JPH0859482A - Alcohol absorption suppressing agent - Google Patents

Abstract

PURPOSE: To provide an alcohol absorption suppressing agent containing beet saponin as an active component, effective for suppressing the alcohol concentration in blood to suppress the development of uncomfortable symptom such as drunken sickness and suitable for preventing the harmful influence of drink by reducing the load on the liver, etc. CONSTITUTION: This suppressing agent contains a beet saponin consisting of oleanolic acid 3-O-β-D-glucopyranoside uronic acid ester of formula as an active component. The compound of formula can be produced by extracting dried beet pulp with a sodium hydroxide solution under heating, treating the extracted liquid with a UF membrane having a fractionation molecular weight of 20,000, acidifying the permeated liquid, separating the precipitate by centrifugal separation, drying and crushing the separated solid to obtain a crude beet saponin and separating and purifying the crude product by silica gel column chromatography. The suppressing agent is administered to an adult by oral administration before drinking at a rate of 20-100mg/dose in terms of the weight of the compound of formula.

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to an alcohol absorption inhibitor containing beet saponin as an active ingredient.

[0002]

BACKGROUND OF THE INVENTION Sugar beet is a plant of the family Rhinoceros and is commonly called beet. It is cultivated in large quantities to produce sugar from this rape root. Beet saponin is added to the leaves and roots in an amount of 0.1 to 0. Contains 2%.

Since there has been no report on the effective use of beet saponin, the present inventors have previously conducted research on this and beet from beet pulp extracted from beet pulp (beet pulp) and the like, which are abundantly discharged in sugar mills. Saponin was easily extracted in good yield, and the crude beet saponin was subjected to a pharmacological test. As a result, the efficacy against hyperlipidemia and ulcer was found (Japanese Patent Publication No. 5-7399).

[0004]

In order to utilize beet saponin more effectively, the alcohol absorption suppressing effect of beet saponin is studied. No report has been made on the effect of beet saponin to suppress alcohol absorption.

[0005]

[Means for Solving the Problems] Therefore, first, a method for producing pure beet saponin was studied, and crude beet saponin was purified by silica gel to obtain the following formula (1).

Embedded image It was found that oleanolic acid 3-O-β-D-glucopyranoside uronic acid (hereinafter abbreviated as OGA) represented by can be produced in good yield.

Next, as a result of research on the alcohol absorption inhibiting effect of OGA and crude beet saponin, it was found that beet saponin has an excellent alcohol absorbing inhibiting effect.

[0007] Therefore, when beet saponin is taken during drinking, the blood alcohol concentration is suppressed to suppress the development of unpleasant symptoms such as sickness, and the burden on the liver and the like is reduced to prevent the harmful effects of drinking. You can

Beet saponin can be orally administered in the form of powder, granules or tablets by itself or in admixture with a suitable pharmacologically acceptable additive.

For example, excipients such as starch, sucrose, lactose, D-sorbitol, crystalline cellulose, binders such as polyvinylpyrrolidone, methyl cellulose, hydroxypropyl cellulose, gum arabic and gelatin, disintegrating agents such as carboxymethyl cellulose calcium, talc. , Magnesium stearate, polyethylene glycol, and other lubricants and flavoring agents can be used to prepare powders, granules, tablets, or the like.

The dose of OGA varies depending on the patient's symptoms, age, weight, etc.
100 mg is orally administered before drinking.

The present invention will be further described below in the form of production examples, test examples and examples of the present invention. Production Example Production of Crude Beet Saponin and OGA To 10 kg of dried beet pulp, 60 l of 0.18% sodium hydroxide solution was added, and after heating at 40 ° C. for 4 hours, this extract was treated with a 20,000 fraction UF membrane to give a permeate. 35% Hydrochloric acid was added to make the mixture acidic, and the precipitate was centrifuged, dried and ground to obtain 171 g of crude beet saponin (purity 22%). 100 g of this crude beet saponin was subjected to silica gel column chromatography (Silica gel G60-230 mesh 3k manufactured by Merck & Co., Inc.).
g, elution solvent chloroform-methanol-water mixed solvent) to obtain 20 g of OGA. This was recrystallized from methanol to obtain colorless needle crystals having a melting point of 264 to 267 ° C (decomposition).

The ¹³ C-NMR spectrum of OGA is shown in Table 1.
Shown in

[Table 1]

Test Example Alcohol Absorption Inhibitory Effect Male Wistar rats (body weight 125-
The test substance was orally administered to 150 g). 20 after an hour
% (V / V) ethanol was orally administered at a rate of 5 ml / kg, and was kept under anesthesia restraint over time (only within 2 minutes when collecting blood)
About 0.4 ml of blood was collected from each jugular vein. The test substance was suspended in gum arabic powder and orally administered at a rate of 5 ml / kg.

The results are shown in Table 2.

[Table 2]

According to Table 2, beet saponin (purity 22
%) In the 200 mg / kg administration group and OGA in the 25 mg, 50 mg and 100 mg / kg administration groups, a significant blood ethanol concentration-suppressing effect is observed at 1 to 3 hours compared with the control group. Oleanolic acid, which is an aglycone of beet saponin, has no inhibitory effect in the 100 mg / kg administration group.

Example 1. Powders The following ingredients are used, and the 12th revised Japanese Pharmacopoeia General Regulations No. 1
A powder was prepared according to item 3. Take 1 packet per adult before drinking.

Example 2. Granules The following ingredients are included in the 12th revised Japanese Pharmacopoeia General Regulations No. 7
The granules were manufactured according to the section. Take 1 packet per adult before drinking.

Example 3. Tablets Take the following ingredients, and twelfth revised Japanese Pharmacopoeia General Regulations No. 1
Tablets were produced according to paragraph 5. Take 2 tablets once per adult before drinking.

[0019]

INDUSTRIAL APPLICABILITY According to the present invention, beet saponin has an excellent inhibitory effect on alcohol absorption, so that it suppresses the development of unpleasant symptoms such as sickness, reduces the burden on the liver and the like, and prevents the harmful effects of drinking alcohol. Can defend.

Claims (1)

[Claims] 1. An alcohol absorption inhibitor containing beet saponin as an active ingredient.