KR20030023172A - fruit bioactive component and extrating process thereof - Google Patents

Abstract

PURPOSE: A method of extracting a fruit like apple, pear, grape, mandarin or the like in the form of an easy-to-take preparation is provided. Whereby, the fruit extract can be used as a pharmaceutically stable antioxidant and free radical scavenger. CONSTITUTION: An apple, pear, grape and mandarin are ground, added 1 to 15 times with ethanol and extracted at room temperature for 1 to 15 days. Thereafter, the extract is concentrated under reduced pressure. For an example, a pharmaceutical tablet contains 60mg fruit extract, 81mg lactose, 50mg microcrystalline cellulose, 1mg silicic acid anhydride, 6mg a crospovidone and 2mg magnesium stearate.

Description

Fruit active ingredient extract and its manufacturing method {fruit bioactive component and extrating process

The present invention relates to a method for extracting active ingredients from fruits and to antioxidant and free radical scavenging agents thereof. In particular, four kinds of fruits such as apples, pears, grapes, and citrus fruits are mixed at a predetermined ratio and solvent-treated. Extraction method of the obtained fruit active ingredient (Fruit Bioactive Component) relates to the antioxidant and free radical scavenging agent.

Aging of the living body is caused by highly reactive free radicals such as hydrogen peroxide, hydroxyl radicals, and superoxide radicals. Aging is caused by cell damage (Ames BN: Endogeneous DNA damage as related to cancer and aging, Mutation Res. , 214 , 41-46 (1989).

When oxygen free radicals attack DNA, the DNA breaks, causing single strand breaks, causing DNA damage, and attacking guanine bases to 8-hydroxy-2'-deoxyguanosine (8-OH2 '). dG) (Park J. W., Cundy KC and Ames BN: Detection of DNA adducts high-performance liquid chromatography with electrochemical detection, Carcinogenesis , 10 , 827-832, 1989). In addition, when oxygen free radicals attack DNA, the DNA is broken (single strand break) and genotoxic on the chromosome.

Therefore, the antioxidant and free radical scavenger which can inhibit lipid peroxidation and DNA oxidative damage suggested in the above example prevents the oxidation of living cells and DNA, and various cancers such as lung cancer, liver cancer, liver hardening, arteriosclerosis, etc. It can prevent cardiovascular disease, delay aging, and various epidemiological studies have shown that high intake of fruits can prevent various cancers and reduce cardiovascular diseases.

Many physiologically active substances are known among the constituents of fruit, and among them, polyphenol compounds including flavonoids have various structures and show various biological activities according to their respective structures (Chi-Tang-Ho: Phenolic compounds). in foods: An overview, Phenolic compounds in food and their effects on health I, ACS symposium series 506, American Chemical Society, Washington DC, pp 2-7, 1992). The activities reported so far are anti-cancer, anti-mutation, hepatoprotective, immune-enhancing, blood circulation improvement, analgesic and other activities have been reported, and their action is not so strong side effects are almost (Mou-Tuan Huang et al., Food phytochemicals for cancer prevention I: An overview, ACS symposium series 546, American Chemical Society, Washington DC, pp 2-16, 1992).

Therefore, in order to prevent the above-mentioned diseases, a large amount of fruit active ingredients containing a large amount of polyphenols such as flavonoids is required. Recently, it is sold to consumers in the form of fruit juice or fruit juice, but a large amount through these products Fruit intake is not possible due to intake limitations.

Accordingly, it is an object of the present invention to provide a method of easily extracting active ingredients from mixed fruits and to provide a pharmaceutical or food preparation using the same as a main ingredient so that a large amount of fruit active ingredients can be easily ingested.

Furthermore, the present invention is to provide a method of extracting active ingredients from apples, pears, grapes, tangerines and the like and preparing them in the form of easy-to-take preparations and their use.

In order to achieve the above object, the present invention washes and grinds four kinds of fruits such as apples, pears, grapes, and citrus fruits with a peel, and then takes a predetermined amount and adds ethanol in an amount of 1-15 times as an extraction solvent. 15 days of immersion to extract the active ingredient, and the extracted solution is concentrated under reduced pressure to produce a fruit active ingredient extract.

In particular, it is preferable to make apples, pears, grapes, and tangerines in a ratio of 1: 1: 1: 1.

In addition, the present invention provides an antioxidant and a free radical scavenging agent, characterized in that the active ingredient extract prepared by the above method as a main ingredient, and an excipient which can be added pharmaceutically can be added thereto.

In particular, the active ingredient extract is preferably added in an amount of 0.01-30.0%.

The free radical scavenging agent and the antioxidant of the present invention are formulated by adding one or more pharmaceutically acceptable carriers to the fruit active ingredient composition prepared according to the above-mentioned manufacturing method. Preferred formulations include tablets, capsules, soft capsules and liquids. Can be mentioned.

The free radical scavenging agent and antioxidant containing the fruit active ingredient of the present invention should contain 60-200 mg of one tablet or 1 capsule or mixed fruit active ingredient composition per bottle, and when used as a free radical scavenging agent or antioxidant, three times a day It is preferable to take 1-2 tablets or capsules or 1 bottle once.

Hereinafter, the present invention will be described in more detail with examples and experimental examples, but the present invention is not limited thereto.

Example 1

Wash apples, pears, grapes, and citrus fruits with peel, crush them, and mix them 250g each, add 1L of 100% ethanol, extract for 7 days, and filter. Concentrate the filtrate to obtain fruit active ingredient extract.

The yield of the fruit active ingredient extract thus obtained is shown in Table 1 below.

Table 1. Yield of fruit active ingredient extract

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Experimental yield (%)

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1 6.8

2 6.6

3 6.7

Average 6.7

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Example 2

The total flavonoid content in the fruit active ingredient extract obtained in Example 1 was quantified as a total flavonoid using Hyperoside E1cm 1% (425 nm) = 500 according to the German Pharmacopeia (Deutsch Arzneibuch, 1988) Betulae Folium term. In summary, 0.2 g of dry powder of fruit is precisely taken, and 1 ml of 0.5% Methenamine, 20 ml of acetone, and 2 ml of 25% hydrochloric acid are added, and a reflux condenser is attached and boiled for 30 minutes. Next, the reaction solution was filtered, and 20 ml of acetone was added to the flask, and the same operation was repeated. Acetone is added to the acetone solution thus obtained to make 100 ml, of which 20 ml is taken in a separatory filter, and then ethyl acetate is added to 15 ml, 15 ml, and 10 ml in this order. 50 ml of water was added twice to the collected ethyl acetate layer, and the mixture was adjusted to 50 ml with ethyl acetate. 1 ml of aluminum chloride solution is added to 10 ml of this solution, 5 ml of methanolic acetic acid is added, and 25 ml of the solution is absorbed at 425 nm. In the blank test, absorbance is measured in the same manner without adding aluminum chloride solution.

As shown in Table 2, the fruit active ingredient extract showed a content of about 0.1% as total flavonoids.

Table 2. Total Flavonoid Content of Fruit Active Ingredient Extracts (%) ^*

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Frequency Total Flavonoid Content (%)

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1 0.097

2 0.095

Average 0.096

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Example 3

1) antioxidant activity

The results of assaying the antioxidant activity of the fruit active ingredient extracts prepared in Example 1 were as shown in Table 3. Antioxidant effect was measured by TBA analysis using lipid peroxidation system by Fenton reaction. That is, after adding ethanol extract of vegetable powder to 5 ml of 25 mM Trizma HCl / o.75 mM Kcl buffer containing 10ul of ethyl linoleate 0.2% SDS, ferrous chloride 10umol, and 2umol of hydrogen peroxide, incubated for 16 hours at 55 ° C. After 50ul of 4% BHT is added, the reaction is stopped. 0.3 ml of this solution is added to a test tube, and 0.05 ml of HCl 3.0 ml, 0.67% TBA solution are added and boiled for 30 minutes. After cooling the reaction solution, 4.0 ml of 85% butanol was added and the absorbance of the butanol layer was measured at 535 nm after centrifugation to determine the antioxidant effect (%).

The fruit active ingredient extract showed a dose-dependent antioxidant effect at a dose concentration of 25-500 ug / ml and showed good activity despite being crude extract, although its activity was lower than that of vitamin E, a known pure antioxidant.

Table 3. Antioxidant Activity of Fruit Active Ingredient Extracts

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Concentration Antioxidant Effect (%) *

(ug / ml)

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Fruit Active Ingredient Extract 25 7.2

50 13.0

100 25.8

200 34.8

Vitamin E 25 66.2

50 80.9

100 88.6

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* 3 experiment average

2) Free radical scavenging action

The results of assaying the free radical scavenging activity of the fruit active ingredient extract prepared in Example 1 were as shown in Table 4.

For free radical scavenging, add 2 ml of DMSO solution of vegetable powder ethanol extract to 2 ml of 60uM 1,1-diphenyl-2-picryl hydrazyl (DPPH) ethanol solution, react for 30 minutes at room temperature, and measure the absorbance at 520 nm. Obtain the radical scavenging effect (%).

The mixed fruit active ingredient composition showed a dose-dependent free radical scavenging effect at a dose concentration of 25-500 ug / ml, and the activity was slightly lower than that of vitamin E, a known pure antioxidant, but good activity despite being crude extract. Indicated.

Table 4. Free radical scavenging activity of mixed fruit active ingredient composition

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Concentration Free Radical Scavenging Effect (%) *

(ug / ml)

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Fruit Active Ingredient Extract 25 2.0

50 3.3

100 4.5

200 6.1

500 13.1

Vitamin E 5 33.0

10 64.9

20 78.8

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* 3 experiment average

Example 4

Acute Toxicity Test of Fruit Active Ingredient Extracts

1) Experiment Method

The fruit active ingredient extract of Example 1 was orally administered to ICR mice and SD rats, and individual mortality was observed within 24 hours.

2) Experiment result

None of the individuals died up to the oral dose of 5 g / kg.

Fruit active ingredient extract of the present invention can be prepared by mixing with auxiliaries such as excipients, binders, lubricants, disintegrants, diluents and the like.

Preparation Example

1) Preparation of Tablets

The following ingredients were mixed homogeneously and compressed into tablets of 200 mg according to the tablet manufacturing method in the pharmacopeia formulation general rules.

Fruit Active Ingredient Extract 60mg

Lactose 81mg

Microcrystalline cellulose 50mg

Light anhydrous silicic acid 1mg

Crospovidone 6mg

Magnesium Stearate 2mg

2) Preparation of capsule

The following raw materials were mixed homogeneously and filled in such a way that 270 mg was contained in one capsule according to the capsule preparation method of the pharmacopeia formulation.

Fruit Active Ingredient Extract 60mg

Lactose 204 mg

Light anhydrous silicic acid 4.8mg

Magnesium Stearate 1.2mg

3) Preparation of soft capsule

The following compositions were filled in such a way that 695 mg of 1 capsule was contained according to the soft capsule preparation method of the pharmacopeia formulation.

1) Filling composition

Fruit Active Ingredient Extract 60mg

Lecithin 20mg

Soybean oil 149.4mg

Coconut Cured Oil 38mg

Lead 12 mg

2) dry skin composition

Gelatin 247.2mg

Concentrated glycerin78mg

Dissorbitol solution 70% 90.05mg

Paraoxybenzoic Acid Methyl 0.28mg

Paraoxybenzoic acid propyl 0.07mg

Echivanillin Correction

Blue No. 1

Yellow No. 203

Titanium Oxide

Fraction palm oil quantity

4) Preparation of liquid

The following raw materials were prepared according to the liquid preparation method in the Pharmacopoeia General Regulations, and filled and sealed in 100 ml brown bottles and pasteurized.

Fruit Active Ingredient Extract 100mg

Citric acid 4mg

Honey 20mg

Liquid Fructose58mg

Niacinamide 20mg

Sodium benzoate 70mg

Povidone

Yellow No. 203, Blue No. 1

Menthol flavored flavor

Purified water

The present invention configured as described above not only provides a method for easily obtaining an extract containing an active ingredient having excellent pharmacological action in fruits such as apples, pears, grapes, and citrus fruits, and the extract obtained thereby as a main component. The composition is a useful invention that can be used as a pharmaceutically stable antioxidant, free radical scavenger.

Claims (3)

Wash and grind four kinds of fruits such as apples, pears, grapes, and citrus fruits with a peel, crush them, take a certain amount each time, and add ethanol in an amount of 1-15 times as an extraction solvent, and deposit the effective ingredient at room temperature for 1-15 days, Method of producing a fruit active ingredient extract, characterized in that to extract the extracted extract solution under reduced pressure to produce a fruit active ingredient extract. Antioxidant based on the extract obtained according to claim 1 as a main component, to which a pharmaceutically acceptable additive is added. A free radical scavenging agent, comprising a extract obtained according to claim 1 as a main ingredient, to which a pharmaceutically acceptable additive is added.