JP5138341B2 - Antiallergic agent - Google Patents
Antiallergic agent Download PDFInfo
- Publication number
- JP5138341B2 JP5138341B2 JP2007289343A JP2007289343A JP5138341B2 JP 5138341 B2 JP5138341 B2 JP 5138341B2 JP 2007289343 A JP2007289343 A JP 2007289343A JP 2007289343 A JP2007289343 A JP 2007289343A JP 5138341 B2 JP5138341 B2 JP 5138341B2
- Authority
- JP
- Japan
- Prior art keywords
- acid
- formulation
- elenolic
- elenolic acid
- antiallergic
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 239000000043 antiallergic agent Substances 0.000 title claims description 13
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Description
本発明は、エレノール酸又はその塩を含有することを特徴とする抗アレルギー剤に関する。さらに、エレノール酸又はその塩を含有する食品、化粧品又は医薬品に関する。 The present invention relates to an antiallergic agent characterized by containing elenolic acid or a salt thereof. Furthermore, it is related with the foodstuffs, cosmetics, or pharmaceutical containing elenolic acid or its salt.
近年、花粉症、アトピー性皮膚炎や気管支喘息等のアレルギー疾患をはじめとする炎症性疾患は急速に増加しており、罹患率が20%を超えるようになってきたことから、深刻な社会問題となってきている。アレルギーはI型(即時型)〜IV型(遅延型)に分けられ、中でも免疫グロブリンE(IgE)抗体が関与するI型アレルギーである花粉症やアトピー性皮膚炎は、発生頻度が非常に高いアレルギーである。 In recent years, inflammatory diseases including allergic diseases such as hay fever, atopic dermatitis and bronchial asthma have been rapidly increasing, and the morbidity has exceeded 20%. It has become. Allergies are classified into type I (immediate type) to type IV (delayed type), and hay fever and atopic dermatitis, which are type I allergies involving immunoglobulin E (IgE) antibodies, are very frequent. Allergic.
I型アレルギーの発症の過程を3段階に分けると、第1段階では、花粉やダニ、ハウスダスト等の外来性の抗原が体内に侵入し、免疫担当細胞系によってIgE抗体が産生される。IgE抗体は、気道、皮膚および消化器等アレルギー反応の好発部位に分布する肥満細胞等に固着して感作が成立する。 When the onset process of type I allergy is divided into three stages, in the first stage, foreign antigens such as pollen, mites, and house dust enter the body, and IgE antibodies are produced by the immunocompetent cell line. IgE antibody adheres to mast cells and the like distributed at sites where allergic reactions are common, such as the respiratory tract, skin and digestive organs, and sensitization is established.
第2段階では、感作が成立した肥満細胞に対して、再び抗原が接触すると、肥満細胞は形態学的変化を引き起こし、ヒスタミン、セロトニンやロイコトリエン等の化学伝達物質を遊離する。 In the second stage, when the sensitized mast cell is contacted with the antigen again, the mast cell causes a morphological change and releases chemical mediators such as histamine, serotonin and leukotriene.
第3段階では、遊離した化学伝達物質によって気管支筋や消化器等の平滑筋の収縮、毛細血管透過性の亢進、好中球の遊走、血小板の凝集等が起こり、その結果、喘息や下痢を伴う消化器アレルギー、鼻アレルギー、蕁麻疹といったアレルギー症状を発現する。 In the third stage, the released chemical mediator causes contraction of smooth muscles such as bronchial muscles and digestive organs, increased capillary permeability, neutrophil migration, platelet aggregation, etc., resulting in asthma and diarrhea Allergic symptoms such as gastrointestinal allergies, nasal allergies and urticaria appear.
このようなI型アレルギーによる疾患の予防又は治療のため、最近の研究では、上記の第2段階による化学伝達物質の遊離抑制作用や第3段階による遊離された化学伝達物質、例えばヒスタミンが引き起こすアレルギーの諸症状を抑制する作用に着目した、より安全性の高い機能性物質の検索が行われている。それと同時に食品、化粧品、医薬品等、広い分野で安心して使用することができるものが好ましいとされている。 In order to prevent or treat such diseases caused by type I allergies, recent studies have shown that the above-mentioned action of inhibiting the release of chemical mediators by the second stage and the allergy caused by the third stage of released chemical mediators such as histamine The search for functional substances with higher safety has been conducted, focusing on the action of suppressing various symptoms. At the same time, those that can be used with peace of mind in a wide range of fields such as food, cosmetics, and pharmaceuticals are preferred.
なお、従来の技術としては、シソ・エゴマ由来の抗アレルギー組成物(特許文献1)、オリーブ葉由来の抗アレルギー剤(特許文献2)等が開示されている。
また、エレノール酸又はその塩に関しては血管新生阻害効果(特許文献3)等が開示されている。しかし、エレノール酸又はその塩の抗アレルギー効果については知られていない。
本発明の目的は、安全性が高い天然物由来の物質の中から、食品、化粧品、医薬品等へ容易に配合可能で抗炎症作用や抗アレルギー作用が優れている物質を見出し、提供することを目的としている。 The object of the present invention is to find and provide a substance that can be easily blended into foods, cosmetics, pharmaceuticals, etc. and has excellent anti-inflammatory and anti-allergic effects from among highly safe substances derived from natural products. It is aimed.
本発明者らは、上記課題について鋭意研究した結果、エレノール酸又はその塩に強いヒスタミン遊離抑制作用を見出し、本発明を完成するに至った。 As a result of intensive studies on the above problems, the present inventors have found a strong histamine release inhibitory action against elenolic acid or a salt thereof, and have completed the present invention.
すなわち、本発明はエレノール酸(1)又はその塩を含有する抗アレルギー剤を提供する。 That is, the present invention provides an antiallergic agent containing elenolic acid (1) or a salt thereof.
また、本発明のエレノール酸は(1)の構造のほか、アルデヒド型(2)をとることもある。
In addition to the structure of (1), the elenolic acid of the present invention may take aldehyde type (2).
本発明のエレノール酸塩は薬理学的に許容される塩の形を用いることができる。例えば、ナトリウム、カリウム、カルシウム、マグネシウムや亜鉛等の一価又は二価以上の無機塩、有機アミンや塩基性アミノ酸等の有機塩又はこれらの組み合わせによって形成される塩が挙げられる。 The enolic acid salt of the present invention can be used in the form of a pharmacologically acceptable salt. Examples thereof include monovalent or divalent or higher inorganic salts such as sodium, potassium, calcium, magnesium and zinc, organic salts such as organic amines and basic amino acids, or salts formed by combinations thereof.
本発明は、上記抗アレルギー剤を含むアレルギー疾患の予防又は治療に用いる食品、化粧品又は医薬品を提供する。また、医薬部外品もこれらに含まれる。 The present invention provides foods, cosmetics or pharmaceuticals used for the prevention or treatment of allergic diseases including the above-mentioned antiallergic agents. In addition, quasi drugs are also included in these.
本発明に用いるエレノール酸は、オレウロペインを酸や酵素を用いて加水分解したり、化学合成して得ることが出来る(非特許文献1)。
本発明に係る抗アレルギー剤の形態は特に問わない。食品や医薬品の場合、例えば、飲料、ガム、チョコレート、キャンディー、麺、パン、ケーキ、ビスケット、缶詰、レトルト食品、畜肉食品、水産練食品、マーガリン、バター、マヨネーズ、カプセル剤、錠剤、顆粒剤、粉末剤、トローチ等の通常の食品、医薬品の形態を採用することができる。一日の投与量は、体重1kg当たり、エレノール酸として0.01mg〜10mg好ましくは0.1mg〜5mg投与することができ、2〜3回に分けて投与するのが望ましい。体重1kgあたり0.01mg未満では十分な効果は望みにくい。10mgを越えて配合した場合、効果の増強は認められにくく不経済である。また、添加の方法については、予め加えておいても、製造途中で添加しても良く、作業性を考えて適宜選択すれば良い。 The form of the antiallergic agent according to the present invention is not particularly limited. In the case of food and medicine, for example, beverage, gum, chocolate, candy, noodles, bread, cake, biscuits, canned, retort food, livestock meat products, marine products, margarine, butter, mayonnaise, capsules, tablets, granules, Conventional food and pharmaceutical forms such as powders and lozenges can be employed. The daily dose can be 0.01 mg to 10 mg, preferably 0.1 mg to 5 mg, as elenolic acid per kg body weight, and it is desirable to administer it in two or three divided doses. If it is less than 0.01 mg / kg body weight, a sufficient effect is hardly expected. When compounding exceeds 10 mg, the enhancement of the effect is hardly recognized and it is uneconomical. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.
また、化粧品の場合、例えば、化粧水、クリ−ム、乳液、ゲル剤、エアゾール剤、軟膏、パップ剤、エッセンス、パック、洗浄剤、ヘヤトニック、浴用剤、ファンデ−ション、打粉、口紅等の皮膚に適用されるものが挙げられる。配合量は全量に対し、0.001〜20重量%好ましくは0.01〜10重量%配合することができる。0.001重量%未満では十分な効果は望みにくい。20重量%を越えて配合した場合、効果の増強は認められにくく不経済である。また、添加の方法については、予め加えておいても、製造途中で添加しても良く、作業性を考えて適宜選択すれば良い。 In the case of cosmetics, for example, skin such as lotion, cream, emulsion, gel, aerosol, ointment, poultice, essence, pack, cleaning agent, hair tonic, bath preparation, foundation, powder, lipstick, etc. Are applicable. The blending amount is 0.001 to 20% by weight, preferably 0.01 to 10% by weight, based on the total amount. If it is less than 0.001% by weight, a sufficient effect is hardly expected. When the blending amount exceeds 20% by weight, the enhancement of the effect is hardly recognized and it is uneconomical. In addition, the addition method may be added in advance or during the production, and may be appropriately selected in consideration of workability.
本発明に係る抗アレルギー剤を含有する食品、化粧品、医薬品には、発明の効果を損なわない範囲において、生薬、ビタミン、ミネラル、アミノ酸等の他に、乳糖、デンプン、セルロース、マルチトール、デキストリン等の賦形剤、グリセリン脂肪酸エステル、ショ糖脂肪酸エステル、ポリオキシエチレン硬化ヒマシ油等の界面活性剤、ゼラチン、プルラン、シェラック、ツェイン等の被膜剤、小麦胚芽油、米胚芽油、シリコーン油等の油脂類、ミツロウ、米糠ロウ、カルナウバロウ等のワックス類、ショ糖、ブドウ糖、果糖、ステビア、サッカリン、スクラロース等の甘味料、並びにクエン酸、リンゴ酸、グルコン酸等の酸味料、グリセリン、ポリエチレングリコール、1,3−ブチレングリコール等の保湿剤、カルボキシビニルポリマー、メチルセルロース、ベントナイト等の増粘剤、流動パラフィン、ワセリン、スクワラン等を適宜配合することができる。生薬としては、高麗人参、アメリカ人参、田七人参、霊芝、プロポリス、アガリクス、ブルーベリー、イチョウ葉及びその抽出物等が挙げられる。ビタミンとしては、ビタミンD、K等の油溶性ビタミン、ビタミンB1、B2、B6、B12、C、ナイアシン、パントテン酸、葉酸、ビオチン等の水溶性ビタミンが挙げられる。 In addition to herbal medicines, vitamins, minerals, amino acids, etc., in addition to herbal medicines, vitamins, minerals, amino acids, etc., foods, cosmetics, pharmaceuticals containing the antiallergic agent according to the present invention, lactose, starch, cellulose, maltitol, dextrin, etc. Excipients, glycerin fatty acid esters, sucrose fatty acid esters, surfactants such as polyoxyethylene hydrogenated castor oil, coating agents such as gelatin, pullulan, shellac, zein, wheat germ oil, rice germ oil, silicone oil, etc. Fats and oils, beeswax, rice bran wax, carnauba wax and other waxes, sucrose, glucose, fructose, stevia, saccharin, sucralose and other sweeteners, and citric acid, malic acid, gluconic acid and other acidulants, glycerin, polyethylene glycol, Moisturizer such as 1,3-butylene glycol, carboxyvinyl polymer Methylcellulose, thickeners such as bentonite, may be formulated as liquid paraffin, vaseline, squalane, etc. as appropriate. Examples of herbal medicines include ginseng, American ginseng, ginseng, ganoderma, propolis, agaricus, blueberries, ginkgo leaves and extracts thereof. Examples of vitamins include oil-soluble vitamins such as vitamins D and K, and water-soluble vitamins such as vitamins B1, B2, B6, B12, C, niacin, pantothenic acid, folic acid, and biotin.
エレノール酸は強いヒスタミン遊離抑制効果を示し、アレルギーの治療や予防に利用できる。 Elenolic acid has a strong inhibitory effect on histamine release and can be used for the treatment and prevention of allergies.
次に、本発明を実施するための最良の形態として実施例を挙げるが、本発明はこれらに限定されるものではない。なお、実施例に示す(%)は重量(%)を示す。 Next, examples are given as the best mode for carrying out the present invention, but the present invention is not limited to these. In the examples, (%) indicates weight (%).
製造例1 エレノール酸の調製
エレノール酸はオレウロペインを酸加水分解して調製した。すなわち、オレウロペイン(フナコシ製)2gに1N硫酸1000mLを加え、100℃で1時間処理した後、冷却し、6N水酸化ナトリウムを用いてpH2.0にして加水分解液を得た。該加水分解液を酢酸エチルによって分液を行い、酢酸エチル層を回収し、濃縮乾固した後、凍結乾燥して凍結乾燥品680mgを得た。該凍結乾燥品をオクタデシル化シリカゲルにより精製し、濃縮乾固した後、凍結乾燥してエレノール酸140mgを得た。
Production Example 1 Preparation of Elenolic Acid Elenolic acid was prepared by acid hydrolysis of oleuropein. That is, 1000 mL of 1N sulfuric acid was added to 2 g of oleuropein (Funakoshi), treated at 100 ° C. for 1 hour, cooled, and adjusted to pH 2.0 with 6N sodium hydroxide to obtain a hydrolyzed solution. The hydrolyzed solution was separated with ethyl acetate, and the ethyl acetate layer was collected, concentrated to dryness, and then freeze-dried to obtain 680 mg of a freeze-dried product. The freeze-dried product was purified by octadecylated silica gel, concentrated to dryness, and then freeze-dried to obtain 140 mg of enolic acid.
1H−NMR(300MHz、CDCl3):δ 9.91(1H,brs),9.68(1H,d,J=2Hz),7.65(1H,s),4.26(1H,dq,J=2.5,6.5Hz),3.73(3H,s),3.39(1H,brd),2.96(1H,dd,J=16,3Hz),2.70(1H,m),2.35(1H,dd,J=16,11Hz),1.57(3H,d,J=6.5Hz) 1 H-NMR (300 MHz, CDCl 3 ): δ 9.91 (1H, brs), 9.68 (1H, d, J = 2 Hz), 7.65 (1H, s), 4.26 (1H, dq) , J = 2.5, 6.5 Hz), 3.73 (3H, s), 3.39 (1H, brd), 2.96 (1H, dd, J = 16, 3 Hz), 2.70 (1H) M), 2.35 (1H, dd, J = 16, 11 Hz), 1.57 (3H, d, J = 6.5 Hz)
製造例2 エレノール酸ナトリウムの調製
エレノール酸100mgを水100mLに溶解し、0.1N水酸化ナトリウムを5mL添加した後、凍結乾燥してエレノール酸ナトリウムを87mg得た。
Production Example 2 Preparation of Sodium Elenolate 100 mg of elenolic acid was dissolved in 100 mL of water, 5 mL of 0.1N sodium hydroxide was added, and freeze-dried to obtain 87 mg of sodium elenoate.
処方例1 錠菓
処方 配合量(%)
1.エレノール酸(製造例1) 2.0
2.砂糖 78.8
3.グルコース 19.0
4.ショ糖脂肪酸エステル 0.2
<製法>
成分1〜3に70%エタノールを適量加えて練和し、押出し造粒した後に乾燥して顆粒を得る。成分4を加えて打錠成形し、1gの錠菓を得る。当該錠菓を1日4錠摂取することで、エレノール酸を80mg/日摂取できる。
Formulation Example 1 Tablet Confectionery Formulation Amount (%)
1. Elenolic acid (Production Example 1) 2.0
2. Sugar 78.8
3. Glucose 19.0
4). Sucrose fatty acid ester 0.2
<Production method>
An appropriate amount of 70% ethanol is added to components 1 to 3, kneaded, extruded and granulated, and dried to obtain granules. Ingredient 4 is added and tableting is performed to obtain 1 g of tablet confectionery. By taking 4 tablets of the tablet confection per day, it is possible to take 80 mg / day of enolic acid.
処方例2 キャンディー
処方 配合量(%)
1.エレノール酸(製造例1) 1.0
2.マルチトール 70.0
3.デンプン糖化物 29.0
<製法>
成分1〜3を120〜170℃で加熱溶解し、金型にて固化させ、3gの飴を得る。当該飴を1日3個摂取することで、エレノール酸を90mg/日摂取できる。
Formulation Example 2 Candy Formulation Amount (%)
1. Elenolic acid (Production Example 1) 1.0
2. Maltitol 70.0
3. Saccharified starch 29.0
<Production method>
Ingredients 1 to 3 are heated and melted at 120 to 170 ° C. and solidified in a mold to obtain 3 g of soot. By ingesting 3 of the persimmons per day, it is possible to ingest 90 mg / day of elenolic acid.
比較処方例1 従来のキャンディー
処方例2においてエレノール酸(製造例1)をデンプン糖化物に置き換えたものを従来のキャンディーとした。
Comparative Formulation Example 1 Conventional Candy A conventional candy was prepared by replacing Elenolic acid (Production Example 1) with a starch saccharified product in Formulation Example 2.
処方例3 顆粒剤
処方 配合量(%)
1.エレノール酸ナトリウム(製造例2) 4.0
2.乳糖 81.0
3.セルロース 15.0
<製法>
成分1〜3に70%エタノールを適量加えて練和して押出し造粒し、乾燥して顆粒剤を得る。当該顆粒剤は、1回1gずつ1日3回摂取することで、エレノール酸ナトリウムを120mg/日摂取できる。
Formulation Example 3 Granule formulation Formulation amount (%)
1. Sodium elenoate (Production Example 2) 4.0
2. Lactose 81.0
3. Cellulose 15.0
<Production method>
An appropriate amount of 70% ethanol is added to components 1 to 3, kneaded, extruded and granulated, and dried to obtain granules. The granule can be ingested 120 mg / day of sodium elenoate by ingesting 1 g at a time 3 times a day.
処方例4 飲料
処方 配合量(%)
1.エレノール酸(製造例1) 0.2
2.ショ糖 6.0
3.クエン酸 0.75
4.香料 適量
5.精製水にて全量を100とする。
<製法>
成分5に成分1〜4を加え、撹拌溶解して濾過し、加熱殺菌して100gとし、これを50gガラス瓶に充填する。当該飲料は、1日1本摂取することでエレノール酸を100mg/日摂取できる。
Formulation Example 4 Beverage Formulation Amount (%)
1. Elenolic acid (Production Example 1) 0.2
2. Sucrose 6.0
3. Citric acid 0.75
4). Perfume appropriate amount 5. Bring the total amount to 100 with purified water.
<Production method>
Add ingredients 1-4 to ingredient 5, stir and dissolve, filter, heat sterilize to 100 g, and fill this into a 50 g glass bottle. The beverage can ingest 100 mg / day of elenolic acid by ingesting one bottle a day.
処方例5 化粧水
処方 配合量(%)
1. エレノール酸(製造例1) 0.1
2. 1,3−ブチレングリコール 8.0
3. グリセリン 2.0
4. キサンタンガム 0.02
5. クエン酸 0.01
6. クエン酸ナトリウム 0.1
7. エタノール 5.0
8. パラオキシ安息香酸メチル 0.1
9. ポリオキシエチレン硬化ヒマシ油(40E.O.) 0.1
10.香料 適量
11.精製水にて全量を100とする
<製法>
成分1〜6及び11と、成分7〜10をそれぞれ均一に溶解し、両者を混合し、濾過して製品とする。
Formulation Example 5 Lotion Formulation Amount (%)
1. Elenolic acid (Production Example 1) 0.1
2. 1,3-butylene glycol 8.0
3. Glycerin 2.0
4). Xanthan gum 0.02
5. Citric acid 0.01
6). Sodium citrate 0.1
7). Ethanol 5.0
8). Methyl paraoxybenzoate 0.1
9. Polyoxyethylene hydrogenated castor oil (40E.O.) 0.1
10. Perfume proper amount11. Make the total amount 100 with purified water <Production method>
Ingredients 1-6 and 11 and ingredients 7-10 are uniformly dissolved, mixed together, and filtered to obtain a product.
比較処方例2 従来の化粧水
処方例5においてエレノール酸(製造例1)を精製水に置き換えたものを従来の化粧水とした。
Comparative Formulation Example 2 Conventional lotion A formula obtained by replacing elenolic acid (Production Example 1) with purified water in Formulation Example 5 was used as a conventional lotion.
処方例6 クリーム
処方 配合量(%)
1. エレノール酸ナトリウム(製造例2) 0.05
2. スクワラン 5.5
3. オリーブ油 3.0
4. ステアリン酸 2.0
5. ミツロウ 2.0
6. ミリスチン酸オクチルドデシル 3.5
7. ポリオキシエチレンセチルエーテル(20E.O.) 3.0
8. ベヘニルアルコール 1.5
9. モノステアリン酸グリセリン 2.5
10.香料 適量
11.パラオキシ安息香酸メチル 0.2
12.パラオキシ安息香酸エチル 0.05
13.1,3−ブチレングリコール 8.5
14.精製水にて全量を100とする
<製法>
成分2〜9を加熱溶解して混合し、70℃に保ち油相とする。成分1及び11〜14を加熱溶解して混合し、75℃に保ち水相とする。油相に水相を加えて乳化して、かき混ぜながら冷却し、45℃で成分10を加え、更に30℃まで冷却して製品とする。
Formulation Example 6 Cream Formulation Amount (%)
1. Sodium elenoate (Production Example 2) 0.05
2. Squalane 5.5
3. Olive oil 3.0
4). Stearic acid 2.0
5. Beeswax 2.0
6). Octyldodecyl myristate 3.5
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Behenyl alcohol 1.5
9. Glycerol monostearate2.5
10. Perfume proper amount11. Methyl paraoxybenzoate 0.2
12 Ethyl paraoxybenzoate 0.05
13.1,3-Butylene glycol 8.5
14 Make the total amount 100 with purified water <Production method>
Ingredients 2-9 are dissolved by heating and mixed, and kept at 70 ° C. to obtain an oil phase. Ingredients 1 and 11 to 14 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring. The component 10 is added at 45 ° C., and further cooled to 30 ° C. to obtain a product.
処方例7 乳液
処方 配合量(%)
1. エレノール酸ナトリウム(製造例2) 0.5
2. スクワラン 5.0
3. オリーブ油 5.0
4. ホホバ油 5.0
5. セタノール 1.5
6. モノステアリン酸グリセリン 2.0
7. ポリオキシエチレンセチルエーテル(20E.O.) 3.0
8. ポリオキシエチレンソルビタンモノオレエート
(20E.O.) 2.0
9. 香料 適量
10.プロピレングリコール 1.0
11.グリセリン 2.0
12.パラオキシ安息香酸メチル 0.2
13.精製水にて全量を100とする
<製法>
成分2〜8を加熱溶解して混合し、70℃に保ち油相とする。成分1および10〜13を加熱溶解して混合し、75℃に保ち水相とする。油相に水相を加えて乳化して、かき混ぜながら冷却し、45℃で成分9を加え、さらに30℃まで冷却して製品とする。
Formulation Example 7 Emulsion
Formulation Amount (%)
1. Sodium elenoate (Production Example 2) 0.5
2. Squalane 5.0
3. Olive oil 5.0
4). Jojoba oil 5.0
5. Cetanol 1.5
6). Glycerol monostearate 2.0
7). Polyoxyethylene cetyl ether (20E.O.) 3.0
8). Polyoxyethylene sorbitan monooleate
(20 EO) 2.0
9. Perfume appropriate amount10. Propylene glycol 1.0
11. Glycerin 2.0
12 Methyl paraoxybenzoate 0.2
13. Make the total amount 100 with purified water <Production method>
Ingredients 2 to 8 are dissolved by heating and mixed, and kept at 70 ° C. to obtain an oil phase. Ingredients 1 and 10-13 are dissolved by heating and mixed, and kept at 75 ° C. to form an aqueous phase. The aqueous phase is added to the oil phase to emulsify, and the mixture is cooled while stirring.
処方例8 ゲル剤
処方 配合量(%)
1. エレノール酸ナトリウム(製造例2) 1.0
2. エタノール 5.0
3. パラオキシ安息香酸メチル 0.1
4. ポリオキシエチレン硬化ヒマシ油(60E.O.) 0.1
5. 香料 適量
6. 1,3−ブチレングリコール 5.0
7. グリセリン 5.0
8. キサンタンガム 0.1
9. カルボキシビニルポリマー 0.2
10.水酸化カリウム 0.2
11.精製水にて全量を100とする
<製法>
成分2〜5と、成分1及び6〜11をそれぞれ均一に溶解し、両者を混合して製品とする。
Formulation Example 8 Gel formulation Formulation amount (%)
1. Sodium elenoate (Production Example 2) 1.0
2. Ethanol 5.0
3. Methyl paraoxybenzoate 0.1
4). Polyoxyethylene hydrogenated castor oil (60 EO) 0.1
5. Perfume appropriate amount 6. 1,3-butylene glycol 5.0
7). Glycerin 5.0
8). Xanthan gum 0.1
9. Carboxyvinyl polymer 0.2
10. Potassium hydroxide 0.2
11. Make the total amount 100 with purified water <Production method>
Ingredients 2 to 5 and ingredients 1 and 6 to 11 are uniformly dissolved, and both are mixed to obtain a product.
処方例9 ファンデーション
処方 配合量(%)
1. エレノール酸(製造例1) 1.0
2. ステアリン酸 2.4
3. ポリオキシエチレンソルビタンモノステアレート
(20E.O.) 1.0
4. ポリオキシエチレンセチルエーテル(20E.O.) 2.0
5. セタノール 1.0
6. 液状ラノリン 2.0
7. 流動パラフィン 3.0
8. ミリスチン酸イソプロピル 6.5
9. カルボキシメチルセルロースナトリウム 0.1
10.ベントナイト 0.5
11.プロピレングリコール 4.0
12.トリエタノールアミン 1.1
13.パラオキシ安息香酸メチル 0.2
14.二酸化チタン 8.0
15.タルク 4.0
16.ベンガラ 1.0
17.黄酸化鉄 2.0
18.香料 適量
19.精製水にて全量を100とする
<製法>
成分2〜8を加熱溶解し、80℃に保ち油相とする。成分19に成分9をよく膨潤させ、続いて、成分1及び10〜13を加えて均一に混合する。これに粉砕機で粉砕混合した成分14〜17を加え、ホモミキサーで撹拌し75℃に保ち水相とする。この水相に油相をかき混ぜながら加え、冷却し、45℃で成分18を加え、かき混ぜながら30℃まで冷却して製品とする。
Formulation Example 9 Foundation Formulation Amount (%)
1. Elenolic acid (Production Example 1) 1.0
2. Stearic acid 2.4
3. Polyoxyethylene sorbitan monostearate (20EO) 1.0
4). Polyoxyethylene cetyl ether (20E.O.) 2.0
5. Cetanol 1.0
6). Liquid lanolin 2.0
7). Liquid paraffin 3.0
8). Isopropyl myristate 6.5
9. Sodium carboxymethylcellulose 0.1
10. Bentonite 0.5
11. Propylene glycol 4.0
12 Triethanolamine 1.1
13. Methyl paraoxybenzoate 0.2
14 Titanium dioxide 8.0
15. Talc 4.0
16. Bengala 1.0
17. Yellow iron oxide 2.0
18. Perfume proper amount19. Make the total amount 100 with purified water <Production method>
Ingredients 2 to 8 are dissolved by heating and kept at 80 ° C. to form an oil phase. Swell component 9 well in component 19, then add components 1 and 10-13 and mix uniformly. To this, components 14 to 17 pulverized and mixed with a pulverizer are added, and the mixture is stirred with a homomixer and kept at 75 ° C. to obtain an aqueous phase. The oil phase is added to this aqueous phase with stirring, cooled, component 18 is added at 45 ° C., and cooled to 30 ° C. with stirring to give a product.
処方例10 ヘヤトニック
処方 配合量(%)
1.エレノール酸(製造例1) 1.0
2.エタノール 63.0
3.グリセリン 2.0
4.精製水にて全量を100とする
<製法>
成分1〜3を成分4に溶解し、製品とする。
Formulation Example 10 Hair Tonic Formulation Amount (%)
1. Elenolic acid (Production Example 1) 1.0
2. Ethanol 63.0
3. Glycerin 2.0
4). Make the total amount 100 with purified water <Production method>
Components 1 to 3 are dissolved in Component 4 to obtain a product.
処方例11 浴用剤
処方 配合量(%)
1.エレノール酸(製造例1) 1.0
2.炭酸水素ナトリウム 50.0
3.黄色202号(1) 適量
4.香料 適量
5.硫酸ナトリウムにて全量を100とする
<製法>
成分1〜5を均一に混合し、製品とする。
Formulation Example 11 Bath formulation Formulation amount (%)
1. Elenolic acid (Production Example 1) 1.0
2. Sodium bicarbonate 50.0
3. Yellow No. 202 (1) Appropriate amount 4. Perfume appropriate amount 5. Make the total amount 100 with sodium sulfate <Production method>
Ingredients 1 to 5 are uniformly mixed to obtain a product.
試験例1 エレノール酸のヒスタミン遊離抑制試験
Wister系雄性ラット(8週齢)腹腔から採取した肥満細胞浮遊液を2×105個/mLとなるように調整し、その650μLにIgE抗体を含むラット血清の8倍希釈液320μLを加え、37℃で30分インキュベートした。次に、エレノール酸(製造例1)又はエレノール酸ナトリウム(製造例2)を0.1あるいは0.3mg/mLとなるように加え、37℃で10分間インキュベートした。さらに、卵白アルブミン20μg及びフォスファチジルセリン30μgを加え、37℃で20分間インキュベートして抗原刺激を行った後、肥満細胞浮遊液を4℃に冷却し、反応を停止させた。十分に冷却した後、3,000回転で5分間遠心分離し、遊離したヒスタミンを含む上清を回収した。
上清のヒスタミンは、n−ヘプタン中で塩酸を加えてヒスタミン塩酸塩とした後、o−フタルアルデヒド法により、蛍光強度を測定することにより定量した。
Test Example 1 Histamine Release Inhibition Test of Elenolic Acid Wistar male rat (8 weeks old) Mast cell suspension collected from the abdominal cavity was adjusted to 2 × 10 5 cells / mL, and 650 μL of the rat containing IgE antibody 320 μL of an 8-fold dilution of serum was added and incubated at 37 ° C. for 30 minutes. Next, elenolic acid (Production Example 1) or sodium elenoate (Production Example 2) was added to 0.1 or 0.3 mg / mL and incubated at 37 ° C. for 10 minutes. Furthermore, after adding 20 μg of ovalbumin and 30 μg of phosphatidylserine and incubating at 37 ° C. for 20 minutes for antigen stimulation, the mast cell suspension was cooled to 4 ° C. to stop the reaction. After cooling sufficiently, the mixture was centrifuged at 3,000 rpm for 5 minutes, and the supernatant containing the released histamine was collected.
The supernatant histamine was quantified by adding hydrochloric acid in n-heptane to form histamine hydrochloride, and then measuring the fluorescence intensity by the o-phthalaldehyde method.
表1に示すように、エレノール酸又はエレノール酸ナトリウムは濃度依存的にヒスタミン遊離抑制効果を示した。 As shown in Table 1, elenolic acid or sodium elenoate showed a histamine release inhibitory effect in a concentration-dependent manner.
試験例2 エレノール酸の花粉症改善効果
花粉症の自覚症状を持つ被験者30名に、処方例2に記載のキャンディーを1日当たり3個、1ヶ月にわたり摂取させ、摂取前後の花粉症の症状についてアンケートを実施し、改善効果を検討した。なお、比較処方例1記載の従来のキャンディーについてもプラセボ群として上記の被験者30名のうち15名に試験を実施した。
Test Example 2 Pollen allergy improvement effect of elenolic acid 30 subjects with subjective symptoms of hay fever were ingested 3 candy per prescription example 2 per day for 1 month, questionnaire about hay fever symptoms before and after ingestion And examined the improvement effect. In addition, about the conventional candy of the comparative prescription example 1, the test was implemented to 15 persons among said 30 test subjects as a placebo group.
表2に示すように、エレノール酸を含有するキャンディーを1ヶ月摂取すると、花粉症の症状である「喉の不快感」、「鼻の不快感」および「くしゃみの回数」を改善した。一方、表3に示すように、エレノール酸を含有しないキャンディーを1ヶ月摂取したプラセボ群は花粉症改善効果を示さなかった。 As shown in Table 2, when candy containing elenolic acid was ingested for one month, the symptoms of hay fever, “throat discomfort”, “nasal discomfort”, and “number of sneezing” were improved. On the other hand, as shown in Table 3, the placebo group that ingested candy that does not contain elenolic acid for 1 month showed no hay fever improvement effect.
試験例3 エレノール酸のアトピー性皮膚炎改善効果
アトピー性皮膚炎の自覚症状を持つ被験者20名に、処方例5記載の化粧水を1日当たり3回、1ヶ月にわたり塗布させ、塗布前後のアトピー性皮膚炎の症状についてアンケートを実施し、改善効果を検討した。なお、比較処方例2記載の従来の化粧水についてもプラセボ群として上記の被験者20名のうち10名に試験を実施した。
Test Example 3 Effect of Elenolic Acid on Improvement of Atopic Dermatitis To 20 subjects with subjective symptoms of atopic dermatitis, lotion described in Formulation Example 5 was applied 3 times a day for 1 month, and atopic properties before and after application A questionnaire was conducted on the symptoms of dermatitis, and the improvement effect was examined. For the conventional lotion described in Comparative Prescription Example 2, the test was conducted on 10 of the 20 subjects as a placebo group.
表4に示すように、エレノール酸を含有する化粧水を1ヶ月塗布すると、アトピー性皮膚炎の症状である「湿疹」、「肌のかゆみ」および「肌荒れ」を改善した。一方、表5に示すように、エレノール酸を含有しない化粧水を1ヶ月摂取したプラセボ群はアトピー性皮膚炎改善効果を示さなかった。 As shown in Table 4, when a skin lotion containing elenolic acid was applied for 1 month, the symptoms of atopic dermatitis, “eczema”, “skin itching” and “rough skin” were improved. On the other hand, as shown in Table 5, the placebo group that ingested the skin lotion not containing elenolic acid for 1 month did not show the atopic dermatitis improving effect.
本発明の抗アレルギー剤は、花粉やハウスダスト等によって引き起こされるアレルギー症状の緩和や改善に適用できる。 The antiallergic agent of the present invention can be applied to alleviate or improve allergic symptoms caused by pollen, house dust and the like.
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JP5138345B2 (en) * | 2007-11-17 | 2013-02-06 | 日本メナード化粧品株式会社 | Antiallergic agent |
JP5730837B2 (en) * | 2012-11-05 | 2015-06-10 | 一丸ファルコス株式会社 | Melanin production inhibitor, moisturizer, whitening cosmetic, beauty food and drink |
FR3119767B1 (en) * | 2021-02-18 | 2023-09-08 | Nmc Lab | Composition to strengthen the immune system |
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AU4139196A (en) * | 1994-11-07 | 1996-05-31 | William R. Fredrickson | Method and composition for antiviral therapy |
JP2000086510A (en) * | 1998-09-16 | 2000-03-28 | Oriza Yuka Kk | Histamine release inhibitor |
JP2005508856A (en) * | 2001-05-23 | 2005-04-07 | ケイ. ハムディ、ハムディ | Methods for inhibiting angiogenesis |
JP2005245346A (en) * | 2004-03-05 | 2005-09-15 | Kazuo Kagami | Compounded health supplemental food |
JP2006335934A (en) * | 2005-06-03 | 2006-12-14 | Shinto Fine Co Ltd | Anti-allergen composition and allergen inactivation method |
JP4954552B2 (en) * | 2006-01-07 | 2012-06-20 | 日本メナード化粧品株式会社 | Antiallergic agent |
JP5374804B2 (en) * | 2006-02-23 | 2013-12-25 | 基市 塚原 | Health functional food |
JP5138345B2 (en) * | 2007-11-17 | 2013-02-06 | 日本メナード化粧品株式会社 | Antiallergic agent |
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