, the oral compositions were prepared by adding predetermined amounts of hinokitiol dissolved in dimethyl sulfoxide or ethanol and a water-soluble copper compound (copper chlorophyllin sodium or copper gluconate) to purified water and thoroughly mixing them.

[0034] The appearance of each oral composition obtained was observed, and the degree of precipitate or insoluble matter formed was judged according to the following criteria to evaluate the solubility of hinokitiol. <Judgment criteria> ⊚: No precipitate or insoluble matter was observed, and hinokitiol was completely dissolved. ◯: Although a small amount of precipitate or insoluble matter was observed, the solubility of hinokitiol was improved and there was no practical problem. ×: Significant precipitates or insoluble matter were observed, the solubility of hinokitiol was not improved, and the product was not suitable for practical use.

[0035] The results are shown in Table 1. In oral compositions containing hinokitiol that did not contain copper chlorophyllin sodium or copper gluconate, significant precipitates or insoluble matter were observed (Comparative Examples 1 and 2). In contrast, in oral compositions containing hinokitiol and copper chlorophyllin sodium or copper gluconate, the solubility of hinokitiol was improved, and the formation of precipitates or insoluble matter was sufficiently suppressed (Examples 1 to 5). In particular, in oral compositions containing hinokitiol and copper chlorophyllin sodium, no precipitates or insoluble matter were observed, and the solubility of hinokitiol was significantly improved (Examples 1 to 3).

[0036] In addition, in Examples 4 and 5, oral compositions were prepared in which copper gluconate was replaced with copper sulfate, copper chloride, or copper nitrate, and the solubility of hinokitiol was evaluated in the same manner as above.The formation of precipitates or insoluble matter was sufficiently suppressed, and the results were similar to those of Examples 4 and 5.

[0037] [Table 1]

[0038] Prescription example A toothpaste having the composition shown in Table 2 and a liquid toothpaste having the composition shown in Table 3 were prepared. Both of these toothpastes and liquid toothpastes improved the solubility of hinokitiol and sufficiently suppressed the formation of precipitates or insoluble matter.

[0039] [Table 2]

[0040] [Table 3]

Claims

1. An oral composition containing hinokitiol and a water-soluble copper compound.

2. The oral composition according to claim 1 , wherein the water-soluble copper compound is sodium copper chlorophyllin or copper gluconate.

3. A method for improving the solubility of hinokitiol in an oral composition containing hinokitiol, comprising: A method for improving solubility by blending hinokitiol and a water-soluble copper compound into an oral composition.

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