Relaxation promoter

Abstract

To provide a composition that can promote a relaxing effect and is applicable to the body.SOLUTION: The combination of (A) capsaicinoid and (B) a nonsteroidal anti-inflammatory agent can promote a relaxing effect by reducing the levels of psychological arousal and / or improving the levels of comfort.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a relaxation effect promoter used to psychologically suppress arousal and / or improve comfort. [Background technology]

[0002] In today's society, where stress is a common source, the effects of stress-induced deterioration of psychological states have become a social problem. A deterioration of psychological states can lead to mental illnesses such as depression, as well as physical illnesses. Therefore, improving psychological states by alleviating stress is important for preventing these illnesses and improving quality of life.

[0003] The effectiveness of physical exercise as a daily activity for stress reduction has been supported in various papers (e.g., Non-Patent Document 1, Non-Patent Document 2, etc.). Furthermore, a two-dimensional mood scale based on arousal and pleasantness has been developed as an objective measure of whether physical exercise actually reduces stress and improves psychological state (Non-Patent Document 3). This scale, called the TDMS-ST Two-Dimensional Mood Scale, measures mental "activity" and "stability" through self-monitoring of the subject's psychological state (mood). The reliability and validity of the scale have been confirmed, and the psychological state at the time of measurement can be quantified by answering eight questions. [Prior art documents] [Non-patent literature]

[0004] [Non-Patent Document 1] Health Science (13), p1-7, 1991 [Non-patent document 2] Journal of the Society of Biomechanisms 35(1), 15-20, 2011 [Non-patent document 3] Bull. Inst. Health & Sport Sci., Iniv. of Tsukuba 26: 27-36, 2003 Summary of the Invention [Problem to be solved by the invention]

[0005] Busy modern people are exposed to stressors, but find it difficult to find time for physical exercise. For this reason, it is desirable to have a more convenient way to achieve relaxation. For example, if there were a composition that could promote relaxation by applying it to the body, it would be a useful means of relaxation for busy modern people exposed to stressors.

[0006] Therefore, an object of the present invention is to provide a composition that has a relaxation-promoting effect and can be applied to the body. [Means for solving the problem]

[0007] As a result of extensive research, the present inventors have found that applying a combination of capsaicinoid and a nonsteroidal anti-inflammatory drug to the body can suppress psychological arousal and / or improve comfort levels based on the TDMS-ST two-dimensional mood scale, thereby promoting a relaxing effect.The present invention was completed through further research based on this finding.

[0008] That is, the present invention provides the following aspects. Item 1. A relaxation effect promoter comprising (A) a capsaicinoid and (B) a nonsteroidal anti-inflammatory agent, which is used to psychologically suppress arousal and / or improve comfort. Item 2. The relaxation effect promoter according to Item 1, wherein the component (B) is selected from the group consisting of loxoprofen and its salts, diclofenac and its salts, glycol salicylate, and methyl salicylate. Item 3. The relaxation effect promoter according to Item 1 or 2, further comprising (C) a monoterpene. Item 4. The relaxation effect promoter according to any one of Items 1 to 3, further comprising (D) an ester derivative of nicotinic acid, and (E) a component selected from the group consisting of tocopherol and its derivatives. Item 5. The agent for promoting relaxation effect according to any one of Items 1 to 4, which is a parasympathetic nerve stimulant. [Effects of the Invention]

[0009] According to the present invention, a composition that can be applied to the body and has a relaxation-promoting effect is provided. DETAILED DESCRIPTION OF THE INVENTION

[0010] The relaxation effect promoter of the present invention is characterized by comprising (A) a capsaicinoid (hereinafter sometimes referred to as "component (A)") and (B) a nonsteroidal anti-inflammatory drug (hereinafter sometimes referred to as "component (B)"), and is used to psychologically suppress arousal and / or improve comfort. Furthermore, the relaxation effect promoter of the present invention may also comprise (C) a monoterpene (hereinafter sometimes referred to as "component (C)"), or may also comprise a component selected from the group consisting of (D) an ester derivative of nicotinic acid (hereinafter sometimes referred to as "component (D)") and (E) tocopherol and its derivatives (hereinafter sometimes referred to as "component (E)"). The relaxation effect promoter of the present invention will be described in detail below.

[0011] (A) Capsaicinoid The relaxation effect promoter of the present invention contains capsaicinoid as component (A). Capsaicinoid is an N-acylvanilylamide, a known component known to promote blood circulation and the like.

[0012] The acyl group in the capsaicinoid may be either linear or branched. The number of carbon atoms in the acyl group in the capsaicinoid is not particularly limited, but may be, for example, 5 to 15, and preferably 6 to 11 from the viewpoint of further enhancing the relaxing effect.

[0013] Specific examples of capsaicinoids include nonanoic acid vanillylamide; and capsaicin derivatives such as capsaicin, dihydrocapsaicin, nordihydrocapsaicin, homocapsaicin, and homodihydrocapsaicin. From the viewpoint of further enhancing the relaxing effect, nonanoic acid vanillylamide is preferred.

[0014] In the relaxation effect promoter of the present invention, one type of capsaicinoid may be used alone as component (A), or two or more types may be used in combination.

[0015] The content of component (A) in the relaxation effect promoter of the present invention is not particularly limited as long as the effects of the present invention are achieved, but examples include 0.0015 to 0.1 wt %, preferably 0.003 to 0.05 wt %, more preferably 0.005 to 0.02 wt %, and even more preferably 0.01 to 0.02 wt %.

[0016] (B) Nonsteroidal anti-inflammatory drugs The relaxation effect promoter of the present invention contains a nonsteroidal anti-inflammatory drug as component (A). A nonsteroidal anti-inflammatory drug alone does not have the effect of promoting relaxation, but when combined with component (A), it exhibits a remarkable relaxation effect promoting effect.

[0017] The non-steroidal anti-inflammatory agent used in the relaxation effect promoter of the present invention is not particularly limited, as long as it is pharmaceutically acceptable, and examples thereof include loxoprofen, diclofenac, glycol salicylate, methyl salicylate, felbinac, indomethacin, ketoprofen, and flurbiprofen.

[0018] Furthermore, the compounds used as nonsteroidal anti-inflammatory agents may be used in the form of a salt if they can take the form of a salt. For example, diclofenac, loxoprofen, etc. may be used in the form of an alkali metal salt such as a sodium salt or a potassium salt.

[0019] In the relaxation effect promoter of the present invention, one type of nonsteroidal anti-inflammatory agent may be used alone as component (B), or two or more types of nonsteroidal anti-inflammatory agents may be used in combination.

[0020] Among these non-steroidal anti-inflammatory agents, from the viewpoint of further enhancing the relaxing effect, preferred are loxoprofen and its salts, diclofenac and its salts, glycol salicylate and methyl salicylate; preferred are loxoprofen and its salts, diclofenac and its salts, and glycol salicylate; more preferred are loxoprofen and its salts, and diclofenac and its salts; and even more preferred are salts of loxoprofen and salts of diclofenac.

[0021] The amount of the nonsteroidal anti-inflammatory agent in the relaxation effect promoter of the present invention is not particularly limited as long as the effects of the present invention are achieved, but may be, for example, 0.01 to 20% by weight, preferably 0.05 to 10% by weight. More specifically, the following ranges are suitable examples of the amount depending on the type of nonsteroidal anti-inflammatory agent used. When using loxoprofen and / or its salts : Usually 0.1 to 10% by weight, preferably 0.5 to 5% by weight, more preferably 0.8 to 2% by weight, and even more preferably 1 to 1.5% by weight When using diclofenac and / or its salts : Usually 0.1 to 10% by weight, preferably 0.3 to 5% by weight, more preferably 0.5 to 2% by weight, and even more preferably 0.8 to 1.5% by weight When using glycol salicylate and / or methyl salicylate : Usually 0.1 to 10% by weight, preferably 1 to 5% by weight, more preferably 2 to 3% by weight

[0022] The ratio of component (A) to component (B) is determined by the content of each of the above components, but from the viewpoint of further enhancing the relaxing effect, the content of component (B) per part by weight of component (A) is preferably 1 to 1500 parts by weight, more preferably 4 to 800 parts by weight. More specifically, the following ranges are suitable examples of blending ratios depending on the type of nonsteroidal anti-inflammatory agent used. When using loxoprofen and / or its salts Usually 8 to 800 parts by weight, preferably 45 to 400 parts by weight, more preferably 50 to 150 parts by weight, even more preferably 50 to 125 parts by weight, and even more preferably 90 to 100 parts by weight When using diclofenac and / or its salts Usually 8 to 800 parts by weight, preferably 25 to 400 parts by weight, more preferably 45 to 150 parts by weight, even more preferably 50 to 120 parts by weight, and even more preferably 80 to 90 parts by weight When using glycol salicylate and / or methyl salicylate Usually 8 to 800 parts by weight, preferably 80 to 400 parts by weight, more preferably 120 to 250 parts by weight, and even more preferably 190 to 220 parts by weight

[0023] (C) Monoterpenes The relaxation effect promoter of the present invention may further contain a monoterpene as component (C) for the purpose of further enhancing the relaxation effect.

[0024] Monoterpenes are terpenoid compounds having 10 carbon atoms and consisting of two isoprene units. The monoterpenes used in the relaxation effect promoter of the present invention are not particularly limited, and examples thereof include menthol, limonene, menthone, carvone, dihydrocarvone, pinene, geraniol, linalool, thymol, borneol, perillaldehyde, citral, citronellal, camphor, and cineole. When optical isomers exist, the monoterpenes used in the present invention may be any of the d-, l-, and dl-isomers.

[0025] The relaxation effect promoter of the present invention may also use an essential oil containing a monoterpene as component (C). The essential oil containing a monoterpene can be appropriately selected from known essential oils, and examples of essential oils containing menthol include peppermint oil, peppermint oil, and spearmint oil.

[0026] In the relaxation effect promoter of the present invention, one type of monoterpene may be used alone as component (C), or two or more types of monoterpenes may be used in combination. Among the components (C), menthol is preferred from the viewpoint of further enhancing the relaxation effect.

[0027] When the relaxation effect promoter of the present invention contains component (C), the content of component (C) is not particularly limited, but may be, for example, 1 to 10% by weight, and from the viewpoint of further enhancing the relaxation effect, preferably 2 to 10% by weight, more preferably 2.5 to 10% by weight, and even more preferably 3 to 10% by weight, 3 to 8% by weight, or 3 to 6% by weight. When an essential oil containing a monoterpene is used as component (C), the amount of essential oil to be blended may be appropriately set depending on the amount of the terpene contained in the essential oil so that the content of the monoterpene in the relaxation effect promoter of the present invention falls within the above range.

[0028] (D) Ester derivatives of nicotinic acid The relaxation effect promoter of the present invention may further contain a nicotinic acid ester derivative as component (D) for the purpose of further enhancing the relaxation effect. Nicotinic acid ester derivatives are known components known to have cell activating effects, etc.

[0029] Ester derivatives of nicotinic acid are not particularly limited as long as they are pharmaceutically acceptable, and examples thereof include nicotinic acid benzyl ester, nicotinic acid β-butoxyethyl ester, nicotinic acid methyl ester, and the like.

[0030] In the relaxation effect promoter of the present invention, one type of nicotinic acid ester derivative may be used alone as component (D), or two or more types of nicotinic acid ester derivatives may be used in combination. Among components (D), nicotinic acid benzyl ester is preferred from the viewpoint of further enhancing the relaxation effect.

[0031] When the relaxation effect promoter of the present invention contains component (D), the content of component (D) is not particularly limited, but may be, for example, 0.002 to 0.1% by weight, and from the viewpoint of further enhancing the relaxation effect, preferably 0.004 to 0.1% by weight, more preferably 0.008 to 0.1% by weight, even more preferably 0.01 to 0.1% by weight, 0.01 to 0.05% by weight, or 0.01 to 0.03% by weight.

[0032] (E) Tocopherol and its derivatives (tocopherols) The relaxation effect promoter of the present invention may further contain tocopherol and its derivatives (hereinafter also referred to as "tocopherols") as component (E) in order to further enhance the relaxation effect. Tocopherol is a well-known component also known as vitamin E.

[0033] Tocopherol may be either d- or dl-isomer, and may have any of the structures α, β, γ, and δ. Specific examples of tocopherol include d-α-tocopherol, d-β-tocopherol, d-γ-tocopherol, d-δ-tocopherol, l-α-tocopherol, l-β-tocopherol, l-γ-tocopherol, l-δ-tocopherol, and mixtures thereof such as dl-α-tocopherol, dl-β-tocopherol, dl-γ-tocopherol, and dl-δ-tocopherol.

[0034] A tocopherol derivative is a compound that has the same skeleton as tocopherol and can be obtained by adding a substituent to tocopherol.

[0035] Like tocopherol, the tocopherol derivative may be either a d- or dl-isomer, and may have any of the α, β, γ, and δ structures. The type of tocopherol derivative is not particularly limited as long as it is pharmaceutically acceptable, and examples thereof include esters of tocopherol and organic acids. Specific examples of esters of tocopherol and organic acids include tocopherol acetate, tocopherol nicotinate, tocopherol succinate, and tocopherol linoleate.

[0036] In the relaxation effect promoter of the present invention, one type of tocopherol may be used alone as component (E), or two or more types of tocopherols may be used in combination. Among the components (E), from the viewpoint of further enhancing the relaxation effect, tocopherol derivatives are preferred, esters of tocopherol and organic acids are more preferred, and tocopherol acetate is even more preferred.

[0037] When the relaxation effect promoter of the present invention contains component (E), the content of component (E) is not particularly limited, but may be, for example, 0.02 to 2% by weight, and from the viewpoint of further enhancing the relaxation effect, preferably 0.04 to 2% by weight, more preferably 0.08 to 2% by weight, even more preferably 0.1 to 2% by weight, 0.1 to 1% by weight, 0.1 to 0.5% by weight, or 0.1 to 0.3% by weight.

[0038] Other ingredients The relaxation effect promoter of the present invention may contain, as necessary, other pharmacological ingredients in addition to the above-mentioned ingredients, as long as the effects of the present invention are not impaired. There are no particular limitations on the other pharmacological ingredients that can be incorporated into the relaxation effect promoter of the present invention, and examples thereof include antihistamines, local anesthetics, and herbal extracts.

[0039] Furthermore, the relaxation effect promoter of the present invention may contain, in addition to the above-mentioned components, a base and / or additives, if necessary.

[0040] Examples of bases include aqueous bases such as water, monohydric lower alcohols (having 1 to 5 carbon atoms), and polyhydric alcohols, and oily bases. Examples of additives include pH adjusters, surfactants, emulsifiers, solubilizers, antiseptics, preservatives, antioxidants, stabilizers, chelating agents, thickeners, fragrances, and colorants.

[0041] Among the above bases, from the viewpoint of further enhancing the relaxing effect, preferred are water and monohydric lower alcohols, more preferably water and ethanol. When the relaxation effect promoter of the present invention contains water, the content of water / ethanol is, for example, 10 to 70% by weight, preferably 15 to 60% by weight, more preferably 20 to 50% by weight, more preferably 25 to 40% by weight, and even more preferably 25 to 30% by weight. When the relaxation effect promoter of the present invention contains ethanol, the content of ethanol is, for example, 30 to 90% by weight, preferably 40 to 85% by weight, more preferably 50 to 80% by weight, more preferably 60 to 75% by weight, and even more preferably 65 to 75% by weight.

[0042] Formulation The formulation of the relaxation effect promoter of the present invention is not particularly limited as long as it is applicable to the body, and can typically be formulated as an external preparation. Specific examples of formulations of the relaxation effect promoter of the present invention include liquids (including lotions, sprays, aerosols, and emulsions), foams, ointments, creams, gels, patches, etc. Among these, liquids or gels are preferred, and liquids are particularly preferred. These formulations can be prepared by formulating them using additives appropriate for the formulation, according to known methods described in the General Provisions for Preparations in the 17th Edition of the Japanese Pharmacopoeia, etc.

[0043] Purpose The agent for enhancing the relaxation effect of the present invention is used for the purpose of enhancing the relaxation effect by suppressing psychological arousal and / or improving comfort.

[0044] Psychological arousal and comfort are measured using the Two-Dimensional Moods Scale-Short Term (TDMS-ST), a scale used to quantify psychological states. This scale measures the subject's mental "activity" and "stability," and its reliability and validity have been confirmed. In other words, the promotion of relaxation effects can be confirmed by confirming the suppression of psychological arousal and / or the improvement of comfort.

[0045] Furthermore, the relaxation effect promoter of the present invention can also stimulate the parasympathetic nervous system, and therefore can also be used as a parasympathetic nervous system stimulator.

[0046] Therefore, specific subjects for which the relaxation effect promoter of the present invention can be used include people who are under psychological stress and need to be relieved of that stress.

[0047] Because the relaxation effect promoter of the present invention can promote relaxation from a psychological perspective, it is preferably used for people who do not have physical symptoms that require the enjoyment of known effects based on the above-mentioned components (A) and (B), and the optionally blended components (C), (D), and / or (E). Examples of physical symptoms that require the enjoyment of such known effects include physical pain such as shoulder pain (including stiff shoulders), lower back pain, neuralgia, and muscle pain. However, the relaxation effect promoter of the present invention can also be used for people who have the above-mentioned physical symptoms in addition to psychological stress, with the aim of relaxing both psychologically and physically.

[0048] When the relaxation effect promoter of the present invention is applied externally, the application site is preferably the neck and / or surrounding areas where nerves are concentrated (for example, shoulders, back, back of the head, etc.). [Example]

[0049] The present invention will be explained in more detail below by showing examples, but the present invention is not limited to these examples.

[0050] Each component shown in Table 1 was weighed out, stirred, and dissolved to prepare a test sample (liquid). The prepared test sample was filled into a container with a sponge application area. A person experiencing psychological stress was selected as the test subject, and the test sample was applied once to the shoulder and then allowed to rest for 10 minutes.

[0051] Before and after applying the test sample, the "comfort level" and "alertness level" based on the TDMS-ST two-dimensional mood scale were measured for seven subjects, and the average values ​​were calculated. The changes in "comfort level" and "alertness level" before and after applying the test sample were calculated using the following formula. Furthermore, LF (low frequency: power value in the low frequency band of 0.04-0.15 Hz that reflects sympathetic nervous function) and HF (high frequency: power value in the high frequency band of 0.15 Hz-0.40 Hz that reflects parasympathetic nervous function) were measured using a heart rate sensor, and the average value of their ratio (LF / HF) was calculated. The reduction value of LF / HF was calculated using the following formula.

[0052]

number

[0053]

number

[0054]

number

[0055] The maximum score for "comfort" is 20 and the minimum score is -20, with a higher score indicating a higher comfort level, i.e., a greater psychological relaxation effect. The maximum score for "alertness" is 20 and the minimum score is -20, with a lower score indicating a lower level of arousal, i.e., a greater psychological relaxation effect. The promotion of relaxation was evaluated by rating the degree of improvement in comfort and suppression of arousal based on the following criteria. The results are shown in Table 1.

[0056] <Improvement in comfort> 8: The change amount of the "comfort" score is 19 or more 7: The change amount of the "comfort" score is 16 or more and less than 19 6: The change amount of the "comfort" score is 13 or more and less than 16 5: The change amount of the "comfort" score is 10 or more and less than 13 4: The change amount of the "comfort" score is 7 or more and less than 10 3: The change amount of the "comfort" score is 4 or more and less than 7 2: The change amount of the "comfort" score is 1 or more and less than 4 1: The change amount of the "comfort" score is less than 1

[0057] <Suppression of arousal> 8: The change amount of the "arousal" score is -19 or less 7: The change amount of the "arousal" score is more than -19 and -16 or less 6: The change amount of the "arousal" score is more than -16 and -13 or less 5: The change amount of the "arousal" score is more than -13 and -10 or less 4: The change amount of the "arousal" score is more than -10 and -7 or less 3: The change amount of the "arousal" score is more than -7 and -4 or less 2: The change amount of the "arousal" score is more than -4 and -1 or less 1: The change amount of the "arousal" score is more than -1

[0058] The lower the LF / HF ratio, the more the parasympathetic nerve is enhanced and the higher the relaxation effect. Based on the following criteria, the degree of reduction in the LF / HF ratio was scored to evaluate the promoting effect of the relaxation effect. The results are shown in Table 1. <LF / HF reduction> 6: The reduction value of the LF / HF ratio is 0.21 or more 5: The reduction value of the LF / HF ratio is 0.16 or more and less than 0.21 4: The reduction value of the LF / HF ratio is 0.10 or more and less than 0.16 3: The reduction value of the LF / HF ratio is 0.06 or more and less than 0.10 2: The reduction value of the LF / HF ratio is 0.01 or more and less than 0.06 1: LF / HF ratio reduction of less than 0.01

[0059] [Table 1]

[0060] As is clear from Table 1, the (A) component alone was not found to be effective in promoting the relaxing effect (Comparative Example 1), and the (B) component alone did not promote the relaxing effect at all (Comparative Example 2). However, when the (A) component and the (B) component were combined, a significant promotion of the relaxing effect was observed (Examples 1 to 6). Furthermore, when the (C) component was further combined, the promoting effect of the relaxing effect was further enhanced (Example 4), and when the (C), (D), and (E) components were combined, the promotion of the relaxing effect was further enhanced (Examples 5 to 6). Furthermore, when the (A) component in Examples 1 to 6 was reduced to 0.02 wt %, a significant promotion of the relaxing effect was observed, similar to Examples 1 to 6.

[0061] This alleviated the psychological stress experienced by the subjects, resulting in a relaxing effect. Among the subjects, there were some who, while experiencing psychological stress, did not suffer from symptoms such as stiff shoulders, which were known to be suitable for use based on the component composition of the test sample. For these subjects, a psychological relaxing effect was observed immediately, just 10 minutes after application. Furthermore, some subjects also suffered from stiff shoulders in addition to psychological stress. For these subjects with stiff shoulders, the psychological relaxing effect due to the alleviation of psychological stress, as shown in Table 1, was confirmed. Furthermore, by continuing to apply the product three times a day, the stiff shoulders were also reduced, and a physical relaxing effect was also observed.

[0062] Prescription example Test samples (liquids) shown in Table 2 were prepared. The test samples were filled into a container with a sponge application section and prepared in the form of a topical composition. The relaxing effect of each test sample was confirmed in the same manner as in the Examples. Formulation Examples 1 to 3 were found to improve comfort and suppress arousal to the same extent as Examples 1 to 3, respectively, and were able to provide a relaxing effect. Furthermore, Formulation Examples 4 to 10 were found to improve comfort and suppress arousal to the same extent as Examples 5 to 6, and were able to provide a relaxing effect.

[0063] [Table 2]

Claims

1. A relaxation effect promoter comprising (A) a capsaicinoid and (B) at least one of diclofenac, a salt of diclofenac, glycol salicylate, and methyl salicylate, which is used to psychologically suppress arousal and / or improve comfort, and is used as a parasympathetic nervous system stimulant.

2. The relaxation effect promoter according to claim 1, further comprising (C) a monoterpene.

3. The relaxation effect promoter according to claim 1 or 2, further comprising (D) at least one of nicotinic acid benzyl ester, nicotinic acid β-butoxyethyl ester, and nicotinic acid methyl ester, and / or (E) at least one of tocopherol and an ester of tocopherol with an organic acid.

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