JP2010260833A - Anti-autoimmune disease agent - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an anti-autoimmune disease agent improving the autoimmune disease by administering the same. <P>SOLUTION: This anti-autoimmune disease agent contains isoflavone and/or isoflavone glycoside, a spicy substance, a bitter substance or an acidulant substance, and a green mussel, cholic acid, and/or scymnol and/or a scymnol ester. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  This invention relates to a new anti-autoimmune disease agent.

The fulfillment of will in the brain, that is, the fulfillment of energy, is governed by serotonin and noradrenaline, which are called brain hormones. Is activated by adrenaline.
Serotonin, noradrenaline, and adrenaline are called biological monoamines. Most monoamines that are secreted by oxidative degradation by the enzyme monoamine oxidase within a maximum of 3 hours or reabsorbed into nerve tissue lose their action. .
This is a clever human body mechanism to prevent fatigue because monoamines cause fatigue by acting for a long time.
By the way, Qi refers to all functions of the human body, but the functions are roughly divided into two types. One of them is the function of each organ, hormone secretion, blood vessels, etc., which is controlled by the autonomic nerve. The other is the function of brain thinking and voluntary muscles that move by commands issued by brain thinking.
It has been pointed out early that the qi expressed by reassurance and morality in Chinese medicine only refers to the function of the autonomic innervation of the former. The command to show how much of these functions is issued from the medulla at the bottom of the brain. Considering that the function of all autonomic innervation is activated rather than activating only a specific organ or organ with an adiabatic agent, the point of action of the adiabatic agent is not the organ or organ but the command source It is considered to be a medulla oblongata. In other words, the action of the aspirating drug is to promote the transmission of commands from the medulla and the enhancement of its transmission. We have found that ablative drugs cause the blood in the body to be unevenly distributed in organs, etc., and this is also one of the important actions of medulla oblongata, which acts for vasoconstriction and dilation, leading to the autonomic nervous system It is achieved by expanding blood vessels and constricting blood vessels toward the brain and brain-regulated organs, and aims to send more nutrients to the necessary parts as a side effect of the aerobic agent.
The inventors have so far made a nutritional agent, digestive agent, health food containing cholic acid, isoflavone and / or isoflavone glycoside (Japanese Patent Laid-Open No. 2002-205998, Japanese Patent Laid-Open No. 2002-204672, Chinese Patent No. ZL01123150.5). U.S. Pat. No. 6,793,943, European Patent No. 1198994), nutrients, digestives, and health foods containing simnole and / or simnol esters, isoflavones and / or isoflavone glycosides 255823, JP 2002-253169, Chinese Patent No. ZL01123149.1), isoflavones and / or isoflavone glycosides, pungent substances, bitter substances or sour substances, in particular curcumin and cholic acid, and / or simanol and / or Nutrients containing simanol esters Digestive organs, health foods (JP 2004-123671, JP 2003-245054, Chinese Patent No. ZL02128298.6, Chinese Patent ZL02157491.X, European Patent No. 12813324, Chinese Patent No. ZL02157443.X), etc. Although it has been developed, it has been found that addition of green mussels has an excellent effect as an anti-autoimmune disease agent, and the present invention has been completed.

JP 2002-205998 JP 2002-204672 A JP 2002-255823 A JP 2002-253169 A JP 2004-123671 A JP 2003-245054 A Chinese Patent No. ZL01123150.5 US Pat. No. 6,793,943 European Patent No. 1198994 Chinese Patent No. ZL01123149.1 Chinese Patent No. ZL02128298.6 Chinese Patent No. ZL02157491. X European Patent No. 1281324 Chinese Patent No. ZL02157443. X

  The object of the present invention is to provide a drug having an extremely excellent effect on autoimmune diseases, particularly rheumatoid arthritis and hay fever.

  The invention of this application is characterized by comprising isoflavone and / or isoflavone glycoside, pungent substance, bitter substance or sour substance, green mussel, and cholic acid, and / or simanol and / or simanol ester The present invention relates to a drug having an excellent effect on autoimmune diseases.

  The present invention relates to the administration of isoflavones and / or isoflavone glycosides, pungent substances, bitter substances or sour substances, green mussels, and cholic acid, and / or simanol and / or simanol esters. Due to the synergistic action, there is an excellent effect that an anti-autoimmune disease agent, an anti-rheumatoid arthritis agent, and an anti-hay fever agent that can treat and prevent autoimmune disease, rheumatoid arthritis, and hay fever more quickly can be provided. In particular, synergism of isoflavones and / or isoflavone glycosides by administration of pungent substances, bitter substances or sour substances, small amounts of green mussels, and cholic acid, and / or simanol and / or simanol esters. By the action, there is an excellent effect that it is possible to provide an anti-autoimmune disease agent, an anti-rheumatoid arthritis agent, and an anti-hay fever agent that can treat and prevent autoimmune diseases, rheumatoid arthritis, and hay fever more quickly.

  The invention of this application includes pungent substances, bitter substances or sour substances, green mussel, isoflavones and isoflavone glycosides, cholic acid, and / or simanol and / or simanol esters, but isoflavones and isoflavone glucosides The body is particularly preferably soybean isoflavone and soybean isoflavone glycosides contained in soybean.

  The daily dose of isoflavone and isoflavone glycoside is preferably 1 to 500 mg, more preferably 5 to 200 mg, and particularly preferably 10 to 100 mg.

トウガラシのカプサイシン、

コショウのピペリン、

ショウガのジンゲロン、

ショウガの［６］−ショーガオール、

ショウガの［６］−ジンゲロール

であることが好ましく、クルクミンがとくに好ましい。
苦味物質は、スウェルチアマリン、ゲンチオピクリン、ロガニンが好ましい。
また、酸味物質は、クエン酸、乳酸が好ましい。 The pungent substance, bitter substance or sour substance of the present invention is preferably a pungent substance.
The pungent substance is turmeric curcumin,

Capsicum capsicum,

Pepperine with pepper,

Ginger gingeron,

Ginger [6]-Shogaol,

[6] -gingerol of ginger

And curcumin is particularly preferred.
The bitter substance is preferably swell thiamarin, gentiopicrin, or loganin.
The sour substance is preferably citric acid or lactic acid.

  The daily dose of the pungent substance is preferably 1 to 1000 mg, more preferably 5 to 300 mg, and particularly preferably 10 to 70 mg.

  The daily dose of cholic acid is preferably 1-1000 mg, more preferably 10-500 mg, and particularly preferably 50-300 mg.

  The daily dose of simnole and / or simnol ester is preferably 0.1 to 100 mg, more preferably 0.1 to 50 mg, and particularly preferably 0.3 to 10 mg.

  The daily dose of green mussel is preferably 0.1 to 1000 mg, more preferably 1 to 500 mg, and particularly preferably 10 to 300 mg.

As other ingredients, pharmaceuticals in general are used, and vitamins, antibiotics, anticancer agents, heme iron, prune extract, and crude drugs are used.
Preferred crude drugs are those that have a correcting effect, such as those that activate the functions of organs, glands and blood vessels that are governed by autonomic nerves, and those that aid digestion.

More than ten kinds of herbal medicines that activate the functions of organs, glands, and blood vessels controlled by autonomic nerves are known. For example, there are apricots, carrots and others, but some active ingredients of these herbal medicines including carrots are It has already been revealed.
Therefore, it is preferable to add these active ingredients. By further adding these active ingredients, the human body function activating effect can be exhibited.
Such herbal medicines include: Akagi, carrots, ginseng, ginseng, taishin, western ginseng, yellow ginseng, birch jutsu, and sanyaku. Licorice, licorice, koji, yellow spirit, quail, etc. are particularly preferred.

  In addition, it is particularly preferable to add hawthorn, shinki (kurin), life comb, malt (bakuga), cereal (kokuga), chicken inner gold (keinaikin), ahi (agi), etc., which are herbal medicines that aid digestion.

また、シムノール硫酸エステルナトリウム塩はつぎの構造式で表される。

Simnole and / or Simnol ester is contained in the bile of salmon.
Simnol is represented by the following structural formula:

Simnol sulfate sodium salt is represented by the following structural formula.

Another material used in the invention of this application is isoflavone and isoflavone glycoside.
The active ingredients for this purpose contained in soybeans are several isoflavone glycosides such as soybean in (Gaidin), glycitin (Glycitin), genistin (Gaistin) and the like, and their aglycones (Daizein), glycitein There are several isoflavones such as (Glycitein) and Genistein.
Soybean is a raw material for producing soybean oil, but the demand for soybean oil is large, and soybean meal, a by-product of the soybean oil, is produced in large quantities at the same time. A part of soybean meal is used as a raw material for producing soybean protein as a raw material for food, but it is mainly used as fertilizer and feed, and its price is extremely low. Soybean isoflavone and soybean isoflavone glycosides can be produced with high purity and low cost from soybean meal that is close to industrial waste.

The invention of this application preferably adds inosinic acid.
It is preferred to add docosahexaenoic acid.

The invention of this application preferably adds odd fatty acids.
As the odd fatty acid, tridecanoic acid, pentadecanoic acid, heptadecanoic acid and nonadecanoic acid are preferable, and pentadecanoic acid and heptadecanoic acid are particularly preferable.

  The invention of this application preferably adds docosahexaenoic acid.

Although it does not specifically limit as a dosage form which administers the anti- autoimmune disease agent of this application invention, It administers as an internal medicine, a suppository, an injection, etc., such as a tablet, a powder agent, a solid agent, and a liquid agent.
In addition, excipients such as lactose and starch, vegetable oils, and others are used.

Hereinafter, the present invention will be described in detail.
The purity of the soy isoflavone and soy isoflavone glycoside used was 40%.
Moreover, the purity of cholic acid used other than a pure product is 90%.

Example 1
Soft capsule cholic acid 150mg
Soy isoflavone (40% product) 100mg
Curcumin 30mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
100mg refined fish oil containing 27% docosahexaenoic acid
Vitamin E (containing 50% or more total tocopherol) 2mg
Beeswax 205mg
Cod liver oil appropriate amount content weight 1960mg
(1 capsule 275mg once 3 capsules 2 times a day)
Similarly, soft capsules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 2
Soft capsule Simnol sulfate Na 2mg
Soy isoflavone (40% product) 100mg
Curcumin 30mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
100mg refined fish oil containing 27% docosahexaenoic acid
Vitamin E (containing 50% or more total tocopherol) 2mg
Beeswax 205mg
Cod oil suitable content weight 1960mg
(1 capsule 275mg once 3 capsules 2 times a day)
Similarly, soft capsules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 3
Tablet curcumin 30mg
Cholic acid 150mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
Lactose 140mg
Magnesium stearate 6mg
Talc 3mg
Crystalline cellulose appropriate amount total 1120mg
(1 tablet, 280 mg, 2 tablets, 2 times a day)
Similarly, tablets were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 4
Tablet curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
Lactose 140mg
Magnesium stearate 6mg
Talc 3mg
Crystalline cellulose appropriate amount total 1120mg
(1 tablet, 280 mg, 2 tablets, 2 times a day)
Similarly, tablets were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 5
Powder
Curcumin 30mg
Cholic acid 150mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
Lactose 800mg
Corn starch
Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, powder was prepared using soy isoflavone glycosides instead of soy isoflavone.

Example 6
Powder
Curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
Lactose 800mg
Corn starch
Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, powder was prepared using soy isoflavone glycosides instead of soy isoflavone.

Example 7
Granule curcumin 30mg
Cholic acid 150mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
Lactose 1500mg
Corn starch appropriate amount Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, granules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 8
Granule curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
Lactose 1500mg
Corn starch appropriate amount Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, granules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 9
Drink curcumin 30mg
Cholic acid 150mg
Soy isoflavone 125mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
100mg refined fish oil containing 27% docosahexaenoic acid
Ginseng extract 10mg
Giant extract 10mg
Royal Jelly 100mg
Thiamine nitrate 10mg
Riboflavin sodium phosphate 5mg
Pyridoxine hydrochloride 10mg
Anhydrous caffeine 50mg
Ethanol 1.2mL
Ethyl paraoxybenzoate 4mg
Purified water
Total 50 mL bottle Similarly, a drink was prepared using soy isoflavone glycoside instead of soy isoflavone.

Example 10
Drink curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 125mg
Green mussel powder 80mg
Inosinic acid 300mg
Heptadecanoic acid 90mg
100mg refined fish oil containing 27% docosahexaenoic acid
Thiamine nitrate 10mg
Ginseng extract 10mg
Giant extract 10mg
Royal Jelly 100mg
Riboflavin sodium phosphate 5mg
Pyridoxine hydrochloride 10mg
Anhydrous caffeine 50mg
Ethanol 1.2mL
Ethyl paraoxybenzoate 4mg
Purified water
Total 50 mL bottle Similarly, a drink was prepared using soy isoflavone glycoside instead of soy isoflavone.

Example 11
Soft capsule cholic acid 100mg
Soy isoflavone (40% product) 100mg
Curcumin 30mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
100mg refined fish oil containing 27% docosahexaenoic acid
Vitamin E (containing 50% or more total tocopherol) 2mg
Beeswax 205mg
Cod liver oil appropriate amount content weight 1960mg
(1 capsule 275mg once 3 capsules 2 times a day)
Similarly, soft capsules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 12
Soft capsule Simnol sulfate Na 2mg
Soy isoflavone (40% product) 100mg
Curcumin 30mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
100mg refined fish oil containing 27% docosahexaenoic acid
Vitamin E (containing 50% or more total tocopherol) 2mg
Beeswax 205mg
Cod oil suitable content weight 1960mg
(1 capsule 275mg once 3 capsules 2 times a day)
Similarly, soft capsules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 13
Tablet curcumin 30mg
Cholic acid 100mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
Lactose 140mg
Magnesium stearate 6mg
Talc 3mg
Crystalline cellulose appropriate amount total 1120mg
(1 tablet, 280 mg, 2 tablets, 2 times a day)
Similarly, tablets were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 14
Tablet curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
Lactose 140mg
Magnesium stearate 6mg
Talc 3mg
Crystalline cellulose appropriate amount total 1120mg
(1 tablet, 280 mg, 2 tablets, 2 times a day)
Similarly, tablets were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 15
Powder
Curcumin 30mg
Cholic acid 100mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
Lactose 800mg
Corn starch
Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, powder was prepared using soy isoflavone glycosides instead of soy isoflavone.

Example 16
Powder
Curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
Lactose 800mg
Corn starch
Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, powder was prepared using soy isoflavone glycosides instead of soy isoflavone.

Example 17
Granule curcumin 30mg
Cholic acid 100mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
Lactose 1500mg
Corn starch appropriate amount Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, granules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 18
Granule curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 100mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
Lactose 1500mg
Corn starch appropriate amount Magnesium stearate 10mg
Total 2000mg
(1 bag 1g twice a day)
Similarly, granules were produced using soy isoflavone glycosides instead of soy isoflavones.

Example 19
Drink curcumin 30mg
Cholic acid 100mg
Soy isoflavone 125mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
100mg refined fish oil containing 27% docosahexaenoic acid
Ginseng extract 10mg
Giant extract 10mg
Royal Jelly 100mg
Thiamine nitrate 10mg
Riboflavin sodium phosphate 5mg
Pyridoxine hydrochloride 10mg
Anhydrous caffeine 50mg
Ethanol 1.2mL
Ethyl paraoxybenzoate 4mg
Purified water
Total 50 mL bottle Similarly, a drink was prepared using soy isoflavone glycoside instead of soy isoflavone.

Example 20
Drink curcumin 30mg
Simanol sulfate Na 2mg
Soy isoflavone 125mg
Green mussel powder 80mg
Inosinic acid 100mg
Heptadecanoic acid 30mg
100mg refined fish oil containing 27% docosahexaenoic acid
Thiamine nitrate 10mg
Ginseng extract 10mg
Giant extract 10mg
Royal Jelly 100mg
Riboflavin sodium phosphate 5mg
Pyridoxine hydrochloride 10mg
Anhydrous caffeine 50mg
Ethanol 1.2mL
Ethyl paraoxybenzoate 4mg
Purified water
Total 50 mL bottle Similarly, a drink was prepared using soy isoflavone glycoside instead of soy isoflavone.

  The present invention provides an excellent anti-autoimmunity comprising isoflavones and / or isoflavone glycosides, pungent substances, bitter substances or sour substances, green mussels, and cholic acid, and / or simanol and / or simanol esters A disease agent, particularly an anti-rheumatoid arthritis agent and an anti-hay fever agent are provided.

Claims (13)

An anti-autoimmune disease agent comprising isoflavone and / or isoflavone glycoside, pungent substance, bitter substance or sour substance, green mussel, and cholic acid, and / or simanol and / or simanol ester . The anti-autoimmune disease agent according to claim 1, wherein the isoflavone and the isoflavone glycoside are soybean isoflavone and soybean isoflavone glycoside. The anti-autoimmune disease agent according to claim 1 or 2, wherein the pungent substance, bitter substance or sour substance is a food. The anti-autoimmune disease agent according to any one of claims 1 to 3, wherein the pungent substance, the bitter substance or the sour substance is a pungent substance. The anti-autoimmune disease agent according to any one of claims 1 to 4, wherein the pungent substance is curcumin. A vitamin agent is added, The anti-autoimmune disease agent in any one of Claims 1-5 characterized by the above-mentioned. A herbal medicine is added, The anti-autoimmune disease agent in any one of Claims 1-6 characterized by the above-mentioned. 8. The anti-autoimmune disease agent according to claim 7, wherein the crude drug has a corrective effect. Herbal medicines are Aki, Ginseng, Ginseng, Taishin, Taijin, Western ginseng, Ogi, Biakujutsu, Sanyaku, Licorice The anti-autoimmune disease agent according to claim 8, wherein the anti-autoimmune disease agent is at least one selected from the group consisting of 1), Daiso, Koi, yellow spirit, and Yohyo. The herbal medicine is one or more of hawthorn, Shinki, life comb, malt (Bakuga), cereal (Kokuga), chicken inner gold (Kainaikin), and Aki (Agi). The anti-autoimmune disease agent described in 1. Inosinic acid is added, The anti-autoimmune disease agent in any one of Claims 1-10 characterized by the above-mentioned. An odd-numbered fatty acid is added, The anti-autoimmune disease agent in any one of Claims 1-11 characterized by the above-mentioned. Docosahexaenoic acid is added, The anti-autoimmune disease agent in any one of Claims 1-12 characterized by the above-mentioned.