JP4077149B2 - Autonomic nervous function improver - Google Patents
Autonomic nervous function improver Download PDFInfo
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- JP4077149B2 JP4077149B2 JP2000335789A JP2000335789A JP4077149B2 JP 4077149 B2 JP4077149 B2 JP 4077149B2 JP 2000335789 A JP2000335789 A JP 2000335789A JP 2000335789 A JP2000335789 A JP 2000335789A JP 4077149 B2 JP4077149 B2 JP 4077149B2
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- Coloring Foods And Improving Nutritive Qualities (AREA)
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Description
【0001】
【発明の属する技術分野】
本発明は、自律神経失調による全身倦怠疲労感、易疲労、肩こり、首こり等の種々の不定愁訴症候群症状に対して有効に作用する自律神経機能向上剤に関する。
【0002】
【従来の技術】
自律神経は交感神経と副交感神経の2つで構成されており、この2つの神経のバランスがくずれると、全身倦怠疲労感、易疲労、手足のしびれ、肩こり、目の疲れ、頭痛や集中力低下等の種々の不定愁訴症候群症状が発生する。
米糠油から得られるγ−オリザノールは、自律神経調整作用を有し、肩こりの回復に有効であり、γ−オリザノールを含んだ医薬品、食品が市販されている。また、γ−オリザノールと中枢神経刺激成分とを併用することにより種々の不定愁訴症候群症状に極めて優れた効果を発揮する(特開平11−302166号公報)。
【0003】
【発明が解決しようとする課題】
しかしながら、γ−オリザノールは水に不溶であって腸内吸収等が困難で、易疲労、肩こり等の回復作用が不充分であった。
本発明は、有効成分の親水性が高くなることにより、全身倦怠疲労感等の不定愁訴症候群症状に対して有効な自律神経機能向上剤及び食品を提供することにある。
【0004】
【課題を解決するための手段】
本発明は、フェルラ酸、クロロゲン酸、カフェ酸及びそれらの薬学的に許容される塩の群から選ばれる化合物を有効成分とする自律神経機能向上剤、不定愁訴改善剤及び疲労改善剤を提供するものである。
また、次の成分(A)及び(B):
(A)フェルラ酸、クロロゲン酸、カフェ酸及びそれらの薬学的に許容される塩の群から選ばれる化合物、
(B)生姜、唐辛子及び胡椒の群から選ばれる辛味成分
を含有する食品を提供するものである。
【0005】
本発明で用いる成分フェルラ酸、クロロゲン酸、カフェ酸及びそれらの薬学的に許容される塩の群から選ばれる化合物(以下、成分(A)と記載することもある)は、化学合成で合成されたものでもよいが、植物等の天然物を用いることができる。植物としては、成分(A)を含有する植物、例えば、コーヒー、タマネギ、ダイコン、レモン、モロヘイヤ、センキュウ、トウキ、マツ、オウレン、アギ、カンショ、トウモロコシ、大麦、コメ等が挙げられる。
【0006】
成分(A)中のカフェ酸、クロロゲン酸は植物の抽出物、例えば、コーヒー生豆、南天の葉、リンゴ未熟果等の植物体から抽出したものでもよく、特に、アカネ科コーヒー(Coffea arabica LINNE)の種子より、温時アスコルビン酸、クエン酸酸性水溶液又は熱水で抽出して得られたものが好ましい。フェルラ酸は、そのエステル体がコメあるいはハトムギ等の天然物、特に植物に含まれる化合物であり、植物から精製物あるいは工業的に得られる合成品として得ることができる。フェルラ酸エステルは、例えば、コメの糠より得られた米糠油を、室温時弱アルカリ性下で含水エタノール及びヘキサンで分配した後、含水エタノール画分に得られる。フェルラ酸は、上記工程より得られたフェルラ酸エステルを加圧加熱下硫酸で加水分解し、精製して得るか、又は細菌(Pseudomonas)を、フトモモ科チョウジノキ(Syzygium aromaticum MERRILL et PERRY)のつぼみ及び葉より水蒸気蒸留で得られた丁子油、又は丁子油から精製して得られたオイゲノールを含む培養液で培養し、その培養液を、分離、精製して得ることができる。また、化学合成によってフェルラ酸を調製する場合は、例えば、バニリンとマロン酸との縮合反応によって製造することができる(Journal of American Chemical Society, 74, 5346, 1952)。なお、カフェ酸、クロロゲン酸、フェルラ酸又はそれらの薬学的に許容される塩には、立体異性体が存在するが、本発明では、純粋な立体異性体又はそれらの混合物を用いることができる。
【0007】
フェルラ酸、クロロゲン酸、カフェ酸を薬学的に許容される塩の形で用いることにより水溶性が向上し、生理学的有効性が増大する。これらの製剤上許容される塩の塩形成用の塩基物質としては、例えば、アルカリ金属あるいはアルカリ土類金属の水酸化物(例えば、水酸化リチウム、水酸化ナトリウム、水酸化カリウム、水酸化マグネシウム、水酸化カルシウム、又は水酸化アンモニウム等)の無機塩基、アルギニン、リジン、ヒスチジン、オルニチンなどの塩基性アミノ酸、又はモノエタノールアミン、ジエタノールアミン、トリエタノールアミンなどの有機塩基が用いられるが、特に好ましいものとして、アルカリ金属あるいはアルカリ土類金属の水酸化物が挙げられる。これらの塩を調製してから、その塩を本発明の高血圧症予防・治療剤に含有させてもよいし、塩形成成分を別々に含有させて系中で反応させてもよい。
【0008】
成分(A)は2種以上を併用してもよい。
【0009】
本発明の成分(A)を有効成分とする自律神経機能向上剤の投与量は、成人(体重60kg)1日当り成分(A)の総量として、1〜500mg、特に5〜50mgであるのが好ましい。
【0010】
また、本発明の自律神経機能向上剤には、更に中枢神経刺激成分を添加させることにより、肩こり等の疲労回復効果の向上があり、好ましい。
【0011】
中枢神経刺激成分は、中枢神経を刺激してヒトの気分、動作を昂揚、増進(興奮)させる成分であって例えば、生姜、唐辛子、胡椒等の辛味成分及びカフェインが挙げられ、これらは2種以上併用してもよい。
【0012】
生姜の辛味成分は、シネロール、ジンゲロン、ショウガオール等が挙げられ、生姜中に約0.6〜1%含有される。唐辛子の辛味成分はカプサイシン等が挙げられ、唐辛子中に約2%含有される。胡椒の辛味成分はピペリン等が挙げられ、胡椒中に約6〜13%含有される。生姜、唐辛子、胡椒の辛味成分は、特に、水、エタノール抽出物が好ましい。また、市販されているこれらの辛味成分でもよい。
【0013】
カフェインは茶葉、コーヒー豆等に存在し、例えば茶葉やコーヒー豆を熱湯等で抽出、濾過し、その蒸発乾固物をエタノール等で再度抽出して得られる。またトラウベ(Traube)法等により合成しても、市販品を用いてもよい。
【0014】
中枢神経刺激成分の投与量は、成人1日当り、辛味成分を含有する場合は、辛味成分として0.1〜50gであって、生姜辛味成分の場合は好ましくは1mg〜50g、特に5mg〜5gが好ましく、唐辛子及び胡椒辛味成分の場合は好ましくは0.1mg〜2g、特に0.1〜100mgが好ましい。またカフェインの場合は、5〜300mg、特に10〜200mgが好ましい。
中枢神経刺激成分は、成分(A)に対して、0.1〜20倍重量含有するのが疲労回復の点で好ましい。
【0015】
本発明の自律神経機能向上剤は、皮膚外用剤、経口投与剤等として用い得るが、経口投与剤に用いることが効果、使用性の観点から好ましい。経口投与剤の形態は、散剤、顆粒剤、カプセル剤、丸剤、錠剤等の固形製剤、水剤、懸濁剤、乳剤等の液剤等に製剤化し得る。製剤化にあたっては、成分(A)、中枢神経刺激成分の他、経口投与剤に用いられる賦形剤、結合剤、崩壊剤、滑沢剤、コーティング剤、基剤、懸濁化剤、乳化剤、保湿剤、保存剤、安定剤、界面活性剤、矯味剤等を適宜添加し製造できる。
【0016】
製剤中においては、成分(A)の含有量は、100g中1〜1000mg、好ましくは5〜100mgである。中枢神経刺激成分の生姜、唐辛子、胡椒の辛味成分の含有量は、100g中0.1〜2000mg、好ましくは5〜500mgである。カフェインの含有量は、100g中5〜300mg、好ましくは10〜200mgである。
【0017】
本発明の自律神経機能向上剤は、食品に含有させることによっても、種々の不定愁訴症候群症状に対しても有効に作用する。更には、辛味成分を併用した食品は、疲労回復の点で優れ特に好ましい。すなわち、成分(A)フェルラ酸、クロロゲン酸、カフェ酸及びそれらの薬学的に許容される塩の群から選ばれる化合物及び成分(B)生姜、唐辛子及び胡椒の群から選ばれる辛味成分を含有する食品であって、また、成分(A)を0.001〜5%及び成分(B)を0.001〜2%含有する食品は、健康食品として嗜好性と効果の両立の点で好ましい。この場合の食品の形態としては、清涼飲料水等のドリンク剤、グミやヨーグルト等の液状・ペースト状食品、ガム、豆腐、ビスケット等の固形状食品、あるいは粉末顆粒状食品等とすることができる。
【0018】
【実施例】
実施例1
不定愁訴症状を有する女性25名が、表1の組成のカプセル(日本薬局方記載カプセルNo.1)を全身疲労、肩、首、背中にこりを感じるときにのんで、その1時間後の症状の変化を次の基準に従い評価した。
評点
4 不定愁訴症状がかなり強い
3 不定愁訴症状が強い
2 不定愁訴症状が弱い
1 不定愁訴症状がかなり弱い
0 不定愁訴症状がない(解消)
評価点:
2 服用前後で評価点差2以上(改善が認められる)
1 服用前後で評価点差1以上(やや改善が認められない)
0 服用前後で評価点差0以上(変化なし)
−1 服用前後で評価点差−1以下(不定愁訴の症状が強くなった)
【0019】
【表1】
【0020】
表1に全身疲労、肩及び首のこり、背中のこりの改善効果(平均評価点)及びこれら平均評価点を合計した改善スコアを示す。
本発明品は、いずれも改善効果、改善スコアが高く、優れた自律神経機能向上効果を示した。
【0021】
実施例2
次の組成のドリンク剤を調製した。
【0022】
不定愁訴症状を強く訴える女性15名に、ドリンク剤を100g/日服用した前後での症状の変化を実施例1と同じ方法で判定した。
被験者全員に、全身疲労、肩、首のこり及び背中のこり評点2段階以上の症状の軽減を認めた。
【0023】
【発明の効果】
製剤化が容易で自律神経失調に基づく全身倦怠疲労感、易疲労、肩、首等のこり等の不定愁訴症候群症状に対して有効な自律神経機能向上効果を有し、また飲食品中に他の食材と一緒にして食用しても同様の効果が得られる。[0001]
BACKGROUND OF THE INVENTION
The present invention relates to an agent for improving autonomic nervous function that effectively acts on various indefinite complaint syndrome symptoms such as general fatigue caused by autonomic ataxia, easy fatigue, shoulder stiffness, and neck stiffness.
[0002]
[Prior art]
Autonomic nerves are composed of sympathetic nerves and parasympathetic nerves. If the balance between these two nerves is lost, general fatigue, easy fatigue, numbness in the limbs, stiff shoulders, tired eyes, headache and reduced concentration Various indefinite complaint syndrome symptoms occur.
Γ-Oryzanol obtained from rice bran oil has an autonomic nerve regulating action and is effective for recovery of stiff shoulders, and pharmaceuticals and foods containing γ-oryzanol are commercially available. Further, the combined use of γ-oryzanol and a central nerve stimulating component exerts an extremely excellent effect on various indefinite complaint syndrome symptoms (Japanese Patent Laid-Open No. 11-302166).
[0003]
[Problems to be solved by the invention]
However, γ-oryzanol is insoluble in water and difficult to absorb in the intestine, etc., and recovery actions such as easy fatigue and shoulder stiffness are insufficient.
An object of the present invention is to provide an agent for improving autonomic nervous function and a food effective for an indefinite complaint syndrome symptom such as general fatigue and fatigue due to an increase in hydrophilicity of an active ingredient.
[0004]
[Means for Solving the Problems]
The present invention provides an autonomic nervous function improving agent , an indefinite complaint improving agent, and a fatigue improving agent comprising as an active ingredient a compound selected from the group of ferulic acid, chlorogenic acid, caffeic acid and pharmaceutically acceptable salts thereof. Is.
In addition, the following components (A) and (B):
(A) a compound selected from the group of ferulic acid, chlorogenic acid, caffeic acid and pharmaceutically acceptable salts thereof,
(B) A food containing a pungent component selected from the group consisting of ginger, chili and pepper.
[0005]
A compound selected from the group of the components ferulic acid, chlorogenic acid, caffeic acid and pharmaceutically acceptable salts thereof used in the present invention (hereinafter sometimes referred to as component (A)) is synthesized by chemical synthesis. However, natural products such as plants can be used. Examples of the plant include a plant containing the component (A), for example, coffee, onion, radish, lemon, moloheiya, senkyu, touki, pine, auren, agi, sweet potato, corn, barley, rice and the like.
[0006]
The caffeic acid and chlorogenic acid in the component (A) may be extracted from plant extracts such as green coffee beans, southern leaves, immature apples, etc., and in particular, Coffea arabica LINNE ) Is preferably obtained by extraction with warm ascorbic acid, citric acid aqueous solution or hot water. Ferulic acid is a compound contained in natural products such as rice or pearl barley, particularly plants, and can be obtained as a purified product from plants or a synthetic product obtained industrially. The ferulic acid ester is obtained, for example, in a water-containing ethanol fraction after partitioning rice bran oil obtained from rice bran with water-containing ethanol and hexane under mild alkalinity at room temperature. Ferulic acid is obtained by hydrolyzing and purifying ferulic acid ester obtained from the above step with sulfuric acid under pressure and heating, or by obtaining bacteria (Pseudomonas) buds of Syzygium aromaticum MERRILL et PERRY and It can be obtained by culturing with clove oil obtained by steam distillation from leaves, or a culture solution containing eugenol obtained by purification from clove oil, and separating and purifying the culture solution. When ferulic acid is prepared by chemical synthesis, it can be produced, for example, by a condensation reaction between vanillin and malonic acid (Journal of American Chemical Society, 74, 5346, 1952). In addition, although a stereoisomer exists in caffeic acid, chlorogenic acid, ferulic acid, or those pharmaceutically acceptable salts, a pure stereoisomer or a mixture thereof can be used in the present invention.
[0007]
Use of ferulic acid, chlorogenic acid, and caffeic acid in the form of a pharmaceutically acceptable salt improves water solubility and increases physiological effectiveness. Examples of basic substances for salt formation of these pharmaceutically acceptable salts include alkali metal or alkaline earth metal hydroxides (for example, lithium hydroxide, sodium hydroxide, potassium hydroxide, magnesium hydroxide, Inorganic bases such as calcium hydroxide or ammonium hydroxide), basic amino acids such as arginine, lysine, histidine, ornithine, or organic bases such as monoethanolamine, diethanolamine, and triethanolamine are used. And alkali metal or alkaline earth metal hydroxides. After preparing these salts, the salts may be contained in the agent for preventing or treating hypertension of the present invention, or the salt-forming components may be separately contained and reacted in the system.
[0008]
Two or more components ( A ) may be used in combination.
[0009]
The dose of the autonomic nervous function improver comprising the component (A) of the present invention as an active ingredient is preferably 1 to 500 mg, particularly 5 to 50 mg as the total amount of the component (A) per day for an adult (body weight 60 kg). .
[0010]
Further, the agent for improving autonomic nervous function of the present invention is preferable because it further improves fatigue recovery effects such as stiff shoulders by further adding a central nerve stimulating component.
[0011]
The central nerve stimulating component is a component that stimulates the central nervous system to lift and enhance human mood and movement (excitement), and examples thereof include pungent components such as ginger, chili, and pepper, and caffeine. Two or more species may be used in combination.
[0012]
Examples of the pungent component of ginger include cinerol, gingeron, gingerol and the like, and are contained in the ginger at about 0.6 to 1%. Capsaicin etc. are mentioned as a hot ingredient of a chili pepper, and it contains about 2% in a chili pepper. Examples of the pungent component of pepper include piperine and the like, and it is contained in pepper by about 6 to 13%. As the pungent component of ginger, chili and pepper, water and an ethanol extract are particularly preferable. Moreover, these pungent components marketed may be sufficient.
[0013]
Caffeine is present in tea leaves, coffee beans, and the like. For example, tea leaves and coffee beans are extracted with hot water and filtered, and the evaporated and dried product is extracted again with ethanol or the like. Moreover, even if it synthesize | combines by the Traube method etc., you may use a commercial item.
[0014]
The dose of the central nervous stimulating component is 0.1 to 50 g as a pungent component when containing a pungent component per day for an adult, and preferably 1 mg to 50 g, particularly 5 mg to 5 g in the case of a ginger pungent component. Preferably, in the case of chili and pepper flavor components, preferably 0.1 mg to 2 g, particularly 0.1 to 100 mg. In the case of caffeine, 5 to 300 mg, particularly 10 to 200 mg is preferable.
The central nerve stimulation component is preferably contained in an amount of 0.1 to 20 times the weight of the component (A) in terms of recovery from fatigue.
[0015]
The autonomic nervous function improving agent of the present invention can be used as an external preparation for skin, an oral administration agent, and the like. Oral dosage forms can be formulated into solid preparations such as powders, granules, capsules, pills and tablets, liquids such as solutions, suspensions and emulsions. In formulation, in addition to component (A) and central nerve stimulating component, excipients used in oral administration, binders, disintegrants, lubricants, coating agents, bases, suspending agents, emulsifiers, A moisturizer, a preservative, a stabilizer, a surfactant, a corrigent and the like can be added as appropriate.
[0016]
In the preparation, the content of the component ( A ) is 1-1000 mg, preferably 5-100 mg, in 100 g. The content of ginger, chili pepper and pungent components of pepper as the central nerve stimulating component is 0.1 to 2000 mg, preferably 5 to 500 mg in 100 g. The content of caffeine is 5 to 300 mg, preferably 10 to 200 mg in 100 g.
[0017]
The autonomic nervous function improving agent of the present invention acts effectively on various indefinite complaint syndrome symptoms even when incorporated in foods. Furthermore, foods using a pungent component are particularly preferred because of excellent fatigue recovery. That is, it contains a component (A) a compound selected from the group of ferulic acid, chlorogenic acid, caffeic acid and their pharmaceutically acceptable salts, and component (B) a pungent component selected from the group of ginger, chili and pepper. A food containing 0.001 to 5% of the component (A) and 0.001 to 2% of the component (B) is preferable as a health food from the viewpoint of compatibility between the palatability and the effect. The form of the food in this case can be a drink such as a soft drink, a liquid / paste food such as gummy or yogurt, a solid food such as gum, tofu or biscuits, or a powdered granular food. .
[0018]
【Example】
Example 1
Twenty-five women with indefinite complaints feel that the capsule of the composition shown in Table 1 (Japanese Pharmacopoeia capsule No. 1) feels general fatigue, stiffness in the shoulders, neck and back. Changes were evaluated according to the following criteria.
Grade 4 Indefinite complaints are quite strong 3 Indefinite complaints are strong 2 Indefinite complaints are weak 1 Indefinite complaints are fairly weak 0 There are no indefinite complaints (resolved)
Evaluation points:
2 Evaluation score difference of 2 or more before and after taking (improvement)
1 Evaluation score difference of 1 or more before and after taking (slight improvement is not recognized)
0 Evaluation score difference between before and after taking 0 (no change)
-1 Evaluation score difference before and after taking -1 or less (the symptoms of indefinite complaints became stronger)
[0019]
[Table 1]
[0020]
Table 1 shows the improvement effect (average evaluation point) of whole body fatigue, shoulder and neck stiffness, and back stiffness, and the improvement score obtained by summing up these average evaluation points.
All of the products of the present invention had high improvement effect and improvement score, and showed excellent autonomic nervous function improvement effect.
[0021]
Example 2
A drink having the following composition was prepared.
[0022]
The change in symptoms before and after taking 100 g / day of a drink was determined in the same manner as in Example 1 for 15 women who strongly complained of indefinite complaints.
All subjects showed general fatigue, relief of symptoms of shoulder, neck stiffness and back stiffness ratings of 2 or more levels.
[0023]
【The invention's effect】
It is easy to formulate and has an effective autonomic nervous function improvement effect on symptoms of indefinite complaint syndrome such as general fatigue caused by autonomic ataxia, easy fatigue, stiffness of shoulders, neck, etc. The same effect can be obtained even when edible with ingredients.
Claims (7)
(A)フェルラ酸、クロロゲン酸、カフェ酸及びそれらの薬学的に許容される塩の群から選ばれる化合物、
(B)生姜、唐辛子及び胡椒の群から選ばれる辛味成分
を含有する食品。The following components (A) and (B):
(A) a compound selected from the group of ferulic acid, chlorogenic acid, caffeic acid and pharmaceutically acceptable salts thereof,
(B) A food containing a pungent component selected from the group of ginger, chili and pepper.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
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JP2000335789A JP4077149B2 (en) | 2000-11-02 | 2000-11-02 | Autonomic nervous function improver |
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JP2000335789A JP4077149B2 (en) | 2000-11-02 | 2000-11-02 | Autonomic nervous function improver |
Publications (3)
Publication Number | Publication Date |
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JP2002145765A JP2002145765A (en) | 2002-05-22 |
JP2002145765A5 JP2002145765A5 (en) | 2005-04-07 |
JP4077149B2 true JP4077149B2 (en) | 2008-04-16 |
Family
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WO2021210673A1 (en) | 2020-04-17 | 2021-10-21 | 花王株式会社 | Agent for improving symptoms of menopause |
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JP5039305B2 (en) * | 2005-02-28 | 2012-10-03 | 花王株式会社 | Prophylactic anti-stress agent |
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US8088428B2 (en) | 2005-03-16 | 2012-01-03 | Kao Corporation | Packaged coffee drink |
JP4911087B2 (en) * | 2008-03-19 | 2012-04-04 | 株式会社カネカ | Condiment containing pepper peel |
JP2011178741A (en) * | 2010-03-03 | 2011-09-15 | Pola Chemical Industries Inc | Activator for autonomic nerve activity |
JP2012246278A (en) * | 2011-05-31 | 2012-12-13 | Takasago Internatl Corp | Psychic energizer and psychic energizer composition |
JP5396500B2 (en) * | 2012-03-12 | 2014-01-22 | 小川香料株式会社 | Menthol products containing a cooling sensation enhancer |
JP6710115B2 (en) * | 2016-06-21 | 2020-06-17 | 花王株式会社 | Gummy candy |
CN111163768A (en) | 2017-10-03 | 2020-05-15 | 花王株式会社 | Hot flash improving agent |
JP2020169124A (en) * | 2019-04-01 | 2020-10-15 | 花王株式会社 | Hotflash improver |
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WO2021210673A1 (en) | 2020-04-17 | 2021-10-21 | 花王株式会社 | Agent for improving symptoms of menopause |
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