WO2010128788A2 - Anti-obesity external dermal agent compositions containing capsaicin or capsaicin-like compounds as active ingredients - Google Patents

Abstract

The present invention relates to novel anti-obesity external dermal agent compositions, and more particularly, to anti-obesity external dermal agent compositions containing capsaicin or capsaicin-like compounds as active ingredients. The anti-obesity external dermal agent compositions containing capsaicin or capsaicin-like compounds according to the present invention stimulate the metabolism of the body to decompose the fat cells of subcutaneous fat, and inhibit body fat accumulation to reduce hypertrophy of fatty tissues, thus eventually reducing weight and efficiently preventing and improving obesity. In addition, the anti-obesity external dermal agent compositions containing capsaicin or capsaicin-like compounds according to the present invention exhibit excellent anti-obesity effects when simply applied to the skin, which enables convenient use and can be used in pharmaceutical compositions and cosmetic compositions which can be directly applied to the skin.

Description

Anti-obesity external composition for skin containing capsaicin or capsaicin-like compound as an active ingredient

The present invention relates to a novel anti-obesity skin external preparation composition.

There are about 20 billion fat cells in the human body, and these fat cells are responsible for accumulating or releasing energy in mammals. Thus, there is a complex control principle for the accumulation and release of energy within cells, where if the supply is much greater than the demand for energy, fat is stored as triglycerides in the cell and then back to free fatty acids and glucose when energy is depleted. Decomposed and used.

On the other hand, obesity occurs when excessive energy accumulates due to an imbalance of energy metabolic processes in vivo, and is believed to be caused by an increase in the size of fat cells or an increase in the number thereof. It is a major factor causing various diseases, and is not preferable for health, and is not preferable for appearance.

However, in recent years, dietary changes due to overnutrition and imbalance have increased the intake of high-calorie fatty acids, which leads to obesity, leading to the incidence of various diseases such as cardiovascular disease, cancer, diabetes, dementia Is rising significantly. Therefore, the problem of reducing subcutaneous fat or inhibiting fat accumulation has become a socially important task regardless of age.

In addition, women's interest in the beautiful body is also rapidly increasing according to women's social status improvement, economic independence and the desire for quality of life, and thus slimming and anti-effectiveness effective in removing excess subcutaneous fat and promoting skin elasticity. Interest in cellulite (anti-celullite) products continues to rise.

Therefore, as a countermeasure for obesity by increasing body fat, external stimulation methods such as diet restriction, exercise and massage have been attempted, and efforts to improve obesity by various methods such as ingesting anti-obesity foods and anti-obesity drugs Are being tried.

However, these prior arts have a problem that is accompanied by a yo-yo phenomenon due to the loss of muscle protein, not only the effect of reducing fat but also a problem such as vomiting and abdominal pain occurs. Therefore, it is urgent to develop an anti-obesity product of a new formulation having excellent effect of reducing body fat while not causing side effects due to ingestion of foods or drugs.

On the other hand, capsaicin (capsaicin) is a kind of alkaloid having a molecular formula of C ₁₈ H ₂₇ NO ₃ , is known as a pungent ingredient of red pepper, and is particularly known to be most contained in red pepper seeds. In the late 1940s, such capsaicin was found to be effective in alleviating analgesic. Since then, research has been actively conducted to develop new analgesics by synthesizing capsaicin derivatives. In addition, capsaicin stimulates the body's metabolic function, exerts energy to diffuse and diffuse, such as sweating in the human body, and this diffusion action promotes secretion of gastric juice, relieves anorexia, and promotes blood circulation. It has been shown to play a role in eliminating depressed and stagnant mood (Korean Journal of Nutrition, 1999, July). Recently, capsaicin has been reported to act on fat cells in the body to promote lipolysis.

Therefore, many people have an interest in capsaicin due to various effects of capsaicin, and various health foods and diet products using the same have been developed. However, the development of external preparations containing capsaicin that can be applied directly to the skin as a use for suppressing or improving obesity has not been attempted yet.

Accordingly, the present inventors developed a new anti-obesity skin external preparation that can be directly applied to the skin, and when applying the skin external preparation containing capsaicin or a similar compound of capsaicin as an active ingredient to the skin, triglycerides were applied to the skin. The present invention is confirmed by not only having an excellent effect of degrading but also reducing the accumulation of fat in the abdomen or intestine, thereby reducing the enlargement of adipose tissue and ultimately reducing the weight to effectively prevent and improve obesity. Completed.

Accordingly, it is an object of the present invention to provide an anti-obesity external skin composition comprising a capsaicin, a capsaicin-like compound or a salt thereof as an active ingredient.

In addition, another object of the present invention is to provide a skin cosmetic for weight loss comprising the anti-obesity skin external preparation composition of the present invention.

In order to achieve the object of the present invention as described above, the present invention is capsaicin (capsaicin); Among the group consisting of dihydrocapsaicin, nordihydrocapsaicin, nordiamide, nonivamide, capsiate, dihydrocapsiate and nordihydrocapsiate Capsaicin like compounds selected; Or it provides an anti-obesity external composition for skin comprising a salt thereof as an active ingredient.

In one embodiment of the present invention, the capsaicin or capsaicin-like compound may be included in an amount of 0.001 to 0.5% by weight based on the total weight of the anti-obesity skin external preparation composition.

In one embodiment of the present invention, the capsaicin or capsaicin-like compound may be included in an amount of 0.01 to 0.10% by weight relative to the total weight of the anti-obesity skin external preparation composition.

In one embodiment of the present invention, the external composition for skin may be a formulation selected from the group consisting of ointment, gel, liquid, cream, patch and paste.

In one embodiment of the present invention, the external preparation composition for skin may be a pharmaceutical composition for reducing body weight by promoting lipolysis and inhibiting body fat accumulation.

The present invention also provides a skin cosmetic for weight loss comprising an anti-obesity external skin composition containing a capsaicin, a capsaicin-like compound or a salt thereof as an active ingredient.

The anti-obesity skin external preparation composition containing capsaicin or a similar compound of capsaicin according to the present invention has the effect of promoting the metabolic function of the body to decompose subcutaneous fat of fat cells, inhibiting the accumulation of fat in the body, It is effective in reducing hypertrophy, and ultimately, it is effective in effectively preventing and improving obesity by reducing weight. In addition, the anti-obesity skin external preparation composition containing a capsaicin or a capsaicin-like compound according to the present invention has an excellent anti-obesity effect even if only applied to the skin, so that it is very easy to use and can be directly applied to the skin. There is an effect that can be used in the composition and the cosmetic composition.

1 is a skin external preparation composition containing capsaicin of the present invention and a skin external preparation composition without capsaicin (petrolatum) for each mouse group fed normal fat diet and high fat diet, respectively, every 24 hours in the abdomen of mice After application, the weight of each group of mice according to breeding time is measured and shown in a graph.

Figure 2 is applied to the abdomen of the mouse every 24 hours the skin external composition of the present invention containing 0.1% and 0.3% by weight of capsaicin for the group of mice fed normal and high fat diet respectively Next, after 5 weeks, the mesenteric adipose tissue, testicular adipose tissue, perirenal adipose tissue and liver adipose tissue were extracted from the group of each mouse, and then the weight of each adipose tissue was measured.

Figure 3 in one embodiment of the present invention was applied to the abdomen of mice fed high-fat diet ointment containing capsaicin by concentration (0.01%, 0.05% and 0.075%), and then measured the weight by time It is a graph comparing the results.

Figure 4 in one embodiment of the present invention after applying the ointment containing 0.075% capsaicin and the ointment containing 0.075% dehydrocapsaicin is applied to the abdomen of a mouse fed a high-fat diet, the weight is measured by time It is a graph comparing the results.

FIG. 5 is an ointment containing 0.075% capsaicin in one embodiment of the present invention, and petroleum jelly containing no capsaicin as a control was applied to the abdomen of a mouse fed with high fat diet, and then blood was collected from each mouse. After, a graph showing the comparison of the measured glucose content, total cholesterol content and triglyceride content in the blood, respectively.

The present invention is characterized by providing an anti-obesity external composition for skin containing capsaicin or a similar compound of capsaicin as an active ingredient.

Generally, capsaicin (capsaicin, trans-8-methyl-N-vanillyl-6-nonenamide) has been used as a food additive for a long time as a main ingredient of the pungent taste of red pepper (Suzuki, T. and Iwai, K., Academic Press) , New York , 227-299, 1994, Cordell, GA and Araujo, OE, Ann. Pharmacother ., 27: 330-336, 1993), and recently reported its efficacy as a non-narcotic analgesic. As it turns out that it is effective in dieting, it is processed and sold in various forms of food for diet food. However, there has not been yet been developed a composition capable of directly applying capsaicin to the skin as a purpose for inhibiting obesity.

On the other hand, in the present invention for the first time to prepare a topical skin composition containing a capsaicin or a similar compound of capsaicin as an active ingredient that can be applied directly to the skin as a purpose for inhibiting and preventing obesity.

In the present invention, the capsaicin-like compound may be a capsaicinoid compound and a capsinoid compound. Preferably, the capsaicinoid compound is not limited thereto, but dihydrocapsaicin and nordi It may be hydrocapsaicin (nordihydrocapsaicin), and the capsinoid compound, but is not limited to this, nonivamide, capsiate, dihydrocapsiate and nordihydrocap Nordihydrocapsiate.

In addition, the capsaicin or capsaicin-like compound which is an active ingredient included in the composition of the present invention may be used in the form of a salt, preferably a pharmaceutically acceptable salt.

As the salt, an acid addition salt formed by a pharmaceutically acceptable free acid is preferable, and an organic acid and an inorganic acid may be used as the free acid. The organic acid is not limited thereto, citric acid, acetic acid, lactic acid, tartaric acid, maleic acid, fumaric acid, formic acid, propionic acid, oxalic acid, trifluoroacetic acid, benzoic acid, gluconic acid, metasulfonic acid, glycolic acid, succinic acid, 4-toluenesulfonic acid, Glutamic acid and aspartic acid. In addition, the inorganic acid may include, but is not limited to, hydrochloric acid, bromic acid, sulfuric acid, and phosphoric acid.

In addition, a capsaicin or capsaicin-like compound according to the present invention can be used that is isolated from nature or prepared by chemical synthesis methods known in the art.

When the capsaicin or capsaicin-like compound is separated from nature, a natural material containing capsaicin or a similar compound thereof can be obtained by using a material extraction method and a separation method known in the art, and preferably, red pepper is prepared in an appropriate solvent. Extraction and the desired extract can be purified using purification methods known to those skilled in the art.

Suitable solvents for the extraction may be water or an organic solvent, preferably purified water, methanol (methanol), ethanol (ethanol), propanol (isopropanol), butanol (butanol), acetone (acetone) ), Or a mixture of various solvents such as ether, benzene, chloroform, ethyl acetate, methylene chloride, hexane, and cyclohexane Can be used.

In addition, the method of separating and purifying the capsaicin or the analogous compound of the present invention from the extract containing the capsaicin or the analogous compound obtained by the above method is filled with various synthetic resins such as silica gel or activated alumina (alumina) Column chromatography and high performance liquid chromatography (HPLC) may be used alone or in combination. However, the extraction and separation and purification method of the active ingredient is not necessarily limited to the above method.

In addition, the capsaicin or capsaicin-like compound of the present invention may be used in the form of a purely isolated and purified compound, and may also be used in the form of an extract containing the same.

The preparation of an anti-obesity skin external preparation composition containing a capsaicin or a capsaicin-like compound according to the present invention can be obtained by capturing a capsaicin or a capsaicin-like compound obtained by the methods described above in a composition for external application of the skin. It may be prepared by adding 0.001 to 1.0% by weight, preferably 0.001 to 0.5% by weight, and more preferably 0.01 to 0.10% by weight based on the total weight of the composition.

In addition, the topical skin composition of the present invention may include any other ingredients used in the preparation of a conventional topical skin composition in addition to the capsaicin or capsaicin-like compound component as an active ingredient, and the ingredients are generally used in the field of dermatology. Can be added.

In one embodiment of the present invention, after dissolving the purified capsaicin powder in 100% ethanol, benzyl alcohol, cetyl alcohol, glyceryl steric acid, isopropyl myristate, PEG-40 steric acid, petroleum The antiobesity skin external preparation composition of the present invention containing the capsaicin component was prepared by mixing with an ointment composition for topical analgesics composed of petrolatum and sorbitol.

On the other hand, the anti-obesity skin external preparation composition containing a capsaicin or a capsaicin-like compound according to the present invention is excellent in promoting the reduction of systemic or local adipose tissue, thereby improving the effect of inhibiting obesity and increasing obesity constitution by increasing body fat The effect is excellent.

Furthermore, the anti-obesity external composition for skin of the present invention has an effect of preventing various diseases that may occur due to obesity through the effect of inhibiting obesity by increasing body fat.

In particular, the place where fat easily accumulates in the body is the abdomen, and the abdomen is composed of mesenteric fat existing between the subcutaneous fat and the intestinal cavity, and obesity with increased mesenteric fat is called abdominal obesity. However, such abdominal obesity causes various adult diseases such as diabetes, hyperlipidemia, hypertension, gout, and has been reported to promote atherosclerosis.

In addition, fatty liver refers to a state in which lipids, especially neutral fats, are excessively accumulated in the liver due to overnourishment or excessive intake of alcohols. Fatty liver of overnutrition caused by obesity is known to be caused by the increase of fatty acid mobilization from peripheral fatty tissue by excess calorie intake, promoted fatty acid synthesis and neutral fat synthesis in the liver.

On the other hand, the anti-obesity skin external preparation composition containing a capsaicin or capsaicin-like compound according to the present invention has an effect of reducing adipose tissue, such as mesenteric adipose tissue, liver adipose tissue, testicular adipose tissue and peri-renal adipose tissue. .

According to one embodiment of the present invention, the skin external preparation composition of the present invention containing the capsaicin prepared in the ointment formulation was applied to the abdomen of the mouse inducing obesity by ingesting a high fat diet, the skin does not contain capsaicin The increase in body weight was decreased compared to the control group coated with the external preparation composition (see FIG. 1), and the weights of the mesenteric adipose tissue, liver adipose tissue, testicular adipose tissue, and peri-dial adipose tissue were measured. Compared with the weight of the adipose tissue was reduced (see Figure 2).

In addition, according to another embodiment of the present invention, in order to investigate the anti-obesity effect of the concentration of capsaicin contained in the external preparation composition for skin of the present invention, the obese mouse ointment containing 0.01%, 0.05% and 0.075% capsaicin After applying to the abdomen, the weight was measured over time, and as a result, the weight loss effect due to the ointment according to the present invention was found to increase depending on the capsaicin concentration dependent (see FIG. 3), and further to the present invention In order to elucidate the anti-obesity effect of capsaicin according to the biochemical analysis, ointment containing capsaicin and petrolatum ointment without capsaicin as a control were applied to the abdomen of obese mice, and then blood was collected from the mice. , Blood glucose content, total cholesterol content and triglyceride content were measured.

As a result, in the group to which the ointment containing capsaicin of the present invention was applied, the blood concentrations of glucose, cholesterol and triglycerides, which are indicators of obesity, were significantly reduced compared to the control group (see FIG. 5).

Therefore, the present inventors have found that the application of the topical skin composition of the present invention containing capsaicin or a capsaicin-like compound to the skin can prevent and suppress obesity by reducing fat accumulation and weight loss in the body. .

In addition, according to another embodiment of the present invention, after applying an ointment containing a dihydrocapsaicin, a capsaicin-like compound to the obese mice with an ointment containing a capsaicin, respectively, the weight is measured by time, In the case of the ointment containing dihydrocapsaicin, it was found that the body weight was reduced compared to the control group (the group coated with the ointment containing no capsaicin or dihydrocapsaicin) as the ointment containing the capsaicin of the present invention (see FIG. 4). .

Therefore, the anti-obesity skin external preparation composition according to the present invention can not only use capsaicin as an active ingredient, but also similar compounds of capsaicin can be used as an active ingredient.

Therefore, the present invention provides an anti-obesity external composition for skin containing capsaicin or a capsaicin-like compound as an active ingredient, and the anti-obesity external composition for skin according to the present invention can be used as a pharmaceutical composition for the prevention and inhibition of obesity. The anti-obesity skin external preparation composition according to the present invention may include a pharmaceutically effective amount of capsaicin or capsaicin-like compound alone or may include one or more pharmaceutically acceptable carriers, excipients or diluents. The pharmaceutically effective amount in the above means an amount sufficient to prevent, ameliorate and treat obesity symptoms.

In addition, "pharmaceutically acceptable" as used herein refers to a composition that is physiologically acceptable and does not normally cause an allergic reaction, such as gastrointestinal disorders, dizziness, or the like when administered to a human. Examples of such carriers, excipients and diluents include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methyl cellulose, Polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. In addition, fillers, anti-coagulants, lubricants, wetting agents, fragrances, emulsifiers and preservatives may be further included.

In addition, the compositions of the present invention may be formulated using methods known in the art to provide rapid, sustained or delayed release of the active ingredient after administration to a mammal. The formulations may be in the form of powders, granules, tablets, emulsions, syrups, aerosols, soft or hard gelatin capsules and sterile powders.

The anti-obesity skin external preparation composition according to the present invention may be administered through various routes including transdermal, subcutaneous and muscle, preferably by topical administration by transdermal administration, more preferably by application.

The dosage of the active ingredient may be appropriately selected depending on several factors such as the route of administration, the age, sex, weight of the patient, and the severity of the patient. In addition, the anti-obesity skin external preparation composition of the present invention can be administered in parallel with a known compound having the effect of preventing, improving or treating obesity symptoms.

The dosage of the anti-obesity skin external preparation composition containing a capsaicin or capsaicin-like compound according to the present invention is administered once to several times a day in an amount of 0.1 to 10.0 ml, preferably 0.5 to 5.0 ml per day, on an adult basis. can do. However, the pharmaceutically effective amount may be appropriately changed depending on the degree of obesity symptoms, the age, weight, health condition, sex, route of administration and duration of treatment of the patient.

On the other hand, most women tend to crave slim and solid bodies in appearance. However, excessive intake and lack of exercise due to dietary changes resulted in overweight, and the appearance of excess body fat often caused the appearance of obesity, and the accumulation of visceral fat in the abdominal cavity frequently occurs not only in obese people but also in normal weight people. Doing.

Therefore, if a substance capable of inhibiting the accumulation of body fat is used in the manufacture of cosmetics that apply directly to the skin, obesity can be prevented and suppressed in an easier and more effective way for both normal and normal people. It can also be solved.

The anti-obesity skin external preparation composition containing the capsaicin or capsaicin-like compound according to the present invention as an active ingredient can be used as a cosmetic composition for the prevention and inhibition of obesity.

When the anti-obesity skin external preparation composition of the present invention is used as a cosmetic composition, the components included in the composition may include components commonly used in cosmetic compositions in addition to capsaicin or capsaicin-like compound as an active ingredient, such as antioxidants, stable Conventional adjuvants and carriers such as agents, solubilizers, vitamins, pigments and flavorings. In addition, the cosmetic composition may further include a skin absorption promoting substance to enhance the effect.

The cosmetic composition of the present invention may be prepared in any formulation as long as it is a formulation of the external preparation composition for skin externally prepared in the art, for example, a solution, a suspension, an emulsion, a paste, a gel, a cream, a lotion, a powder, a soap. , Surfactant-containing cleansing, oils, powder foundations, emulsion foundations, wax foundations, sprays, and the like, but is not limited thereto. More specifically, it may be prepared in the form of a flexible lotion, nutrition lotion, nutrition cream, massage cream, essence, eye cream, cleansing cream, cleansing foam, cleansing water, pack, spray or powder.

When the formulation of the external preparation composition for skin according to the present invention is a paste, cream or gel, the carrier component is animal oil, vegetable oil, wax, paraffin, starch, tracant, cellulose derivative, polyethylene glycol, silicone, bentonite, silica, talc or oxidation Zinc and the like may be used, and when the formulation of the present invention is a powder or a spray, lactose, talc, silica, aluminum hydroxide, calcium silicate or polyamide powder may be used as the carrier component, particularly in the case of a spray It may additionally include propellants such as chlorofluorohydrocarbons, propane / butane or dimethyl ether.

In addition, when the formulation of the external preparation composition for skin of the present invention is a solution or an emulsion, a solvent, a solubilizer or an emulsifier may be used as a carrier component, for example, water, ethanol, isopropanol, ethyl carbonate, ethyl acetate, benzyl. Alcohols, benzyl benzoate, propylene glycol, 1,3-butylglycol oil, glycerol aliphatic esters, polyethylene glycols or fatty acid esters of sorbitan can be used. In addition, when the formulation of the present invention is a suspension, liquid carrier diluents such as water, ethanol or propylene glycol, suspending agents such as ethoxylated isostearyl alcohol, polyoxyethylene sorbitol ester and polyoxyethylene sorbitan ester, Microcrystalline cellulose, aluminum metahydroxy, bentonite, agar or tracant and the like can be used.

In addition, when the formulation of the external preparation composition for skin of the present invention is a surfactant-containing cleansing agent, as a carrier component, an aliphatic alcohol sulfate, an aliphatic alcohol ether sulfate, a sulfosuccinic acid monoester, an isethionate, an imidazolinium derivative, a methyltaurate, Sarcosinates, fatty acid amide ether sulfates, alkylamidobetaines, fatty alcohols, fatty acid glycerides, fatty acid diethanolamides, vegetable oils, lanolin derivatives or ethoxylated glycerol fatty acid esters and the like can be used.

Hereinafter, the present invention will be described in detail by way of examples. However, these examples are intended to illustrate the present invention in more detail, and the scope of the present invention is not limited to these examples.

<Example 1>

Preparation of an anti-obesity ointment containing capsaicin according to the present invention

The present inventors prepared the anti-obesity skin external preparation composition which can be applied directly to the skin in the form of an ointment as follows. First, 50 mg of purified capsaicin powder (Sigma Aldrich) was dissolved in 200ul of 100% ethanol, and then the ointment composition containing 0.1% capsaicin (i.e. benzyl alcohol, cetyl alcohol, glyceryl steric acid, isopropyl myristate) myristate), PEG-40 stearic acid, petrolatum, a mixture of sorbitol and capsaicin) to prepare an anti-obesity ointment containing finally 0.3% capsaicin. In addition, in the anti-obesity effect measurement experiment performed below, the ointment compositions containing 0.1% and 0.3% of capsaicin were used, and the control ointment was prepared by the same method except for capsaicin in the preparation of the capsaicin-containing ointment composition. Was used.

<Example 2>

Obesity Inhibitory Effect of Anti-obesity Ointment

The present inventors confirmed through the following experiment that the anti-obesity ointment of the present invention containing the capsaicin prepared in Example 1 as an active ingredient actually inhibits obesity.

<2-1> Breeding of animal model and treatment of anti-obesity ointment according to the present invention

As an experimental animal model to which the anti-obesity ointment of the present invention prepared in Example 1 can be applied, mice raised as follows were used.

20 male mice, C57BL / 6 (5 weeks old, Samtako Ltd., Osan, Korea) were ingested for 2 weeks in the general diet, and then stabilized, and 10 of them were gin cord sand (11.5% fat). The normal fat diet of Genecode Ltd (Korea) was taken, and the other 10 animals were fed the high fat diet of Genecode Ltd (Korea) with 45% fat content. Thereafter, the 20 mice were divided into respective experimental groups, and the anti-obesity ointment of the present invention was applied to each experimental group as follows. That is, among the 10 mice fed the normal diet, three put 0.1% capsaicin ointment on the abdomen, five doses of 0.3% capsaicin ointment on the abdomen, and the control group contained capsaicin on the abdomen. Two mice with petroleum jelly (green pharmaceutical) not used were used. Of the 10 other high-fat dieted mice, three were given 0.1% capsaicin ointment in the abdomen and 0.3% capsaicin ointment in the five abdomen, and the control group did not contain capsaicin in the abdomen. 2 mice with petroleum jelly (Green Pharmaceuticals) were used. At this time, the abdomen of each mouse was applied ointment after removing all the hair, all were given a constant amount of 200ul every 24 hours, and breeding for 5 weeks while observing the weight change of the mouse every 24 hours. In addition, the experiment was repeated three times.

<2-2> Measurement of weight loss effect and adipose tissue reduction effect by the anti-obesity ointment according to the present invention

After applying the anti-obesity ointment of the present invention every 24 hours for each experimental group experimented with the mouse of Example <2-1>, the weight change of the mouse was measured for 15 days at 1 day intervals. .

In addition, the experimental and control mice of Example <2-1> were examined whether anti-obesity ointment containing capsaicin according to the present invention can reduce obesity by reducing the weight of adipose tissue. To this end, the mice of the experimental group and the control group were dissected using the method of killing by cervical dislocation, and the adipose tissue of the testis, visceral adipose tissue, mesenteric fat tissue around the small intestine, adipose tissue around the kidney and liver fat tissue were extracted. It was. After that, the weight of the adipose tissue was measured.

As a result, as shown in Figure 1, when the ointment containing capsaicin is applied to the group of mice fed the normal and high fat diet, body weight over time compared to the group receiving the petrolatum not containing capsaicin In the case of the mouse group fed the high fat diet and the ointment of the present invention containing capsaicin, the body weight after 15 days was found to be the same as the body weight of the normal diet fed mouse group. It appeared to be almost similar.

In addition, as a result of measuring the weight of the adipose tissue extracted from the mice of each experimental group, the weight of the adipose tissue of the groups of mice fed high-fat diet was higher than the mice fed the normal diet. In the case of the mouse group fed the normal fat diet and the high fat diet and the anti-obesity ointment according to the present invention, the weight of all the adipose tissue was reduced compared to the group applying the ointment containing no capsaicin. Appeared.

<2-3> Measurement of weight loss effect according to capsaicin concentration

In order to investigate the anti-obesity effect according to the concentration of capsaicin in the anti-obesity ointment of the present invention prepared in Example 1, the content of capsaicin in the method of Example 1 0.01%, 0.05% and 0.075% An ointment for anti-obesity according to the present invention was prepared in the same manner except that it was used by adjusting. Thereafter, the anti-obesity ointment containing 0.01%, 0.05% and 0.075% of capsaicin was applied to the abdomen of the high-fat diet mouse used in Example <2-2>, and the weights of the mice were measured by time. At this time, a mouse coated with only an ointment containing no capsaicin was used as a control.

As a result, as shown in Figure 3, the anti-obesity ointment mice according to the present invention, the weight was shown to be reduced as a whole compared to the mice only ointment containing no capsaicin, the weight loss degree is the concentration of capsaicin It has been shown that the weight loss effect by capsaicin is sustained for a long time more than 30 days.

<2-4> Preparation of ointment containing capsaicin-like compound and measurement of weight loss effect

As the present inventors have found that the capsaicin of the present invention has an anti-obesity effect as a result of the above, to confirm whether dihydrocapsaicin, a similar compound of capsaicin, also has an anti-obesity effect, in <2-3> An ointment containing dihydrocapsaicin was prepared in the same manner except that dihydrocapsaicin was used instead of capsaicin. Subsequently, the high fat diet used in Example <2-2> was applied to the abdomen of the mouse after the 0.075% capsaicin-containing anti-obesity ointment and 0.075% dihydrocapsaicin-containing ointment prepared in <2-3>, respectively, Body weight was measured. At this time, as the control group, mice coated with an ointment containing no dihydrocapsaicin or capsaicin were used.

As a result, as shown in Figure 4, in the case of the mice coated with the ointment containing capsaicin and dihydrocapsaicin according to the present invention, the weight was significantly reduced compared to the control group, after applying the ointment, After 30 days or more, it was confirmed that all of the ointments containing capsaicin or dihydrocapsaicin had almost the same anti-obesity effect.

<2-5> Biochemical Analysis of Blood by Capsaicin

Furthermore, the inventors of the present invention contain 0.075% of capsaicin to investigate whether the capsaicin component of the present invention has an effect of effectively reducing the content of glucose, cholesterol and triglyceride, which are indicators of obesity in the blood. The ointment was applied to the abdomen of mice (8 mice), and after 10 days, blood was collected from the mice, and then the contents of glucose, total cholesterol, and triglycerides in the blood were measured, respectively. As a control group, mice (10 mice) coated with only petrolatum without capsaicin were used. In addition, all the values measured in each mouse were added, and the average value was calculated and measured. At this time, 0.02 ml of serum (or standard solution) in blood collected from each mouse was mixed well with 3 ml of diluted enzyme solution (Asan Pharmaceutical Co., Ltd.) and then left at 37 ° C for 10 minutes to measure glucose, cholesterol and triglyceride. The absorbance was measured at 550 nm with the reagent blank as a control, and then each content was calculated according to the following formula.

Glucose amount (mg / dl) = (sample absorbance / standard solution absorbance) X standard solution concentration (200mg / dl)

Triglyceride amount (mg / dl) = (sample absorbance / standard solution absorbance) X standard solution concentration (300mg / dl)

Total Cholesterol Amount (mg / dl) = (Sample Absorption / Standard Solution Absorbance) X Standard Solution Concentration (300mg / dl)

As a result, in the mouse group coated with the ointment containing capsaicin of the present invention, it was shown that the glucose content, total cholesterol content and triglyceride content in the blood were significantly reduced compared to the control group. It was found to be markedly reduced.

Therefore, the present inventors can effectively reduce the weight of fat tissue without causing other side effects by simply applying the anti-obesity skin external preparation composition of the present invention containing capsaicin or a similar compound of capsaicin to the skin. In addition, it was found that blood glucose content, total cholesterol content and triglyceride content can be reduced, and thus the composition of the present invention can be usefully used for the purpose of preventing, improving and treating obesity, as well as obesity. It can be seen that it can be useful for the prevention of various diseases that can occur due to.

So far I looked at the center of the preferred embodiment for the present invention. Those skilled in the art will appreciate that the present invention can be implemented in a modified form without departing from the essential features of the present invention. Therefore, the disclosed embodiments should be considered in descriptive sense only and not for purposes of limitation. The scope of the present invention is shown in the claims rather than the foregoing description, and all differences within the scope will be construed as being included in the present invention.

Claims (6)

1. Capsaicin; From the group consisting of dihydrocapsaicin, nordihydrocapsaicin, nordiamide, nonivamide, capsiate, dihydrocapsiate and nordihydrocapsiate Capsaicin like compounds selected; Or an external anti-obesity composition comprising a salt thereof as an active ingredient.
2. The method of claim 1,

   The capsaicin or capsaicin-like compound is an anti-obesity skin external preparation composition, characterized in that it comprises 0.001 to 0.5% by weight based on the total weight of the anti-obesity skin external preparation composition.
3. The method of claim 2,

   The capsaicin or capsaicin-like compound is an anti-obesity skin external preparation composition, characterized in that it comprises 0.01 to 0.10% by weight relative to the total weight of the anti-obesity skin external preparation composition.
4. The method of claim 1,

   The skin external preparation composition is an anti-obesity skin external preparation composition, characterized in that the formulation is selected from the group consisting of ointment, gel, liquid, cream, patch and paste.
5. The method of claim 1,

   The external composition for external skin composition for anti-obesity is characterized in that the pharmaceutical composition for reducing the weight by promoting fat decomposition and inhibit body fat accumulation.
6. A skin cosmetic for weight loss comprising the composition according to any one of claims 1 to 5.

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