CN1985891B - Compound Chinese medicine preparation with liver protecting function and its preparing process - Google Patents
Compound Chinese medicine preparation with liver protecting function and its preparing process Download PDFInfo
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- CN1985891B CN1985891B CN2006101632644A CN200610163264A CN1985891B CN 1985891 B CN1985891 B CN 1985891B CN 2006101632644 A CN2006101632644 A CN 2006101632644A CN 200610163264 A CN200610163264 A CN 200610163264A CN 1985891 B CN1985891 B CN 1985891B
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- China
- Prior art keywords
- schisandrae chinensis
- fructus schisandrae
- radix astragali
- group
- ethanol
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- Medicines Containing Plant Substances (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The compound Chinese medicine preparation with liver protecting function consists of total lignin extracted from schisandra and total polysaccharide extracted from astragalus root in certain ratio. The compound Chinese medicine preparation has less impurity content and raised pharmacological effect and clinical curative effect, and may be further prepared into different medicine preparations for treating liver damage.
Description
Technical field
The present invention relates to medical technical field; be specifically related to have the effective ingredient in Chinese composition and method of making the same of protection hepatic injury, specifically effective ingredient in Chinese compound preparation of forming by total lignans in five tastes of medicinal herb and the Radix Astragali Mongolici total polysaccharide in the Radix Astragali and preparation method thereof.
Background technology
Modern medicine is more deep to the research of hepatic injury; inquired into the mechanism of hepatic injury from many aspects; and film protective agent such as phospholipid and how unsaturated lecithin etc. have been developed; antioxidant such as reduced form paddy light liver peptide etc.; medicines such as anti-immune response agent such as calcineurin inhibitor; but the still difficult people's will to the greatest extent of curative effect, and, limited clinical practice because of its toxic and side effects.
Fructus Schisandrae Chinensis is a conventional Chinese medicine, studies show that Fructus Schisandrae Chinensis has the activity of significant liver function protecting, and its main active is a cyclohexyl biphenyl octene type lignanoid.Schisandrol extract and deoxyschizandrin, second element, third element, pure first, pure second, ester first, ester the second grade composition have significant protective effect to the animal liver cell damage that chemical toxicant causes, can suppress transaminase's release, make the active reduction of ALT; Obviously inducing mouse and rat liver microsomes cytochrome P-450 activity increase the liver detoxification ability.Though, there is literature research to show that the lignan component in the Fructus Schisandrae Chinensis is the main component of its liver-protecting activity at present, the content of lignan component is not high in the Fructus Schisandrae Chinensis extrat that obtains with conventional method, influences clinical therapeutic efficacy.
The Radix Astragali is clinical conventional Chinese medicine, has many-sided pharmacological actions such as antiinflammatory, analgesia, heart tonifying, immunological enhancement, is the main medicine in treatment hepatitis, the nephritis prescription.But Radix Astragali the liver protecting rough endoplasmic reticulum; and rough endoplasmic reticulum is increased; increase the content of interior rRNA of cell and mRNA; suppress ribonuclease activity, thereby promote protein synthesis, serum albumin (PA), albumin (ALB) raise; alanine aminotransferase (ALT) descends; thereby improve the complex functionality of liver cirrhosis patient hepatic protein, and can protect liver plasma membrane, the control hepatic injury.
We find that by the research back hepatic injury that the Chinese medicine compound that Fructus Schisandrae Chinensis and Radix Astragali compatibility are formed causes carbon tetrachloride has significant protective effect.But the Chinese medicine compound recipe exists to become to be hard to tell, mechanism is not clear, the difficult control of quality, the unsteady shortcoming of curative effect.
Summary of the invention
The object of the present invention is to provide a kind of pharmaceutical composition of forming by the effective site of five tastes of medicinal herb and the Radix Astragali; it is the modern Chinese medicine compound preparation; its definite ingredients, easy to control the quality, curative effect is reliable; can be used for protecting hepatic injury; reduce the transaminase of hepatitis, and propose the preparation method of this compound Chinese medicinal preparation.
The effective ingredient in Chinese compound preparation that the present invention proposes is to be that former material assembly forms by the Fructus Schisandrae Chinensis total lignanoid that extracts in the Fructus Schisandrae Chinensis with by the Radix Astragali Mongolici total polysaccharide that extracts in the Radix Astragali.
The crude drug composition and the proportioning of pharmaceutical composition of the present invention are as follows:
Fructus Schisandrae Chinensis total lignanoid 1-5 weight portion
Radix Astragali Mongolici total polysaccharide 0.5-6 weight portion
The preparation method of the present composition is: get Fructus Schisandrae Chinensis, alcohol heating reflux with 10 times of amount 50-95% extracts 3 times, each 1.5-2 hour, merge extractive liquid,, behind the concentrating under reduced pressure, with 25-30% ethanol dilution concentrated solution, pass through macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 10kg macroporous resin packed column, earlier with 30% ethanol elution of 4-6 times of volume, again with 95% alcoholic solution eluting of 8-10 times of volume, collect eluent, 60 ℃ of concentrating under reduced pressure are dried to constant weight, promptly get Fructus Schisandrae Chinensis total lignanoid; Get the Radix Astragali, the water reflux, extract, 3 times that adds 10 times of amounts, each 1.5 hours, merge extractive liquid, was evaporated to relative density 1.25-1.4g/ml, the ethanol of adding 95% precipitates, after the placement, collecting precipitation, purification precipitate repeatedly, dry, promptly get Radix Astragali Mongolici total polysaccharide, perhaps behind the extracting solution concentrating under reduced pressure, pass through macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 10kg macroporous resin packed column, water with 12 times of volumes carries out eluting again, collects eluent, concentrates and promptly gets Radix Astragali Mongolici total polysaccharide, with above-mentioned two kinds of components by the proportioning mix homogeneously, at last directly or add pharmaceutically acceptable excipient and make clinical acceptable forms through conventional operation.
Described dosage form is injection, injectable powder, tablet, capsule, slow releasing tablet, drop pill, electuary, microgranule.
Described excipient is the conventional adjuvant of various preparations.
Make each efficacy of drugs produce synergism after the pharmaceutical composition of the present invention, obviously improve the hepatic injury of carbon tetrachloride induced mice, the necrosis of antagonism mouse liver cell.
The test example is used to further specify the present invention below.
The test of test example 1 prescription screening
Lung, the heart, kidney channel are returned in the sub-nature and flavor acid of five tastes of medicinal herb, sweet, warm, and function convergence is astringent or styptic treatment for spontaneous sweating, supplementing QI for promoting the production of body fluid, kidney calming, has tangible function for protecting liver and reducing enzyme activity, and its main active is a lignanoid.But result of use is undesirable separately, we are guidance with the Chinese medicine basic theories, in conjunction with modern pharmacology, adopt carbon tetrachloride acute liver damage mouse model, activity with the variation of murine liver tissue pathological section and serum T-BIL, D-BIL, TP, ALB, GLB, A/G, ALT, AST is an index, observes protecting the liver behind the medical material compatibilities such as Fructus Schisandrae Chinensis and Radix Et Rhizoma Rhei, Radix Salviae Miltiorrhizae, the Radix Astragali, the Radix Paeoniae Alba, Semen Astragali Complanati, Radix Bupleuri, Semen Cuscutae, Fructus Cnidii, effect of reducing enzyme levels.
1, experiment material
1.1 medicine
(1) is subjected to the reagent thing
Fructus Schisandrae Chinensis, the Radix Astragali, Radix Et Rhizoma Rhei, Radix Salviae Miltiorrhizae, the Radix Paeoniae Alba, Semen Astragali Complanati, Radix Bupleuri, Semen Cuscutae, Fructus cnidii extract.Extracting method is as follows.
Fructus Schisandrae Chinensis: the dry coarse powder of the material of getting it filled, with 10 times of amount 95% ethanol ultrasonic extraction 2 times, each 1h filters, and filtrate concentrates standby.
Radix Et Rhizoma Rhei: with 5 times of amount 75% ethanol ultrasonic extraction 2 times, each 1h filters, and filtrate concentrates standby.
Radix Salviae Miltiorrhizae: with 10 times of amount 95% ethanol, supersound extraction 2 times, each 1h filters, and filtrate concentrates standby.
The Radix Astragali: 8 times of water gagings, 65 ℃ of reflux, extract, 2 times, 1.5h+1h adds 2 times of amount 95% ethanol precipitations after being concentrated into 5 times of amounts, and taking precipitate is standby, is mainly the astragalus polysaccharides constituents through this precipitate of chemical composition analysis.
Radix Bupleuri: 80% ethanol, 10 times of amounts, supersound extraction 2 times, each 1h filters, and filtrate concentrates standby.
Semen Astragali Complanati: 10 times of ultrasonic 30 minutes of petroleum ether of amount+15 minute twice, the elimination petroleum ether, medicinal residues are flung to petroleum ether, with 10 times of amount 60% ethanol, supersound extraction 2 times, each 1h filters, and filtrate concentrates standby.
Fructus Cnidii: 95% ethanol, 10 times of amounts, supersound extraction 2 times, each 1h filters, and filtrate concentrates standby.
The Radix Paeoniae Alba: 10 times of amount 70% ethanol, supersound extraction 2 times, each 1h filters, and filtrate concentrates standby.
Semen Cuscutae: 95% ethanol, 10 times of amounts, supersound extraction 2 times, each 1h filters, and filtrate concentrates standby.
The Fructus Schisandrae Chinensis clinical dosage is by 2005 editions pharmacopeia regulation 6g, and animal is irritated stomach dosage 10 times in clinical dosage.Each extract and Fructus Schisandrae Chinensis extrat compatibility be all by 1: 1 proportional meter of crude drug, is made into 10% concentration with distilled water, and Fructus Schisandrae Chinensis extrat is made into 5% concentration, and cryopreservation is standby.
(2) positive drug
Bifendate drop pill: Zhejiang Medicine Co produces, batch number: 050910.Animal is pressed 150mg/kg.d-1, is made into 0.75% concentration with distilled water, and cryopreservation is standby.
1.2 animal
The ICR mice: male and female half and half, body weight 18-20g is provided by The 2nd Army Medical College Animal Experimental Study center.The quality certification number: SCXK (Shanghai) 2002-0006
1.3 instrument and reagent
Instrument: day island proper Tianjin fully automatic blood biochemistry analyzer.
Reagent: carbon tetrachloride solution, it is standby to be made into 1% concentration with Oleum Brassicae campestris.
2, experimental technique
Get 120 of ICR mices, male and female half and half, be divided into blank group, model group, positive group, Fructus Schisandrae Chinensis group, Fructus Schisandrae Chinensis+Radix Astragali group, Fructus Schisandrae Chinensis+Radix Et Rhizoma Rhei group, Fructus Schisandrae Chinensis+Radix Salviae Miltiorrhizae group, Fructus Schisandrae Chinensis+Radix Paeoniae Alba group, Fructus Schisandrae Chinensis+Semen Astragali Complanati group, Fructus Schisandrae Chinensis+Radix Bupleuri group, Fructus Schisandrae Chinensis+Semen Cuscutae group, Fructus Schisandrae Chinensis+Fructus Cnidii group at random, 10 every group.Irritate stomach distilled water, distilled water, bifendate and the corresponding reagent thing 20ml/kg.d that is subjected to respectively by group
-1, continuous 7d.The 7th day, 1h behind the filling stomach was except that the blank group, by group difference lumbar injection 1% carbon tetrachloride solution 10ml/kg.Behind the fasting 16h, pluck eyeball and get blood, with the centrifugal 15min of 3000r/min, separation of serum is measured total bilirubin (T-BIL), bilirubin direct (D-BIL), total protein (TP), albumin (ALB), globulin (GLB), albumins/globulins (A/G), alanine aminotransferase (ALT), Aspartic Acid transferring enzyme (AST) in the serum.Experimental result adopts SPSS 11.0 statistical software one factor analysis of variance to handle.
3, experimental result
After the modeling of model group mice 16 hours, serum T-BIL, D-BIL, ALT, AST obviously raise, and A/G obviously reduces, and with the blank group significant difference is arranged relatively.The prevention administration is after 7 days continuously, Fructus Schisandrae Chinensis group D-BIL, ALT, AST, Fructus Schisandrae Chinensis+Radix Astragali group T-BIL, D-BIL, TP, GLB, ALT, AST, Fructus Schisandrae Chinensis+Radix Bupleuri group ALT, AST, Fructus Schisandrae Chinensis+Radix Paeoniae Alba group D-BIL, Fructus Schisandrae Chinensis+Radix Salviae Miltiorrhizae group T-BIL, ALT, Fructus Schisandrae Chinensis+Fructus Cnidii group ALT, AST, Fructus Schisandrae Chinensis+Semen Astragali Complanati group T-BIL, D-BIL, TP, Fructus Schisandrae Chinensis+Radix Et Rhizoma Rhei group ALT, AST, Fructus Schisandrae Chinensis+Semen Cuscutae group T-BIL, D-BIL, ALT, AST obviously reduce; Fructus Schisandrae Chinensis+the Radix Paeoniae Alba group TP, ALB, Fructus Schisandrae Chinensis+Radix Astragali group A/G obviously raises; With model group significant difference is arranged relatively.Compare with the Fructus Schisandrae Chinensis group, Fructus Schisandrae Chinensis+Radix Astragali group T-BIL, GLB, AST obviously reduce, and A/G obviously raises; Fructus Schisandrae Chinensis+the Radix Paeoniae Alba group TP, ALB raises; Fructus Schisandrae Chinensis+Radix Et Rhizoma Rhei group ALB raises; Difference has significance.The result sees table 1 for details.
Table 1 Fructus Schisandrae Chinensis and with the other medicines compatibility after to the influence of carbon tetrachloride hepatic injury Mouse Liver function (X ± SD)
Annotate: compare △ P＜0.05, △ △ △ P＜0.001 with the blank group; Compare * P＜0.05, * * P＜0.01, * * * P＜0.001 with model group; Compare with the Fructus Schisandrae Chinensis group, ▲ P＜0.05, ▲ ▲ ▲ P＜0.001.
Each compatibility group of Fructus Schisandrae Chinensis group and Fructus Schisandrae Chinensis all has the effect that improves the Mouse Liver function in various degree, and is especially obvious to ALT and AST effect.In each administration group, Fructus Schisandrae Chinensis+Radix Astragali group effect is the most remarkable.Results suggest, Fructus Schisandrae Chinensis+Radix Astragali group are improved the liver function comprehensive function and are optimum than Fructus Schisandrae Chinensis group and other compatibility groups.
Test example 2 Study on extraction process
1 extracts the influence of solvent to the Lignanoids compounds extraction efficiency
Schisandra chinensis medicinal material 10g, difference water, 10%, 30%, 50%, 70% and 95% alcohol heating reflux extracts 2 times, and each 2 hours, after extracting solution merges, concentrating under reduced pressure is settled in the 50ml volumetric flask, measures the wherein content of Lignanoids compounds with the HPLC method.
As known from Table 2, along with the increase of concentration of alcohol, it is more little to extract solvent polarity, and the extraction efficiency of lignan component is high more in the Fructus Schisandrae Chinensis.
Table 2 extracts the influence of solvent to schisandra lignan chemical compound extraction efficiency
2 orthogonal tests
2.1 Orthogonal Experiment and Design
The main component of this prescription Chinese crude drug mostly is less polar composition, and extraction process adopts alcohol reflux, and four factors such as quantity of solvent, etoh solvent concentration, extraction time and extraction time are investigated the influence of extraction effect.This experiment is with the content size of the schisandrin in the sample, deoxyschizandrin, the schisandrin B investigation index as extraction effect.We select orthogonal test four factors three levels to carry out orthogonal test.
Experimental program such as table 3.
Table 3 L9 (34) orthogonal test scheme table
2.2 orthogonal experiments
With schisandrin, deoxyschizandrin, schisandrin B is that index orthogonal test analysis result is as shown in table 4, content is followed successively by eight＞four＞nine＞six＞two＞seven＞three＞five＞one, the factor affecting size is A＞D＞C＞B, be concentration of alcohol＞extraction time＞extraction time＞quantity of solvent, each factor optimum level is A
3B
3C
2D
3, promptly measure 90% ethanol extraction 3 times, each 1.5 hours for 10 times.
Table 4 is the orthogonal test analysis result of index with schisandrin, deoxyschizandrin, schisandrin B
| The experiment marshalling | A (concentration) | B (consumption) | C (time) | D (number of times) | Result (mg/ml) |
| One | 1(50％) | 1(6) | 1(1) | 1 | 0.45 |
| Two | 1(50％) | 2(8) | 2(1.5) | 2 | 0.87 |
| Three | 1(50％) | 3(10) | 3(2) | 3 | 0.76 |
| Four | 2(70％) | 1(6) | 2(1.5) | 3 | 0.98 |
| Five | 2(70％) | 2(8) | 3(2) | 1 | 0.66 |
| Six | 2(70％) | 3(10) | 1(1) | 2 | 0.87 |
| Seven | 3(90％) | 1(6) | 3(2) | 2 | 0.84 |
| Eight | 3(90％) | 2(8) | 2(1.5) | 3 | 1.00 |
| Nine | 3(90％) | 3(10) | 1(1) | 1 | 0.94 |
| I | 2.08 | 2.27 | 2.27 | 2.06 | |
| II | 2.52 | 2.52 | 2.84 | 2.58 | |
| III | 2.78 | 2.58 | 2.26 | 2.74 | |
| R | 0.70 | 0.17 | 0.58 | 0.68 |
The purification of 3 Fructus Schisandrae Chinensis total lignanoids
Schisandra chinensis medicinal material is measured 90% ethanol extractions 3 times with 10 times, each 1.5 hours, merge extractive liquid,, concentrating under reduced pressure became thick extractum, ethanol suspension extractum with 30%, make every milliliter to be equivalent to about 1g schisandra chinensis medicinal material, extracting solution by the AB-8 macroporous resin column, is used 30%, 50%, 70% and 95% ethanol elution respectively again, collect the each several part eluent, concentrating under reduced pressure, and dry to constant weight, the content of schisandra lignan component in the each several part measured with the HPLC method.
As shown in table 5, schisandra lignan component mainly is present in 50%, 70% and 95% the ethanol elution part.
The distribution of table 5 schisandra lignan component in different concentration ethanol
| Sample | Weight (g) | Schisandrin (%) | Deoxyschizandrin (%) | Schisandrin B (%) | Total content (%) |
| 30％EtOH | 17.46 | 0.18 | 0.05 | 0.08 | 0.31 |
| 50％EtOH | 6.65 | 13.48 | 2.83 | 0.25 | 16.56 |
| 70％EtOH | 6.79 | 5.66 | 16.34 | 38.58 | 60.58 |
| 95％EtOH | 6.59 | 10.59 | 12.26 | 30.42 | 53.27 |
According to The above results, we determine that the purification process of Lignanoids compounds in the Fructus Schisandrae Chinensis is: Fructus Schisandrae Chinensis extractive solution is by the AB-8 macroporous resin column, elder generation carries out eluting with 30% ethanol, then carry out eluting with 95% ethanol, 95% ethanol elution part concentrating under reduced pressure, dry to constant weight, be Fructus Schisandrae Chinensis total lignanoid.The results are shown in Table 6, wherein lignan component content is 54.34%
The distribution of table 6 schisandra lignan component in different concentration ethanol
| Sample | Weight (g) | Schisandrin (%) | Deoxyschizandrin (%) | Schisandrin B (%) | Total content (%) |
| 30％EtOH | 16.40 | 4.29 | - | - | 4.29 |
| 95％EtOH | 18.36 | 16.14 | 12.36 | 25.84 | 54.34 |
The preparation of 4 Radix Astragali Mongolici total polysaccharide
Milkvetch Root adds the water reflux, extract, 2 times after pulverizing, merge extractive liquid,, and behind the concentrating under reduced pressure, making relative density is 1g medical material/ml, and concentrated solution is by the AB-8 macroporous resin column, and water carries out eluting, and eluent decompression, vacuum drying promptly get Radix Astragali Mongolici total polysaccharide.Use ultraviolet spectrophotometry, with glucose as a standard product are measured, and the polysaccharide component content is 64% in the Radix Astragali Mongolici total polysaccharide.
The pharmacodynamics test of test example 3 Fructus Schisandrae Chinensis total lignanoids and Radix Astragali Mongolici total polysaccharide compositions
For the total lignans of investigating different proportionings and the drug effect of Radix Astragali Mongolici total polysaccharide, find the prescription of optimum curative effect, the design different tests is observed the influence to carbon tetrachloride hepatic injury Mouse Liver function of Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide.The proportioning of experimental selection is 1: 0.5,1: 1,1: 2,1: 4,1: 6, and Fructus Schisandrae Chinensis total lignanoid dosage is 0.02g/kg.Other adds positive controls bifendate drop pill, negative control group and model group.
Test is undertaken by the method for relevant reported literature, successive administration 7d.The 7th day, 1h behind the filling stomach was except that the blank group, by group difference lumbar injection 1% carbon tetrachloride solution 10ml/kg.Behind the fasting 16h, pluck eyeball and get blood, with the centrifugal 15min of 3000r/min, separation of serum is measured total bilirubin (T-BIL), bilirubin direct (D-BIL), total protein (TP), albumin (ALB), globulin (GLB), albumins/globulins (A/G), alanine aminotransferase (ALT), Aspartic Acid transferring enzyme (AST) in the serum.After getting blood, cut open and get liver, drop into 10% formalin internal fixation immediately, paraffin embedding, section, HE dyeing, optical microscope is observed down.The hepatic necrosis situation is carried out the classification score by following standard.Non-viable non-apoptotic cell is not seen in～(0 minute); + (1 minute) accidental lobule central authorities are dispersed in the hepatic necrosis kitchen range; ++ kitchen range shape necrosis of (2 minutes) minority lobule central cell or part lobule necrocytosis, but level is less; 3 minutes +++() non-viable non-apoptotic cell more extensively is present in lobules of liver central authorities, is kitchen range shape or lamellar; ++ ++ (4 minutes) non-viable non-apoptotic cell diffusivity is present in lobules of liver central authorities, and level is more.Experimental result adopts SPSS11.0 and DPS statistical software to handle.
Experimental result is as follows:
(1) Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide are to the influence of carbon tetrachloride hepatic injury Mouse Liver function
After the modeling of model group mice 16 hours, serum T-BIL, GLB, ALT, AST obviously raise, and A/G obviously reduces, and with the blank group significant difference is arranged relatively.The prevention administration is after 7 days continuously, and the every detection index of each proportion compatibility group all has in various degree to be improved.Wherein, 1: 0.5 group of T-BIL, D-BIL, 1: 1 group of T-BIL, GLB, ALT, AST, 1: 2 group of T-BIL, D-BIL, GLB, ALT, AST, 1: 4 group of T-BIL, 1: 6 group of T-BIL, D-BIL, GLB, ALT, AST obviously reduce; 1: 4 group and 1: 6 group of A/G obviously raise; Compare with model group, have significantly or utmost point significant difference.Compare there was no significant difference between 1: 4 group and 1: 6 group two groups.The result sees table 7 for details.
Each proportion compatibility group of table 7 is to the influence of carbon tetrachloride hepatic injury Mouse Liver function (X ± SD)
Annotate: compare △ P＜0.05, △ △ P＜0.01, △ △ △ P＜0.001 with the blank group; Compare * P＜0.05, * * P＜0.01, * * * P＜0.001 with model group.
(2) Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide are to the influence of carbon tetrachloride murine liver tissue damage
The blank group is not seen other abnormal changes except that the accidental lymphoid cell of individual animal soaks into.The model group mice occur extensively and diffusivity based on the Histological change of lobule center hepatic necrosis, necrosis region sees that hepatocyte has a liking for Yihong and strengthen, no normal hepatocytes plate structure, nuclear disappearance or examine and contract, as seen eosinkorper; And accidental ballooning degeneration of liver cells, cavity change, cloudy swelling and little focal hemorrhage and cell infiltration.Each administration group liver cell lesion all obviously alleviates, and with model group significance or utmost point significant difference is arranged relatively.The result sees table 8 for details.
Each proportioning dosage of table 8 is carefully to the influence of carbon tetrachloride hepatic necrosis mice
Annotate: compare △ △ △ P＜0.001 with the blank group; Compare * P＜0.05, * * P＜0.01, * * * P＜0.001 with model group.
Each proportion compatibility group of Fructus Schisandrae Chinensis lignanoid and Radix Astragali Mongolici total polysaccharide all can obviously be improved the hepatic injury of carbon tetrachloride induced mice, obviously resists the mouse liver cell necrosis.Wherein improve liver function with 1: 2 ratio compatibility and the hepatocyte injury comprehensive function is best with Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide.
The specific embodiment
Embodiment 1:
Fructus Schisandrae Chinensis total lignanoid 40g
Radix Astragali Mongolici total polysaccharide 20g
Get Fructus Schisandrae Chinensis 2kg, alcohol heating reflux with 10 times of amounts 95% extracts 3 times, each 1.5 hours, merge extractive liquid,, behind the concentrating under reduced pressure, 30% ethanol dilution concentrated solution with 2000ml, pass through ZTC-1 macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 2kg macroporous resin packed column, elder generation is with 30% ethanol elution of 6 times of volumes, again with 95% alcoholic solution eluting of 10 times of volumes, collect eluent, 60 ℃ of concentrating under reduced pressure are dried to constant weight, promptly get the Fructus Schisandrae Chinensis total lignanoid extract, wherein contain deoxyschizandrin, schisandrin B, schisantherin A and schisandrin are 56.8%; Get Radix Astragali 100g, the water reflux, extract, 3 times that adds 10 times of amounts, each 1.5 hours, merge extractive liquid,, be evaporated to relative density 1.25-1.4g/ml, the ethanol of adding 95% precipitates, after the placement, and collecting precipitation, to precipitate after repeatedly washing precipitate with ethanol, the taking precipitate drying promptly gets the Radix Astragali Mongolici total polysaccharide extract again, and the content of its Radix Astragali Mongolici total polysaccharide is 53.2%; By said ratio with Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide mix, drying, cross 100 mesh sieves, again 30g starch, 40g lactose were pulverized 100 mesh sieves, mixing.Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide compositions, 5g carboxymethyl starch sodium are added in the starch and lactose of mixing mixing.7% starch slurry that adds 100ml is mixed thoroughly, granulates through 16 order ferrum silk screen nets, and dry below 60 ℃, granulate adds 1% magnesium stearate 1.55g mixing, tabletting behind the analysis content.Can be made into 1000 every tablet tablet that contains Fructus Schisandrae Chinensis total lignanoid 40mg and Radix Astragali Mongolici total polysaccharide 20mg.Oral, every day 3 times, each 2.
Embodiment 2:
Fructus Schisandrae Chinensis total lignanoid 15g
Radix Astragali Mongolici total polysaccharide 45g
Get Fructus Schisandrae Chinensis 750g, alcohol heating reflux with 10 times of amounts 50% extracts 3 times, 2 hours for the first time, each 1.5 hours of second and third time, merge extractive liquid, is behind the concentrating under reduced pressure, with the 25% ethanol dilution concentrated solution of 750ml, pass through AB-8 macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 750g macroporous resin packed column.With 30% ethanol elution of 4 times of volumes, with 95% alcoholic solution eluting of 8 times of volumes, collect eluent more earlier, 60 ℃ of concentrating under reduced pressure, dry to constant weight, promptly get Fructus Schisandrae Chinensis total lignanoid, wherein containing deoxyschizandrin, schisandrin B, schisantherin A and schisandrin is 58.4%; Get Radix Astragali 225g, add the water reflux, extract, 3 times of 10 times of amounts, each 1.5 hours, merge extractive liquid, behind the concentrating under reduced pressure, by in the D-101 macroporous resin column, was promptly used 225g macroporous resin packed column according to amount of resin and medical material amount 1: 1.Water with 12 times of volumes carries out eluting again, collects eluent, concentrates and promptly gets the astragalus polysaccharides crude product, and repeatedly with after the washing with alcohol, drying promptly gets the Radix Astragali Mongolici total polysaccharide extract with the astragalus polysaccharides crude product, and the content of its Radix Astragali Mongolici total polysaccharide is 62.4%; By said ratio with Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide mix, drying, pulverized 100 mesh sieves, add in 160g starch, the 10g starch silica gel, mixing, directly incapsulate, can be made into 1000, every capsule that contains 15mg Fructus Schisandrae Chinensis total lignanoid and 45mg Radix Astragali Mongolici total polysaccharide.Oral, every day 3 times, each 2.
Embodiment 3:
Fructus Schisandrae Chinensis total lignanoid 85.7g
Radix Astragali Mongolici total polysaccharide 514.3g
Get Fructus Schisandrae Chinensis 4285g, alcohol heating reflux with 10 times of amounts 95% extracts 3 times, each 1.5 hours, merge extractive liquid,, behind the concentrating under reduced pressure, 30% ethanol dilution concentrated solution with 4285ml, pass through ZTC-1 macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 4285g macroporous resin packed column, elder generation is with 30% ethanol elution of 6 times of volumes, again with 95% alcoholic solution eluting of 10 times of volumes, collect eluent, 60 ℃ of concentrating under reduced pressure are dried to constant weight, promptly get the Fructus Schisandrae Chinensis total lignanoid extract, wherein contain deoxyschizandrin, schisandrin B, schisantherin A and schisandrin are 54.6%; Get Radix Astragali 2571.5g, the water reflux, extract, 3 times that adds 10 times of amounts, each 1.5 hours, merge extractive liquid,, be evaporated to relative density 1.25-1.4g/ml, the ethanol of adding 95% precipitates, after the placement, and collecting precipitation, to precipitate after repeatedly washing precipitate with ethanol, the taking precipitate drying promptly gets the Radix Astragali Mongolici total polysaccharide extract again, and the content of its Radix Astragali Mongolici total polysaccharide is 60.8%; By said ratio with Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide mix, dry, be crushed to 200 orders, join in the 200g sodium carboxymethyl cellulose (CMC-Na) that swelling is good, stir, add distilled water to 100000ml, stir into suspendible, promptly get every milliliter of suspensoid that contains Fructus Schisandrae Chinensis total lignanoid 0.0857mg and Radix Astragali Mongolici total polysaccharide 5.143mg.Oral, every day 3 times, each 20ml.
Embodiment 4:
Fructus Schisandrae Chinensis total lignanoid 50g
Radix Astragali Mongolici total polysaccharide 60g
Get Fructus Schisandrae Chinensis 2500g, alcohol heating reflux with 10 times of amounts 50% extracts 3 times, 2 hours for the first time, each 1.5 hours of second and third time, merge extractive liquid, is behind the concentrating under reduced pressure, with the 25% ethanol dilution concentrated solution of 2500ml, pass through AB-8 macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 2500g macroporous resin packed column.With 30% ethanol elution of 4 times of volumes, with 95% alcoholic solution eluting of 8 times of volumes, collect eluent more earlier, 60 ℃ of concentrating under reduced pressure, dry to constant weight, promptly get Fructus Schisandrae Chinensis total lignanoid, wherein containing deoxyschizandrin, schisandrin B, schisantherin A and schisandrin is 52.5%; Get Radix Astragali 300g, add the water reflux, extract, 3 times of 10 times of amounts, each 1.5 hours, merge extractive liquid, behind the concentrating under reduced pressure, by in the D-101 macroporous resin column, was promptly used 300g macroporous resin packed column according to amount of resin and medical material amount 1: 1.Water with 12 times of volumes carries out eluting again, collects eluent, concentrates and promptly gets the astragalus polysaccharides crude product, and repeatedly with after the washing with alcohol, drying promptly gets the Radix Astragali Mongolici total polysaccharide extract with the astragalus polysaccharides crude product, and the content of its Radix Astragali Mongolici total polysaccharide is 54.6%; By said ratio with Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide mix, drying, pulverized 100 mesh sieves, add in 160g starch, the 10g starch silica gel, mixing, directly incapsulate, can be made into 1000, every capsule that contains 50mg Fructus Schisandrae Chinensis total lignanoid and 60mg Radix Astragali Mongolici total polysaccharide.Oral, every day 3 times, each 2.
Embodiment 5:
Fructus Schisandrae Chinensis total lignanoid 25g
Radix Astragali Mongolici total polysaccharide 50g
Get Fructus Schisandrae Chinensis 1250g, alcohol heating reflux with 10 times of amounts 95% extracts 3 times, each 1.5 hours, merge extractive liquid,, behind the concentrating under reduced pressure, 30% ethanol dilution concentrated solution with 1250ml, pass through ZTC-1 macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use 1250g macroporous resin packed column, elder generation is with 30% ethanol elution of 6 times of volumes, again with 95% alcoholic solution eluting of 10 times of volumes, collect eluent, 60 ℃ of concentrating under reduced pressure are dried to constant weight, promptly get the Fructus Schisandrae Chinensis total lignanoid extract, wherein contain deoxyschizandrin, schisandrin B, schisantherin A and schisandrin are 60%; Get Radix Astragali 250g, the water reflux, extract, 3 times that adds 10 times of amounts, each 1.5 hours, merge extractive liquid,, be evaporated to relative density 1.25-1.4g/ml, the ethanol of adding 95% precipitates, after the placement, and collecting precipitation, to precipitate after repeatedly washing precipitate with ethanol, the taking precipitate drying promptly gets the Radix Astragali Mongolici total polysaccharide extract again, and the content of its Radix Astragali Mongolici total polysaccharide is 65%; By said ratio with Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide mix, drying, cross 100 mesh sieves, again 30g starch, 40g lactose were pulverized 100 mesh sieves, mixing.Fructus Schisandrae Chinensis total lignanoid and Radix Astragali Mongolici total polysaccharide compositions, 5g carboxymethyl starch sodium are added in the starch and lactose of mixing mixing.7% starch slurry that adds 100ml is mixed thoroughly, granulates through 16 order ferrum silk screen nets, and dry below 60 ℃, granulate adds 1% magnesium stearate 1.55g mixing, tabletting behind the analysis content.Can be made into 1000 every tablet tablet that contains Fructus Schisandrae Chinensis total lignanoid 25mg and Radix Astragali Mongolici total polysaccharide 50mg.Oral, every day 3 times, each 2.
Claims (2)
1. effective ingredient in Chinese compound preparation with hepatoprotective effect, it is characterized in that: this compound preparation is made by following raw material medicaments:
Fructus Schisandrae Chinensis total lignanoid 1-5 weight portion
Radix Astragali Mongolici total polysaccharide 0.5-6 weight portion
Wherein Fructus Schisandrae Chinensis total lignanoid is made by following method: get Fructus Schisandrae Chinensis, alcohol heating reflux with 10 times of amount 50-95% extracts 3 times, each 1.5-2 hour, merge extractive liquid,, behind the concentrating under reduced pressure, with 25-30% ethanol dilution concentrated solution, pass through macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use the macroporous resin packed column, earlier with 30% ethanol elution of 4-6 times of volume, again with 95% alcoholic solution eluting of 8-10 times of volume, collect eluent, 60 ℃ of concentrating under reduced pressure are dried to constant weight, promptly get Fructus Schisandrae Chinensis total lignanoid;
Wherein Radix Astragali Mongolici total polysaccharide is made by following method: get the Radix Astragali, the water reflux, extract, 3 times that adds 10 times of amounts, each 1.5 hours, merge extractive liquid,, be evaporated to relative density 1.25-1.4g/ml, the ethanol of adding 95% precipitates, after the placement, collecting precipitation, purification precipitate repeatedly, drying promptly gets Radix Astragali Mongolici total polysaccharide, perhaps behind the extracting solution concentrating under reduced pressure, pass through macroporous resin column at 1: 1 according to amount of resin and medical material amount, promptly use the macroporous resin packed column, the water with 12 times of volumes carries out eluting again, collect eluent, concentrate and promptly get Radix Astragali Mongolici total polysaccharide.
2. a kind of effective ingredient in Chinese compound preparation with hepatoprotective effect according to claim 1 is treated in preparation, the medicine of prevention hepatic injury reaches has the health-care effect Application in Food to hepatic injury.
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| FR3044577B1 (en) | 2015-12-07 | 2017-12-22 | Timothee Boitouzet | METHOD FOR PARTIAL DELIGNIFICATION AND FILLING OF A LIGNOCELLULOSIC MATERIAL, AND STRUCTURE OF COMPOSITE MATERIAL OBTAINED BY THIS PROCESS |
| FR3077895B1 (en) | 2018-02-09 | 2020-02-28 | Sas Woodoo | TACTILE DETECTION DEVICE WITH TACTILE INTERFACE IN COMPOSITE MATERIAL |
| FR3067275B1 (en) | 2017-06-07 | 2022-08-12 | Timothee Boitouzet | PROCESS FOR PARTIAL DELIGNIFICATION BY SUPERCRITICAL OR SUBCRITICAL ROUTE AND FILLING OF A LIGNO-CELLULOSIC MATERIAL |
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