JP6369931B2 - Anti-obesity agent - Google Patents

Description

The present invention relates to an anti-obesity agent containing an extract obtained by extracting a mixture of North American ginseng, Yamakiko, Mulberry leaves, Satoshi Konne, Takeshi Fuji, Car Maeko, and licorice with a polar solvent.

Obesity causes various diseases such as lifestyle-related diseases, and it is necessary to prevent and improve obesity in order to lead a healthy life. In recent years, attempts have been made to reduce the risk of lifestyle-related diseases by introducing the concept of metabolic syndrome. In addition, there are many people who want to lose weight in order to maintain health and beauty even if they are not obese.

Conventionally, a herbal medicine used as a raw material for traditional Chinese medicine has been used as an anti-obesity agent for suppressing, eliminating or improving obesity. For example, a diet food containing a mushroom chlorella extract and a plant fermented product obtained by fermenting ginseng, etc. (see prior document 1), mulberry leaf extract, gymnema extract, garnicia extract, and metabolic syndrome containing soybean saponin A food composition comprising a preventive / therapeutic agent (see Prior Literature 2), a processed product of Tochu tea, and a metabolic syndrome improving agent (See Prior Literature 3), capsinoids, gymnema, mulberry leaf, guava leaf, etc. (See Prior Literature 4), Preadipocyte differentiation inhibitor (see Prior Literature 5) and the like, including Kawaratake, Kanokoso, Gymnema Sylvestre, and the like are known.

JP2012-085591A JP 2010-030950 A JP 2007-230969 A JP 2006-212020 A Japanese Patent Application Laid-Open No. 2004-075640

The present invention provides an anti-obesity agent having a remarkable anti-obesity effect and preventing / ameliorating obesity based on a combination of herbal medicines and an active ingredient extraction method. Furthermore, a weight gain inhibitor, a functional food having a diet effect, a neutral fat lowering agent, a metabolic syndrome preventive / ameliorating agent, and the like are provided.

The present invention is an anti-obesity agent containing an extract obtained by extracting a mixture of North American ginseng, Yamako, Mulberry leaves, Koei Hideki, Takeshi-to, Carmae and licorice with a polar solvent.

In another embodiment of the present invention, the polar solvent is water.

Yet another aspect of the present invention is an anti-obesity agent used to be administered to a person who has been stimulated to the gastric point of the auricle.

Yet another invention is an antiobesity agent used such that a mixture of about 15 mg / kg body weight to about 50 mg / kg body weight per day is administered for more than 4 weeks.

In another aspect of the present invention, the polar solvent is water or ethanol, acetic acid or a mixture thereof.

In another aspect of the present invention, the extraction temperature in the extraction is in the range from room temperature to the boiling point of the solvent under normal pressure or increased pressure.

Yet another aspect of the invention is in the form of a powder formulation, granule, tablet, pill, capsule, or liquid formulation.

The present invention also provides a non-therapeutic dieting method characterized by administering an anti-obesity agent, and administering the anti-obesity agent to a person who has been stimulated to the stomach point of the auricle. A non-therapeutic diet method is provided.

By the anti-obesity agent of the present invention, obesity can be suppressed, eliminated, or improved. Further, the anti-obesity agent of the present invention used so as to be administered to a person who has been stimulated to the stomach point of the auricle can obtain a more remarkable effect. In addition, effects such as suppression of weight gain, diet, triglyceride lowering, prevention and improvement of metabolic syndrome can be obtained.

It is the figure which showed the anti-obesity effect by the anti-obesity agent of this invention. It is the figure which showed the anti-obesity effect by the anti-obesity agent of this invention.

The present invention is an anti-obesity agent containing an extract obtained by extracting a mixture of North American ginseng, Yamako, Mulberry leaves, Koei Hideki, Takeshi-to, Carmae and licorice with a polar solvent. Hereinafter, embodiments for carrying out the present invention will be described in detail.

The North American ginseng, Yamasuko, Mulberry leaves, Satoshi Koei, Takeshi Fuji, Kamaeko, and licorice used in the present invention are called herbal medicines, and each has a unique medicinal effect.

North American ginseng (Hanabein ginseng, scientific name: Panax quinquefolium) is also called American ginseng, flower flag ginseng, Western ginseng, Cantonese ginseng, and leaves or roots are cut or shredded, crushed and crushed as they are or dried. A powdered product is preferably used. The present inventors have recognized an effect of lowering lipids in blood and an effect of lowering blood glucose level and blood pressure.

A hawthorn is a fake flower of a deciduous shrub of the Rosaceae family, and hawthorn or its related species can be used. Specific examples include hawthorn (scientific name: Crataegus cuneata), sea hawthorn (scientific name: Crataegus pinnatifida Bge), and hawthorn (scientific name: Crataegus oxyacantha). These fake flowers can be used either directly or in a dry state. Cut, crossed, cut, crushed, pulverized, or powdered is preferably used.

Mulberry leaves are the leaves of mulberry (scientific name: Mourus), which is a deciduous tree, and those that have been cut vertically, crossed, cut, crushed, crushed, or powdered as they are or in a dry state are preferably used. It is done. Specific examples of mulberries include logwa (scientific name: Mourus lhou), yamaguwa (scientific name: Mourus bombycis), nagamiguwa (scientific name: Mourus laevigata), kegwa (scientific name: Mourus tiliaefolia), and ogasawa ragwa (scientific name: Mourus boninensis). ), Tenguguwa (scientific name: Mourus serrata), Red Mulberry (scientific name: Morus rubra), Karaya Magwa (scientific name: Morus alba), White Mulberry (scientific name: Morus alba), Black Mulberry (scientific name: Morus nigra), Black Mulberry (scientific name: Morus) mesozygia).

The root of the genus Dandelion (Scientific name: Taraxacum) is the root of the asteraceae (Taraxacum), and it is preferably used as it is or in a dry state, vertically cut, crossed, cut, crushed, crushed, or powdered. It is done. As dandelions, Mako dandelion (scientific name: Taraxacum mongolicum), Sina dandelion (scientific name: Taraxacum platypecidum), Keirin dandelion (scientific name: Taraxacum coreanum), Kantou dandelion (scientific name: taxacar um) , Shinano Dandelion (scientific name: Taraxacum platycarpum subsp. Hondoense), Kansai Dandelion (scientific name: Taraxacum japonicum), Japanese dandelion (scientific name: Taraxacum officinale), etc.

Wisteria wisteria (Bukatou, scientific name: Gymnema sylvestre R.), also called Gymnema, is a creeping plant belonging to the genus Musca. As the martial arts, those obtained by longitudinally cutting, crossing, cutting, crushing, crushing, or pulverizing the leaves as they are or in a dried state are preferably used.

Shazenshi refers to the perennials of the genus Psyllium, Psyllium (Scientific name: Plantago asiatica), Psyllium (Scientific name: Plantago asiatica), psyllium (Scientific name: Plantago lanceolata), etc. Alternatively, it is preferable to use a product that has been dried, vertically cut, crossed, cut, crushed, pulverized, or powdered.

Licorice is a licorice (Glycyrrhiza uralensis Fisch) or licorice (Glycyrrhiza glabra Linne (Leguminosae)) roots and stronts, or their pericarps removed (cutting licorice) as it is or dried. What was done can be used preferably.

Furthermore, the present invention may include bitter leaves, gold-silver flowers (honeysuckle), and buds (aloe) as herbal medicines. In other words, the present invention is selected from the group consisting of ginseng leaves, gold and silver flowers, and persimmons, in addition to North American ginseng, yamako, mulberry leaves, konne hidene, samurai, car maiko, and licorice. The anti-obesity agent containing the extract obtained by extracting the mixture containing 1 or more by a polar solvent.

The extract used in the present invention is the above-described herbal medicine (preferably dried herbal medicine) as it is or after being cut, chopped, crushed (preferably cut, chopped, crushed around several mm to 1 cm), or crushed. Alternatively, it can be obtained by extracting from a mixture in which powders are mixed with an extraction solvent.

In the mixture of the present invention, each herbal medicine is blended in dry weight as 30 mg to 9 g parts by weight of ginseng, 30 mg to 9 g parts by weight of Yamaniko, 30 mg to 9 g parts by weight of mulberry leaves, 30 mg to 9 g parts by weight of Koei Ei, 30 mg of Takeuchi. -9 g parts by weight, 30 mg to 9 g parts by weight of a carrot, and 30 mg to 9 g parts by weight of licorice, preferably 1 g to 9 g parts by weight of ginseng (1,2,3,4,5,6, 7,8,9 g parts by weight), Yamagiko 1 g-9 g parts by weight (1,2,3,4,5,6,7,8,9 g parts by weight, mulberry leaves 1 g-9 g parts by weight (1,2,3, 4,5,6,7,8,9g parts by weight, 1g to 9g parts by weight (1,2,3,4,5,6,7,8,9g parts by weight), 1 g to 9g parts by weight Parts (1,2,3,4,5,6,7,8,9 g parts by weight, 1 g to 9 g parts by weight (1,2, 4,5,6,6,7,8,9 g parts by weight, licorice 1 g-9 g parts by weight (1,2,3,4,5,6,7,8,9 g parts by weight) Further preferred.

In the present invention, the solvent used for the extraction is preferably a pharmaceutically or food hygienically acceptable polar solvent. Examples of the polar solvent include water (eg, purified water, distilled water, tap water), ethanol, a mixed solvent of water and ethanol (hydrous ethanol), acetic acid or a mixed solvent of acetic acid and water, water, ethanol and acetic acid, and the like. And the like. Water or water-containing ethanol is preferred. The water content in hydrous ethanol is 1 to 99% by volume. An acid may be added to water or hydrous ethanol. Preferred examples of the acid include inorganic acids such as hydrochloric acid, and organic acids such as malic acid and citric acid.

The extraction method is not particularly limited, and an immersion method or a countercurrent extraction method can be employed. Moreover, it can extract by heating in the range to the boiling point of a solvent under normal temperature extraction or a normal pressure, and you may extract under pressure reduction or pressurization as needed. The pressurization may be a pressure exceeding 1 atm, and preferably about 2 to 3 atm. For example, in a mixture of North American ginseng, yamako, mulberry leaves, sae konne, takeshifuji, car maiko, and licorice, the extraction solvent (polar solvent) is 10 to 100 times the amount of the herbal medicine mixture, preferably 10 to 40 Add a double amount, and usually immerse for 30 minutes to 5 hours, preferably 1 to 3 hours (1, 2, 3 hours) in the range from room temperature to normal pressure or under the boiling point of the solvent, and filter by a known method. By doing so, an extract can be obtained. The extract can be used as an extract as it is. Moreover, what concentrated the said extract, what concentrated and dried or freeze-dried can also be used as an extract.

The anti-obesity agent of the present invention can be taken orally by mixing the above-mentioned extract and a pharmaceutically or food hygienically acceptable carrier optionally blended by a known method. It can be prepared as a formulation or food. The food includes health foods, functional foods and supplements.

The formulation of the extract in the present invention can be, for example, a solid preparation or a liquid preparation. Examples of solid preparations include powder preparations, granules, tablets, pills or capsules. Granules and tablets may be coated with a sugar coating or a film coating agent. The liquid preparation is not limited as long as it is a liquid internal preparation, and includes, for example, emulsion, syrup, suspension, shaking mixture, limonase, elixir and the like.

As the pharmaceutically or food hygiene acceptable carrier in the present invention, various organic or inorganic carrier substances commonly used as pharmaceutical materials are used, and excipients, lubricants, binders, disintegrants in solid preparations; liquid preparations Solvents, solubilizers, suspending agents (emulsifiers, thickeners) and the like. If necessary, preparation additives such as preservatives, antioxidants, coloring agents, sweetening agents, and fragrances can be used.

Suitable examples of excipients include sugars or sugar alcohols such as lactose, corn starch, maltose, mannitol; starch or starch derivatives such as corn starch, dextrin, pregelatinized starch; celluloses such as crystalline cellulose and hydroxypropyl cellulose And cellulose derivatives; light anhydrous silicic acid and the like. Preferable examples of the lubricant include magnesium stearate, calcium stearate, talc, colloidal silica and the like.

Examples of binders include crystalline cellulose, sucrose, mannitol, dextrin, hydroxypropylcellulose, hydroxypropylmethylcellulose, polyvinylpyrrolidone and the like. Examples of disintegrants include starch, carboxymethyl cellulose, carboxymethyl cellulose calcium, croscarmellose sodium, carboxymethyl starch sodium, and the like.

Examples of the solvent include water (tap water, purified water, distilled water, etc.), alcohol, propylene glycol, macrogol, sesame oil, corn oil and the like. Examples of the solubilizer include polyethylene glycol, propylene glycol, D-mannitol, benzyl benzoate, ethanol, trisaminomethane, cholesterol, triethanolamine, sodium carbonate, sodium citrate and the like.

Examples of suspending agents include surfactants such as stearyltriethanolamine, sodium lauryl sulfate, laurylaminopropionic acid, lecithin, benzalkonium chloride, benzethonium chloride, glyceryl monostearate, sucrose fatty acid ester; Hydrophilic polymers such as polyvinyl alcohol, polyvinyl pyrrolidone, sodium carboxymethyl cellulose, methyl cellulose, hydroxymethyl cellulose, hydroxyethyl cellulose, hydroxypropyl cellulose; xanthan gum, soybean saponin, dextran, pectin and the like.

Examples of preservatives include, for example, paraoxybenzoates (for example, isobutyl paraoxybenzoate, isopropyl paraoxybenzoate, methyl paraoxybenzoate, ethyl paraoxybenzoate, butyl paraoxybenzoate, propyl paraoxybenzoate, etc.), sulfurous acid [ Hydrogen] sodium, dehydroacetic acid, sorbic acid, potassium metabisulfite, sodium metabisulfite and the like.

Examples of antioxidants include sulfites (eg, sodium sulfite, sodium bisulfite, etc.), ascorbic acid, sodium ascorbate, erythorbic acid, sodium erythorbate, citric acid, enzyme-treated rutin, sodium hyposulfite, meta Examples include potassium bisulfite and sodium metabisulfite.

Examples of the colorant include, for example, Blue No. 1, Red No. 2, Red No. 40, Red No. 102, red cabbage, anthocyanin, caramel pigment, gardenia pigment and the like. Examples of sweetening agents include sucrose, licorice extract, xylitol, saccharin, stevia and the like. Examples of the fragrances include cinnamic acid, methyl salicylate, menthol and the like.

Furthermore, when the anti-obesity agent of the present invention is prepared as a food, it can be prepared in the same manner as in the preparation described above.

The content of the extract in the anti-obesity agent of the present invention is, for example, about 1% by weight to about 99% by weight, preferably about 5% by weight to about 90% by weight of the preparation as a dry extract in the case of a solid preparation. %, More preferably from about 10% to about 80% by weight. In the case of a liquid preparation, it is about 0.0001% to about 80% by weight, preferably about 0.001% to about 50% by weight, more preferably about 0.1% as a dry extract. % By weight to about 20% by weight. Moreover, the liquid formulation can also use the concentrate which concentrated the extract of the crude drug as it is. Preferably, 10 to 1000 times as much polar solvent (preferably water) is used as the mixture of crude drugs, and the extract extracted by heating for 1 to 3 hours (1, 2, 3 hours) is directly used as a liquid preparation. be able to.

The antiobesity agent of the present invention is preferably administered orally. Moreover, it is more preferable to take after meal, before meal or between meals. The dosage and frequency of administration of the anti-obesity agent of the present invention vary depending on age, body weight, dosage form and the like. For example, in the antiobesity agent of the present invention, the dry weight of the extract obtained by extracting from a mixture of a plurality of herbal medicines is usually about 1 mg to 500 mg, preferably about 5 mg to 300 mg per kg body weight per adult day. Is taken to be about 15 mg to 50 mg. Moreover, it is preferable to take this amount in 1 to several times, preferably 1 to 3 times. In the case of a liquid preparation, for example, a liquid containing an extract obtained by extracting a mixture of North American ginseng, yamako, mulberry leaves, sae konne, takeshifuji, kamaeko, and licorice with a polar solvent (preferably water). It is preferable to take the preparation, and it is preferable to divide the liquid preparation containing the daily dose of the extract into 1 to several times, preferably 1 to 3 times. The administration period is usually 4 weeks or longer, preferably 8 weeks or longer, and more preferably 12 weeks or longer.

The subject of administration (or ingestion) of the anti-obesity agent of the present invention is preferably human, but mammals such as mice, rats, rabbits, dogs, cats, cows, monkeys, pigs, birds such as chickens, red sea bream, yellowtail ( Hamachi), amberjack, puffer fish, flounder, eel, bluefin tuna and other fishes may be administered (or ingested).

Furthermore, another anti-obesity agent of the present invention is adjusted to be used for a person who has been stimulated to the stomach point of the auricle. The stomach point is also called a point reaction point and corresponds to the distribution region of the vagus nerve pinna. By stimulating the stomach point, the vagus nerve is given a suppressive stimulus, so appetite can be controlled. The anti-obesity effect of the anti-obesity agent of the present invention was remarkably recognized when taken by a person who received stimulation to the stomach point of the auricle. It is preferable to continuously give stimulation to the stomach point of the auricle, and it is more preferable to always give stimulation by wearing a clip or the like except at bedtime and bathing.

Furthermore, a non-therapeutic diet method characterized by administering the above-mentioned anti-obesity agent is provided. More preferably, the non-therapeutic diet method is such that the stomach point of the pinna of a person undergoing the non-therapeutic diet method is stimulated.

In the present invention, a mixture of ginseng, yamako, mulberry leaves, sae konne, takeshifuji, car maiko, and licorice is an anti-obesity agent, weight gain inhibitor, functional food with diet effect, neutral fat It can be used as a reducing agent, metabolic syndrome preventive / ameliorating agent, and the like.

Hereinafter, the present invention will be described in more detail through examples. However, the scope of the present invention is not limited to these examples.

[Preparation of anti-obesity agent]
Water was added to a mixture of North American ginseng, Yamasuko, Mulberry leaves, Koei Sakaki, Takeshi Fuji, Kamaeko, and licorice, followed by boiling extraction at 2-3 atm for 2 hours with a pressure extractor, followed by filtration. The obtained filtrate was packaged in an aluminum pack for each daily intake. Each herbal medicine used was obtained by cutting dry herbal medicine into several millimeters to about 1 cm. From 6 g of the crude drug mixture, 200 mL of a filtrate containing an extract corresponding to a dry weight of 1000 mg was obtained.

[Verification of anti-obesity action 1]
1. Test substance The anti-obesity agent packaged in the aluminum pack obtained in Example 1 was used as the test substance.
2. Subjects 23 healthy adult women who wanted to diet (average age: 32.3 ± 2.4 years, average weight: 56.1 ± 1.4 kg) were subjects.
3. Method The test subject took the test substance twice a day for 12 consecutive weeks. The daily test substance intake was 200 mL for subjects with a body weight of less than 53 kg, 240 mL for subjects with a weight of 53 kg or more and less than 60 kg, and 280 mL for subjects with a weight of 60 kg or more.

4). Results The change in body weight before and after ingestion is shown in FIG. The body weight, which averaged 56.1 kg before ingestion, decreased over time. After ingestion of the test substance for 12 weeks after ingestion, the average amount was 50.1 kg, and a remarkable anti-obesity effect of the test substance was observed.

[Verification of anti-obesity action 2]
1. Test substance The anti-obesity agent packaged in the aluminum pack obtained in Example 1 was used as the test substance.
2. Subjects 7 healthy adult women who wanted to diet (average age: 34.4 ± 4.4 years, average weight: 62.2 ± 1.9 kg) were subjects.
3. Method The test subject took the test substance twice a day for 12 consecutive weeks. The daily test substance intake was 200 mL for subjects with a body weight of less than 53 kg, 240 mL for subjects with a weight of 53 kg or more and less than 60 kg, and 280 mL for subjects with a weight of 60 kg or more.
Acupuncture-like pressure stimulation was applied to the stomach point of the auricle using a resin clip. Resin clips were always worn except during bedtime and bathing, and additionally, the clips were pinched about 10 times before each meal.

4). Results The change in body weight before and after ingestion is shown in FIG. The body weight, which was 62.2 kg on average before ingestion, averaged 53.9 kg after ingestion of the test substance for 12 weeks, and the anti-obesity effect of the test substance was observed. In particular, the test substance was shown to have a significant anti-obesity effect when ingested by a person who has been stimulated to the stomach point of the auricle. In addition, it was reported that some subjects had a significant reduction in blood triglyceride concentration, suggesting the possibility of reducing triglycerides.

Claims (7)

North American ginseng, hawthorn, mulberry leaves, a method of dandelion roots, Takekutsufuji, psyllium, and mixtures of licorice, obtaining the extract was extracted with a polar solvent, to produce an anti-obesity agent containing the extract The method for producing an anti-obesity agent according to claim 1, wherein the polar solvent is water. The method for producing an anti-obesity agent according to claim 1 or 2, wherein the anti-obesity agent is used to be administered to a person who has been stimulated to the stomach point of the auricle. The method for producing an antiobesity agent according to any one of claims 1 to 3, wherein the mixture of about 15 mg / kg body weight to about 50 mg / kg body weight per day is used so as to be administered for 4 weeks or more. The method for producing an antiobesity agent according to any one of claims 1 to 4, wherein the polar solvent is water, ethanol, acetic acid, or a mixture thereof. The method for producing an antiobesity agent according to any one of claims 1 to 5, wherein an extraction temperature in the extraction is in a range from normal temperature to normal pressure or a boiling point of the solvent under pressure. The method for producing an antiobesity agent according to any one of claims 1 to 6, wherein the antiobesity agent is in the form of a powder preparation, a granule, a tablet, a pill, a capsule, or a liquid preparation.