KR20190138456A - Pharmaceutical composition comprising Astragali radix derivatives and Lithospermi radix derivatives for anti-diabetes - Google Patents

Abstract

The present invention relates to an anti-diabetic pharmaceutical composition, and more particularly, to an anti-diabetic pharmaceutical composition that can effectively reduce blood sugar levels and has less side effects. The anti-diabetic pharmaceutical composition of the present invention has an excellent inhibitory effect on the increase in blood glucose levels according to diabetes, thereby being able to be widely used in the anti-diabetic pharmaceutical composition and anti-diabetic health functional food.

Description

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

The present invention relates to a pharmaceutical composition for antidiabetic, and more particularly, to an antidiabetic pharmaceutical composition that can effectively reduce blood sugar levels and has fewer side effects.

Recently, the prevalence of chronic diseases such as diabetes, hypertension, and immune diseases such as inflammatory diseases has increased significantly due to aging, increased social stress, and rapid changes in dietary culture.

In particular, diabetes mellitus is classified as a metabolic syndrome along with obesity and hyperlipidemia.It is caused by the lack of insulin secreted by the pancreas or abnormal function, which leads to an increase in blood sugar levels and nutrient use, and that blood sugar is excreted in urine or blood. It is a disease that is converted into heavy cholesterol or triglycerides. If you have diabetes, you may not be able to make as much insulin as your body needs or the insulin produced may not work properly on your cells, resulting in high blood sugar levels and the excretion of excess sugar in your urine, resulting in loss of energy and fatigue. Will cause.

In Korea, about 5% of adults are known to have diabetes, and if not treated properly, complications such as diabetic retinopathy, diabetic nephropathy, vascular disorders, neurological disorders and atherosclerosis complications occur. It is a serious disease that accounts for the third cause.

Inflammatory reactions are involved in the metabolic syndrome, including diabetes. In other words, if the inflammatory stimulus occurring in the body becomes chronic, metabolic diseases are caused. Therefore, metabolic diseases such as diabetes are effective for preventing and enhancing the improvement of the diabetic symptoms and suppressing the inflammatory response.

Drugs for the purpose of treating diabetes have already been developed, insulin-dependent diabetes mellitus [type 1 diabetes mellitus; a kind of autoimmune disease; insulin preparations are effective for insulin-dependent diabetes mellitus (IDDM), and insulin-dependent diabetes mellitus (type 2 diabetes mellitus; Non-insulin-dependent diabetes mellitus (NIDDM)] includes sulphonylurease (tolbutamide, chloropropamide, glibenclamide, etc.) and biguanides (metofrmin). It is essential to use a combination, and to prevent the worsening of diabetes, careful attention is always required in daily life such as diet control and weight management.

Therefore, it is necessary to develop a functional food that has an effective action in preventing and treating by naturally ingesting it in the same way as a regular meal.

However, side effects such as drugs and foods used for conventional diabetes have insufficient sustained effects and cause kidney toxicity and hepatotoxicity in the body. Therefore, it was required to develop a product that can reduce the side effects and at the same time find a natural product in the form of a food having a good pharmacological effect to be used for preventing diabetes.

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 effects 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 antidiabetic effects of the combination of Astragalus and Chichi extracts have been reported, and the present inventors can overcome the limitations of drugs developed for treating diabetes, effectively reduce blood sugar levels, and have side effects. As a result of conducting research to develop new drugs, the present invention was completed by confirming that the complex of Astragalus extract and Chichi extract has excellent antidiabetic effect.

Republic of Korea Patent Publication No. 10-2006-0121576

An object of the present invention is to provide an antidiabetic pharmaceutical composition that can effectively reduce blood sugar levels and has fewer side effects.

In addition, the present invention has another object to provide an anti-diabetic health functional food with an excellent inhibitory effect on increasing blood sugar levels.

In order to solve the above problems of the present invention, the present invention provides a pharmaceutical composition for antidiabetic, comprising Astragali radix extract and Lithospermi radix extract 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 30 ~ 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: l.

The present invention also provides an anti-diabetic health functional food comprising Astragali radix extract and Lithospermi radix extract as active ingredients.

The antidiabetic pharmaceutical composition of the present invention can be widely used in the antidiabetic pharmaceutical composition and the anti-diabetic health functional food with an excellent inhibitory effect on the increase in blood glucose levels according to diabetes.

Figure 1a is a graph showing the weight change over time of each experimental group.
Figure 1b is a graph showing the dietary intake of each experimental group.
2 is a graph showing blood glucose values with time of each experimental group.
Figure 3 is a graph showing the pancreas weight measurement results of each experimental group.
Figure 4a is a graph showing the liver weight of each experimental group.
Figure 4b is a graph showing the spleen weight of each experimental group.
Figure 4c is a graph showing the lung weight of each experimental group.
Figure 4d is a graph showing the kidney weight of each experimental group.

The present invention sought to solve the above problems by providing an antidiabetic pharmaceutical composition comprising 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-diabetic effect by effectively suppressing the increase in blood sugar level 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 antidiabetic 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 30 ° C. to 90 ° C., and the extract of Astragalus and Jachi extract in the above temperature range may further increase the content of the active ingredient exhibiting an antidiabetic effect.

Astragalus extract and branch extract extracted by the above-described embodiment is better in the anti-diabetic effect compared to the case where the astragalus extract or the support extract is used alone as 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-diabetic health functional food comprising Astragali radix extract and Lithospermi radix extract as active ingredients.

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-diabetic 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

Dibasic calcium phosphate 55 mg

Potassium Citrate 90 mg

Calcium Carbonate 100 mg

Magnesium chloride 24.8 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 experimental group was divided into a normal group, an alloxan treatment group, an astragalus complex administration group in which the AOL complex was administered to the astragalus complex, and a guava leaf extract administration group in which the guava leaf extract was administered to the alloxan treatment group.

In order to observe the anti-diabetic effect, the oxalic complex and guava leaf extract were administered orally once a day at a concentration of 1 mg / mouse and 3 mg / mouse, respectively.

Referring to FIG. 1A, it can be seen that the body weight of the alloxan treated group was significantly reduced 9 days after the induction of diabetes compared to the normal group.

The 1 mg / mouse concentration of Astragalus complexes showed better weight loss inhibition effect than the 3 mg / mouse concentration of Astragalus complexes, which was similar to that of the Guava leaf extract group.

Diabetes is accompanied by a number of complications or accompanying symptoms, one of which is the increase in the amount of food. This phenomenon is caused by polyuria and abnormal glucose uptake, also observed in animals that induced diabetes.

Dietary intake was measured by fasting the mice for 12 hours, then fasting and feeding them for 4 hours.

Referring to Figure 1b, it can be seen that the dietary intake of the alloxan treated group significantly increased compared to the normal group, the decrease in dietary intake according to the concentration of the Astragalus complex administration group did not show a significant difference.

Experimental Example 2 Blood Sugar Level Measurement

Since the blood glucose level increases with the induction of diabetes, the blood glucose level of each experimental group was measured after the induction of diabetes, and the results are shown in FIG. 2.

Referring to FIG. 2, the normal group did not show a change in blood glucose level after diabetes induction, and the alloxan treated group showed a significant increase in blood glucose level over time after diabetes induction. 9 days after the induction of diabetic Astragalus complex administration group was confirmed that can reduce the blood sugar level to the level similar to the normal group, it can be confirmed that the effect of reducing blood glucose level than the group administered the guava leaf extract, a notification type raw material.

Experimental Example 3 Measurement of Pancreatic Weight Change

Since the weight is reduced by pancreatic injuries according to the induction of diabetes, the weight of the pancreas of each experimental group was measured 9 days after the induction of diabetes, and the results are shown in FIG. 3.

Referring to FIG. 3, it can be seen that the pancreatic weight of the alloxan treated group was significantly reduced compared to the normal group.

The 1 mg / mouse concentration of the Astragalus complex administration group was superior to the 3 mg / mouse concentration of the Astragalus complex administration group, and showed better inhibitory effect on the reduction of pancreatic weight, and was superior to the Guava leaf extract administration group.

Experimental Example 4 Toxicity Evaluation

The weight of four tissues (liver, spleen, lung and kidney) was measured 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. 4A to 4D. As a result of measuring the tissue weight of the group administered with the Astragalus complex, the Astragalus extract did not have a significant effect on the weight reduction, but the Astragalus complex administered group at 1 mg / mouse concentration had a smaller long-term weight loss than the Astragalus complex administered group at 3 mg / mouse concentration. You can see that.

Claims (5)

An antidiabetic pharmaceutical composition comprising Astragali radix extract and Lithospermi radix extract as active ingredients.
The method of claim 1,
The Astragalus extract and branch extract is antidiabetic 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 ℃ antidiabetic pharmaceutical composition.
The method of claim 1,
The Astragalus extract and branch extract is an antidiabetic pharmaceutical composition comprising a weight ratio of 5: 5 to 9: 1.
An anti-diabetic health functional food comprising Astragali radix extract and Lithospermi radix extract as active ingredients.

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