CN104884066B - Composition for inhibiting amylase activity containing chitosan oligosaccharide - Google Patents
Composition for inhibiting amylase activity containing chitosan oligosaccharide Download PDFInfo
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- CN104884066B CN104884066B CN201380067629.1A CN201380067629A CN104884066B CN 104884066 B CN104884066 B CN 104884066B CN 201380067629 A CN201380067629 A CN 201380067629A CN 104884066 B CN104884066 B CN 104884066B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/702—Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/87—Vitaceae or Ampelidaceae (Vine or Grape family), e.g. wine grapes, muscadine or peppervine
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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Abstract
The present invention provides a composition for inhibiting amylase activity, which contains chitosan oligosaccharide as an active ingredient, and an anti-obesity agent containing the composition. The present invention can be applied to an anti-obesity agent because the activity of amylase is inhibited and an excellent glycolysis inhibition effect is obtained by using chitosan oligosaccharide alone as an active ingredient or chitosan oligosaccharide and a grape seed extract as active ingredients.
Description
Technical Field
The present invention relates to a composition for inhibiting the activity of an amylase (amylase) containing a chitosan Oligosaccharide (Chito Oligosaccharide).
Background
In modern society, a phenomenon of weight gain due to excessive intake of nutrients and obesity-related diseases frequently occur. Also, in the process of controversy for the development of drugs effective for the treatment of obesity, the only obesity therapeutic agent that has received FDA approval is an absorption inhibitor (xenoical). It is a pancreatic lipase inhibitor (pancreatic lipase inhibitor) which is a product developed on the basis of the characteristics of western people who are mainly high-fat foods.
However, eastern people such as koreans are mainly high-carbohydrate foods, which are different from the dietary life of western people. Since carbohydrates are also stored in the body as fats and cause metabolic diseases such as obesity and diabetes, it is necessary to develop a sugar inhibitor suitable for the dietary habits of korea.
Disclosure of Invention
Technical problem to be solved by the invention
To solve the above problems, the present invention aims to: an amylase activity inhibitory composition containing a chitosan oligosaccharide having an amylase inhibitory activity as an active ingredient or containing a chitosan oligosaccharide and a grape seed extract as active ingredients and having a good glycolysis inhibitory effect, and an anti-obesity agent containing the same are provided.
Technical scheme for solving problems
In order to solve the above problems, the present invention provides a composition for inhibiting amylase activity, which contains chitosan oligosaccharide as an active ingredient.
In an embodiment of the present invention, the composition further includes a grape seed extract as an active ingredient.
In an embodiment of the present invention, the composition further includes green tea extract as an active ingredient.
In an embodiment of the present invention, the composition contains 1 to 99.9 wt% of the chitosan oligosaccharide based on the total weight of the composition.
In an embodiment of the present invention, the composition contains 1 to 50 wt% of the grape seed extract in the total amount of the composition.
In an embodiment of the present invention, the composition contains the green tea extract in an amount of 1 to 50 wt% based on the total weight of the composition.
In one embodiment of the present invention, the composition is one or more selected from the group consisting of powder, tablet, capsule, powder, ointment composition, solution, gel, paste, patch (patch), and granule.
The present invention also provides an anti-obesity agent containing the composition for inhibiting amylase activity.
ADVANTAGEOUS EFFECTS OF INVENTION
The composition for inhibiting amylase activity of the present invention can be applied to an anti-obesity agent because it can inhibit the activity of amylase and has an excellent effect of inhibiting glycolysis by using chitosan oligosaccharide alone or chitosan oligosaccharide and a grape seed extract together as active ingredients.
Drawings
Fig. 1 is a graph showing amylase activity of active ingredients contained in an amylase activity inhibition composition according to an embodiment of the present invention.
FIG. 2 is a photograph showing the result of iodine reaction of the active ingredient contained in the composition for inhibiting amylase activity according to one embodiment of the present invention.
Fig. 3 is a graph showing the amylase activity of the active ingredient contained in the composition for inhibiting amylase activity according to the embodiment of the present invention.
FIG. 4 is a photograph showing the result of iodine reaction of the active ingredient contained in the composition for inhibiting amylase activity according to one embodiment of the present invention.
Fig. 5 is a graph showing the amylase activity of the active ingredient contained in the composition for inhibiting amylase activity according to the embodiment of the present invention.
Detailed Description
In order that those skilled in the art who have the technical fields of the present invention and have a general technical knowledge can easily practice the present invention, preferred embodiments of the present invention will be described in detail below.
A general glycolysis process is shown in the following chemical formula, wherein α -amylase (amylolytic enzyme) decomposes starch (starch) into maltose (maltose), α -glucosidase (oligosaccharide) into glucose (glucose), α -glucosidase is clinically used as a diabetes therapeutic agent, but undigested saccharides are used by microorganisms in the large intestine, thereby causing side effects.
The present invention provides an amylase activity inhibiting composition containing chitosan oligosaccharide as an active ingredient.
The chitosan oligosaccharide of the present invention may be a product obtained by a known method, and the present invention is not limited thereto. For example, chitin can be obtained by subjecting crab shells, shrimp shells, and the like to a process of crushing, desalting, removing proteins, and removing impurities, followed by separation and purification, followed by deacetylation (Acetylation) to produce chitosan (chitosan), and then subjecting the chitosan to a chemical decomposition method using an inorganic acid such as hydrochloric acid or a decomposition method using an enzyme. The specific decomposition method using the above enzyme is as follows: adding purified water to chitosan, adding 2-3% hydrochloric acid, and stirring at 40-60 deg.C to obtain chitosan dispersion containing 5-10% hydrochloric acid as solid component; then, after completely dissolving the chitosan, adjusting the pH value to 4-6, dissolving Cellulase (cellulose) serving as chitosan lyase in refined water, and putting the Cellulase into the refined water; then hydrolyzing for 14-20 hours at the temperature of 40-60 ℃, and carrying out heat treatment for 30 minutes at the temperature of 80 ℃ to inactivate the enzyme; then the chitosan oligosaccharide is obtained through the processes of filtering and drying. In the above-mentioned production process, the molecular weight of the chitosan oligosaccharide is changed by the addition of cellulase. Based on the enzyme input amount, 10% of chitosan can obtain chitosan oligosaccharide with the molecular weight of below 1000, 6% of chitosan can obtain chitosan oligosaccharide with the molecular weight of 1500-2000, and 3% of chitosan can obtain chitosan oligosaccharide with the molecular weight of 7000-10000.
Generally, chitosan oligosaccharide has a larger molecular weight than chitosan, which increases the organism absorption rate and utilization rate. The chitosan oligosaccharide used in the present invention may be a mixture of 2 to 8 saccharides having an average molecular weight of about 1100.
Chitosan oligosaccharides are known to have a fat excretion effect, but the glycolytic activity thereof, as well as the amylase activity inhibitory effect, are not known. The present inventors have found that chitosan oligosaccharide also has an amylase activity inhibitory effect. This can be confirmed by the following experimental examples 1 and 2.
In the present invention, the composition may contain 1 to 99.9% of the chitosan oligosaccharide based on the total amount of the composition. If the content of the chitosan oligosaccharide is less than 1%, the desired effect cannot be obtained, and if the content of the chitosan oligosaccharide exceeds 99.9% by weight, the space of the excipient decreases, and various desired pharmaceutical forms cannot be produced.
In the present invention, the composition may further contain a grape seed extract as an active ingredient in addition to chitosan oligosaccharide. The grape seed extract has effects of inhibiting amylase activity and inhibiting glycolysis. In particular, the present inventors have found that when a chitosan oligosaccharide and a grape seed extract are used together, a synergistic effect is obtained and a more excellent amylase activity inhibitory effect is obtained, as compared with the case where the grape seed extract is used alone. This was confirmed in experimental example 2.
In the present invention, the composition may include the grape seed extract in an amount of 1 to 50 wt% based on the total amount of the composition. When the content of the grape seed extract is less than 1% by weight, the desired effect cannot be obtained, and when the content of the grape seed extract exceeds 50% by weight, the addition space of the excipient becomes insufficient, and the synergistic effect with chitosan oligosaccharide becomes half.
In the present invention, green tea extract may be further contained as an active ingredient of the composition. The green tea extract can inhibit not only sugar decomposition but also lipolysis (EGCG). Therefore, the present invention provides a full-scale effect of inhibiting the absorption of nutrients by comprising chitosan oligosaccharide which inhibits glycolysis and promotes the excretion of fat, grape seed extract which inhibits glycolysis, and green tea extract which inhibits glycolysis and lipolysis.
In the present invention, the composition may include the green tea extract in an amount of 1 to 50 wt% based on the total amount of the composition. When the content of the green tea extract is less than 1 wt%, no sugar decomposition effect is observed, and when the content of the green tea extract exceeds 50 wt%, no further effect is observed, so that it is not necessary to use an excessive amount of green tea.
Grape seed extract and green tea extract used in the present invention include: examples of the extract include, but are not limited to, extracts of grape seeds and green tea, extracts obtained by decoction, concentrates obtained by concentrating a part or all of the extracts, or extracts, decoctions, tinctures, mobile extracts obtained by further drying the concentrates, and chemical substances contained in crude drugs that exert main effects.
The composition of the present invention may be one or more selected from the group consisting of powder, tablet, capsule, powder, ointment composition, solution, gel, paste, patch and granule, but is not limited to the above-mentioned dosage forms.
The composition of the invention may be a pharmaceutical composition. In the pharmaceutical composition, the concentration of the active ingredient in all the compositions is preferably kept at 1 to 90% by weight. Since it is difficult to obtain the above-mentioned effects at a concentration of less than 1% by weight, and it is difficult to add excipients, diluents and the like at a concentration of more than 90% by weight, and it is difficult to prepare various dosage forms.
The pharmaceutical composition of the present invention may further comprise suitable carriers, excipients and diluents which are generally used in the manufacture of pharmaceutical compositions.
The form of pharmaceutical administration of the composition of the present invention may be used in the form of a pharmaceutically acceptable salt thereof, and may be used not only alone or in combination with other pharmaceutically active compounds but also in an appropriate combination.
The pharmaceutical composition of the present invention may be prepared into any dosage forms suitable for pharmaceutical preparations, such as powder, granule, tablet, capsule, suspension, emulsion, syrup, spray, ointment, cream, suppository, sterile injection, and the like, according to the conventional methods.
The preferred amount of the composition of the present invention to be administered varies depending on the age, sex, body weight, symptoms, degree of disease, drug form, route of administration and period of administration of the subject, and can be appropriately selected by those skilled in the art according to the actual circumstances. In order to obtain better effect, the 1-day input amount of the effective components is preferably kept between 0.01 and 20mg/kg, and the administration can be carried out once a day or several times a day. The dose can be increased or decreased as appropriate depending on the age, sex, body weight, disease level, route of administration, and the like. The dose can be arbitrarily selected, and is not a feature that limits the scope of the present invention.
The composition of the present invention can be administered to mammals such as rats, white rats, livestock, and humans by various routes such as parenteral and oral administration, and the administration method is various, for example, oral administration, rectal administration, or intravenous, intramuscular, subcutaneous, endometrial, or intracerebroventricular injection.
The amylase activity inhibiting composition containing the chitosan oligosaccharide can inhibit the activity of amylase and finally inhibit the sugar decomposition, so that the composition can be applied to the field of preventing and treating obesity. In addition, the chitosan oligosaccharide of the invention has no toxicity and side effect, and can be used for treatment purpose without worry. Accordingly, the present invention also provides an anti-obesity agent comprising the composition for inhibiting amylase activity of the present invention.
The present invention will be described in more detail by the following examples. However, the following examples are illustrative of the present invention, and the present invention is not limited to the following examples.
(Experimental example 1)
α -amylase (10U) and 1% starch (1ml) were mixed and then reacted at room temperature for 1 hour.
The activity and stability of α -amylase were increased by adding chlorine (chloride) as a cofactor (cofactor). As general experimental conditions, 1 to 5mU of α -amylase was used, and the experimental conditions of the present invention were very strict (enzyme concentration was 2000 times or more).
To the above mixture were added grape seed extract, white kidney bean extract, green tea extract, gamboge each 100ppm and chitosan oligosaccharide 500ppm, respectively.
The reducing power generated during the starch decomposition was converted into a color reaction by a solution of Sodium potassium tartrate (Sodium potassium tartrate) +3, 5-dinitrosalicylic acid (dinitrosalicylic acid), and the color reaction was measured by placing it on a 1cm light path (light path) at 540 nm.
As a result, it was found that α -amylase 10U + chloride in combination all starches were decomposed, but when the amylase was 1U, the reaction was not sufficient even in the presence of chloride, and the results of the α -amylase activity measurements on grape seed extract, white kidney bean extract, green tea extract, gamboge and chitosan oligosaccharide are shown in FIG. 1.
The results of iodine reaction by grape seed extract, white kidney bean extract, green tea extract, gamboge and chitosan oligosaccharide are shown in fig. 2.
As is clear from FIGS. 1 and 2, the inhibitory effect of α -amylase activity is most pronounced in the case of chitosan oligosaccharide and grape seed extract, and also in the case of green tea extract, whereas in contrast, the inhibitory effect of α -amylase activity is weaker in the case of kidney bean extract and Garcinia cambogia which has been approved as a functional component of a glycolysis inhibitor than in the case of chitosan oligosaccharide and grape seed extract.
(Experimental example 2)
An experiment was carried out in the same manner as in example 1, except that α -amylase activity was measured at 100ppm in total, which contained 50ppm of grape seed extract and 50ppm of chitosan oligosaccharide, and α -amylase activity was measured at 200ppm in total, which contained 100ppm of grape seed extract and 100ppm of chitosan oligosaccharide, in addition to 100ppm of grape seed extract and 100ppm of chitosan oligosaccharide.
The results are shown in FIG. 3. it is seen from FIG. 3 that the α -amylase activity inhibitory effect is more pronounced when a mixture of grape seed extract and chitosan oligosaccharide is used than when each component is used alone.
(Experimental example 3)
An experiment was carried out by the same method as in experimental example 1, except that α -amylase activity was measured in the case of mixing 2 or 3 kinds of components in addition to 50ppm of grape seed extract, 50pmm of green tea extract and 50ppm of chitosan oligosaccharide, and the components of the mixture and the results thereof were shown in FIGS. 4 and 5, wherein [ chitosan ] represents chitosan oligosaccharide, [ glucan ] represents grape seed extract and [ green ] represents green tea extract in FIG. 5.
As is clear from fig. 4 and 5, the combination of the components has a significantly enhanced α -amylase activity inhibitory effect as compared with the method using the components alone, that is, the synergistic effects of the grape seed extract, the green tea extract and the chitosan oligosaccharide are known.
Claims (2)
1. Use of a composition comprising chitosan oligosaccharide, grape seed extract and green tea extract as active ingredients for the manufacture of a glycolysis inhibitor for the prevention or treatment of obesity, wherein the content of the chitosan oligosaccharide in the total amount of the composition is 1 to 99.9% by weight, the content of the grape seed extract in the total amount of the composition is 1 to 50% by weight, the content of the green tea extract in the total amount of the composition is 1 to 50% by weight, and the sum of the contents of the components does not exceed 100%.
2. The use according to claim 1, wherein the composition is one or more selected from the group consisting of tablets, capsules, powders, ointments, solutions, gels, pastes, patches and granules.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR10-2012-0132264 | 2012-11-21 | ||
| KR1020120132264A KR101965591B1 (en) | 2012-11-21 | 2012-11-21 | Composition for inhibiting activity of amylase containing chitooligosaccharide |
| PCT/KR2013/010623 WO2014081220A1 (en) | 2012-11-21 | 2013-11-21 | Amylase-activity-inhibiting composition containing chito-oligosaccharide |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104884066A CN104884066A (en) | 2015-09-02 |
| CN104884066B true CN104884066B (en) | 2020-06-02 |
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| CN201380067629.1A Expired - Fee Related CN104884066B (en) | 2012-11-21 | 2013-11-21 | Composition for inhibiting amylase activity containing chitosan oligosaccharide |
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| Country | Link |
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| JP (2) | JP2016500070A (en) |
| KR (1) | KR101965591B1 (en) |
| CN (1) | CN104884066B (en) |
| HK (1) | HK1209333A1 (en) |
| WO (1) | WO2014081220A1 (en) |
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| CN108434191B (en) * | 2018-05-18 | 2020-10-23 | 广东药科大学 | Composition with weight-losing and lipid-lowering effects and preparation method thereof |
| CN108578374B (en) * | 2018-06-01 | 2020-04-03 | 广东药科大学 | Chitosan oligosaccharide granules and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105942074A (en) * | 2016-06-17 | 2016-09-21 | 蚌埠市华东生物科技有限公司 | Waxberry beverage containing stevioside and preparation method thereof |
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| JP3836894B2 (en) * | 1995-04-24 | 2006-10-25 | 焼津水産化学工業株式会社 | Antifeedant |
| JPH09227398A (en) * | 1996-02-20 | 1997-09-02 | Zeria Pharmaceut Co Ltd | Antiobese agent |
| KR100377313B1 (en) * | 2000-03-22 | 2003-03-26 | (주)현덕비엔티 | Method Of Fabricating Green tea Extractive |
| JP2002010753A (en) * | 2000-04-24 | 2002-01-15 | Marukin Chuyu Co Ltd | Amylase inhibitor containing olive leaf or extract thereof and food for person having hyperglycemia |
| JP2003012702A (en) * | 2001-04-24 | 2003-01-15 | Sankyo Co Ltd | Method for producing low molecular chitosan |
| KR100448447B1 (en) * | 2002-12-17 | 2004-09-13 | 주식회사 엔바이오테크놀러지 | Composition comprising the extract of grape seed having α-glucosidase inhibitory activity, the preparation method and the use thereof |
| KR100509682B1 (en) * | 2003-11-26 | 2005-08-23 | 주식회사 렉스진바이오텍 | Pharmaceutical Composition For Preventing And Treating Of Metabolic Bone Disease Comprising Extract Of Sophorae Fructus |
| JP4625750B2 (en) * | 2005-10-21 | 2011-02-02 | 焼津水産化学工業株式会社 | Food and drink containing chitosan |
| KR100989834B1 (en) | 2006-11-30 | 2010-10-29 | (주)아모레퍼시픽 | Composition for Reducing Fatigue Containing Chito-Oligosaccharide |
| KR20090119319A (en) * | 2008-05-16 | 2009-11-19 | 동국대학교 산학협력단 | Composition for anti-obesity comprising deep sea water and chitosan oligosaccharides |
| KR20110045284A (en) * | 2009-10-26 | 2011-05-04 | 주식회사 키토라이프 | Anti obesity agent comprising chitosan oligosaccharides an active ingredient |
| JP2012144569A (en) * | 2012-04-26 | 2012-08-02 | Fisheries Research Agency | Blood pressure elevation-inhibitory composition |
| CN102670864B (en) * | 2012-06-01 | 2014-05-21 | 山东卫康生物医药科技有限公司 | Medicine composition with antioxidant function for treating cardiovascular and cerebrovascular diseases and sugar diabetes |
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2012
- 2012-11-21 KR KR1020120132264A patent/KR101965591B1/en active IP Right Grant
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2013
- 2013-11-21 WO PCT/KR2013/010623 patent/WO2014081220A1/en active Application Filing
- 2013-11-21 CN CN201380067629.1A patent/CN104884066B/en not_active Expired - Fee Related
- 2013-11-21 JP JP2015542963A patent/JP2016500070A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN105942074A (en) * | 2016-06-17 | 2016-09-21 | 蚌埠市华东生物科技有限公司 | Waxberry beverage containing stevioside and preparation method thereof |
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| Publication number | Publication date |
|---|---|
| CN104884066A (en) | 2015-09-02 |
| JP2016500070A (en) | 2016-01-07 |
| HK1209333A1 (en) | 2016-04-01 |
| KR101965591B1 (en) | 2019-04-04 |
| KR20140065125A (en) | 2014-05-29 |
| JP2018138582A (en) | 2018-09-06 |
| WO2014081220A1 (en) | 2014-05-30 |
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