JP2002363092A - Antihyperlipidemic composition and method for producing the same - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a new antihyperlipidemic composition having an excellent cholesterol reducing effect. SOLUTION: The antihyperlipidemic composition contains the root of Panax japonicus as an active ingredient, and a good cholesterol redicing effect is expressed by the composition.

Description

DETAILED DESCRIPTION OF THE INVENTION

3. A method for producing an antihyperlipidemic composition, comprising a step of extracting a root of a plant selected from a ginseng and its closely related species with water and / or alcohol.

[0001]

TECHNICAL FIELD The present invention has an anti-hyperlipidemic activity, and in particular, has a total cholesterol and / or LDL
The present invention relates to a composition having a cholesterol-lowering effect.

[0002]

2. Description of the Related Art Carrots and other roots of plants belonging to the araliaceae family and their extracted components have long been used as crude drugs. However, the cholesterol lowering effect of ginseng, particularly the LDL cholesterol lowering effect, is not yet known.

On the other hand, for hyperlipidemia in which the blood cholesterol level is high, various known therapeutic agents are known. HMG-CoA reductase inhibitor preparations such as pravastatin and simvastatin, clofibrate preparations such as clinofibrate and besafibrate, nicotinic acid preparations such as niceritrol and euperanicotinate, cholestyramine anion exchange resin, and enzyme preparations There are certain elastase, dextran preparations, linoleic acid preparations, EPA preparations and the like.

[0004]

However, these therapeutic agents are excellent in the action of lowering total cholesterol, but all have side effects. Then, an object of the present invention is to provide an anti-hyperlipidemic composition having a good cholesterol lowering action. Another object of the present invention is to provide an anti-hyperlipidemic composition having no or sufficiently reduced side effects.

[0005]

Means for Solving the Problems The present inventor has long studied the pharmacological action of the roots of an araliaceae plant, and among the araliaceae plants, ginseng ginseng is effective in lowering blood cholesterol. This led to the completion of the present invention. That is, the above-mentioned issues
The problem is solved by an anti-hyperlipidemic composition containing, as an active ingredient, a root of a plant selected from a ginseng and its closely related species. In particular, the problem is solved by an anti-hyperlipidemic composition comprising, as an active ingredient, a water and / or alcohol extract component of roots of a plant selected from a ginseng and related species thereof. In addition, the above-mentioned problem is also provided by a method for producing an anti-hyperlipidemic composition, comprising a step of extracting roots of a plant selected from a ginseng and its closely related species with water and / or alcohol.

[0006]

BEST MODE FOR CARRYING OUT THE INVENTION Hereinafter, embodiments of the present invention will be described in detail. Panax ginseng CA Meyer is one of the medicinal carrots of araliaceae plants
In addition to this, there are American ginseng (P. quinquefolium L.), saccharin (Ginseng ginseng, P. notogingseng), bamboo ginseng (Chisseng carrot) (pearl ginseng, P. japonicus CA Meyer), etc. In the present invention, it is preferable to use roots of plants selected from ginseng and its closely related species (hereinafter referred to as roots of ginseng and the like). Most preferably, ginseng. The roots of these carrots, including the roots of the ginseng and related plants, are usually dried.

[0007] The composition of the present invention only needs to contain roots such as ginseng as an active ingredient. Therefore, roots such as carrots may be directly contained as a solid active ingredient such as a powder or a strip. In addition, the composition of the present invention can contain, as an active ingredient, an extracted component obtained by extracting roots such as ginseng with water and / or alcohol.

[0008] In the extraction, it is preferable that the roots of the carrots are pulverized or the like to make them into powdery or strip form. More preferably, it is a crushed piece having a size of about 5 mm square or less, and still more preferably a flake having a size of 0.5 mm to 2 mm square. In the case of extracting with water, the water to be used is not particularly limited, but it is preferable to heat in the extraction. Preferably, 80-100
° C, more preferably 90-95 ° C. The extraction time is not particularly limited, but is preferably within one hour, more preferably 30 minutes or more and 60 minutes or less. Further, the amount of water relative to the extraction raw material (carrot root) is not particularly limited.
It is preferably 00 ml. For the extraction operation, it is preferable to use an open-to-air container, particularly a material made of glass, enamel, ceramics, or a metal part coated or processed with a corrosion-resistant coating. It is preferably carried out using a reflux condenser.

The following operation can be mentioned as a typical example of extracting roots such as carrots with water. 800 ml of hot water is added to 3 g of the dried root of the ginseng, which has been crushed into small pieces, and decocted so that the remaining amount of the extract is 500 ml in the above-mentioned heating range. Preferably,
The heating is adjusted so that the volume becomes 500 ml in about 30 minutes. The extract obtained by such an operation (especially when a reflux condenser is used) becomes a liquid having a concentration suitable for oral administration as it is.

In the case of extracting with alcohol, it is preferable that the alcohol to be used is a drinkable alcohol in consideration of a case where the alcohol may be drunk as it is. That is, it is preferable to use ethanol. When extraction is performed using alcohol, the extraction may be performed using only the alcohol, but it is preferable that the extraction is performed using a mixed liquid after mixing with water. Preferably, the alcohol concentration is 50 v / v%
Lower, more preferably about 35 v / v%. The alcohol-containing extract is not particularly limited, but is preferably heated during extraction. Preferably it is 50-80 degreeC, More preferably, it is 75 degreeC or less, More preferably, it is 70 degreeC or less. The extraction time is not particularly limited, but is preferably 10 hours or more, more preferably 20 hours or more, and most preferably about 30 hours or more. In addition, at the time of final oral administration, it is preferable that the alcohol concentration is about 20 v / v%. For example, when extracting with an alcohol solution having a concentration of more than 20 v / v%, it is preferable to dilute with water after the extraction so that the concentration becomes 20 v / v%. Further, the amount of the extract with respect to the extraction raw material (carrot root) is not particularly limited, but is preferably 1000 ml with 30 g of the raw material. As the container for extraction, it is preferable to use the same container as used for extraction with water only. The extraction operation is preferably performed using a reflux condenser.

The following operation can be mentioned as a typical example of extracting roots of carrots and the like with a water / alcohol mixture. A 35 v / v% ethanol solution was added to 30 g of the dried root of the carrot,
ml and keep the solution at about 70 ° C. for about 30 hours. After 30 hours, add hot water (or water) so that the total volume becomes 1000 ml. It is preferable that the alcohol concentration finally becomes about 20 v / v%. The extract obtained by such an operation becomes a liquid having a concentration suitable for oral administration as it is.

The obtained extract is filtered if necessary. The extract may be used as an active ingredient as it is. Also,
If necessary, it can be concentrated and concentrated, and this can be used as an active ingredient. Further, by evaporating the water, an extractable component as a solid content is also obtained, and by drying it as necessary, a desired dry extractable component is obtained.
Further, in consideration of the administration form and dosage form of the present composition, an additive which stabilizes the extract or a formulation can be added when the extract is concentrated or dried.

The active ingredient contained in the composition of the present invention has a blood cholesterol lowering effect. In particular, relatively large amounts of LDL cholesterol can be reduced. Therefore, the present composition can be used as a therapeutic agent for hyperlipidemia. Further, the composition of the present invention can effectively reduce hypercholesterolemia and / or LDL cholesterol by effectively acting on hyperlipidemia as a complication in patients with diabetes, particularly non-insulin-dependent diabetes. Therefore, the composition of the present invention can be used as a therapeutic agent for hyperlipidemia as a complication in diabetes. The effect of lowering total cholesterol and LDL cholesterol is more remarkable in a composition containing an active ingredient starting from the root of ginseng as compared with other carrots. In addition, the composition of the present invention also has an insulin-like action. That is, when administered to a diabetic patient, a decrease in the blood concentration of C-peptide has been observed.

In the composition of the present invention, no or only minor side effects are observed. In other words, the side effects commonly observed when administering antihyperlipidemic drugs are numbness in the limbs, weakness in the limbs, body weakness, muscle pain, swelling, decreased urine output, fever, cough, and constipation , Abdominal pain, chest pain, tiredness, nosebleed, complexion, poor appetite, headache, etc. are not found.On the contrary, after starting administration, numbness of limbs is eliminated, physical strength is felt, body pain is alleviated, Phenomena such as less fatigue, improved complexion, and increased appetite are observed.

The active ingredient in the present invention is mixed with a pharmaceutically acceptable carrier or additive and used as a composition suitable for administration. The form of the composition is not particularly limited, but may be a liquid, syrup, suspension, powder, granule, tablet, pill, capsule, emulsion, troche, chewable, suppository, eye drop, injection, aerosol. , Elixirs and the like. It is also preferable to add water at the time of use to obtain a solid (powder) agent capable of recovering a liquid material.

The composition of the present invention can be administered orally or parenterally. Preferably, it is administered orally. The general dosage for oral administration is shown below.
The dose is appropriately set according to symptoms, physical strength of the individual, and the like. A general dose (normal dose) is, for example, 2% as a dry root weight of ginseng and the like (preferably ginseng) used as an extraction raw material.
g to 5 g / day / patient (weight: 60 kg; the same applies hereinafter). More preferably, 2.5 g to 3.0 g /
Days / patient. For example, in the case of the above-mentioned typical example of the administration of a ginseng root aqueous solution alone, 400 ml to 500 /
Days / patient, for example, preferably administered twice daily. In addition, in the case of single administration of the ethanol / water mixture extract of the ginseng root of the typical example described above, 80 to 100 m
1 / day / patient, preferably administered twice daily. In addition, in the combined administration of the water extract and the ethanol / water mixture extract of the typical example, the water extract is 180 to 220 m
l (preferably 200 ml) / day / 45-55 ml (preferably 50 m
l) / day / patient, preferably administered twice daily.

Since the composition of the present invention has extremely low toxicity and does not cause any serious side effects, it can be safely administered at a high dose depending on the symptoms.

[0018]

According to the present invention, there is provided an anti-hyperlipidemic composition having a good cholesterol lowering effect and having no or sufficiently reduced side effects.

[0019]

EXAMPLES (Example 1) Hereinafter, the present invention will be described with reference to specific examples, but the present invention is not construed as being limited to these examples. (Preparation of composition) Water extraction composition To 3 g of dry root of ginseng, which was crushed into pieces of about 0.5 to 2 mm square, 800 ml of hot water was added,
It was decocted so that the remaining amount of the extract became 500 ml in about 30 minutes. This extract was directly used as a composition for oral administration. 2. Alcohol / water mixture extraction composition A 0.5 v to 2 mm square strip of crushed ginseng, 30 g of dry root, is added with 35% v / v% ethanol solution to make 1000 ml, and the solution is brought to about 70 ° C. About 3
Decooked for 0 hours. After 30 hours, hot water was added so that the total amount was 1000 ml. Note that the final alcohol concentration was about 20 v / v%. This extract was directly used as a composition for oral administration.

(Example 2) (Clinical administration example) The two compositions obtained in Example 1 were orally administered to 5 patients with non-insulin-dependent diabetes mellitus in combination. For administration, these compositions were drunk as they were. The dose was 200 ml / day of the aqueous extract composition (one each in the morning and evening).
00 ml) and 50 ml of an alcohol / water mixture composition
/ Day (25 ml each in the morning and evening). Dosing was performed for 28 consecutive days. In addition, these patients were on a diet therapy, and during the administration period, no other drugs including the therapeutic agent for diabetes were administered at all other than the present composition.
Nor were there plant allergies, neuropathy, gastroenteritis, liver dysfunction, or kidney dysfunction.

For these patients, blood was collected before the start of administration and after the end of the administration period, and the results of measurement of the concentrations of total cholesterol, LDL cholesterol, and C-peptide in the blood are shown in Table 1.

[Table 1]

As shown in Table 1, the blood levels of total cholesterol, LDL cholesterol, and C-peptide decreased in all patients. Total cholesterol is on average 75.85% before administration, LDL cholesterol is also 78.78% and c-peptide is
It was also 84.5%. In addition, it is considered that the blood concentration of the C-peptide decreases because the present composition exhibits an insulin-like action. Moreover, in these five patients, symptoms considered as side effects were not observed during the administration period. Conversely, during the administration period, relief of body pain, less fatigue, feel power, improve complexion,
Conditions such as appetite enhancement were observed.

(Comparative Example) (Clinical Administration Example) The blood concentration of red ginseng (a kind of ginseng) powder before and after administration of total cholesterol and LDL cholesterol in an example of administration to a diabetic patient was measured.
A total of 67 patients were administered. All patients had non-insulin-dependent diabetes mellitus and were being treated on diet alone with no concomitant medications. The dose is 2.7 g /
It was administered orally on a day (administered 3 times a day before 3 meals) for 30 consecutive days. Table 2 shows the results.

[Table 2] As shown in Table 2, red ginseng contains total cholesterol and L
It had a DL cholesterol lowering effect, but all were lower than 10%.

For reference, Table 3 shows an outline of the cholesterol lowering effect of a commercially available antihyperlipidemic agent.

[Table 3]

Claims (2)

[Claims] 1. An anti-hyperlipidemic composition comprising, as an active ingredient, a plant root selected from ginseng and related species thereof. 2. An anti-hyperlipidemic composition comprising, as an active ingredient, a root and water and / or alcohol extract component of a plant selected from Panax ginseng and closely related species thereof.