KR20080035853A - A composition having protective function from alcoholic hangover comprising dropwort extract as active ingredient and functional health food using the same - Google Patents

Abstract

A hangover reducing composition containing a dropwort extract as an active ingredient is provided. A functional health food is prepared by using the same which exerts excellent effects of preventing and treating a hangover without causing any side effect on the body. A whole plant or aerial part of a dropwort is extracted with one or more solvents selected from the group consisting of water and C1-4 lower alcohol at 80 to 100deg.C for 1hr to 1 day. A hangover reducing composition contains an extract of the whole plant or aerial part of dropwort and a food acceptable additive. The solvent is selected from hexane, methylene chloride, acetone, ethyl acetate and chloroform.

Description

A composition having protective function from alcoholic hangover comprising dropwort extract as active ingredient and functional health food using the same}

FIG. 1 is a chart showing the change in blood ethanol concentration after intravenous administration of Buttercup hot water extract to New Zealand rabbit (New zealand white).

Figure 2 is a secondary fraction of the hot water extract of Buttercup extract with n-hexane, methylene chloride, ethyl acetate, n-butanol, etc., ICR mice orally ingested the extract with ethanol, and shows the change in blood ethanol concentration chart.

Figure 3 is a graphical representation of the effect of removing the ethanol in blood according to the amount of n-butanol extract when n-butanol secondary fraction extract of Buttercup hot water extract orally with ethanol in ICR mice.

FIG. 4 is a graph showing the effects of oral intake of Buttercup hot water extract and its n-butanol secondary fraction extract on ICR mice on blood ethanol concentration (4a) and blood acetaldehyde concentration (4b), respectively.

 The present invention relates to a hangover releasing composition containing the buttercup extract as an active ingredient and a functional health food using the same, and more particularly to preparing a hangover releasing composition comprising the extract of the hot water extract and its fraction of the buttercup and as an active ingredient The present invention relates to a food composition having the effect of treating or preventing a hangover by promoting the metabolism of alcohol and acetaldehyde in blood to reduce the physiological side effects of the hangover by preparing a functional health food using the same.

In general, alcohol is said to have the highest concentration in the blood 30 minutes after ingestion on an empty stomach, and 1 hour with diet. Ingested alcohol can be absorbed in small amounts in the gastrointestinal tract, but it is absorbed quickly when moving to the small intestine, which determines the rate of absorption of alcohol is determined by the gastric emptying time of alcohol. Stomach discharge time of alcohol may vary depending on the type and amount of food ingested together. Alcohol absorbed into the blood from the gastrointestinal tract causes a number of central and peripheral physiological reactions, and this action is caused by acetaldehyde, the primary metabolite rather than alcohol itself (Goodman and Gilman's The pharmacological bassis of therapeutics, p 384, 6th ed., 1980). The breakdown of alcohol occurs mainly in the liver. The first process involves the conversion of alcohol in the blood to acetaldehyde by alcohol dehydrogenase in liver cells, which is then decomposed into acetic acid by acetaldehyde dehydrogenase in the liver. Finally metabolized to water and carbon dioxide (Goodman and Gilman's The pharmacological bassis of therapeutics, p 383, 6th ed., 1980).

As mentioned above, the physiological reaction by alcohol is mainly caused by acetaldehyde in the blood, which is characterized by excitement, peripheral vasodilation, headache, etc., and the unpleasant physiological reaction after drinking is called hangover. . Therefore, the main factor that determines the degree of hangover is the amount or activity of acetaldehyde dehydrogenase, which is known to be different according to race or individual. For example, Asians lack acetaldehyde dehydrogenase type II compared to Caucasians and are known to have a severe hangover compared to Caucasians.

Alcohol itself and acetaldehyde can damage cell membranes and cause them to die. Among them, chronic alcohol intake may kill nerve cells that are vulnerable to alcohol and may cause alcoholic dementia and psychosis (Goodman and Gilman's The pharmacological bassis of therapeutics, p 381, 6th ed., 1980).

Recently, many studies and experiments have been conducted to reduce the detoxification of alcohol. RU-21, which was known to be used by the Soviet KGB during the Cold War, suppresses the action of alcohol dehydrogenase and slowly increases the concentration of acetaldehyde in the blood. It is designed to show relatively low hangover phenomenon by suppressing brain function and making body reaction less. However, since RU-21 inhibits the action of alcohol dehydrogenase, blood alcohol concentration is maintained for a longer time, so the poisoning effect of alcohol itself is greater. Therefore, it is preferable to have a function of increasing the action of both alcohol dehydrogenase and acetaldehyde dehydrogenase in order to reduce the detoxification of alcohol itself.

Therefore, the present inventors extract the water by boiling water in the buttercups, the composition containing the extract as an active ingredient to increase the action of both alcohol dehydrogenase and acetaldehyde dehydrogenase in vivo to reduce the blood ethanol and blood acetaldehyde concentration The present invention was completed by confirming the efficacy in improving hangover relief.

It is an object of the present invention to provide a hangover relief composition comprising the buttercup extract as an active ingredient, and a pharmaceutical and functional health food that can be used for the treatment and prevention of the hangover including the same.

The present invention has been made in view of the above-mentioned problems, the purpose of which is to extract a specific ingredient of natural foods and to include it as a certain amount of active ingredient harmless to the living body and has no hangover effect without hangover at all hangover It is to provide a composition for elimination.

Hereinafter, the configuration and operation of the present invention.

In order to achieve the above object, the present invention provides a hangover relief composition comprising the buttercup extract as an active ingredient.

The present invention also provides a method for producing a hangover relief composition using the buttercup extract as a raw material.

In addition, the present invention provides a medicament and functional health food that can treat or prevent the hangover including the composition and a pharmaceutically acceptable carrier or a food acceptable additive.

Hereinafter, the present invention will be described in detail.

The hangover composition of the present invention was obtained by extracting the outpost or ground part of the apiaceae with hot water. At this time, the asteraceae plants include Ostericum coreanum , Oenanthe Javanica javanica ), Oenante Stallonifera ( Oenanthe stolonifera ), including all apiaceae plants.

In addition, in the present invention, water, an organic solvent or a mixed solvent thereof is used as an extraction solvent using an outpost or ground part of the apiaceae plant, and then the active ingredient is extracted and filtered. In this case, the extraction solvent may be water, a low-cost alcohol or dilution of alcohol having 1 (C1) to 4 carbon atoms (C4), but is not limited thereto. The low cost alcohol may be any one of ethanol, methanol, n-butanol, n-propanol, and isopropanol, but is not limited thereto. Preferably, n-butanol may be used. In particular, in the present invention, the buttercup extract is prepared by reflux extraction at 50 to 110 ° C with water, preferably at 80 to 100 ° C for 1 hour to 1 day, and preferably 2 to 3 hours. After extracting the buttercups under reflux with hot water as described above, the content of persicarin as an indicator was analyzed by HPLC, and the persicarin content was 0.23%.

In addition, the buttercup hydrothermal extract may be further fractionated using one or more solvents selected from the group consisting of n-hexane, methylene chloride, acetone, ethyl acetate and n-butanol. The preparation temperature of the fraction fractionated by using an additional solvent to the extract or extract may be 20 to 50 ℃, but is not limited thereto. Extraction time is not particularly limited, but is preferably extracted within 10 minutes to 1 day, and the extraction device may be a conventional extraction device, ultrasonic grinding extractor or fractionator. The extract thus prepared may be removed by hot air drying, reduced pressure drying, and / or lyophilization, but is not limited thereto. Preferably, the extract may be dried under reduced pressure to remove the solvent.

In addition, the present invention provides a pharmaceutical and functional health food that can treat or prevent diarrhea and constipation, comprising the composition and a pharmaceutically acceptable carrier or food acceptable additive.

In order to find out how the hangover composition prepared above substantially affects in vivo , the buttercup extract with ethanol was prepared in New zealand rabbit and ICR mouse. As a result of measuring the concentration of ethanol and blood acetaldehyde in the blood after administration, it was confirmed that the concentration of ethanol and blood acetaldehyde in blood was significantly reduced in the experimental group to which the buttercup extract was administered compared to the control group (FIGS. 1 to 2 and 4). It was confirmed that the efficacy is concentration-dependent (see Figure 3). This is because the composition of the present invention promotes metabolism after ingesting alcohol, thereby lowering blood ethanol and blood acetaldehyde concentrations, and thus can be used as pharmaceuticals and functional health foods that are effective in treating and preventing undesirable phenomena caused by hangovers. It means that there is.

In the present invention, the composition may be used alone, but is not limited thereto. The composition may additionally include a pharmaceutically acceptable carrier or excipient according to the formulation and purpose of use. Excipients including the pharmaceutically acceptable carriers or diluents, preservatives, stabilizers, wetting agents, emulsifiers, solubilizers, sweeteners, coloring agents, osmotic pressure control agents and antioxidants can be used in the conventional formulations, if formulated Fillers, extenders, wetting agents, disintegrating agents or surfactants may be used. At this time, representative diluents or excipients may include water, dextrin, calcium carbonate, lactose, propylene glycol, liquid paratin and physiological saline.

In addition, the composition can be administered orally or parenterally, the formulation of the formulation (PLASTERS), granules (GRANULES), lotions (LOTIONS), powders (POWDERS), syrups (SYRUPS), liquid ( LIQUIDS AND SOLUTIONS), AEROSOLS, OINTMENTS, FLUIDEXTRACTS, Emulsions, EMULSIONS, CAPSULES or PILLS, but are not limited thereto. In addition, the compositions of the present invention may be preferably formulated using methods known in the art or described in Remington's Pharmaceutical Science (latest version), Mack Publishing Company, Easton, PA. The dosage or amount of the composition is preferably used in consideration of the body weight, age, sex, health condition, diet, time of administration, administration method, excretion rate and severity of the disease, the dosage is usually 1 to 250mg / kg, frequency of administration can be administered once or several times a day, preferably in the case of adult (70Kg) divided into 0.5 ~ 2g, three times or four times a day, the administration period is not particularly limited. . In addition, the composition may be used in addition to any food, in addition to oral administration alone.

In addition, the composition of the present invention is useful for suppressing digestion and intestine, obesity, diabetes and hyperlipidemia, as well as diarrhea and constipation, and can be used as a functional health food or health food supplement because it can be taken for a long time without toxicity and side effects. have. In this case, the health food may include drugs, food and beverages, and specifically, various foods, candy, chocolate, drinks, gum, tea, vitamin complexes, health supplements, and the like, powders, granules, tablets It can be used in the form of capsules or beverages. In addition, the amount of the composition added to the food or beverage is not particularly limited, but may be used in 1 to 80% by weight, preferably 1 to 20% by weight of the total food weight, in the case of a health beverage, 0.1 per 100ml To 10 g, preferably 0.5 to 2 g.

At this time, the functional health food may further include a food supplement acceptable food additive with the composition of the present invention. For example, the liquid component used in the health beverage containing the composition is not particularly limited, and may include various flavors or natural carbohydrates as additional ingredients, such as conventional drinks. At this time, examples of the natural carbohydrates include monosaccharides such as glucose and fructose; Disaccharides such as maltose and sucrose; Conventional sugars such as polysaccharides such as dextrin, cyclodextrin and the like and sugar alcohols such as xylitol, sorbitol, and erythritol. In addition, the flavoring agent may be a natural flavoring agent (tauumatin, stevia extract (e.g., Baudioside A, glycyrrhizin, etc.) or synthetic flavoring agents (saccharin, aspartame, etc.). At this time, the ratio of the natural carbohydrate is 0.1 to 20g, preferably 0.5 to 2g per 100ml of the health beverage composition.

In addition, the functional health food includes various nutrients, vitamins, minerals (electrolytes), natural or synthetic flavors, colorants or fillers (such as cheese and chocolate), pectic acid or salts thereof, alginic acid or salts thereof, organic acids, protective properties. It may contain colloidal thickeners, pH adjusters, stabilizers, preservatives, glycerin, carbonation agents used in alcoholic or carbonated beverages, and the like, and may also contain flesh to produce natural fruit or vegetable beverages. At this time, the components may be used alone or in combination. In addition, the ratio of the additive is not particularly limited, but may be selected in the range of 1 to 20% by weight per 100% by weight of the functional health food.

Hereinafter, the specific method of the present invention will be described in detail with reference to Examples, but the scope of the present invention is not limited only to these Examples.

Example  1: buttercup Hydrothermal  Extract manufacturer

After drying the Minari purchased from Pyongyang-ri, Cheongdo-eup, Cheongdo-gun, Gyeongbuk, Korea for 1 week, take 600g and crush it. 164.0g-185.8g was obtained by the yield of 27-31% (Table 1). As a result of analyzing the hot water extract of Buttercup hot water by HPLC, the content of persicarin as an indicator was 0.23%. The HPLC used at this time was Shimadzu LC-10A dual pump, SCL-10vp Controller, SIL-AF autoinjector, and SPD. The SPD-M 10Avp diode array detector was used, and the outflow solvent was flowed through the Shim-pak CLC-ODS at a flow rate of 6 ml / min. The effluent was detected at a wavelength of 253 nm. Methanol was used as the A liquid and distilled water was used as the B liquid, and the solvent was distilled out using the concentration gradient of the two solvents.

Yield According to Extraction Time in Extracting Hot Water from Buttercup Extraction time (hours) Extract (g) yield(%) One 164.0 27.3 2 166.6 27.4 3 185.8 31.0

Example  2: buttercup Hydrothermal  Activity on Ethanol Metabolism of Extracts

In order to observe the change in blood ethanol concentration according to the administration of the buttercup extract, a Newzealand white rabbit (n = 9) weighing about 2.5 kg in body weight and a 20% ethanol solution containing 10% of buttercup hydrothermal extract (yield 27.4%) Plasma ethanol concentration was measured over 5 minutes, 1 hour, 3 hours and 5 hours after administering 500 ul per kg body weight to the vein in the 20% ethanol solution containing 10% physiological saline instead of the administration group and buttercup extract. It was. At this time, metadoxine (metadoxine (trade name; Aldotel)) was used as a control drug and 50 mg / kg body weight was administered in the same manner. In the first experiment, the control group, the buttercup extract group, and the metadoxine group were three dogs, and the group was changed sequentially every week to start the experiment so that the population of each group was nine. Treated with paired and non-paired samples. At this time, the plasma ethanol concentration was used by purchasing a blood ethanol measurement kit of Sigma, USA.

As a result, the plasma ethanol concentration after 5 minutes of administration was no difference between the buttercup extract and the control group, 215 ± 11 mg / dl and 213 ± 13 mg / dl, respectively. The treatment group was 111 ± 5.0mg / dl, which was 9% lower than the control group's 122 ± 6.1mg / dl (p <0.001). After 3 hours, it was 50 ± 2.3mg / dl and the control group was 69 ± 3.3mg / dl. It was 28% lower than the control group (p <0.001), and after 5 hours, it was 33 ± 2.1 mg / dl, which was 39% lower than the control group's 54 ± 2.7 mg / dl (p <0.001). In the currently available metadoxin-administered group, 216 ± 15mg / dl after 5 minutes of ethanol administration, 108 ± 6.2mg / dl after 1 hour, 48 ± 2.5mg / dl after 3 hours and 30 ± 3.0mg / dl after 5 hours Similar to the buttercup extract group, the blood alcohol concentration removal effect was shown. Therefore, the concentration of alcohol decreased to 0.05% of legal alcohol that could be operated after 3 hours of administration of Buttercup extract group and metadoxin, but the control group had a concentration of 54 ± 2.7mg / dl after 5 hours. Exceeded (FIG. 1).

Example  3: buttercup Hydrothermal  Secondary fraction of extract

The hot water extract of Buttercup was suspended in 2 L of distilled water, and extracted three times with the same amount of n-hexane. The n-hexane soluble part was collected, and the solvent was concentrated under reduced pressure to obtain an n-hexane fraction. The remaining water layer was concentrated to 1.5 L, and the same amount of methylene chloride was added and extracted three times. The extracts were combined and the solvent was concentrated to remove the methylene chloride fraction. The remaining water layer was concentrated to 1.2 L again, and then the same amount of ethyl acetate was added and extracted three times. The extracts were put together to form an ethyl acetate fraction. The remaining water layer was concentrated to 1 L again, followed by extraction three times with the same amount of n-butanol, and the extracts were collected, and the solvent was concentrated and removed to obtain n-butanol fraction. The remaining water layer was completely concentrated to give a water fraction.

Example  4: buttercup Hydrothermal  Activity on Ethanol Metabolism of Secondary Fractions of Extracts

Secondary fraction samples of the five kinds of Buttercup hot water extracts obtained in Example 3 were examined for ethanol metabolism in ICR mice (about 30 gram body weight). While administering 30% ethanol or 8 ml / kg body weight to ICR mice, each of the secondary fractions of the buttercup hydrothermal extract was orally administered to 200 mg in the dry parsley weight per kg body weight, and blood ethanol concentration was administered. Measured after 2 hours.

As a result, the blood ethanol concentration was 68 ± 8.1mg / dl in the n-hexane fraction group, 83 ± 1.9mg / dl in the methylene chloride fraction group, 70 ± 14.3mg / dl in the ethyl acetate fraction group, and in the n-butanol fraction group. 15 ± 1.1 mg / dl, and 70 ± 5.7 mg / dl in the control group (Fig. 2). Therefore, only n-butanol fraction in the secondary fraction of Buttercup hot water extract significantly decreased blood ethanol concentration, which was similar to blood ethanol concentration (14 ± 2.9mg / dl) obtained from the control group metadoxin administration group. This means that the n-butanol fraction of the hot water extract of Buttercup contains the active ingredient which decreases the ethanol concentration in the blood and resolves hangover.

In order to confirm whether the hangover activity of the n-butanol fraction of Buttercup hot water extract is concentration-dependent, and to investigate the effective concentration, the buttercup hot water was orally administered 30 ml of ethanol to 8 ml / kg of body weight. The n-butanol fraction of the extract was orally administered to 25, 50, 100, and 200 mg of dry buttercup per kg body weight, respectively, and the blood ethanol concentration was measured 2 hours after administration. As a result, when the n-butanol fraction was administered at 25 mg / kg of mouse weight, the blood ethanol concentration was 72 ± 8.8mg / dl, which was not different from the blood ethanol concentration 77 ± 7.2mg / dl in the control group. In the case of administration, the blood ethanol concentration was 65 ± 7.6 mg / dl, 100 mg / kg was 51 ± 6.8 mg / dl, and 200 mg / kg was 40 ± 5.9 mg / dl. It was found that the decrease was dependent on the dose depending on the dose of the n-butanol fraction. Especially, when the n-butanol fraction corresponding to 200 mg / kg was administered, the serum ethanol concentration (35 ± 3.8 mg / dl) (Figure 3). Therefore, it was found that there is an active substance which can reduce the concentration of ethanol in blood in the n-butanol fraction of the hot water extract of Buttercup, and this active substance has a concentration-dependent effect on the removal of blood ethanol.

Example  5: buttercup Hydrothermal  Extracts and n- Butanol  Hangover Relief Activity of Fractions

Since the n-butanol fraction of the Buttercup hot water extract in Example 4 showed a strong ethanol removal effect, in order to determine whether the Buttercup hot water extract and its n-butanol fraction exhibit hangover activity, acetaldehyde causing hangover The blood concentration of was observed. Specifically, oral administration of 30% ethanol to 8 ml / kg body weight of male ICR mice, oral administration of the Buttercup hydrothermal extract and its n-butanol fraction to 200 mg in the dry amount of parsley before extraction per kg of body weight, administration 2 After time, blood ethanol concentration and blood acetaldehyde concentration were measured. At this time, the concentration of acetaldehyde in blood was measured by the Boehringer Mannheim measuring kit.

As a result, the blood ethanol concentration of the Buttercup hot water extract administration group was 42 ± 3.9 mg / dl, 44% lower than 75 ± 8.2mg / dl of the control group, and 70 ± 22 ± 3.0mg / dl in the n-butanol secondary fraction administration group. The percentage was decreased by 67% at 25 ± 2.8 mg / dl in the control group metadoxin (Figure 4a).

On the other hand, blood acetaldehyde concentration was 0.325 ± 0.031mg / dl in the hot water extract administration group of Buttercup, which was reduced by 24% compared to 0.425 ± 0.039mg / dl obtained in the control group, and 0.305 ± 0.029mg / in the n-butanol secondary fraction administration group. It was measured in dl and decreased by 28%. However, in the control group metadoxin-treated group was observed 0.355 ± 0.025 mg / dl showed a tendency to decrease only 16% (Fig. 4b).

In general, the faster the ethanol removal, the higher the acetaldehyde concentration in the blood. Thus, the actual acetaldehyde concentration in the blood was 47% compared to the control group compared to the control group, and 47% compared to the control group, but it was 58 in the n-butanol secondary fraction group. %, Metadoxin can be estimated to have a 50% acetaldehyde removal effect in the group.

Example  5: buttercup Hydrothermal  Extracts and n- Butanol  Observation of tissue change according to fractional administration

In order to observe the occurrence of acute side effects according to the administration of the Buttercup hot water extract and its n-butanol fraction, the dose in Example 4 was increased by 10 times and administered to ICR mice in the same manner, and the brain, cerebellum, Each tissue such as heart, liver, kidney, small intestine, pancreas, and skeletal muscle was cut and examined, but no significant tissue changes were observed in each tissue compared with the normal control group.

As described above, as described through the examples, the buttercup extract, preferably the hydrothermal extract or n-butanol fraction thereof of the present invention shows activity in preventing and resolving hangover by reducing blood ethanol and blood acetaldehyde concentration, Since it is not observed, pharmaceuticals and functional health foods containing buttercup extracts can be used as effective hangover-removing compositions. Especially, by extracting and producing certain ingredients of natural foods, they are harmless to humans and have excellent side effects without hangovers. It is expected to be effective and relatively less toxic than a large dose of a single component, and not expected to be addictive compared to chemically synthesized and marketed drugs, which can provide a hangover prevention and remedy that is harmless to the human body. Has excellent effect, so food, pharmaceutical acid The very useful inventions.

Claims (8)

Hangover relief composition comprising an extract of the outpost or ground portion of the apiaceae plant extracted with at least one extraction solvent selected from the group consisting of water and 1 to 4 carbon atoms of low cost alcohol. According to claim 1, The extract is a hangover relief composition extracted by reflux for 1 hour to 1 day at 80 ~ 100 ℃ with water. The method of claim 1, wherein the extract is hexane, methylene chloride, acetone, ethyl acetate and chloroform composition for the hangover, characterized in that further fractionated using one or more solvents selected from the group consisting of. Method of producing a hangover relief composition comprising the step of extracting the outpost or the ground part of the apiaceae plant with at least one extraction solvent selected from the group consisting of water and a low-cost alcohol having 1 to 4 carbon atoms and removing the extraction solvent . The method of claim 4, wherein the extraction solvent is water or n-butanol. The method of claim 4, further comprising the step of extracting with an extraction solvent and fractionating using at least one solvent selected from the group consisting of n-hexane, methylene chloride, acetone, ethyl acetate and n-butanol. Method of producing a composition for elimination. Hangover reliever comprising a composition according to any one of claims 1 to 3 and a pharmaceutically acceptable carrier. A functional health food for hangover resolution comprising the composition according to any one of claims 1 to 3 and a food supplement acceptable food supplement.

Images