JP6959594B2 - Anti-inflammatory topical agent - Google Patents

Description

The present invention relates to an anti-inflammatory external preparation, and more specifically, by containing an oily extract fraction or an aqueous extract fraction as an active ingredient, it is possible to motivate exercise and to apply it before exercise. It relates to an anti-inflammatory external preparation that can suppress local inflammation caused by exercise.

It has been a long time since lifestyle-related diseases such as hypertension, diabetes, dyslipidemia, and locomotive syndrome have become problems. We all acknowledge that continuous exercise is necessary to prevent these lifestyle-related diseases. On the other hand, everyone also realizes that continuous exercise is difficult.

There are multiple techniques that motivate the exercise itself for the purpose of achieving continuous exercise. For example, Patent Document 4 is an exercise motivation system that enables continuous walking by delivering music that matches the user's preference and exercise amount target, and Patent Document 5 is for detecting and storing a plurality of user's exercise actions. In addition to outputting voice at the timing that matches each movement, we also provide a movement promotion robot that is designed to move in response to each movement.

These are technologies based on the hypothesis that users can always exercise in response to motivation. However, in reality, exercise has caused new factors that inhibit continuous exercise, and a particularly serious factor is local inflammation. Local inflammation causes pain such as muscle pain and inhibits continuous exercise as mental stress as well as physical stress. Therefore, in order to enable continuous exercise, local inflammatory care is required not only to motivate the above-mentioned exercise but also to maintain the optimum physical condition.

Although local inflammatory care can be performed during exercise as well as before and after exercise, it is generally performed after exercise, and non-steroidal anti-inflammatory external preparations are widely used. Non-steroidal anti-inflammatory topical agents, which are pharmaceutical products, are generally used after recognition of local inflammation, and inevitably cannot suppress pain caused by exercise, and physical and mental stress load due to pain. Due to this, continuous exercise is a difficult situation.

In recent years, anti-inflammatory external preparations derived from natural products different from the above non-steroidal anti-inflammatory external preparations have been widely used. For example, Patent Document 3 describes a skin external preparation containing a mixed essential oil consisting of peppermint leaf oil, lemon oil, Italian itosugi oil, labandura hybrida oil, and kisstus ladifer oil. Provided is an anti-inflammatory agent containing a Camellia plant extract, and Patent Document 5 provides a skin external preparation comprising an extract of a Pinaceae plant of the genus Camellia. There is. However, none of them has been able to suppress the local inflammation caused by exercise. Therefore, an anti-inflammatory external preparation capable of suppressing local inflammation caused by exercise by applying it before exercise has been desired.

From the above, an anti-inflammatory external preparation that can motivate exercise to realize continuous exercise and can suppress local inflammation caused by exercise by applying it before exercise. Development was desired.

Japanese Unexamined Patent Publication No. 2003-305146 Japanese Unexamined Patent Publication No. 2013-090758 Japanese Unexamined Patent Publication No. 2005-0752827 Japanese Unexamined Patent Publication No. 2014-0804009 Japanese Unexamined Patent Publication No. 2013-010698

The present invention has been made in view of the above circumstances, and an object of the present invention is to provide motivation for exercise and to suppress local inflammation caused by exercise in order to realize continuous exercise. Is to provide an anti-inflammatory topical agent capable of producing.

As a result of diligent research to solve the above-mentioned problems, the present inventors have found that the external preparation contains an oily extract fraction or an aqueous extract fraction extracted from the branches and / or leaves of the genus Fir of the Pinaceae family as an active ingredient. As a result, it was found that an anti-inflammatory external preparation having a high anti-inflammatory effect and an additional effect of motivating exercise can be obtained, and based on this finding, the present invention has been completed.
That is, the present invention is as shown in the following (1) to (7).
(1) An anti-inflammatory external preparation containing an oily extract fraction or an aqueous extract fraction extracted from branches and / or leaves of a plant belonging to the genus Fir of the Pinaceae family as an active ingredient exhibiting an anti-inflammatory effect.
(2) The anti-inflammatory external preparation according to (1) above, wherein the plant belonging to the genus Fir of the Pinaceae family is Abies sachalinensis.
(3) The anti-inflammatory external preparation according to (1) or (2) above, wherein the content of the oily extract fraction is 0.1 to 10% by mass in the base material.
(4) The anti-inflammatory external preparation according to (1) or (2) above, wherein the content of the aqueous extract fraction is 25 to 99.9% by mass in the base material.
(5) The anti-inflammatory external preparation according to any one of (1) to (4) above, which has a gel-like or stick-like shape.
(6) The anti-inflammatory external preparation according to any one of (1) to (5) above, which adds motivation to exercise.

As described above, the present invention has a high anti-inflammatory effect and anti-exercise by adding an oily extract fraction or an aqueous extract fraction extracted from the branches and / or leaves of the Pinaceae family Fir as an active ingredient to an external preparation. It is possible to provide an anti-inflammatory external preparation that exerts a motivational additional effect.

An example of the configuration of a microwave distillation apparatus used to obtain a distillate of a plant belonging to the genus Fir of the Pinaceae family used as an active ingredient of the anti-inflammatory external preparation of the present invention is schematically shown.

Hereinafter, the anti-inflammatory external preparation of the present invention will be described in detail. The examples described in the present specification do not particularly limit the present invention.

The "anti-inflammatory effect" of the present invention means the "edema suppression rate" calculated from the "edema rate" of each test external preparation application group, and those having an edema suppression rate of 15% or more have an anti-inflammatory effect. I decided. "Edema rate" means edema volume when 100 g of weight for precision balance is dropped from a height of 1 m on the right hind limb instep of a rat to cause edema and the limb volume is measured. It means the ratio of the difference between the volume of the evoked hind limb and the volume of the edema-induced forefoot. The "edema suppression rate" is a test for the edema rate of the control external preparation application group that does not contain the oily extract fraction or the aqueous extract fraction extracted from the branches and / or leaves of the plants of the genus Pinaceae. It means the ratio of the difference between the edema rate of the control external preparation group and the edema rate of the test external preparation group, which is reduced by the application of the external preparation.

The "motivational addition effect" on exercise of the present invention means the "motivational addition rate" of each external preparation application group, and the motivational addition rate is 60% (3 out of 5 persons) or more. It was judged that there was an additional motivational effect. The "motivational addition rate" means the rate at which the subject wants to exercise due to the olfactory stimulation of the oily extract fraction or the aqueous extract fraction extracted from the branches and / or leaves of the plants of the genus Fir of the Pinaceae family.

The active ingredient used in the anti-inflammatory external preparation of the present invention is an oily extract fraction or an aqueous extract fraction extracted from the branches and / or leaves of plants of the genus Fir of the Pinaceae family.
Examples of plants belonging to the genus Fir of the Pinaceae family include Abies sachalinensis, Fir, Abies homolepis, Abies veitchii, Abies veitchii, Abies veitchii, Balsam fur, Fir fir, White fur, Amabilis fur, Abies sachalinensis, California red fur, Grand fir and Noble fur. Preferred is Abies sachalinensis.

As a method for obtaining an oil-based extract fraction or an aqueous-extracted fraction from the branches and / or leaves of a tree belonging to the genus Fir of the Pinaceae family, a conventional method such as solvent extraction and distillation can be used. The extraction solvent is preferably a polar solvent, for example, an alcohol solvent such as water, ethanol, methanol, butyl alcohol, ethylene glycol, propylene glycol and glycerin; a halogen-containing solvent such as chloroform; an ether solvent such as dioxane; acetone. And carbonyl solvents such as ethyl acetate, and mixed solutions thereof. The distilled product can be obtained by atmospheric distillation, vacuum distillation, steam distillation and the like.

Of these, distilled products are preferable, and those obtained by heating under reduced pressure and performing distillation are particularly preferable. Further, the heating may be performed by a heater, but heating by a microwave is preferable, and it is particularly preferable to irradiate the microwave without adding water. By irradiating with microwaves, water molecules contained in the plant are directly heated to generate steam, which acts as a mobile phase to distill volatile components in the plant. Therefore, this distillation method is volatile. It is considered to include a vacuum distillation element depending on the boiling point of the component and a steam distillation element.

Such a distillate can be obtained, for example, by using the apparatus shown in FIG.
In this apparatus 1, microwaves provided on the upper surface of the distillation tank 2 are provided in the distillation tank 2 by putting the branches and / or leaves of the genus Fir of the Pinaceae family, which is the raw material to be the distillation object 12, into the distillation tank 2 and stirring with a stirring splash 4. The raw material is heated by radiating microwaves from the heating device 3. The distillation tank 2 communicates with the airflow inlet 5 and the distillation outflow pipe 6. The airflow inflow pipe 5 introduces an inert gas such as air or nitrogen gas into the reaction vessel 2, and this airflow is introduced from the lower part of the reaction vessel 2. Further, the distillate outflow pipe 6 leads out the distillate from the raw material from the upper part of the reaction tank 2 to the outside.
The temperature and pressure inside the reaction vessel 2 can be measured by a temperature sensor and a pressure sensor (both not shown) attached to the reaction vessel 2, and can be adjusted via the heating control device 8, the pressure control device 11, and the pressure adjusting valve 10, respectively. ..
Further, the gaseous distillate flowing out from the distillation tank 2 through the distillate outflow pipe 6 is replaced with a liquid by the cooling device 7 to obtain the distillate 13. The distillate 13 contains an oil-based fraction 13a and an aqueous fraction 13b, of which the aqueous fraction 13b is preferably used.

In the distillation, the pressure in the distillation tank 2 may be 10 to 95 kPa, preferably 15 to 60 kPa, more preferably about 20 to 40 kPa, and the steam temperature at that time is 40 ° C to 100 ° C. When the pressure is 10 kPa or less, the increase in vapor pressure of the volatile component in the plant is suppressed, and the vacuum distillation element due to the boiling point of each component is the main component rather than the steam distillation element, and the one with the lowest boiling point flows out in order. Therefore, it is not preferable in that the components having a boiling point higher than that of water cannot be efficiently extracted. Further, if it is 95 kPa or more, the temperature of the raw material becomes high, so that the energy loss is large and the oxidation of the raw material is promoted, which is not preferable. The distillation time may be about 0.2 to 8 hours, preferably about 0.4 to 6 hours. If it is 0.2 hours or less, a large amount of unextracted components in the plant will remain, and if it is 8 hours or more, the raw material will be in a state close to dryness, which is not preferable in that the extraction efficiency is lowered.

The oily extract fraction or the aqueous extract fraction obtained by such a method is preferable because it contains a high concentration of monoterpenes and can give a refreshing aroma component.
Further, the gas to be introduced into the distillation tank 2 may be air, but an inert gas such as nitrogen gas, helium gas and argon gas is preferable, and the flow rate thereof is the flow rate per minute in the distillation tank 2. It may be about 0.001 to 0.1 times the capacity of.

The content of the oily extract fraction used in the anti-inflammatory external preparation of the present invention is preferably in the range of 0.1 to 20% by mass, more preferably 1.0 to 10% by mass, based on the total content of the external preparation. Is. If the content of the oily extract fraction is less than 0.1% by mass, the motivational addition effect and the anti-inflammatory effect on exercise cannot be obtained, which is not preferable. Further, if the content of the oily extract fraction is more than 20% by mass, skin irritation and skin sensitization may occur, which is not preferable.

The content of the aqueous extract fraction used in the anti-inflammatory external preparation of the present invention is preferably in the range of 25 to 99.9% by mass, more preferably 30 to 98% by mass, based on the total content of the external preparation. .. If the content of the oily extract fraction is less than 25% by mass, the motivational addition effect and the anti-inflammatory effect on exercise cannot be obtained, which is not preferable. Further, if the content of the aqueous extract fraction is more than 99.9% by mass, it is difficult to form an external preparation, which is not preferable.

Examples of the dosage form of the anti-inflammatory external preparation of the present invention include an ointment, a gel, a stick, a cream, a tape, a pap, and a lotion. It is preferably gel-like in that it is not sticky, but when it is rubbed on the skin using a container, it is preferably stick-like in which the container and the external preparation are integrated and can withstand the rubbing.

When the anti-inflammatory external preparation of the present invention is in the form of a gel, an oil-based extract fraction or an aqueous extract fraction, a gelling agent and water are essential components.

Examples of the gelling agent used for the gel-like anti-inflammatory external preparation include xanthan gum, carboxyvinyl polymer, pectin, polyethylene, bead wax, barafin and sodium polyacrylate, and may be used alone or in combination of two or more. Can be done. The content of the gelling agent is preferably in the range of 0.01 to 10% by mass, more preferably 0.1 to 5% by mass, based on the total content of the external preparation. If the content of the gelling agent is less than 0.01% by mass, a sufficient viscosity cannot be obtained as a gel composition, which is not preferable. Further, when the content of the gelling agent is more than 10% by mass, the viscosity of the gel composition is too high and stickiness is conspicuous, which is not preferable.

Examples of the water used for the anti-inflammatory external preparation having a gel-like shape in the present invention include purified water, sterilized purified water, and water for injection, and can be used alone or in combination of two or more.

In addition to the above-mentioned essential components, the anti-inflammatory external preparation having a gel-like shape of the present invention contains various components generally used for gel base materials such as cosmetics and pharmaceuticals, that is, oils and fats, as long as the effects of the present invention are not impaired. , Rows, ester oils, hydrocarbon oils, silicones, surfactants, lower alcohols, moisturizers, water-soluble polymers, UV absorbers, metal ion blockers, pH adjusters, antioxidants, antibacterial agents, etc. Anti-inflammatory agents, fragrances and the like can be appropriately blended.

Examples of fats and oils include flaxseed oil, camellia oil, macadamia nut oil, corn oil, mink oil, palm oil, palm oil, palm kernel oil, cacao fat, beef fat, sheep fat, pork fat, horse fat, hardened oil and hardened castor bean paste. Examples include oil, which can be used alone or in combination of two or more.

Examples of waxes include beeswax, candelilla wax, cotton wax, carnauba wax, baby wax, ibotarou, whale wax, montan wax, nukarou, lanolin, reduced lanolin, hard lanolin, capoc wax, sugar cane wax and hohobarou. Two or more types can be used in combination.

Examples of the ester oil include octanoic acid ester, tri-2-ethylhexaenoic acid glycerin, isooctanoic acid ester, lauric acid ester, isopropyl myristate, myristic acid ester, palmitate, stearic acid ester, isostearic acid ester, and iso. Examples thereof include palmitic acid ester, oleic acid ester and sebacic acid diester, and they can be used alone or in combination of two or more.

Examples of the hydrocarbon oil include liquid paraffin, ozokerite, squalene, squalene, pristane, paraffin, isoparaffin, selecin, petrolatum and microcrystalline wax, and can be used alone or in combination of two or more.

Examples of the silicone include chain silicones such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, dodecamethylcyclohexasiloxane, and the like, either alone or. Two or more types can be used in combination.

Examples of the surfactant include sodium laurate, benzalkonium chloride, 2-undecyl-N, N, N- (hydroxyethylcarboxymethyl) -2-imidazoline sodium, sorbitan monooleate and the like, and may be used alone or. Two or more types can be used in combination.

Examples of the lower alcohol include methanol, ethanol, propanol, isopropanol and butanol, and can be used alone or in combination of two or more.

Examples of the moisturizer include sorbitol, polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, glycerin and diglycerin, and can be used alone or in combination of two or more.

Examples of the water-soluble polymer include arabic rubber, tragacanth gum, galactan, carob gum, guar gum, xanthan gum, kalaya gum, carrageenan, pectin, canten, collagen, casein, albumin, gelatin, methyl cellulose, nitrocellulose, ethyl cellulose, methyl hydroxypropyl cellulose, and the like. Cellulose Sodium sulfate, hydroxypropyl cellulose, sodium carboxymethyl cellulose, crystalline cellulose, sodium alginate, propylene glycol alginate, polyvinyl alcohol, polyvinyl methyl ether, polyvinylpyrrolidone, polyethyl acrylate, polyacrylamide, bentonite, aluminum magnesium silicate and the like. , Can be used alone or in combination of two or more.

Examples of the ultraviolet absorber include benzoic acid-based ultraviolet absorbers such as paraaminobenzoic acid, methyl anthranylate, octyl salicylate, phenyl salicylate, homomethyl salicylate, isopropyl paramethoxycinnamate, octyl paramethoxycinnamate, and paramethoxycinnamate. Examples thereof include 2-ethylhexyl sicate, mono-2-ethylhexanate diparamethoxycinnamate, glyceryl 2,4-dihydroxybenzophenone and 2-hydroxy-4-methoxybenzophenone, which may be used alone or in combination of two or more. Can be done.

Examples of the metal ion sequestering agent include sodium edetate, sodium polyphosphate, sodium metaphosphate and phosphoric acid, and can be used alone or in combination of two or more.

Examples of the pH adjuster include lactic acid, citric acid, glycolic acid, succinic acid, tartaric acid, dl-malic acid, potassium carbonate, sodium hydrogencarbonate and ammonium hydrogencarbonate, and may be used alone or in combination of two or more. Can be done.

Examples of the antioxidant include ascorbic acid, α-tocopherol, dibutylhydroxytoluene and butylhydroxyanisole, which can be used alone or in combination of two or more.

Examples of the antibacterial agent include benzoic acid, salicylic acid, phenolic acid, sorbic acid, paraoxybenzoic acid ester, parachlormethacresol, hexachlorophene, benzalkonium chloride, chlorhexidine chloride, trichlorocarbanilide, phenoxyethanol and the like, and alone. Alternatively, two or more types can be used in combination.

Other anti-inflammatory agents include, for example, menthol, camphor, zinc oxide, mephenamic acid and its derivatives, phenylbutazone and its derivatives, indomethacin and its derivatives, ibuprofen and its derivatives, ketoprofen and its derivatives, diclofenac sodium, diphenhydramine, tranexam. Acids and their derivatives, dexamethasone, cortisone and its esters, hydrocortisone and its esters, corticosteroids such as prednisone, prednisolone, anti-histamines, ages, sardines, citrus fruits, senkyo, senburi, sardines, biwa, lavender, rosemary and other plants or Examples include plant-derived components, which can be used alone or in combination of two or more.

Examples of the fragrance include hydrocarbon fragrances such as pinen and limonene, alcohol fragrances such as linalol, geraniol, citronellol, menthol, borneol, benzyl alcohol, anis alcohol and β-phenethyl alcohol, and phenolic fragrances such as anetol and eugenol. , N-butylaldehyde, isobutylaldehyde, hexylaldehyde, citral, citroneral, benzaldehyde, synamic aldehyde and other aldehyde-based fragrances, carboxylic, menton, cypress, acetphenone, ionone and other ketone-based fragrances, γ-butyllactone, coumarin, cineole Examples thereof include lactone-based fragrances such as octyl acetate, benzyl acetate, cinnamyl acetate, butyl propionate, and ester-based fragrances such as methyl benzoate, which can be used alone or in combination of two or more.

When the anti-inflammatory external preparation of the present invention has a stick-like shape, an oily extract fraction or an aqueous extract fraction, an alkali metal salt of a higher fatty acid, water, a monohydric alcohol and a polyhydric alcohol are essential components.

Examples of alkali metal salts of higher fatty acids used in stick-like anti-inflammatory external preparations include sodium stearate, sodium palmitate, sodium myristate, sodium behenate, potassium stearate, potassium palmitate, potassium myristate and behenic acid. Examples thereof include potassium, which can be used alone or in combination of two or more. The content of the alkali metal salt of the higher fatty acid used in the anti-inflammatory external preparation having a stick-like shape of the present invention is preferably in the range of 3 to 15% by mass, more preferably 5 of the total content of the external preparation. It is 10% by mass. If the content of the alkali metal salt of the higher fatty acid is less than 3% by mass, it becomes gel-like and the shape of the stick cannot be maintained, which is not preferable. Further, if the content of the alkali metal salt of the higher fatty acid is more than 15% by mass, it becomes brittle and cannot withstand rubbing, which is not preferable.

Examples of the water used for the anti-inflammatory external preparation having a stick-like shape in the present invention include purified water, sterilized purified water, and water for injection, and can be used alone or in combination of two or more.

Examples of the monohydric alcohol used for the anti-inflammatory external preparation having a stick-like shape in the present invention include methanol, ethanol, isopropanol, propanol and butanol, and can be used alone or in combination of two or more. The content of the monohydric alcohol used in the anti-inflammatory external preparation having a stick-like shape of the present invention is preferably in the range of 10 to 50% by mass, more preferably 15 to 30% by mass of the total content of the external preparation. %. If the content of the monohydric alcohol is less than 10% by mass, the alkali metal salt of the higher fatty acid is not sufficiently dissolved, which is not preferable. Further, when the content of the monohydric alcohol is more than 50% by mass, the odor peculiar to the monohydric alcohol becomes strong and hinders the motivational addition effect on the exercise based on the olfactory stimulus, which is not preferable.

Examples of the polyhydric alcohol used for the anti-inflammatory external preparation having a stick-like shape in the present invention include glycerin, ethylene glycol, propylene glycol, 1,3-butanediol, polyethylene glycols, diethylene glycol and sorbitol. , Can be used alone or in combination of two or more. The content of the polyhydric alcohol used in the anti-inflammatory external preparation having a stick-like shape of the present invention is preferably in the range of 15 to 50% by mass, more preferably 20 to 40% by mass of the total content of the external preparation. %. If the content of the polyhydric alcohol is less than 15% by mass, the alkali metal salt of the higher fatty acid is not sufficiently dissolved, which is not preferable. Further, if the content of the polyhydric alcohol is more than 50% by mass, the stickiness becomes strong, which is not preferable.

The anti-inflammatory external preparation having a stick-like shape of the present invention is a variety of components generally used for stick base materials such as cosmetics and pharmaceuticals, that is, fats and oils, waxes, ester oils and hydrocarbon oils generally used for the gel base material. , Silicone, surfactants, lower alcohols, moisturizers, water-soluble polymers, UV absorbers, metal ion blockers, pH regulators, antioxidants, antibacterial agents, other anti-inflammatory agents and fragrances, as well as lower carboxylic acids An alkali metal salt of an acid, an alkali metal salt of an inorganic acid, or the like can be appropriately blended.

Examples of the alkali metal salt of the lower carboxylic acid include sodium acetate, sodium propionate, sodium lactate, sodium malate and sodium tartrate, and can be used alone or in combination of two or more.

Examples of the alkali metal salt of the inorganic acid include sodium hydrogen carbonate, sodium carbonate, sodium chloride, sodium monohydrogen phosphate, sodium dihydrogen phosphate and sodium sulfate, and may be used alone or in combination of two or more. can.

In the production of the anti-inflammatory external preparation having the shape of the present invention in the form of a gel or a stick, a method conventionally known as an example described later, a method for producing a gel or a stick, or a method newly provided in the future. Can be used to produce an anti-inflammatory external preparation having a gel-like or stick-like shape, which is the object of the present invention.

The anti-inflammatory external preparation having a gel-like shape of the present invention can be produced, for example, by the following method.
It can be produced by adding a gelling agent and an oil-based extract fraction or an aqueous extract fraction to purified water and stirring the mixture with a stirrer or the like until it becomes uniform.

The anti-inflammatory external preparation having a stick-like shape of the present invention can be produced, for example, by the following method.
Alkali metal salts of higher fatty acids, purified water, monovalent alcohols, polyhydric alcohols, alkali metal salts of lower carboxylic acids or alkali metal salts of inorganic acids and branches of plants of the genus Fir and oily extract fractions in suitable containers. Can be produced by adding, stirring at 70 to 90 ° C. until uniform, and placing the obtained solution in a suitable stick container, cooling and hardening.

Hereinafter, the present invention will be described in more detail with reference to Examples, but the present invention is not limited to the Examples.
(Manufacturing Example 1)
Method for Producing Oily Extraction Fragment and Aqueous Extraction Fragment of Todomatsu Approximately 50 kg of Todomatsu leaf crushed by a crushing type crusher (manufactured by KYB Mfg. Co., Ltd.) was put into the distillation tank of the microwave distillation apparatus shown in FIG. 1 and stirred. While maintaining the pressure in the distillation tank under a reduced pressure condition of about 20 kPa (steam temperature is about 67 ° C.), the distillation was carried out by irradiating with microwaves for 1 hour. From the obtained distillate, about 180 g (about 180 mL) of an oil-based extract fraction and about 5 kg (about 5 L) of an aqueous extract fraction were collected.

(Example 1)
Based on the formulation shown in Table 1, it was prepared by the method of Preparation Method 1 described later to obtain an anti-inflammatory external preparation 1 having a gel-like shape of the present invention. When the obtained anti-inflammatory external preparation 1 having a gel-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 80%, and there was a motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 15.9%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Preparation method 1)
0.4 g of the carboxyvinyl polymer (1) was added to 19.4 g of purified water (2), and the mixture was stirred and swollen. 0.2 g of the oily extract fraction (3) was added thereto, and the mixture was further stirred until it became uniform to obtain an anti-inflammatory external preparation having a gel-like shape.

(Test Example 1)
Motivational additional confirmation test A series of movements in which 1 g of each topical agent is applied to the Achilles tendon and gastrocnemius muscle (calf) site over 2 minutes, and after application, walking is performed at a speed of 60 m to 70 m per minute for 30 minutes. Was carried out for 3 consecutive days. After two rest days were set from the last implementation day, the subjects were allowed to smell the same topical agent for 2 minutes, and the percentage of subjects who answered that they would like to walk again was defined as the motivational addition rate (%).

(Test Example 2)
Rat bruising edema suppression test The normal right hind limb volume of 5 rats (Wistar / ST, 5 weeks old, male, Nippon SLC Co., Ltd.) was measured with a foot volume measuring device (TK-101CMP, Muromachi Kikai Co., Ltd.). ..
Parafilm (Pechiney Plastic) in which 0.1 mL of each external preparation was added dropwise.
On Packing), the right hind limb of the rat was reciprocated 5 times on both the front and back sides, and each external preparation was applied to the right hind limb of the rat. After rubbing, the right hind limb of the rat was covered with a parafilm to which each external preparation was attached, and the rat was allowed to stand in the fixing holder. After standing for 3 hours, the parafilm was removed and each external preparation adhering to the surface of the right hind limb was wiped off. The control group was 5 rats obtained by repeating exactly the same operation except that no external preparation was added on the parafilm.
An 100 g weight for a precision balance was dropped from a height of 1 m onto the instep of the right hind limb of the rat to cause edema. Four hours after the induction of edema, the volume of the right hind limb of the rat was measured again, and the edema rate was calculated from Equation 1.

[Number 1]
Edema rate (%) = (limb volume after edema induction / limb volume before edema induction-1) × 100 ... Equation 1
In addition, the edema suppression rate was calculated from Equation 2.

[Number 2]
Edema suppression rate (%) = (1-Average edema rate of each topical agent / Average edema rate of control group) x 100 ...
・ ・ Equation 2

(Example 2)
In Example 1, the same preparation method as in Example 1 was repeated except that the oily extract fraction content was increased from 0.2 g to 0.6 g and the amount of purified water was reduced from 19.4 g to 19.0 g. Therefore, an anti-inflammatory external preparation 2 having a gel-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 2 having a gel-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Moreover, the edema suppression rate when the rat bruise edema suppression test was carried out according to Test Example 2 was 26.7%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Example 3)
In Example 1, the same preparation method as in Example 1 was repeated except that the oily extract fraction content was increased from 0.2 g to 2.0 g and the amount of purified water was reduced from 19.4 g to 17.6 g. Therefore, an anti-inflammatory external preparation 3 having a gel-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 3 having a gel-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Moreover, the edema suppression rate when the rat bruise edema suppression test was carried out according to Test Example 2 was 15.8%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Example 4)
In Example 1, the preparation was exactly the same as in Example 1 except that the oil-based extract fraction was changed to the aqueous extract fraction so that the content was 3.96 g, and the amount of purified water was reduced from 19.4 g to 15.64 g. By repeating the method, an anti-inflammatory external preparation 4 having a gel-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 4 having a gel-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 19.8%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Example 5)
In Example 4, the same preparation method as in Example 4 was repeated except that the amount of the aqueous extract fraction was increased from 3.96 g to 9.8 g and the amount of purified water was reduced by that amount from 15.64 g to 9.8 g. An anti-inflammatory external preparation 5 having a gel-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 5 having a gel-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Further, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 33.6%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Example 6)
In Example 4, the amount of the aqueous extract fraction was increased from 3.96 g to 19.6 g, and the same preparation method as in Example 4 was repeated except that purified water was removed by that amount, and the shape of the present invention was gel-like. A certain anti-inflammatory external preparation 6 was obtained. When the obtained anti-inflammatory external preparation 6 having a gel-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Further, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 18.1%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Comparative Example 1)
In Example 1, exactly the same preparation method as in Example 1 was repeated except that 0.2 g of the oil-based extract fraction was not blended and the amount of purified water was increased from 19.4 g to 19.6 g, and the shape was gel-like. External preparation 1 was obtained. When the obtained external preparation 1 having a gel-like shape was subjected to the motivational addition confirmation test according to Test Example 1, the motivational addition rate was 20%, and there was no motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 6.7%, and there was no anti-inflammatory effect. The results are shown in Table 2.

(Comparative Example 2)
In Example 1, the same preparation method as in Example 1 was repeated except that the oil-based extract fraction content was reduced from 0.2 g to 0.06 g and the amount of purified water was increased from 19.4 g to 19.54 g. Then, an external preparation 2 having a gel-like shape was obtained. When the obtained external preparation 2 having a gel-like shape was subjected to the motivational addition confirmation test according to Test Example 1, the motivational addition rate was 20%, and there was no motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 14.9%, and there was no anti-inflammatory effect. The results are shown in Table 2.

(Example 7)
Based on the formulation shown in Table 3, it was prepared by the method of Preparation Method 2 described later to obtain an anti-inflammatory external preparation 7 having a stick-like shape of the present invention. When the obtained anti-inflammatory external preparation 7 having a stick-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 80%, and there was a motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 19.2%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Preparation method 2)
Five components from sodium stearate (1) to purified water (5) were mixed and heated to reflux for 30 minutes with stirring at 70 to 90 ° C. Further, 0.3 g of the oily extract fraction (6) was added and stirred, and the obtained uniform solution was placed in a stick container and hardened at room temperature to obtain an anti-inflammatory external preparation having a stick-like shape.

(Example 8)
In Example 7, the same preparation method as in Example 7 was repeated except that the oily extract fraction content was increased from 0.3 g to 1.0 g and the amount of purified water was reduced from 42.0 g to 41.3 g accordingly. Therefore, an anti-inflammatory external preparation 8 having a stick-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 8 having a stick-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 19.5%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Example 9)
In Example 7, the same preparation method as in Example 7 was repeated except that the oily extract fraction content was increased from 0.3 g to 3.0 g and the amount of purified water was reduced from 42.0 g to 39.3 g. Therefore, an anti-inflammatory external preparation 9 having a stick-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 9 having a stick-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 24.5%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Example 10)
In Example 7, the same preparation method as in Example 7 was repeated except that the oily extract fraction content was increased from 0.3 g to 10.0 g and the amount of purified water was reduced from 42.0 g to 32.3 g accordingly. Therefore, an anti-inflammatory external preparation 10 having a stick-like shape of the present invention was obtained. When the obtained anti-inflammatory external preparation 10 having a stick-like shape was subjected to a motivational addition confirmation test according to Test Example 1, the motivational addition rate was 100%, and there was a motivational addition effect on exercise. Further, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 32.5%, and there was an anti-inflammatory effect. The results are shown in Table 2.

(Comparative Example 3)
In Example 7, exactly the same preparation method as in Example 7 was repeated except that 0.3 g of the oil-based extract fraction was not blended and the amount of purified water was increased from 42.0 g to 42.3 g by that amount, and the shape of the present invention was formed. Obtained an external preparation 3 having a sticky shape. When the obtained external preparation 3 having a stick-like shape was subjected to the motivational addition confirmation test according to Test Example 1, the motivational addition rate was 0%, and there was no motivational addition effect on exercise. Moreover, when the rat bruise edema suppression test was carried out according to Test Example 2, the edema suppression rate was 10.3%, and there was no anti-inflammatory effect. The results are shown in Table 2.

The present invention relates to an anti-inflammatory external preparation that can add motivation to exercise and prevent inflammation that may be caused by exercise in order to contribute to continuous exercise throughout the life, and is industrially related to the present invention. It is fully usable.

1 ……… Microwave distillation device 2 ……… Distiller 3 ……… Microwave heating device 4 ……… Stirring splash 5 ……… Airflow inflow pipe 6 ……… Distillate outflow pipe 7 ……… Cooling device 8 ……… Heating control device 9 ……… Pressure reducing pump 10 ……… Pressure control valve 11 ……… Pressure control device 12 ……… Distillation target 13 ……… Distillate 13a ……… Oil-based extraction fraction 13b ……… Aqueous extraction fraction

Claims (4)

As an active ingredient exerting an anti-inflammatory effect, it is characterized by containing an aqueous extract fraction of a distillate obtained by heating and distilling from branches and / or leaves of Abies sachalinensis belonging to the genus Fir of the Pinaceae family under reduced pressure. Anti-inflammatory external preparation. The anti-inflammatory external preparation according to claim 1, wherein the content of the aqueous extract fraction is 25 to 99.9% by mass in the base material. The anti-inflammatory external preparation according to claim 1 or 2 , which is gel-like or stick-like in shape. The anti-inflammatory external preparation according to any one of claims 1 to 3, which adds motivation to exercise.

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