JP2003137788A - Agent for mitigating discomfortable symptom in alcoholic drinking - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an agent for promoting the excretion of acetaldehyde causing drunken sickness from the body without changing the blood concentration of alcohol. SOLUTION: The acetaldehyde excretion promoting agent contains sodium ion and glucose at a sodium ion: glucose molar ratio of 1:(1.5-3.0).

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention exerts an excellent effect in suppressing and / or preventing unpleasant symptoms such as nausea and other discomforts caused by excessive drinking, nausea, vomiting, hangover, dizziness, and bad breath. Acetaldehyde excretion enhancer.

[0002]

2. Description of the Related Art Unpleasant symptoms such as nausea and other discomfort, nausea, vomiting, hangover, and dizziness, which are harmful effects due to excessive drinking, are considered to be mainly due to acetaldehyde, which is a metabolic product of alcohol, according to conventional studies. Research on methods for reducing acetaldehyde has been made in the past.

As such a method, a method of increasing the activity of acetaldehyde dehydrogenase whose main purpose is to promote the metabolism of alcohol, and a method of administering amino acids such as cysteine and ascorbic acid have been reported. ("Alcohol metabolism", Shinko Medical Publishing Co., Ltd., 1988). In addition, an alcohol metabolism promoter using corn protein as a raw material (JP-A-7-
258881), D-cysteine and / or an alcohol metabolism promoter containing a salt thereof (JP-A-3-7432).
7), an alcohol metabolism promoter (Japanese Unexamined Patent Publication (Kokai) No. 6-14746), which contains a quercetin glycoside, a divalent metal ion and a licorice extract as essential components, is disclosed.

[0004] However, when the metabolism of alcohol is promoted, the blood concentration of alcohol decreases, so that the effects of intoxication, uplifting feeling, stress relief, fatigue recovery, and appetite gain obtained by ingesting alcohol are lost. Will end up.

[0005]

In view of the above problems, an object of the present invention is to provide an agent for promoting excretion of acetaldehyde, which causes harmful effects of drinking, without changing the blood concentration of alcohol. Especially.

[0006]

Means for Solving the Problems The inventors of the present invention include sodium ion and glucose, and the molar ratio of sodium ion and glucose is 1: 1.5 to 3.0, preferably Na ⁺ 30 to 90 mEq / L K ^{+ 10 to} 30 mEq / L Ca ^{2+ 0 to 3} mEq / L Mg ^{2+ 0 to 3} mEq / L phosphorus 0 to 3 mmol / L organic acid 0 to 50 mEq / L drinking water-electrolyte beverage or jelly It was found that ingestion before and after promotes excretion of acetaldehyde, which is an alcohol metabolite, regardless of the amount of alcohol consumed. Further, the present inventors have found that the above-mentioned water electrolyte beverage or jelly does not change the blood concentration of alcohol and reduces only the blood concentration of acetaldehyde, and further studied based on these findings. As a result, the present invention has been completed.

That is, the present invention provides (1) an acetaldehyde excretion enhancer after drinking, characterized in that the molar ratio of sodium ion to glucose is 1: 1.5 to 3.0, which contains sodium ion and glucose. . (2) The acetaldehyde excretion enhancer according to (1) above, which has an osmotic pressure of 250 to 350 mOsm / L. (3) The acetaldehyde excretion enhancer according to the above (1) or (2), which contains the following components. Na ⁺ 30 to 90 mEq / L K ⁺ 10 to 30 mEq / L Ca ^{2+ 0 to 3} mEq / L Mg ^{2+ 0 to 3} mEq / L Phosphorus 0 to 3 mmol / L Organic acid 0 to 50 mEq / L (4) Contains components of the following composition The acetaldehyde excretion enhancer according to (1) or (2) above. Na ⁺ 40-60 mEq / L K ⁺ 16-24 mEq / L Ca ²⁺ 0-3 mEq / L Mg ²⁺ 0-3 mEq / L Phosphorus 0-3 mmol / L Organic acid 0-50 mEq / L (5) Being a beverage or jelly The acetaldehyde excretion enhancer according to any one of (1) to (4) above. Regarding

[0008]

BEST MODE FOR CARRYING OUT THE INVENTION In the present invention, Na ⁺ , K ⁺ ,
As a source of Ca ²⁺ , Mg ²⁺ , phosphorus or an organic acid, one known per se may be used. The electrolyte component may be an inorganic electrolyte component or an organic electrolyte component. Examples of the inorganic electrolyte component include salts of alkali metals or alkaline earth metals such as chlorides, sulfates, carbonates, and phosphorus oxides. Further, as the organic electrolyte component, for example, citric acid, lactic acid,
Examples thereof include salts of amino acids (eg, glutamic acid, aspartic acid, etc.), alginic acid, malic acid or gluconic acid, and alkali metals or alkaline earth metals. These may be used alone or in combination of two or more.

In the present invention, the sodium ion concentration is preferably about 30 to 90 mEq / L, more preferably about 40 to 60 mEq / L. Examples of the source of sodium ions include sodium chloride, sodium sulfate, sodium lactate, sodium glycerophosphate, sodium acetate, sodium phosphate, sodium hydrogen phosphate or sodium dihydrogen phosphate, and the like. Sodium lactate or sodium dihydrogen phosphate, or a mixture of any two or more thereof is preferable.

In the present invention, the concentration of potassium ion is
It is preferably about 10 to 30 mEq / L, more preferably about 16 to 24 mEq / L. Examples of the source of potassium ions include potassium chloride, potassium sulfate, potassium glycerophosphate, potassium lactate, potassium acetate, potassium phosphate, potassium hydrogen phosphate, potassium dihydrogen phosphate, and the like, with potassium chloride being preferred. .

In the present invention, the concentration of magnesium ion is preferably about 0 to 3 mEq / L, more preferably about 1.9 to 2.1 mEq / L. Examples of the magnesium ion supply source include magnesium chloride, magnesium sulfate, magnesium lactate, magnesium glycerophosphate, magnesium acetate, and the like, with magnesium sulfate being preferred.

In the present invention, the concentration of calcium ion is preferably about 0 to 3 mEq / L, more preferably about 1.9 to 2.1 mEq / L. Examples of the calcium ion supply source include calcium chloride, calcium gluconate, calcium lactate, calcium glycerophosphate, calcium acetate, and the like. Among them, calcium gluconate is preferable, and calcium glycerophosphate is more preferable.

In the present invention, the concentration of phosphorus is preferably about 0 to 3 mmol / L, more preferably about 1.9 to 2.
It is 1 mmol / L. Here, the phosphoric acid is partially dissociated in an aqueous solution to generate H ₂ PO ₄ ⁻ , HPO ₄ ^2−, or PO ₄
^{Yields 3-} . Therefore, in the present invention, the total sum of these phosphorus is expressed as "mmol / L". Examples of the source of phosphorus include phosphoric acid or salts of phosphoric acid with an alkali metal or an alkaline earth metal, among which sodium phosphate, sodium hydrogen phosphate,
Sodium dihydrogen phosphate, potassium phosphate, potassium hydrogen phosphate, potassium dihydrogen phosphate, calcium phosphate or calcium hydrogen phosphate is preferable, and sodium dihydrogen phosphate is more preferable.

In the present invention, the concentration of the organic acid is preferably about 0-50 mEq / L, more preferably about 15-50.
mEq / L, more preferably about 15-33 mE with lactic acid
About 15-45 mEq / q / L and / or citric acid
Let L. When lactic acid and citric acid are used together as the organic acid, the total content of lactic acid and citric acid is 50 mEq.
/ L shall not be exceeded. As a source of organic acid,
Examples thereof include salts of citric acid, lactic acid, amino acids (eg, glutamic acid, aspartic acid, etc.), alginic acid, malic acid or gluconic acid, and alkali metals or alkaline earth metals. Alternatively, two or more of these may be mixed. Among them, lactic acid, sodium lactate, citric acid, trisodium citrate or a mixture thereof is preferable.

In the present invention, sodium ions and glucose are mixed in a molar ratio of preferably about 1: 1.5 to 3.0, more preferably about 1: 1.8 to 2.5. Is a preferred embodiment of the present invention. The glucose content can be determined immediately from the above.

The water electrolyte beverage or jelly according to the present invention preferably has an osmotic pressure of about 250 to 350 mOsm.
/ L, more preferably about 270-310 mOsm / L. This is because such an osmotic pressure is close to the osmotic pressure of body fluid and the water-electrolyte beverage or jelly according to the present invention is easily absorbed.

In addition to the above-mentioned components, the water electrolyte beverage according to the present invention may optionally contain various nutrients, vitamins, flavorings such as synthetic flavors or natural flavors, coloring agents, flavor substances such as cheese and chocolate, or synthetic sweeteners. Etc. may be added and blended. The vitamins may be water-soluble or fat-soluble, for example, retinol palmitate, tocopherol, bisbentamine, riboflavin, pyridoxine hydrochloride, cyanocobalamin, sodium ascorbate, cholecalciferol, nicotinamide, pantothene. Calcium acid, folic acid, biotin, choline bitartrate and the like can be mentioned. Moreover, since the water-electrolyte beverage according to the present invention is used as a fruit juice drink or a vegetable drink, natural fruit juice or pulp may be added. The above additives may be used alone or in any combination of two or more. The mixing ratio of the above additives is not particularly limited, but for example, the water electrolyte beverage 100 according to the present invention
It can be selected from the range of about 0 to 20 parts by weight with respect to parts by weight.

Further, the present invention may be a jelly confectionery.
In this case, as a gelling agent, for example, agar, gelatin, carrageenan, gellan gum, xanthan gum, locust bean gum, pectin, sodium alginate,
It is possible to use potassium alginate or one or more of the thickening polysaccharides that can be usually used. Preferably agar,
At least one of carrageenan, xanthan gum, and locust bean gum is used. The mixing ratio of these gelling agents is
A ratio of 2 parts by weight or less is preferable with respect to 100 parts by weight of jelly confectionery.

When all of the above components are prepared as the water-electrolyte beverage or jelly according to the present invention, the preparation method is not particularly limited, and all components may be mixed at the same time. It may be prepared by adding and mixing other components or a mixture of other components to the mixture prepared by mixing them separately. The mixing operation of each of the above components may be carried out at room temperature or may be carried out under a slight heating.

The water-electrolyte beverage or jelly according to the present invention exerts an action of promoting excretion of acetaldehyde during drinking, and therefore has an effect of preventing hangover, hangover, dizziness, vomiting and the like by ingesting before and after drinking. can get. The water-electrolyte beverage or jelly according to the present invention has a better effect, preferably when ingested after drinking.

The ingestion amount of the water-electrolyte beverage or jelly according to the present invention varies depending on the age, weight, and degree of alcohol consumption of the ingesting person, and therefore cannot be said to be unconditional. Further, since the toxicity is extremely low, You may take as much as you want. For example, the water electrolyte beverage according to the present invention is 1 to 50 m
L / kg / hour or 1 to 100 mL / kg / day is preferably ingested.

[0022]

EXAMPLES Example 1 With the composition shown in Table 1, each component was dissolved in 800 mL of distilled water, and after stirring, distilled water was further added to bring the total amount to 1 L. The solution was sterilized at 115 ° C. for 30 seconds, cooled to 93 ° C. and filled in a PET bottle to obtain a water electrolyte beverage according to the present invention. The obtained water electrolyte beverage is referred to as OS-1 in the following test examples.

[0023]

[Table 1] (*) The phosphorus concentration in the table is not mEq / L but m
It is mol / L.

Example 2 The electrolyte, glucose and powder agar shown in Table 2 were dissolved in 800 mL of distilled water, and after stirring, distilled water was further added to bring the total amount to 1 L. 80 the solution
The powder agar was melted at 5 ° C for 5 minutes, then filled in a cheer bag and sterilized at 95 ° C for 33 minutes to obtain a water electrolyte jelly according to the present invention.

[0025]

[Table 2] (*) The phosphorus concentration in the table is not mEq / L but m
It is mol / L.

[Test Example 1] Effect on linear walking disorder in mice 20 Crj: CD-1 (ICR) male mice (purchased from Japan Charles River KK) fasted for 24 hours were administered with OS-1. 6 mL / kg (50 v / 50 mg / kg) as ethanol for all mice.
12 mL / kg) was orally administered as v% ethanol. 45 minutes, 60 minutes, and 75 minutes after administration of ethanol, OS-1 or distilled water was added to each group at 40 mL / k.
Oral administration was performed. 30 minutes, 90 minutes after administration of ethanol,
After 120 minutes, 150 minutes, 180 minutes, and 240 minutes, the influence of ethanol on the linear walking of mice was examined.

For straight walking, width 2c installed at an angle of 45 degrees
m, the distance the mouse walks on a 100 cm long rod is 1
It was measured for 0 minutes. Maximum measurement distance within 10 minutes (100c
When it reached m), it was 100 cm, and when it was difficult to fall off or walk further, the distance to it was used as the measured value of the solid. The results are shown in Table 3 and FIG.

[0028]

[Table 3] The values in the table represent mean ± standard error. (※※: vs Water at P <0.01, St
undent-t test)

After the oral administration of ethanol, the mice were drunk in the distilled water administration group, the walking distance gradually decreased, and the mice hardly moved 120 minutes to 180 minutes after the oral administration of ethanol. 240 minutes after oral administration of ethanol, a partial recovery tendency was shown. On the other hand, the OS-1 administration group showed a rapid recovery tendency after ethanol administration, and a significant recovery was observed after the 150-minute value as compared with the distilled water administration group (P <0.0.
1, P <0.05). After 180 and 240 minutes,
Almost all mice climbed a 100 cm stick.

[Test Example 2] Effects on plasma ethanol and acetaldehyde concentrations in mice OS: 48 Crj: CD-1 (ICR) male mice (purchased from Japan Charles River Co., Ltd.) fasted for 24 hours were used as OS. -1 (prepared with the same composition as in Test Example 1) administration group and distilled water administration group. Within each group, it was further divided into 3 groups of blood sampling groups at 90 minutes, 150 minutes and 240 minutes after ethanol administration, and each group had 8 animals. After oral administration of 6 mL / kg as ethanol (12 mL / kg as 50 v / v% ethanol) to all mice, 4
After 5 minutes, 60 minutes, and 75 minutes, 40 mL / kg of OS-1 or distilled water was orally administered. 9 after administration of ethanol
After 0 minutes, 150 minutes, and 240 minutes, one group each was collected under ether anesthesia from the abdominal inferior aorta, and EDTA-2K was used.
Anticoagulation treatment was performed with and plasma was collected. Plasma ethanol was analyzed by the HS-GC / MS method, and acetaldehyde was analyzed by the derivatization HPLC-FL method. The results are shown in Table 4,
5 and FIGS.

[0031]

[Table 4] The values in the table represent mean ± standard error.

[0032]

[Table 5] The values in the table represent mean ± standard error. (※※: vs Water at P <0.01, St
undent-t test)

The OS-1 administration group showed no significant difference in plasma ethanol concentration compared with the distilled water administration group, but the plasma acetaldehyde concentration was 9 after administration of ethanol.
A significant reduction (decreased to 50% or less, P <0.01) was observed at the 0-minute value and the 150-minute value.

[Test Example 3] Rat plasma GOT, GPT
Effects of 24 CrJ: Wistar male rats (purchased from Japan Charles River KK) fasted for 24 hours
S-1 (prepared with the same composition as in Test Example 1) administration group and distilled water administration group were divided into two groups. After oral administration of 7 mL / kg as ethanol to all rats, 45
After 60 minutes, 60 minutes, and 75 minutes, 20 mL / kg of OS-1 or distilled water was orally administered, and 240 minutes after the administration of ethanol, whole blood was collected from the inferior abdominal vena cava under ether anesthesia. GOT and GPT activities were measured for blood sampling. The results are shown in Table 6 and FIG.

[0035]

[Table 6] The values in the table represent mean ± standard error.

In the distilled water administration group, GOT activity and GP
Although an increasing tendency was observed in both T activity, the OS-1 administration group showed almost normal values.

[0037]

The acetaldehyde excretion enhancer of the present invention has the effect of promoting excretion of acetaldehyde without changing the alcohol concentration in the blood. Therefore, by ingesting it as a drink or jelly before and after drinking alcohol, It is expected to be effective in preventing unpleasant symptoms such as hangover, nausea, and nausea. Further, by ingesting the acetaldehyde excretion enhancer of the present invention, an effect of preventing organ damage such as liver caused by ingesting alcohol can be obtained.

[Brief description of drawings]

FIG. 1 is a diagram comparing straight-line walking distances between an OS-1 administration group and a distilled water administration group. In the figure, the black square is OS-
One administration group is shown, and a black diamond indicates a distilled water administration group. ** in the figure is vs Water at P <0.01, St
FIG. 7 shows a unit-t test.

FIG. 2 is a diagram comparing blood ethanol concentrations in an OS-1 administration group and a distilled water administration group. The white bar graph on the left shows the distilled water administration group, and the bar graph on the right shows OS.
-1 shows the administration group.

FIG. 3 is a diagram comparing blood acetaldehyde concentrations in the OS-1 administration group and the distilled water administration group. The white bar graph on the left shows the distilled water administration group, and the bar graph on the right shows the OS-1 administration group. * In the figure is vs Wat
er at P <0.01, Student-t test.

FIG. 4 is a diagram comparing the plasma GOT and GPT activities of the OS-1 administration group and the distilled water administration group. The white bar graph on the left shows the distilled water administration group, and the bar graph on the right shows the OS-1 administration group. The thick horizontal line in the figure shows the background data of healthy rats.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 33/42 A61K 33/42 4C206 A61P 3/00 A61P 3/00 // A23L 1/06 A23L 1/06 1/29 1/29 2/38 2/38 Z 2/52 2/00 FF term (reference) 4B017 LC03 LK01 LK12 LL09 4B018 LB01 LB08 LE04 LE05 MD02 MD28 ME14 4B041 LD01 LK02 LK10 4C076 AA09 AA12 BB01 CC21 CC40 4C086 AA01 AA02 EA01 HA02 HA04 HA19 HA24 MA02 MA03 MA04 MA17 MA28 MA52 NA14 ZC21 4C206 AA01 AA02 DA02 DA34 MA02 MA03 MA04 MA37 MA48 MA72 NA14 ZC21

Claims (5)

[Claims] 1. A sodium ion-to-glucose molar ratio including sodium ions and glucose is 1: 1.5 to 3.
An acetaldehyde excretion enhancer after drinking characterized by being 0. 2. The acetaldehyde excretion enhancer according to claim 1, which has an osmotic pressure of 250 to 350 mOsm / L. 3. The acetaldehyde excretion enhancer according to claim 1, which contains the following components. Na ⁺ 30 to 90 mEq / L K ⁺ 10 to 30 mEq / L Ca ^{2+ 0 to 3} mEq / L Mg ^{2+ 0 to 3} mEq / L Phosphorus 0 to 3 mmol / L Organic acid 0 to 50 mEq / L 4. The acetaldehyde excretion enhancer according to claim 1, which contains the following components. Na ⁺ 40 to 60 mEq / L K ⁺ 16 to 24 mEq / L Ca ^{2+ 0 to 3} mEq / L Mg ^{2+ 0 to 3} mEq / L Phosphorus 0 to 3 mmol / L Organic acid 0 to 50 mEq / L 5. The acetaldehyde excretion enhancer according to claim 1, which is a beverage or jelly.