JP2002212085A - Uric acid value-reducing agent - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a new uric acid value-reducing agent which does not cause a side effect, and to provide a drink or food which does not cause a side effect, has excellent safety, and is effective for correcting hyperuricemia and for treating and preventing complications such as hypertension. SOLUTION: This uric acid value-reducing agent contains a ginkgo leaf extract as an active ingredient, and the drink or food contains the same.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

[0001] The present invention relates to a uric acid level-decreasing agent containing a ginkgo biloba leaf extract as an active ingredient, and a food or drink characterized by containing the agent.

[0002]

BACKGROUND OF THE INVENTION Gout, the most typical disease of uric acid metabolism disorders, is a very old disease that has been known since the time of Hippocrates in ancient Greece. However, the relationship between gout pathology and abnormal uric acid metabolism was clarified in 18
At the end of the century, until now gout was identified with joint pain attacks and colchicine was used to treat pain attacks.

[0003] At present, it has been revealed that uric acid is present in high concentrations in the blood of gout patients, and it is most important in the treatment of gout patients to reduce not only pain attacks but also blood uric acid levels. It is believed that. For this purpose, uric acid excretion promoters and synthetic inhibitors are used as uric acid level lowering agents. Among them, allopurinol, which inhibits the action of xanthine oxidase that acts on the process from hypoxanthine to uric acid via xanthine, is widely used in gout treatment as the only known uric acid synthesis inhibitor (Japanese clinical, Nippon clinical company, 1081-1085
1991).

[0004] Furthermore, correction of hyperuricemia is necessary for prevention of arteriosclerosis and myocardial infarction, and is also considered to be significant for prevention of hypertension through exacerbation of renal failure (Nihon clinical, Nihon clinical, 988-993, 1991).

[0005] However, administration of allopurinol caused fever, rash, liver damage, renal dysfunction, etc. (Medical Drugs, Japan Pharmaceutical Collection, Pharmaceutical Times, 157
Oxypurinol, a metabolite of allopurinol, has been reported to accumulate in the body at high concentrations in dialysis patients, causing blood damage and liver damage (Disease and Therapeutic Drugs, Nankodo). , P. 212, 19
96).

[0006] Under such circumstances, uric acid level lowering agents having no side effects are demanded. In addition, there is a need for foods and drinks which contain the above-mentioned uric acid level lowering agent, are effective in correcting hyperuricemia, and treating or preventing complications such as hypertension, and have excellent safety.

[0007]

SUMMARY OF THE INVENTION Accordingly, an object of the present invention is to find a novel uric acid-lowering agent having no side effects and containing the same, having no side effects, correcting hyperuricemia and complicating hypertension and the like. It is an object of the present invention to provide foods and drinks that are effective for treating and preventing diseases and that are excellent in safety.

[0008]

Means for Solving the Problems The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, have found that ginkgo biloba leaf extract has an excellent uric acid level-lowering effect. It was found to be useful as a hypotensive agent and the like. In addition, they have found that ingestion of a food containing a ginkgo biloba leaf extract can also correct hyperuricemia and alleviate hypertension and the like, and have completed the present invention.

[0009] That is, the present invention provides a uric acid level lowering agent containing a ginkgo biloba leaf extract as an active ingredient.

[0010] The present invention also provides a food or drink characterized by containing the above-mentioned uric acid level lowering agent.

[0011]

BEST MODE FOR CARRYING OUT THE INVENTION Ginkgo biloba leaf extract used as a uric acid level lowering agent in the present invention is, for example, ginkgo biloba leaves as they are or by chopping them, using water or an organic solvent (alcohol, alcohol, etc.).
Ether, acetone, etc.), etc., and purification by a known method used for the separation and extraction of plant components, such as partitioning between ethyl acetate and other organic solvents and water, column chromatography, etc., alone or in an appropriate combination. Thus, it can be easily obtained. In addition, the obtained extract,
Further, after removing impurities by means of filtration or the like, a substance concentrated under reduced pressure or a substance dried by means of spray drying or natural drying may be used.

A particularly preferred method for producing a ginkgo leaf extract is a method in which dried ginkgo leaves are shredded, extracted with 3 to 10 times the amount of aqueous alcohol, and the resulting extract is dried. . As the aqueous alcohol used for the extraction, aqueous ethanol is preferably used from the viewpoint of the uric acid level lowering effect, and 70 to 90% by mass of aqueous ethanol is particularly preferable.

When a ginkgo biloba leaf extract is used as the uric acid level-lowering agent of the present invention and a food containing the same, the amount of ginkgo biloba extract to be taken is from 20 mg to 360 in terms of the solid content of the extract.
mg / day, particularly preferably from 40 mg to 120 mg / day.

The ginkgo biloba leaf extract used in the present invention has low toxicity. For example, even when a large amount of this is administered to mice,
No fatal cases were observed until around the g administration, and the LD ₅₀ value was 15.3 g per kg of body weight in mice. By the way, LD ₅₀
However, the level of 15.3 g / kg can be said to be extremely low in acute toxicity as compared with various additives used in foods. In addition, fatal cases due to large doses show a more acute osmotic shock rather than digestion / absorption results. Was. From the above results, it is judged that the possibility of adverse effects when a large amount is taken at once is small.

The ginkgo biloba extract used in the uric acid level lowering agent of the present invention has an excellent uric acid level lowering action and is extremely safe, as will be apparent from the examples described later. In addition to being used in foods and drinks, it can also be used as various pharmaceuticals by utilizing this effect.

When used in foods and drinks, various foods and drinks may contain ginkgo biloba extract. Specific foods and drinks include soft drinks, fermented milk, kefir, fruit juice drinks,
Examples include soups, rice crackers, cookies, tablet confections and the like. Among them, beverages containing various crude drugs are preferable from the viewpoint of flavor.

The production of foods and drinks may be carried out according to a conventional method.
For example, a beverage can be manufactured as follows. First, after mixing and dissolving the ginkgo biloba extract and other auxiliary ingredients,
It is homogenized, heat-sterilized using an HTST sterilizer or the like, filled in a container, and sealed. The container may be any container such as a can, a PET container, a bottle, and paper.

[0018] As auxiliary ingredients for foods and drinks, for example, kokushi, licorice, litchi, agaricus, enokitake, panax ginseng, panax ginseng, chlorella, shiitake mushroom,
Shiromaitake, Hampi, Propolis, Maitake, Yamabushidake, Royal Jelly, American Carrot, Echinacea, Oyster Meat, Kumazasa, Gentiana, St. John's wort, Chixetus carrot, Eucommia persica, Dokudami, Tochibanjin, Nameko-mushroom, Scallop Crude drugs, sucrose, isomerization, etc., sugars such as glucose, fructose, palatinose, trehalose, lactose, xylose, sorbitol, xylitol, erythritol,
Sugar alcohols such as lactitol, palatinit, reduced starch syrup, reduced maltose syrup, high-potency sweeteners such as aspartame, sucralose, acesulfame potassium, stevia, emulsifiers such as sucrose fatty acid ester, glycerin fatty acid ester, lecithin, carrageenan, xanthan gum, guar gum Thickening (stabilizing) agents such as corn, pectin, locust bean gum, acidulants such as citric acid, lactic acid and malic acid, juices such as lemon juice, orange juice and berry juice, vitamins A, vitamins B and vitamin C , Vitamins such as vitamin E, minerals such as calcium, iron, manganese, and zinc; and ume extract. In particular, when a sweetener and a crude drug such as kokushi, liquorice and litchi are combined, the flavor of the final product is favorable because the flavor is good.On the other hand, when the sugar alcohols are used in combination, the stability when a beverage is produced is preferable. It is preferable because the property is improved.

When used as a medicament, ginkgo biloba extract is used as an active ingredient, and a commonly used inorganic or organic carrier is added thereto. It can be formulated into a parenteral preparation such as an external preparation.

Formulations for oral administration include tablets, pills, granules, soft and hard capsules, powders, fine granules, powders,
Emulsions, suspensions, syrups, pellets, elixirs and the like can be mentioned. As a preparation for parenteral administration,
Injections, drops, infusions, ointments, lotions, tonics,
Sprays, suspensions, oils, emulsions, suppositories and the like can be mentioned.
Formulation of the active ingredient of the product of the present invention may be carried out according to a conventional method, including a surfactant, an excipient, a coloring agent, a flavor, a preservative, a stabilizer, a buffer, a suspending agent, and isotonic. Agents and other commonly used auxiliaries are used as appropriate.

[0021]

EXAMPLES The present invention will now be described specifically with reference to examples, but these examples do not limit the present invention in any way.

REFERENCE EXAMPLE 1 <Production of Ginkgo biloba leaf extract> Five times the amount of 80% by mass aqueous ethanol was added to shredded ginkgo biloba leaves, and the mixture was added at 60 ° C.
Time extracted. The obtained extract was concentrated under reduced pressure to a volume of 1/5, and then filtered to remove impurities. This concentrate was sterilized at 80 ° C. for 30 minutes, and then spray-dried with a spray dryer to extract ginkgo biloba leaf dry powder 2.5 k
g was obtained.

Example 1 Measurement of blood uric acid level lowering and blood pressure lowering effects in humans: Ginkgo biloba leaf extract was tested for its human blood uric acid level lowering and blood pressure lowering effects as follows.

<Test Method> The test subjects were divided into two groups of eight adults, each of which was 16 adults living a clinically healthy daily life with a systolic blood pressure of 140 mmHg or a diastolic blood pressure of 85 mmHg or more. The test subjects were divided into two groups,
Ginkgo biloba extract drink having the following composition, or a control drink in which only the ginkgo biloba extract was removed from this ginkgo biloba extract drink, was ingested once a day for 12 weeks. Before ingestion, and at the end of ingestion, after a hunger of 12 hours or more, blood was collected and uric acid levels were measured. In addition, a skilled public health nurse measured blood pressure using a mercury sphygmomanometer and measured heart rate. The blood pressure was measured three times in a sitting position after at least 5 minutes of rest. The average value of three individual blood pressures was adopted.

(Prescription) (g) Ginkgo biloba leaf extract ^* 0.04 Carbohydrate 16.6 Sodium 0.011 Kukoshi extract Appropriate quantity Licorice extract Appropriate quantity Reishi extract Appropriate quantity Plum extract Appropriate quantity *: Prepared in Reference Example 1.

<Evaluation method> Regarding the antihypertensive effect, the difference between the systolic blood pressure, the diastolic blood pressure and the average blood pressure before and after 12 weeks of ingestion was compared. (Clinical Evaluation Guidelines for New Drugs, Yakuji Nippo-sha, 308-3
32, 1994). The degree of blood pressure reduction was determined by classifying the degree of blood pressure into four stages, and when the classification by systole and the classification by diastole did not match, the classification by mean blood pressure was used.

All the results showed the mean ± standard error.
The t-test was used to test the difference between the mean values of both groups. Further, the change with time was compared with that before ingestion using a paired t-test. In each statistical processing, the significance level was set to 5% or less, and two-sided test was performed.

<Test Results> No change was observed in the uric acid value of the control beverage group, but the uric acid value of the ginkgo leaf extract beverage group after 12 weeks of ingestion was significantly lower than that before ingestion. Was. Furthermore, comparing the uric acid value of the control beverage group and the uric acid value of the ginkgo leaf extract beverage group 12 weeks after ingestion, the uric acid value of the ginkgo leaf extract beverage group was significantly lower.

[0029]

[Table 1]

The differences in systolic blood pressure, diastolic blood pressure and mean blood pressure before and after 12 weeks of ingestion were compared, and the effectiveness of the ginkgo biloba leaf extract beverage was evaluated based on the criteria for the evaluation of blood pressure reduction. Those who showed a downward or downward tendency were considered effective, and the values were determined. The value was as high as 75% in the ginkgo leaf extract beverage group compared to 25% in the control beverage group.

[0031]

[Table 2]

Example 2 Production of a soft drink: Each component was blended according to a conventional method according to the following formulation, and homogenized to obtain a soft drink. The obtained soft drink was filled in a brown bottle, sealed with an aluminum cap, and subjected to a heat treatment. These were good in both appearance and flavor.

(Prescription) (g) Ginkgo biloba leaf extract ^* 0.8 Fragrance 0.8 Water 55.32 Reduced starch saccharified product 24 Fructose 18 Kukoshi extract 0.1 Licorice extract 0.1 Ganoderma extract 0.1 Plum extract 0.1 1 Citric acid 0.3 *: produced in Reference Example 1.

Example 3 Production of Tablets: Various components were mixed according to the following formulation, granulated, dried and sized, followed by tableting to produce tablets.

(Formulation) (mg) Ginkgo biloba leaf extract ^* 40 Microcrystalline cellulose 100 Lactose 80 Magnesium stearate 0.5 Methylcellulose 12 Talcum powder 5 *: Produced in Reference Example 1.

[0036]

The uric acid level-lowering agent comprising the ginkgo biloba leaf extract of the present invention as an active ingredient and a food or drink containing the same reduce hyperuricemia, and thus gout and artery associated with hyperuricemia. It can be effectively used for prevention or treatment of sclerosis, myocardial infarction, renal failure, hypertension and the like. that's all

 ──────────────────────────────────────────────────続 き Continued on the front page (72) Inventor Satoshi Matsubara 1-1-19 Higashi-Shimbashi, Minato-ku, Tokyo Yakult Honsha Co., Ltd. (72) Inventor Harue Sone 1-1-19, Higashi-Shimbashi, Minato-ku, Tokyo No. Yakult Honsha Co., Ltd. (72) Inventor Masaaki Watanuki 1-1-19 Higashi-Shimbashi, Minato-ku, Tokyo Incorporation Yakult Honsha Co., Ltd. (72) Inventor Takashi Furue 3-8- Mizoguchi, Takatsu-ku, Kawasaki City, Kanagawa Prefecture 3 F-term in Teikyo University Mizoguchi Hospital (reference) 4B017 LC03 LG15 LL09 4B018 MD61 ME14 MF01 4C088 AB02 AC05 BA08 MA52 NA06 NA14 ZC31

Claims (2)

[Claims] 1. A uric acid level lowering agent comprising a ginkgo biloba leaf extract as an active ingredient. 2. A food or drink comprising the uric acid level-lowering agent according to claim 1.