Composition for relieving skin itching or irritation containing thymol trimethoxycinnamate

Abstract

To provide a composition having a superior effect of relieving skin itch or skin irritation.SOLUTION: The present disclosure discloses a composition for relieving skin itch or irritation, which contains thymol trimethoxycinnamate or a stereoisomer, salt, hydrate or solvate thereof as an active ingredient, and a method for relieving skin itch or skin irritation by administering the composition to a subject in need of reliving of skin itch or irritation. The composition according to an aspect of the present disclosure has a superior effect of relieving skin itch or skin irritation by inhibiting the voltage-gated sodium channel Nav1.7 without side effects.SELECTED DRAWING: Figure 1

Description

Technical Field

[0001] This specification relates to a composition for relieving skin itching or irritation.

Background Art

[0002] Itching is a major symptom of skin diseases, referring to the feeling that causes the urge to scratch, which is an avoidance reaction to harmful stimuli and can also be caused by systemic or mental diseases in addition to skin diseases.

[0003] Both central and peripheral mediators play important roles in pruritus (itching). Pro-inflammatory mediators cause pruritus in inflammatory skin diseases such as eczema. Most of these mediators can also cause other signs of inflammation, namely pain, erythema due to vasodilation, increased vascular permeability, etc. In addition, itching can be caused by factors secreted from histamine and other mast cells, and increased activity of prostaglandins. In addition, itching signals can also be transmitted through various receptors distributed in peripheral nerves by bile acids, proteolytic enzymes, cytokines, neuropeptides, and compounds such as chloroquine and opioids. Although anti-itch agents are used for these various targets, drugs have limitations. Locally, calamine lotion has a weak effect on relieving itching, and steroids can reduce inflammation and relieve itching, but it is difficult to use them in the long term. In the case of calcineurin inhibitors, it is known that they cause pain temporarily and increase the risk of malignant tumors. Menthol and capsaicin lotion can contribute to the relief of itching by activating ion channels (such as TRPM8 and TRPV1) distributed in each nerve, but they have the disadvantage of being too stimulating. Anti-histamine agents have the limitation that they are limited to cases where pruritus is caused by histamine, such as eczema. (Non-Patent Document 1)

[0004] On the other hand, local anesthetics such as lidocaine, pramoxine, and prilocaine also reduce the passage of sodium ions through the nerve membrane that transmits nerve signals, preventing the transmission of signals of irritation and itching, and are thus used for relieving itching and pain.

[0005] Thus, receptors for various stimuli, pain, and itching mediators are distributed on the skin and skin nerves, which are the main peripheral tissues that sense stimuli. Each stimulus received by such receptors is transmitted to the central nervous system in the form of an electrical signal in the nervous system. As the main ion channel that plays such a role, the voltage-gated sodium channel is known. In particular, the correlation between the voltage-dependent sodium channel and itching has recently been reported in papers. (Non-Patent Document 2; Non-Patent Document 3; Non-Patent Document 4). Also, lidocaine, pramoxine, etc., which are local anesthetics used as itching relievers, are traditional non-selective sodium channel blockers.

Prior Art Documents

Non-Patent Documents

[0006]

Non-Patent Document 1

Non-Patent Document 2

Non-Patent Document 3

Non-Patent Document 4

Summary of the Invention

Problems to be Solved by the Invention

[0007] In one aspect, the present invention aims to provide a composition having an excellent effect of relieving skin itching or skin irritation.

Means for Solving the Problems

[0008] In one aspect, the present invention provides a composition for relieving skin itching or irritation, comprising thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates as an active ingredient.

[0009] In an exemplary embodiment, the thymol trimethoxycinnamate can be represented by the following Chemical Formula 1.

[0010]

Chemical Formula

[0011] In an exemplary embodiment, the dosage of the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates may be 0.37 to 37 mg / kg / day.

[0012] In an exemplary embodiment, the active ingredient can inhibit the voltage-dependent sodium channel Nav1.7.

[0013] In an exemplary embodiment, the itching or irritation of the skin may be caused by a chemical substance.

[0014] In an exemplary embodiment, the chemical substance may be a veratrum alkaloid, and the veratrum alkaloid may be veratridine.

[0015] In an exemplary embodiment, the composition may be a composition for external use on the skin.

[0016] In an exemplary embodiment, the composition may be a food, cosmetic or pharmaceutical composition.

Advantages of the Invention

[0017] On one hand, the composition containing thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates according to the present invention as an active ingredient has an excellent effect of relieving skin itching without side effects.

[0018] On another hand, the composition containing thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates according to the present invention as an active ingredient has an excellent effect of relieving skin irritation without side effects.

[0019] On another hand, the composition containing thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates according to the present invention as an active ingredient can inhibit the voltage-gated sodium channel Nav1.7.

Brief Description of the Drawings

[0020]

Figure 1

Figure 2

DETAILED DESCRIPTION OF THE INVENTION

[0021] The present invention will be described in detail below.

[0022] In one aspect, the present invention provides a composition for relieving skin itching or irritation, comprising thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates as an active ingredient.

[0023] In one embodiment, the thymol trimethoxycinnamate can be represented by the following Chemical Formula 1: (5-methyl-2-propan-2-ylphenyl)(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate.

[0024]

CHEMICAL

[0025] As used herein, "stereoisomers" include optical isomers, such as essentially pure enantiomers, essentially pure diastereomers, or mixtures thereof.

[0026] As used herein, "essentially pure", when used in connection with, for example, enantiomers or diastereomers, means that a specific compound, which can be exemplified by the enantiomers or diastereomers, is present in an amount of about 90% or more, preferably about 95% or more, more preferably about 97% or more or about 98% or more, still more preferably about 99% or more, and even more preferably about 99.5% or more (w / w).

[0027] As used herein, "salt" means a salt according to one aspect of the present invention that is acceptable in pharmaceuticals, cosmetics and foods and has the preferred activity of the parent compound. The salt is formed by (1) an inorganic acid such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, etc.; or an acid addition salt formed by an organic acid such as acetic acid, propionic acid, hexanoic acid, cyclopentanepropionic acid, glycolic acid, pyruvic acid, lactic acid, malonic acid, succinic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, benzoic acid, 3-(4-hydroxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, 4-methylbicyclo[2,2,2]-oct-2-ene-1-carboxylic acid, glucoheptonic acid, 3-phenylpropionic acid, trimethylacetic acid, tert-butylacetic acid, lauryl sulfuric acid, gluconic acid, glutamic acid, hydroxynaphthoic acid, salicylic acid, stearic acid, muconic acid; or (2) a salt formed when the acidic proton present in the parent compound is replaced. Also, the salt may be a pharmaceutically acceptable salt.

[0028] As used herein, "pharmaceutically acceptable" means that it can be used in animals, more specifically in humans, by avoiding significant toxic effects when used at normal medicinal dosages, and can be approved by a government or a regulatory agency equivalent thereto, or has been approved, or is listed in a pharmacopoeia, or is otherwise recognized as being described in a common pharmacopoeia.

[0029] As used herein, "hydrate" means a compound to which water is bonded, and is a broad concept including inclusion compounds in which there is no chemical bonding force between water and the compound.

[0030] As used herein, "solvate" means a higher-order compound formed between the molecules and ions of a solute and the molecules and ions of a solvent.

[0031] As used herein, "active ingredient" means a component that can exhibit the desired activity alone or in combination with a carrier having no self-activity.

[0032] In one embodiment, the content of thymol trimethoxycinnamate, its stereoisomer, salt, hydrate or solvate may be 0.001 to 20% by weight based on the total weight of the composition. When the content of thymol trimethoxycinnamate, its stereoisomer, salt, hydrate or solvate is less than 0.001% by weight, the itching or irritation-relieving effect on the skin decreases, and when it exceeds 20% by weight, the stability of the dosage form decreases. Specifically, the content of thymol trimethoxycinnamate, its stereoisomer, salt, hydrate or solvate is 0.001% by weight or more, 0.002% by weight or more, 0.003% by weight or more, 0.004% by weight or more, 0.005% by weight or more, 0.01% by weight or more, 0.02% by weight or more, 0.03% by weight or more, 0.04% by weight or more, 0.05% by weight or more, 0.06% by weight or more, 0.07% by weight or more, 0.1% by weight or more, 0.2% by weight or more, 0.3% by weight or more, 0.4% by weight or more, 0.5% by weight or more, 0.6% by weight or more, 0.7% by weight or more, 1% by weight or more, 1.5% by weight or more, 2% by weight or more, 2.5% by weight or more, 3% by weight or more, 3.5% by weight or more, 4% by weight or more, 4.5% by weight or more or 5% by weight or more, and may be 20% by weight or less, 19.9% by weight or less, 19.8% by weight or less, 19.7% by weight or less, 19.6% by weight or less, 19.5% by weight or less, 19.4% by weight or less, 19.3% by weight or less, 19.2% by weight or less, 19.1% by weight or less, 19% by weight or less, 18.8% by weight or less, 18.6% by weight or less, 18.4% by weight or less, 18.2% by weight or less, 18% by weight or less, 17.8% by weight or less, 17.6% by weight or less, 17.4% by weight or less, 17.2% by weight or less, 17% by weight or less, 16.8% by weight or less, 16.6% by weight or less, 16.4% by weight or less, 16.2% by weight or less, 16% by weight or less, 15.5% by weight or less, 15% by weight or less, 14.5% by weight or less, 14% by weight or less, 13.5% by weight or less, 13% by weight or less, 12.5% by weight or less, 12% by weight or less, 11.5% by weight or less, 11% by weight or less, 10.5% by weight or less or 10% by weight.

[0033] In one embodiment, the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates may be administered at a dosage of 0.37 to 37 mg / kg / day. When the dosage of the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates is less than 0.37 mg / kg / day, the itching or irritation-relieving effect on the skin decreases, and when it exceeds 37 mg / kg / day, it may cause irritation to the skin.Specifically, the dosage of thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates by administration of the composition is 0.37 mg / kg / day or more, 0.38 mg / kg / day or more, 0.39 mg / kg / day or more, 0.4 mg / kg / day or more, 0.41 mg / kg / day or more, 0.42 mg / kg / day or more, 0.43 mg / kg / day or more, 0.44 mg / kg / day or more, 0.45 mg / kg / day or more, 0.5 mg / kg / day or more, 0.55 mg / kg / day or more, 0.6 mg / kg / day or more, 0.65 mg / kg / day or more, 0.7 mg / kg / day or more, 0.8 mg / kg / day or more, 0.9 mg / kg / day or more, 1 mg / kg / day or more, 1.1 mg / kg / day or more, 1.2 mg / kg / day or more, 1.3 mg / kg / day or more, 1.5 mg / kg / day or more, 1.7 mg / kg / day or more, 2 mg / kg / day or more, 3 mg / kg / day or more, 4 mg / kg / day or more, 5 mg / kg / day or more, 6 mg / kg / day or more, 7 mg / kg / day or more, 8 mg / kg / day or more, 9 mg / kg / day or more, 10 mg / kg / day or more, 11 mg / kg / day or more, 12 mg / kg / day or more, 13 mg / kg / day or more, 14 mg / kg / day or more or 15 mg / kg / day or more, and may be 37 mg / kg / day or less, 36.5 mg / kg / day or less, 36 mg / kg / day or less, 35.5 mg / kg / day or less, 35 mg / kg / day or less, 34.5 mg / kg / day or less, 34 mg / kg / day or less, 33.5 mg / kg / day or less, 33 mg / kg / day or less, 32.5 mg / kg / day or less, 32 mg / kg / day or less, 31.5 mg / kg / day or less, 31 mg / kg / day or less, 30.5 mg / kg / day or less, 30 mg / kg / day or less, 29.5 mg / kg / day or less, 29 mg / kg / day or less, 28.5 mg / kg / day or less, 28 mg / kg / day or less, 27.5 mg / kg / day or less, 27 mg / kg / day or less, 26.5 mg / kg / day or less, 26 mg / kg / day or less, 25.5 mg / kg / day or less, 25 mg / kg / day or less, 24.5 mg / kg / day or less, 24 mg / kg / day or less, 23.5 mg / kg / day or less or 23 mg / kg / day or less.

[0034] In one embodiment, the composition can inhibit the voltage-dependent sodium channel Nav1.7.

[0035] In one embodiment, the itching or irritation of the skin may be caused by a chemical substance. For example, the chemical substance may be a veratrum alkaloid, and preferably the veratrum alkaloid is veratridine.

[0036] In one embodiment, the administration route of the composition is not limited, but may preferably be transdermal or for external use on the skin.

[0037] In one embodiment, the composition may be a cosmetic composition. The cosmetic composition may be, for example, a softening lotion, a astringent lotion, a nutritive lotion, a nutritive cream, a massage cream, an eye cream, an eye essence, an essence, a cleansing cream, a cleansing lotion, a cleansing foam, a cleansing water, a pack, a powder, a body lotion, a body cream, a body essence, a body wash, a hair dye, a shampoo, a conditioner, a hair styling agent, a hair nourishing agent, an ointment, a gel, a cream, a patch, an aerosol, a powder agent, and a skin patch type, etc., but is not limited thereto.

[0038] Also, in each dosage form, other components other than the essential components described above can be easily and appropriately selected and formulated by those skilled in the art according to the type of other external preparations or the purpose of use, etc.

[0039] The cosmetic composition may be provided in any dosage form suitable for topical application. For example, it may be provided in the dosage form of a solution, an emulsion obtained by dispersing an oil phase in an aqueous phase, an emulsion obtained by dispersing an aqueous phase in an oil phase, a suspension, a solid, a gel, a powder, a paste, a microneedle, a foam or an aerosol composition. The composition of such a dosage form may be produced by a conventional method in the art.

[0040] In addition to the compounds described herein, the cosmetic composition according to the present specification may further contain functional additives and components contained in general cosmetic compositions. The functional additives may include components selected from the group consisting of water-soluble vitamins, oil-soluble vitamins, high molecular weight peptides, high molecular weight polysaccharides, sphingolipids, and seaweed extracts. The cosmetic composition according to the present specification may contain other components that can preferably provide a synergistic effect to the main effect, within the range that does not impair the main effect. Further, the cosmetic composition according to the present specification may further contain a humectant, an emollient, a surfactant, an ultraviolet absorber, a preservative, a bactericide, an antioxidant, a pH adjuster, organic and inorganic pigments, a fragrance, a cooling agent, or an antiperspirant. The blending amount of the above components can be easily selected by those skilled in the art within the range that does not impair the object and effect of the present specification, and the blending amount may be 0.001 to 10% by weight, specifically 0.01 to 3% by weight based on the total weight of the composition.

[0041] In one embodiment, the composition may be a food composition. The dosage form of the food composition is not particularly limited, and for example, it can be formulated into tablets, granules, pills, powders, liquid preparations such as drink preparations, caramels, gels, bars, tea bags, etc. Each dosage form of the food composition can, in addition to the active ingredient, be easily and appropriately selected and blended by those skilled in the art with components commonly used in the relevant field according to the dosage form or the purpose of use, and when applied in combination with other raw materials, a synergistic effect may occur.

[0042] A food composition according to an embodiment may include various nutrients, vitamins, minerals (electrolytes), flavoring agents such as synthetic flavoring agents and natural flavoring agents, coloring agents, and enhancers (such as cheese and chocolate), pectic acid and its salts, alginic acid and its salts, organic acids, protective colloid thickeners, pH adjusters, stabilizers, preservatives, glycerin, alcohol, carbonating agents used in carbonated beverages, and the like. Further, a food composition according to an embodiment may include pulp for the production of natural fruit juices, fruit juice beverages, and vegetable beverages. Such components can be used independently or in combination. The ratio of such additives is not so important, but it is generally included in the range of 0 to about 50 parts by weight per 100 parts by weight of the composition according to an embodiment.

[0043] In one embodiment, the composition may be a pharmaceutical composition. The pharmaceutical composition can be administered orally, parenterally, rectally, topically, transdermally, intravenously, intramuscularly, intraperitoneally, subcutaneously, and the like. Dosage forms for oral administration may be tablets, pills, soft and hard capsules, granules, powders, fine granules, solutions, emulsions, or pellets, but are not necessarily limited thereto. Dosage forms for parenteral administration may be solutions, suspensions, emulsions, gels, injections, drip infusions, suppositories, patches, or sprays, but are not necessarily limited thereto. The dosage forms can be easily manufactured according to ordinary methods in the art and may further include surfactants, excipients, hydrating agents, emulsification promoters, suspending agents, salts or buffers for osmotic pressure adjustment, coloring agents, flavoring agents, stabilizers, preservatives, storage agents, or other commonly used adjuvants.

[0044] In another aspect, the present invention provides a method for relieving skin itching or skin irritation, including the step of administering to an individual in need of relieving skin itching or skin irritation a composition containing an effective amount of thymol trimethoxycinnamate or a stereoisomer, salt, hydrate, or solvate thereof. In one aspect, the administration of the above method may be performed according to the administration methods and dosages described herein.

[0045] On the other hand, the present invention provides the use of thymol trimethoxycinnamate or its stereoisomers, salts, hydrates or solvates for producing a composition for relieving skin itching or skin irritation.

[0046] In still another aspect, the present invention provides the use of thymol trimethoxycinnamate or its stereoisomers, salts, hydrates or solvates for relieving skin itching or skin irritation.

[0047] Hereinafter, the present invention will be described in more detail through examples and the like. It will be apparent to those of ordinary skill in the art that these examples are merely for illustrative purposes of the present invention and should not be construed as limiting the scope of the present invention by these examples.

[0048] [Example 1] Thymol Trimethoxycinnamate Thymol trimethoxycinnamate with CAS number 504394-57-4 was obtained from COSMANN Co., Ltd. (located in Hwaseong City, Gyeonggi-do).

[0049] [Experimental Example 1] Evaluation of the inhibitory effect on voltage-gated sodium channel Nav1.7 To evaluate the inhibitory effect of thymol trimethoxycinnamate on the voltage-gated sodium channel Nav1.7 as follows, the Human Nav1.7-HEK293 cell line (Millipore) was used. The Human Nav1.7-HEK293 cell line is a cell line obtained by transforming HEK293 (human embryonic kidney 293) cells with the human Nav1.7 gene and stabilizing it. One day before the experiment, Human Nav1.7-HEK293 cells were seeded at 8×10 in a 96-well plate. 4After dispensing the cells at a rate of cells per well, they were cultured in a 37°C, 5% CO2 incubator for 24 hours. The medium used during the culture was DMEM / F12 medium containing 10% fetal bovine serum (FBS), and Geneticin (Gibco®; Thermo Fisher Scientific) was added to maintain the stabilized cells.

[0050] After 24 hours, the 96-well plate was washed once with 20 mM HEPES Hanks’ Balanced Salt solution (HBSS) buffer (hereinafter referred to as reaction buffer; Invitrogen®; Thermo Fisher Scientific), and then the FLIPR® membrane potential fluorescence dye (Molecular Devices) was added to the Human Nav1.7-HEK293 cells. After reacting for 40 minutes in a 37°C, 5% CO2 incubator, the thymol trimethoxysinnamate of Example 1 was treated with the Human Nav1.7-HEK293 cells. After reacting for 10 minutes, the change in membrane potential that occurs when treating with 30 μM veratridine, which is a stimulus source, was measured for 55 seconds per well volume using a FlexStation3 (Molecular Device, USA), which is a fluorescence plate reader.

[0051] For Example 1, the difference between the initial value and the maximum value of the values obtained by measuring the change in fluorescence for 55 seconds after treatment with only the reaction buffer and after treatment with veratridine was determined respectively. The suppression rate was determined by comparing the difference in values when treating with only the reaction buffer during veratridine treatment with the value when treating with only the reaction buffer during the treatment of Example 1. By the same method, after determining the suppression rate of lidocaine (Sigma), which is a local anesthetic and is used as an antipruritic agent, the results are shown in Table 1 and FIG. 1 below in comparison with Example 1.

[0052]

Table 1

[0053] As a result, it was confirmed that thymol trimethoxycinnamate of Example 1 suppressed the voltage-dependent sodium channel Nav1.7 in a concentration-dependent manner and alleviated skin itching and skin irritation. In addition, it was confirmed that Example 1 was superior to lidocaine at the same concentration in the inhibitory effect on the voltage-dependent sodium channel Nav1.7.

[0054] [Experimental Example 2] Patch Clamp Evaluation (Nav1.7 Human Sodium Ion Channel Cell Based Automated Patch Clamp Assay) Patch clamp evaluation was performed using Nav1.7 Human Sodium Ion Channel Cell Based Automated Patch Clamp Assay (Eurofins, CYL8011QP2). The current amplitude exceeding 200 pA was analyzed at the control stage. The amplitude of the current was calculated by measuring the difference between the peak inward current and the current remaining at the end of the step when stepping the stage at -10 mV (i.e., the peak of the current). The current was evaluated after the vehicle control condition and then after application of each compound for 5 minutes each.

[0055] Sodium channels exist in a) a resting or closed state at -120 mV and b) a non-inactivated state that is transiently opened at 0 mV. Suppression of open channels (pulse 1) was measured through sodium current measurement within 1 - 2 ms at 0 mV. To fully inactivate the sodium channels and promote drug binding in the inactivated state-dependent manner, the channels were maintained in the open state (0 mV) for a longer time and then stepped back to -120 mV for 10 ms to recover to the resting or closed state in the inactivated state. Then, to measure the sodium channels that could be opened, the suppression of the inactivated state (pulse 2) was evaluated by stepping to 0 mV for 50 ms. Each concentration of the compound was applied for 5 minutes, and the results are shown in Table 2 below.

[0056]

Table 2

[0057] As can be confirmed from the results in Table 2 above, Example 1 showed a suppressive effect in both Pulse 1 and Pulse 2 depending on the concentration.

[0058] [Experimental Example 3] Evaluation of Clinical Efficacy on Itch Relief The itch-relieving efficacy was evaluated for subjects who chronically felt itchy due to ordinary skin dryness, atopic dermatitis, sensitive skin, etc. When itching occurred for 30 minutes or more, a lotion containing Example 1 at a concentration of 0.5% was applied, and the itch level before and after application was evaluated using a Numerical Rating Scale that evaluates the itch level in scores. When the itch situation occurred for each subject on a scale from 0 (no itch) to 10 (the worst imaginable itch), it was evaluated as time passed at 2 minutes, 10 minutes, and 30 minutes, and the results are shown in Figure 2 (** p<0.01, *** p<0.001). The composition of the lotion containing Example 1 above is as shown in Table 3 below.

[0059]

Table 3

[0060] As shown in Figure 2, when comparing the same time before and after application of the lotion containing Example 1 in pairs, it was found that itching was significantly suppressed at all times.

[0061] [Dosage Form Example 1] Lotion According to the composition described in Table 4 below, a lotion was produced by a normal method.

[0062]

Table 4

[0063] [Dosage form example 2] Cream A cream was manufactured in a conventional method according to the composition described in Table 5 below.

[0064]

Table 5

[0065] [Dosage form example 3] Lotion A lotion was manufactured in a conventional method according to the composition described in Table 6 below.

[0066]

Table 6

[0067] [Dosage form example 4] Massage cream A massage cream was manufactured in a conventional method according to the composition described in Table 7 below.

[0068]

Table 7

[0069] [Dosage form example 5] Pack A pack was manufactured in a conventional method according to the composition described in Table 8 below.

[0070]

Table 8

[0071] [Dosage form example 6] Gel A gel was manufactured in a conventional method according to the composition described in Table 9 below.

[0072]

Table 9

[0073] [Dosage form example 7] Ointment An ointment was produced in a conventional manner according to the composition described in Table 10 below.

[0074]

Table 10

[0075] [Dosage form example 8] Hair lotion A hair lotion was produced in a conventional manner according to the composition described in Table 11 below.

[0076]

Table 11

[0077] [Dosage form example 9] Soft capsule 100 mg of thymol trimethoxycinnamate, 160 mg of L-carnitine, 320 mg of soybean oil, 2 mg of palm oil, 8 mg of vegetable hardened oil, 4 mg of yellow wax, and 6 mg of lecithin were mixed and filled into one capsule according to a conventional method to produce a soft capsule.

[0078] [Dosage form example 10] Purification 120 mg of thymol trimethoxycinnamate, 500 mg of galactooligosaccharide, 80 mg of lactose, and 220 mg of maltose were mixed, granulated using a fluidized bed dryer, then 6 mg of sugar ester was added and tableted using a tableting machine to produce tablets.

[0079] [Dosage form example 11] Granules 100 mg of thymol trimethoxycinnamate, 250 mg of anhydrous crystalline glucose, and 550 mg of starch were mixed and formed into granules using a fluidized bed granulator, then filled into packages to produce granules.

[0080] [Dosage form example 12] Drink After mixing 120 mg of thymol trimethoxycinnamate, 10 g of glucose, 0.6 g of citric acid, and 25 g of liquid oligosaccharide, 500 ml of purified water is added and each bottle is filled with 200 ml. After filling the bottles, they are sterilized at 130 °C for 4 to 5 seconds to produce a drink.

[0081] This specification is further illustrated by the following embodiments which do not limit the scope of the claims.

[0082] Embodiment 1. A composition for relieving skin itching or irritation, containing thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates as an active ingredient.

[0083] Embodiment 2. The composition of Embodiment 1, wherein the thymol trimethoxycinnamate is represented by the following Chemical Formula 1.

[0084] [Chemical Formula]

[0085] Embodiment 3. The composition of Embodiment 1 or Embodiment 2, wherein the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates are administered at a dosage of 0.37 to 37 mg / kg / day.

[0086] Embodiment 4. Any composition of Embodiments 1 to 3, wherein the content of the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates is 0.001 to 20% by weight based on the total weight of the composition.

[0087] Embodiment 5. Any composition of Embodiments 1 to 4, wherein the composition inhibits the voltage-gated sodium channel Nav1.7.

[0088] Embodiment 6. A composition which is any of the compositions of Embodiments 1 to 5, wherein the itching or irritation of the skin is caused by a chemical substance.

[0089] Embodiment 7. A composition which is any of the compositions of Embodiments 1 to 6, wherein the composition is a topical skin composition.

[0090] Embodiment 8. A composition which is any of the compositions of Embodiments 1 to 7, wherein the composition is a food composition.

[0091] Embodiment 9. A composition which is any of the compositions of Embodiments 1 to 8, wherein the composition is a cosmetic composition.

[0092] Embodiment 10. A composition which is any of the compositions of Embodiments 1 to 9, wherein the composition is a pharmaceutical composition.

Claims

1. A composition for relieving skin itching or irritation, comprising thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates as an active ingredient.

2. The composition according to claim 1, wherein the thymol trimethoxycinnamate is represented by the following chemical formula 1. 【Chemical Formula 1】

3. The composition according to claim 1 or 2, wherein the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates are administered at a dosage of 0.37 to 37 mg / kg / day.

4. The composition according to any one of claims 1 to 3, wherein the content of the thymol trimethoxycinnamate, its stereoisomers, salts, hydrates or solvates is 0.001 to 20% by weight based on the total weight of the composition.

5. The composition according to any one of claims 1 to 4, wherein the relief of skin itching or irritation is achieved by suppressing the voltage-gated sodium channel Nav1.

7.

6. The composition according to any one of claims 1 to 5, wherein the skin itching or irritation is caused by a chemical substance.

7. The composition according to any one of claims 1 to 6, wherein the composition is a topical skin composition.

8. The composition according to any one of claims 1 to 6, wherein the composition is a food composition.

9. The composition according to any one of claims 1 to 6, wherein the composition is a cosmetic composition.

10. The composition according to any one of claims 1 to 6, wherein the composition is a pharmaceutical composition.

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