JPS6124597A - Antidiabetic agent - Google Patents

Abstract

PURPOSE:To provide an antidiabetic agent containing ginsenoside-Rb2 of ginseng saponins separated from ginseng, as an active component, having hypoglycemic activity, and administrable continuously for a long period without causing side effects. CONSTITUTION:The objective antidiabetic agent can be prepared by (1) using ginsenoside Rb2 which is a ginseng saponin separated from ginseng (e.g. Panax ginseng), represented by the formula (ara is alpha-L-arabinopyranose; glc is beta-D- glucose) and having the chemical name of 20S-protopanaxadiol-3-[O-beta-D-glucopyranosyl(1 2)-beta-D-glucopyranoside]-20-[O-alpha-L-arabinopyranosyl( 1 6 )-beta-D-glucopyranoside], as an active component, (2) mixing the ginsenoside with lactose or corn starch, and (3) granulating the mixture by using hydroxypropylcellulose as a binder.

Description

DETAILED DESCRIPTION OF THE INVENTION (Industrial Application Field) The present invention relates to an antidiabetic agent containing ginsenoside Rb2 as an active ingredient.

(Prior art and problems to be solved by the invention) Ginsenoside Rbtij, ginseng (Panax ginseng P)
Anax ginseng C, A, MEYER root) is a carrot saponin isolated by the chemical name and chemical structure shown below (Chemical & Pharma 7 Euthycarbretein (S, 5ANAD et, al.
,.

Chem, Pharm, Bull,) Volume 22, 42
1, 1974).

Chemical name=208-grotopanaxadiol-3-[1β
-D-Curcohyranosyl(1→2)-β-〇-/L-arabinopyranosyl(1→6)-β-D-Glucobyranosidol aha-α −
L-7 Rabinobilanose glc-β-D-glucose Carrots have been known to have a wide variety of pharmacological actions, but no clear empirical research has been conducted on the antidiabetic action of saponin components in carrots. Report on wood, armpits, etc. (published by Kyoritsu Publishing Co., Ltd., medicinal ginseng, first edition 169 pages)
according to.

The hypoglycemic effect of carrot saponin on alloxan-induced diabetic mice is rather negative.

(Means for Solving the Problems) The present inventors have been investigating the effects of various carrot saponins on biological metabolism for many years, but quite unexpectedly, we found that ginsenoside Rb2 in carrot saponins has a significant Antidiabetic effects were observed.

As a method for investigating the above pharmacological action of ginsenoside Rb2, a method of measuring the glucose content in the serum of hyperglycemic rats is adopted. The hypoglycemic effect, toxicity, etc. of ginsenoside Rb will be shown below along with test methods.

Experiment 1. Hyperglycemia lowering test on streptocytosine-induced diabetic rats (1) Preparation of pathological animals Wistar male rats (body weight around 120 g) were used.

Solid feed (24.0% CE-2 protein manufactured by Nippon Talea).

Fat (3.5%, carbohydrate 60.5%) and water were available ad libitum, and the breeding room was maintained at constant temperature and humidity (25° C., relative humidity 60%), with a light/dark cycle every 12 hours. Streptocytosine was added at 65μ/kg body weight (10mM, citrate buffer (
After 4 to 5 days, blood was collected from the tail vein and measured using an enzyme method (glucose oxidase method), and the blood sugar level was confirmed. They served as a subject group and a control group.

(2) Antidiabetic action 10111 g of ginsenoside Rb was added to 0.0 g of physiological saline.
The solution was dissolved in 5 ml and intraperitoneally administered to test rats once a day, every day for 1 to 9 days. Breeding conditions and blood sugar levels were measured using the same methods as above. Blood was collected 12 hours after administration.

(3) Results p<o, ol p<o, os p<o, ol Experiment 2 Acute-''Toxicity Experiment Method A group of 10 male DD mice was used, and the sample was dissolved in physiological saline and administered intraperitoneally. LD was calculated from the number of deaths after 1 day.

bJ Ginsenosidol-LD. :305■/kg (effect of the invention) As is clear from the above experiments, ginsenoside-Rb,
Both single administration and continuous administration over several days significantly reduce high serum glucose concentrations, and although the effect becomes even more pronounced with continuous administration, it does not cause hypoglycemic symptoms and Even if the drug is discontinued, the effect is persistent. Therefore, administration according to the basic rules is effective in improving the condition of diabetes.

It is therapeutically useful.

Diabetes is not just an increase in blood sugar levels, but is often accompanied by accompanying symptoms such as an increase in lipids such as triglycerides and an increase in ketone bodies. Ginsinosedo-Rb also exhibits a remarkable improving effect on these.

On the other hand, no abnormalities were observed in the animal's kinetics or physical activity even after long-term continuous administration.

Jinmono used in the present invention. Cyto-Rb can be administered orally or parenterally as it is or mixed with appropriate pharmaceutical carriers, excipients, and diluents in the form of powder, granules, tablets, capsules, injections, and the like. The dosage for adults is, for example, 301 Qg to 1000 N per day, preferably 50 fQg to 3001 Qg, divided into 1 to 3 doses and administered orally or injected for a 9 year old and 9 body weight.

Needless to say, the dose may be increased or decreased depending on the symptoms.

Next, formulation examples of the antidiabetic agent of the present invention will be described.

(1) Granules ginsenoside Rh210011tg, lactose 616U
and Cornstarch 264■ are mixed uniformly, and a 10% aqueous hydroxypropylcellulose (RPC) solution is used as a glue to prepare granules according to the section on granules in 1. General Rules for Preparations in the Japanese Pharmacopoeia.

(2) Injection Ginsenoside Rb250■ is dissolved in 2.5 ml of 20% propylene glycol distilled water solution and sterilized by heat to prepare an injection according to the Japanese Pharmacopoeia General Preparations Section for Injections.

Claims (1)

[Claims] Antidiabetic agent containing ginsinosedo-Rb_2 as an active ingredient