CN112007092A

CN112007092A - Anti-alcohol composition and preparation method thereof

Info

Publication number: CN112007092A
Application number: CN202011053587.4A
Authority: CN
Inventors: 梁京
Original assignee: Beijing Jiafurui Biological Technology Co ltd
Current assignee: Beijing Jiafurui Biological Technology Co ltd
Priority date: 2020-09-29
Filing date: 2020-09-29
Publication date: 2020-12-01

Abstract

The invention discloses an anti-alcohol composition, which comprises the following components in percentage by weight: 10 to 60 percent of ampelopsis grossedentata leaves, 1 to 20 percent of hovenia dulcis thunb, 1 to 10 percent of dark plum fruit, 1 to 10 percent of boat-fruited sterculia seed, 0.1 to 1 percent of vitamin C and 25 to 60 percent of auxiliary materials. The invention also discloses a preparation method of the composition, application of the composition in preparing functional food for relieving alcoholism and application of the composition in preparing medicines for preventing acute and/or chronic alcoholism, and the composition can be prepared into tablets, granules, capsules, soft capsules, powder or oral liquid and other dosage forms. According to the invention, the new resource food and a plurality of medicinal and edible traditional Chinese medicinal materials are scientifically and reasonably compounded to prepare the functional food composition with good taste, and relevant experiments prove that the composition can obviously decompose the alcohol concentration in blood, reduce the alcohol absorption, improve the activity of an anti-inebriation enzyme, prevent the effects of anti-inebriation and liver protection and prevent hangover, and has a prevention effect on acute and/or chronic alcoholism.

Description

Anti-alcohol composition and preparation method thereof

Technical Field

The invention relates to an anti-alcoholism composition and a preparation method thereof, belonging to the technical field of functional foods and pharmacy.

Background

Wine has a long history in China, and forms a wine culture, so that the wine can not help the happiness of relatives and businesses with much reward. However, when people are happy, the symptoms such as nausea, vomiting and emotional instability are caused by drunkenness, and coma and respiratory function are exhausted and die in severe cases.

Alcohol intake affects most organ systems, and alcohol metabolism disorders (AUDs) play a crucial role in the brain, as alcohol alters the balance between GABA (the major inhibitory neurotransmitter) and glutamate (the major excitatory neurotransmitter) in the brain, leading to toxic, sedative, anxiolytic, tonic, and addictive symptoms. GABAA receptor (GABAAR) -mediated inhibitory neurotransmitters are enhanced by the action of alcohol, and it has been reported that there is a direct effect on both presynaptic GABA release and enhancement of postsynaptic GABAARs cells. GABAARs formed by a family of subunits located postsynaptic or extrasynaptic membranes exhibit different sensitivities to alcohol, forming a regulated dynamic transport state between cell pools, and extrasynaptic GABAARs are sensitive to alcohol concentrations in the blood during social drinking. Changes in the levels of several GABAAR subunits caused by alcohol are accompanied by behavioral disorders such as loss of righting reflex (LORR).

In animal experiments, rats taken alcohol for a long period of time produced profound GABAAR plasticity, which plays a key role in alcohol withdrawal and dependence. After acute drinking, some GABAARs are rapidly down-regulated, producing physiological and pharmacological changes consistent with tolerance and withdrawal symptoms in vivo as GABAARs become plastic. Alcohol-induced behavioral changes and GABAAR plasticity can be used as a screen for drugs that improve AUDs.

About 95% of alcohol entering human body undergoes oxidative metabolism by liver enzyme system (mainly alcohol dehydrogenase and acetaldehyde dehydrogenase), and alcohol is oxidized into acetaldehyde in liver mainly under the catalysis of Alcohol Dehydrogenase (ADH) and then into acetic acid under the catalysis of acetaldehyde dehydrogenase (ALDH). Thus, ADH and ALDH are the most important enzymes in vivo to reduce alcohol concentration.

The antialcoholic product is a series of products which can decompose the alcohol concentration, enhance the activity of acetaldehyde dehydrogenase and the like after a human body ingests a large amount of alcohol, and can be generally divided into three types, namely chemical drugs, Chinese medicinal preparations and health-care functional foods. The chemical product and the Chinese medicinal preparation can cause metabolic burden on liver and kidney while relieving alcoholism, thereby causing different degrees of damage to human body. The functional food serving as a diet product for assisting in improving adverse reaction symptoms after drinking does not generate any toxic or side effect on a body, can also play a role in repairing and nourishing damaged liver cells, is safe and reliable, and is favored by more and more consumers.

At present, relatively few functional foods for relieving alcoholism sold in the market exist, the additive components are single, the effect is slow, the effects of quickly relieving alcoholism and relieving hangover cannot be achieved, and obvious side effects and the like exist after the foods are taken, so that the expectations and appeal of the public drinking people on the antialcoholic product cannot be met. The composition is constructed by screening various pure plant flavonoid raw materials, so that the components can be synergized and act together, and the alcohol removal is promoted by improving the activities of Alcohol Dehydrogenase (ADH) and acetaldehyde dehydrogenase (ALDH), so that the alcoholic liver injury is improved, and the hangover is relieved.

Disclosure of Invention

One of the purposes of the invention is to provide an anti-alcoholism composition which has the effects of enhancing the activity of alcohol dehydrogenase in vivo, relieving alcoholism and protecting liver, relieving hangover, resisting acute alcoholic liver injury and preventing acute and chronic alcoholism;

the invention also aims to provide a preparation method of the anti-alcoholism composition.

Based on the above purpose, the invention firstly provides a composition, which is prepared from the following components in percentage by weight: 10 to 60 percent of ampelopsis grossedentata leaves, 1 to 20 percent of hovenia dulcis thunb, 1 to 10 percent of dark plum fruit, 1 to 10 percent of boat-fruited sterculia seed, 0.1 to 1 percent of vitamin C and 25 to 60 percent of auxiliary materials.

In the composition, Ampelopsis grossedentata leaf is a new resource food approved by the national health and wellness Commission, and can be used as a common food raw material. The ampelopsis grossedentata leaf extract contains rich flavonoids, can improve the activity of antialcoholic enzymes (alcohol dehydrogenase and acetaldehyde dehydrogenase) in the liver, effectively prolong the intoxication latency, shorten the sobering time, protect the liver, accelerate the rapid decomposition of ethanol metabolite acetaldehyde to become a nontoxic substance, reduce the damage to liver cells, improve the activity increase of serum lactate dehydrogenase caused by liver cell damage, thereby playing the role of protecting the liver, greatly reducing the damage of ethanol to the liver and rapidly recovering the normal state of the liver.

The raisin tree seed is a product with homology of medicine and food, the raisin tree seed is neutral and nontoxic and enters spleen and stomach channels, and related experimental results show that flavonoid substances in the raisin tree seed extract can resist the damage of alcohol to a central nervous system, show that the flavonoid substances can shorten the lethargy time of an acute alcoholism mouse, reduce the number of autonomous activities caused by excitation of the central nervous system due to small-amount drinking, improve the learning and memory capacity, effectively reduce the content of alcohol in blood and increase the activity of alcohol dehydrogenase in liver. In a word, the hovenia dulcis thunb extract can rapidly relieve acute alcoholism symptoms, promote the metabolism of alcohol in the liver by inhibiting the absorption of alcohol in the gastrointestinal tract, accelerate the decomposition of alcohol and play an effective role in relieving alcoholism and preventing drunkenness.

The dark plum is also called plum, has sour, astringent and neutral taste, and is a product of homology of medicine and food. The dark plum contains flavonoid substances and various organic acids, can improve the function of the liver, and has the effect of helping an organism to relieve alcoholism.

Boat-fruited sterculia seed is sweet in taste, cold in nature, enters lung and large intestine meridians and is a product with homology of medicine and food. The boat-fruited sterculia seed extract also contains abundant flavonoids, and has the effects of clearing heat, moistening lung, relieving sore throat, easing up voice, relaxing bowel and accelerating metabolism of a human body.

In a preferred embodiment of the invention, the composition comprises the following components in the following compatible proportion by weight percentage: 30 to 50 percent of ampelopsis grossedentata leaves, 1 to 10 percent of hovenia dulcis thunb, 1 to 5 percent of dark plum fruit, 1 to 5 percent of boat-fruited sterculia seed, 0.1 to 0.5 percent of vitamin C and 35 to 50 percent of auxiliary materials.

In a more preferred embodiment, the composition comprises the following components in the following compatible proportions by weight percent: 50% of ampelopsis grossedentata leaves, 5% of hovenia dulcis thunb, 2% of dark plum fruit, 2% of boat-fruited sterculia seed, 0.15% of vitamin C and 40.85% of auxiliary materials.

More preferably, the Ampelopsis grossedentata leaf in the composition is Ampelopsis grossedentata leaf powder or powdered extract of Ampelopsis grossedentata leaf, preferably powdered extract of Ampelopsis grossedentata leaf.

The semen Hoveniae in the composition for relieving hangover is semen Hoveniae powder or semen Hoveniae powder extract, preferably semen Hoveniae powder extract.

The fructus mume in the anti-hangover composition is fructus mume powder or fructus mume powder extract, preferably fructus mume powder extract.

The semen Scaphii Lychnophori in the composition for relieving alcoholic intoxication is semen Scaphii Lychnophori powder or semen Scaphii Lychnophori powder extract, preferably semen Scaphii Lychnophori powder extract.

In a preferred embodiment of the invention, the adjuvant in the composition is selected from one or more of lactose, microcrystalline cellulose, maltodextrin, isomaltooligosaccharide, fruit and vegetable powder, concentrated fruit and vegetable juice, magnesium stearate, silicon dioxide, titanium dioxide, beeswax, purified water, sucralose, essence, pigment, glycerol, povidone K30, and gelatin.

Secondly, the invention provides a preparation method of the composition, and the method comprises the step of mixing Ampelopsis grossedentata leaves, Hovenia dulcis seeds, dark plum fruits, scaphium scaphigerum and vitamin C according to a compatible proportion.

In a preferred embodiment of the present invention, the Ampelopsis grossedentata leaves, Hovenia dulcis, Prunus mume and Sterculia Lychophora are all processed into powders before mixing.

In the process for preparing powders, the following are the specific embodiments adopted by the present invention:

1) the preparation method of the ampelopsis grossedentata leaf powder comprises the following steps:

the method comprises the following steps: picking dried Ampelopsis grossedentata leaves, and screening to remove impurities;

step two: and (3) crushing the ampelopsis grossedentata leaves subjected to impurity removal in the step one by using a crusher under proper conditions, preferably, the proper crushing conditions of the ampelopsis grossedentata leaves are that the humidity is less than 30% and the temperature is less than 25 ℃, the mesh number of the crushed ampelopsis grossedentata leaves is 40-80 meshes, and the moisture is controlled to be less than 5%.

2) The preparation method of the hovenia dulcis thunb powder comprises the following steps:

the method comprises the following steps: taking fresh and mature fruits of hovenia dulcis thunb as a raw material, soaking and cleaning, and draining water, wherein preferably, the soaking and rinsing time of the hovenia dulcis thunb is 5-15 min;

step two: spreading the drained hovenia dulcis thunb in the step one on a tray of a drying machine for drying, preferably, the drying temperature of the hovenia dulcis thunb is 45-55 ℃, the humidity is 5-20%, and the drying time is 3-7 h;

step three: and (2) crushing the dried hovenia dulcis thunb in the step two, preferably, the crushing condition of the hovenia dulcis thunb is that the humidity is less than 30% and the temperature is less than 25 ℃, the mesh number of the crushed hovenia dulcis thunb powder is between 50 and 100 meshes, and the moisture is controlled to be less than 5%.

3) The preparation method of the dark plum powder comprises the following steps:

pulverizing oven-dried or naturally sun-dried mume fructus with a pulverizer, preferably, the mume fructus is pulverized under the conditions of humidity less than 30% and temperature less than 25 deg.C, and the pulverized mume fructus has a mesh size of 60-100 meshes and water content below 5%.

4) The preparation method of the boat-fruited sterculia seed powder comprises the following steps:

the method comprises the following steps: fresh mature fruits of boat-fruited sterculia seeds are taken as raw materials, soaked and cleaned, and then drained, and preferably, the soaking and rinsing time of the boat-fruited sterculia seeds is 5-15 min;

step two: spreading the drained boat-fruited sterculia seed in the step one on a tray of a drying machine for drying, preferably, the drying temperature of the boat-fruited sterculia seed is 45-55 ℃, the humidity is 5-20%, and the drying time is 3-7 h;

step three: and D, crushing the dried boat-fruited sterculia seed in the step two, preferably, the crushing condition of the boat-fruited sterculia seed is that the humidity is less than 30 percent and the temperature is less than 25 ℃, the mesh number of the crushed boat-fruited sterculia seed powder is between 50 and 100 meshes, and the moisture is controlled to be less than 5 percent.

In a more preferred embodiment of the present invention, the Ampelopsis grossedentata leaf, Hovenia dulcis seed, Prunus mume and Sterculia Lychophora are all processed into powder extracts before mixing.

In the method for preparing the powdery extract, the following are specific embodiments adopted in the present invention:

1) the preparation method of the ampelopsis grossedentata leaf powdery extract comprises the following steps:

step two: crushing the ampelopsis grossedentata leaves subjected to impurity removal in the step one by using a crusher; preferably, the mesh number of the crushed Ampelopsis grossedentata is 40-80 meshes;

step three: weighing a certain amount of the crushed Ampelopsis grossedentata leaves obtained in the second step, adding ethanol for reflux extraction, extracting for three times, and then combining the filtrates; preferably, 5 times volume of ethanol is added into the Ampelopsis grossedentata leaves, and reflux extraction is carried out for 50 min;

step four: concentrating the combined filtrate in the third step under vacuum condition to obtain extract; preferably, the concentration condition of the ampelopsis grossedentata leaf extracting solution is 0.6-0.8 Mpa of vacuum degree;

step five: adding water into the leaching paste, and standing at normal temperature for crystallization; preferably, 7 times of water with the pH value less than 7 at normal temperature is added into the extract, and the mixture is placed for crystallization for 24 hours;

step six: skimming the upper layer floating black oily substance in the fifth step, filtering the lower light green precipitate, and drying;

step seven: completely dissolving the crude product in the sixth step by using pure water, adding activated carbon for decolorization, and then removing impurities to finally obtain a powdery substance, namely the ampelopsis grossedentata leaf extract; preferably, the crude product is dissolved in 18 to 20 times the amount of pure water having a pH of less than 7 and decolorized with 10% activated carbon.

2) Preparing a hovenia dulcis thunb powdery extract:

the method comprises the following steps: taking fresh and mature fruits of hovenia dulcis thunb as raw materials, and crushing the hovenia dulcis thunb properly by using a wall breaking machine;

step two: weighing a certain amount of the hovenia dulcis thunb crushed in the step one, taking alcohol as a solvent, extracting by a hot reflux extraction method for 2-4 times, and then combining filtrates; preferably, the hovenia dulcis thunb is extracted by 75% alcohol through hot reflux for 2 hours, the addition amount of the alcohol is 8 times, and the extraction times are 2-4 times;

step three: concentrating the filtrate in the second step under vacuum condition to obtain concentrated solution; preferably, the hovenia dulcis thunb extract is concentrated to the relative density of 1.1-1.5 g/cm under the vacuum degree of 0.6-0.8 Mpa³；

Step four: spray drying the concentrated solution in step three by using a centrifugal spray drying tower, and crushing into fine powder after drying to obtain the hovenia dulcis thunb extract; preferably, the air inlet temperature of the hovenia dulcis thunb is 150-180 ℃ and the air outlet temperature is 70-90 ℃ during spray drying, and the hovenia dulcis thunb is dried and crushed into 80-100 meshes of fine powder, and the water content is controlled to be below 5%.

3) Preparing a dark plum powder extract:

the method comprises the following steps: pulverizing oven-dried or naturally sun-dried mume fructus with pulverizer;

step two: weighing the dark plum powder in the step one, adding ethanol for reflux extraction, extracting for 1-2 times to obtain dark plum extract, mixing the dark plum extract, filtering while hot, centrifuging, collecting supernatant, and performing suction filtration to obtain a concentrated solution; preferably, the dark plum is added with 50-95% of ethanol by mass percent for reflux extraction, the mass volume (kg/L) ratio of the dark plum to the ethanol is 1: 5-1: 25, the dark plum and the ethanol are extracted in a water bath at 50-70 ℃ for 1-3 hours, and the extraction is carried out for 1-2 times;

step three: spray-drying the concentrated solution in the step two by adopting a centrifugal spray-drying tower, and crushing into fine powder after drying to obtain a dark plum extract; preferably, the air inlet temperature of the dark plum extract is 150-180 ℃ and the air outlet temperature is 70-90 ℃ during spray drying, and the dark plum extract is dried and crushed into 80-100 meshes of fine powder, wherein the water content is controlled to be below 5%.

4) Preparing the boat-fruited sterculia powder extract:

the method comprises the following steps: using fresh and mature fruits of boat-fruited sterculia seed as raw material, and crushing the boat-fruited sterculia seed by using a wall breaking machine;

step two: weighing a certain amount of the crushed boat-fruited sterculia seeds in the step one, taking alcohol as a solvent, and extracting by adopting a hot reflux extraction method. Extracting for 2-3 times, and mixing filtrates; preferably, the sterculia lychnophora is extracted by a hot reflux extraction method for 2 hours by using 75% alcohol as a solvent, the adding amount of the alcohol is 8 times, and the extraction times are 2-4 times;

step three: concentrating the boat-fruited sterculia seed extract in the second step to a certain relative density under vacuum condition to obtain a concentrated solution; preferably, the boat-fruited sterculia seed extracting solution is concentrated to the relative density of 1.1-1.5 g/cm under the vacuum degree of 0.6-0.8 Mpa³；

Step four: spray drying the concentrated solution in the third step by using a centrifugal spray drying tower, and crushing into fine powder after drying to obtain the boat-fruited sterculia seed extract; preferably, the air inlet temperature of the boat-fruited sterculia seed concentrated solution is 150-180 ℃ and the air outlet temperature is 70-90 ℃ during spray drying, and the boat-fruited sterculia seed concentrated solution is dried and crushed into 80-100 meshes of fine powder, and the water content is controlled to be below 5%.

The invention also provides application of the composition in preparing functional food for relieving alcoholism.

Finally, the invention provides the use of the above composition for the preparation of a medicament for the prevention of acute and/or chronic alcoholism.

In a preferred embodiment, the composition is prepared as a powder, a tablet, a granule, a capsule, a soft capsule, or an oral liquid.

Compared with the prior art, the invention has the beneficial effects that:

the invention scientifically and reasonably compounds and organically combines new resource food and traditional Chinese medicines with homology of medicine and food, and flavonoid substances in the raw materials supplement each other in efficacy and act together, thus having no toxic or side effect on human bodies. Relevant experiments prove that the composition can increase the activity of acetaldehyde dehydrogenase in vivo, promote the rapid decomposition of alcohol in vivo, rapidly relieve the effect of alcohol of a large number of people who take alcohol, protect the liver, improve acute alcoholic liver injury, improve alcoholism dependence, relieve hangover and play a role in preventing acute and chronic alcoholism. Has good application and development prospect in the anti-alcohol market and related fields. The composition can be made into various dosage forms, has stable product and is easy for industrial production.

Drawings

The following describes embodiments of the present invention in further detail with reference to the accompanying drawings.

FIG. 1 is a graph showing the change in ADH activity of experimental mice in application example 2, and shows that the anti-hangover composition of the present invention increases the ADH activity of alcoholic mice.

Fig. 2 is a graph showing the comparison of the righting reflex time of the experimental rats in application example 3, which shows that the hangover alleviating composition of the present invention has an obvious recovery of the LORR time of the acute alcoholism rats.

FIG. 3 is a graph showing the results of electrophoresis of GABAAR a1 and a4 subunits and representative protein expression in hippocampal tissues of rats tested in example 3, showing that alcoholism significantly reduced the expression of GABAAR a1 subunit in hippocampal tissues, while the expression of GABAAR a4 subunit was significantly increased.

Fig. 4 is a statistical result chart of efficacy verification experiments in a human body feeding trial test using the anti-hangover composition of example 4.

Fig. 5 is a graph comparing the GABAAR a1 subunit and the a4 subunit proteins in the hippocampal tissues of the experimental rat in example 3, which shows that alcoholism significantly reduces the expression of GABAAR a1 subunit in the hippocampal tissues, while the expression of GABAAR a4 subunit is significantly increased, and the anti-inebriation composition of the present invention can significantly reverse these changes.

Detailed Description

The present invention is further illustrated below with reference to specific examples, which are to be construed as merely illustrative, and not limitative of the remainder of the disclosure. It will be apparent to those skilled in the art that various changes and modifications may be made in the invention without departing from the spirit and scope of the invention as defined in the following claims.

Preparation of example 1

The anti-inebriation composition is powder, and the formula compatibility among the raw materials of the anti-inebriation composition is as follows (the weight percentage is shown in brackets): 1.5g (50%) of ampelopsis grossedentata leaves, 0.15g (5%) of hovenia dulcis thunb, 0.05g (1.67%) of dark plum fruits, 0.05g (1.67%) of scaphium scaphigerum, 0.0045g (0.15%) of vitamins and auxiliary material components: 0.006g of sucralose (0.2%), 1.2395g of isomaltooligosaccharide (41.32%) and a mass ratio of raw materials to auxiliary materials of 1: 0.7. Wherein the auxiliary materials comprise sucralose as a sweetening agent and isomaltooligosaccharide as a filling agent.

The preparation method of the powder of the anti-alcoholism composition is carried out according to the following scheme:

the first step is as follows: preparation of a Ampelopsis grossedentata leaf powdery extract (Sanyuan Longsheng Biotechnology Limited liability company, 30%), a hovenia dulcis thunb powdery extract (Sanyuan Longsheng Biotechnology Limited liability company, 10:1 ratio extract), a dark plum powdery extract (Sanyuan Longsheng Biotechnology Limited liability company, 10:1 ratio extract), a sterculia scaphigera powdery extract (Sanyuan Longsheng Biotechnology Limited liability company, 10:1 ratio extract):

1) preparing a powdery extract of Ampelopsis grossedentata leaves:

step two: crushing Ampelopsis grossedentata leaves by a crusher, wherein the mesh number is controlled between 40 meshes and 80 meshes;

step three: weighing a certain amount of Ampelopsis grossedentata leaves, adding 5 times of ethanol, reflux-extracting for 50min, extracting for three times, and mixing filtrates;

step four: concentrating the ampelopsis grossedentata leaf extracting solution to be paste-like under the vacuum degree of 0.6-0.8 Mpa;

step five: adding 7 times of water with pH less than 7 at normal temperature according to the volume ratio of the extract to the water of 1:7, standing and crystallizing for 24 h;

step six: skimming off the upper layer floating black oily substance, suction filtering to obtain the lower light green precipitate, and drying;

step seven: and (3) dissolving the crude product by using 18-20 times of pure water with the pH value of less than 7, adding 10% of activated carbon for decolorization after the crude product is completely dissolved, and removing impurities to finally obtain a powdery substance.

2) Preparing a hovenia dulcis thunb powdery extract:

step two: weighing a certain amount of crushed hovenia dulcis thunb, taking 75% alcohol as a solvent, adopting a hot reflux extraction method, extracting for 2 hours, adding 8 times of alcohol, extracting for 2-4 times, and combining filtrates;

step three: the raisin tree seed extract is concentrated under the vacuum degree of 0.6-0.8 Mpa until the relative density is 1.1-1.5 g/cm³Then obtaining concentrated solution;

step four: spray drying in a centrifugal spray drying tower at air inlet temperature of 150-180 deg.c and air outlet temperature of 70-90 deg.c, crushing into 80-100 mesh powder with water content below 5%.

3) Preparing a dark plum powder extract:

the method comprises the following steps: pulverizing dried or naturally sun-dried mume fructus with pulverizer

Step two: weighing dark plum powder, adding 50-95% by mass of ethanol for reflux extraction, extracting dark plum and ethanol in a water bath at 50-70 ℃ for 1-3 h for 1-2 times to obtain dark plum extract, combining the dark plum extracts, filtering while hot, centrifuging, collecting supernatant, and performing suction filtration;

step three: spray drying in a centrifugal spray drying tower at air inlet temperature of 150-180 deg.c and air outlet temperature of 70-90 deg.c, crushing into 80-100 mesh powder with water content below 5%.

4) Preparing the boat-fruited sterculia powder extract:

step two: weighing a certain amount of crushed boat-fruited sterculia seeds, taking 75% alcohol as a solvent, adopting a hot reflux extraction method, extracting for 2 hours, adding 8 times of ethanol, extracting for 2-4 times, and combining filtrates;

step three: the extracting solution of boat-fruited sterculia seed is concentrated to the relative density of 1.1 to 1.5g/cm under the vacuum degree of 0.6 to 0.8Mpa³Then obtaining concentrated solution;

And secondly, mixing and sieving the powdered extract of Ampelopsis grossedentata leaves, the powdered extract of Hovenia dulcis, the powdered extract of smoked plum and the powdered extract of Sterculia Lychophora according to the formula amount with vitamin C and auxiliary materials according to the formula amount to obtain the powder of the anti-alcoholism composition.

The third step: and (4) sequentially sterilizing, layering, boxing and plastic packaging the hangover-alleviating composition powder prepared in the second step to obtain a finished product of the hangover-alleviating composition powder, namely the hangover-alleviating composition solid beverage.

Preparation of example 2

The anti-inebriation composition is powder, and the formula compatibility among the raw materials of the anti-inebriation composition is as follows: 1.2g (40%) of ampelopsis grossedentata leaves, 0.08g (2.67%) of hovenia dulcis thunb, 0.04g (1.33%) of dark plum fruits, 0.04g (1.33%) of boat-fruited sterculia seeds, 0.0035g (0.12%) of vitamin C and auxiliary material components: 0.004g of sucralose (0.13%), 1.6325g of isomaltooligosaccharide (54.48%) and a mass ratio of raw materials to auxiliary materials of 1: 1.2. Wherein the auxiliary materials comprise sucralose as a sweetening agent and isomaltooligosaccharide as a filling agent.

The preparation method of the powder of the anti-alcoholism composition is carried out according to the following scheme: sieving Ampelopsis grossedentata leaf powder extract, semen Hoveniae powder extract, mume fructus powder extract, semen Scaphii Lychnophori powder extract, vitamin C, sucralose and isomaltooligosaccharide, and mixing.

Preparation of example 3

The anti-alcoholism composition is in the form of granules, and the formula compatibility proportion of the raw materials is as follows: 1.5g (50%) of ampelopsis grossedentata leaves, 0.15g (5%) of hovenia dulcis thunb, 0.05g (1.67%) of dark plum fruits, 0.05g (1.67%) of boat-fruited sterculia seeds, 0.0045g (0.15%) of vitamin C and auxiliary material components: 0.006g (0.2%) of sucralose, 1.2395g (41.32%) of maltodextrin and 1:0.7 of raw and auxiliary materials in mass ratio. Wherein the auxiliary materials comprise sucralose as a sweetening agent and maltodextrin as an anticaking agent and a filling agent.

The preparation method of the antialcoholic composition granules comprises the following steps: the oral liquid is prepared from Ampelopsis grossedentata leaf powder extract, Hovenia dulcis Thunb powder extract, mume fructus powder extract, semen Scaphii Lychnophori powder extract, vitamin C, sucralose and maltodextrin by sieving, mixing, granulating, oven drying and sieving.

Preparation of example 4

The anti-alcoholism composition is an oral liquid, and the formula compatibility proportions of the raw materials are as follows: 1.5g (50%) of ampelopsis grossedentata leaves, 0.15g (5%) of hovenia dulcis thunb, 0.05g (1.67%) of dark plum fruits, 0.05g (1.67%) of boat-fruited sterculia seeds, 0.0045g (0.15%) of vitamin C and auxiliary material components: 0.006g (0.2%) of sucralose, 1.24g (41.3%) of juicy peach concentrated juice (Heilongjiang Shanghai Zhi green wild berry, LLC, 8 times of concentrated peach concentrated juice), and the mass ratio of the raw materials to the auxiliary materials is 1: 0.7. Wherein the auxiliary materials comprise sucralose as a sweetening agent and concentrated juicy peach juice as a flavoring agent.

The preparation method of the anti-alcoholism composition oral liquid comprises the following steps: dissolving Ampelopsis grossedentata leaf powder extract, semen Hoveniae powder extract, mume fructus powder extract, semen Scaphii Lychnophori powder extract, vitamin C and sucralose in 30mL of purified water, filtering, instantly sterilizing at high temperature, and cooling to obtain the final product.

Preparation of example 5

The anti-alcoholism composition is a tablet, and the formula compatibility proportion of the raw materials is as follows: 1.5g (50%) of ampelopsis grossedentata leaves, 0.15g (5%) of hovenia dulcis thunb, 0.05g (1.67%) of dark plum fruits, 0.05g (1.67%) of boat-fruited sterculia seeds, 0.0045g (0.15%) of vitamin C and auxiliary material components: 1.241g of lactose (41.3%), 0.003g of magnesium stearate (0.1%), 0.0015g of silicon dioxide (0.05%) and a mass ratio of raw materials to auxiliary materials of 1: 0.7. Wherein, in the auxiliary material components, lactose is used as a filling agent, magnesium stearate is used as a lubricating agent, and silicon dioxide is used as a glidant.

The preparation method of the anti-alcoholism composition tablet comprises the following steps: lactose, ampelopsis grossedentata leaf powder extract, hovenia dulcis thunb powder extract, dark plum fruit powder extract, sterculia scaphigera powder extract and vitamin C, sieving, mixing with formula amounts of auxiliary materials of lactose, magnesium stearate and silicon dioxide, and tabletting.

Preparation of example 6

The anti-alcoholism composition is a capsule, and the formula compatibility proportions of the raw materials are as follows: 1.5g (50%) of ampelopsis grossedentata leaves, 0.15g (5%) of hovenia dulcis thunb, 0.05g (1.67%) of dark plum fruits, 0.05g (1.67%) of boat-fruited sterculia seeds, 0.0045g (0.15%) of vitamin C and auxiliary material components: 0.0009g (0.3) of silicon dioxide, 0.06g (2) of titanium dioxide, 0.87g (29) of gelatin, 0.025g (8.3) of glycerol, 0.2896g (9.65) of purified water and 1:0.7 of raw and auxiliary materials in mass ratio. Wherein in the auxiliary material components, silicon dioxide is used as a glidant, titanium dioxide is used as an opacifier, gelatin is used as a shaping agent, glycerol is used as a plasticizer, and purified water is used as a dissolving agent.

The preparation method of the anti-alcoholism composition capsule comprises the following steps: the capsule is prepared by sieving powdered extract of Ampelopsis grossedentata leaf, powdered extract of Hovenia dulcis Thunb, powdered extract of Prunus mume, powdered extract of Sterculia Lychophora seed and vitamin C, mixing, and encapsulating.

Preparation of example 7

The preparation form of the composition is a soft capsule, and the compatibility proportion of the raw materials is as follows: 1.5g (50%) of ampelopsis grossedentata leaves, 0.15g (5%) of hovenia dulcis thunb, 0.05g (1.67%) of dark plum fruits, 0.05g (1.67%) of boat-fruited sterculia seeds, 0.0045g (0.15%) of vitamin C and auxiliary material components: 0.5g (16.67%) of gelatin, 0.25g (8.3%) of glycerol, 0.5g (16.67%) of purified water and a mass ratio of raw materials to auxiliary materials of 1: 0.7. Wherein gelatin is used as a plasticizer, glycerin is used as a plasticizer, and purified water is used as a dissolving agent.

The preparation method of the anti-alcoholism composition soft capsule comprises the following steps: sieving Ampelopsis grossedentata leaf powder extract, semen Hoveniae powder extract, mume fructus powder extract, semen Scaphii Lychnophori powder extract and vitamin C, mixing, making into capsule shell, and pressing.

Application example 1 taste evaluation test

In this embodiment, a taste verification experiment of the anti-hangover composition prepared in preparation example 1 is considered, and the specific test process is as follows:

the anti-hangover composition prepared in preparation example 1 was used for taste and sensory evaluation, 10 persons were randomly selected for testing, and the color, taste, smell and other indicators of the product were examined and evaluated comprehensively. The evaluation indexes and standards are as follows:

TABLE 1 test index and evaluation Standard

The test results were as follows:

TABLE 2 test results score summary

The taste evaluation and summary results and data analysis show that the anti-alcoholism medicine prepared by the invention has the characteristics of uniform color, pleasant flavor, saturated and rich taste, high overall acceptance of the public and certain market development prospect.

Application example 2 Effect of the antialcoholic composition on Alcohol Dehydrogenase (ADH) Activity

In this example, the effect of the anti-hangover compositions prepared in preparation examples 1 and 2 on alcohol dehydrogenase Activity (ADH) in animal models was examined, and the specific test procedures are as follows:

1. experimental Material

Male BALB/C mice (body weight 30-35g) were from experimental animal center of guangdong province (SPF grade, certificate No. 2005a047, 2006a059), gavage, edible alcohol, physiological saline, the anti-hangover composition of preparation example 1, ADH assay kit, and the like.

2. Grouping of laboratory animals

The chronic alcoholism mice were divided into 5 groups of 8 mice each. All animals were kept under controlled temperature and humidity conditions in a 12h/12h light/dark cycle with free access to food and water. Animal experiments were approved by the ethical committee for animal research at river-south university.

3. Experimental methods

(1) Chronic alcoholic mouse model

Alcohol (25%, v/v) was gavaged, 0.2mL/10g body weight, and 250mg and 500mg per kg body weight were administered for 30min before or after the treatment in the preparation of the anti-hangover composition of example 1 or 2, 1 time per day for 12 consecutive days. The body weight of the mice was monitored every two days. After the experiment, mice were sacrificed and livers were dissected for Alcohol Dehydrogenase (ADH) assay.

(2) ADH assay

After the chronic alcohol treatment was over, the mice were sacrificed and the liver was dissected on ice. Liver homogenates were homogenized manually in 2mL glass jars and centrifuged (X3000 g, Beckmann J2-21 centrifuge, Beckmann instruments, Germany) for 10 min. Supernatants were collected for ADH assay. The ADH determination kit is purchased from Nanjing, China to build a biological laboratory, and experiments are carried out according to the manufacturer instructions. The general procedure was to add Nicotinamide Adenine Dinucleotide (NAD) in oxidized form to the liver sample, the absorbance of the reaction mixture was recorded at 340nm, and ADH activity was calculated from the absorbance values and protein content. ADH activity was expressed in units of 1nmoL ADH per mg protein per minute at 37 deg.C (U/mg), i.e., 1U/mg.

4. Results of the experiment

Alcohol had a significant effect on mouse body weight, with the mean body weight of the saline group increasing from 20.7 ± 1.25g to 30.36 ± 2.06g, while the mean body weight of the alcohol + saline group decreased from 22.52 ± 0.43g to 18 ± 2.88g [ P ═ 0.007] (table 3). From day 4 to day 12, the animal body weights of the high-concentration anti-hangover composition + alcohol group of preparation example 1 and the low-concentration anti-hangover composition + alcohol group of preparation example 2 were significantly higher than those of the alcohol + physiological saline group [ P ═ 0.02] (table 3), and from table 3, it can be seen that the high-concentration anti-hangover composition of preparation example 1 and the low-concentration anti-hangover composition of preparation example 2 were dose-dependent on the weight loss effect of the alcoholic mice.

ADH activity was significantly decreased in alcoholic mice compared to normal mice [ P ═ 0.002 ]. The anti-hangover composition reversed the decrease in ADH activity in the liver of alcoholism mice in a dose-dependent manner (fig. 1), indicating that the anti-hangover composition could exert its anti-alcoholism effect by enhancing ADH activity. In fig. 1, 1: normal saline + normal saline, 2: alcohol + normal saline, 3: the low concentration anti-hangover composition + alcohol of preparation example 2, 4: the high concentration anti-hangover composition + alcohol of preparation example 1, 5: alcohol + the high concentration anti-hangover composition of preparation example 1, 6: the high concentration anti-hangover composition of example 1 + physiological saline was prepared. Preparation example 1 the high concentration anti-hangover composition is added with 1.5g of ampelopsis grossedentata leaves, 0.15g of hovenia dulcis thunb, 0.05g of dark plum, 0.05g of sterculia lychnophora, 0.0045g of vitamin C, 1.2455g of auxiliary materials, and 3.0g of the total. Wherein, 1.755g of main material is added, accounting for 58.5 percent; preparation example 2 the low concentration anti-hangover composition is added with 1.2g of ampelopsis grossedentata leaves, 0.08g of hovenia dulcis thunb, 0.04g of dark plum, 0.04g of sterculia lychnophora, 0.0035g of vitamin C, 1.6365g of auxiliary materials, and 3.0g of the total. Wherein, 1.364g of main material is added, accounting for 45.5 percent. The main material ratio of the high-concentration anti-inebriation composition in the preparation example 1 is 1.3 times of that of the low-concentration anti-inebriation composition in the preparation example 2.

ADH reduces alcohol concentration in the body and is one of the most important enzymes in alcohol metabolism in the human body. When ADH activity decreases, the alcohol concentration in blood increases, exacerbating alcohol damage to the brain, liver and other vital organs. The anti-hangover composition can improve ADH activity and prevent weight loss after chronic alcohol contact. The increased ADH activity may be responsible for the alcohol detoxification of hepatocytes by the anti-hangover composition. In addition to the antidotal effect, the anti-hangover composition also inhibits voluntary alcohol consumption in alcohol-preference rats.

TABLE 3 Effect of antialcoholic compositions on body weight in alcoholism mice

Packet details

1. Normal saline + normal saline;

2. alcohol + normal saline;

3. preparation example 2 low concentration anti-hangover composition + alcohol;

4. preparation example 1 high concentration anti-hangover composition + alcohol;

5. alcohol + high concentration anti-hangover composition of preparation example 1;

6. the high concentration anti-hangover composition + physiological saline in preparation example 1 was prepared.

Note: data are presented as mean ± standard deviation (n ═ 8). P <0.05 compared to "alcohol + saline" treatment group; p <0.05 compared to "saline + saline" treatment group P < 0.05.

Experiment for improving acute alcoholism by using anti-alcoholic composition in example 3

In this example, the improvement effect of the anti-hangover composition prepared in preparation example 1 on alcoholism rats was examined, and the specific test procedures were as follows:

1. experimental Material

Male Sprague-Dawley rats (body weight 300-.

2. Grouping of laboratory animals

The acute alcohol test rats were divided into 5 groups of 6 rats each. All animals were kept under controlled temperature and humidity conditions in a 12h/12h light/dark cycle with free access to food and water. Animal experiments were approved by the ethical committee for animal research at river-south university.

3. Experimental methods

(1) Acute alcoholic rat model

Before or 30min after the treatment of the anti-hangover composition of preparation example 1, 25% (v/v) alcohol was gavaged at a dose of 2mL per 100g of body weight. Preparation of the antialcoholic composition of example 1 was administered at 1mL/100g or 500mg per kg body weight, respectively. After two days of rest, the protective effect of the anti-hangover composition was evaluated by the righting reflex (LORR) test. Rats were sacrificed and rat brain hippocampal tissue was dissected using western blot for GABAAR subunit analysis.

(2) Righting Reflex (LORR) test

Two days after alcoholism and abstinence, all animals received intraperitoneal injections (30mg/kg body weight) of diazepam (Shanxi Xin Bao Yuan pharmaceuticals Co., Ltd.). LORR and righting reflex recovery were observed. After each injection, animals were placed in a supine position in cages with iron wire lids. LORR was recorded as the time when the animal failed to turn. The animal was left in a supine position until the righting reflex was restored. The recovery of righting reflex was defined as the time the animal was able to recover 3 times in 60 s. The time to recovery of positive reflex was recorded for each animal.

(3) Protein sample preparation and western blot analysis

Following the LORR experiment, rats were anesthetized and tissues were isolated. Individual hippocampal tissues were dissected from the brain of each rat on ice. The P2 membrane fraction was homogenized, centrifuged at low speed in 0.32M sucrose, and the supernatant centrifuged (X12000 g, Beckman J2-21 centrifuge, Beckman Instruments, Germany) for 20 min. The particles were resuspended and washed with 20 volumes of phosphate buffered saline (PBS, 150mM NaCl, 10mM Na2HPO4/NaH2PO4, pH 7.4). The final pellets were recast into five rolls and PBS and protein concentrations were determined using the Bradford assay kit (Bio-Rad Laboratories, USA). 40 pounds of protein per sample was separated by 10% SDS-polyacrylamide gel electrophoresis. The protein was then transferred to a polyvinylidene fluoride membrane. The blot was stained with anti-peptide a1 or a4 antibody (1:1000, Santa Cruz Biotechnology, USA), followed by either horseradish peroxidase-labeled rabbit anti-antibody (1:2000, Zymed laboratories, USA) or anti-goat IgG (1:5000, Vector laboratories, Canada). The bands were detected with DAB staining (Sigma, usa). Beta-actin antibody (1: 1000). The optical density measurement was performed using an image analysis system (densitometer, Rudolph, usa), and bands of different groups of the respective molecular weights of the subunits were analyzed and the values thereof were compared.

4. Results of the experiment

As shown in fig. 2, 1: normal saline and normal saline, 2 normal saline and anti-inebriation composition, 3 alcohol and normal saline, 4 alcohol and 5 alcohol and anti-inebriation composition. In acute alcoholism rats (alcohol + saline group), LORR induced by diazepam was significantly reduced [ P ═ 0.0003], and the duration of gavage administration was about 60min in normal rats (saline + saline group), whereas LORR in acute alcoholism rats was 9.8 ± 3.27min, which was significantly different from that in normal rats [ P ═ 0.0003 ]. The anti-hangover composition of preparation example 1 had no significant effect on LORR duration in normal rats. The anti-hangover composition prepared in preparation example 1 has an obvious recovery effect on LORR time of acute alcoholism rats, as shown in a column 4 in fig. 2, and a measured value is 53.83 ± 6.11min [ P ═ 0.001], and the result shows that the anti-hangover composition has a significant anxiolytic effect in a LORR test induced by diazepam. But the therapeutic effect of administering an anti-hangover composition after alcohol intake is poor (as shown in fig. 2, bar 5). These data indicate that the composition can prevent, but not alleviate, alcohol disorders.

Figure 3 shows that alcoholism significantly reduced the expression of GABAAR a1 subunit in hippocampal tissues, while expression of GABAAR a4 subunit was significantly elevated (B in figures 3 and 5). In fig. 3, 1: normal saline + normal saline; 2: normal saline + anti-hangover composition; 3: normal saline and alcohol; 4: the anti-alcoholism composition plus normal saline; 5: alcohol + physiological saline. Figure 5 is a graph of the effect of an anti-hangover composition on the changes in GABAAR a1 subunit and a4 subunit expression in an alcoholic rat model. (A) Changes in GABAAR a1 subunit expression; (B) changes in GABAAR a4 subunit expression were measured as mean values, where 1: normal saline and normal saline, 2 the normal saline and the antialcoholic composition, 3 the normal saline and the alcohol, 4 the antialcoholic composition and the alcohol, and 5 the alcohol and the antialcoholic composition. GABAARs are a major target of alcohol activity, and a single dose of alcoholism may result in altered GABAAR plasticity, such as increased transcription of a4 and a2 and decreased a1 subunit, with preferential insertion of newly formed a4 into the synapse. To study alcohol withdrawal and dependence in humans, we established a model of Chronic Intermittent Ethanol (CIE) intoxication in rats. CIE rats showed changes in GABAAR subunit composition and subcellular localization. The current research shows that the single-dose alcohol treatment increases the expression of GABAAR a4 subunit and reduces the expression of GABAAR a1 subunit, and by detecting the expressions of GABAAR subunits a1 and a4 by using western blot, the recovery effect of the anti-alcoholism composition on LORR is related to the change of the GABAAR subunits, namely the anti-alcoholism composition can obviously reverse the change, namely the expression of a1 subunit is up-regulated, and the expression of a4 subunit is down-regulated. This data is consistent with the effect of the anti-hangover composition on diazepam-induced LORR recovery.

Efficacy verification of human body feeding trial test applying the anti-hangover composition of example 4

In this embodiment, the efficacy of the anti-hangover composition prepared in preparation example 1 in a human body eating trial test is examined, and the specific test process is as follows:

the powders for preparing the anti-hangover composition prepared in example 1 were administered to 60 drinkers, respectively, and the physical characteristics and the proportion of anti-hangover effect of the anti-hangover composition prepared in example 1 were observed and recorded, with the results shown in fig. 4. In fig. 4, 48 of the test takers who took the anti-hangover composition in the human body test results fed back that the composition has a significant anti-hangover effect, accounting for 80%, which is significantly different from the test takers who fed back no effect (accounting for 20%), indicating that the anti-hangover composition of the present invention can increase the activity of acetaldehyde dehydrogenase in vivo, promote the rapid decomposition of alcohol in vivo, rapidly relieve the hangover of a large number of alcohol intakers, protect the liver, improve acute alcoholic liver injury, improve alcoholism dependency, relieve hangover, and play a role in preventing acute and chronic alcoholism.

Claims

1. The composition is characterized by comprising the following components in percentage by weight:

10 to 60 percent of ampelopsis grossedentata leaves, 1 to 20 percent of hovenia dulcis thunb,

dark plum 1-10 wt%, boat-fruited sterculia seed 1-10 wt%,

0.1 to 1 percent of vitamin C and 25 to 60 percent of auxiliary materials.

2. The composition according to claim 1, wherein the composition comprises the following components in the following proportions by weight:

30 to 50 percent of ampelopsis grossedentata leaves, 1 to 10 percent of hovenia dulcis thunb,

1 to 5 percent of dark plum fruit, 1 to 5 percent of boat-fruited sterculia seed,

0.1 to 0.5 percent of vitamin C and 35 to 50 percent of auxiliary materials.

3. The composition according to claim 2, wherein the composition comprises the following components in the following proportions by weight:

50 percent of ampelopsis grossedentata leaves, 5 percent of hovenia dulcis thunb,

2 percent of dark plum fruit, 2 percent of boat-fruited sterculia seed,

0.15 percent of vitamin C and 40.85 percent of auxiliary material.

4. The composition as claimed in claim 1 to 3, wherein the composition comprises processed powdered extracts of Ampelopsis grossedentata leaf, Hovenia dulcis seed, Prunus mume and Sterculia Lychophora.

5. The composition according to claims 1-3, wherein the auxiliary materials in the composition are selected from one or more of lactose, microcrystalline cellulose, maltodextrin, isomaltooligosaccharide, fruit and vegetable powder, concentrated fruit and vegetable juice, magnesium stearate, silicon dioxide, titanium dioxide, beeswax, purified water, sucralose, edible salt, essence, pigment, glycerol, povidone K30 and gelatin.

6. A preparation method of the composition as claimed in claims 1 to 3, wherein the method comprises the step of mixing Ampelopsis grossedentata leaves, Hovenia dulcis Thunb, Prunus mume, Sterculia lychnophora, vitamin C according to the compatibility ratio.

7. The method of claim 6, wherein the Ampelopsis grossedentata leaves, Hovenia dulcis seeds, Prunus mume, and Sterculia Lychophora are processed to obtain powdered extracts before mixing.

8. Use of the composition of claims 1-3 in the preparation of a functional food for alleviating hangover.

9. Use of a composition according to claims 1 to 3 for the preparation of a medicament for the prevention of acute and/or chronic alcoholism.

10. The use according to claim 9, wherein the composition is prepared as a powder, tablet, granule, capsule, soft capsule or oral liquid.