JP2006290782A - Antiedemic composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide an oral agent having high effect on prophylaxis and improvement of edema, namely an antiedemic composition. <P>SOLUTION: The antiedemic composition is prepared by formulating, in good balance, at least an extract of Melilotus officinalis containing a coumarin or its derivatives as a first component with an extract derived from natural products, selected from a group consisting of Fucus vesiculosus, Piper retrofractum, Coix lachryma-jobi L., Humulus lupulus and Aloe vera and promoting metabolism as a second component and a vitamin B group as a third component. <P>COPYRIGHT: (C)2007,JPO&INPIT

Description

  The present invention relates to an anti-edema composition useful for preventing or ameliorating edema.

  Due to long standing, sitting, etc., edema occurs spontaneously in the body, especially in the lower limbs. Edema refers to a state where extra-cellular extracellular fluid (tissue interstitial fluid) is excessively stored in the tissue gap, and is generally referred to as swelling. This swelling causes a feeling of fatigue and physical obstacles such as the inability to wear shoes, and many people suffer from such a situation. Swelling is also associated with lower limb varices.

In order to improve these swellings, diuretics and herbal medicines containing extracts of Merilotus officinalis and Butchers bloom (Ruscus aculeatus L.) are widely used.
Merirot is a leguminous plant also called shrimp, and includes coumarin, rutin, and flavones. In particular, since coumarin and rutin are useful for improving edema, the extract of Merrilot has long been used in Europe as an ameliorating agent for varicose veins.
Butcher's bloom is a lily family plant that grows in the Mediterranean Sea, also known as Nagikada, and is known to be useful for promoting blood circulation and improving edema.

Japanese Patent No. 3310649 (Patent Document 1) discloses a food composition for the prevention or improvement of foot swelling comprising a plant containing coumarins such as shrimp or a derivative thereof and a branched chain amino acid. .
In addition, a diuretic containing a butcher's bloom extract and γ-tocopherol as active ingredients is disclosed in JP-A-2002-226388 (Patent Document 2).
Furthermore, an oral preparation having an action of improving body fluid circulation, ie, eliminating swelling, is disclosed in Japanese Patent Application Laid-Open No. 2004-359694 (Patent Document 3), and this oral preparation is a plant containing coumarins or derivatives thereof. Contains shrimp hagi and butchers bloom.

Japanese Patent No. 3310649 JP 2002-226388 A JP 2004-359664 A

  The inventors of the present invention have conducted intensive research on the development of an oral preparation having a higher effect on the prevention and improvement of swelling, that is, an anti-edema composition. As a result, surprisingly, the vitamin B group is added as a third component to a mixture of an extract of Merrilot as the first component and an extract derived from natural products such as fucus and hibatsu as the second component Has found that the effect of improving the fatigue and swelling of the lower limbs is promoted, and the present invention has been completed.

  The present invention includes, as a first component, a merryrot extract, a second component, a natural product-derived extract selected from the group consisting of fucus extract, hinoki extract, pearl barley extract, hop extract and aloe vera extract, or a combination thereof, and An anti-edema composition containing vitamin B group as three components is provided.

Fucus (vesuculosus) is a seaweed (brown algae) that adheres to the rocks of the northern seas and the Atlantic coast of the North Sea, also known as Hibamata, and is known to be effective in promoting fat burning and blood circulation, and to activate metabolism. ing.
Hiperu (Piper retrofractum) is a creeping woody plant native to the pepper family South Asia, and is known to dilate blood vessels to increase blood flow and promote metabolism.
Barley (Coix lachryma-jobi L.) is a grass family plant, has a diuretic action, and has an action of promoting metabolism.
Hop (Humulus lupulus) is a plant of the mulberry family and has a healthy stomach, sedation, and diuretic action.
Aloe vera is a succulent plant of the lily family and has an action of expanding peripheral blood vessels, an action of softening blood vessels, and a laxative diuretic action, and is known to increase metabolism.

The vitamin B group is a group of water-soluble vitamins present in cereal germs, livers, and the like, and is involved in the metabolism of substances as a component of coenzymes in enzyme reactions in vivo.
The vitamin B group that can be used in the present invention includes thiamines such as thiamine hydrochloride and thiamine nitrate; riboflavins such as riboflavin and sodium riboflavin phosphate; pyridoxines such as pyridoxine hydrochloride; nicotinic acids such as nicotinic acid and nicotinamide. Pantothenic acids such as sodium pantothenate and calcium pantothenate; or a combination thereof.

The anti-edema composition of the present invention can be processed into various forms such as liquid forms such as drinks and solid preparations such as granules and tablets.
When the anti-edema composition of the present invention is processed into a drink, in addition to the first, second and third components described above, ingredients commonly used for producing a drink, such as fructose glucose liquid sugar, Honey, granulated sugar, citric acid, sodium benzoate, fragrance, purified water and the like can be added.
In addition, when the anti-edema composition of the present invention is processed into a solid preparation such as a granule or a tablet, in addition to the above first to third components, ingredients commonly used for producing a solid preparation, for example, Lactose, reduced maltose starch syrup, starch such as corn starch, hydroxypropyl cellulose, glycerin fatty acid ester, fragrance and the like can be added.

  According to the anti-edema composition of the present invention, it was possible to obtain a higher effect on the swelling of the lower limbs including feet and legs and the improvement of fatigue feeling as compared with the conventional anti-edema composition.

  The anti-tumor composition of the present invention comprises at least a natural product-derived extract selected from the group consisting of a merirot extract as a first component, a fucus extract, a chickweed extract, a pearl extract, a hop extract and an aloe vera extract as a second component, or those And, as a third component, a vitamin B group selected from the group consisting of thiamine hydrochloride, thiamine nitrate, riboflavin, sodium riboflavin phosphate, pyridoxine hydrochloride, nicotinic acid, nicotinamide, sodium pantothenate and calcium pantothenate Including combinations thereof.

  In the present invention, “extract” means a product obtained by concentrating a juice or a leachate obtained by a method such as pressing or solvent immersion of a natural product, and depending on the degree of concentration, a liquid, semi-solid, or powdered solid However, when the extract is in a liquid form, it can also be used as an extract powder by adding excipients such as dextrin.

When preparing extracts derived from natural products such as merirot, fucus, chickweed, pearl barley, hops and aloe vera used in the present invention, the use site of these natural products is not particularly limited, and the whole or flowers, leaves, stems, roots are used. Specific parts such as seeds, fruits and buds can be used raw or dried.
In the present invention, the natural products described above may be directly used after being dried and ground without using the natural products as extracts.
In the present invention, particularly preferably used parts are the above-ground part of Merirot, the stem part of Fucus, the ears of cypress, the seeds of pearl barley, the seeds of hops and the mesophyll of aloe vera.

  The natural product-derived extract in the present invention can be extracted from a raw use site or a product obtained by crushing or grinding a dried product thereof. Extraction can be performed by a commonly used method such as compression or immersion in various solvents. Solvents that can be used for extraction include water, organic solvents such as lower alcohols such as ethanol, ethers, acetone, or mixtures thereof.

Example 1
A. Extract Preparation (1) Preparation of Merirot Extract The ground part of Merirot was dried and pulverized, and extracted by adding 35% ethanol consisting of 35% by volume of ethanol and 65% by volume of water. The extract was filtered, then the filtrate was concentrated under reduced pressure and the concentrate was purified. The purified product was spray-dried to obtain a merirot extract.

(2) Preparation of Fucus Extract Fucus stems were dried and pulverized and extracted with water-containing ethanol. The extract was filtered and then the filtrate was concentrated under reduced pressure. The concentrate was purified. The purified product was spray-dried to obtain a fucus extract.

(3) Preparation of Hihatsu Extract The ears of Hihatsu were dried and extracted by adding hot water to the pulverized one. The extract was filtered and then the filtrate was concentrated under reduced pressure. The concentrate was purified. The purified product was spray-dried to obtain a hihatsu extract.

(4) Preparation of pearl barley extract 30% ethanol consisting of 30 volume% ethanol and 70 volume% water was added to the pearl seed and extracted. This extraction was repeated twice, and the obtained extracts were combined and filtered, and then the filtrate was sterilized to obtain a barley extract.

(5) Preparation of hop extract 30% ethanol consisting of 30% by volume ethanol and 70% by volume water was added to the crushed fruit of mature hops for extraction. The obtained extract was filtered, and then the filtrate was sterilized to obtain a hop extract.

(6) Preparation of aloe vera extract The juice obtained by squeezing aloe vera mesophyll was concentrated under reduced pressure. The concentrate was dried with hot air or freeze-dried to obtain an aloe vera extract.

B. Preparation of a drink preparation An extract preparation solution was prepared by dissolving 50 mg of Merrilot extract, 50 mg of Fucus extract, 30 mg of citric acid and 1.2 mg of sodium benzoate in purified water to a total amount of 2 g.
The resulting extract preparation solution, nicotinamide 5 mg, fructose glucose solution 1500 mg, honey 2000 mg, granulated sugar 1000 mg, citric acid and sodium benzoate are dissolved in purified water, and after adding the fragrance, the total volume is 50 mL. Further, purified water was added to obtain a drink. The final formulation of this drink is shown in Table 1.
Moreover, pH of the drink obtained at this time was 3.1, and precipitation and turbidity were not confirmed by visual observation.

Examples 2-6
In the same manner as in Example 1, drinks having the formulations shown in Table 1 were obtained. The pH of these drinks was also 3.1, and no precipitation or turbidity was confirmed by visual observation.

Comparative Examples 1-6
In the same manner as in Example 1, drinks having the formulations shown in Table 2 were obtained. The pH of these drinks was also 3.1, and no precipitation or turbidity was confirmed by visual observation.

Example 7
Mellilot extract 100 mg, Fucus extract 100 mg, citric acid 30 mg and sodium benzoate 1.2 mg were dissolved in purified water to prepare an extract preparation solution with a total amount of 2 g.
The resulting extract preparation solution, nicotinamide 15 mg, calcium pantothenate 30 mg, fructose glucose solution 2000 mg, honey 2000 mg, granulated sugar 1000 mg, citric acid, sodium benzoate are dissolved in purified water, and the total amount is added Purified water was further added so as to be 50 mL to obtain a drink. The final formulation of this drink is shown in Table 3.
Moreover, pH of the drink obtained at this time was 3.1, and precipitation and turbidity were not confirmed by visual observation.

Examples 8-11
In the same manner as in Example 7, drinks having the formulations shown in Table 3 were obtained. The pH of these drinks was also 3.1, and no precipitation or turbidity was confirmed by visual observation.

Example 12
Melilot extract 50 mg, Fucus extract 50 mg, pearl extract 50 mg, pearl extract 5 mg, hop extract 5 mg, aloe vera extract 3 mg, citric acid 5 mg and sodium benzoate 1.2 mg were dissolved in purified water to prepare an extract preparation solution with a total amount of 2 g. .
The resulting extract preparation solution, 2 mg thiamine nitrate, 2 mg sodium riboflavin phosphate, 2 mg pyridoxine hydrochloride, 5 mg nicotinic acid amide, 5 mg calcium pantothenate, 1500 mg fructose glucose solution, 2000 mg honey, 1000 mg granulated sugar, sodium benzoate in purified water After dissolving and adding a fragrance, purified water was further added so that the total amount became 50 mL to obtain a drink. The final formulation of this drink is shown in Table 4.
Moreover, pH of this drink was 4.0, and precipitation and turbidity were not confirmed by visual observation.

Examples 13-15
A drink with the formulation shown in Table 4 was obtained in the same manner as in Example 12 except that citric acid was added to the resulting extract preparation to make the final amount of citric acid 90 mg, 150 mg or 200 mg. It was.
The pH values of the drinks of Examples 13 to 15 were 2.9, 2.65, and 2.2, respectively. In any of the drinks, no precipitation or turbidity was confirmed by visual observation.

Example 16
Preparation of granules Merilot extract, fucus extract, thiamine nitrate, riboflavin sodium phosphate, pyridoxine hydrochloride, lactose and corn starch are each sieved and mixed in a mixer. To the obtained mixture, a binding solution prepared by dissolving hydroxycellulose in purified water is added, kneaded with a kneader, granulated with an extrusion granulator, dried and sized. As a result, granules having a total amount of 1500 mg were obtained. The final formulation of this granule is shown in Table 5.

Examples 17-20
In the same manner as in Example 16, granules having the composition shown in Table 5 were obtained.

Example 21
Preparation of tablets Merilot extract, fucus extract, nicotinic acid amide, calcium pantothenate, pyridoxine hydrochloride, sodium riboflavin phosphate, thiamine nitrate, reduced maltose starch syrup and corn starch were mixed and then mixed with glycerin fatty acid ester. Added and mixed. Thereafter, tableting was performed to obtain a tablet having a total amount of 650 mg. The final formulation of this tablet is shown in Table 6.

Examples 22-25
In the same manner as in Example 21, tablets having the formulations shown in Table 6 were obtained.

Example 26
Improvement effect on swelling and fatigue of lower limbs Drinks prepared in Examples 1-6 and Comparative Examples 1-6 for women who have a lot of standing work and suffer from swelling and fatigue of legs and legs. The effect of the agent on the swelling and fatigue of the lower limbs was monitored.
Specifically, 5 women (n = 5) arbitrarily selected for each drink were ingested 50 mL of drink between work, and after the work was completed, swelling of the lower limbs and improvement of fatigue A questionnaire survey was conducted on the degree. The degree of improvement was evaluated in four stages: “very effective”, “effective”, “somewhat effective”, and “no effect”, and the score was 3, 2, 1, and 0, respectively. The number of people who performed each evaluation is shown in Tables 7 to 10, and the total number of values obtained by multiplying the number of points by the number of points is also shown.

In the drinks of Examples 1 to 6 in which three components of the first component, which is a merirot extract, the second component such as a fucus extract, and the third component of the vitamin B group were blended, a high evaluation exceeding 10 points was obtained. However, the drinks obtained in Comparative Examples 1 to 6 lacking any of the above three components were only able to obtain a low evaluation of 5 points or less. For example, since the drink of Comparative Example 2 contains the first component and the second component but does not contain the vitamin B group that is the third component, the evaluation was four points. Moreover, since the drink of Comparative Examples 3-6 contains a 1st component and a 3rd component, but does not contain a 2nd component, it was evaluation of 0-2 points.
From this result, it was found that the anti-edema composition of the present invention containing the first component, the second component, and the third component in a well-balanced manner has a very high effect of improving swelling and fatigue of the lower limbs. .

Example 27
Beautiful skin effect The drinks of Examples 7-11 contain more 1st components and 2nd components compared with the drinks of Examples 1-6. When the drinks of Examples 7 to 11 were continuously taken for 50 weeks a day for 1 week, an answer that a skin-beautifying effect such as an improvement in skin condition was felt was obtained.
That is, it was confirmed that the anti-edema composition of the present invention has not only an improvement effect on swelling and fatigue of the lower limbs but also a skin beautifying effect by adjusting the blending amounts of the first component and the second component.

Example 28
Storage stability evaluation Drinks may become turbid or precipitate after long-term storage. It is known that the occurrence of turbidity and precipitation in the drink is mainly caused by the aggregation of the drink component, and the occurrence of this aggregation depends on the pH.
Therefore, in order to confirm the temporal stability of the drink of the present invention, an acceleration test was performed using four kinds of drinks having different pHs.
First, in Examples 12-15, the drink which reduced pH stepwise by increasing the compounding quantity of the citric acid contained in 50 mL of drink from 5 mg to 200 mg was prepared. In these drinks, the amount of ingredients other than citric acid is the same.
Immediately after the preparation of each drink, and after 1 month, 2 months, and 3 months of storage in a thermostat at 50 ° C., the turbidity of the drink and the occurrence of precipitation were visually observed.
Table 11 shows the pH of each drink and the results of visual observation at each period.

  According to Table 11, long-term storage stability is good if the pH of the drink is 2.9 or higher, but if the pH is below 2.65, turbidity occurs after one month of storage, and storage February It was confirmed that precipitation occurred later.

  The pH of the drinks obtained in Examples 1 to 11 is 3.1 and is in the storage stable region. Thus, by using the anti-edema composition of the present invention, it is possible to obtain a drink having a high anti-edema effect and a skin beautifying effect and good storage stability.

When the anti-edema composition of the present invention is used, a preparation having an anti-edema effect higher than that of the conventional anti-edema composition can be obtained, and the anti-edema composition of the present invention is in a liquid form such as a drink. And can be processed into various forms such as solid preparations such as granules and tablets.

Claims (2)

  As a first component, at least as a merorot extract, as a second component, a natural product-derived extract selected from the group consisting of fucus extract, hinoki extract, pearl barley extract, hop extract and aloe vera extract, or a combination thereof, and as a third component, An anti-edema composition comprising vitamin B group. The anti-edema composition according to claim 1, wherein the vitamin B group is thiamine hydrochloride, thiamine nitrate, riboflavin, riboflavin sodium phosphate, pyridoxine hydrochloride, nicotinic acid, nicotinic acid amide, sodium pantothenate, calcium pantothenate or a combination thereof. .