KR20130130995A - A preparation method of an effervescent tablet comprising an extract of kyungokgo or crude drug - Google Patents

Abstract

The present invention relates to a production method of an effervescent tablet containing kyungokgo, or extracts of medical herbs including red ginseng, acanthopanax, fruit of Maximowiczia typica, Angelica gigas NAKAI, fruit of Chinese matrimony vine, hedge parsley, Rubus coreanus, cuscuta seeds, cnidium, gastrodia, dried ginger, and jujube. More specifically the present invention has fast-acting and slow releasing effects by forming the kyungokgo or a wood-cultivated ginseng extract which is useful for fatigue recovery into the effervescent tablet, and enables users to easily eat the effervescent tablet after dissolving in water. [Reference numerals] (AA) Kyungokgo

Description

Process for preparing effervescent tablet containing jadeite or herbal extract {A PREPARATION METHOD OF AN EFFERVESCENT TABLET COMPRISING AN EXTRACT OF KYUNGOKGO OR CRUDE DRUG}

The present invention relates to a method of producing effervescent tablets containing medicinal herbs such as jadeite, or red ginseng, ogapi, Schisandra chinensis, Angelica, goji berry, casualty, Bokbunja, Tosa, Cheongung, Cheonma, Health, Jujube.

Ishiyama M. etal, 1996. Bio Pharm Bull 19: 1518-1520

2 Blois MS. 1958.Nature 181: 1199-1203

The present invention relates to a method for producing effervescent tablets containing jade or goat ginseng extract.

Gyeongokgo is a traditional medicine related to health promotion recorded in Dongbobogam. It is a prescription made in Korea by adding ginseng, Baekbongryeong, Saenghwanghwang, honey, sewage, macmundong, and huts, extracting jadeite and natural products and increasing the yield of soluble ingredients. When added to food, the effects of saponin, pacman (betaglucan), and pachymic acid in jadeite and natural products can double the effects of fatigue, strengthening immune function, protecting skin, moisturizing and anti-aging. By mixing with vitamins and minerals to develop a foamed formulation, it is excellent for the human body, easy to carry and take, and can provide products that help nutrition and health for all ages.

In general, effervescent tablets are tablet-type formulations. When the effervescent tablets are added to water, the effervescent tablets are bubbled in water to dissolve and the components of the conventional tablets are present in the aqueous solution. It is to increase the efficacy by ingesting an aqueous solution.

As mentioned above, effervescent tablets are widely used in the food, medicine, health and environment fields, but relatively little are still used in the food field. Effervescent tablets are dissolved in water and the final formulation is in the form of an aqueous solution. Aqueous formulations are commonly used in food-related fields, but these beverages are still filled in containers such as cans, PET, and glass bottles to be provided as commodities.

However, none of this document discloses or teaches a method for producing effervescent tablets containing jadeite or goat's ginseng extract.

Therefore, this study solves these troublesome and difficult problems in order to improve the inconvenience of the conventional method of ironing jadeite with the conventional technology, and by quantifying the jadeite in order to make it easy to take it, it is easy to take it from time to time. Antioxidant activity such as preparation method of effervescent tablet containing jadeite or goat's ginseng extract and measurement of electron donation (DPPH) activity, measurement of SOD-like activity, measurement of Xanthine oxidase inhibitory activity, etc. The present invention was completed by verifying medical effects such as cancer-causing effects using CCRF fibroblast line of mice.

In order to achieve the above object,

The present invention is a mixture of (1) vitamins, herbal extracts or jadeite, organic acids, sugar alcohols to obtain a first mixture, by mixing one or more components selected from amino acids, flavors, salts, food additives, and sweeteners to the first mixture A first step of obtaining a mixture of two; (2) a second step of mixing the first mixture and the second mixture followed by adding a stabilizer to the mixture; (3) a third step of adding and mixing the binder and the blowing agent to the mixture to which the stabilizer of the second step is added; (4) a fourth step of adding and mixing a lubricant, a disintegrant, a colorant, and a preservative, respectively, to the mixture of the third step; (5) Provides a method for producing effervescent tablets containing jadeite or goat ginseng extract comprising the fifth step of the tableting the mixture of the fourth step.

More specifically, the present invention is (1) 2 to 14% by weight of vitamin, preferably 2 to 10% by weight, 1 to 18% by weight of herbal extract or jadeite, preferably 2 to 10% by weight, organic acid 1 to 14 1% to 12% by weight of sugar alcohols are mixed to obtain a first mixture, 0.5 to 2% by weight of amino acids, 6 to 10% by weight of fragrances, 0.2 to 0.6% by weight of salt, and 1 to 2% by weight of food additives. %, And a first step of mixing the sweetener 1 to 2% by weight to obtain a second mixture; (2) a second step of mixing the first mixture and the second mixture followed by adding 1 to 12% by weight of a stabilizer to the mixture; (3) a third step of adding and mixing 20 to 40% by weight of the binder and 4 to 56% by weight of the blowing agent, preferably 20 to 30% by weight, to the mixture to which the stabilizer of step (2) is added; (4) about 30 to 90% by weight, preferably 50 to 70% by weight of the lubricant of 1 to 12% by weight, preferably 1% or less, and a disintegrant, colorant and preservative in the mixture of step (3) A fourth step of adding and mixing%; It provides a method for producing effervescent tablets containing jadeite or goat ginseng extract comprising the fifth step of the step of tableting the mixture of the fourth step.

In the first step of the manufacturing method, the vitamin is a water-soluble vitamin, preferably, vitamin C, or any one or more vitamins selected from vitamin B1, vitamin B2, vitamin B6, vitamin B12, nicotinamide, pantothenic acid, biotin, folic acid, and more. Preferably vitamin C.

The organic acid that can be used as a fatigue recovery material in the first step of the production method is citric acid, maleic acid, lactic acid, tartaric acid, succinic acid, or puma At least one selected from fumaric acid, and preferably citric acid.

In the first step of the manufacturing method, the herbal medicine is goat ginseng, red ginseng, ogapi, Schisandra chinensis, Angelica, Gugija, casualty, Bokbunja, Tosa, Cheongung, Cheonma, Health, or Jujube; The jadeite is a compounding ratio of ginseng, sewage, raw sulfur, Bokryeong, earth tree, ganmundong, brown root and honey, preferably ginseng 1 to 6% by weight, sewage 3 to 15% by weight, raw sulfur to 20 to 40% by weight, Bokyeong 2 to The jadeite or goat's ginseng extract, which is composed of a composition of 10% by weight, 10-20% by weight, 1-6% by weight of McMoon-Dong, 1-10% by weight, and 10-30% by weight of honey, is preferably in the form of an extract powder. The powder may be an extraction method commonly used in the art, for example, a hot water extraction method using hot water, a solvent extraction method using a solvent such as ethanol.

Alternatively, the extract extracted by the extraction method can be concentrated to use a concentrate of 20 to 65 brix, preferably 30 to 45 brix. Extract obtained by the extraction method as described above may be dried and powdered by lyophilization and fluidized bed drying method to formulate in a powder form that is easy to tablet.

Extraction conditions of the hot water extraction method or solvent extraction method may be carried out using conditions widely used in the food or pharmaceutical related fields. As an example of such extraction conditions, hot water extraction method which is extracted for 10 to 60 minutes in hot water of 60 to 120 ℃, preferably 80 to 100 ℃ or 20 to 80 ℃, preferably 40 to 50 ℃ water, methanol, ethanol, Butanol or a solvent extraction method may be used to extract for 10 to 120 minutes, preferably 30 to 60 minutes as a mixed solvent thereof. In addition, as an example of the drying conditions of obtaining the extract from the herbal medicine by using a hot water extraction method or a solvent extraction method and drying it, -10 ℃ to -60 ℃, preferably -30 ℃ to -40 ℃ freeze-drying, or spray dryer Extract may be powdered by performing spray drying.

Herbal medicines as defined herein are goat's ginseng, red ginseng, ogapi, schisandra, Angelica, wolfberry, casualty, bokbunja, earth and sand, cheongung, cheonma, health, or jujube, and preferably goat or ginseng.

As the first mixture in the first step of the production method, the sugar alcohol has a component that exhibits sweetness, and has a characteristic different from that of a commonly used sweetener. For example, sugar alcohols are stable under acidic conditions, do not change in the range of pH 2 to 10, have moderate solubility, exhibit indigestion in the intestine, and can be added to various foods as low calorie substances of about 2.0 to 2.4 kcal / g. Therefore, it is widely used as a low calorie, obesity prevention, sugar substitute sweetener for diabetics as a food material. Examples of such sugar alcohols in the present invention include mannitol, sorbitol, maltitol, xylitol, erythritol, lactitol, glycitol, glicitol, and ribitol. It is characterized in that any one or more selected from galactitol (galactitol), preferably one or more sugar alcohols selected from D-sorbitol or mannitol.

At least one component selected from amino acids, flavors, salts, food additives, and sweeteners may be optionally added to the first mixture in the first step of the preparation method as the second mixture, preferably, 0.5 to 2% by weight of amino acids, A second mixture can be produced by mixing 6 to 10% by weight of fragrance, 0.2 to 0.6% by weight of salt, 1 to 2% by weight of food additives, and 1 to 2% by weight of sweetener.

Amino acids, such as taurine, aspartic acid, threonine, which can be used as a fatigue recovery material or protein feeder that can be added as a second mixture in the first step of the manufacturing process , Serine, Glutamic acid, Proline, Glycine, Alanine, Cysteine, Valine, Methionine, Isoleucine, Tyrosine One or more selected from (Tyrosine), phenylalanine (Phenylalanine), tryptophane (Tryptophane), lysine (Lysine), histidine (Histidine), arginine (Arginine).

As the fragrance which can be added as the second mixture in the first step of the manufacturing process, any of the fragrances used to dissolve the effervescent tablets in water to improve the organoleptic functionality can be used as long as they are food acceptable. As an example of the flavor in the present invention pineapple flavor, apple flavor, orange flavor, lemon flavor, grape flavor, cherry flavor, peach flavor, apricot flavor, strawberry flavor, mango flavor, lime flavor, melon flavor, plum flavor, mulberry flavor, bokbunja Incense, ginseng flavor, red ginseng flavor, jujube flavor, ginger flavor, citron flavor can be used any one or more selected.

The salt added in order to contain a suitable salt in the effervescent tablet which can be added as a 2nd mixture in the said 1st step of the said manufacturing process can be used as long as it can be used conventionally in food science. In the present invention, as one example of such a salt, any one or more selected from potassium chloride (Potassium Chloride, KCl) and sodium chloride (NaCl) may be used.

Food additives added to improve the functionality of the foamed tablets that can be added as the second mixture in the first step of the manufacturing process can be used as long as they can be used conventionally in food science. As an example of such a food additive in the present invention, sodium gluconate (C 6 H 11 O 7 Na) may be used.

In the first step of the manufacturing process, the sweetening agent added as a second mixture in order to improve the functionality of taste can be used as long as it can be used in food. As an example of such a sweetener in the present invention, any one or more selected from aspartame, sugar, saccharin, acesulfame potassium, stevioside, glucose, fructose and sugar may be used.

In preparing the foamed tablet in the present invention, in order to achieve the object of the present invention, it is preferable to first obtain the first mixture in the step (1), and then obtain the second mixture in the step (1) and then mix the respective mixtures. . At this time, in order to produce effervescent tablets according to the object of the present invention (1) in the step of vitamins, herbal extract powder, organic acid and sugar alcohols mixed in various contents bar vitamin 3-4% by weight, herbal extract powder 1-2% by weight , 36.4 to 57.3% by weight of organic acid, and 4 to 6% by weight of sugar alcohol may be mixed to obtain a first mixture. In addition, amino acids, flavors, salts, food additives, and sweeteners are mixed with respect to various contents in step (1), and 0.5 to 2% by weight of amino acids, 6 to 10% by weight of flavors, 0.2 to 0.6% by weight of salts, and food additives 1 to 1. It is good to mix 2 weight% and the sweetener 1-2 weight%, and to obtain a 2nd mixture.

1 to 20% by weight, preferably 2 to 10, of a stabilizer which can be used for food preparation after mixing the first mixture and the second mixture of step (1) in the second step of the manufacturing process. Addition in weight percent amounts to stabilize the mixture. In the step (2), if the stabilizer is used below the above-mentioned numerical range, there is no meaning of using the stabilizer. If the stabilizer is used above the above-mentioned numerical range, there is a concern that the time for dissolving the expanded tablet in water may increase. Therefore, the stabilizer in the step (2) is preferably used within the above-described numerical range. The stabilizer used in the step (2) can be used as long as it can be used in food. As an example of such a stabilizer in the present invention, it can be used as a stabilizer in food production, selected from among tricalcium phosphate, calcium phosphate, sodium tartrate, sodium fumarate or DL malic acid with good solubility in water. Any one or more, preferably any one or more selected from tricalcium phosphate or monobasic calcium phosphate can be used.

The binder usable in the third step of the manufacturing process can be added in an amount of 10 to 60% by weight, preferably 2 to 40% by weight, and as binders conventional in the art, preferably lactose, CMC-Ca , Water, organic solvent, polyvinylpyrrolidone, hydroxypropylcellulose, microcrystalline cellulose, hydroxypropylmethylcellulose, dextrin, gelatin, methylcellulose, hydroxycellulose, hydroxymethylcellulose, polyvinyl alcohol, pre-gelatinized It may further comprise at least one component selected from starch (Pregelatinized Starch) or gum arabic, preferably at least one component selected from lactose, CMC-Ca,

Foaming property in which the foaming tablet is dissolved in water by adding and mixing the blowing agent in an amount of 1 to 20% by weight, preferably 2 to 15% by weight, to the mixture to which the stabilizer is added in the third step to the second step of the manufacturing process. You can have it. In the step (3), if the blowing agent is used below the above-mentioned numerical range, there is no meaning of using the blowing agent, and if the blowing agent is used above the above-mentioned numerical range, there is a problem that it takes a long time to dissolve when the foaming tablet is dissolved in water. have. Therefore, the blowing agent in the step (3) is preferably used within the above-described numerical range. The foaming agent used in the above (3) step can be used as long as it can be used in food. As an example of such a blowing agent in the present invention, one or more components selected from sodium bicarbonate and sodium bicarbonate (NaHCO 3) may be used.

In the fourth step of the manufacturing process, the lubricant used in the present application may be added in an amount of 1 to 5% by weight, preferably 1 to 3% by weight, and as a conventional lubricant, preferably magnesium stearate, Mg Stearate, One or more mixtures of talc, stearic acid or light silicic anhydride (SiO ₂ ) may be used,

In the fourth step of the manufacturing process, optional disintegrant, colorant, and preservative components conventionally known in the art may be mixed in an amount of 1 to 50% by weight, preferably 1 to 30% by weight, respectively. It may further contain a flavourant, stabilizer, or diluent.

Disintegrants usable herein include, as conventional disintegrants, sodium starch glycolate, crospovidone, cross-linked sodium carboxymethyl cellulose, low-substituted hydroxypropyl cellulose. Hydroxypropylcellulose), hydroxypropylmethylcellulose, polyvinylpyrrolidone, starch, carboxymethyl cellulose calcium and combinations thereof, and may include one or more thereof.

In addition, if necessary, a colorant may be included in the tablet, and may include one or more selected from titanium dioxide, iron oxide, magnesium carbonate, calcium sulfate, magnesium oxide, magnesium hydroxide, aluminum lake, and the like.

Preservatives usable herein may include one or more selected from benzoic acid, methylparaben, ethylparaben or propylparaben and the like.

In the step (4), the mixture in which the blowing agent is added in the third step and the foaming tablet composition is mixed can be prepared by tableting using a tableting machine. At this time, when tableting the foamed tablet composition including the foaming agent, the tableting conditions may be prepared using the conditions generally used in manufacturing foamed tablets. At the time of such tableting conditions, the tableting conditions for tableting the foamed tablet composition including the foaming agent may be prepared using the conditions generally used in manufacturing foamed tablets. As an example of such tableting conditions, a foamed tablet can be obtained by tableting with a tableting machine such as a single tableting machine at a temperature of 22 to 24 ° C and a relative humidity of 10 to 30%.

The method for producing the expanded tablet of the present invention for achieving the above-mentioned object can be obtained by using the fatigue recovery material as a main material, and the food-acceptable excipient as a subsidiary material. In this case, as an example of the fatigue recovery material, vitamins, herbal herb extract powders, organic acids and amino acids may be used, and as the other excipients, food additives, stabilizers, sweeteners, sugar alcohols, salts, flavorings, and foaming agents allowed to be used in foods may be used. .

In another aspect, the present invention provides an effervescent tablet preparation excellent in antioxidant activity and anticancer activity prepared by the above production method.

The preferred dosage of the composition of the present invention varies depending on the condition and the weight of the patient, the degree of disease, the type of drug, the route of administration and the period of time, but can be appropriately selected by those skilled in the art.

Accordingly, the present invention provides a pharmaceutical preparation for the prevention and treatment of antioxidant and cancer diseases, which contains the herb extract or jadeite as an active ingredient.

The pharmaceutical composition of the present invention comprises 0.1 to 50% by weight of the above extract, based on the total weight of the composition.

However, the composition is not limited thereto, and may vary depending on the condition of the patient, the type of disease, and the progress of the disease.

Since the extract of the present invention has little toxicity and side effects, it can be safely used even for long-term administration for the purpose of prevention.

The compositions of the present invention may further comprise suitable carriers, excipients and diluents conventionally used in the manufacture of pharmaceutical compositions.

The composition of the present invention may be formulated in the form of powders, granules, tablets, capsules, suspensions, emulsions, syrups, aerosols and the like, oral preparations, suppositories and sterilized injection solutions, Examples of carriers, excipients and diluents that can be included in the composition containing the extract include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate , Cellulose, methylcellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. In the case of formulation, a diluent or excipient such as a filler, an extender, a binder, a wetting agent, a disintegrant, or a surfactant is usually used. Solid preparations for oral administration include tablets, pills, powders, granules, capsules, and the like, and the solid preparations may include at least one excipient such as starch, calcium carbonate, sucrose in the extract. ) Or lactose, gelatin and the like are mixed. In addition to simple excipients, lubricants such as magnesium stearate talc are also used. Examples of the liquid preparation for oral use include suspensions, solutions, emulsions, and syrups. In addition to water and liquid paraffin, simple diluents commonly used, various excipients such as wetting agents, sweeteners, fragrances, preservatives and the like may be included . Formulations for parenteral administration include sterilized aqueous solutions, non-aqueous solutions, suspensions, emulsions, freeze-dried preparations, and suppositories. Examples of the suspending agent include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, injectable ester such as ethyl oleate, and the like. Examples of suppository bases include witepsol, macrogol, tween 61, cacao butter, laurin, glycerogelatin, and the like.

The preferred dosage of the composition of the present invention varies depending on the condition and the weight of the patient, the degree of disease, the type of drug, the route of administration and the period of time, but can be appropriately selected by those skilled in the art. However, for the desired effect, the extract of the present invention is preferably administered at 0.5 g / kg to 5 g / kg, preferably 1 g / kg to 3 g / kg per day. The administration may be carried out once a day or divided into several doses. Thus, the dosage amounts are not intended to limit the scope of the invention in any manner.

The composition of the present invention may be administered to mammals such as rats, mice, livestock, humans, and the like in various routes. All modes of administration may be expected, for example, by oral, rectal or intravenous, intramuscular, subcutaneous, intra-uterine or intracerebroventricular injections.

In addition, the present invention provides a health functional food for the prevention and improvement of antioxidant and cancer diseases containing the herbal extract or jadeite as an active ingredient obtained by the above production method.

&Quot; Health functional food "as defined herein means food prepared and processed using raw materials or ingredients having functionality useful to the human body in accordance with Law No. 6727 on Health Functional Foods." Functional " Structure and function of the nutrient to control or physiological effects, such as to obtain a beneficial effect for health is intended to eat.

The dietary supplement for antioxidant and cancer prevention of the present invention comprises the extract in an amount of 0.01 to 95%, preferably 1 to 80% by weight, based on the total weight of the composition.

In addition, it is possible to manufacture and process as a dietary supplement in the form of tablets, capsules, powders, granules, liquid, pills for the purpose of preventing obesity.

The present invention provides a dietary supplement comprising the above-mentioned herbal extract or jadeite ointment showing the effects of antioxidant and cancer prevention and treatment. Examples of foods to which the extract can be added include various foods, beverages, gums, tea, vitamin complexes, and health functional foods.

The composition containing the extract of the present invention can be used in various ways, such as drugs, foods and drinks for the prevention and improvement of antioxidants and cancer. Examples of the foods to which the extract of the present invention can be added include various foods, beverages, gums, tea, vitamin complexes, health supplements and the like, and they can be used as powders, granules, tablets, capsules or beverages have.

In another aspect, the present invention provides a food additive containing an herbal extract or jadeite as an active ingredient obtained by the above production method having antioxidant activity and anticancer activity. Extract of the present invention may be added to food or beverage for the purpose of preventing and improving cancer diseases. At this time, the amount of the extract in the food or beverage is generally the health food composition of the present invention can be added to 1 to 5% by weight of the total food weight, the health beverage composition is 0.02 to 10 g, preferably based on 100 ml Can be added in a ratio of 0.3 to 1 g.

The health beverage composition of the present invention, in addition to containing the extract as an essential ingredient in the indicated ratio, there is no particular limitation on the liquid component and may contain various flavors or natural carbohydrates, etc. as additional ingredients, like ordinary drinks. Examples of the above-mentioned natural carbohydrates are conventional monosaccharides such as disaccharides such as glucose and fructose, such as maltose, sucrose and the like, and polysaccharides such as dextrin, cyclodextrin and the like. Sugars and sugar alcohols such as xylitol, sorbitol, and erythritol. As natural flavors other than those described above, natural flavors (such as tau martin, stevia extract (e.g., rebaudioside A, glycyrrhizin)) and synthetic flavors (saccharin, aspartame, etc.) have. The proportion of such natural carbohydrates is generally about 1 to 20 g, preferably about 5 to 12 g per 100 ml of the composition of the present invention.

In addition to the above, the composition of the present invention includes various nutrients, vitamins, minerals (electrolytes), flavors such as synthetic flavors and natural flavors, coloring and neutralizing agents (such as cheese and chocolate), pectic acid and salts thereof, alginic acid and its Salts, organic acids, protective colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohols, carbonation agents used in carbonated drinks, and the like. In addition, the compositions of the present invention may contain flesh for the production of natural fruit juices and vegetable beverages. These components may be used independently or in combination. The proportion of such additives is not so critical, but is generally selected in the range of 0 to about 20 parts by weight per 100 parts by weight of the composition of the present invention.

As described above, effervescent tablets containing jadeite or goat's ginseng extract of the present invention can be easily taken at any time, and measuring the electron donation (DPPH) activity of the jadeite or goat's ginseng extract, SOD-like activity measurement, The excellent medicinal efficacy has been proven in antioxidant activity such as Xanthine oxidase inhibitory activity measurement and anticancer activity using CCRF fibroblast line of mouse, and can be usefully used as a composition and formulation of medicines and health functional foods.

1 is a diagram showing the results of experiments measuring the cell viability of jadeite extract;
Figure 2 is a diagram showing the results of the cell survival rate measurement of goat ginseng extract;
Figure 3 is a diagram showing the experimental results of measuring the DPPH radical scavenging activity of the individual extracts;
4 is a diagram showing the results of experiments measuring the SOD-like activity of the individual extracts;
5 is a diagram showing the results of experiments measuring the xanthine oxidase inhibitory activity of the individual extracts;
6 is a view showing an experimental result confirming the foaming effect of the foamed tablets.

Hereinafter, the present invention will be described in detail with reference to the following Reference Examples and Experimental Examples.

However, the following Reference Examples and Experimental Examples are merely illustrative of the present invention, and the content of the present invention is not limited by the following Reference Examples and Experimental Examples.

Reference Example  One. Jadeite  Preparation of extract

The jadeite used in the experiment was purchased with herbal medicine in Daegu Yangnyeongsi, and the jadeite purchased (Yangnyeongsi Co., Ltd.) ( www.w-herbmall.com ) manufactured with the composition of Table 1 was used.

Jadeite prescription Raw material name Ratio (w / w%) Remarks (Solvent) Ginseng 4 H ₂ O: EtOH = 5: 5 Sewage 10 H ₂ O: EtOH = 5: 5 Living place 30 H ₂ O Ghost 8 H ₂ O: EtOH = 5: 5 Earth tree 15 H ₂ O: EtOH = 5: 5 McMundong 3 H ₂ O: EtOH = 5: 5 Root 5 H ₂ O: EtOH = 5: 5 honey 25 Sum 100

After dissolving the prepared jadeite in water and centrifuging with a centrifuge (Centrifuge continental R and Hanil Science Industrial Co., Ltd.) at 12,000 rpm, the precipitate is discarded and the supernatant is 0.8 μm membrane filter (DISMIC). The powder obtained by lyophilization with lyophilizer (10-RT, ilshin Lab Co., Ltd.) and fluidized bed granulator (TIM-G30, Jaeilkigong) after filtration using -25CS, Advantec) It was used in the following experimental example.

Reference Example  2. Goat's ginseng  Preparation of extract

Goat ginseng used in the experiment was filtered for 8 years and extracted with reflux extracted at 100 ° C for 4 hours with water for 8 years (Daegu Yangnyeongsi), and then centrifuged at 12,000 rpm with centrifuge continental R and Hanil Science Industrial Co., Ltd. After separation, discard the precipitate and filter the supernatant with a 0.8㎛ membrane filter (DISMIC). The powder obtained by lyophilization with lyophilizer (10-RT, ilshin Lab Co., Ltd.) and fluidized bed granulator (TIM-G30, Jaeilkigong) after filtration using -25CS, Advantec) It was used in the following experimental example.

Example  One. Effervescent tablet  Produce

Effervescent tablets containing vitamins were prepared using the following procedure.

(1) 8.0% by weight of vitamin C, 2.0% by weight of herbal extract, 7.5% by weight of citric acid and 6.0% by weight of mannitol were mixed to obtain a first mixture. In addition to the first mixture, 1.0% by weight of D-sorbitol and 6.0% by weight of mannitol were mixed as a sweetener to obtain a second mixture.

(2) After mixing the first mixture and the second mixture, 1.0% by weight of tricalcium phosphate and 1.0% by weight of monobasic calcium phosphate were mixed as a stabilizer.

(3) 30.0% by weight of lactose, 2.0% by weight of CMC-Ca, and 10.0% by weight of sodium hydrogencarbonate as a blowing agent were added to the mixture to which the stabilizer was added in step (2), followed by mixing.

(4) 1.5 wt% of magnesium stearate as a lubricant was added to the mixture to which the blowing agent was added in the step (3), followed by mixing.

(5) The mixture was compressed into tablets using a rotary tablet press at a temperature of 20 ° C. and a relative humidity of 30% to prepare circular foamed tablets having a weight of 2,000 mg, a diameter of 1.8 cm, and a thickness of 6 mm.

The herbal extract powder was obtained by extracting the herbal extracts for 180 minutes at 100 ℃ and concentrated to 30 brix (brix) and then lyophilized. On the other hand, the foamed tablet composition and content are shown in Table 2 below.

Effervescent tablet composition Configuration designation Formulation ratio (%) Unit weight (mg) Remarks Usage Main ingredient Vitamin-C 8.0 160 100% Functional raw materials Supplementary material Anhydrous citric acid 7.5 150 99.5% ↑ Organic acid D-sorbitol 1.0 20 glucose Sweetener (sugar alcohol) Tricalcium phosphate 1.0 20 90% ↑ Other stabilizers Stearic acid
magnesium 1.5 30 100% Lubricant CMC-Ca 2.0 40 Carboxymethyl
Cellulose calcium Binder Mannitol 6.0 120 100% Sweetener (sugar alcohol) Calcium primary phosphate 1.0 20 100% Other stabilizers Lactose 30.0 600 Lactose 95%
(Milk / U.S.),
Dextrin 5% Binder Starch (corn) 30.0 600 100% (import) Disintegration Sodium hydrogencarbonate 10.0 200 100% blowing agent Herbal Extract
(KOG) 2.0 40 Saengjihwang, Sewao, Fuling, Brown root, Ginseng, Macmundong Functional raw materials Sum 100 2,000

The experimental results, the main ingredient not less than (Vit C, suitable reference geongisik) as result a reference capacitance calculation and selected, (1) vitamins, extract powder is blended with 10% or less, (2) organic acids, and can broaden the addition range , (3) 20 to 25% of foaming agent is suitable, (4) 50 to 70% of binder, disintegrant, and lubricant other than carbonate can be blended. (5) Very small amount of magnesium stearate or sodium benzoate as lubricant. It is suitable to mix it with 1% or less, (6) It is good to add about 5 ~ 20% of starch that holds moisture, and (7) MC crystalline cellulose is good for tableting, but the more turbid and sludge, the more 1% ~ 20% range (7) It was confirmed that it is necessary to confirm that the other insoluble impurities are necessary for checking the water solubility, and whether or not the impurities float and the sludge after the frozen extract powder is dissolved.

Experimental Example 1. Validation of anticancer activity of Kyongokgo and Goatsam extract

In order to confirm the anticancer activity of the sample obtained in the above example, the experiment was performed by applying the method described in the literature (Ishiyama M. etal, 1996. Bio Pharm Bull 19: 1518-1520).

1.1. Cell culture

CCRF fibroblasts from mice were cultured from Korea Cell Line Bank and cultured at 37 ° C in DMEM medium (Dulbecco's modified Eagle's medium) containing 50 ㎍ / ml of FBS (gentamicin) and 5% inactivated FBS (fetal bovine serum). , 5% CO ₂ incubator.

1.2. Cell viability measurement

Culturing the fibroblast cells of the CCRF mouse to stabilize after a frequency division number such as 8 X 10 ⁴ cells / ml in 96 well plate and the respective gyeongokgo prescription and extract three Samyang After extracting hot water and EtOH, the concentrated and lyophilized powder was treated at a concentration of 0.1 ~ 10mg / ml and incubated for 24 hours, the culture solution was removed, MTT reagent (3- [4,5-dimethylthiazol-2-yl] -2, 30 μl of 5-diphenyltetrazolium bromide (0.5 mg / ml) was added, and 37 ° C CO ₂ for 3 hours. React in the incubator. The insoluble formazan crystals were dissolved in 100 μl of dimethylsulfoxide (DMSO), and the absorbance was measured at a wavelength of 570 nm using a microplate reader (Sunrise Basic Tecan, TECAN). The cytotoxicity was confirmed using the measured value. Each extract was added to the medium at concentrations of 0.1, 0.5, 1, 2 mg / ml, and cell viability was measured by MTT assay.

As a result of the experiment, the jadeite extract showed 86% cell viability at a concentration of 2 mg / ml, and a high cell viability of 90% or more up to a concentration of 1 mg / ml. Therefore, jadeite extract could be identified as a good material for cell viability. Goat ginseng extract showed 60% cell viability at the concentration of 2mg / ml, and cell viability was lower than that of jadeite extract. (See Figures 1 and 2)

Experimental Example 2. Antioxidant Activity of Gyogogo and Goat Ginseng Extracts

In order to confirm the antioxidant activity of the sample obtained in the above example, the experiment was performed by applying the method described in the literature (Blois MS. 1958. Nature 181: 1199-1203.)

To add the functionality of the effervescent tablet development was prepared by the addition of jadeite extract and goat ginseng extract. These materials are known to have excellent antioxidant activity. Antioxidant-related functions include anti-aging, arteriosclerosis, inflammation inhibition, virus inhibition, cold inhibition, physiological disorders, improvement of disease resistance, stress resistance, digestibility improvement, and intestinal microorganisms. It is known to have a mechanism such as stability and confirmed the efficacy on antioxidant (Son SH et al ., 1999. Biotechnol. Bioprocess Eng. 4: 119-123). As a positive control, BHA (Butylated hydroxyanisole) and vitamin C, which are known to have the highest sulfate activity, have been compared.

2.1. Electron donation DPPH ) Active measurement

Electron-donating (DPPH) activity was tested to confirm the use of jadeite extract and goat ginseng extract as anti-oxidant agents in effervescent tablets. The reducing power of the sample was measured by the electron donating effect on 1,1-diphenyl-2-picryl hydrazyl (DPPH) of each sample. That is, 0.5 mL of 0.4 mM DPPH solution was added to 1 mL of each sample prepared for each concentration, and the reaction solution was reacted for 30 minutes at 37 ° C after vortex mixing for 10 seconds, and then the absorbance was measured at 517 nm using a spectrophotometer. It was.

As a result of the experiment, the extracts were confirmed to have an inhibitory effect on the electron donor (DPPH) activity at concentrations of 0.1, 0.5, 1, and 2 mg / ml. As a result, the antioxidant activity was found to be 80% or higher in the jadeite extract at the concentration of 2 mg / ml. In case of goat ginseng extract, the inhibitory effect of 85% was confirmed. These results showed that jadeite and goat ginseng extracts were higher than BHA (Butylated hydroxyanisole), which was used as a positive control. (See Fig. 3)

2.2. SOD - like  Active measurement

SOD-like activity was tested to examine the antioxidant effects using jadeite extract and goat ginseng extract.

3 mL of tris-HCl buffer (50 mM tris [hydroxymethyl] aminomethane + 10 mM EDTA) and 0.2 mL of 7.2 mM pyrogallol were added to 0.2 mL of each sample, and the mixture was left at 25 ° C for 10 minutes, followed by 1 mL of 1 N HCl. After stopping the reaction, the absorbance at 420 nm was measured.

As a result of this study, the SOD-like activity of the extracts at 0.1, 0.5, 1, and 2 mg / ml concentrations showed 78% inhibition of jadeite extract at 2 mg / ml concentration and 88% of goat ginseng extract. The inhibitory effect of was confirmed. These results were compared with vitamin C, which showed the highest antioxidant efficacy as a natural material, as a positive control. As a result, the jadeite extract, which is an extract, was lower in activity than the vitamin C, which is a single substance, but was higher in the case of goat ginseng extract (see FIG. 4). ).

2.3. Xanthine oxidase  Measurement of inhibitory activity

Xanthine oxidase inhibitory activity was tested to examine the antioxidant effect by the different experimental methods using jadeite extract and goat ginseng extract.

Add 0.1 mL of the sample solution and 0.2 mL of 2 mM xanthine substrate solution to 0.6 mL of 0.1 M potassium phosphate buffer at pH 7.5, add 0.1 mL of 0.2 unit / mL xanthine oxidase, and react for 5 minutes at 37 ° C. After completion of the reaction, uric acid generated in the reaction solution was measured at an absorbance of 292 nm. Xanthin oxidase inhibitory activity was shown by the absorbance decrease rate of the sample solution addition group and no addition group.

As a result, Xanthine oxidase inhibitory activity of the extract at 0.1, 0.5, 1, 2 mg / ml concentration was confirmed. As a result, the inhibitory activity of 77% was observed in the jadeite extract at 2 mg / ml concentration. An inhibitory effect of 82% was confirmed. These results showed that the jadeite extract, which had a lower activity than the 84% of BHA, a single substance used as a positive control, had a lower activity, but was similar for goat ginseng extract (see FIG. 5).

As described above, as a result of confirming to develop effervescent functional material by using jadeite extract and goat ginseng extract, the antioxidant effect of goat extract was generally higher than that of jadeite extract, and the material with the highest antioxidant effect was positive control. In comparison, the activity did not drop and was similar or higher.

Experimental Example  3. Herbal Medicine Extract Effervescent tablet  Development effect verification

In order to confirm the foaming effect of the sample obtained in the above example, the experiment was performed by applying the method described in the literature (Blois MS. 1958. Nature 181: 1199-1203.).

Experiment to confirm the foaming effect of the sample according to the foaming component and its content as shown in Table 3.

Foaming ingredient and its content Configuration designation Mixing ratio
(%) Unit weight
(mg) Remarks Usage Main ingredient Red ginseng, Ogapi, Schisandra, Angelica, wolfberry, casualty, Bokbunja, earth and sand, Cheongung, Cheonma, Healthy jujube 10.0 ~ 20.0 200 100% Functional raw materials Supplementary material Anhydrous citric acid 7.5-19.5 390 99.5% ↑ Organic acid D-sorbitol 4.0 80 glucose Sweetener (sugar alcohol) Tricalcium phosphate 1.0 20 90% ↑ Other stabilizers Magnesium stearate 1.5 30 100% Lubricant CMC-Ca 2.0 40 Carboxymethyl
Cellulose calcium Binder Mannitol 6.0 120 100% Sweetener (sugar alcohol) Calcium primary phosphate 1.0 20 100% Other stabilizers Lactose 30.0 600 Lactose 95%
(Milk / U.S.),
Dextrin 5% Binder Sodium hydrogencarbonate 10.0-30.0 500 100% blowing agent Sum 100 2,000

As a result of this experiment, the dissolution time was about 2 minutes, and in terms of the content of sodium hydrogen carbonate as an auxiliary material, 10% and 25% were dissolved almost the same regardless of the content of sodium hydrogen carbonate, and the extraction powder was 15%. (Working with extract powder) confirmed that the dissolution rate was considerably slow, and when jadeite was added, it was necessary to add it in liquid form.In addition, when the extract powder was added, the dissolution rate was slow but the volume of the foamed salt was 10 ~. It was confirmed that use within 25% is preferred (see Fig. 6).

Claims (20)

(1) A first mixture is obtained by mixing vitamins, herbal extracts or jadeite, organic acids and sugar alcohols, and the second mixture is mixed with one or more components selected from amino acids, flavors, salts, food additives, and sweeteners. Obtaining a first step; (2) a second step of mixing the first mixture and the second mixture followed by adding a stabilizer to the mixture; (3) a third step of adding and mixing the binder and the blowing agent to the mixture to which the stabilizer of the second step is added; (4) a fourth step of adding and mixing a lubricant, a disintegrant, a colorant, and a preservative, respectively, to the mixture of the third step; (5) A method for producing effervescent tablets containing jadeite or goat ginseng extract comprising a fifth step of tableting the mixture of the fourth step The method of claim 1,
(1) 2 to 14% by weight of vitamins, 1 to 18% by weight of herbal extract or jadeite, 1 to 14% by weight of organic acid, and 1 to 12% by weight of sugar alcohol to obtain a first mixture, and 0.5 to amino acids of the first mixture. A first step of mixing a 2 wt%, 6-10 wt% fragrance, 0.2-0.6 wt% salt, 1-2 wt% food additive, and 1-2 wt% sweetener to obtain a second mixture; (2) a second step of mixing the first mixture and the second mixture followed by adding 1 to 12% by weight of a stabilizer to the mixture; (3) a third step of adding and mixing 20 to 40% by weight of the binder and 4 to 56% by weight of the blowing agent to the mixture to which the stabilizer of step (2) is added; (4) the amount of the lubricant 1 to 12% by weight in the mixture of step (3); And a fourth step of adding and mixing about 30 to 90% by weight of the disintegrant, the colorant, and the preservative together; Method for producing effervescent tablet containing jadeite or goat ginseng extract comprising the fifth step of the step of tableting the mixture of the fourth step. The method of claim 1,
In the first step of the manufacturing method, the vitamin is vitamin C, or any one or more vitamins selected from vitamin B1, vitamin B2, vitamin B6, vitamin B12, nicotinic acid amide, pantothenic acid, biotin, folic acid. The method of claim 1,
In the first step of the manufacturing method, the organic acid is selected from citric acid, maleic acid, lactic acid, lactic acid, tartaric acid, succinic acid, or fumaric acid. Method for producing any one or more. The method of claim 1,
In the first step of the manufacturing method, the herbal medicine is goat ginseng, red ginseng, ogapi, Schisandra chinensis, Angelica, Gugija, casualty, Bokbunja, Tosa, Cheongung, Cheonma, Health, or jujube. The method of claim 1,
In the first step of the production method, the jadeite is 1 to 6% by weight of ginseng, 3 to 15% by weight of sewage, 20 to 40% by weight of raw sulfur, 2 to 10% by weight of Fuling, 10 to 20% by weight of earthworm, 1 to 1 6 wt%, brown root 1-10 wt% and honey 10-30 wt%. The method of claim 1,
As the first mixture in the first step of the manufacturing method, the sugar alcohol is mannitol, sorbitol, maltito xylitol, erythritol, lactitol, glycitol (Glicitol), ribitol (Ribitol), galactitol (galactitol) is any one or more of the production method characterized in that the sugar alcohol. The method of claim 1,
As a second mixture in the first step of the preparation method, the amino acid is taurine, aspartic acid, threonine, serine, glutamic acid, proline, or proline. ), Glycine, Alanine, Cysteine, Valine, Methionine, Isoleucine, Tyrosine, Phenylalanine, Tryptophane, Lysine (Lysine) ), Histidine (Histidine), arginine (Arginine) any one or more selected from the manufacturing method. The method of claim 1,
As a second mixture in the first step of the manufacturing method, the flavor is pineapple flavor, apple flavor, orange flavor, lemon flavor, grape flavor, cherry flavor, peach flavor, apricot flavor, strawberry flavor, mango flavor, lime flavor, melon flavor, Method of producing at least one selected from plum flavor, mulberry flavor, bokbunja flavor, ginseng flavor, red ginseng flavor, jujube flavor, ginger flavor, citron flavor. The method of claim 1,
In the first step of the preparation method, the salt is the second mixture, wherein the salt is any one or more selected from potassium chloride (Potassium Chloride, KCl) and sodium chloride (NaCl). The method of claim 1,
The food additive as a second mixture in the first step of the manufacturing method is sodium gluconate (Sodium Gluconate, C 6 H 11 O 7 Na) characterized in that the manufacturing method. The method of claim 1,
The sweetener as a second mixture in the first step of the production method is any one or more selected from aspartame, sugar, saccharin, acesulfame potassium, stevioside, glucose, fructose, sugar. The method of claim 1,
In the second step of the preparation method, the stabilizer is any one or more selected from calcium triphosphate, calcium phosphate monobasic, sodium tartrate (Sodium Tartrate), sodium fumarate (Mono Sodium Fumarate), DL malic acid. The method of claim 1,
In the third step of the preparation method, the binder is lactose, CMC-Ca, water, an organic solvent, polyvinylpyrrolidone, hydroxypropyl cellulose, microcrystalline cellulose, hydroxypropylmethyl cellulose, dextrin, gelatin, methyl cellulose, and hydride. At least one selected from hydroxycellulose, hydroxymethyl cellulose, polyvinyl alcohol, pre-gelatinized starch, or gum arabic. The method of claim 1,
In the third step of the production method, the blowing agent is characterized in that at least one selected from sodium bicarbonate, sodium bicarbonate (Sodium Bicarbonate, NaHCO ₃ ). The method of claim 1,
In the fourth step of the production method, the glidant is characterized in that at least one mixture consisting of magnesium stearate (Mg Stearate), talc, stearic acid or light silicic anhydride (SiO ₂ ). The method of claim 1,
In the fourth step of the preparation method, the disintegrant is starch glycolate sodium, crospovidone, cross-linked sodium carboxymethyl cellulose, low-substituted hydroxypropylcellulose. ), Hydroxypropyl methyl cellulose, polyvinylpyrrolidone, starch, carboxymethyl cellulose calcium, and a combination thereof. The method of claim 1,
In the fourth step of the manufacturing method, the coloring agent is at least one selected from titanium dioxide, iron oxide, magnesium carbonate, calcium sulfate, magnesium oxide, magnesium hydroxide or aluminum lake (aluminium lake). The method of claim 1,
In the fourth step of the production method, the preservative is characterized in that at least one selected from benzoic acid, methyl paraben, ethyl paraben or propyl paraben. Effervescent tablet preparation excellent in antioxidant activity and anticancer activity prepared by the method of claim 1.

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