JP3319870B2 - Skin external composition and bath agent - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

The present invention relates to a novel and safe antiallergic agent and its application. More specifically, it can be used as an antiallergic agent containing a plant, flutter, and comfrey extract, and various skin external compositions and bath agents containing the agent, and specifically, liquid, emulsion,
Cream, ointment, gel, powder, granule, solid, or foamy, 1) topical medicines, 2) quasi-drugs, 3) topical or systemic skin cosmetics, 4) Pharmaceutical and / or cosmetic preparations applied to the scalp and hair (for example,
Shampoos, rinsing agents, treatment agents, permanent solutions, hair styling agents, hair tonics, hair growth / hair restoration materials, etc.), and 5) bath agents to be poured into bath water for use.

[0002]

2. Description of the Related Art Allergic reactions in the human body are generally classified into type I-III (immediate type) allergies and type IV (delayed) allergies, and type I allergies occur most frequently. The mechanism of action of this type I allergy is that basophils and mast cells strongly bind to the IgE antibody on the cell surface, and when the antigen binds to this IgE antibody, the resulting chemical mediators such as histamine, cetronin, leukotriene, etc. It is released extracellularly and suppresses diffusion of antigen to other tissues and facilitates removal of antigen. However, when this reaction proceeds excessively, the target organ is locally attacked and allergy is developed (FIG. 1).

[0003]

FIG.

A typical example of type I allergy is pollen allergy, which occurs when a person producing an IgE antibody that specifically reacts to a certain pollen comes in contact with the same pollen. Recently, it has become a very serious problem since itching of eyes and inflammation of mucous membranes cause secretion of runny nose and tears.

[0005] Also, the reaction of IgE antibodies and antigens, phospholipase A ₂ enzyme in the membrane is activated, this enzyme cuts out the arachidonic acid from phospholipids is a component of the cell, further arachidonic acid lipoxygenase It is said that it is converted to leutocorien by the action of an enzyme, and is also converted to prostaglandin by the action of a cyclooxygenase enzyme. This arachidonic acid metabolism reaction (Fig. 2)
Finally, both leutocollien and prostaglandin produce chemical mediators involved in inflammation, and therefore, substances that suppress the metabolic activity of arachidonic acid can be used as antiallergic agents due to various factors,
Recently, it is considered to be effective as a therapeutic agent for atopic dermatitis, which is said to develop from children to adults.

[0006]

FIG. 2

[0007] Among allergic reactions, there is a type IV (delayed) allergic reaction apart from the type I-III (immediate type) allergy, which is activated by activated T cells reacting with the antigen. When activated T cells react with the same antigen again in the body, they release various inflammatory lymphokines (Fig. 3), which further participate in cell-mediated immunity. It is said that macrophages and lymphocytes gather at the reaction site, block macrophage migration, increase vascular permeability, and the like, and the combined action of various lymphokines causes inflammation.

[0008]

FIG. 3

[0009]

The essence of the onset of allergy is that even if a lesion is caused in a local area where an antigen (bacteria, virus, etc.) has entered, the antigen is prevented from entering the whole body and the antigen is eliminated. In view of this, it is a manifestation of the body's defense response, however, recently, the number of people complaining of allergic symptoms has greatly increased, causing local or systemic symptoms. In addition, various types of allergic properties exist due to recent changes in dietary culture / environment, development of pharmaceuticals and cosmetics, and for example, allergy to food, allergy to pollen, allergy to drugs, and allergy to contact are well known. Symptoms are currently causing great distress to people.

Therefore, recently, a large number of antiallergic agents such as drugs that inhibit the release of chemical mediators, drugs that antagonize the released chemical mediators, and drugs that specifically inhibit IgE antibody production have been developed. Is being developed. However, these antiallergic agents have insufficient efficacy, and have problems in safety and side effects.

[0011]

Means to be Solved by the Invention Based on the usefulness of a plant that has been around for a long time, elucidation of the biological action mechanism of its pharmacological action and physiological activity, and applications derived therefrom Although these have been studied, there are still few that have been actively utilized as a form reflected in general daily life.

Therefore, the present inventors have considered the above circumstances,
Various types of plant extracts that are useful as anti-allergic agents are the subject of development, and have immediate- to delayed-type allergies by having antihistamine action, arachidonic acid metabolic activity inhibitory action, and anti-contact dermatitis action. The present invention has been attained by finding an antiallergic agent and providing an excellent skin external composition and a bathing agent containing the antiallergic agent, which are more safe and contain the antiallergic agent.

The flata used in the present invention (Operculina altis)
sima Meissn (Batata-de-Puruga)) is a plant belonging to the genus Astragalus in the family Hiragionidae. It is a herbaceous plant in South America, vineless and has no tendrils. Its leaves are egg-shaped and have no serrated but slightly horny.
The upper leaves are dark green and the lower leaves are blue-white.
In the present invention, extracts obtained from leaves, rhizomes and whole plants of batata are preferred, and batata extracts are not known to have any antiallergic activity at all.

Furthermore, comfrey used in the present invention (Symphy
tum officinale Linne) is a perennial plant native to Europe belonging to the genus Echinacea, which is distributed from Europe to West Siberia and Central Asia, and has a plant height of 40-90 cm.
There are short white coarse hairs throughout. The roots are spun and branched, the stems are branched and somewhat finned. Also, the leaves are oblong oval to dermatome needles and sharply pointed. In the present invention, extracts obtained from leaves, rhizomes and whole plants of comfrey are preferred, and it is not known at all that comfrey extracts have an antiallergic effect.

[0015] The extraction from flata and comfrey is the extraction of raw or dried, further pulverized and extracted with a solvent. As the extraction solvent, a polyol-based organic solvent, water or hot water is used, and if necessary, a polyol-based organic solvent or a mixed solvent with water may be used. Can also be used in a state where. In addition, as a polyol organic solvent, methanol, ethanol, n-butanol, acetone, chloroform, ethyl acetate, n-hexane,
Examples include 1,3-butylene glycol and propylene glycol.

The extraction conditions are not particularly limited, but may be usually within the range of the boiling point of the solvent at normal temperature to normal pressure. After extraction, the solvent is filtered, concentrated and dried to obtain a solution or paste. , Gel or powder. In many cases, it can be used as it is, but if necessary, purification treatment such as deodorization and decolorization may be added as long as the effect is not affected. As a means for purification treatment such as deodorization and decolorization, an activated carbon column or the like may be used, and ordinary means generally applied to an extracted substance may be arbitrarily selected.

As the one or more plants selected from the flap and comfrey of the present invention, commercially available products may be used, and those obtained by culturing microorganisms may also be used.

[0018] Batata used in the present invention, one or more plant extracts selected from comfrey, in addition to be directly used as an antiallergic agent, the amount of the external composition for skin and bath agents, cosmetic of Type, quality of extract used,
Depending on the expected degree of action, usually 0.0
5 to 20% by weight (hereinafter expressed as%), preferably 1 to 1%
0% is good. When the amount is less than 0.05%, the effect is not sufficient, and when the amount exceeds 20%, the effect corresponding to the amount cannot be expected.

The antiallergic agent of the present invention or the composition for external use on the skin and the bath containing the antiallergic agent may be added, if necessary, in addition to the above essential components, within a range that does not impair the effects of the present invention. It can be produced by using components and additives used in preparations such as cosmetics, pharmaceuticals, and quasi-drugs in combination.

[0020] For example, oils and fats (avocado oil, almond oil, fennel oil, perilla oil, olive oil, orange oil,
Orange ruffer oil, sesame oil, cocoa butter, chamomile oil,
Carrot oil, cucumber oil, beef tallow, tallow fatty acid, kuku nut oil, safflower oil, soybean oil, camellia oil, corn oil, rapeseed oil, persic oil, castor oil, cottonseed oil, peanut oil, turtle oil, mink oil, egg yolk oil, Cocoa butter, palm oil, palm kernel oil, mokuro, coconut oil, tallow,
Lard, hydrogenated oil, hydrogenated castor oil, etc.)

[0021] waxes (beeswax, carnauba wax, spermaceti, lanolin, liquid lanolin, reduced lanolin, hard lanolin, candelilla wax, montan wax, such as shellac wax)

[0022] mineral oils (liquid paraffin, vaseline, paraffin, Ozokeraido, ceresin, microcrystalline Chris Tan wax, polyethylene powder, squalene, squalane,
Pristane, etc.)

[0023] fatty acids (lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, oleic acid, 1
Natural fatty acids such as 2-hydroxystearic acid, undecylenic acid, tall oil, lanolin fatty acid, isononanoic acid,
Caproic acid, 2-ethylbutanoic acid, isopentanoic acid, 2
-Synthetic fatty acids such as methylpentanoic acid, 2-ethylhexanoic acid and isopentanoic acid)

The alcohol (ethanol, Isopiropanoru, lauryl alcohol, cetanol, stearyl alcohol, oleyl alcohol, lanolin alcohol,
Natural alcohols such as cholesterol and phytosterol, synthetic alcohols such as 2-hexyldecanol, isostearyl alcohol and 2-octyldodecanol), and polyhydric alcohols (ethylene oxide, ethylene glycol, diethylene glycol, triethylene glycol, ethylene glycol monoethyl) Ether, ethylene glycol monobutyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, polyethylene glycol, propylene oxide, propylene glycol, polypropylene glycol, 1,3-butylene glycol, glycerin, batyl alcohol, pentaerythritol, sorbitol, mannitol, glucose, Sugar, etc.)

[0025] esters (isopropyl myristate,
Isopropyl palmitate, butyl stearate, hexyl laurate, myristyl myristate, oleyl oleate, decyl oleate, octyl dodecyl myristate, hexyl decyl dimethyloctanoate, cetyl lactate, myristyl lactate, diethyl phthalate, dibutyl phthalate, acetic acid Lanolin, ethylene glycol monostearate, propylene glycol monostearate, propylene glycol dioleate, etc.)

The metal soap (aluminum stearate, magnesium stearate, zinc stearate, calcium stearate, zinc palmitate, magnesium myristate, zinc laurate, etc. zinc undecylenate)

The gum and water-soluble polymer compound (gum arabic, benzoin gum, Danmarugomu, guaiac, Ireland moss, karaya gum, gum tragacanth, Kyarobugomu, Quincy de, agar, casein, dextrin,
Gelatin, pectin, starch, carrageenan, carboxyalkyl chitin or chitosan, hydroxyalkyl chitin or chitosan, low molecular weight chitosan, chitosan salt, sulfated chitin or chitosan, phosphorylated chitin or chitosan, alginic acid and its salts, hyaluronic acid and its salts,
Chondroitin sulfate, heparin, ethylcellulose, methylcellulose, carboxymethylcellulose, carboxyethylcellulose, sodium carboxyethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, nitrocellulose, crystalline cellulose, polyvinyl alcohol, polyvinylmethylether, polyvinylpyrrolidone, polyvinylmethacrylate, polyacrylate , Polyalkylene oxides such as polyethylene oxide and polypropylene oxide or cross-linked polymers thereof, carboxyvinyl polymer, polyethyleneimine, etc.)

[0028] Surfactants "anionic surfactant (carboxylate, sulfonate, sulfate, phosphate salt)", "cationic surfactant (an amine salt, quaternary ammonium salt)", "amphoteric surfactant Surfactants: Carboxylic acid type amphoteric surfactants (amino type, betaine type), sulfate ester type amphoteric surfactants, sulfonic acid type amphoteric surfactants, phosphate ester type amphoteric surfactants "," Nonionic surfactants " (Ether type nonionic surfactant, ether ester type nonionic surfactant, ester type nonionic surfactant,
Block polymer type nonionic surfactant, nitrogen-containing nonionic surfactant) "," Other surfactants (natural surfactants, protein hydrolyzate derivatives, polymer surfactants, including titanium and silicon) Surfactants, fluorocarbon-based surfactants)

[0029] vitamins "Vitamin Group A: retinol,
Retinal (vitamin A1), dehydroretinal (vitamin A2), carotene, lycopene (provitamin A), "vitamin B group: thiamine hydrochloride, thiamine sulfate (vitamin B1), riboflavin (vitamin B
2), pyridoxine (vitamin B6), cyanocobalamin (vitamin B12), folate, nicotinic acid, pantothenic acid, biotin, choline, inositol ”,
"Vitamin C group: ascorbic acid and its derivatives",
"Vitamin D group: ergocalciferol (vitamin D
2), cholecalciferol (vitamin D3), dihydrotaxerol "," vitamin E group: tocopherol and its derivatives, ubiquinones "," vitamin K group: phytonadione (vitamin K1), menaquinone (vitamin K2), menadione (vitamin K3), menadiol (vitamin K4) ", ferulic acid, γ-oryzanol, etc.

The amino acids (valine, leucine, isoleucine, threonine, methionine, phenylalanine, tryptophan, lysine, glycine, alanine, asparagine, glutamine, serine, cysteine, cystine, tyrosine, proline, hydroxyproline, aspartic acid, glutamic acid, hydroxylysine, Arginine, ornithine, histidine, etc., and their sulfates, phosphates, nitrates, citrates, and amino acid derivatives such as pyrrolidone carboxylic acid)

Furthermore, in the animal tissues or plants, herbal extracts (plants such as water, an organic solvent (ethanol, propylene glycol, 1,3-butylene glycol, etc.)
An extract extracted with one or a mixture of two or more of the above is desirable. In addition, in the case of animal tissues, in addition to the extract obtained by the same method as the above-mentioned plant, an extract obtained by hydrolyzing the tissue may be used. These are used as moisturizing ingredients or for various cosmetic and medical effects known so far. ), For example, Asenyaku (Asenyaku),
Ashitaba, Acerola, Altea, Arnica, Avocado,
Amacha (sweet tea), aloe, aloe vera, nettle, ginkgo (ginko leaves, ginkgo), fennel (fenka), turmeric (precious gold), usubasaishin (spicy), plum (crow plum), urajirogashi, uwaurushi, neubara (real fruit), Hioki-koshi (prolonged life grass), Ougi (horseradish), Koganebana (Ohgon), Yamazakura (cherry bark), Yellowfin (yellow), Ouren (yellow), Panax ginseng (carrot), Hypericum perforatum (brother's cut grass), Odorikosou, Dutch mustard, orange , Itohimemegi (Enshi), Nepenthes (Summer hay), Tsurukudami (Hanshu crow), Enju (Gossip flower), Artemisia (Gay leaf), Gejutsu (Garajutsu), Kudzu (Kuzukane),
Valeriana (Kikose root), Chamomile, Chikarasuuri (Ururone), Kawamuragi (Inchinko), Licorice (licorice), Raspberry, Kiwi fruit, Kikyo (Kikyo), Chrysanthemum (Chrysanthemum), Kisage (Azusa), Mandarin orange Genus plant fruit (Kikomi), Tachibana (Tachibana bark), Cucumber, Udo or Shishudo (Kang activity, independent activity), Apricot (Almond jelly), Wolfberry (Skeletal bark, Ginkgo biloba, Kikugi leaf), Clara
(Difficult), camphor tree, Kumazasa, grapefruit fruit,
Nikkei (cinnamon bark), Kaigai (Kaigai), Ebisugusa (Keiko), Malva Asagao or Asagao (Ken beef), Safflower (Safflower), Gobishi (Fivefold), Gardenia (Gardenia), Gentian, Honoki (Popular), Hinata no Kozuchi ( Cow knee),
Goshuyu (goshuyu), burdock, ginseng (gomiko), rice, rice bran, wheat, mishimasaiko (saiko), saffron, sabonso, hawthorn (yamazako), sansho (sansho), salvia, sanshinjinjin (san 7 ginseng), shiitake mushroom, jiou (jihuang), shikunshi (mikomiko), murasaki (purple root), perilla (purple leaves, perilla), oyster (persimmon), peonies
(Shakuyaku), psyllium (vegetable child, vegetative grass), ginger (ginger),
Shobu (iris), horned rice mochi (female child), spiraea, birch, stevia, honeysuckle (gold and silver flowers, Shinobi winter),
Ivy ivy, Achillea millefolium, A. niger, Azuki (red azuki bean), Elderberry (bone-attached tree), Zeniaoi, Senkyu (Kawakyu), Assemblage (Drug), Mulberry (Mulberry bark, Mulberry leaf), Jujube (Dajutsu), Soybean, taro tree, carrot, bamboo ginseng, hanasuge (chic),
(Jiyu), Dokudami (Jyuku), Fuyushinatsukutaketake (Cycanoderma), Pepper, physalis (Torone), Tachijakosou, Ryokucha (green tea), Kocha (tea), Chouzi
(Clove), unshuang mandarin (chen), camellia, camellia,
Pepper (Pepper), Touki (Toki), Calendula officinalis, Daidai (Orange skin), Warmoko (Jiyu), Maize (Nanban hair), Eucommia (Tonaka, Tonakaha), Tomato, Nanten (Nantami), Garlic (Large sun), barley (malt), hakusen (white moss bark), janohige (wheat karyu), parsley, mint (light load),
Hamamelis, rose, loquat leaf (loquat leaf), matsuhodo (bukuryo), grape or its leaves, loofah, bodaiju, button (peony), hop, maikai (my rose flower), pine needle, marronnier, mannenrou, mukuroji, melissa , Melilot, bokeh, sprouts, peaches, peaches
(Shadow), betel nut (betel wax), swordfish (mother grass),
Knapweed, Saxifeng (Tiger Eargrass), Bayberry (Yellow Plum Skin), Barley (Adler, Yokuinin), Mokogomigi, Yamagomi, Lavender, Apple Fruit, Mannentake (Lingzhi), Lemon Fruit, Forsythia, Rengeso, Gennoshoko (Old) Tokusou), Hasiridokoro (Roth Root), Chicken Tosaka, Bovine / Human Placenta Extract, Pig / Cattle Stomach, Duodenum, or Intestinal Extract or Its Decomposition, Water-Soluble Collagen, Water-Soluble Collagen Derivative, Collagen Hydrogen Hydrolyzate, elastin, elastin hydrolyzate, water-soluble elastin derivative, silk protein, silk protein hydrolyzate, bovine blood cell protein hydrolyzate, etc.)

[0032] Microbial cultures metabolites (yeast extract, selenium-containing yeast extract, rice fermented extract, Euglena extract, such as non-fat dry milk lactic acid fermentation product) and α- hydroxy acids (glycolic acid, citric acid, malic acid, tartaric acid, lactic acid Such)

[0033] Inorganic pigments (anhydrous silicic acid, magnesium silicate, talc, kaolin, bentonite, mica, mica titanium, bismuth oxychloride, zirconium oxide, magnesium oxide, zinc oxide, titanium oxide, calcium carbonate,
Magnesium carbonate, yellow iron oxide, red iron oxide, black iron oxide, gunjou, chromium oxide, chromium hydroxide, carbon black, calamine, etc.)

The ultraviolet absorber (p- aminobenzoic acid derivatives, salicylic acid derivatives, anthranilic acid derivatives, coumarin derivatives, amino acid-based compounds, benzotriazole derivatives, tetrazole derivatives, imidazoline derivatives, pyrimidine derivatives, dioxane derivatives, camphor derivatives, furan derivatives , Pyrone derivative, nucleic acid derivative, allantoin derivative, nicotinic acid derivative, vitamin B6 derivative, oxybenzone, benzophenone, guaiazulene, shikonin, baicalin, baicalein, berberine)

The astringents (lactic acid, tartaric acid, succinic acid, citric acid, allantoin, zinc chloride, zinc sulfate, zinc oxide, calamine, p- zinc phenolsulfonate, aluminum potassium sulfate, resorcinol, ferric chloride, etc. tannic acid )

The antioxidants (ascorbic acid and salts thereof, stearic acid esters, tocopherol and its ester derivatives, nordihydrocapsaicin guar Serre Ten acid, butylated hydroxytoluene (BHT), butylated hydroxy anisole (BHA), p-hydroxy anisole, gallic acid Propyl, sesamol, sesamolin, gossypol, etc.)

[0037] Anti-inflammatory agents (ichthammol, indomethacin, kaolin, salicylic acid, sodium salicylate, methyl salicylate, acetylsalicylic acid, diphenhydramine hydrochloride, d or dl- camphor, hydrocortisone,
Guaiazulene, camazulene, chlorpheniramine maleate, glycyrrhizic acid and its salts, glycyrrhetic acid and its salts)

The disinfection agent (acrinol, sulfur, benzalkonium chloride, benzethonium chloride, Mechirurozanirin, cresol, calcium gluconate, chlorhexidine gluconate, sulfamic, mercurochrome, lactoferrin or a hydrolyzate thereof, etc.)

The hair dosage (selenium disulfide, alkyl bromide isoquinolinium solution, zinc pyrithione, biphenamine,
Chiantol, castal tincture, ginger tincture,
Pepper tincture, quinine hydrochloride, strong aqueous ammonia, potassium bromate, sodium bromate, thioglycolic acid, etc.)

The perfume (musk, civet, castoreum, natural animal perfumes such as ambergris, anise essential oil, angelica essential oil, ylang-ylang essential oils, Iris essential oil,
Fennel essential oil, orange essential oil, cananga essential oil, caraway essential oil, cardamom essential oil, guaiac wood essential oil, cumin essential oil, black letter essential oil, cinnamon essential oil, cinnamon essential oil, geranium essential oil, copaiba balsam essential oil, coriandel essential oil, perilla essential oil, cedarwood essential oil, citronella essential oil , Jasmine essential oil, gingergrass essential oil, cedar essential oil, spearmint essential oil, western mint essential oil, fenfa essential oil, tuberose essential oil, c-shaped essential oil, orange flower essential oil, winter green essential oil, true balsam essential oil, baturi essential oil, rose essential oil, palmarosa essential oil, cypress Essential oil, Hiba essential oil, Sandalwood essential oil, Petit gren essential oil, Bay essential oil, Vetiva essential oil, Bergamot essential oil, Peruvian balsam essential oil, Boad rose essential oil, sycamore essential oil, Mandarin essential oil, Eucalyptus essential oil, Lime essential oil, Lavender essential oil, Linaloe essential oil, Lemongra Essential oil, lemon essential oil, rosemary essential oil, vegetable flavoring such as Japanese mint essential oils, and other synthetic fragrances)

In addition, humectants, hormones, sequestering agents, pH adjusters, chelating agents, preservatives / anti-binders, pigments / colorants, fresheners, stabilizers, animal / vegetable proteins and their degradation products Animal and plant polysaccharides and their degradation products, animal and plant glycoproteins and their degradation products, blood flow promoters, anti-inflammatory and antiallergic agents, cell activators, keratolytic agents, wound healing agents,
There are foaming agents, thickeners, oral agents, deodorants / deodorants, etc., depending on the combination of the antiallergic agent of the present invention and components having an anti-inflammatory agent / antiallergic effect known to date. An additive and synergistic anti-allergic / anti-inflammatory action can be expected.

The form of the antiallergic agent of the present invention or the composition for external use of the skin and the bath containing the antiallergic agent may be of any type, such as liquid, emulsion, cream, ointment, gel and powder. External medicines such as granules, solids, powders, foams, sheets, quasi-drugs for external use, skin,
It can be used by blending it into cosmetics for hair and bath agents, and can also be used for general foods.

[0043] More specifically, for example, lotion, milky lotion, cream, ointment, lotion, oil, basic cosmetics such as packs, facial cleansers and skin cleanser, shampoo, rinse, hair treatment, hair dressing, perming agents, Hair cosmetics such as hair tonics, hair dyes, hair growth and hair restoration, foundations, lipsticks, blushers, eye shadows, eye liners,
Make-up cosmetics such as mascara, perfumes, bath agents,
Other examples include oral drugs, oral compositions, liquid odor / odor control agents, sanitary cotton, and wet tissues.

[0044]

EXAMPLES The present invention will be described in more detail with reference to the following Examples, but it should not be construed that the present invention is limited thereto.

[0045] Example 1 Histamine Release Inhibition Test [Test Method] Report of Tsuji et al.
2. VOL, 25 NO.4, p246-253)
Of histamine release on mast cells obtained from rice
Efficiency was measured. [Preparation of Sample and Comparative Sample] Sample: Comfrey 50% ethanol extract and water extract. 30% ethanol extract of batata.  Copaiba, Bataata, Comfrey Mixed Plant Ethanol: Water
(1: 3) Extract from the mixture. Comparative sample: Dipotassium glycyrrhizinate powder (manufactured by Tokiwa Plant Chemicals)
Dissolved in water. [Animals] Slc: Wister male rats, 2-3 rats each (approx.
7-9 weeks old)

[0046] [Test Results] The results are as shown in Table 1, the free action of both plant extracts of the present invention is histamine was not observed, release inhibiting effect of histamine was observed by the converter ° und Bu (Compound) 48/80 reversed It was found to be excellent as a type I antiallergic agent.

[0047]

[Table 1]

[0048]Example 2: Inhibition test of arachidonic acid ear edema [Test method] Shinno et al.'S method (“3,4-Dihydroxychalcone”
Of mosquitoes on mouse arachidonic acid ear edema ": Nippon Pharmaceutical
113th Annual Meeting of the Society)
5% w / w arachidonic acid dissolved in acetone (SIGMA)
Ears coated with 20 μL and 60 minutes later with arachidonic acid
Punch cut (5.0mm in diameter), and cut left ear pinna as well
Arachidonic acid ear edema based on the weight difference between the left and right auricles
The expansion was measured. The sample and the comparative sample were arachidone.
A total of 3 times 0, 15, 30 minutes after acid application was applied to the right pinna for 20 ±
Apply 3mg carefully with your finger to rub it carefully about 30 times.
After a minute, the sample and the comparative sample attached to the pinna are wiped off.
Judgment was compared with the control group in which only the base was applied to the right auricle.
Ear edema inhibition rate was determined. Ointments are shown below.
The test was performed using the following formulation examples. [Preparation of sample and comparative sample] Sample: Comfrey 50% ethanol extract and water extract
After being obtained, the solvent was distilled off and concentrated. After obtaining a 30% ethanol extract of batata, the solvent is distilled off.
Concentrated.  Copaiba, Bataata, Comfrey Mixed Plant Ethanol: Water
(1: 3) After obtaining the mixed solution, the solvent is distilled off and concentrated.
What you did. Comparative sample: Dipotassium glycyrrhizinate powder (manufactured by Tokiwa Plant Chemicals)
Dissolved in water. [Animals used] Slc: ICR female mice, 8-9 each (about 6
Week old)

[0049] Formulation Example; ointment "preparation" oil layer were mixed (white petrolatum 95.0g and polyoxyethylene lauryl ether 5.0 g), dissolved by heating at 70 ° C., each sample and comparative sample separately from the present invention The amount which can be adjusted to 1,5,10,20% ointment in terms of evaporation residue was gradually added while stirring the oil layer portion, and the mixture was stirred to 30 ° C, and then cooled naturally to prepare an ointment. .

[0050] [Test Results] The results are as shown in Table 2 below, a plant extract of the present invention are both observed arachidonic acid ear edema suppressing effect was found to be excellent as a type I antiallergic agent.

[0051] Example 3: IV allergy Inhibition Test [Test method] Nakamura et al. (Japan Pharmacology Journal, 76,595 (1980))
Oxazolone-induced contact dermatitis reaction was performed with reference to FIG. That is, 3 w / w% oxozolone (manufactured by Aldrich) 0.1 dissolved in ethanol was applied to the shaved abdominal skin of mice.
After 5 days, 20 μL of 3 w / w% oxazolone dissolved in acetone was applied to both sides of the right auricle skin by application. Approximately 24 hours later, the pinna to which oxazolone was applied was punch-excised (5.0 mm in diameter), and the left auricle was similarly excised, and the swelling rate was measured from the difference in weight between the left and right auricles. Was done. The sample and the comparative sample were applied to the right pinna 7 times a total of about 1,2,3,20,21,22,23 hours after the inoculation so that 20 ± 3 mg was carefully rubbed with a finger about 30 times. After about 24 hours, the sample and the comparative sample are wiped off. In the judgment, the inhibition rate was determined by comparing with the control group in which only the base was applied to the right auricle. In addition, sample and comparative sample,
The test was carried out using the same ointment as in Example 2. [Animals used] Slc: ICR female mice, 8-9 each (about 5
Week old)

[0052] [Test Results] The results are as shown in Table 2 below, various plant extracts of the present invention are all type IV allergy suppressive action was observed, it was found that excellent as type IV antiallergic agents.

[0053]

[Table 2]

[0054] Example 4: Safety Test [primary skin irritation test] comfrey, rabbits (3 animals per group, weighing 3.8kg longitudinal) ethanol extract of each plant were depilated back of Batata to the skin of Affixed. Judgment was performed using erythema and edema as indices 24, 48, 72 hours after application by the primary irritation scoring method,
As a result, in all animals, no erythema and edema were observed, and the animals were determined to be negative.

[0055] Example 5: milky lotion was prepared by using the following test Examples 6-8 Various external preparations for creams and bath agents, male and female adults allergic disease (20 people) as a panelist, emulsions, in cream, daily , Use at least twice a day in the morning and at night, and then freely for two months,
In addition, the bath preparation was used at least once daily for free for at least two months, and a questionnaire survey on the effect of use was requested. The evaluation method is based on the following criteria.
The results are as shown in Table 3, and the numerical values in the table represent the number of people.

[0056] "skin anti-aging effect" effective: the skin of the beam, the gloss was improved. Slightly effective: Skin abrasion, gloss slightly improved. Ineffective: No change from before use.

[0057] "eczema, skin roughness improvement effect" effective: skin of eczema and rough has been improved. Somewhat effective: Eczema and roughness of skin slightly improved. Ineffective: No change from before use.

[0058]

[Table 3]

[0059] [Test Results] The results are as shown in Table 3, the present invention Batata, emulsions formulated with comfrey extract, cream, bath agents, skin anti-aging effect and eczema, skin roughness-improving effect both good results Obtained and confirmed to be effective.

[ Manufacture of Various External Preparations] External preparations were manufactured using the antiallergic agent of the present invention. The formulation examples are shown below, which can be manufactured by a conventional method,
The use of the antiallergic agent according to the present invention is not limited to these.

[0061] Example 6: milk weight percent 1. Liquid paraffin 10.0 2. Stearic acid 5.0 3. Cetanol 2.0 4. Carboxyvinyl polymer 5.0 5.1 1,3-butylene glycol 10.0 6. 6. Bata extract (20% 1,3-butylene glycol ex.) 10.0 7. Preservative qs. Appropriate amount of fragrance 9. Purified water 100 residue

[0062] Example 7: Cream% by weight of one. Squalane 20.0 2. Beeswax 5.0 3. Refined jojoba oil 5.0 4. Glycerin monostearate 2.05. Polyoxyethylene (20) sorbitan monostearate 2.06. Glycerin 5.0 7. Comfrey extract (1,3-butylene glycol ex.) 5.0 8. Preservative qs 9. Appropriate amount of fragrance 10. Purified water 100 residue

[0063] Example 8: bath agent wt% 1. Sodium bicarbonate 58.0 2. 2. anhydrous sodium sulfate 30.0 Borax 2.0 4. Dry powder of plant extract mixed with cohabita, vatata and comfrey 10.0 (50% ethanol, 30% 1,3-butylene glycol, water = 1: 1: 3 ex.)

Example 9 : Body soap weight% 1. Potassium laurate 15.0 2. Potassium myristate 5.0 3. Propylene glycol 5.0 4. 4. Kohaiha / Potata / Comfrey-mixed plant extract 10.0 (20% phenolic recall ex.) pH adjuster qs 6. Appropriate perfume amount 7. Preservative qs. Purified water 100 residue

[0065] Example 10: Hair tonic% by weight of one. Ethanol 40.0 2. 2. Ethyl oleate 1.0 3. Polyoxyethylene (40) hydrogenated castor oil 2.0 Comfrey extract (50% ethanol ex.) 5.0 5. Purified water 100 residue

[0066]

The antiallergic agent containing one or more plant extracts selected from flaps and comfrey according to the present invention has an antihistamine action, an arachidonic acid metabolic activity inhibitory action, and an anti-contact dermatitis action. Has the effect of suppressing immediate-delay allergies and is highly safe, so eczema,
It is effective for prevention and treatment of various allergic diseases such as urticaria, atopic dermatitis, allergic rhinitis, and hay fever. Further, various skin external compositions and bath preparations containing an antiallergic agent also have an effect of preventing skin aging and an effect of improving eczema and rough skin, and thus are similarly suitable for prevention and treatment of various allergic diseases. In addition, the plant-derived extract of the present invention can be used and developed for oral compositions and foods.

[Brief description of the drawings]

FIG. 1 is a diagram showing a type I allergic reaction.

FIG. 2 is a diagram showing an arachidonic acid metabolism reaction.

FIG. 3 is a diagram showing a type IV allergic reaction.

Continuation of the front page (51) Int.Cl. ⁷ identification code FI A61P 17/00 A61P 17/00 37/08 37/08 (58) Investigated field (Int.Cl. ⁷ , DB name) A61K 35/78 A61K 7/00 A61K 7/48 A61K 7/50 BIOSIS (DIALOG) CA (STN) MEDLINE (STN)

Claims (2)

(57) [Claims] 1. An extract obtained by extracting at least one plant selected from flata and comfrey with at least one solvent selected from water, hot water, lower alcohols and polyol organic solvents. An antiallergic agent characterized in that: 2. A composition for external use on the skin and a bath agent comprising the antiallergic agent according to claim 1.