CN1299694C - Flavone composition for sobering and liver protection and its use - Google Patents
Flavone composition for sobering and liver protection and its use Download PDFInfo
- Publication number
- CN1299694C CN1299694C CNB2005100536170A CN200510053617A CN1299694C CN 1299694 C CN1299694 C CN 1299694C CN B2005100536170 A CNB2005100536170 A CN B2005100536170A CN 200510053617 A CN200510053617 A CN 200510053617A CN 1299694 C CN1299694 C CN 1299694C
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- Prior art keywords
- flavone
- composition
- medicine
- preparation
- puerarin
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Abstract
The present invention discloses flavone composition for obviously lightening the damage of a machine body because of excess ethanol ingestion, which is composed of puerarin flavone and silymarin flavone. Discovered from the study, puerarin flavone and the silymarin flavone have obvious synergy on the aspects of oxidation resistance, liver protection and ethanol elimination in a body, and the present invention also discloses the application of the composition in the field of health care food and medicine.
Description
Technical field
This invention discloses a kind of flavone composition that is applied to medicine, field of health care food, is specifically related to said composition and is applied to prevent and treat with different preparations carriers and damages due to the excessive consumption of alcohol.
Background technology
It is a kind of ancient general drinking in China, and long traditional social usage is arranged.China is one of country of early start wine brewing in the world, and the Xia dynasty before apart from modern more than 4000 year just utilizes grain to be raw material, the record of brewed wine.China remains the country of alcoholic beverage volume of production and marketing maximum in the world at present.Be accompanied by the strong growth of China's economic, the volume of production and marketing of annual alcoholic beverage increases above 25%.
Right amount alcohol is taken in the inhibit feature that can make brain and is reduced, thereby reaches the effect that body and mind loosens, and modern medicine study shows that also responsible drinking can reduce the sickness rate of cardiovascular and cerebrovascular disease.But excessive consumption of alcohol is a global social problem at present, and it is disease, injury, violence that hazardness is drunk, particularly at one of women and child's violence, deformity, social problem and early death most important basic reason.Excessive consumption of alcohol produces serious noci-influence to health, studies show that excessive consumption of alcohol can cause diseases such as liver cirrhosis, hepatocarcinoma, hypertension, apoplexy, also comprise simultaneously owing to drive when intoxicated causing injury etc. in the vehicle accident, strengthened the burden of family and society.
Reason in China owing to profound levels such as Social Culture; and present economy of living in high speed developing period; spirits culture all must be faced in the different personnel's of stratum social activity; reducing ethanol is the makeshift that is not able to health affected; before ethanol is taken in reduction positive, initiatively, adopt medicament protection alcohol user's health, have great social significance; this is not to be to encourage to drink, but can effectively alleviate the burden of society and family.
Summary of the invention
Liver is directly seriously involved in excessive consumption of alcohol, because liver is the chemical plant of human body, ethanol is transferred to liver with blood after gastrointestinal absorption, carry out metabolism and elimination at liver.Oral enter intravital ethanol surpass 80% in liver by the cytochrome p450 system metabolism.Earlier be oxidized to acetaldehyde by cytosol and Intramitochondrial ethanol dehydrogenase, that continues is oxidized to acetic acid by aldehyde dehydrogenase in the mitochondrion, and last acetic acid is released into blood by liver, becomes carbon dioxide and water at the periphery tissue oxidizing.Ethanol can produce a large amount of free radicals in the process of liver intracellular metabolite, produced simultaneously intermediate acetaldehyde can be to P450 enzyme system and glutathion combination in the body, and influence is to the elimination effect of free radical; The free radical of piling up in the liver can cause the liver plasma membrane lipid peroxidation, and disrupting biofilm flowability, permeability and integrity finally cause the pathology of liver to change, and cause alcoholic fatty liver, hepatitis, liver cirrhosis etc.
In the middle of the research process to the Natural antioxidant, we find that unexpectedly puerarin and silymarin have powerful synergism aspect the reduction liver oxidative damage.Systematic study shows that the flavone composition that is made of puerarin and silymarin not only has extremely significant synergism aspect the anti-liver oxidative damage, and aspect the ethanol elimination certain synergism is arranged also in promoting body.
One, flavone composition is at the test data that protects the liver aspect the antioxidation
Experimental animal model:
Ethanol chronic hepatic injury model
Adopt the Wistar rat, oral administration gavage gives 60% alcoholic solution, and dosage is 5ml/kg (the weight of animals), gives 75 continuously, and duration of test gives animal pattern simultaneously and lacks nutritional feed.Be subjected to the reagent thing to adopt preventive administration, measure the serological index of animal subject after the off-test: AST, ALT; And some other liver indexs: hepatic tissue lipid peroxide (LPO), glutathion (GSH), glutathion peroxidase indexs such as (GSH-Px).
Be subjected to reagent thing and dosage thereof:
| Ratio silymarin/puerarin | Dosage mg/kg (the weight of animals) | |
| Silymarin group 1 | - | 50 |
| Silymarin group 2 | - | 100 |
| Puerarin group 1 | - | 150 |
| Puerarin group 2 | - | 300 |
| Compositions group 1 | 1∶3 | 200 |
| Compositions group 2 | 1∶3 | 300 |
Test data:
| Number of animals (n) | AST(u/L) | ALT(u/L) | Hepatic tissue LPO (nmol/g) | Hepatic tissue GSH (μ g/g) | Liver is carefully knitted GSH-Px (u/ml) | |
| The blank group | 10 | 75.1±12.5 | 33.2±8.7 | 30.2±15.1 | 913.4±115.3 | 66.7±3.1 |
| The pathological model group | 12 | 136.9±33.9 | 59.6±15.1 | 66.7±17.5 | 442.1±101.7 | 41.9±2.9 |
| Silymarin group 1 | 12 | 88.3±25.2 ** | 44.8±18.3 * | 39.6±17.6 ** | 790.5±124.8 ** | 54.9±3.4 * |
| Silymarin group 2 | 12 | 71.2±22.6 ** | 39.6±13.2 ** | 34.5±10.9 ** | 879.6±123.6 ** | 60.8±4.4 ** |
| Puerarin group 1 | 12 | 128.7±38.2 | 60.3±18.5 | 44.9±19.0 * | 456.3±89.9 | 50.2±5.1 |
| Puerarin group 2 | 12 | 101.2±27.9 * | 51.7±18.2 | 40.5±15.9 * | 523.4±99.1 * | 55.3±3.4 * |
| Compositions group 1 | 12 | 86.3±22.4 ** | 42.1±16.6 * | 30.3±13.8 ** | 821.5±111.6 ** | 60.9±3.8 ** |
| Compositions group 2 | 12 | 66.7±17.5 *** | 35.8±9.8 ** | 25.4±11.9 *** | 932.4±121.4 *** | 667±4.0 ** |
Compare with matched group:
*Show P＜0.05;
*Show P＜0.01;
* *Show P＜0.001
According to above-mentioned test data, can learn with single Flavonoid substances and compare, the compositions of puerarin and silymarin significantly is lower than the respective value 71.2 ± 22.6 (P＜0.05) and puerarin group 2 respective value 101.2 ± 27.9 (P＜0.01) of silymarin group 2 having certain synergism aspect the reduction liver oxidative damage as the AST value 66.7 ± 17.5 of compositions 2.
Aspect antioxidation, then shown very significant synergism, show that liver is caused the variation of oxidisability index by ethanol: reduced the generation of peroxide, as the decline of LPO index; Strengthen the detoxification system of liver, the data of promptly eliminating some reproducibility indexs of peroxide injury rise, as GSH, GSH-Px.The significant difference of the These parameters data of compositions and the index of single Flavonoid substances has shown the synergism aspect antioxidation between the different material.
Two, flavone composition test data aspect the ethanol in eliminating body
Adopt the Wistar rat, fasting 12h, oral administration gavage give 60% alcoholic solution, and dosage is 10ml/kg, and medicine adopts preventive administration, 3d administration in advance, and bid, dosage is followed successively by: puerarin 150mg/kg; Compositions group 1 200mg/kg; Compositions group 2 300mg/kg; Behind the animals received ethanol 1,2,3,5h posterior orbit venous blood collection, the BAC method is measured ethanol content.
Result of the test shows that giving silymarin separately eliminates basic not influence (free of data) to the intravital ethanol of animal subject, puerarin can influence alcoholic acid elimination, but find that unexpectedly flavone composition has significant synergism aspect the intravital ethanol of elimination animal subject, have certain dose-effect relationship simultaneously, concrete test data sees table.
| Blood determining alcohol (mg/L) | 0.5h | 1h | 2h | 3h | 5h | |
| Matched group | 66.7±5.9 | 93.8±8.6 | 87.5±5.7 | 81.2±4.5 | 75.2±6.6 | |
| The puerarin group | 60.7±3.9 | 88.7±6.7 | 80.5±4.4 | 70.5±3.5 | 61.2±2.9 | P＜0.05 |
| Compositions group 1 | 48.9±3.1 | 75.7±4.6 | 70.4±3.3 | 62.3±2.2 | 50.2±1.9 | P＜0.01 |
| Compositions group 2 | 41.2±2.3 | 69.8±5.9 | 63.7±4.2 | 55.8±3.1 | 45.1±2.1 | P＜0.001 |
Each is organized animal subject and accepts that the blood determining alcohol figure of different time sees Figure of description behind the ethanol
The composition that above-mentioned test data has shown kudzu root flavone, Herba Silybi mariani flavone anti-oxidant, to protect the liver, relieve the effect of alcohol act synergistically aspect three significantly; In conjunction with other datas, " accident " effect has positive effect aspect the elimination excessive consumption of alcohol between this flavone composition as can be known. It may be to obtain by following factor that comprehensive literature and our research data, above-mentioned significant synergy obtain:
(1) promote the alcohol dehydrogenase effect, accelerating alcohol is to the metabolism of acetaldehyde. Kudzu root flavone is a kind of medicament for expanding vascellum still not, and present such material that studies show that may have the effect that activates alcohol dehydrogenase;
(2) Herba Silybi mariani flavone can be eliminated the metabolite acetaldehyde of ethanol fast as a kind of natural, has indirectly promoted the metabolism of ethanol to acetaldehyde;
(3) reduce the generation of free radical in the liver by above-mentioned link, alleviated the damage of alcohol to liver;
(4) the liver plasma membrane protective effect that possesses of milk thistle is strengthened via Puerarin.
Three, the preparation of flavone composition
Kudzu root flavone
The dry root of legume pueraria lobata Pueraria lobata or sweet kudzu Pueraria thomsonii, it is the medicinal material that permanent applicating history is arranged in the middle of the traditional Chinese medical science simply, modern study shows that the Flavonoid substances in the middle of the root of kudzu vine has stronger vasodilative effect, is mainly used in the treatment cardiovascular and cerebrovascular disease at present. In the middle of traditional medicine, the root of kudzu vine and FI puerariae are regarded as the good medicine that relieves the effect of alcohol always, the traditional Chinese medical science use root of kudzu vine relieving alcoholism have more than 4000 year history as in " prescriptions worth thousand gold ", putting down in writing " root of kudzu vine master relieving alcoholism ".
The present kudzu root flavone system that studies show that is made of a series of isoflavone like substance, is mainly Puerarin, and other comprise daidzin, daidzein etc. The related kudzu root flavone of this invention can be selected from Puerarin, daidzin, daidzein, and contains the Kudzu Flavonoids Extracts that surpasses 20% Puerarin. Present conventional method preparation (being mainly chromatography or solvent method) is adopted in the preparation of Puerarin and Kudzu Flavonoids Extracts, because Puerarin is to use clinically more cardiovascular medicament, so Puerarin or the at present existing more data of the preparation of Kudzu Flavonoids Extracts are published.
Herba Silybi mariani flavone
Milk thistle is composite family artichoke plant milk thistle Silybum marianum fruit, and the Flavonoid substances in the middle of its fruit has hepatoprotective effect, Haller first Application milk thistle treatment liver disease in 1755; China introduced milk thistle in 1972 from Germany, in the success of various places popularizing planting.
Use in the medicine that protects the liver clinically at present, silymarin, legalon, silybin derivant all derive from the extract of milk thistle, and active material all is flavonoids. Use wider with silymarin at present. Silymarin is one mainly to comprise the mixture of the materials such as legalon (silybin), silydianin (silidianin), silicristin (silichristin) and Isosilybin (isosilybin). The content of legalon is the highest in the middle of these compounds, and activity is also the strongest. The Herba Silybi mariani flavone that this invention relates to is selected from silymarin, legalon, Silibinin-n-methylglucamine and other contain the Herba Silybi mariani flavone extract that surpasses 20% legalon. Because silymarin, legalon extensively have application clinically, so its extraction and preparation technique adopts present conventional method preparation (being mainly solvent method).
Appropriate solvent is adopted in the preparation of kudzu root flavone Herba Silybi mariani flavone composition, after two kinds of substance dissolves, flings to solvent, is drying to obtain. Because kudzu root flavone and Herba Silybi mariani flavone lattice energy are all higher, poor solubility; Before making preparation, this flavone composition and suitable carrier can be made solid dispersions, to improve dissolution rate and the bioavilability of the preparation of being made by this flavone composition. Also can adopt flavone composition is carried out first the micronize processing, improve the stripping of preparation.
In sum, this invention requires as follows:
1, a kind of flavone composition for Antialcoholic liver-protecting is characterized in that described composition is comprised of kudzu root flavone and Herba Silybi mariani flavone.
2, compositions according to claim 1 is characterized in that two kinds of flavone have the following weight proportioning:
10～600 parts of 50～600 parts of Herba Silybi mariani flavones of Radix Puerariae flavone.
3, compositions according to claim 1 and 2 is characterized in that described Herba Silybi mariani flavone is selected from silymarin, silibinin, and contains and surpass in the Herba Silybi mariani flavone extract of 20% silibinin any.
4, compositions according to claim 1 is characterized in that described Radix Puerariae refers to that described Radix Puerariae flavone is puerarin, daiazi from pulse family Pueraria lobota platymiscium Herba Gelsemii Elegantis or Radix Puerariae, and contains and surpass in the Radix Puerariae flavone extract of 20% puerarin any.
5, the application of a kind of flavone composition according to claim 1 in the preparation medicine.
6, a kind of according to the application of the described flavone composition of claim 1 in the preparation health food.
7, according to the described flavone composition of claim 5 in the application of preparation in the medicine, it is characterized in that described medicine made by this flavone composition and pharmaceutically acceptable excipient.
8, the application of flavone composition according to claim 5 in the preparation medicine is characterized in that flavone composition being made solid dispersion or carrying out micronize and handle, to improve the dissolution of the oral solid formulation of being made by this flavone composition; Described solid dispersion be flavone composition and phospholipid, Polyethylene Glycol, polyvinylpyrrolidone any make.
9, the application of flavone composition according to claim 5 in the preparation medicine, the dosage form that it is characterized in that described medicine is any in conventional tablet, dispersible tablet, effervescent tablet, soft capsule, drop pill, hard capsule, granule and the oral liquid.
10, a kind of flavone composition according to claim 5 is in the application of preparation in the medicine, it is characterized in that adding in the nutrient substance of following promotion liver metabolism one or more in the middle of described medicine: vitamin, aminoacid, soybean phospholipid, inosine, coenzyme, taurine.
The specific embodiment
The preparation of embodiment 1, flavone composition phospholipid solid dispersion
The principal agent proportioning:
Puerarin 100g
Silymarin 100g
Soybean phospholipid 20g
Take by weighing principal agent and adjuvant soybean phospholipid according to said ratio, place in the middle of the round-bottomed flask of 2000ml, add 95% ethanol 800ml, be heated to the total material dissolving, solvent is flung in decompression, and drying promptly gets the flavone composition solid dispersion.
Embodiment 2, flavone composition preparation tablets 1
Tablet formulation:
Puerarin 200g
Silymarin 100g
Microcrystalline Cellulose 75g
Lactose 80g
Hyprolose 25g
95% ethanol q.s.
Cross-linking sodium carboxymethyl cellulose 25g
Micropowder silica gel 3g
Make 1000
Method for making: according to above-mentioned preparation prescription, take by weighing principal agent puerarin and silymarin, add microcrystalline Cellulose, lactose and 15g hydroxypropyl cellulose, with 95% alcohol granulation, 60 ℃ of dryings, granulate; Add tabletting behind all the other adjuvant mix homogeneously, make 1000.
Embodiment 3, flavone composition preparation tablets 2
Tablet formulation:
Puerarin 240g
Silibinin 60g
Vc 20g
Inosine 50g
Microcrystalline Cellulose 75g
Pregelatinized Starch 75g
Hyprolose 25g
Calcium sulfate 50g
Micropowder silica gel 3g
Make 1000
Method for making: according to above-mentioned preparation prescription, take by weighing principal agent and cross 100 mesh sieves, adjuvant is also crossed 100 mesh sieves, and principal agent after sieving and adjuvant are fully mixed, and direct compression is made 1000, packing, promptly.
Embodiment 4, flavone composition granule
Preparation prescription:
Herba Silybi mariani flavone extract 500g
Puerarin 50g
Pig liver extract 300g
Microcrystalline Cellulose 100g
Sodium benzoate 3.0g
Cross-linking sodium carboxymethyl cellulose 30g
Sodium lauryl sulphate 3g
CHENPI DING 20ml
Sucrose 1600g
Make 1000 bags
Method for making: after mistake 80 is sieved respectively with principal agent, cross-linking sodium carboxymethyl cellulose, mix with sucrose in the middle of putting blender, with sodium benzoate, CHENPI DING, the sodium lauryl sulphate wetting agent of making soluble in water: with above-mentioned principal agent and wetting agent mixing, granulate, drying is crossed 30 mesh sieve granulate, packing, packing promptly gets granule.
Embodiment 5, flavone composition capsule
Preparation prescription:
Silymarin 90g
Puerarin 100g
Soybean phospholipid 20g
Pregelatinized Starch 20g
Carboxymethyl starch sodium 10g
SDS 3.0g
Mannitol 30g
Make 1000
Preparation: at first flavone composition and phospholipid are made solid dispersion according to the method among the embodiment 1; Get solid dispersion, cross 100 mesh sieves,, encapsulated after all the other adjuvants sieve with the major ingredient mix homogeneously, packing, promptly.
Embodiment 6, flavone composition soft capsule
Preparation prescription:
Silibinin 30g
Radix Puerariae total flavones (containing 60% puerarin) 200g
PVP 20g
Propylene glycol 30g
Water 10g
PEG400 210g
Make 1000
Preparation: at first flavone composition and PVP (polyvinylpyrrolidone) are made solid dispersion according to the method among the embodiment 1; Get solid dispersion, with substrate mixing, compression moulding, packing, promptly.
Embodiment 7, the preparation of flavone composition dispersible tablet
Preparation prescription:
Silibinin 70g
Puerarin 200g
Soybean phospholipid 27g
Mannitol 100g
CMS-Na 25g
Microcrystalline Cellulose 100g
L-HPC 25g
Crosslinked CMC-Na 25g
5％PVP
K30 100g
Magnesium stearate 3g
Micropowder silica gel 6g
Make 1000
According to above-mentioned dispersible tablet formulation, get silibinin, puerarin and soybean phospholipid and make solid dispersion according to the method described in the embodiment 1; Get solid dispersion and carry out micronize and handle, above-mentioned solid dispersion is placed in the middle of the jet mill, fully pulverize, cross 400 mesh sieves.
Get above-mentioned micronize flavone composition, the CMS-Na that adds microcrystalline Cellulose, crosslinked CMC-Na, 1/3 recipe quantity puts in the wet-mixing granulator, and mixed 2min adds adhesive (5% PVP
K30Alcoholic solution), 30 mesh sieves are granulated, 50～80 ℃ of dryings; Dried granule is crossed 20 mesh sieve granulate, adds magnesium stearate and micropowder silica gel in the middle of dried particles, and the CMS-Na and the remaining mannitol that remain 2/3, mixing, and tabletting, packing promptly gets the compositions dispersible tablet.
The compositions dispersible tablet that makes according to above-mentioned preparation prescription is no more than 10min disintegration; Silibinin 30min dissolution is not less than 80%, and puerarin 30min dissolution is not less than 90%.
Embodiment 8, the preparation of flavone composition effervescent tablet
Preparation prescription:
Silibinin 35g
Puerarin 70g
Taurine 30g
Must aminoacid 60g
DPN diphosphopyridine nucleotide 0g
Cyclamate 10g
Saccharin sodium 1g
Citric acid 175g
Sodium bicarbonate 125g
Micropowder silica gel 3g
Make 1000
Method for making: main materials and auxiliary materials is crossed 100 mesh sieves respectively, 50～60 ℃ of dry 3h of principal agent, and 80 ℃ of dry 3h of adjuvant, under the condition of relative humidity less than RH45%, each supplementary material mixing, tabletting, check packs, promptly immediately.
Embodiment 9, the preparation of flavone composition drop pill
Silibinin 10g
Puerarin 20g
Soybean phospholipid 5g
PEG4000 9.0g
PEG6000 15g
Make 1000
Method for making: 9.0g Macrogol 4000 and 13.5g polyethylene glycol 6000 are put in the container, heating and melting in 85～90 ℃ oil bath, add silibinin and puerarin immediately, stir, move into drop pill machine reservoir then, airtight and the insulation at 80～85 ℃, the system of dripping, the drop pill that oozes cools off through 10～15 ℃ liquid paraffin, and drop is paraffin to the greatest extent, make 1000, promptly.
Embodiment 10, composition oral liquid preparation preparation
Silibinin phthalic monoester sodium salt 20g
Radix Puerariae flavone extract (containing puerarin 30%) 800g
Ethyl hydroxybenzoate 0.5g
Cyclamate 10g
Saccharin sodium 1g
Menthol spirit 10ml
Distilled water adds to 15000ml
Make 1000 bottles
Method for making: get distilled water 1000ml, boil, add cyclamate, saccharin sodium and ethyl hydroxybenzoate, after the stirring and dissolving, filter, add principal agent in the filtrate, stirring and dissolving is put coldly, adds menthol spirit and an amount of distilled water, and making full dose is 15000ml, stir evenly, sterilization, packing, promptly.
Claims (10)
1, a kind of flavone composition that is used for Antialcoholic liver-protecting is characterized in that described compositions is made up of Radix Puerariae flavone and Herba Silybi mariani flavone.
2, compositions according to claim 1 is characterized in that two kinds of flavone have the following weight proportioning:
10～600 parts of 50～600 parts of Herba Silybi mariani flavones of Radix Puerariae flavone.
3, compositions according to claim 1 and 2 is characterized in that described Herba Silybi mariani flavone is selected from silymarin, silibinin, and contains and surpass in the Herba Silybi mariani flavone extract of 20% silibinin any.
4, compositions according to claim 1 is characterized in that described Radix Puerariae refers to that described Radix Puerariae flavone is puerarin, daiazi from pulse family Pueraria lobota platymiscium Herba Gelsemii Elegantis or Radix Puerariae, and contains and surpass in the Radix Puerariae flavone extract of 20% puerarin any.
5, a kind of according to the application of the described flavone composition of claim 1 in the preparation medicine.
6, a kind of according to the application of the described flavone composition of claim 1 in the preparation health food.
7, flavone composition according to claim 5 is in the application of preparation in the medicine, it is characterized in that described medicine made by this flavone composition and pharmaceutically acceptable excipient.
8, the application of flavone composition according to claim 5 in the preparation medicine is characterized in that flavone composition being made solid dispersion or carrying out micronize and handle, to improve the dissolution of the oral solid formulation of being made by this flavone composition; Solid dispersion be flavone composition and phospholipid, Polyethylene Glycol, polyvinylpyrrolidone any make.
9, the application of flavone composition according to claim 5 in the preparation medicine, the dosage form that it is characterized in that described medicine is any in conventional tablet, dispersible tablet, effervescent tablet, soft capsule, drop pill, hard capsule, granule and the oral liquid.
10, a kind of flavone composition according to claim 5 is in the application of preparation in the medicine, it is characterized in that adding in the middle of the described medicine in the nutrient substance of following promotion liver metabolism one or more: vitamin, aminoacid, soybean phospholipid, inosine, coenzyme, taurine.
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| CNB2005100536170A CN1299694C (en) | 2005-03-09 | 2005-03-09 | Flavone composition for sobering and liver protection and its use |
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| CNB2005100536170A CN1299694C (en) | 2005-03-09 | 2005-03-09 | Flavone composition for sobering and liver protection and its use |
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| CN1299694C true CN1299694C (en) | 2007-02-14 |
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| CN102599503B (en) * | 2012-03-14 | 2014-04-16 | 上海善力健保健食品有限公司 | Sober-up and liver-protecting health food and making method thereof |
| CN102671066A (en) * | 2012-05-18 | 2012-09-19 | 江西农业大学 | Hangover-alleviating compound and preparation method thereof |
| CN103623046A (en) * | 2013-12-24 | 2014-03-12 | 浙江康乐药业股份有限公司 | Composite playing auxiliary protection role in chemical and alcoholic liver injury, preparation method of composite and application of composite in health-care food |
| CN105942497A (en) * | 2016-05-04 | 2016-09-21 | 江苏神华药业有限公司 | Composition with effects of neutralizing effect of alcoholic drinks and nourishing liver and preparation method of composition |
| CN106721793A (en) * | 2016-12-05 | 2017-05-31 | 张俊宝 | A kind of caulis bambusae in taenian hangover-alleviating health-care oral liquid |
| CN108244658B (en) * | 2018-04-20 | 2021-08-20 | 大连军门保健食品有限公司 | An anti-hangover and hepatoprotective agent containing herba Cichorii nutrients, and its preparation method |
| CN110432418A (en) * | 2018-05-05 | 2019-11-12 | 陈泂杉 | A kind of production method of liver-protecting and alcoholism-relieving drink |
| CN110038044A (en) * | 2019-04-23 | 2019-07-23 | 陈飞筱 | A kind of alcohol-decomposing powder and preparation method thereof |
| CN110237155A (en) * | 2019-07-31 | 2019-09-17 | 王鹏 | One kind sober up patch and preparation method thereof |
| CN111494564B (en) * | 2020-04-30 | 2021-07-27 | 江苏中兴药业有限公司 | Preparation method of compound liver-protecting and alcohol-dispelling tablet |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1163127A (en) * | 1996-04-25 | 1997-10-29 | 赵爱平 | Puerarin and its extracting method |
| CN1188800A (en) * | 1997-01-22 | 1998-07-29 | 山东省达瀚实业总公司 | Wine with liver protective function and making method thereof |
| US20040162270A1 (en) * | 2003-02-18 | 2004-08-19 | Better Living Chemistry | Compositions for prevention and treatment of symptoms associated with ethyl alcohol consumption |
| CN1560062A (en) * | 2004-03-11 | 2005-01-05 | 白栓锁 | Process of extracting puerariae and making food and medicine addied with it |
-
2005
- 2005-03-09 CN CNB2005100536170A patent/CN1299694C/en not_active Expired - Fee Related
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1163127A (en) * | 1996-04-25 | 1997-10-29 | 赵爱平 | Puerarin and its extracting method |
| CN1188800A (en) * | 1997-01-22 | 1998-07-29 | 山东省达瀚实业总公司 | Wine with liver protective function and making method thereof |
| US20040162270A1 (en) * | 2003-02-18 | 2004-08-19 | Better Living Chemistry | Compositions for prevention and treatment of symptoms associated with ethyl alcohol consumption |
| CN1560062A (en) * | 2004-03-11 | 2005-01-05 | 白栓锁 | Process of extracting puerariae and making food and medicine addied with it |
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