JP6985328B2 - Metabolism activator - Google Patents

Description

The present invention relates to a method for efficiently activating the metabolism of lipids and sugars, and a metabolic activator.

Salacia oblonga (Salacia oblonga), Salacia reticulata (Salacia reticulata), Salacia chinensis (Salacia chinensis (same species as Salacia prinoides)) It is a vine perennial plant of the family Salacia oblonga that grows in southern areas. These Salacia plants have been used as natural drugs in traditional medicine in India, Sri Lanka, and Southeast Asian countries, and in recent years, extracts of these plants have medicinal properties such as hypoglycemic action and lipase inhibitory action. (Patent Documents 1 to 5).

For effective obesity elimination, it is said that it is effective to make the metabolism of lipids dominant when exercising. In addition, lifestyle-related diseases and cardiovascular diseases caused by overnutrition and lack of exercise are deeply related to hyperglycemia and dyslipidemia. It has been reported that plant-derived components and plant extracts have a lipid metabolism promoting action (Patent Documents 6 to 8).

Japanese Unexamined Patent Publication No. 9-301882 Japanese Unexamined Patent Publication No. 11-1164946 Japanese Unexamined Patent Publication No. 11-29472 Japanese Unexamined Patent Publication No. 2001-261569 Japanese Unexamined Patent Publication No. 2005-8572 Japanese Unexamined Patent Publication No. 2004-161616 Japanese Unexamined Patent Publication No. 2005-232145 Japanese Unexamined Patent Publication No. 2007-297343

It is an object of the present invention to provide an effective, safe and continuously ingestible metabolic activator, particularly lipid and carbohydrate metabolic activators.

The present inventor has carried out diligent research to solve the above-mentioned problems, and found a good lipid and sugar metabolism activating effect in an extract of a plant belonging to the genus Salacia, and completed the present invention.
According to one aspect of the invention, there is provided a metabolic activator comprising an extract of a plant selected from Salacia chinensis, Salacia reticulata and Salacia oblonga as an active ingredient. In one embodiment of the invention, the metabolic activator of the invention activates lipid metabolism and / or glucose metabolism.

As the Salacia plant used as an extraction raw material, for example, a stem, root, leaf, or a cut or crushed bark of the stem and root can be used, which has been dried after collection.
Extraction can be carried out by appropriately using a conventional method, and for example, continuous extraction, immersion extraction, countercurrent extraction, supercritical extraction and the like may be used.

The extraction solvent is not particularly limited, but it is preferable to use a hydrophilic solvent such as water, lower alcohol (methanol and ethanol), acetone, or a mixed solvent thereof, and it is particularly preferable to use water. It is preferable to heat at the time of extraction, and for example, extraction can be performed at the reflux temperature of the extraction solvent. When water is used as a solvent, extraction can be carried out at a temperature of, for example, 60 to 110 ° C., preferably 80 to 98 ° C., for example, for an extraction time of 1 to 24 hours, preferably 1 to 4 hours.

As the extract used in the present invention, an undiluted solution of an extract, a concentrate of an extract, or a solid obtained by drying an extract concentrate can be used, and the solidified concentrate can be used from the viewpoint of efficiency of ingestion. It is preferable to use. As a method for concentrating the extract, the prior art can be appropriately used, and for example, a vacuum drying method, a freeze drying method, a spray drying method and the like can be performed.

Extracts of Salacia plants may be subjected to purification treatment. Examples of the refining treatment include treatment with an adsorbent such as activated carbon and an ion adsorbent resin, and liquid-liquid countercurrent distribution treatment.
As the extract of the genus Salacia, a commercially available product may be used.

The intake amount of the metabolic activator of the present invention can be appropriately adjusted depending on the body type, age, physical condition, etc. of the subject. For example, for an adult weighing 60 kg, the extract of the genus Salacia is applied at a dose of 300 mg / day or more, preferably 450 mg / day or more, more preferably 900 mg / day or more, and for example, 3000 mg / day or less, preferably 2400 mg. It can be administered at a dose of / day or less, more preferably 1800 mg / day or less.

The metabolic activator of the present invention can be provided as a pharmaceutical product with some processing or as it is. According to another aspect of the present invention, there is provided a pharmaceutical composition comprising a metabolic activator comprising an extract of a plant selected from Salacia kinensis, Salacia reticulata and Salacia oblonga as an active ingredient.

The metabolic activator of the present invention is a food (health food (nutritional functional food, food for specified health use, supplement, etc.), food for the sick, etc.) or beverage (tea, refreshing beverage, etc.) with some processing or as it is. ) Can be used. Therefore, according to yet another aspect of the present invention, there is provided a food or drink containing a metabolic activator containing an extract of a plant selected from Salacia kinensis, Salacia reticulata and Salacia oblonga as an active ingredient. To.

According to yet another aspect of the present invention, there is provided an oral ingestion composition comprising a metabolic activator comprising an extract of a plant selected from Salacia kinensis, Salacia reticulata and Salacia oblonga as an active ingredient. Will be done. The compositions for oral ingestion of the present invention include the pharmaceutical compositions and foods and drinks of the present invention as defined herein.

If necessary, the pharmaceutical composition and food and drink can be prepared by blending components such as conventionally known colorants, preservatives, flavors, flavoring agents, and coating agents.
In addition, the pharmaceutical composition and food and drink of the present invention may be prepared by blending one or more additional components. Examples of additional ingredients include antioxidants, hypoglycemic agents, anticholesterol agents, immunostimulators, vitamins, amino acids, peptides, proteins, minerals (iron, zinc, magnesium, iodine, etc.), fatty acids (EPA, DHA, etc.) ) And so on.

Here, examples of the antioxidant are not particularly limited, but are dry yeast, glutathione, lipoic acid, quercetin, catechin, coenzyme Q10, enzogenol, proanthocyanidins, anthocyanidins, anthocyanins, carotins, lycopene, flavonoids, and lysa. Examples include veratrol, isoflavones, zinc, melatonin, and plant-derived components (eg, ginkgo leaves, moon peach leaves, hibiscus, or extracts thereof).

Examples of hypoglycemic agents include, but are not limited to, indigestible dextrin, α-linolenic acid, bean drum extract, wheat albumin, L-arabinose, and plant-derived components (eg, guava leaves, mulberry leaves, ginger, etc.). Jiaogulan, barley, kidachi aloe, dandelion, daidai, dandelion, garlic, adlay, banaba, blueberry, black kohosh, makomo, morus alba, evening primrose, kaiapo, niggauri, madegurcil or extracts thereof).

Examples of anticholesterol agents are not particularly limited, but are limited to soybean protein, phospholipid-binding soybean peptide, chitosan, plant sterol, plant sterol ester, plant stanol ester, refractory dextrin, sodium alginate, psyllium seed coat, astaxanthin, and inositol. , Coenzyme A, calcium, magnesium, carnitine, silk protein, taurine, methionine, α-linolenic acid, guagam, chondroitin sulfate, soy saponin, and plant-derived ingredients (eg, amachadul, alfalfa, ginkgo, oyster, barley, oat, Olives, gajutsu, gymnema, cat's claw, cuco, chlorella, spirulina, western saponin, chili, garlic, bilberry, benibana, yukka, rafuma, agarix, red koji, or extracts thereof).

Examples of immunostimulators are, but are not limited to, lactoferrin, arginine, tryptophan, valine, leucine, chitin, chitosan, and plant-derived components (eg, agarix, winter worm, aloe, kidachi aloe, echinacea, ougi, cat's claw, etc. Kuco, spirulina, honeybee, red flower, maca, macomo, rafuma, or an extract thereof) and the like.

Examples of vitamins are not particularly limited, but vitamins belonging to the vitamin A group [eg, retinal, retinol, retinoic acid, carotene, dehydroretinal, lycopene and their pharmacologically acceptable salts (eg, retinol acetate). , Etc.), Vitamin B group [eg thiamine, thiamine disulfide, disetiamine, octothiamine, sicothiamine, bisibuchiamine, bisbenchamine, prosultiamine, benfothamine, flusulfiamine, Riboflavin, flavinadenine dinucleotide, pyridoxin, pyridoxal, hydroxocobalamine, cyanocobalamine, methylcobalamine, deoxyadenocobalamine, folic acid, tetrahydrofolic acid, dihydrofolic acid, nicotinic acid, nicotinic acid amide, nicotinic alcohol, pantothenic acid, pantenol, biotin, Colin, inositol, pangamic acid and their pharmacologically acceptable salts (eg thiamine hydrochloride, thiamine nitrate, disetiamine hydrochloride, flusultiamine hydrochloride, riboflavine butyrate, flavin adenindinucleotide sodium, pyridoxin hydrochloride, pyridoxal phosphate, Pyridoxal calcium phosphate, hydroxocobalamine hydrochloride, hydroxocobalamine acetate, calcium pantothenate, sodium pantothenate, etc.)], vitamins belonging to the vitamin C group [ascorbic acid and its derivatives, erythorbic acid and its derivatives, and pharmacologically acceptable These salts (eg, sodium ascorbate, sodium erythorbate, etc.)], vitamins belonging to the vitamin D group [eg, ergocalciferol, cholecalciferol, hydroxycholecalciferol, dihydroxycholecalciferol, dihydrotaxosterol , And their pharmacologically acceptable salts, etc.], vitamins belonging to the Vitamin E group [eg, tocopherols and derivatives thereof, ubiquinone derivatives and their pharmacologically acceptable salts (tocopherol acetate, tocopherol nicotinate, etc.) Tocopherol succinate, tocopherol succinate, calcium, etc.)], other vitamins [eg, carnitine, ferulic acid, γ-orizanol, orotic acid, rutin (vitamin P), eriocitrin, hesperidin, and pharmacologically acceptable Those salts (such as carnitine chloride) Do] and so on.

Examples of amino acids are not particularly limited, but leucine, isoleucine, valine, methionine, threonine, alanine, phenylalanine, tryptophan, lysine, glycine, aspartic acid, aspartic acid, serine, glutamine, glutamic acid, proline, tyrosine, cysteine and histidine. , Ornithine, hydroxyproline, hydroxylysine, glycine glycine, aminoethylsulfonic acid (taurine), cystine, or their pharmacologically acceptable salts (eg, potassium aspartate, magnesium aspartate, cysteine hydrochloride, etc.) Can be mentioned. Preferred examples are branched chain amino acids such as valine, leucine and isoleucine, glutathione, cysteine, glutamate, glycine, serine, tryptophan, tyrosine, phenylalanine, histidine, methionine, threonine, lysine, cystine, arginine, alanine, aspartic acid, proline, Aminoethyl sulfonic acid.

The metabolic activator of the present invention is, for example, a granule (including dry syrup) or a capsule so that it can be easily taken continuously as a pharmaceutical composition or a food or drink (particularly, a functional food, a health food, a supplement, etc.). (Soft capsules, hard capsules), tablets (including chewables), powders (powder), various solid formulations such as pills, or liquids for internal use (including liquids, suspensions, syrups) It can be prepared in the form of a liquid preparation such as, and is preferably in the form of a capsule or tablet from the viewpoint of stability of ingredients and convenience of ingestion, but is not particularly limited.

The metabolic activator of the present invention in the form of capsules or tablets can be produced using known additives that are acceptable as pharmaceuticals or foods, and are conventional formulations adopted in the field of pharmaceuticals or foods. The technique can be applied. For example, tablets can be prepared by adding and blending each component according to a formulation, pulverizing, granulating, drying, sizing and mixing, and tableting the obtained preparation mixture.

Additives for formulation include, but are not limited to, excipients, lubricants, binders, disintegrants, fluidizers, dispersants, wetting agents, preservatives, thickeners, pH adjustments. Examples thereof include agents, colorants, flavoring agents, surfactants, and solubilizing agents. Further, in the form of a liquid preparation, a thickener such as pectin, xanthan gum, or guar gum can be blended. Further, a coating agent can be used to make a coated tablet or a paste-like glue. Further, even when the preparation is made into another form, the conventional method may be followed.

Further, the metabolic activator of the present invention is used, for example, as various foods and drinks such as beverages, confectionery, breads and soups or as an additive component thereof; or as various pet foods such as dog food and cat food or an additive component thereof. be able to. The method for producing these foods and drinks is not particularly limited as long as it does not impair the effects of the present invention, and the methods used by those skilled in the art for each use may be followed.

The metabolism activator of the present invention has an excellent metabolism activating effect. The metabolic activator of the present invention is highly safe and suitable for continuous ingestion.

Hereinafter, preferred embodiments of the present invention will be described in more detail, but the present invention is not limited to these examples. In addition, the percentage shown in this specification means% by weight unless otherwise specified.

The Salacia kinensis water extract used in the test was prepared by the following method. Hot water (20 kg) was added to a chip (1 kg) obtained by cutting the trunk of Salacia kinensis into 5 mm squares, and the mixture was stirred and extracted at 98 ° C. for 120 minutes. The obtained extract is concentrated under reduced pressure using a rotary evaporator (concentration temperature 45 ° C., until Brix = 30), and the concentrate is freeze-dried to obtain the Saracia kinensis extract (98.5 g) of the present invention. Obtained.

The Salacia oblonga water extract used in the test was prepared in the same manner as the Salacia Kinensis water extract. That is, hot water (20 kg) was added to a chip (1 kg) obtained by cutting the trunk portion of Salacia oblonga into 5 mm squares, and the mixture was stirred and extracted at 98 ° C. for 120 minutes. The obtained extract is concentrated under reduced pressure using a rotary evaporator (concentration temperature 45 ° C., until Brix = 30), and the concentrate is freeze-dried to obtain the Saracia oblonga extract (97.0 g) of the present invention. Obtained.

"Salacia reticulata extract powder" (manufactured by Mona Co., Ltd.) was used as the Salacia reticulata water extract. Further, as a comparative example, Sanphenon 100S (manufactured by Taiyo Kagaku Co., Ltd.), which is a tea extract, was used.
[Test Example 1]
Capsules containing water extracts of Salacia kinensis, Salacia reticulata and Salacia oblonga (300 mg each) were prepared according to conventional methods. Three groups of subjects (n = 7) divided into four groups took each capsule three times a day after each meal and continued it for one week. Subjects in the placebo group were administered capsules containing crystalline cellulose (trade name: Theoras PH-101, manufactured by Asahi Kasei Chemicals, 300 mg).

Before the start of administration and after 1 week, each subject was subjected to a measurement test of lipid metabolism and carbohydrate metabolism by exercise. Walk at 4 km / h for 30 minutes, measure the lipid metabolism and sugar metabolism for 30 minutes with a respiratory metabolism measuring device (VO2000, manufactured by Medical Graphics Corporation) (unit: Kcal), and increase the measured value before ingestion. The proportion of the amount (%) was calculated. The results are shown in Tables 1 and 2.

From this test example, it was confirmed that ingestion of Salacia extract activates the metabolism of lipids and sugars. In particular, it was confirmed that the metabolic activation effect of the Salacia plant extract on lipids was remarkable, and the amount of increase in metabolism was 60 to 97 times that of placebo.
[Test Example 2]
Capsules containing 150 mg, 300 mg, 450 mg and 600 mg of water extract of Saracia kinensis were prepared and divided into 6 groups including a placebo group (crystalline cellulose, 300 mg) and a tea extract (Sanphenon 100S, 300 mg) (n). = 7) was administered in the same manner as in Test Example 1. Before the start of administration and after 1 week, each subject was subjected to a measurement test of lipid metabolism and carbohydrate metabolism by exercise in the same manner as in Test Example 1. The results are shown in Tables 3 and 4.

From this test example, it was confirmed that ingestion of Salacia kinensis extract activates the metabolism of lipids and sugars. It was also confirmed that the metabolic activation effect of Salacia kinensis extract was particularly remarkable for lipids.

Claims (5)

A lipid metabolism activator comprising a hot water extract of Saracia kinensis as an active ingredient, and the extract is used so as to be ingested in an amount of 300 mg or more per day. The lipid metabolism activator according to claim 1, wherein the extract is used so as to be ingested in an amount such that the daily intake is 450 mg or more. The lipid metabolism activator according to claim 1 or 2, wherein the extract is used so as to be ingested in an amount such that the daily intake is 2400 mg or less. To any one of claims 1 to 3 comprising a lipid metabolism activator described, the active lipid metabolism
A pharmaceutical composition used to make it. To any one of claims 1 to 4 comprising a lipid metabolism activator described, the active lipid metabolism
Food and drink used to make it.