Suitable components for nasal mucosa

Abstract

To provide novel applications of naturally occurring components that can improve a sleep disorder.SOLUTION: A nasal mucosa-applicable composition is provided that contains a Mentha plant extract and is used in preventing and / or improving a sleep disorder. The composition is effective in preventing and / or improving the sleep disorder.SELECTED DRAWING: None

Description

Technical Field

[0001] The present invention relates to a nasal mucosa-applied composition used for preventing and / or improving sleep disorders.

Background Art

[0002] In recent years, it is said that one in five Japanese people has some kind of sleep disorder, and about one in three people aged 60 or over. Sleep disorder has become a problem that can even be called a national disease.

[0003] For sleep disorders, drug therapy is generally selected. Since drug therapy needs to be carefully applied under a doctor's prescription, the hurdle is high, and there is also a tendency to avoid long-term use due to concerns about side effects.

[0004] Therefore, improvement of sleep disorders with components derived from natural products has been studied. In particular, there are many reports on the utilization of lavender mainly composed of linalyl acetate for improving sleep (for example, Non-Patent Document 1, Patent Document 1, etc.).

[0005] On the other hand, plant-derived aromatic components are known to have various physiological effects in addition to their effects on sleep. For example, it is known that peppermint, which is a raw material for producing menthol and peppermint oil, has an excitatory effect (Non-Patent Document 2), etc.

Prior Art Documents

Non-Patent Documents

[0006]

Non-Patent Document 1

Non-Patent Document 2

[0007] [Patent Document 1] Japanese Patent Publication No. 2011-051970 [Overview of the project] [Problems that the invention aims to solve]

[0008] The sleep-enhancing effects of naturally derived ingredients, such as lavender, are widely accepted. However, these naturally derived ingredients have distinctive aromas, and individual preferences vary greatly. For those who dislike the scent of the ingredient itself, it can even become a source of stress, and therefore may not effectively improve sleep. For this reason, there is a need for more options when it comes to naturally derived ingredients used to improve sleep disorders.

[0009] Therefore, the present invention aims to provide new uses for naturally derived ingredients that can improve sleep disorders. [Means for solving the problem]

[0010] As a result of diligent research, the inventors unexpectedly discovered that extracts from mint plants, which generally have stimulant effects, also have the effect of improving sleep disorders. This invention was completed by further research based on this finding.

[0011] In other words, the present invention provides inventions in the following embodiments. Item 1. A nasal mucosal composition containing an extract of a plant of the genus Mentha, used for the prevention and / or improvement of sleep disorders. Item 2. The nasal mucosal application composition according to Item 1, wherein the Mentha genus plant is selected from the group consisting of peppermint, spearmint, lavender mint, bergamot mint, and mint. Item 3. The nasal mucosal application composition according to item 1 or 2, wherein the extract comprises a component selected from the group consisting of menthol, menthone, menthofuran, limonene, pinene, carvone, dihydrocarvone, terpinyl acetate, and cineole. Item 4. A composition for nasal irrigation, which is a composition for application to the nasal mucosa in the nasal cavity as described in any of Items 1 to 3. Item 5. The nasal mucosal application composition according to any one of Items 1 to 4, wherein the sleep disorder is a sleep disorder not caused by a respiratory disease. Item 6. The nasal mucosal application composition according to any one of Items 1 to 5, wherein the sleep disorder is a sleep disorder not caused by an ear, nose, and throat disease. [Effects of the Invention]

[0012] According to the present invention, a new use for naturally derived ingredients that can improve sleep disorders is provided. [Modes for carrying out the invention]

[0013] The nasal mucosal composition of the present invention contains an extract of a plant belonging to the genus Mentha and is characterized by its use in preventing and / or improving sleep disorders. The nasal mucosal composition of the present invention will be described in detail below.

[0014] Extracts from plants of the Mentha genus. The genus Mentha is not particularly limited, but examples include peppermint, spearmint, lavender mint, bergamot mint, and mint.

[0015] In the present invention, the extract of a plant of the genus Mentha may be an extract of one of the above-mentioned plants used alone, or a combination of extracts from two or more plants may be used.

[0016] Extracts from plants of the genus Mentha can be obtained from the leaves of the above-mentioned plants by steam distillation or solvent extraction. In the case of extraction by steam distillation, high-temperature steam (gas) generated by heating is applied to the raw material to lower the boiling point of the required high-boiling-point substances and distillate them, resulting in an extract (essential oil). In the case of extraction by solvent extraction, examples include hydrocarbon solvents such as n-pentane, isopentane, n-hexane, cyclohexane, petroleum ether, ligroin, methylene chloride, ethylene dichloride, carbon tetrachloride, benzene, and toluene; lower monohydric alcohols such as methanol, ethanol, n-propanol, isopropanol, n-butanol, and isobutanol; ketone solvents such as acetone; ether solvents such as diethyl ether; and ester solvents such as methyl acetate and ethyl acetate. Extracts are obtained by extraction treatment using these solvents and then removing the solvent. Among these extracts, from the viewpoint of improving the effect of preventing and / or improving sleep disorders, extracts from plants of the genus Mentha are preferably extracts (essential oils) obtained by steam distillation.

[0017] Extracts of plants of the genus Mentha may contain components derived from the above-mentioned plants without particular limitation. For example, extracts of plants of the genus Mentha may contain components selected from the group consisting of menthol, menthone, menthofuran, limonene, pinene, carvone, dihydrocarvone, terpinyl acetate, and cineole. From the viewpoint of improving the preventive and / or ameliorative effect on sleep disorders, extracts of plants of the genus Mentha preferably contain menthol, menthone, menthofuran, and cineole, and more preferably contain 10 to 50 parts by weight of menthol, 0.5 to 5 parts by weight of menthone, 10 to 50 parts by weight of menthofuran, and 2 to 10 parts by weight of cineole per 100 parts by weight of the extract of plants of the genus Mentha.

[0018] Among the extracts of the above-mentioned Mentha plants, from the perspective of improving the preventive and / or ameliorative effects on sleep disorders, particularly preferably, an extract obtained by steam distillation of peppermint (peppermint oil) is mentioned. Most preferably, peppermint oil containing 20 to 40 parts by weight of menthol, 2 to 4 parts by weight of menthone, 20 to 30 parts by weight of menthofuran, and 4 to 9 parts by weight of cineole per 100 parts by weight of peppermint oil is mentioned.

[0019] Regarding the content of the extract of the Mentha plant in the nasal mucosa-applying composition of the present invention, it may be appropriately set according to the degree of the preventive and / or ameliorative effects on sleep disorders to be imparted. For example, 0.0005 to 0.1% by weight, preferably 0.001 to 0.01% by weight, more preferably 0.002 to 0.006% by weight can be mentioned. The content of the extract of the Mentha plant means the content of only the components derived from the Mentha plant. When the extract contains other components other than the components derived from the Mentha plant, such as the solvent used in the extraction operation, it means the amount excluding the content of such other components.

[0020] Other ingredients In the nasal mucosa-applying composition of the present invention, in addition to the above-mentioned extract of the Mentha plant, other bases and / or additives required for formulation and the like may be included as long as the effects of the present invention are not impaired. Such bases and additives are not particularly limited as long as they are pharmaceutically acceptable. For example, water, monohydric lower alcohols having 1 to 5 carbon atoms, polyhydric alcohols, surfactants, isotonic agents, preservatives, coloring agents, thickeners, pH adjusters, wetting agents, preservatives, stabilizers, antioxidants, chelating agents, adhesives, buffers, solubilizing aids, solubilizers, preservatives and other additives can be mentioned.

[0021] These base materials and additives may be used alone or in combination of two or more. The content of these base materials and additives can be appropriately set according to the dosage form and the like.

[0022] The above-mentioned surfactants specifically include nonionic surfactants, and more specifically, polyoxyethylene hydrogenated castor oil, sorbitan fatty acid esters, glycerin fatty acid esters, propylene glycol fatty acid esters, glycerin alkyl ethers, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene sorbitan fatty acid esters, polyoxyethylene glycerin fatty acid esters, polyoxyethylene fatty acid esters, polyoxyethylene alkyl or arachidyl ethers, polyoxyethylene / polyoxypropylene alkyl ethers, etc. Examples of the above-mentioned polyoxyethylene sorbitan fatty acid esters include polyoxyethylene sorbitan trioleate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan tristearate, polyoxyethylene sorbitan monostearate, polyoxyethylene sorbitan monopalmitate, polyoxyethylene sorbitan monolaurate, etc. The average number of moles of ethylene oxide (EO) added to the above-mentioned polyoxyethylene sorbitan fatty acid esters is not particularly limited, but for example, 5 to 40 moles, preferably 10 to 30 moles, more preferably 15 to 25 moles, and even more preferably 18 to 22 moles. These surfactants may be used individually or in combination of two or more. Among these surfactants, nonionic surfactants are preferred, more preferably polyoxyethylene sorbitan fatty acid esters, and even more preferably polyoxyethylene sorbitan monooleate (polyoxyethylene (18-22) sorbitan monooleate) with an added mole of 18-22 moles of ethylene oxide (EO). When the nasal mucosal application composition of the present invention contains a surfactant, the surfactant content may be, for example, 0.02-0.12% by weight, preferably 0.04-0.09% by weight, and more preferably 0.05-0.08% by weight.

[0023] In addition to the components described above, the nasal mucosal application composition of the present invention may contain other pharmacological components as needed, provided that they do not impair the effects of the present invention. Examples of such pharmacological components include vitamins, antihistamines, local anesthetics, anti-inflammatory agents, mucosal protective agents, blood circulation promoting components, cooling agents, mucopolysaccharides, and the like. These pharmacological components may be used individually or in combination of two or more. When these pharmacological components are included, their content should be appropriately determined according to the type of pharmacological component used, the desired effect, and so on.

[0024] form The form of the nasal mucosa composition of the present invention is not particularly limited as long as it is in a form that can be applied to the nasal mucosa, and examples include liquid formulations and semi-solid formulations (ointments, gels, etc.), with liquid formulations being preferred.

[0025] Purpose The nasal mucosal application composition of the present invention is used for the prevention and / or improvement of sleep disorders. In the present invention, "sleep disorder" refers to a condition in which the overall score of the Pittsburgh Sleep Quality Index (PSQIG) is 5.5 or higher. Preferably, in the present invention, the sleep disorder is a sleep disorder not caused by a respiratory disease and / or a sleep disorder not caused by an ENT disease.

[0026] The nasal mucosal composition of the present invention exhibits excellent effects in improving sleep disorders, and therefore, effective improvement can be expected even in cases of severe sleep disorders. From this viewpoint, a suitable degree of sleep disorder in the present invention is a PSQIG score of 7 or higher, preferably 8 or higher, and more preferably 8.5 or higher.

[0027] More specifically, the nasal mucosal application composition of the present invention can be used to improve sleep quality, shorten the time to fall asleep, extend the duration of sleep, improve sleep efficiency, alleviate sleep difficulties, reduce the frequency of sleep aid use, and / or improve daytime wakefulness.

[0028] Dosage / Usage The nasal mucosal application composition of the present invention is used by being applied to the mucous membrane inside the nasal cavity. The specific application method is not particularly limited as long as it is a method in which the nasal mucosal application composition of the present invention comes into contact with the nasal mucosa, and examples include washing, spraying, and coating, but washing is preferred. For this reason, the nasal mucosal application composition of the present invention is preferably used as a nasal cavity washing composition.

[0029] Specific methods of using the nasal mucosa application composition of the present invention are not particularly limited as long as the effects of application are achieved, but examples include methods of directly pouring it into the nasal cavity for cleaning, spraying it onto the mucosa with a spray, etc., and applying it directly to the mucosa using a jig. Preferably, methods of directly pouring it into the nasal cavity for cleaning are mentioned. More specifically, methods of directly pouring it into the nasal cavity for cleaning include pouring the nasal mucosa application composition, which has been prepared as a nasal cavity cleaning composition, into the nasal cavity and spitting it out through the mouth, and pouring the nasal mucosa application composition, which has been prepared as a nasal cavity cleaning composition, into one nostril and spitting it out through the other nostril.

[0030] The dosage of the nasal mucosa application composition of the present invention is appropriately set according to the degree of the sleep disorder prevention and / or improvement effect to be provided, age, etc., but for example, when converted to the amount of mint plant extract applied to the nasal mucosa per day, it is for example 5 to 100 mg, preferably 10 to 80 mg, more preferably 20 to 60 mg.

[0031] Furthermore, there are no particular limitations on the timing of applying the nasal mucosal composition of the present invention to the nasal mucosa. Examples include when waking up, before going out, when returning home, before bathing, before going to bed, etc.

[0032] The nasal mucosal application composition of the present invention is preferably applied continuously to effectively prevent and / or improve sleep disorders. For example, the nasal mucosal application composition of the present invention can be applied continuously for two weeks or more, preferably three weeks or more, and more preferably four weeks or more. [Examples]

[0033] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0034] Test example Test samples with the compositions shown in Table 1 were prepared in the form of nasal irrigation compositions. The peppermint fragrance material shown in Table 1 contains 7.33% by weight of peppermint oil (essential oil obtained by steam distillation of peppermint leaves), 52.0% by weight of ethanol, 0.2% by weight of glycerin fatty acid ester, 0.07% by weight of extracted tocopherol, and 40.4% by weight of purified water. Per 100 parts by weight of peppermint fragrance, it contains 30 parts by weight of menthol (2.2% by weight of the fragrance material), 25 parts by weight of menthofuran (1.8% by weight of the fragrance material), 6 parts by weight of cineole (1,8-cineole) (0.44% by weight of the fragrance material), and 3 parts by weight of menthone (0.22% by weight of the fragrance material).

[0035] [Table 1]

[0036] Twenty-two subjects who reported experiencing symptoms of sleep disorder, did not regularly use nasal irrigation, and were free from respiratory and ENT diseases were divided into two groups (11 in the comparative example group and 11 in the example group). Both the comparative and example groups were given nasal irrigation twice a day, after waking and before going to bed, for four weeks, using the nasal irrigation compositions of the comparative and example groups, respectively. 50 ml of the nasal irrigation composition was used per session. The Pittsburgh Sleep Quality Index (PSQI) was used for evaluation before the start of the study and at the end of the four-week study. Table 2 shows the average PSQIG score, rounded to the third decimal place. A PSQIG score of 5.5 or higher was considered indicative of sleep disorder.

[0037] [Table 2]

[0038] Table 3 also shows the improvement rate for each item of the PSQI score. The score improvement rate was calculated by rounding the value derived from the following formula to the first decimal place.

[0039]

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[0040] [Table 3]

[0041] As is clear from Table 2, applying the nasal irrigation composition of the example resulted in a PSQI score below 5.5 and an improvement in sleep disorders. Furthermore, as shown in Table 3, significant improvements were observed in each of the PSQI scores.< / url:>

Claims

1. A nasal mucosal composition containing only peppermint oil as an essential oil in an amount of 0.002 to 0.006% by weight, for the prevention and / or improvement of sleep disorders and for nasal irrigation.

2. The nasal mucosal application composition according to claim 1, wherein the sleep disorder is a sleep disorder not caused by a respiratory disease.

3. The nasal mucosal application composition according to claim 1 or 2, wherein the sleep disorder is a sleep disorder not caused by an ear, nose, and throat disease.

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