JP6290618B2 - Nasal symptom improving agent - Google Patents

Description

  The present invention relates to a nasal symptom improving agent capable of alleviating and eliminating nasal unpleasant symptoms such as sneezing, runny nose and nasal congestion.

  For various nasal symptoms such as sneezing, runny nose and nasal congestion, medical approaches have been taken from various directions. However, pharmaceuticals have side effects such as drowsiness and are used for pregnant women. There may be problems in use such as caution.

  On the other hand, plant-derived essential oils are components of plant fragrances, and are widely applied to fields such as cosmetics, toiletries, indoor fragrances, and aroma therapy (aromatherapy) as raw materials for fragrances and synthetic fragrances. However, it is known that essential oils and perfume ingredients of specific plants have the action of eliminating sneezing, runny nose, nasal congestion, and the like.

  For example, Patent Document 1 discloses that a menthol-containing mask is useful for preventing and improving sneezing, nasal discharge, and nasal congestion. Patent Document 2 describes that a mask carrying at least one selected from peppermint oil, L-menthol, hiba oil, hinokitiol and an essential oil component alleviates sneezing, runny nose and nasal congestion. Further, Patent Document 3 includes olive oil, cinnamon oil, jojoba oil, castor oil, camellia oil, evening primrose oil, safflower oil, safflower oil, peanut oil, squalane, bergamot oil, avocado oil, sunflower oil, eucalyptus oil, turpentine oil, A sustained-release antiallergic agent comprising one or more vegetable essential oils selected from cacao oil, rose oil, corn oil, rapeseed oil, cottonseed oil, coconut oil and poppy oil and dl-menthol as active ingredients is described. Patent Document 4 discloses that essential oils of cedar branches, cypress branches, eucalyptus branches and leaves are effective for sneezing, runny nose, stuffy nose, itchy eyes and the like. In addition, nasal sprays containing sesame oil and eucalyptus oil or cineol (Patent Document 5), essential oils such as fennel and sage, essential oil components such as l-menthol, dl-camphor and d-borneol, peppermint oil, eucalyptus Nose drops or nasal rinses containing essential oils such as oil have been disclosed (Patent Document 6).

  However, those using menthol are too irritating, and those using other essential oils cannot sufficiently relieve nasal symptoms such as sneezing.

  By the way, due to lack of successors and falling timber prices, the forests are not well maintained, and their devastation is a major problem. The maintenance of this forest is mainly thinning and pruning, but if there is no economic value for the thinned wood and the branches and leaves that were dropped by pruning, and it only costs money, this kind of maintenance is neglected. It is natural to become. Therefore, in order to promote the maintenance of the forest, it has been desired to develop a processing method and a new application for converting the trees to be thinned or pruned into effective resources.

  The present inventors have developed an antiviral agent containing a pressed solution, extract or distillate of a plant belonging to the genus Piraceae as an active ingredient, and has filed a patent application separately (Patent Document 7).

Japanese Unexamined Patent Publication No. 63-209666 JP 7-148280 A JP 2002-370974 A JP 2000-327580 A JP 2012-193159 A Japanese Patent No. 4733333 JP 2011-173805 A

  An object of the present invention is to provide an agent for ameliorating nasal symptoms such as sneezing, runny nose and stuffy nose using thinned and pruned trees.

  The inventors of the present invention have made extensive studies to achieve the above problems, and found that essential oils obtained from specific trees have an excellent improvement effect on sneezing, runny nose, etc. It came to be completed.

  That is, the present invention relates to a nasal symptom containing, as an active ingredient, one or more woody parts and / or leaf essential oils of a tree selected from the group consisting of the genus Piraceae, the genus Koyamaki, and the genus Asunaro. It is an improving agent.

According to the present invention, it is possible to effectively relieve and improve nasal symptoms such as sneezing, runny nose and stuffy nose and uncomfortable feelings derived therefrom, and the effects can be sustained over a long period of time. .
In addition, since the active ingredient is an essential oil derived from natural plants, it has excellent biodegradability, high safety such as not affecting the hormone balance in the living body, and the advantage that resistance does not develop even after continued use Have

  Furthermore, if branches and leaves generated at the felling lumber site and thinned wood are used as raw materials for the nasal symptom improving agent of the present invention, these can be used effectively and forest degradation can be prevented.

It is a figure which shows typically the structure of the microwave distillation apparatus used in order to obtain the plant distillate used as an active ingredient of the nasal symptom improving agent of this invention. It is a figure which shows the volatilization apparatus used in order to volatilize the nose symptom improving agent of this invention to space. It is a figure which shows the pressurized air atomizer used in order to spray the nasal symptom improving agent of this invention in space.

  The nasal symptom improving agent of the present invention comprises, as an active ingredient, one or more woody parts and / or leaf essential oils of a tree selected from the group consisting of the genus Firaceae, the genus Koyamaki and the genus Asunaro. To do.

  Trees of the genus Firaceae are Todomatsu, Fir, Virgin Fir, Shirabiso, Greater Silvia, Silabe, Balsam Fir, Mitsumine Fir, White Fir, Amabilis Fir, Aoto Domatsu, California Red Fir, Grand Fir, Noble Fir, etc. As the tree, Koyamaki, etc. are used, and as the tree of the cypress Asuna family, hiba, Asunaro, Hinoki Asunaro, Hosoba Asunaro, etc. are mentioned, among which Todomatsu, Fir, Koyamaki, Hiba etc. are preferably used. .

  As the kind of tree, a tree belonging to the genus Firaceae is preferable because it has an excellent effect of improving nasal symptoms, and particularly, Todomatsu and fir are preferable.

  The woody part and / or leaves of these trees are used, and for example, the woody part of a tree that has been cut into pieces of a tree having a leaf or chipped can be used. Of these, leaves are preferred because they are excellent in improving nasal symptoms. The leaf portion may be used as it is, but it is preferable to use it after chopping, pulverization or the like.

  The essential oil can be obtained by a conventionally known method such as extraction or distillation. Specifically, alcohol solvents such as water, ethanol, methanol, butyl alcohol, ethylene glycol, propylene glycol, and glycerol; halogen-containing solvents such as chloroform; ether solvents such as dioxane; carbonyl systems such as acetone and ethyl acetate It can be obtained by solvent extraction with a solvent, a mixed solution thereof or the like, or distillation such as atmospheric distillation, vacuum distillation, steam distillation or the like.

  Among these, an essential oil obtained by distillation is suitable because it is excellent in nasal symptom improving effect, and those obtained by distillation under heating under reduced pressure are particularly preferred. In addition, heating with a heater may be used, but from the viewpoint of effects on nasal symptoms, heating by microwave is preferable, and a method of irradiating microwave without adding water is particularly preferable. By irradiating microwaves, water molecules contained in plants are directly heated to generate water vapor, which acts as a mobile phase and distills volatile components in the plants. 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 the figure, 1 is a microwave distillation apparatus, 2 is a distillation tank, 3 is a microwave heating apparatus, 4 is a stirring splash, 5 is an airflow inflow pipe, 6 is a distillate outflow pipe, 7 is a cooling apparatus, and 8 is heating control. Device, 9 is a pressure reducing 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 Pinaceae, which is a raw material to be distilled 12, is placed in a distillation tank 2, and is heated with microwaves provided on the upper surface of the distillation tank 2 while stirring with a stirring splash 4. Microwaves are emitted from the apparatus 3 to heat the raw material. The distillation tank 2 communicates with the air flow inlet 5 and the distillate outflow pipe 6. The airflow inlet pipe 5 introduces an inert gas such as air or nitrogen gas into the reaction tank 2, and this airflow is introduced from the lower part of the reaction tank 2. The distillate outflow pipe 6 leads the distillate from the raw material to the outside from the upper part of the reaction tank 2.

  The temperature and pressure of the inside of the reaction tank 2 are measured by a temperature sensor and a pressure sensor (both not shown) attached to the reaction tank 2, and a heating control device 8, a pressure control device 11, and a pressure adjusting valve are measured. 10 are adjusted respectively.

  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 and obtained as a distillate 13. The distillate 13 includes an oily fraction 13a and an aqueous fraction 13b. Of these, the oily fraction 13a is preferably used.

In the distillation, the pressure in the distillation tank 2 may be 10 to 95 kilopascals, preferably 15 to 60 kilopascals, more preferably 20 to 40 kilopascals. To 100 ° C. When the pressure is 10 kPa or less, the increase in the vapor pressure of the volatile components in the plant is suppressed, and the vacuum distillation component due to the boiling point of each component is the main component from the steam distillation component, and it flows out in order from the lowest boiling point. Therefore, it is not preferable in that extraction of a component having a boiling point higher than that of water is not efficiently performed. Moreover, since the temperature of a raw material becomes high at 95 kilopascals or more, it is not preferable at the point that an energy loss is large and the oxidation of a raw material will be promoted. 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 remain in the plant, and if it is 8 hours or more, the raw material becomes nearly dry, which is not preferable in that the extraction efficiency decreases.

  Furthermore, the gas introduced into the distillation tank 2 may be air, but an inert gas such as nitrogen gas, helium gas, or argon gas is preferable, and the flow rate per minute is the distillation tank 2. It may be about 0.001 to 0.1 times the capacity.

  The essential oil thus obtained includes monoterpene compounds having a conjugated double bond, such as α-terpinene, myrcene, alloocimene, isoprene, osimene, pyroneene, cryptotenene, β-ferrandrene, 2,4 (8). -P-menthadiene, menogellene, sesxitronene, gingiveberene, sabinene, 3,8 (9) -p-menthadiene, terpinen-4-ol, citronellal, bornyl acetate, α-terpineol, δ-3-carene, terpinolene, γ- Terpinene, 1,8-cineole and the like can be contained. Of these, β-ferrandrene, myrcene, terpinolene, γ-terpinene and the like are preferably contained, and β-ferrandrene is particularly preferably contained.

  The essential oil obtained as described above can be used as it is as an active ingredient of the nasal symptom improving agent of the present invention, but it may be further concentrated or purified by a conventional method as necessary. These essential oils may be used as the nasal symptom improving agent of the present invention as they are, or may be further combined with an appropriate solvent, for example, water, ethanol, isopropyl alcohol, propyl alcohol or other alcohol solvents, propylene glycol, ethylene In the solvent such as glycol solvent such as glycol, glycol ether solvent such as ethylene glycol monomethyl ether, propylene glycol monomethyl ether, propylene alcohol monoethyl ether, 3-methoxy-3-methyl-1-butanol The nasal symptom improving agent of the present invention can be prepared by dissolving at a concentration of about 0.01% by mass to 99% by mass.

  Further, in the production of the nasal symptom improving agent of the present invention, when it is used after being solubilized in water or a water-soluble solvent, a bactericide, a surfactant, a hydrotrope, or the like can be used as necessary.

  In addition, the nasal symptom improving agent of the present invention can be formulated as a blended fragrance by blending other fragrance components. Other perfume ingredients include, for example, alcoholic perfumes such as linalool, geraniol, citronellol, menthol, borneol, benzyl alcohol, anis alcohol, β-phenethyl alcohol, phenolic perfumes such as anethole and eugenol, n-butyraldehyde, isobutyl Aldehyde fragrances such as aldehyde, hexyl aldehyde, citral, benzaldehyde, cinnamic aldehyde, ketone fragrances such as carvone, menthone, camphor, acetophenone, ionone, lactone fragrances such as γ-butyllactone, coumarin, octyl acetate, benzyl acetate And ester perfumes such as cinnamyl acetate, butyl propionate and methyl benzoate.

  In the nasal symptom improving agent of the present invention, a component having an anti-inflammatory action can be used in combination. Such ingredients include peppermint oil, menthol, hiba oil, hinokitiol, olive oil, cinnamon oil, jojoba oil, castor oil, camellia oil, evening primrose oil, safflower oil, safflower oil, peanut oil, squalane, bergamot oil, avocado oil , Essential oils such as sunflower oil, eucalyptus oil, turpentine oil, cacao oil, rose oil, corn oil, rapeseed oil, cottonseed oil, coconut oil, poppy oil, cedar branch, cypress essential oil, eucalyptus essential oil and the like. Furthermore, it can be used in combination with commercially available or medical inhalation bronchodilators, inhaled steroids, antiallergic agents, anticholinergic agents and the like.

  The nasal symptom improving agent of the present invention thus obtained is applied directly into the nasal cavity by suction, nasal spray, spraying, etc. as a dosage form such as a spray, inhalant, spray, nasal drop, etc. Can be used. Thus, by acting by suction etc., it can be made to act directly on an affected part, it is excellent in immediate effect, and an effect can be exhibited even in a trace amount. Furthermore, there are very few side effects, such as an in-vivo detoxification period and the influence on an excretory organ, and it is excellent also in safety.

  In addition, as one aspect of using the nasal symptom improving agent of the present invention, the nasal symptom improving agent of the present invention is infiltrated into a tissue, cloth, or nonwoven fabric using liquid or spray, and the volatile component generated therefrom is sucked. It can also be used by sucking by wearing a mask with a nasal symptom improving agent.

  In addition, a commercially available or medical electric inhaler, nebulizer, dropper type nasal inhaler, nasal spray device, machine, instrument or the like may be used for aspiration.

  Furthermore, the nasal symptom improving agent of the present invention is an active ingredient by volatilizing or spraying it into the atmosphere in the form of aerosol, heat transpiration agent, blown transpiration agent, non-heat transpiration agent, fumigation agent, gel agent, etc. It is also possible to exert a nasal symptom improvement effect by sucking. Specifically, the nasal symptom improving agent is volatilized as it is or using an appropriate volatilization device, or atomization of pump spray, aerosol, ultrasonic vibrator, pressurized liquid spray, pressurized air atomization spray device, etc. The method of making it volatilize in the atomized state using an apparatus etc. is mentioned, The nasal symptom improving agent can be floated in normal living space by these methods.

  Hereinafter, the present invention will be described more specifically with reference to examples. However, the present invention is not limited to the examples.

Manufacturing example 1
Using Todomatsu leaves as a raw material, Todomatsu essential oil was obtained as follows. That is, about 50 kg of crushed todomatsu leaves with a crushing type crusher (manufactured by KYB Seisakusho) is put into the distillation tank of the microwave steam distillation apparatus shown in FIG. 1, and the pressure in the distillation tank is set to about 20 KPa while stirring. The essential oil was distilled by microwave irradiation for 1 hour (vapor temperature was about 67 ° C.). The amount of the essential oil obtained was 180 mL, and the ratio of the essential oil to the input sample was 0.34%.

Manufacturing example 2
Using the same Todomatsu leaves as in Production Example 1, Todomatsu essential oil was obtained by the following steam distillation method. That is, about 101 g of cedar leaves pulverized with a pressure pulverizer (manufactured by KYB Mfg. Co., Ltd.) are placed in a Pyrex (registered trademark) glass flask, 5 to 8 times the amount of water is added, and then the flask is heated in a hot water bath. Heat to ~ 100 ° C and boil. The essential oil sampling tube was filled with water up to the baseline before heating. When the essential oil was distilled by continuing to boil for 6 hours, 0.8 mL of the essential oil was obtained. The ratio of essential oil to the input sample was 0.79%.

Example 1
Using the essential oil produced in Production Example 1, a patient with a nasal congestion symptom was allowed to inhale headspace vapor, and the number of nasal congestion before and after that was counted. That is, the number of nostrils was counted every 15 minutes during 45 minutes before suction. Thereafter, 20 ml of a screw mouth bottle screw vial (trade name SV-20: manufactured by Tech Jam Co., Ltd.), which was previously covered with 20 ml of essential oil, was opened, and the headspace vapor was sucked three times. The number of nostrils was counted every 15 minutes for 1 hour after aspiration. The results are shown in Table 1.

  From the above results, the number of nasal congestion clearly decreased before and after the suction of the nasal symptom improving agent of the present invention. The effect appeared about 15 minutes after the suction, and the effect lasted for about 1 hour or more.

Example 2
Aerosols A and B for improving nasal symptoms were produced according to the following formulation.
(Aerosol A for improving nasal symptoms)
Todomatsu essential oil of Production Example 1 6.3g
Propellant (LPG) 18.7g
(Aerosol B for improving nasal symptoms)
Todomatsu Essential Oil 4.0g of Production Example 1
Menthol 0.3g
Solvent (ethanol) 2.0g
Propellant (LPG) 18.7g

  A male patient with nasal congestion symptoms sprayed aerosol B for nasal symptom improvement on a tissue for about 2 seconds to suck the essential oil vapor, and the nasal congestion symptoms improved after about 30 minutes.

  When a male patient with nasal congestion was sprayed with a nasal symptom-improving aerosol A for about 2 seconds and the essential oil vapor was aspirated, the nasal congestion improved after about 15 minutes. This improvement effect lasted for about 4 hours or more.

Example 3
Two drops (about 0.05 g) of todomatsu essential oil produced in Production Example 1 were added to the mask. When this mask was worn on a male patient with nasal congestion, the symptoms of nasal congestion improved.

Example 4
For patients with symptoms such as severe nasal congestion, the aerosol A for improving nasal symptoms produced in Example 2 was sprayed on the tissue for about 2 seconds, and the essential oil vapor was sucked. After a certain period of time, essential oil vapor was sucked in the same manner. Immediately after the first aspiration, the interval until the nose clogs again after biting the nose increased, and the effect lasted for about 1.5 hours. After the second suction, the interval until the nose clogged again became longer, and improvement in nasal congestion was observed.

Product example 1
Spray:
The spray of the following formulation was stored in a commercially available 150 ml trigger type spray container to prepare a spray type nasal symptom improving agent.
Active ingredient: Todomatsu essential oil of Production Example 1 0.1 g
Solvent: Ethanol 10g
Fragrance 0.05g
Surfactant 0.1g
Ion exchange water 88.85g
When this was sprayed into the indoor space once every two hours, an effect of improving nasal congestion was observed.

Product example 2
Fumigant:
10 g of Todomatsu essential oil of Production Example 1, 55 g of azodicarbonamide and 35 g of talc were kneaded, granulated and dried to prepare a fumigation type nasal symptom improving agent.

Preparation Example 3
Heating transpiration agent:
A 3 cm × 3 cm pulp mat was impregnated with 100 mg of Todomatsu essential oil of Production Example 1 to obtain a heat transpiration type nasal symptom improving agent. This was heated using a commercially available evaporator (trade name: Vapor Mat: manufactured by Huma Killer) to evaporate the nasal symptom improving agent in the room.

Product example 4
Blow transpiration agent:
50 g of pulp impregnated body (average particle size 5 mm) was impregnated with 50 mL of Todomatsu essential oil of Production Example 1 to obtain a blown transpiration agent. The active ingredient was evaporated by using a fan-type chemical vaporizer.

Product example 5
A nasal symptom improving agent for space spray was produced by dispersing 0.1% by mass of Todomatsu essential oil obtained in Production Example 1 in 99.9% by mass of water. When this nasal symptom improving agent was sprayed into the space using an ultrasonic atomizer (Echotech Co., Ltd.), nasal congestion was resolved.

Product example 6
3 g of κ-carrageenan as a gelling agent was dispersed in a mixed solution of 3.0 g of todomatsu essential oil obtained in Production Example 1 and 10 g of propylene glycol and 84 g of water, and after heat dispersion at about 60 ° C., a cup-shaped container with an open top surface. And solidified by cooling to produce a gel-like volatile nasal symptom improving agent. When installed in the indoor space and volatilized, the nasal congestion relief effect lasted for about one month.

Product example 7
2 mass% of todomatsu essential oil obtained in Production Example 1 was solubilized in water with 5 mass% of a surfactant (polyoxyethylene alkyl ether) to produce a nasal symptom improving agent for space volatilization. When this nasal symptom improving agent was installed in an indoor space using a volatilization device as shown in FIG. 2 and volatilized, the nasal congestion relieving effect lasted for about 3 months.

Product Example 8
Todomatsu essential oil obtained in Production Example 1 was sprayed indoors at 5 ml / min for 8 hours using a pressurized air atomizing spray device as shown in FIG. Nose clogging has been resolved compared to before use.

  Since the nasal symptom improving agent of the present invention is derived from a plant, it is highly safe for animals and the human body and can be used without worrying about side effects. Therefore, it can be widely used for the purpose of improving nasal symptoms such as sneezing, runny nose and nasal congestion.

  In addition, the present invention can be used in resource recycling, forestry management, and the like as a technique for producing an economical substance from the leaves of most coniferous trees.

DESCRIPTION OF SYMBOLS 1 ...... Microwave distillation apparatus 2 ... Distillation tank 3 ...... Microwave heating apparatus 4 ...... Stirring splash 5 ...... Airflow inflow pipe 6 ...... Distillate outflow pipe 7 ...... Cooling apparatus 8 ...... Heating control apparatus 9 ...... Pressure reducing pump 10 ... ... Pressure regulating valve 11 ... ... Pressure control device 12 ... ... Distillation target 13 ... ... Extract 21 ... ... Volatilization device 22 ... ... Volatilizer 23 ... ... Suction core 24 ... ... Container 25 ... ... Remover 30…… Pressurized air atomization spray device 31…… Gas-liquid mixing spray nozzle 32…… Two-liquid flow rate adjustment supply device 33…… Compressor 34…… Essential oil 35…… Water 36…… Air

Claims (12)

One or more wood and / or nasal symptom improvement agent shall be the active ingredient essential oil of the leaves of trees Pinaceae Abies.   A tree of the genus Firaceae is selected from the group consisting of Todomatsu, Fir, Virgin fir, Silaviso, Greater Silvia, Silabe, Balsam fur, Mitsune fir, White fur, Amabilis fur, Aotodomatsu, California red fur, Grand fur and Noble fur The nasal symptom improving agent according to claim 1. Essential oils, beta-phellandrene, myrcene, terpinolene and γ- those containing a monoterpene compound having one or more conjugated double bonds selected from the group consisting terpinene according to claim 1 or 2, wherein Nasal symptom improving agent. The nasal symptom improving agent according to any one of claims 1 to 3 , wherein the dosage form is an inhalant, a nasal drop, or a spray. The nasal symptom improving agent according to any one of claims 1 to 3 , wherein the dosage form is an aerosol, a heat transpiration agent, a blown transpiration agent, a non-heat transpiration agent, a fumigant or a gel agent. A method for producing a nasal symptom-improving agent containing only one or more xylem parts and / or leaf essential oils of a tree of the genus Piraceae, as an active ingredient, wherein the essential oil comprises the xylem part and / or leaves of a tree. A method for producing a nasal symptom improving agent , which is an oily fraction of a distillate obtained by distillation under heating under reduced pressure. The method for producing a nasal symptom improving agent according to claim 6 , wherein the heating is performed by microwave irradiation. The method for producing a nasal symptom improving agent according to claim 5 or 6 , wherein the pressure during distillation is 10 to 95 kilopascals. The method for producing a nasal symptom improving agent according to any one of claims 6 to 8 , wherein the vapor temperature during distillation is 40 to 100 ° C. The essential oil contains a monoterpene compound having one or more conjugated double bonds selected from the group consisting of β-ferrandrene, myrcene, terpinolene and γ-terpinene. A method for producing a nasal symptom improving agent according to any one of the above items . The method for producing a nasal symptom improving agent according to any one of claims 6 to 10, wherein the dosage form is an inhalant, a nasal drop, or a spray . The method for producing a nasal symptom improving agent according to any one of claims 6 to 10, wherein the dosage form is an aerosol, a heat transpiration agent, a blown transpiration agent, a non-heat transpiration agent, a fumigant or a gel agent .

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