JP2011178690A - Salacia-containing composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a composition which includes a high content of an extract of a plant belonging to the genus Salacia to be used as a food or a drug, has high storage stability, and particularly inhibits the discoloration due to long-term storage and the extension of disintegration time. <P>SOLUTION: The composition includes an extract of a plant belonging to the genus Salacia, silicon dioxide, and carboxymethyl cellulose or a metal salt thereof. <P>COPYRIGHT: (C)2011,JPO&INPIT

Description

  The present invention relates to a composition containing a Salacia plant component, and particularly to a composition containing a Salacia plant component used as a food.

  Salacia oblonga (Salacia reticulata), Salacia chinensis; Salacia prinoides (same species as Salacia prinoides); It is a vine perennial plant that grows in the southern region. These Salacia plants have been used as natural drugs in traditional medicine in India, Sri Lanka, and Southeast Asian countries. In recent years, it has been reported that extracts of these plants have medicinal effects such as a preventive action against diabetes and obesity, a hypoglycemic action, and a lipase inhibitory action (Patent Documents 1 to 5 and Non-Patent Document 1). ).

  A composition or food for ingesting a plant component of the genus Salacia has been reported, focusing on various effects useful for health promotion or health maintenance of such a genus Salacia plant (Patent Documents 6 to 11).

Japanese Patent Laid-Open No. 9-301882 Japanese Patent Application Laid-Open No. 11-116496 JP-A-11-29472 Japanese Patent Laid-Open No. 2001-26169 JP 2005-8572 A JP 2010-11749 A JP 2010-70 A JP 2009-219370 A JP 2009-215276 A JP 2009-215275 A JP 2009-60792 A

Pharmacology and Treatment (JPT), 2008, 36, 1, 39-48

  When a Salacia plant component is used as a raw material for foods, pharmaceuticals, etc., a Salacia extract powder obtained by concentrating, drying and pulverizing an extract of a Salacia plant can be used. Extracts of Salacia plants such as Salacia extract powder contain various medicinal ingredients possessed by Salacia plants and can be preferably used as raw materials for health foods, functional foods and the like. However, Salacia plant extracts are easily oxidized, and foods containing Salacia plant extracts may undergo discoloration due to oxidation during storage. In addition, because Salacia extract powder has high hygroscopicity and has the property of increasing stickiness due to moisture absorption, foods containing Salacia extract powder are prone to quality degradation due to moisture absorption during storage. However, the problem is that the disintegration property of the tablet is lowered during storage. On the other hand, in order to efficiently ingest Salacia plant components, it is desired to develop foods and pharmaceuticals containing a high content of Salacia plant extracts.

  In addition, when silicon dioxide is added to the composition in order to prevent oxidation and moisture absorption of the extract of the plant belonging to the genus Salacia and increase the storage stability of the composition, it is also a problem that silicon dioxide lowers the binding property of the composition. Become. For example, when the composition is in the form of a tablet, there is a problem in that tablet hardness becomes insufficient when the content of silicon dioxide is increased in order to obtain sufficient storage stability.

  An object of the present invention is to provide a composition containing a Salacia plant extract used as a food or a medicine, which has high storage stability, and in particular, discoloration and prolonged disintegration time due to long-term storage are suppressed. That is. The composition is also suitable for making a tablet having sufficient binding properties and appropriate hardness.

  The present inventor made extensive research to solve the above problems, and as a result, a composition having a high degree of storage stability by blending a Salacia plant extract with carboxymethylcellulose or a metal salt thereof and silicon dioxide. The present invention was completed by finding that the product can be prepared.

  According to one aspect of the present invention, a composition comprising a Salacia plant extract, silicon dioxide, and carboxymethylcellulose or a metal salt thereof is provided. The composition may be in the form of, for example, a granule, a capsule, or a tablet.

According to a further aspect of the present invention, there is provided a tablet or granule comprising a Salacia plant extract, silicon dioxide, carboxymethylcellulose or a metal salt thereof.
According to another aspect of the present invention, a food product comprising a Salacia plant extract, silicon dioxide, carboxymethylcellulose or a metal salt thereof is provided. The composition may be in the form of, for example, a granule, a capsule, or a tablet.

  According to yet another aspect of the present invention, there is provided an orally ingestible composition comprising silicon dioxide together with a Salacia plant extract, carboxymethylcellulose or a metal salt thereof. The composition for oral intake of the present invention can be used as a medicine or food, and may be in the form of granules, capsules, tablets, or the like.

  The composition of the present invention containing a plant extract of the genus Salacia has high storage stability, in particular, discoloration and disintegration deterioration due to long-term storage are suppressed, and further has sufficient binding properties, thus having an appropriate hardness. It has the excellent property of being suitable for tablet production. The composition of the present invention is suitable for long-term storage, suitable for safe and continuous ingestion of Salacia plant components, and can be used as a food for ingestion particularly for the purpose of maintaining health or promoting health.

  Examples of Salacia plants used as an extraction raw material include Salacia plants such as Salacia chinensis, Salacia reticulata and Salacia oblonga, which are dried stems, roots, leaves, fruits or stems after collection. In addition, a material obtained by cutting or pulverizing a bark of a root portion can be used. Extraction can be performed by appropriately using a conventional method, and for example, it may be performed by a method such as continuous extraction, immersion extraction, countercurrent extraction, supercritical extraction, or column extraction.

  Although it does not specifically limit as an extraction solvent, It is preferable to use hydrophilic solvents, such as water, a lower alcohol (methanol and ethanol), acetone, or those mixed solvents, and it is preferable to use water especially. It is preferable to heat at the time of extraction, for example, extraction can be performed at the reflux temperature of the extraction solvent. When water is used as a solvent, the extraction can be performed at a temperature of 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 an extract used in the present invention, a solid obtained by drying an extract concentrate can be used. As a method for concentrating the extract, conventional techniques can be appropriately used. For example, a vacuum drying method, a freeze drying method, a spray drying method, or the like can be performed. In particular, the solidified concentrate and powdered powder can be used preferably in the present invention.

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

  The amount of the extract of the plant belonging to the genus Salacia contained in the composition of the present invention can be appropriately set from the viewpoint of the efficiency of intake and the characteristics required for each form of the composition. For example, the composition of the present invention may contain 50% by weight or less, preferably 40% by weight or less, particularly 35% by weight or less of a Salacia plant extract based on the whole composition. In addition, the composition of the present invention may contain, for example, 5% by weight or more, preferably 10% by weight or more, particularly 30% by weight or more of Salacia plant extract based on the whole composition. In one embodiment of the invention, the amount of Salacia plant extract is 5 to 50% by weight, preferably 10 to 40% by weight, in particular 30 to 35% by weight, based on the total composition. The intake amount of the plant extract of the genus Salacia by the composition of the present invention can be appropriately adjusted according to the body shape, age, physical condition, etc. of the subject. For example, for an adult weighing 60 kg, the extract of Salacia plant is administered at a dose of 150 mg / day or more, preferably 200 mg / day or more, more preferably 300 mg / day or more, and for example 3000 mg / day or less, preferably 2400 mg. / Day or less, more preferably 1800 mg / day or less.

  Examples of carboxymethyl cellulose or a metal salt thereof used in the present invention include carboxymethyl cellulose and its sodium salt, potassium salt and calcium salt, and mixtures thereof, and carboxymethyl cellulose and its metal salt may be used in combination. . In particular, carboxymethyl cellulose or carboxymethyl cellulose calcium can be preferably used, or it is also preferable to use both in combination. Carboxymethylcellulose or a metal salt thereof is not particularly limited as long as it can be used as a food additive or a pharmaceutical raw material. For example, the degree of etherification can be 0.45 to 1.0 (mol / C6). Specifically, NS-300 (manufactured by Nichirin Chemical Industry Co., Ltd.), E.I. C. G-505 (manufactured by Nichirin Chemical Co., Ltd.), E.I. C. G-FA (manufactured by Nichirin Chemical Industry Co., Ltd.) or the like can be used.

  The amount of carboxymethyl cellulose or a metal salt thereof contained in the composition of the present invention can be appropriately set. For example, the composition of the present invention contains 2.0% by weight or less, preferably 2.0% or less, particularly 1.8% by weight or less of carboxymethyl cellulose and / or a metal salt thereof based on the whole composition. Also good. Further, the composition of the present invention contains, for example, 0.5% by weight or more, preferably 1.0% by weight or more, particularly 1.5% by weight or more of carboxymethyl cellulose and / or a metal salt thereof based on the whole composition. You may contain. In one embodiment of the invention, the amount of carboxymethylcellulose and / or its metal salt is 0.1-2.0% by weight, preferably 0.5-2.0% by weight, in particular 1%, based on the total composition. 0.0 to 1.8% by weight.

  The silicon dioxide used in the present invention is not particularly limited as long as it is used as a food additive or a pharmaceutical additive. In one embodiment of the present invention, silicon dioxide having an average particle size of 15 μm or less can be used as silicon dioxide. Specifically, Aerosil 200, Aerosil 200FAD (registered trademark, manufactured by Nippon Aerosil Co., Ltd.), Carplex # 67, Carplex FPS-500 (Registered trademark, manufactured by DSL Japan Co., Ltd.) and the like can be used.

  The amount of silicon dioxide contained in the composition of the present invention can be appropriately set. For example, the composition of the present invention may contain less than 1% by weight of silicon dioxide, preferably 0.75% by weight or less, in particular 0.75% by weight or less, based on the total composition. Further, the composition of the present invention may contain, for example, 0.25% by weight or more, preferably 0.5% by weight or more, particularly 0.75% by weight or more of silicon dioxide based on the whole composition. In one embodiment of the invention, the amount of silicon dioxide is 0.25 to 0.75% by weight, preferably 0.5 to 0.75% by weight, in particular 0.75% by weight, based on the total composition. .

  If necessary, the composition of the present invention may be prepared by using conventionally known excipients (eg, lactose, sucrose, starch, crystalline cellulose, etc.), binders (eg, hydroxypropylcellulose, starch, sodium alginate, povidone, etc.), disintegration, and the like. Agents (eg, starch, agar, low substituted hydroxypropyl cellulose, etc.), lubricants (eg, magnesium stearate, calcium stearate, sucrose fatty acid ester, talc, etc.), colorants (eg, caramel, gardenia pigments, etc.) ), Preservatives (eg, L-ascorbic acid, etc.), fluidizing agents (eg, silicon dioxide, etc.), preservatives (eg, benzoic acid, etc.), pH adjusters (eg, potassium carbonate, sodium bicarbonate, etc.), Surfactant (for example, saponin, lecithin, sucrose fatty acid ester, etc.), coaty Grayed agents (e.g., shellac, hydroxypropyl cellulose) can also be prepared by blending the components, such as.

  The composition of the present invention is preferably prepared as a tablet. Tablets can be prepared by a method well known in the technical field to which the present invention belongs, for example, a compression molding method using a tableting machine. For tableting, the mixed components may be compressed as they are, or the mixed components may be subjected to a granulation step and the resulting granules may be compressed. In one embodiment, the tablet of the present invention can be prepared by adding and blending each component according to the formulation, mixing, granulating, drying, sizing and mixing, and tableting the resulting preparation mixture. . Moreover, you may make a coated tablet using a coating agent after shaping | molding of a tablet.

The composition of the present invention may be prepared as granules. Granules can be prepared by methods well known in the technical field to which the present invention belongs, for example, rolling granulation method, fluidized bed granulation method, compression granulation method, extrusion granulation method, stirring granulation method and the like. . The granule may be produced, for example, by wet granulation using bound water or dry granulation. Capsules can be prepared by filling the granules into capsules. The composition of the present invention may be prepared by blending one or more additional components. Examples of additional ingredients include hypoglycemic agents, anticholesterol agents, immunostimulants, antioxidants, vitamins, amino acids, peptides, proteins, minerals (iron, zinc, magnesium, iodine, etc.), fatty acids (EPA, DHA, etc.) ) And the like.

  Here, examples of the hypoglycemic agent are not particularly limited, but include indigestible dextrin, α-linolenic acid, bean extract, wheat albumin, L-arabinose, and plant-derived components (eg, guava leaf, mulberry leaf) , Ginger, sweet potato, barley, yellow aloe vera, dandelion, red daisies, daffodil, garlic, pearl barley, banaba, bilberry, black cohosh, makomo, chufu, evening primrose, caiapo, bitter gourd, madeglucil or extracts thereof).

  Examples of anticholesterol agents include, but are not limited to, soy protein, phospholipid-bound soy peptide, chitosan, plant sterol, plant sterol ester, plant stanol ester, resistant digestive dextrin, sodium alginate, psyllium seed coat, astaxanthin, inositol , Coenzyme A, calcium, magnesium, carnitine, silk protein, taurine, methionine, α-linolenic acid, guar gum, chondroitin sulfate, soy saponin, and plant-derived ingredients (eg, macaque, alfalfa, ginkgo, plantain, barley, oat, Olive, Gadju, Gymnema, Cat's Claw, Cuco, Chlorella, Spirulina, Hawthorn, Pepper, Garlic, Bilberry, Safflower, Yucca, Rahma, Agariku , Red yeast or extracts thereof) and the like.

  Examples of immunostimulants include, but are not limited to, lactoferrin, arginine, tryptophan, valine, leucine, chitin, chitosan, and plant-derived components (eg, Agaricus, Cordyceps, Aloe, Kidachi aloe, Echinacea, Ogi, Cats claw, Wolfberry, spirulina, pearl barley, safflower, maca, makomo, luffa, or an extract thereof).

  Examples of antioxidants include, but are not limited to, dry yeast, glutathione, lipoic acid, quercetin, catechin, coenzyme Q10, enzodinol, proanthocyanidins, anthocyanidins, anthocyanins, carotenes, lycopene, flavonoids, resaveratrol, Examples include isoflavones, zinc, melatonin, and plant-derived components (for example, ginkgo biloba, moon peach leaf, hibiscus, or an extract thereof).

  Examples of vitamins include, but are not limited to, vitamins belonging to the vitamin A group [eg, retinal, retinol, retinoic acid, carotene, dehydroretinal, lycopene, and pharmacologically acceptable salts thereof (eg, retinol acetate). , Retinol palmitate, etc.), vitamins belonging to vitamin B group [for example, thiamine, thiamine disulfide, dicetiamine, octothiamine, chicotiamine, bisbutiamine, bisbenchamine, prosultiamine, benfotiamine, fursultiamine, Riboflavin, flavin adenine dinucleotide, pyridoxine, pyridoxal, hydroxocobalamin, cyanocobalamin, methylcobalamin, deoxyadenocobalamin, folic acid, tetrahydrofolic acid, dihydrofolic acid, nicoti Acids, nicotinamide, nicotinic alcohol, pantothenic acid, panthenol, biotin, choline, inositol, pangaminic acid and their pharmaceutically acceptable salts (eg thiamine hydrochloride, thiamine nitrate, dicetiamine hydrochloride, fursulfuric acid hydrochloride) Thiamine, riboflavin butyrate, sodium flavin adenine dinucleotide, pyridoxine hydrochloride, pyridoxal phosphate, calcium pyridoxal phosphate, hydroxocobalamin hydrochloride, hydroxocobalamin 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 salts thereof (for example, sodium ascorbate, sodium erythorbate) Etc.], vitamins belonging to the vitamin D group (for example, ergocalciferol, cholecalciferol, hydroxycholecalciferol, dihydroxycholecalciferol, dihydrotaxosterol, and pharmacologically acceptable salts thereof), Vitamins belonging to the vitamin E group [for example, tocopherol and derivatives thereof, ubiquinone derivatives and pharmacologically acceptable salts thereof (such as tocopherol acetate, tocopherol nicotinate, tocopherol succinate, tocopherol calcium succinate, etc.), etc. Vitamins [eg carnitine, ferulic acid, γ-oryzanol, orotic acid, rutin (vitamin P), eriocitrin, hesperidin, and pharmacologically acceptable salts thereof (such as carnitine chloride). ] And the like.

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

  The present invention to be used as food or medicine can be produced using known additives acceptable for food or medicine, and the usual formulation method adopted in the field of food or medicine is applied. Can do.

  The composition of the present invention can be used as food (health food (nutrient functional food, food for specified health use, supplement, etc.), sick food, etc.) with some processing added or as it is. Moreover, when this invention is a foodstuff, this invention can be implemented with forms, such as a functional food, health food, food for specified health use, food for special uses, a supplement. According to a preferred embodiment of the present invention, in a food for specified health use or a food for special use containing an amount of a plant belonging to the genus Salacia or an extract thereof having a blood glucose level reducing action, a GLP-1 activity enhancing action, a diabetes preventing action, or a pancreatic protecting action A food and drink is offered. Here, description regarding the action effect (blood glucose level lowering action, GLP-1 activity enhancing action, diabetes preventing action, pancreas protecting action) may be attached to the packaging, package, package insert or advertisement of the food.

  EXAMPLES Hereinafter, although the preferable Example of this invention is described in detail, this invention is not limited to these Examples. In addition, the percentage shown in this specification means weight% unless there is particular mention.

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

  In addition, as other components, crystalline cellulose (Theolas FD301, manufactured by Asahi Kasei Chemicals Corporation), carboxymethylcellulose calcium (referred to as CMC-Ca, ECG-FA, manufactured by Nichirin Chemical Industries, Ltd.), silicon dioxide (Aerosil) 200 FAD, manufactured by Nippon Aerosil Co., Ltd.) and magnesium stearate (manufactured by Saneigen FFI Co., Ltd.) were used.

Using a hydraulic press machine (manufactured by Riken Seiki Co., Ltd.) and the corresponding mortar and pestle, each mixture of formulations shown in the following tables (Examples 1 to 12 and Comparative Examples 1 to 6) is pressure of 100 kg / cm ² . Was compressed to form tablets with a diameter of 9 mm and a weight of 320 mg.

  The tablets were sealed in an aluminum pouch, stored for 10 days at a temperature of 50 ° C. and a humidity of 60%, and the discoloration and disintegration time of the tablets were compared before and after storage. For the evaluation of discoloration, the discoloration was confirmed visually by comparison with a tablet that was light brown immediately after production. As for the evaluation criteria, ◎ when no discoloration is observed, ◯ when weak discoloration is observed in a part of the tablet, discoloration is recognized throughout the tablet, but the color of the tablet is △, A strong discoloration was observed in the whole tablet, and the tablet was black or a color close to it was indicated as x.

  The disintegration time of the tablets was determined by the disintegration test method of the immediate release preparation described in the Japanese Pharmacopoeia (“6.09 Disintegration Test Method” 15th revision Japanese Pharmacopoeia-Articles and Comments-, Yodogawa Shoten, pages 241-245. ). For disintegration, compared to the time until disintegration of the tablet immediately after production (disintegration time), the disintegration time extension of the tablet after storage is less than 3 minutes ◎ 3 minutes or more and less than 6 minutes ◯ for those that were 6 or more and less than 10 minutes, and Δ for those that were observed to be extended for 10 minutes or more.

  Tablet hardness was measured using a tablet hardness meter (PC-30, manufactured by Okada Seiko Co., Ltd.) for the tablets immediately after production. Those with 90N or more were shown as ◎, those with less than 90N, those with 70N or more, ○, those with less than 70N, those with 40N or more, Δ, and those with less than 40N as ×.

  The test results are shown in the table below.

  From the above test results, the tablet of the comparative example had an unacceptable degree of discoloration and disintegration after storage for 10 days, whereas in the case of the tablet of the present invention, discoloration and disintegration time extension were significantly suppressed. It was confirmed that For example, even when the tablet of Example 1 (0.25% by weight of silicon dioxide, 0.5% by weight of CMC-Ca) was compared with Comparative Example 4 containing 4 times the amount of silicon dioxide, It was confirmed that it was clearly superior in discoloration and disintegration.

Claims (7)

  A composition comprising a Salacia plant extract, silicon dioxide, and carboxymethylcellulose or a metal salt thereof.   The composition according to claim 1, comprising 0.5% by weight or more of carboxymethylcellulose or a metal salt thereof based on the whole composition.   The composition of Claim 1 or 2 which contains 0.25 to 0.75 weight% of silicon dioxide with respect to the whole composition.   The composition according to any one of claims 1 to 3, wherein the carboxymethylcellulose or a metal salt thereof is selected from carboxymethylcellulose and carboxymethylcellulose calcium.   The composition according to any one of claims 1 to 4, wherein the Salacia plant extract is an extract of a Salacia plant selected from Salacia chinensis, Salacia reticulata and Salacia oblonga.   The composition according to any one of claims 1 to 5, which is a tablet or a granule.   The composition according to any one of claims 1 to 6, which is used as a food.