A kind of preparation method and applications of the yew amylose with drop high lithemia effect

文档序号:1750764 发布日期:2019-11-29 浏览:24次 中文

阅读说明:本技术 一种具有降高尿酸作用的红豆杉多糖的制备方法及其应用 (A kind of preparation method and applications of the yew amylose with drop high lithemia effect ) 是由 李晓 王赞 于 2019-05-06 设计创作,主要内容包括:本发明公开了一种具有降高尿酸作用的红豆杉多糖的制备方法及其应用,具体的红豆杉多糖的制备方法包括以下步骤:A)预处理;B)水提醇沉;C)洗涤;D)去蛋白;E)透析;F)冷冻干燥。并且公开了使用该方法制备得到的红豆杉多糖在降高尿酸方面的应用,以及公开了使用该方法制备得到的红豆杉多糖而制备得到的降高尿酸的药剂。本发明提取红豆杉多糖成本低,提取率以及纯度高,得到的红豆杉多糖具有降低高尿酸的功效,对肾脏有保护作用。(The invention discloses a kind of preparation method and applications of yew amylose with drop high lithemia effect, and the preparation method of specific yew amylose is the following steps are included: A) pretreatment;B) water extract-alcohol precipitation;C it) washs;D) deproteinized;E it) dialyses;F it) is freeze-dried.And application of the yew amylose being prepared using this method in terms of dropping high lithemia is disclosed, and discloses the medicament for the drop high lithemia being prepared using the yew amylose that this method is prepared.Present invention extraction yew amylose is at low cost, recovery rate and purity is high, and obtained yew amylose has effects that reduce high lithemia, has protective effect to kidney.)

1. a kind of preparation method of the yew amylose with drop high lithemia effect, which comprises the following steps:

A it) pre-processes

The dry waste material of Chinese yew after extracted complete taxol and 10-DABIII is taken, is crushed, ethyl alcohol is added to carry out Soxhlet extraction, It is spare that the dregs of a decoction are collected by filtration;

B) water extract-alcohol precipitation

Step A) described in the dregs of a decoction appropriate purified water is added, stirring to the dregs of a decoction is waterlogged, and Soxhlet extraction filters, and is concentrated under reduced pressure; Ethyl alcohol, stand at low temperature is added in concentrate, and filtration obtains extract;

C it) washs

Step B) in it is extract obtained be successively slowly added dropwise dehydrated alcohol, acetone, ethyl acetate, it is dry after crude product;

D) deproteinized

Step C) in gained crude product be dissolved in appropriate hot water, it is more after obtaining removing protein with Sevage method protein isolate matter Sugar juice;

E it) dialyses

Step D) in gained polysaccharide solution, using flowing water dialysis remove solution small molecular substance;

F it) is freeze-dried

Step E) in solution after dialysis be concentrated under reduced pressure, be freeze-dried after precooling, obtain Chinese yew Thick many candies;

Step A) in plus ethyl alcohol carry out Soxhlet extraction solid-liquid ratio be 1:8-12.

2. a kind of preparation method of the yew amylose as described in claim 1 with drop high lithemia effect, which is characterized in that Step A) in smash the dry waste material of Chinese yew mesh number be 50-100 mesh, concentration of alcohol 75-90%, add ethyl alcohol carry out Soxhlet extraction Solid-liquid ratio is 1:10, extraction time 1-5h;Step B) water extraction twice is carried out, it is 1:8- that purified water solid-liquid ratio is added for the first time 12, second purified water solid-liquid ratio is added is 1:5-10, step B) in be concentrated under reduced pressure into crude drug concentration be 0.8-1.5g/mL;It is dense 3-6 times of volume ethanol, concentration of alcohol 85-97% is added in contracting liquid, and the temperature of stand at low temperature is 2-8 DEG C, time of repose 15-36h.

3. a kind of preparation method of the yew amylose as described in claim 1 with drop high lithemia effect, which is characterized in that Step C) in be added dehydrated alcohol, acetone, ethyl acetate volume be that southerm yew feeds intake 0.05-0.2 times of quality.

4. a kind of preparation method of the yew amylose as described in claim 1 with drop high lithemia effect, which is characterized in that step Rapid E) dialysis time be 2-5 days, the dialysis bag retention molecular weight 8000-14000 that dialysis uses;Solution decompression after dialysis It is concentrated into crude drug concentration 2.90-3.10g/mL.

5. a kind of preparation method of the yew amylose with drop high lithemia effect according to any one of claims 1-4 is made Application of the standby obtained yew amylose in drop high lithemia.

Technical field

The invention belongs to pharmaceutical technology field more particularly to a kind of preparation sides of the yew amylose with anti-trioxypurine effect Method and application.

Background technique

Hyperuricemia refers to that the uric acid concentration in blood exceeds a kind of fuselage state of normal range (NR), it is considered that male When uric acid concentration in blood is greater than 400 μm of ol/L, the uric acid concentration in women blood is considered as when being greater than 360 μm of ol/L as height Uricacidemia.In recent years studies have shown that hyperuricemia is not only the most important biochemical basis of gout, and be also to cause high blood Pressure, hyperlipidemia, atherosclerosis, obesity, insulin resistance, metabolic syndrome cardiovascular disease occur and death it is important Factor, it has also become threaten one of main metabolic disease of human health.

The chemicals of clinical treatment hyperuricemia at present, mainly with inhibit uric acid generate Allopurinol and uricosuric Based on the drugs such as eccritic probenecid, Benzbromarone.These adverse drug reactions are more, and patient tolerability is poor, significantly impact height The treatment of uricacidemia.In recent years, traditional Chinese medicine achieved very big effect in terms of reducing serum uric acid level.

China Patent Publication No. is that the patent of invention of CN101879264A discloses a kind of " Chinese traditional medicine composition for anti-trioxypurine Object " extracts various composition using smilax, rhizoma alismatis as raw material, is prepared into oral preparation, injection, is used for anti-trioxypurine;Xiao Fuzhou " medicinal herb tea for reducing uric acid of patient with gout ", using herba lysimachiae, Asiatic plantain, Radix Angelicae Sinensis and Ilex Latifolia Thunb as raw material, is crushed into powder, medicine is made Tea, patient drink tea daily, can anti-trioxypurine;Yi Lian " Chinese materia medica preparation and composition of prevention and treatment hyperuricemia and its preparation Method " forms or extracts alkaloid, volatile oil and flavones therein etc. with " Cortex Phellodendri, rhizoma atractylodis, smilax, caulis lonicerae " proportion It matches, is found to have significant anti-trioxypurine activity;From wherein it will be seen that smilax, rhizoma alismatis are edema-alleviating diuretic;Vehicle Preceding grass is stranguria-relieving diuretic;Herba lysimachiae is damp-excreting anti-icteric medicinal;These can be classified as damp-clearing drug.It can be seen that being controlled in terms of Chinese medicine Treating high lithemia is based on clearing damp and promoting diuresis.

Chinese yew has the function of clearing damp and promoting diuresis as medicinal material, and Chinese medicine treats high lithemia based on decocting, through studying It was found that Chinese yew, in addition to it can extract anti-cancer medicine paclitaxel, the main component of water decoction is yew amylose, therefore of the invention Just based on this point, the branches and leaves of yew after efficiently using industrially extracted complete taxol and 10-DAB III is original Material extracts yew amylose, and does purification process, not only economizes on resources, but also further excavates the medicinal valence of yew amylose Value provides to realize the reasonable of rare Chinese yew resource and maximized effectively application for mankind's medical and health field The exploitation in source provides more possibilities.

Summary of the invention

The object of the present invention is to provide a kind of yew amylose and preparation method thereof, realize that it treats antihyperuricemic in preparation Application in disease drug.

A kind of preparation method of yew amylose provided by the invention comprising following steps:

A it) pre-processes

The dry waste material of Chinese yew after extracted complete taxol and 10-DAB III is taken, is crushed, ethyl alcohol is added, Soxhlet is carried out and mentions It takes, it is spare that the dregs of a decoction is collected by filtration.

B) water extract-alcohol precipitation

Step A) described in the dregs of a decoction appropriate purified water is added, stirring to the dregs of a decoction is waterlogged, and Soxhlet extraction filters, decompression Concentration;Ethyl alcohol, stand at low temperature is added in concentrate, and filtration obtains extract.

C it) washs

Step B) in it is extract obtained be successively slowly added dropwise dehydrated alcohol, acetone, ethyl acetate, it is dry after crude product.

D) deproteinized

Step C) in gained crude product be dissolved in appropriate hot water, it is more after obtaining removing protein with Sevage method deproteinized Sugar juice.

E it) dialyses

Step D) in gained polysaccharide solution, using flowing water dialysis remove solution small molecular substance.

F it) is freeze-dried

Step E) in solution after dialysis be concentrated under reduced pressure, be freeze-dried after precooling, obtain Chinese yew Thick many candies.

Preferably, the step A) in be added 80% ethyl alcohol Soxhlet extraction solid-liquid ratio be 1:5-15.

This case is before water extract-alcohol precipitation first with 80% alcohol pre-treatment Chinese yew powder, in order to remove remaining in medicinal material Fat-soluble compound and part monosaccharide, can be improved step B polysaccharide from medicinal materials extraction efficiency in this way, increase recovery rate and mention The purity of high red bean polysaccharide.The solid-liquid ratio of ethyl alcohol Soxhlet extraction influences whether the degree of removal of impurities, and the present invention is by repeatedly attempting, really With good dust removal rate when the solid-liquid ratio of fixed 80% ethyl alcohol Soxhlet extraction is 1:5-15, and cost is minimum, further preferably 80% ethyl alcohol Soxhlet extraction solid-liquid ratio be 1:8-12, further preferred 1:10.

Step B) water extraction twice is carried out, it is 1:8-12, second of addition purified water that purified water solid-liquid ratio is added for the first time Solid-liquid ratio is 1:5-10, step B) in be concentrated under reduced pressure into crude drug concentration be 0.8-15g/mL;3-6 times of volume second is added in concentrate Alcohol, concentration of alcohol 85-97%, the temperature of stand at low temperature are 2-8 DEG C, time of repose 15-36h.

Water extract-alcohol precipitation is that current polysaccharide from medicinal materials extracts most common method, and method is similar, but lacks to extraction process There are larger differences, and production efficiency is improved in the case where keeping recovery rate, reduces cost, and the present invention carries out water twice and extracts, It is 1:8-12 that purified water solid-liquid ratio is added for the first time, and second purified water solid-liquid ratio is added is 1:5-10, further preferred the Solid-liquid ratio is 1:10, and second is 1:8.

In order to guarantee that washing step can effectively remove polysaccharide loss when impurity reduces washing, inventor is washed by observing The method that polyoses content is tested in journey cleaning solution color change and cleaning solution confirms washers to investigate best washing methods Skill.

Finally determining washing methods is dehydrated alcohol, acetone, ethyl acetate to be added with this, and the volume guaranteed is all Southerm yew feeds intake 0.05-0.2 times, preferably 0.1 times of quality.

Step E) in the dialysis bag retention molecular weight 8000-14000 that uses of dialysis.

The present invention also provides a kind of application of yew amylose in preparation treatment antihyperuricemic disease drug.

Yew amylose in preparing antihyperuricemic disease drug, can be made and pharmaceutically be connect as main active The various preparations received, the dosage form of preparation includes but is not limited to: enema;Tablet;Capsule, such as hard capsule;Oral solution;Mouthful Containing agent;Granule;Electuary;Pill;Pill;Powder;Paste;Sublimed preparation;Suspension;Pulvis;Solution;Suppository;Liniment;Frost Agent;Spray;Powder spray;Aerosol;Drops;Pastille and patch.

The auxiliary material for preparing various dosage forms is the excipient substance of pharmaceutical field routine, and auxiliary material includes but is not limited to: adhesive is filled out Fill agent, diluent, tablet agent, lubricant, disintegrating agent, colorant, flavoring agent, wetting agent and surfactant etc..

In above-mentioned application, it will be understood by those skilled in the art that can be produced by the conventional production process of pharmaceutical field, red bean The active component content of China fir polysaccharide is in 1%-99.5%.

Usage amount of the invention can change according to administration route, weight, severity of hyperuricemia of patient etc., Its dose can be 0.01-2g/kg, can be in single or divided doses.

The present invention is using the dry waste material of Chinese yew after extracted complete taxol and 10-DAB III as extraction Chinese yew The raw material of polysaccharide reduces cost, while increasing the utilization rate of Chinese yew, and it is more by the setting of technique to improve Chinese yew The recovery rate and purity of sugar, while it is non-toxic to demonstrate the yew amylose for extracting and obtaining.

The effect of present invention finds yew amyloses to high lithemia is reduced, and corresponding preparation has been prepared, and verify With yew amylose be active constituent made of drug in the test of high lithemia mouse species, show that yew amylose is excellent Anti-trioxypurine and its depressor muscle acid anhydride effect, and have protective effect to kidney;It is that active constituent is made drug and exists with yew amylose Yew amylose is showed in clinical trial apparent anti-trioxypurine effect.

Specific embodiment

To be best understood from the present invention, further specific elaboration is made to the present invention below by following embodiment, but not It can be regarded as limitation of the invention.

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