KR20190138455A - Pharmaceutical composition comprising Astragali radix derivatives and Lithospermi radix derivatives for anti-obesity - Google Patents

Abstract

The present invention relates to a pharmaceutical composition for anti-obesity, and more particularly, to a pharmaceutical composition for anti-obesity having an excellent inhibitory effect on weight gain and body fat increase due to obesity and having less side effects. The pharmaceutical composition for anti-obesity of the present invention has the excellent inhibitory effect on weight gain and body fat increase according to obesity, thereby being able to be widely used in the pharmaceutical composition for anti-obesity and health functional food for anti-obesity.

Description

Pharmaceutical composition comprising Astragali radix derivatives and Lithospermi radix derivatives for anti-obesity

The present invention relates to a pharmaceutical composition for anti-obesity, and more particularly, to the Astragalus complex with excellent side effects and an inhibitory effect on weight gain and body fat increase due to obesity.

Obesity is a form in which body fat is increased due to an imbalance between energy intake and consumption. It is a condition in which fat is accumulated in the body rather than an increase in body weight, and hypertension, hyperlipidemia, heart disease, diabetes, cancer, etc. It can cause serious health problems around the world. Therefore, in 1996, the World Health Organization (WHO) classified obesity as a 'disease' and recognized it as a risk factor for major chronic diseases. have.

This obesity population is increasing rapidly worldwide, and WHO announced that the global obesity population will increase to 1.5 billion by 2015 to 1.2 billion. In addition, according to published OECD (Organization for Economic Cooperation and Development ), a 31% obesity 3.2% of the country's population has more than BMI 30 kg / m ² of the US population.

As a result, the market for obesity drugs is growing rapidly, and the global market for obesity drugs is expected to grow by about 20% annually from 2014 to $ 200 billion in 2008.

However, at present, the biggest problem of obesity treatment is the drug preference, and it is a problem because it is abused even when the drug is not used or drug treatment is not required. In particular, psychotropic obesity treatments have to be restricted to use as an adjuvant therapy for obesity only for a few weeks, but there is a big problem in that they are not actively managed. In particular, as serious side effects such as blood pressure rise, respiratory increase, consciousness disorder, and hypothyroidism were reported by Sibutramine, an appetite suppressant that occupied half of the domestic anti-obesity drugs, it was discontinued in Korea after 2010 in Europe and the United States. Action was taken. Since the supply of pendimetrazine (phendimetrazine) component is increased, the supply of obesity drugs is maintained at the normal level, but the side effects of taking the drug still remains a big problem.

Weight control methods for the treatment of obesity, in addition to the drug treatment, there is a diet, exercise therapy, behavior modification therapy, etc., diet-related industries, such as weight control preparations, diet health functional food, health center, obesity clinic use It is formed throughout the field. In particular, the size of the domestic diet food market is about 150 to 200 billion won, growing 7 to 10% every year. Recently, as the serious side effects of anti-obesity drugs are known, the focus is on foods using natural products that are more accessible and less side effects than medicines. have. Conjugated linolenic acid (CLA) is a double-linked conjugated isomer of linoleic acid. Several experiments have been reported to reduce the number of adipocytes by increasing apoptosis of adipocytes, and the average weight loss of 2.5 kg and 15 to 20% of body fat after 3 months when a person consumes about 3 g daily Has been found in clinical trials. However, these weight loss effects are not consistent and have been reported to increase insulin resistance and cause fatty liver, so be careful to administer polylinoleic acid products to patients with increased insulin resistance, including those with type 2 diabetes. Is being requested.

No dietary supplement that is being used to treat obesity is more effective than the drugs currently being prescribed for the treatment of obesity. In addition, if the price of each product varies greatly and false advertisements on functionality cause confusion in product selection from the consumer's point of view and the therapeutic effect is considered, it is not so cheap. Foods that are claimed to have weight loss effects should be combined with regular exercise and dietary control of the intake of consumers to gain weight loss, but objectively effective because there is a high market for products that do not prove effective in the vague expectation of food efficacy. It is urgent to develop foods derived from natural products that can prove that.

Astragalus is a perennial herb belonging to the legume family, which grows in the northern and northern regions of Korea, and is widely cultivated for medicinal purposes. In oriental medicine, its root is mainly used as a medicinal herb. Hepatoprotective, immune-promoting, anticancer, and tonic Efficacy of diuretic effect, and antimicrobial activity, antioxidant activity, a large amount of polyphenols and physiological activity according to the content of isoflavonoid (Isoflavonoid) has been reported.

Lithospermum erythorihizon Shiebold et.Zuccarini is a perennial plant belonging to the Borraginaceae genus Lithospermum and is a representative plant containing roots of shikonin and its derivatives in the roots. It is a plant. Chichi has already been used in prescriptions for anti-inflammatory, detoxification and antipyretic purposes. It has bactericidal and anti-inflammatory properties and is used as ointment for swelling, burns, frostbite, eczema and hemorrhoids. .

However, to date, no anti-obesity effect of the combination of Astragalus and Chichi extracts has been reported, and the present inventors have overcome the limitations of drugs developed for the treatment of obesity, have high anti-obesity effects, and have little side effects. As a result of research to develop the drug, the present invention was completed by confirming that the complex of the Astragalus extract and the branch extract was excellent in anti-obesity effect.

Republic of Korea Patent No. 10-0878331

An object of the present invention is to provide an anti-obesity pharmaceutical composition having an excellent inhibitory effect on weight gain and body fat increase due to obesity and low side effects.

In addition, the present invention is another object to provide an anti-obesity health functional food having an excellent inhibitory effect on weight gain and body fat increase according to obesity.

In order to solve the above problems of the present invention, the present invention provides an anti-obesity pharmaceutical composition comprising an extract of Astragali radix and Lithospermi radix as an active ingredient.

According to one embodiment of the invention, the Astragalus extract and branch extract can be extracted with at least one solvent selected from water, C ₁ ~ C ₄ alcohol, ethyl acetate, chloroform and hexane.

In addition, according to an embodiment of the present invention, the temperature of the solvent may be 70 ~ 90 ℃.

In addition, according to an embodiment of the present invention, the Astragalus extract and branch extract may be included in a weight ratio of 5: 5 to 9: 1.

In another aspect, the present invention provides an anti-obesity health functional food comprising an Astragali radix extract and Lithospermi radix extract as an active ingredient.

The anti-obesity pharmaceutical composition of the present invention can be widely used in the anti-obesity pharmaceutical composition and anti-obesity health functional food because it has an excellent inhibitory effect on weight and body fat increase according to obesity.

Figure 1a is a graph showing the weight change over time of each experimental group.
Figure 1b is a graph showing the weight of each experimental group after 4 weeks.
Figure 2a is a graph showing the abdominal fat weight of each experimental group.
Figure 2b is a graph showing the weight of the epididymal fat of each experimental group.
Figure 3a is a graph showing the liver weight of each experimental group.
Figure 3b is a graph showing the spleen weight of each experimental group.
Figure 3c is a graph showing the lung weight of each experimental group.
3D is a graph showing the kidney weight of each experimental group.

The present invention sought to solve the above-mentioned problems by providing an anti-obesity pharmaceutical composition comprising an Astragali radix extract and Lithospermi radix extract as an active ingredient. Through this, it can be used as a pharmaceutical composition or health functional food with excellent anti-obesity effect by effectively reducing the side effects and increasing weight and body fat when applied in vivo.

The term “pharmaceutical composition” refers to a mixture of other chemical components such as diluents or carriers in a mixture of the Astragalus extract and the branch extract of the present invention.

The term “carrier” is defined as a compound that facilitates the addition of a compound into a cell or tissue. For example, dimethyl sulfoxide (DMSO) is a commonly used carrier that facilitates the incorporation of many organic compounds into cells or tissues of an organism.

The term “diluent” is defined as a compound that not only stabilizes the biologically active form of the compound of interest, but also is diluted in water to dissolve the compound. Salts dissolved in buffer solutions are used as diluents in the art. A commonly used buffer solution is phosphate buffered saline, because it mimics the salt state of human solutions. Because buffer salts can control the pH of a solution at low concentrations, buffer diluents rarely modify the biological activity of a compound.

Unless otherwise defined, all technical terms used in the present invention are used in the meaning as commonly understood by those skilled in the art in the related field of the present invention. Also described herein are preferred methods or samples, but similar or equivalent ones are within the scope of the present invention.

Hereinafter, exemplary embodiments of the present invention will be described in detail with reference to the accompanying drawings so that those skilled in the art may easily implement the present invention. As those skilled in the art would realize, the described embodiments may be modified in various different ways, all without departing from the spirit or scope of the present invention.

The present invention provides an anti-obesity pharmaceutical composition comprising Astragali radix extract and Lithospermi radix extract as active ingredients.

The Astragalus extract may be extracted by applying a method used for extraction of Astragalus known in the art, for example, may be a solvent extraction method, but is not limited thereto. In addition, the Astragalus extract may be prepared as a purified fraction by further performing an additional fractionation process using column chromatography.

The Astragalus to be extracted can be used by purchasing a commercially available, it is preferable to use after removing the foreign matter such as soil before performing the extraction process.

The branch extract may be extracted by applying a method used for extraction of branches known in the art, for example, may be a solvent extraction method, but is not limited thereto. In addition, the branch extract may be prepared as a purified fraction by further performing an additional fractionation process using column chromatography.

The subject matter to be extracted can be purchased and used commercially available, it is preferable to use after removing the foreign matter such as soil before performing the extraction process.

When extracting the above-mentioned Astragalus and branching by the solvent extraction method, the solvent used may be extracted with a solvent alone or in a mixed form such as water, lower alcohols of C1 to C4, ethyl acetate, chloroform or hexane, more preferably. Preferably an alcohol of C ₁ to C ₄ , even more preferably ethanol.

In addition, the solvent may have a temperature of 70 to 90 ° C., and the Astragalus extract and the branch extract extracted in the temperature range may further increase the content of the active ingredient exerting a hepatocyte protective effect.

Astragalus extract and chichi extract extracted by the above-described embodiment is excellent in anti-obesity effect compared to the case where the astragalus extract or support extract is used alone as the mixture is used, the expression of a more elevated effect on the effect In one preferred embodiment of the present invention, for the extract and the extract may be included in a weight ratio of 5: 5 to 9: 1.

The pharmaceutical compositions according to 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 sterile injectable solutions, respectively, according to conventional methods. Can be used.

The pharmaceutical compositions of the present invention may be prepared in unit dosage form by formulating with a pharmaceutically acceptable carrier and / or excipient according to methods which can be easily carried out by those skilled in the art. Or may be prepared by incorporation into a multi-dose container.

Pharmaceutically acceptable carriers included in the pharmaceutical compositions of the present invention are those commonly used in the preparation, such as lactose, dextrose, sucrose, sorbitol, mannitol, starch, acacia rubber, calcium phosphate, alginate, gelatin, Calcium silicate, microcrystalline cellulose, polyvinylpyrrolidone, cellulose, water, syrup, methylcellulose, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, mineral oil, and the like, It is not limited to this.

In addition to the above components, the pharmaceutical composition of the present invention may further include a lubricant, a humectant, a sweetener, a flavoring agent, an emulsifier, a suspending agent, a preservative, and the like. Suitable pharmaceutically acceptable carriers and formulations are described in detail in Remington's Pharmaceutical Sciences (19th ed., 1995).

The pharmaceutical composition of the present invention may be administered orally or parenterally, and in the case of parenteral administration, intravenous injection, subcutaneous injection, intramuscular injection, intraperitoneal injection, endothelial administration, topical administration, intranasal administration, pulmonary administration and rectal administration Or the like. When orally administered, the protein or peptide is digested so that the oral composition should be formulated to coat the active agent or protect it from degradation in the stomach. The pharmaceutical composition may also be administered by any device in which the active agent may migrate to the target cell.

Suitable dosages of the pharmaceutical compositions of the present invention vary depending on factors such as the formulation method, mode of administration, age, weight, sex, morbidity, food, time of administration, route of administration, rate of excretion and response to response of the patient, Usually a skilled practitioner can easily determine and prescribe a dosage effective for the desired treatment or prophylaxis.

The pharmaceutical compositions of the present invention may be administered as individual prophylactic or therapeutic agents or in combination with other therapeutic agents and may be administered sequentially or simultaneously with conventional therapeutic agents.

In addition, the present invention also provides an anti-obesity health functional food comprising Astragali radix extract and Lithospermi radix extract as an active ingredient.

The type of health functional food composition is not particularly limited as long as it is usually manufactured and / or sold. For example, dairy products including meat, sausages, bread, chocolate, candy, snacks, confectionery, pizza, ramen, other noodles, gums, ice cream, various soups, drinks, tea, drinks, alcoholic beverages and vitamin complexes. It can be used in the form of pills, powders, granules, acupuncture, tablets, capsules or beverages and includes all of the health functional foods in the conventional sense.

The health beverage composition of the present invention is not particularly limited to the liquid component except for containing the Astragalus extract and the branch extract, and may contain various flavors or natural carbohydrates, etc. as additional ingredients, as in general beverages.

Typically, the amounts of the Astragalus extract and branch extract in the health functional food may be included in 0.1 to 50% by weight, preferably 1 to 40% by weight of the total food weight. In addition, in the case of long-term intake for the purpose of health and hygiene or for the purpose of health control may be below the above range, since there is no problem in terms of safety, the active ingredient may be used in an amount above the above range.

Hereinafter, an example of manufacturing an anti-obesity health functional food of the present invention will be described, but the present invention is not intended to be limited thereto but is intended to be described in detail.

<Manufacture example 1>

Astragalus Extract 140 mg

Chichi Extract 60mg

70 μg of Vitamin A Acetate

Vitamin E 1.0 mg

Vitamin B 1 0.13 mg

Vitamin B 2 0.15 mg

Vitamin B 6 0.5 mg

0.2 μg of vitamin B 12

Vitamin C 10 mg

Biotin 10 ㎍

Nicotinic Acid 1.7 mg

Folate 50 ㎍

Calcium Pantothenate 0.5mg

Ferrous Sulfate 1.75 mg

Zinc Oxide 0.82 mg

Magnesium carbonate 25.3 mg

Potassium monophosphate 15 mg

Hereinafter, the present invention will be described in more detail with reference to the following examples. However, these drawings and the following embodiments are merely examples for easily explaining the contents and scope of the technical idea of the present invention, and thus the technical scope of the present invention is not limited or changed. In addition, various modifications and changes can be easily determined by those skilled in the art based on the examples.

(Example 1)

1-1. Preparation of Astragalus Extract

Chichisan 1 year root (Jecheon-san) sample was purchased from the Korea Herbal Medicine Association, and then pulverized with a powder, and then added to 50% ethanol of 15 times the weight of the dry sample and the dry sample and refluxed at 80 ℃ for 4 hours. Reflux extraction was repeated two times under the same conditions, followed by filtration and concentration to produce the Astragalus extract.

1-2. Preparation of Fermented Extract

Chichisan 1 year root (Jecheon-san) sample was purchased from the Korea Herbal Medicine Association and then coarsely pulverized, and then added to the dry sample and 70% ethanol of 15 times the weight of the dry sample and refluxed at 80 ℃ for 4 hours. Reflux extraction was repeated two times under the same conditions, followed by filtration and concentration to prepare branch extract.

1-3. Mix of Astragalus Extract and Branch Extract

The Astragalus extract and the branch extract were mixed at a weight ratio of 7: 3 and concentrated to prepare a Astragalus complex.

(Comparative Example 1)

Guava leaf extract used as a control in the present invention was purchased from Natural F & P Co., Ltd. as a functional ingredient approved by the KFDA.

Experimental Example 1 Weight Change Measurement

The whole experimental group was treated with normal diet fed mice (Normal), high fat diet fed high fat diet (HFD), high fat diet administered Astragalus complex, high fat diet group guava leaf extract Was classified into the group administered.

In order to observe the anti-obesity effect, the high fat diet group was orally administered with 3 mg / mouse of Astragalus complex and guava leaf extract (p.o).

Referring to Figure 1a, it can be seen that the weight gain of the high fat diet group significantly increased compared to the normal group.

In addition, the high fat diet group, the group administered with Astragalus complex or guava leaf extract has an effect of inhibiting weight gain, in particular, the group administered with Astragalus complex can be confirmed that the weight gain inhibitory effect is more excellent.

In addition, as shown in Figure 1b, compared to the weight gained to the last day (4 weeks), the group administered with the Astragalus complex was confirmed to exhibit a level of weight almost similar to the normal group, guava leaf material It can be seen that the weight increase inhibitory effect is superior to the extract administration group.

Experimental Example 2 Measurement of Abdominal Fat and Epididymal Fat Weight

Obesity and epididymal fat weights were checked by using the fact that body fat weight increases with weight gain during obesity induction according to the high fat diet.

2A and 2B are graphs showing the abdominal fat and epididymal fat weight of the experimental groups, respectively. Referring to Figure 2a and Figure 2b, it can be seen that the Astragalus complex administration group is superior to the abdominal fat and epididymal fat production inhibitory effect than the guava leaf extract administration group is a notification type raw material.

Experimental Example 3 Toxicity Evaluation

The weight of four tissues (liver, spleen, lung and kidney) was measured in order to confirm the organ toxicity by administration of the Astragalus complex and high fat diet, and the results of the gravimetric measurement are shown in FIGS. 3A to 3D. As a result of measuring the tissue weight of the group administered the Astragalus complex, it can be seen that Astragalus extract does not have a significant effect on the weight reduction.

Claims (5)

A pharmaceutical composition for anti-obesity comprising Astragali radix extract and Lithospermi radix extract as active ingredients.
The method of claim 1,
The Astragalus extract and branch extract is an anti-obesity pharmaceutical composition extracted with at least one solvent selected from water, C ₁ ~ C ₄ alcohol, ethyl acetate, chloroform and hexane.
The method of claim 2,
The temperature of the solvent is 30 ~ 90 ℃ anti-obesity pharmaceutical composition.
The method of claim 1,
The Astragalus extract and branch extract is an anti-obesity pharmaceutical composition comprising a weight ratio of 5: 5 to 9: 1.
Anti-obesity health functional food containing Astragali radix extract and Lithospermi radix extract as active ingredients.

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