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 and having improved solubility of hinokitiol.

Background Art

[0002] In recent years, due to the diversification of eating habits and the like, oral diseases such as dental caries and periodontal diseases have been spreading. Dental caries and periodontal diseases are bacterial infectious diseases in which oral bacteria in dental plaque formed in hard tissues or periodontal pockets are greatly involved in the onset. As causative bacteria of dental caries, streptococci such as Streptococcus mutans (S. mutans) are known, and as causative bacteria of periodontal diseases, Porphyromonas gingivalis (P. gingivalis) and the like are known. 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, in order to reduce the number of pathogenic bacteria of dental caries and periodontal diseases, a bactericide has been incorporated into oral compositions such as dentifrices and mouthwashes. Although various bactericides incorporated into oral compositions are known, hinokitiol is widely used in oral compositions because of its low toxicity and broad antibacterial spectrum. Conventionally, various formulations of oral compositions containing hinokitiol have been proposed. For example, Patent Document 1 discloses that the bactericidal action can be synergistically improved by incorporating lemongrass citral together with hinokitiol into an oral composition.

[0004] On the other hand, hinokitiol has a drawback that its solubility in water is low, and when it is incorporated into an oral composition, it is difficult to solubilize or precipitates are likely to be formed. Therefore, in an oral composition containing hinokitiol, the development of a formulation technology for enhancing the solubility of hinokitiol is required.

Prior Art Documents

Patent Documents

[0005]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0006] An object of the present invention is to provide a formulation technology that can enhance the solubility of hinokitiol and suppress the formation of precipitates and insoluble substances caused by hinokitiol in an oral composition containing hinokitiol.

Means for Solving the Problems

[0007] As a result of intensive studies to solve the above problems, the present inventors have found that in an oral composition, by blending a water-soluble copper compound together with hinokitiol, the solubility of hinokitiol is improved and the formation of precipitates and insoluble substances caused by hinokitiol can be suppressed. The present invention has been completed by further studies based on such findings.

[0008] That is, the present invention provides an invention in 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 sodium copper chlorophyllin or copper gluconate. Item 3. A method for improving the solubility of hinokitiol in an oral composition containing hinokitiol, A method for improving solubility, wherein an oral composition is blended with hinokitiol and a water-soluble copper compound.

Effects of the Invention

[0009] According to the present invention, in an oral composition containing hinokitiol, the solubility of hinokitiol can be enhanced and the formation of precipitates and insoluble substances caused by hinokitiol can be suppressed.

Modes for Carrying Out the Invention

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

[0011] [Hinokitiol] The oral composition of the present invention contains hinokitiol. Hinokitiol is a known compound having a bactericidal action and the like.

[0012] In the present invention, hinokitiol may be a natural product-derived one or a chemically synthesized one. Further, the hinokitiol used in the present invention may be a purified product or a roughly purified product. For example, a hinokitiol-containing essential oil obtained from trees can also be used.

[0013] The content of hinokitiol in the oral composition of the present invention may be appropriately set according to the type of the oral composition, the degree of the bactericidal action to be imparted, etc. For example, 0.0005 to 1% by weight, preferably 0.005 to 0.8% by weight, more preferably 0.01 to 0.5% by weight can be mentioned.

[0014] [Water-soluble copper compound] The oral composition of the present invention contains a water-soluble copper compound in addition to hinokitiol. In the oral composition of the present invention, the water-soluble copper compound plays a role of enhancing the solubility of hinokitiol and suppressing the formation of precipitates and insoluble matters by hinokitiol.

[0015] The water-soluble copper compound is a water-soluble copper complex and a copper salt. The types of the water-soluble copper complex are not particularly limited as long as they are applicable in the oral cavity. For example, alkali metal salts of copper chlorophyllin (such as sodium copper chlorophyllin) and the like can be mentioned. Further, the types of the water-soluble copper salts are not particularly limited as long as they are applicable in the oral cavity. For example, copper gluconate, copper sulfate, copper chloride, copper nitrate, copper acetate, copper lactate, copper butyrate, copper formate, copper phosphate, copper malate, copper succinate, copper malonate, copper maleate and the like can be mentioned.

[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, preferably alkali metal salts of copper chlorophyllin, copper gluconate, more preferably alkali metal salts of copper chlorophyllin, and even more preferably sodium copper chlorophyllin can be mentioned.

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

[0018] In the oral composition of the present invention, the ratio of hinokitiol to the water-soluble copper compound is determined according to the respective contents of these two components. For example, per 1 part by weight of hinokitiol, the total amount of the water-soluble copper compound 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 aforementioned components.

[0020] When the oral composition of the present invention contains dimethyl sulfoxide, its content is not particularly limited. For example, it is 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 as needed. In the present invention, the monohydric lower alcohol refers to a monohydric alcohol having 1 to 5 carbon atoms.

[0022] Regarding the types of monohydric lower alcohols, there are no particular restrictions as long as they are applicable in the oral cavity. For example, ethanol, n-propanol, isopropanol, n-butanol, sec-butanol, tert-butanol, n-amyl alcohol, sec-amyl alcohol, isoamyl alcohol, tert-amyl alcohol, neopentyl alcohol, etc. can be mentioned. These monohydric lower alcohols may be used alone or in combination of two or more.

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

[0024] When the oral composition of the present invention contains a monohydric lower alcohol, its content is not particularly limited. For example, 0.001 to 5% by weight, preferably 0.01 to 2% by weight, more preferably 0.05 to 1% by weight can be mentioned.

[0025] [Water] The oral composition of the present invention contains water as a solvent. Regarding the water content in the oral composition of the present invention, it may be the remainder excluding the components to be added. For example, 30 to 99% by weight, preferably 40 to 99% by weight, 50 to 98% by weight can be mentioned.

[0026] [Other components] The oral composition of the present invention may contain other medicinal components as necessary in addition to the aforementioned components. Such medicinal components are not particularly limited as long as they can be formulated in pharmaceuticals, oral care products, etc. For example, iodine-based bactericidal components, bronchodilators, cough suppressants, expectorants, anti-inflammatory agents, glucosyltransferase inhibitors, plaque inhibitors, hypersensitivity inhibitors, tartar prevention agents, analgesics, antihistamines, bactericides, gastric mucosal protectants, caffeine, vitamins, Chinese herbal medicines, crude drug components, etc. can be mentioned.

[0027] In addition, the oral composition of the present invention may contain a base or an additive in order to obtain a desired dosage form. Such bases and additives are not particularly limited as long as they can be incorporated into pharmaceuticals, oral care products, etc. Examples include oily components, polyhydric alcohols, surfactants, cooling agents, preservatives, thickeners, fragrances, flavoring agents, pigments, deodorizing components (other than water-soluble copper compounds), colorants, buffers, pH adjusters, and the like.

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

[0029] The dosage form of the oral composition of the present invention is not limited as long as it can be applied in the oral cavity and retained therein for a certain period of time. Examples include oral care products such as liquid dentifrices, paste dentifrices, mouthwashes, oral sprays (including throat sprays), gargles, oral cooling agents, oral pastes, and gum massage creams. Among these, liquid dentifrices, paste dentifrices, mouthwashes, and gargles are preferred, and liquid dentifrices and paste dentifrices are more preferred.

[0030] 2. Method for improving 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, characterized by incorporating hinokitiol and a water-soluble copper compound into the oral composition.

[0031] In the method for improving solubility of the present invention, the types and amounts of components used, the shape and dosage form of the oral composition, etc. are as described in the section of "1. Oral composition" above.

Examples

[0032] Examples are shown below to more specifically explain the present invention, but the present invention is not limited thereto.

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

[0034] The appearance of each obtained oral composition was observed, and the degree of precipitates or insolubles formed was judged according to the following criteria to evaluate the solubility of hinokitiol. <Judgment Criteria> ◎: No precipitates or insolubles are formed at all, and hinokitiol is completely dissolved. ○: Slight precipitates or insolubles are observed, but the solubility of hinokitiol is improved, and there is no problem in practical use. ×: Precipitates or insolubles are significantly observed, the solubility of hinokitiol is not improved, and it cannot be put into practical use.

[0035] The results are shown in Table 1. In the oral composition containing hinokitiol, when sodium copper chlorophyllin or copper gluconate was not contained, significant precipitates or insolubles were observed (Comparative Examples 1 and 2). In contrast, in the oral composition containing hinokitiol and sodium copper chlorophyllin or copper gluconate, the solubility of hinokitiol was improved, and the formation of precipitates or insolubles was sufficiently suppressed (Examples 1 to 5). In particular, in the oral composition containing hinokitiol and sodium copper chlorophyllin, no precipitates or insolubles were observed at all, and the solubility of hinokitiol was significantly improved (Examples 1 to 3).

[0036] Also, in Examples 4 and 5, an oral composition in which copper gluconate was changed to copper sulfate, copper chloride, or copper nitrate was prepared, and the solubility of hinokitiol was evaluated in the same manner as above. As a result, the formation of precipitates or insolubles was sufficiently suppressed, and the same results as in Examples 4 and 5 were obtained.

[0037]

Table 1

[0038] Formulation Example A dentifrice having the composition shown in Table 2 and a liquid dentifrice having the composition shown in Table 3 were prepared. In both of these dentifrices, the solubility of hinokitiol was improved, and the formation of precipitates or insoluble substances was sufficiently suppressed.

[0039] [Table 2]

[0040] [Table 3]

Claims

1. A dental composition containing hinokitiol and a water-soluble copper compound, further containing dimethyl sulfoxide and / or a monohydric alcohol having 1 to 5 carbon atoms.

2. The dental 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 a dental composition containing hinokitiol, The method for improving solubility, which comprises blending hinokitiol, a water-soluble copper compound, dimethyl sulfoxide and / or a monohydric alcohol having 1 to 5 carbon atoms into the dental composition.

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