JP7326085B2 - muscle hardness reducer - Google Patents

Description

The present invention relates to a muscle stiffness reducing agent.

It has been reported that muscle hardness (muscle hardness) increases after a certain period of time has passed after unaccustomed or excessive exercise. Continuing to exercise in a state where muscle hardness has increased (so-called muscle stiffness) increases the risk of inducing injury, and also causes the form required for proper performance to be compromised. end up

In recent years, along with office automation, people tend to sit in a chair for a long time in the same posture, or tend to slouch forward. . Lumbar pain and stiff shoulders are symptoms accompanied by muscle pressure, discomfort, pain, etc., caused by muscle tension.

Muscle relaxants are used to improve such muscle tension (muscle tightness). Eperisone, tizanidine and the like are generally used as muscle relaxants, but they are used for neuropsychiatric symptoms such as light-headedness, dizziness, drowsiness and weakness, gastrointestinal symptoms such as nausea, loss of appetite and abdominal pain, and hypersensitivity such as rash and itching. Various side effects such as dysbiosis may occur.

On the other hand, there is disclosed a skin tension relaxant containing herbal ingredients together with active ingredients such as oily ingredients, inorganic salts, vitamins, mucopolysaccharides and amino acids (Patent Document 1). There is a need for substances that can relieve or relax the tension in the body.

On the other hand, due to the lack of successors and falling timber prices, the maintenance of forests has become difficult, and the devastation has become a major problem. The maintenance of this forest consists mainly of thinning and pruning. It is natural to become Therefore, in order to promote the maintenance of forests, it has been desired to develop processing methods and new uses for turning thinned and pruned trees into effective resources.

The present inventors have studied a method of heat treatment by microwave irradiation under reduced pressure as a method for effectively utilizing such felled tree branches and leaves, and the obtained distillate is a nasal symptom improving agent, It has already been reported that it can be used as an allergen-reducing agent and a harmful oxide remover such as nitrogen dioxide (Patent Documents 2, 3 and 4).

JP-A-11-246335 JP 2015-117197 A JP 2015-30704 A International publication WO2010/98439 pamphlet

The present invention has been made in view of the above circumstances, and an object thereof is to provide a highly safe muscle hardness-reducing agent derived from a natural product.

In order to solve the above problems, the present inventors have been searching for a component that has the effect of alleviating muscle tension. and completed the present invention.

That is, the present invention is a muscle hardness-reducing agent characterized by containing as an active ingredient a pressurized liquid, extract or distillate of a plant belonging to the genus Fir of the family Pinaceae.

By applying the muscle hardness-reducing agent of the present invention, it is possible to relieve and relax the already-occurring muscle tension, and by applying it in advance, muscle tension is less likely to occur. It can prevent and improve low back pain. In addition, muscles that have been subjected to a load due to exercise harden, and when the load is large, the muscle hardness may increase for several days after the exercise. By applying the muscle hardness-reducing agent of the present invention before exercise, hardening of muscles during exercise can be suppressed, breakdown can be prevented, performance can be maintained and exhibited, and muscle hardness can be reduced after exercise. It can suppress the rise and reduce the feeling of fatigue.

1 is a diagram schematically showing the configuration of a microwave distillation apparatus used for obtaining a distillate of a plant belonging to the genus Fir of the Pinaceae family, which is used as an active ingredient of the muscle hardness-reducing agent of the present invention. FIG. 4 is a graph showing the rate of change in muscle hardness in Test Example 1. FIG.

The active ingredient of the muscle hardness-reducing agent of the present invention is a pressed liquid, extract or distillate of a plant belonging to the genus Fir of the Pinaceae family.

Plants belonging to the fir genus of the family Pinaceae used as raw materials include Sakhalin fir, fir fir, white fir, white fir, white fir, balsam fir, fir fir, white fir, amabilis fir, red fir, California red fir, ground fir, noble fir, and the like. can be done. Among these, Sakhalin fir is preferably used because it is excellent in the effect of reducing muscle hardness.

In the preparation of the active ingredient in the present invention, all or part of the plant body of the plant belonging to the genus Fir of the family Pinaceae (for example, fruits, seeds, leaves, bark, rhizomes, flowers, etc.) is used. Of these, branches and/or leaves are preferably used from the viewpoint of effective utilization of trees to be thinned or pruned, and from the viewpoint of high suppressing effect. Branches and/or leaves may be used as they are, but are preferably used after being pulverized and crushed by a pulverizer, a crusher, or the like.

The active ingredient of the present invention is obtained as a juice, extract or distillate from the whole or part of a plant belonging to the genus Fir of the family Pinaceae. Among these, the squeezed liquid can be produced using a known press. The extract can also be produced according to a conventional method, but it is preferable to use a polar solvent as the extraction solvent, specifically water, ethanol, methanol, butyl alcohol, ethylene glycol, propylene glycol, glycerin. halogen-containing solvents such as chloroform; ether solvents such as dioxane; carbonyl solvents such as acetone and ethyl acetate; A distillate can be obtained by atmospheric distillation, vacuum distillation, steam distillation, or the like.

Among these, distillates are preferred from the viewpoint of the effect of reducing muscle hardness, and particularly those obtained by distillation under reduced pressure with heating are preferred. Since this product contains a high concentration of monoterpenes without the need for concentration, purification, etc., it has a refreshing aroma and is highly palatable, and is also excellent in reducing muscle hardness.

Heating for the distillation may be performed by heating with a general heater or the like, but heating with microwaves is preferable from the viewpoint of heating efficiency, and it is particularly preferable to heat by irradiating microwaves without adding water. By irradiating microwaves, the water molecules contained in the plant are directly heated to generate water vapor, which acts as a mobile phase to distill the volatile components in the plant. It is believed to include vacuum distillation elements and steam distillation elements depending on the boiling points of the components.

Such a microwave-irradiated distillate can be obtained, for example, by using the apparatus shown in FIG. In the figure, 1 is a microwave distillation device, 2 is a distillation tank, 3 is a microwave heating device, 4 is a stirring splash, 5 is an air flow inlet pipe, 6 is a distillate outlet pipe, 7 is a cooling device, and 8 is a heating control. An apparatus, 9 is a decompression pump, 10 is a pressure regulating valve, 11 is a pressure control device, 12 is an object to be distilled, and 13 is a distillate.

In this apparatus 1, a plant belonging to the genus Fir of the Pinaceae family, which is a raw material to be distilled 12, is placed in a distillation tank 2, and stirred with a stirring blade 4. A microwave heating device is provided on the upper surface of the distillation tank 2. Microwaves are emitted from 3 to heat the raw material. The distillation tank 2 communicates with an air flow inlet 5 and a distillate outlet pipe 6 . The airflow inlet pipe 5 introduces air or an inert gas such as nitrogen gas into the distillation tank 2 , and this airflow is introduced from the bottom of the distillation tank 2 . Further, the distillate outflow pipe 6 leads out the distillate from the raw material from the upper part of the distillation tank 2 .

Inside the distillation tank 2, the temperature and pressure are measured by a temperature sensor and a pressure sensor (both not shown) attached thereto. 10 to be adjusted respectively.

Further, the gaseous distillate discharged from the distillation tank 2 through the distillate outlet pipe 6 is converted into a liquid by the cooling device 7 and obtained as the distillate 13 . The distillate 13 contains an oily fraction 13a and an aqueous fraction 13b, of which the oily fraction 13a is preferably used.

Distillation may be carried out at a pressure of 3 to 95 kilopascals, preferably 3 to 40 kilopascals, more preferably 3 to 20 kilopascals, and the steam temperature is 40°C. to 100°C. When the pressure is 3 kpa or less, the increase in vapor pressure of volatile components in the plant is suppressed, and the boiling point of each component becomes the main factor of vacuum distillation rather than the steam distillation factor, and the components with the lowest boiling point flow out in order. Therefore, it is not preferable in that the extraction of components having a boiling point higher than that of water is not efficiently performed, and that a large amount of high boiling point components with low repelling efficiency and poor odor preference are extracted. On the other hand, if the temperature is 95 kilopascals or more, the temperature of the raw material becomes high, which is not preferable in that the energy loss is large and the oxidation of the raw material is accelerated.

Also, the distillation time should be about 0.2 to 8 hours, preferably about 0.4 to 6 hours. If it is less than 0.2 hours, many unextracted components in the plant will remain, and if it is more than 8 hours, the raw material will be in a state close to dryness, which is not preferable in that the extraction efficiency is lowered.

Furthermore, the gas introduced into the distillation tank 2 may be air, but inert gases such as nitrogen gas, helium gas, and argon gas are preferable. 0.001 to 0.1 times the capacity.

As an active ingredient in the muscle hardness-reducing agent of the present invention, the juice, extract or distillate of the plant belonging to the genus Fir of the family Pinaceae can be used as it is. It may be used after being further concentrated or purified according to the method.

The content of juice, extract or distillate of a plant belonging to the genus fir of the family Pinaceae in the agent for reducing muscle hardness of the present invention is preferably in the range of 0.1 to 20% by mass, more preferably 0.1% by mass. 5 to 10% by mass, more preferably 1.0 to 5% by mass. If the content is less than 0.1% by mass, the effect of reducing muscle hardness may not be sufficiently obtained, while if the content is more than 20% by mass, skin irritation may occur.

The muscle hardness-reducing agent of the present invention includes various ingredients commonly used in cosmetics and pharmaceuticals, such as oils and fats, waxes, ester oils, hydrocarbon oils, silicones, surfactants, A lower alcohol, a humectant, a water-soluble polymer, an ultraviolet absorber, a sequestering agent, a pH adjuster, an antioxidant, an antibacterial agent, an anti-inflammatory agent, a fragrance, and the like can be appropriately blended.

Fats and oils include, for example, linseed oil, camellia oil, macadamia nut oil, corn oil, mink oil, coconut oil, palm oil, palm kernel oil, cocoa butter, beef tallow, mutton tallow, lard, horse fat, hydrogenated oil and hydrogenated castor oil. oils, etc., and can be used singly or in combination of two or more.

Examples of waxes include beeswax, candelilla wax, cotton wax, carnauba wax, bayberry wax, wart wax, whale wax, montan wax, bran wax, lanolin, reduced lanolin, hard lanolin, kapok wax, sugarcane wax and jojoba wax. Alternatively, two or more kinds can be mixed and used.

Ester oils include, for example, octanoate, tri-2-ethylhexaenoic acid glycerol, isooctanoate, laurate, isopropyl myristate, myristate, palmitate, stearate, isostearate, iso Palmitate, oleate, sebacate diester and the like can be mentioned, and can be used singly or in combination of two or more.

Hydrocarbon oils include, for example, liquid paraffin, ozokerite, squalane, squalene, pristane, paraffin, isoparaffin, ceresin, petrolatum, microcrystalline wax, and the like, and may be used alone or in combination of two or more.

Examples of silicones include linear silicones such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane, octamethylcyclotetrasiloxane, decamethylcyclopentasiloxane, and dodecamethylcyclohexasiloxane. Alternatively, two or more kinds can be mixed and used.

Examples of surfactants include sodium laurate, benzalkonium chloride, 2-undecyl-N,N,N-(hydroxyethylcarboxymethyl)-2-imidazoline sodium and sorbitan monooleate. Alternatively, two or more kinds can be mixed and used.

Examples of lower alcohols include methanol, ethanol, propanol, isopropanol and butanol, and one or a mixture of two or more thereof can be used.

Moisturizing agents include, for example, sorbitol, polyethylene glycol, propylene glycol, dipropylene glycol, 1,3-butylene glycol, glycerin, diglycerin and the like, and may be used singly or in combination of two or more.

Examples of water-soluble polymers include gum arabic, tragacanth gum, galactan, carob gum, guar gum, xanthan gum, karaya gum, carrageenan, pectin, agar, collagen, casein, albumin, gelatin, methylcellulose, nitrocellulose, ethylcellulose, methylhydroxypropylcellulose, Sodium cellulose sulfate, hydroxypropyl cellulose, sodium carboxymethyl cellulose, crystalline cellulose, sodium alginate, propylene glycol alginate, polyvinyl alcohol, polyvinyl methyl ether, polyvinyl pyrrolidone, polyethyl acrylate, polyacrylamide, bentonite and magnesium aluminum silicate. , can be used singly or in combination of two or more.

Examples of ultraviolet absorbers include benzoic acid-based ultraviolet absorbers such as para-aminobenzoic acid, methyl anthranilate, octyl salicylate, phenyl salicylate, homomethyl salicylate, isopropyl paramethoxycinnamate, octyl paramethoxycinnamate, and paramethoxycinnamate. 2-ethylhexyl formate, glyceryl mono-2-ethylhexanoate dip-paramethoxycinnamate, 2,4-dihydroxybenzophenone and 2-hydroxy-4-methoxybenzophenone, etc., and a mixture of one or more of them. can be used

The sequestering agent includes, for example, sodium edetate, sodium polyphosphate, sodium metaphosphate, phosphoric acid and the like, and can be used singly or in combination of two or more.

Examples of pH adjusters include lactic acid, citric acid, glycolic acid, succinic acid, tartaric acid, dl-malic acid, potassium carbonate, sodium hydrogen carbonate and ammonium hydrogen carbonate. can be used

Antioxidants include, for example, ascorbic acid, α-tocopherol, dibutylhydroxytoluene, butylhydroxyanisole, and the like, and may be used singly or in combination of two or more.

Antibacterial agents include, for example, benzoic acid, salicylic acid, carbolic acid, sorbic acid, paraoxybenzoic acid ester, parachlormetacresol, hexachlorophene, benzalkonium chloride, chlorhexidine chloride, trichlorocarbanilide and phenoxyethanol. A species or a mixture of two or more species can be used.

Anti-inflammatory agents include, for example, menthol, camphor, zinc oxide, mefenamic acid and its derivatives, phenylbutazone and its derivatives, indomethacin and its derivatives, ibuprofen and its derivatives, ketoprofen and its derivatives, diclofenac sodium, diphenhydramine, tranexamic acid and Derivatives, dexamethasone, cortisone and its esters, hydrocortisone and its esters, prednisone, adrenocortical hormones such as prednisolone, antihistamines, aging, Phellodendron bark, licorice, Senkyo, Japanese juniper, mint, loquat, lavender, rosemary and other plants or plants derived components, etc., and can be used singly or in combination of two or more.

Examples of fragrance components include hydrocarbon fragrances such as pinene and limonene, alcohol fragrances such as linalool, geraniol, citronellol, menthol, borneol, benzyl alcohol, anise alcohol, and β-phenethyl alcohol, and phenol fragrances such as anethole and eugenol. Fragrance, aldehyde fragrance such as n-butyraldehyde, isobutyraldehyde, hexylaldehyde, citral, citronellal, benzaldehyde, cinnamic aldehyde, ketone fragrance such as carvone, menthone, camphor, acetophenone, ionone, γ-butyl lactone, coumarin, Examples include lactone fragrances such as cineole, ester fragrances such as octyl acetate, benzyl acetate, cinnamyl acetate, butyl propionate and methyl benzoate.

As the dosage form of the agent for reducing muscle hardness of the present invention, external preparations such as ointments, gels, sticks, creams, tapes, cataplasms and lotions are suitable. A gel form is particularly preferred because it is not sticky when rubbed.

In the case of a gel dosage form, it contains a gelling agent and water in addition to the press, extract or distillate of the plant belonging to the genus Fir of the family Pinaceae.

Gelling agents include, for example, xanthan gum, carboxyvinyl polymer, pectin, polyethylene, beeswax, paraffin, and sodium polyacrylate. The content of the gelling agent is generally preferably 0.01 to 10% by mass, more preferably 0.1 to 5% by mass, although it depends on the type of gelling agent. If the content of the gelling agent is less than 0.01% by mass, it may not be possible to obtain a sufficient viscosity for the gel composition. The viscosity of the composition is too high and stickiness may occur.

On the other hand, the water content is not particularly limited, but from the viewpoint of usability such as non-stickiness, it is preferably 75.0 to 99.5% by mass, more preferably 80.0 to 90.0% by mass.

The muscle hardness-reducing agent of the present invention can be formulated according to a known method. For example, it can be produced by stirring the above active ingredient and other optional ingredients with a stirrer or the like until uniform.

The agent for reducing muscle hardness of the present invention may be applied by coating, spraying, or pasting an appropriate amount to the site where muscle hardness is desired to be reduced or an increase in muscle hardness is desired to be suppressed. It may be applied before or after the application of stress, but it is preferable to apply it in advance to areas where muscle tension is likely to occur due to exercise or areas where stiff shoulders or lumbago may occur.

In the present invention, "muscle hardness reduction" includes the effect of suppressing or alleviating the increase in muscle hardness associated with exerting a load on muscles such as exercise, and suppressing the increase in muscle hardness over time after applying a certain load. Alternatively, it includes the effect of relaxing, the effect of relaxing muscle tension that has already occurred in a non-loaded state, and reducing muscle hardness.

The present invention will be described in more detail below with reference to Production Examples, Examples and Formulation Examples, but the present invention is not limited to these Production Examples and the like.

Manufacturing example 1
Sakhalin fir leaves were used as a raw material, and Sakhalin fir essential oil was obtained in the following manner. That is, about 50 kg of Sakhalin fir leaves pulverized by a crushing type pulverizer (manufactured by KYB Manufacturing) is put into the distillation tank of the microwave distillation apparatus shown in FIG. It was kept under reduced pressure conditions (vapor temperature was about 67° C.) and was subjected to microwave irradiation for 1 hour for distillation. 180 g (approximately 180 mL) of oily fraction was collected from the resulting distillate.

Example 1
It was prepared by the following preparation method to obtain a gel-like muscle hardness-reducing external preparation (product of the present invention).

(Preparation method)
0.4 g of carboxyvinyl polymer (trade name: Carbopol 941 BF, manufactured by Goodrich) was added to 16.6 g of purified water and stirred to swell. To this, 3.0 g of the oily fraction of Sakhalin fir distillate obtained in Production Example 1 was added, and the mixture was further stirred until uniform to obtain a gel-like external preparation.

Test Example 1: Suppression Test of Increase in Muscle Hardness Due to Exercise A test was conducted to confirm the effect of suppressing the increase in muscle hardness due to exercise. First, 5 test subjects (3 males, 2 females) were measured at a location 20 cm above the knee of the quadriceps femoris muscle using a digital muscle hardness tester (NEUTON TDM-Z1 (RB): manufactured by Tryall Co., Ltd.). . After that, the topical gel preparation (product of the present invention) prepared in Example 1 was evenly applied to the entire quadriceps femoris muscle, and 5 minutes after the application, squats were performed 100 times. After resting for 2 minutes, 3 sets of 100 squats were performed. Immediately after 3 sets (after 0 days), after 1 day, after 2 days, and after 3 days, muscle hardness was measured in the same manner. The rate of change in muscle hardness with respect to the muscle hardness before squats was calculated by the following formula. The results are shown in Tables 1 (muscle hardness) and 3 (change rate of muscle hardness) and FIG. For comparison, one week after the end of the test, the same subject was subjected to 3 sets of squats in the same manner as in the above test, except that the product of the present invention was not applied, and the muscle hardness was measured and the rate of change. asked for The results are shown in Tables 2 (muscle hardness) and 4 (change rate of muscle hardness) and FIG.

Rate of change in muscle hardness (%) = {(muscle hardness per day - muscle hardness before squat) / muscle hardness before squat} x 100

From the above results, when the product of the present invention was not applied, the muscle hardness increased immediately after squatting compared to before squatting, and a tendency to gradually increase over time was observed, whereas the muscle hardness of the present invention tended to increase over time. When the product was applied, there was no significant change in muscle hardness immediately after squat, 1 day, 2 days, and 3 days after squat compared to before squat. It was confirmed that the use of the product of the present invention suppresses muscle hardening during exercise and suppresses or alleviates the increase in muscle hardness over time even after exercise.

Test Example 2: Muscle Hardness Reduction Test Using the gel-type external preparation prepared in Example 1, a test was conducted to confirm the muscle hardness reduction effect due to the muscle relaxant action. Measurements were taken with a muscle durometer (TDM-NA1: manufactured by Sato Shoji Co., Ltd.) at a location 20 cm above the right quadriceps knee of two subjects (male). After that, the product of the present invention prepared in Example 1 was evenly applied to the quadriceps femoris muscle, and the subject was asked to lead a normal life. The test was performed 5 times at intervals, and the average value was obtained. Table 5 shows the results.

From the above results, it was confirmed that by applying the product of the present invention, it is possible to relieve or relax the muscle tension and reduce muscle hardness in a non-loaded state.

Formulation example 1 (stick)
Based on the following formulation, a stick-like muscle hardness-reducing topical preparation was prepared by the following preparation method.

(prescription)
(Component) (% by mass)
1. Sodium stearate *1 7.0
2. Sodium lactate 50% aqueous solution *2 5.0
3. Polyethylene glycol *3 30.0
4. Isopropanol*4 15.0
5. Purified water 39.3
6. Todomatsu distillate oily fraction of Production Example 1 3.0
*1 Fcomem AB: manufactured by ADEKA Co., Ltd. *2: manufactured by Wako Pure Chemical Industries, Ltd. *3: Macrogol 400: manufactured by Sanyo Chemical Industries, Ltd. *4: Wako Pure Chemical Industries, Ltd. Manufactured by Kogyo Co., Ltd.

(Manufacturing method)
The five components except for the oily fraction of the distillate of Sakhalin fir in Production Example 1 were mixed and heated under reflux with stirring at 70 to 90°C for 30 minutes. Further, 0.3 g of the oily fraction of Sakhalin fir distillate of Production Example 1 was added and stirred, and the obtained uniform solution was placed in a stick container and solidified at room temperature to obtain a muscle hardness reducing agent having a stick shape. When this preparation was evenly applied to the shoulders of a man suffering from stiff shoulders and had him perform office work, the symptoms of stiff shoulders could be alleviated.

Formulation Example 2 (Poultice)
(prescription)
(Component) (% by mass)
1. Todomatsu distillate oily fraction of Production Example 1 0.075
2. Methyl salicylate 1.500
3. l-menthol 4.500
4. Peppermint oil 1.120
5. Tocopherol acetate 0.500
6. dl-camphor 1.800
7. Shiunko 30.000
8. Aluminum hydroxide 0.100
9. Sodium polyacrylate 7.000
10. Carboxymethylcellulose sodium 2.500
11. Carboxyvinyl polymer 1.000
12. Glycerin 12.000
13. Titanium oxide 1.000
14. Sorbitol 15.000
15. Remaining amount of purified water

(Manufacturing method)
Carboxyvinyl polymer is swelled in purified water, sorbitol is added and stirred. A mixture obtained by dispersing sodium polyacrylate, sodium carboxymethylcellulose, titanium oxide and aluminum hydroxide in glycerin was added thereto and kneaded to obtain a poultice base composition. Next, Shiunko is dissolved by heating, and the oily fraction of Sakhalin fir distillate and dl-camphor (Components 1 to 6) of Production Example 1 are added and dissolved with stirring, added to the poultice base composition and kneaded, A cataplasm base was obtained. The resulting poultice base was spread evenly on a support using a spreader, layered with a release liner, and cut into a predetermined shape to obtain a poultice.

The muscle hardness-reducing agent of the present invention can relieve and relax existing muscle tension, and can suppress increases in muscle hardness by applying it in advance, thereby preventing and improving stiff shoulders and back pain. It can be effectively used as a target drug, quasi-drug, or the like.

1 ... Microwave distillation device 2 ... Distillation tank 3 ... ... Microwave heating device 4 ... ... Stirring splash 5 ... Air flow inflow pipe 6 ... Distillate outflow pipe 7 ... Cooling device 8 ... Heating control device 9 ... Decompression pump 10 ... Pressure regulating valve 11 ... Pressure control device 12 ... Distillation object 13 ... Distilled matter 13a ... Oily fraction 13b ... Aqueous fraction

Claims (4)

A muscle hardness-reducing agent comprising, as an active ingredient , an oily fraction of a distillate obtained by heating and distilling Sakhalin fir leaves under reduced pressure . The muscle hardness reducing agent according to claim 1, wherein the content of the oily fraction of the distillate obtained by heating and distilling the leaves of Sakhalin fir under reduced pressure is 0.1 to 20% by mass. The muscle hardness reducing agent according to claim 1 or 2, which is in gel form. The muscle hardness-reducing agent according to any one of claims 1 to 3 , which is an external preparation.