CN108524493A - Application of the dihydromyricetin promotor composition in resisting alcoholic liver oxidative damage - Google Patents
Application of the dihydromyricetin promotor composition in resisting alcoholic liver oxidative damage Download PDFInfo
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- CN108524493A CN108524493A CN201810660967.0A CN201810660967A CN108524493A CN 108524493 A CN108524493 A CN 108524493A CN 201810660967 A CN201810660967 A CN 201810660967A CN 108524493 A CN108524493 A CN 108524493A
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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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
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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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
Abstract
The present invention provides a kind of preparation method of dihydromyricetin composition product：Take the water of Dendrobium officinale polysaccharide 30~50 parts of additions, 5~15 times of weight, 5~15 parts of Puerarin is added, 20~35 parts of dihydromyricetin is added, 5~10min is deoxygenated using ultrasonic wave when being stirred, after being dried in vacuo 30~60min, adds 20~40 parts of astragalus polyose, after 10~30min of ultrasonication, tabletting after vacuum drying, then saved backup using being packed after vacuum drying after being coated with conventional enteric piece solution, wherein dihydromyricetin is dissolved with 0.5~6 times of w ethanol.The obtained dihydromyricetin composition product of the present invention is used directly for the application in resisting alcoholic liver oxidative damage or protect liver.
Description
Technical field
The present invention relates to a kind of application of dihydromyricetin promotor composition in resisting alcoholic liver oxidative damage, belong to natural
Product processing technique field.
Background technology
Dihydromyricetin DMY is that ampelopsis grossdentata is also known as one of main active ingredient of vine tea, is civil traditional medication,
Once be widely used in treating the infectious diseases such as skin disease, furuncle and osteomyelitis, acute lymphoblastic inflammation, can inhibit it is a variety of have fall ill
Bacterium.Solubility is 4% in 25 DEG C of water, solubility bigger in hot water；It is soluble in methanol, ethyl alcohol and acetone, it is atomic to be dissolved in acetic acid
Ethyl ester；It is insoluble in chloroform, petroleum ether.Lin Shuying etc. investigates DMY stability and influence factor, it was demonstrated that dihydromyricetin
Solution easily aoxidizes, and stability is poor, and no more than 100 DEG C, heating time is no more than 30min and acidity and neutrallty condition
It can keep its steady chemical structure, and transiting state metal ion A l3+、Fe3+、Cu2+Play inducing catalysis Deng to the oxidation of DMY.
DMY has the function of relieving alcoholism and protecting livers protect liver.Zhong Zhengxian etc. is using mouse as the hepatoprotective effect of scale-model investigation DMY.It grinds
Study carefully and shows:When DMY can be substantially reduced the acute liver caused by D-galactosamine, carbon tetrachloride and isothiocyanic acid naphthalene vinegar
AST activity, ALT and T-BIL contents, reduce the denaturation and necrosis of hepatic tissue, improve haemolysis cellulose content and monokaryon in serum
The huge phagocytic function for sleeping cell, it was demonstrated that DMY has the function of reducing enzyme and treating jaundice liver protection.OshimaY et al. researchs also confirm that DMY pairs
Hepatic injury caused by anti-galactosamine and carbon tetrachloride has obvious effect and has apparent anti-hepatitis detoxifying function.In addition, DMY
The increase of serum lactic deoxidation enzyme activity caused by hepatocellular injury can be improved, inhibit the formation of liver property M cell collagen fibers,
To play the role of liver protecting, damage of the ethyl alcohol to liver is greatly lowered, liver normal condition is made to be restored rapidly.
Metabolin is acetic acid to ethyl alcohol in vivo, acetaldehyde be cause the main matter of liver damage and easily cause it is dizzy after drinking and
It dislikes liquor-saturated.The researchs such as Hase-K find that DMY has good sober-up function；Its relieving mechanism, which is DMY, can mitigate internal ethylism,
Ethyl alcohol is reduced to the damage of liver to protect liver.Liu builds the newly equal water boiled with plant-ampelopsis grossdentata and carries out experiment of relieving the effect of alcohol.
The result shows that with the increasing for the decocting agent concentration drunk, the percentage of the instability of gait of people and the hundred of reaction is fallen after drinking
Point rate is decreased obviously, since the principle active component in porcelain ampelopsis is DMY, then prove DMY have mitigate it is internal
The effect of ethylism also confirms that DMY has the function of alleviating drunk and promotes to sober up after drinking.
Dioxy myricetin is had a wide range of applications due to its good physiological activity.In its structure there is superdelocalizability can make
Entire molecule forms the total often system of one big 7C keys, and the oxygen atom in molecule has stronger coordination ability, the acid light base of powder
It is all easy to react with metal ion with base is cut out at network group, this space structure of parent nucleus is conducive to the shape of complex
At can be used as the good tie ligand of metal ion.Has the research of the metal ion match of a small amount of dihydromyricetin at present.
Guo Qingquan etc. prepares the complex of dioxy myricetin-iron and studies its inoxidizability.The result shows that dioxy myricetin is easy to iron hair
It gives birth to mating reaction and fit rate is higher, obtained complex has good inoxidizability.Burnt minor benefit etc. is by the two of equimolar amounts
Oxygen myricetin and zinc acetate prepare dioxy myricetin-Zn complex under alkaline environment, and use MTT, RT-PCR method pair two
Hydrogen myricetin-Zn complex anti tumor activity in vitro is studied.Mtt assay detects complex treated Hela cell activity knots
Fruit find carefully with the extension of incubation time, the survival rate of each group tumour cell is on a declining curve, and inhibiting effect with
The increase of object concentration and the extension of action time are closed, the inhibiting effect is cumulative strong；RT-PCR shows caspase-3 with complex concentration
Increase and raise, bcl-2 gene expressions increase with complex concentration and lowered.Conclusion:DMY- Zn complexes show stronger
Antitumor activity.
Dendrobium candidum also known as iron bracketplant, iron sheet orchid, ribbed hedyotis herb are gained the name because epidermis is in iron green, are had unique medicinal
Value, have enriching yin qi-restoratives, promoting production of body fluid and nourishing the lung, spleen benefiting and stimulating the appetite, nourish the liver to improve visual acuity, moisturizing, beauty treatment, anti-aging nourishing Yin and clearing heat promotes the production of body fluid only
Thirsty effect.Clinical research shows that dendrobium candidum can not only enhance insulin active, while can significantly reduce blood glucose level,
Keep blood normal；G cells can be directly stimulated, gastrin secretion is made to increase, serum gastrin concentration increases, and gastrin stimulates wall thin
Born of the same parents make gastric acid secretion increase；It can promote cycle, expansion blood vessel, reduce cholesterolemia and triglyceride.
Radix Astragali, also known as continuous stilbene, polysaccharide have enhancing body's immunity, liver protection, diuresis, anti-aging, resisting stress, decompression and
Wide antibacterial action.The update of serum and hepatic protein can be remarkably promoted.The synthesis of spleen protein matter can be increased, and made
Spleen cell hyperplasia, endochylema include a large amount of rough surfaced endoplasmic reticulum (RER)s.Radix Astragali is in dual regulation to glycometabolism, can significantly reduce grape
The blood glucose level of mouse after glucose load to the blood glucose rise caused by antiadrenergic drug, and can fight the mouse caused by insoral
Blood glucose reduces.
The Chinese patent of Publication No. CN104127406A discloses a kind of dihydromyricetin and is preparing liver cell oxidation
Dihydromyricetin is made after various dosage forms and directly takes orally by the application in the inhibitor of damage, dihydromyricetin tablet
Manufacturing method is 75 grams of dihydromyricetin, and 25.95 grams of starch is dissolved in 150 grams of water, and it is micro- that dihydromyricetin is made in spray drying
Capsule particle.By microcapsules grain and 37.5 grams of lactose, 10.5 grams of crosslinked carboxymethyl fecula sodium, 1.05 grams of mixing of magnesium stearate add
Enter into three-dimensional motion mixer, incorporation time is 15-20 minutes, obtains total mixture.Then direct tablet compressing is obtained 1000
Piece, every 0.15 gram, 75 milligram/of dihydromyricetin cellulose content；The manufacturing method of dihydromyricetin cellulose capsule is dihydromyricetin 30
Gram, 18 grams of gelatin is dissolved in 150 grams of water, and dihydromyricetin microcapsule granule is made in spray drying.27.5 grams of casein phosphoric acid
Peptide, 23 grams of D-mannitals, 1.5 grams of magnesium stearates and microcapsule granule are put into multidigit mixing machine and are sufficiently mixed uniformly, are made wet
Grain, crosses 20 mesh sieve, and capsule is made with capsule filler packing in dry, whole grain；The manufacturing method of dihydromyricetin beverage is 37.5
Gram dihydromyricetin, 10 grams of citric acids, 435 grams of honey, 150 grams of Aspartames, 5 grams of vanillas of vanilla, 9362.5 grams of water are mixed
It closes uniformly, boils, sterile filling beverage bottle to obtain the final product.
The Chinese patent of Publication No. CN104666293A discloses a kind of dihydromyricetin cyclodextrin inclusion compound and its system
Preparation Method includes the following steps：(1) 100-500 parts of dihydromyricetin is dissolved in 100-39600 parts of solvent A, is made
Dihydromyricetin solution；(2) 200-600 parts of cyclodextrin and/or cyclodextrine derivatives are directly added into above-mentioned dihydromyricetin
Solution and/or 200-600 parts of cyclodextrin and/or cyclodextrine derivatives are dissolved in 100-39600 parts of solvent B, are made
Above-mentioned dihydromyricetin solution is added in cyclodextrin and/or cyclodextrine derivatives solution；(3) mixed solution is sheared with cutter,
When microscopy being used in combination to have complex compound formation, then packet connect completions, be then spray-dried with spray tower, obtain powder solid dihydromyricetin and
Cyclodextrin and/or cyclodextrin derivant clathrate.
The Chinese patent of Publication No. CN107007813A discloses a kind of efficient relieving alcoholism and protecting liver composition, preparation method
And application.The composition is with the dehydration ampelopsis grossdentata leaves of 280~390 parts of parts by weight, 210~580 parts of parts by weight
The A Sayi fruit instant powder groups of 90~130 parts of hoveniae semoveniae semen, the corn oligopeptide powder of 140~300 parts of parts by weight and parts by weight
At.Wherein, dehydration ampelopsis grossdentata leaf is through ultrasonic extraction, and extractive total flavone content >=35%, dihydromyricetin cellulose content 25~
32%；Hoveniae semoveniae semen is extracted through alcohol heat reflux, extractive total flavone content >=8%.Ah's Sai fruit instant powder is beaten by A Sayi fruits
Slurry, filtering and removing slag, filtrate concentration, addition auxiliary material, combination drying are made.
The Chinese patent of Publication No. CN101569614 discloses a kind of method of puerarin lagging cover slowly-releasing dripping pill, including
Following step：A, Puerarin rapid-released droppills capsule core is prepared：Macrogol 6000 is as matrix, by itself and Puerarin bulk pharmaceutical chemicals powder
It is with weight ratio：10: 1~3: 1 mixing prepares dripping pill capsule core using fusion method with pill dripping machine, and melting temperature is 70~90 DEG C, medicine
Liquid holding temperature is 60~80 DEG C；B, it is coated：Using acetone: absolute ethyl alcohol=95: film forming is added as solvent in the mixed solution of 5v/v
Agent, plasticizer, perforating agent place it in 4~5h of ultrasonic dissolution in Ultrasound Instrument, and ultrasound condition is 80W to get coating solution；With packet
Clothing pot is coated dripping pill capsule core using turnadle pan coating, is coated 40 DEG C of temperature, and coating pan rotating speed is 30~50 turns per minute,
Weightening 5%~10% is to get puerarin lagging cover slowly-releasing dripping pill.
The Chinese patent of Publication No. CN1977975 discloses a kind of system of Puerarin/cyclodextrin composite of inclusion state
Preparation Method, step are：By in beta-cyclodextrin, hydroxypropyl-β-cyclodextrin, Sulfobutyl ether β _ cyclodextrin three one kind or in which
Both arbitrary or three mixture and 1~5 mass ratio pure water are mixed into suspension or solution, and cyclodextrin 0.2~1.0 is added and rubs
The Puerarin of your ratio, is sufficiently mixed, and heats 60~80 DEG C and stirs 1 hour, cooling, press filtration, solids is dried under reduced pressure；Or in 50 DEG C
Lower decompression water removal is to get solid clathrates.
The Chinese patent of Publication No. CN102934768A discloses a kind of Puerarin, pollen pini and propolis complex tablet
Preparation method, following steps：(1) main raw material(s) mixes：Bee glue powder, broken wall preserved egg are weighed according to above-mentioned mass percent
Powder, Puerarin are uniformly mixed；(2) adhesive makes：Sucrose and dextrin are weighed according to above-mentioned mass percent, water is added, so
Sucrose, dextrin are cooked into the slurry of a concentration of 45%-55% as adhesive afterwards；(3) wet granulation：Above-mentioned bee glue powder, broken wall
Pollen pini, Puerarin mixture and sucrose are mixed with the adhesive that dextrin makes, using wet granulation, drying temperature 65
DEG C -75 DEG C, whole grain is sieved with 12 mesh, and control pellet moisture is≤5.0%, granule sealed is got well what is pelletize for use；(4) tablet system
Make：Sodium carboxymethyl starch and microcrystalline cellulose are weighed according to above-mentioned mass percent, the particle after granulation is formed sediment with carboxymethyl
Powder sodium, microcrystalline cellulose are uniformly mixed, and it is multiple then to carry out tabletting obtained Puerarin, pollen pini and propolis of the present invention in tablet press machine
Close tablet.
Invention content
In order to preferably play repair of the Flavonoid substances such as dihydromyricetin and Puerarin to hepatic injury, and reduce
It acts on gastrointestinal irritation, and to solve, the dissolved solution degree of dihydromyricetin is poor, bioavailability is low, to the pH of light, solution
Value and the metal ion-sensitives such as iron, aluminium, it is oxidizable rotten the shortcomings of.It is wrapped using embedded material and is connect, reaches and improves dihydro poplar
The stability of syphilis and the purpose of bioavailability.
Therefore, first purpose of the invention is to provide a kind of dihydromyricetin promotor composition in resisting alcoholic liver oxidative damage
Application, Puerarin and dihydromyricetin carry out packet and connect, formed Puerarin and dihydromyricetin promotor composition, improve two by this method
Hydrogen red bayberry promotor composition is to the metal ions such as light, oxygen, solution ph, iron, aluminium unstability and bioavailability.
Therefore, first purpose of the invention is to provide a kind of preparation method of dihydromyricetin composition product：Take iron sheet
The water of dendrobium polysaccharide 30~50 parts of additions, 5~15 times of weight, is added 5~15 parts of Puerarin, 20~35 parts of dihydromyricetin is added,
5~10min is deoxygenated using ultrasonic wave when being stirred, after being dried in vacuo 30~60min, adds astragalus polyose 20~40
Part, after 10~30min of ultrasonication, tabletting after vacuum drying, then use vacuum after being coated with conventional enteric piece solution
Packaging saves backup after drying, and wherein dihydromyricetin is dissolved with 0.5~6 times of w ethanol.
In a specific embodiment, wherein each material composition is formed with following parts by weight：Take Dendrobium officinale polysaccharide 40
The water of 5~15 times of weight of~50 parts of additions, is added 10~15 parts of Puerarin, 30~35 parts of dihydromyricetin is added, mixed in stirring
5~10min is deoxygenated using ultrasonic wave when conjunction, after being dried in vacuo 30~50min, adds 30~40 parts of astragalus polyose, ultrasonic wave
After handling 20~30min, tabletting after vacuum drying, then packed after using vacuum drying after being coated with conventional enteric piece solution
It saves backup, wherein dihydromyricetin is dissolved with 1~4 times of w ethanol.
In another embodiment, wherein each material composition is formed with following parts by weight：Take Dendrobium officinale polysaccharide
The water of 45 parts of additions, 10 times of weight, is added 15 parts of Puerarin, 30 parts of dihydromyricetin is added, ultrasonic wave is used when being stirred
10min is deoxygenated, after being dried in vacuo 30min, adds 35 parts of astragalus polyose, after ultrasonication 25min, is pressed after vacuum drying
Piece, then saved backup using being packed after vacuum drying after being coated with conventional enteric piece solution, wherein dihydromyricetin is with 2 times
W ethanol is dissolved.
Second purpose of the invention is to provide the preparation method of above-mentioned composition product, is as follows：
A, it takes Dendrobium officinale polysaccharide that water is added, Puerarin is added and obtains mixture I；
B, it takes dihydromyricetin that ethyl alcohol is added to be dissolved, mixture I is added thereto, when being stirred using ultrasound
Wave deoxygenates 5~10min, obtains mixture II after being dried in vacuo 30min, wherein dihydromyricetin is dissolved with 5 times of w ethanols；
C, it is added astragalus polyose into mixture II, after ultrasonication 25min, piece is pressed into after vacuum drying and obtains sheet
Object；
D, 1000g acrylic resins 2 are weighed, 50mL diethyl phthalates, 100mL castor oil, 50mL Tween-80s,
150g talcum powder adds to 5000mL with absolute ethyl alcohol, obtains mixture III；
E, it uses to pack after being dried in vacuo after being coated tablet with mixture III and save backup.
Third purpose of the present invention is to provide a kind of preparation method of Dendrobium officinale polysaccharide and astragalus polyose, step packet
It includes：
(1) dry dendrobium candidum or Radix Astragali are crushed, 80-90% ethanol waters are added, after 30~80min is extracted in stirring,
50~140min is stood, upper solution of the layering removal containing ethyl alcohol obtains precipitation I.
(2) a certain amount of water is added into precipitation I, is heated with stirring to 70-85 DEG C, after keeping the temperature 30~80min, 5000rpm
10~20min is centrifuged, supernatant is obtained, goes precipitation II.
(3) supernatant is concentrated under reduced pressure into certain volume at 50-65 DEG C, adds 95% ethyl alcohol to final concentration and reaches
75% or more, alcohol precipitation 10-20h are filtered, and it is dendrobium candidum or astragalus polyose to obtain filter residue.
In one embodiment, the volume L of 80-90% ethanol waters described in step (1) and dendrobium candidum or Huang
Stilbene weight kg ratios are 2~5：1.
In one embodiment, the volume L and dendrobium candidum or astragalus weight kg ratios of water are added described in step (2)
It is 2~6：1.
In one embodiment, certain volume described in step (3) refers to the 1/10-1/40 of original volume.
In one embodiment, it is filtered described in step (3)：Membrane aperture is that 0.22 μm of ceramic membrane filter is primary.
Above-mentioned acquisition dihydromyricetin composition product is used directly in resisting alcoholic liver oxidative damage or protect liver
Using.
Technique effect
1, Dendrobium officinale polysaccharide and astragalus polyose form a large amount of cavernous structure by dihydromyricetin under the action of ethyl alcohol
It is effectively embedded with Puerarin, improves the utilization rate of the Flavonoid substances such as dihydromyricetin and Puerarin.
2, it is embedded by enteric coatel tablets, effectively prevents dihydromyricetin and Puerarin reacts under one's belt, just
In the release in small intestine, the stimulation to small intestine is not only reduced by Dendrobium officinale polysaccharide and astragalus polyose effect, and enhance
The protect liver effect of its product.
Specific implementation mode
The essentiality content further illustrated the present invention below with the embodiment of the present invention, but this is not limited with this
Invention.
Embodiment 1：The preparation of Dendrobium officinale polysaccharide
Dry dendrobium candidum 100kg is crushed, 90% ethanol water 250L is added, after 60min is extracted in stirring, is stood
100min, upper solution of the layering removal containing ethyl alcohol, obtains precipitation I.350L water is added into precipitation I, is heated with stirring to 85 DEG C,
After keeping the temperature 60min, 5000rpm centrifuges 20min, obtains supernatant, goes precipitation II.Supernatant is concentrated under reduced pressure into 10L at 55 DEG C,
It adds 95% ethyl alcohol to final concentration and reaches 75% or more, alcohol precipitation 16h is filtered, and it is Dendrobium officinale polysaccharide to obtain filter residue.
Embodiment 2：The preparation of astragalus polyose
Dry Radix Astragali 100kg is crushed, 90% ethanol water 250L is added, after 60min is extracted in stirring, stands 100min,
Upper solution of the layering removal containing ethyl alcohol, obtains precipitation I.350L water is added into precipitation I, is heated with stirring to 85 DEG C, heat preservation
After 60min, 5000rpm centrifuges 20min, obtains supernatant, goes precipitation II.Supernatant is concentrated under reduced pressure into 10L at 55 DEG C, then is added
Enter 95% ethyl alcohol to final concentration and reach 75% or more, alcohol precipitation 16h is filtered, and it is astragalus polyose to obtain filter residue.
Embodiment 3
It takes Dendrobium officinale polysaccharide 4.5kg that 45kg water is added, Puerarin 1.5kg is added and obtains mixture I.Take 3kg dihydromyricetins
Element after being dissolved with 5L ethyl alcohol, is added in mixture I, and 10min is deoxygenated using ultrasonic wave when being stirred, and vacuum is dry
After dry 30min, astragalus polyose 3.5kg is added, after ultrasonication 25min, tabletting after vacuum drying obtains tablet.It weighs
1000g acrylic resins 2,50mL diethyl phthalates, 100mL castor oil, 50mL Tween-80s, 150g talcum powder, with nothing
Water-ethanol adds to 5000mL, obtains mixture III；It is packed after using vacuum drying after after being coated to tablet with mixture III
It saves backup.After testing, dihydromyricetin embedding rate reaches 86.56% in obtained tablet, and Puerarin embedding rate reaches
88.62%.
Comparative examples 1
It takes Dendrobium officinale polysaccharide 4.5kg that 45kg water is added, Puerarin 1.5kg is added, is directly added into 3kg dihydromyricetin powder
End, adds astragalus polyose 3.5kg after being stirred, and after ultrasonication 25min, tabletting after vacuum drying obtains tablet.
Weigh 1000g acrylic resins 2,50mL diethyl phthalates, 100mL castor oil, 50mL Tween-80s, 150g talcum powder,
5000mL is added to absolute ethyl alcohol, obtains mixture III；After vacuum drying being used after after being coated to tablet with mixture III
Packaging saves backup.After testing, dihydromyricetin embedding rate reaches 32.88% in obtained tablet, and Puerarin embedding rate reaches
To 60.27%.
Comparative examples 2
It takes Dendrobium officinale polysaccharide 4.5kg that 45kg water is added, Puerarin 1.5kg is added, is directly added into 3kg dihydromyricetin powder
End deoxygenates 10min when being stirred using ultrasonic wave, after being dried in vacuo 30min, adds astragalus polyose 3.5kg, ultrasonic wave
After handling 25min, tabletting after vacuum drying obtains tablet.Weigh 1000g acrylic resins 2,50mL phthalic acid diethyls
Ester, 100mL castor oil, 50mL Tween-80s, 150g talcum powder add to 5000mL with absolute ethyl alcohol, obtain mixture III；With mixing
It packs and saves backup after use vacuum drying after object III is coated tablet.After testing, dihydro in obtained tablet
Myricetin embedding rate reaches 43.71%, and Puerarin embedding rate reaches 78.48%.
Comparative examples 3
It takes Dendrobium officinale polysaccharide 4.5kg that 45kg water is added, Puerarin 1.5kg is added and obtains mixture I.Take 3kg dihydromyricetins
Element after being dissolved with 5L ethyl alcohol, is added in mixture I, after placing 10min, adds astragalus polyose 3.5kg, ultrasonic wave
After handling 25min, tabletting after vacuum drying obtains tablet.Weigh 1000g acrylic resins 2,50mL phthalic acid diethyls
Ester, 100mL castor oil, 50mL Tween-80s, 150g talcum powder add to 5000mL with absolute ethyl alcohol, obtain mixture III；With mixing
It packs and saves backup after use vacuum drying after object III is coated tablet.After testing, dihydro in obtained tablet
Myricetin embedding rate reaches 67.93%, and Puerarin embedding rate reaches 83.47%.
Embodiment 4
1 gram of various products are taken, carries out being placed at room temperature for experiment after simulation small intestine digestive juice 30mL is added, be detected using HPLC methods
Dihydromyricetin and puerarin content variation in its solution, the result is shown in Tables 1 and 2s.
1. various products of table dihydromyricetin changes of contents table in different time
2. various products of table puerarin content in different time changes table
Embodiment 5：Repairing effect of the various products to mouse alcoholic liver hepatic injury
NIH mouse, male and female dual-purpose, 18~22g of weight are provided by Hunan Province's animal experimental center, and quality certification number is dynamic for Hunan
Word the 20163026th.Experimental animal environment：Clean Facility.22-25 DEG C of laboratory temperature, humidity 55-65%.NIH mouse
It is randomly divided into 8 groups, every group 10.It will continue gavage, each 2mL/kg/ only one month with 50 degree of white wine, blood test detection is
It is no to reach moderate alcoholic hepatic injury degree, then continue gavage with various products, it is to compare with water, each 1mL/kg/ only one month,
Blood extracting assay detects, then liver microscopy is taken after killing, and result situation is shown in Table 3.
Repairing effect table of 3. various products of table to hepatic injury
| Product | The repair rate % of hepatic injury |
| Embodiment 1 | 11.53% |
| Embodiment 2 | 24.26% |
| Embodiment 3 | 85.68% |
| Comparative examples 1 | 35.72% |
| Comparative examples 2 | 50.45% |
| Comparative examples 3 | 67.27 |
Claims (6)
1. a kind of preparation method of dihydromyricetin composition product：Take Dendrobium officinale polysaccharide 30~50 parts of additions, 5~15 times of weights
The water of amount, be added 5~15 parts of Puerarin, be added 20~35 parts of dihydromyricetin, when being stirred using ultrasonic wave deoxidation 5~
10min adds 20~40 parts of astragalus polyose after being dried in vacuo 30~60min, and after 10~30min of ultrasonication, vacuum is dry
Tabletting after dry, then saved backup using being packed after vacuum drying after being coated with conventional enteric piece solution, wherein dihydromyricetin
Element is dissolved with 0.5~6 times of w ethanol.
2. the method for claim 1 wherein each material compositions to be formed with following parts by weight：40~50 parts of Dendrobium officinale polysaccharide is taken to add
Enter the water of 5~15 times of weight, 10~15 parts of Puerarin is added, 30~35 parts of dihydromyricetin is added, is used when being stirred
Ultrasonic wave deoxygenates 5~10min, after being dried in vacuo 30~50min, adds 30~40 parts of astragalus polyose, and ultrasonication 20~
After 30min, tabletting after vacuum drying, then after being coated with conventional enteric piece solution it is standby using preservation pack after vacuum drying
With wherein dihydromyricetin is dissolved with 1~4 times of w ethanol.
3. the method for claim 1 wherein each material compositions to be formed with following parts by weight：45 parts of Dendrobium officinale polysaccharide is taken to be added 10
15 parts of Puerarin is added in the water of times weight, and 30 parts of dihydromyricetin is added, and 10min is deoxygenated using ultrasonic wave when being stirred,
After being dried in vacuo 30min, 35 parts of astragalus polyose is added, after ultrasonication 25min, tabletting after vacuum drying, then with routinely
Enteric coatel tablets solution be coated after using packing and saving backup after vacuum drying, wherein dihydromyricetin with 2 times of w ethanols into
Row dissolving.
4. the method for claim 1-3, wherein the preparation method of the composition product, is as follows：
A, it takes Dendrobium officinale polysaccharide that water is added, Puerarin is added and obtains mixture I；
B, it takes dihydromyricetin that ethyl alcohol is added to be dissolved, mixture I is added thereto, is gone using ultrasonic wave when being stirred
5~10min of oxygen obtains mixture II after being dried in vacuo 30min, and wherein dihydromyricetin is dissolved with 5 times of w ethanols；
C, it is added astragalus polyose into mixture II, after ultrasonication 25min, piece is pressed into after vacuum drying and obtains tablet；
D, 1000g acrylic resins 2,50mL diethyl phthalates, 100mL castor oil, 50mL Tween-80s, 150g are weighed
Talcum powder adds to 5000mL with absolute ethyl alcohol, obtains mixture III；
E, it uses to pack after being dried in vacuo after being coated tablet with mixture III and save backup.
5. the method for claim 4, wherein the preparation method of the Dendrobium officinale polysaccharide and astragalus polyose, step include：
(1) dry dendrobium candidum or Radix Astragali are crushed, 80-90% ethanol waters are added, after 30~80min is extracted in stirring, is stood
50~140min, upper solution of the layering removal containing ethyl alcohol, obtains precipitation I.
(2) a certain amount of water is added into precipitation I, is heated with stirring to 70-85 DEG C, after keeping the temperature 30~80min, 5000rpm centrifugations
10~20min obtains supernatant, goes precipitation II.
(3) supernatant is concentrated under reduced pressure into certain volume at 50-65 DEG C, add 95% ethyl alcohol to final concentration reach 75% with
On, alcohol precipitation 10-20h is filtered, and it is dendrobium candidum or astragalus polyose to obtain filter residue.
6. the dihydromyricetin composition product prepared by the method for claim 1-5 is used directly for the oxidation of resisting alcoholic liver
Application in damage or protect liver.
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| CN111150727A (en) * | 2019-12-05 | 2020-05-15 | 华南农业大学 | Application of dihydromyricetin in preparation of medicine for relieving intestinal cell injury caused by vomitoxin |
| US20230285352A1 (en) * | 2018-11-14 | 2023-09-14 | The Trustees Of Princeton University | Dihydromyricetin Hot Melt Extrusion Formulations and Methods for Forming Them |
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| US20230285352A1 (en) * | 2018-11-14 | 2023-09-14 | The Trustees Of Princeton University | Dihydromyricetin Hot Melt Extrusion Formulations and Methods for Forming Them |
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