TWI654986B - Use of extraction mixture in preparing pharmaceutical composition for reducing triglyceride production - Google Patents

Abstract

An extract combination is used for preparing a medicinal composition for reducing triglyceride production, wherein the extract combination comprises a licorice extract, a white kidney bean extract and a garcinia cambogia extract. This composition can also be used to reduce waist size or reduce height and body mass index (BMI).

Description

Use of extract combination for preparing pharmaceutical composition for reducing triglyceride production

The present invention relates to the use of an extract combination for the preparation of a medicinal composition for reducing the production of triglyceride, in particular to a combination of licorice extract, white kidney bean extract and garcinia cambogia extract for preparing a reduced triglyceride. Use of a pharmaceutical composition for the production of glycerides.

Due to adequate nutrition and lack of exercise, modern people often eat more calories than the body needs. The human body instinctively stores these excess calories in case the body cannot obtain the required calories, and stores the excess calories in the form of triglycerides in liver cells and fat cells for emergency needs.

However, when triglycerides are continuously accumulated in liver cells and fat cells, the body fat rate of the human body increases, and the body shape of the human body also changes accordingly, such as weight gain, waist circumference increase, or height and body mass index increase. Furthermore, the presence of excessive body fat in the human body may also cause various health problems such as hypertension, heart disease, and cerebrovascular disease. Therefore, for modern people with obesity problems, how to reduce the body fat rate and how to adjust the body shape are urgent issues to be solved.

The present invention provides the use of a combination of Glycyrrhizae extract, white kidney bean extract and garcinia cambogia extract for the preparation of a pharmaceutical composition for reducing the production of triglyceride, thereby reducing the body fat rate of the human body, thereby reducing Weight, waist, or height body mass index.

The invention discloses the use of an extract combination for preparing a medicinal composition for reducing triglyceride production. This extract combination contains extracts of Glycyrrhiza indica, white kidney bean and Garcinia cambogia.

According to the use of the extract combination disclosed in the present invention for preparing a pharmaceutical composition for reducing triglyceride production, edible Glycyrrhizae extract, kidney kidney bean extract, and Garcinia cambogia extract can reduce triglyceride in the body. Ester production. In this way, the amount and rate of triglyceride accumulation in the body can be further reduced, thereby achieving the effect of reducing the body fat rate, weight, waist circumference, or height and body mass index of the human body.

The above description of the contents of this disclosure and the description of the following embodiments are used to demonstrate and explain the spirit and principle of the present invention, and provide a further explanation of the scope of the patent application of the present invention.

FIG. 1 is an infrared absorption spectrum of an extract of licorice used in Examples 1 to 8 of the present invention.

FIG. 2 is a high-performance liquid chromatogram of the extract of licorice used in Examples 1 to 8 of the present invention.

FIG. 3 is a schematic diagram of the effects of the extracts of licorice used in Examples 1 to 8 of the present invention at different concentrations on the amount of triglyceride induced by oleic acid in hepatocytes.

FIG. 4 is a schematic diagram showing the effects of the examples, comparative examples 1, comparative examples 2 and control examples on the amount of weight loss.

FIG. 5 is a schematic diagram showing the influence of the embodiment, the comparative example 1, the comparative example 2 and the control example on the amount of body fat reduction.

FIG. 6 is a schematic diagram showing the influence of the embodiment, the comparative example 1, the comparative example 2 and the control example on the waist circumference drop amount.

FIG. 7 is a schematic diagram showing the influence of the embodiment, the comparative example 1, the comparative example 2 and the control example on the amount of decrease in height and body mass index.

The detailed features and advantages of the present invention are described in detail in the following embodiments. The content is sufficient for any person skilled in the art to understand and implement the technical contents of the present invention. Anyone skilled in the relevant art can easily understand the related objects and advantages of the present invention. The following examples further illustrate the viewpoints of the present invention in detail, but do not limit the scope of the present invention in any way.

Yu Ganzi (such as Phyllanthus Emblica or Emblica Officinale), also known as Yu grapefruit, nectarine, Amalaka, Pokok Melaka, Indian Gooseberry, belongs to the genus Emblica (Emblica) ), Deciduous sub-arbor, distributed from India to Malaysia and southern China, India is generally considered as the origin.

The method for obtaining the extract of licorice used in the present invention is, for example, carbon dioxide as a supercritical fluid for extracting licorice fruit, or methanol, ethanol, acetone, ethyl acetate, 0.1 to 5% by weight sodium chloride aqueous solution, A potassium chloride aqueous solution, a calcium chloride aqueous solution, a magnesium chloride aqueous solution, or a sodium chloride ethanol solution, a potassium chloride ethanol solution, a calcium chloride ethanol solution, and a magnesium chloride ethanol solution with a concentration of 0.1 to 5% by weight are used as a solvent to extract the fruit of the berry. A primary extract was obtained. Next, the primary extract is filtered and purified to obtain the licorice extract used in the present invention. The ganko extract can be spray-dried or vacuum-dried to obtain a ganko extract powder which is easy to preserve.

The extracts of licorice used in Examples 1 to 8 of the present invention contain a mixture of Emblicanin-A and Emblicanin-B in a percentage of 35% to 55% by weight, Punigluconin in a percentage of 4% to 15% by weight, and 10% to 20% by weight Pedunculagin, Rutin, 5% to 15% by weight, and Gallo-ellagitannoids, 10% to 30% by weight.

The structure of Emblicanin-A (2,3-di-O-galloyl-4,6- (S) -hexahydroxy diphenoyl-2-keto-glucono-lactone) is shown in Formula 1.

The structure of Emblicanin-B (2,3,4,6-bis- (S) -hexahydroxydiphenoyl-2-keto-glucono-lactone) is shown in Formula 2.

Punigluconin (2,3-di-O-galloyl-4,6- (S) -hexahydroxyd The structure of iphenoyl gluconic acid) is shown in Formula 3.

The structure of Pedunculagin (2,3,4,6-bis- (S) -hexahydroxydiphenoyl-D-glucose) is shown in Formula 4.

The structure of Rutin (3 ', 4', 5,7-tetrahydroxyflavono-1,3-O-rhamnogl ucoside) is shown in Formula 5.

The fruit extract of Emblica Officinalis used in the experiment of the present invention is that the fruit of Emblica Officinalis is immersed in a 1% by weight sodium chloride aqueous solution, and then heated in a steam bath at 65 ° C to 75 ° C. Hours, followed by filtration, followed by freezing for another 3 days, followed by a spray dry procedure to obtain the powder of the guacamole extract. After drying, the type of the extract of licorice was brown powder. Emblican extract contains 27% by weight of Emblicanin-A, 23% by weight of Emblicanin-B, 8% by weight of Punigluconin, 14% by weight of Pedunculagin, 10% by weight of Rutin and 10% to 30% by weight % Of Gallo-ellagitannoids. The licorice extract of the present invention is not limited to the extract of Emblica Officinalis , and other licorice extracts with different scientific names but similar components also have the same effect.

FIG. 1 is an infrared absorption spectrum of an extract of licorice used in Examples 1 to 8 of the present invention. FIG. 2 is a high-performance liquid chromatogram of the extract of licorice used in Examples 1 to 8 of the present invention. As shown in FIG. 1, the infrared absorption spectrums of the extracts of licorice used in Examples 1 to 8 of the present invention are 3403.6 cm ^-1 (cm ^-1 ), 2931.6 cm ^-1 (cm ^-1 ), 1385.0 cm ^-1 ( cm ^-1 ), 1318.6 cm ^-1 (cm ^-1 ), 1623.5 cm ^-1 (cm ^-1 ), 1451.3 cm ^-1 (cm ^-1 ), 1352.1 cm ^-1 (cm ^-1 ), 1218.4 cm ^-1 ( cm ^-1 ), 1148.6 cm ^-1 (cm ^-1 ), 1035.7 cm ^-1 (cm ^-1 ), 3403.6 cm ^-1 (cm ^-1 ) have characteristic absorption peaks. As shown in FIG. 2, the HPLC chromatograms of the extracts of licorice used in Examples 1 to 8 of the present invention have characteristic peak signals at 1.620 minutes, 2.148 minutes, 3.265 minutes, and 4.370 minutes.

FIG. 3 is a schematic diagram of the effects of the extracts of licorice used in Examples 1 to 8 of the present invention at different concentrations on the amount of triglyceride induced by oleic acid in hepatocytes. The cells used in the experiment were Hep-G2 cells. Experimental samples were prepared by implanting 20,000 hepatocytes into each well of the well plate and culturing for 24 hours. In the course of the experiment, firstly, an aqueous solution of the extract of Coconut Seed Extract was added to the well where the liver cells were located and soaked for 24 hours. Next, remove the aqueous holes located in the hepatocytes, and the molar volume of 0.7 microliters per mole concentration (0.7 μ M) of oleic acid dimethyl sulfoxide (Dimethyl sulfoxide, DMSO) was added to the wells And soak for 24 hours to complete the preparation of samples one to four. The preparation method of sample five is similar to that of sample one to sample four, but hepatocytes are not soaked with the extract of licorice, but after removing the aqueous solution in the well where the hepatocytes are located, the volumetric molar concentration is 0.7 mol per microliter (0.7 μ M) of oleic acid dimethyl sulfoxide was added to the wells and soak for 24 hours. Sample 6 was prepared by implanting 20,000 hepatocytes into each well of the well plate and culturing for 24 hours. Next, the aqueous solution in the well where the hepatocytes are removed, and the same volume of dimethyl sulfene as the oleic acid dimethyl sulfide solution in sample five was added to the well and soaked for 24 hours.

In sample one, the concentration of the aqueous solution of the extract of licorice was 100 micrograms (μg / ml) per milliliter. In sample two, the concentration of the aqueous solution of the licorice extract was 250 micrograms (μg / ml) per milliliter. In sample three, the concentration of the aqueous solution of the licorice extract was 500 micrograms (μg / ml) per milliliter. In sample four, the concentration of the aqueous solution of the extract of licorice was 1000 micrograms (μg / ml) per milliliter.

As shown in FIG. 3, based on the optical absorbance of triglyceride in the liver cells of sample six (Absorbance), the optical absorbance of triglyceride in liver cells of samples 1 to 4 is divided by the The percentage of the optical absorption of triglyceride in liver cells is lower than the optical absorption of triglyceride in liver cells of sample five divided by the optical absorption of triglyceride in liver cells of sample 6. Percentage. The measuring device for measuring optical absorbance is a spectrophotometer, and the wavelength of light used is 490 nanometers (nm). This shows that the amount of triglyceride produced and accumulated in liver cells from samples one to four is lower than that of sample five. The amount of triglyceride produced and accumulated in hepatocytes. From the percentage change of the optical absorbance of triglyceride in liver cells from sample one to sample four, it can be known that the higher the concentration of the extract of glycyrrhizae provided to liver cells, the more effective is the effect of inhibiting the production and accumulation of triglyceride in liver cells. it is good.

The extracts of licorice shown in FIG. 1 and FIG. 2 and used in FIG. 3 are the extracts of licorice used in Examples 1 to 8 of the present invention, and are only used to illustrate the experimental results of Examples 1 to 8 of the present invention. It is not intended to limit the invention.

White kidney beans, also known as white kidney beans and navy beans, are native to the Americas and are a type of Phaseolus vulgaris . White kidney beans are characterized by white and kidney-like shapes. The whole kidney kidney bean was ground and extracted with water for 4 hours, then filtered, concentrated under vacuum and pasteurized, and then spray-dried to obtain a white powder, which is a kidney kidney bean extract. The white kidney bean extract contains α-amylase inhibitor, which can effectively block the degradation of starch by amylase, thereby reducing the intake of calories and thereby inhibiting the formation of triglyceride.

Garcinia cambogia (Garcinia cambogia) is a tree Dicotyledon Garcinia, but also名马拉巴罗tamarind, native to South Asia. Garcinia cambogia extract is hydroxycitric acid (HCA) obtained by extracting the outer skin of Garcinia cambogia fruit at room temperature using water as a solvent. Hydroxycitric acid can be provided to cells in the form of potassium, calcium, or calcium potassium salts when used. Hydroxycitric acid has the effect of blocking the action of ATP-citrate lyase, thereby inhibiting the formation of triglycerides.

An embodiment of the present invention discloses a method for adjusting body posture, including consuming a composition to reduce body fat or body weight. The composition comprises a licorice extract, a white kidney bean extract and a garcinia cambogia extract. Coconut Extract, Kidney Bean Extract, and Garcinia Cambogia Extract have the effect of reducing the accumulation and accumulation rate of triglycerides in the body, thereby reducing the body fat rate, weight, waist circumference or height and body mass index (BMI) effect.

When the present invention ingests the composition containing the extract of ganganzi, white kidney bean extract and garcinia cambogia by mouth, the effective dose of ganganzi extract is 150 milligrams. Grams (mg) to 300 milligrams (mg), the effective dose of white kidney bean extract is more than 250 milligrams (mg) and less than 1500 milligrams (mg), and the effective dose of Garcinia cambogia extract is 250 milligrams (mg) Above and below 2500 milligrams (mg). The effective dose here is obtained after conversion and adjustment according to the conversion formula of the effective dose of animal experiments and the kilogram of human body and the general conversion rules commonly used in the art. The conversion formula is as follows: human effective dose = (effective dose for animal experiments (kg) / mouse weight (kg)) × conversion factor × human weight (kg). The conversion factor is obtained from a look-up table of dose conversion coefficients per kilogram of body weight of animals and humans. When the mouse weighs 20 grams and the human kilogram weighs 60 kilograms, the conversion factor is 0.081.

In order to facilitate the oral ingestion of a composition containing the extract of ganganzi, white kidney beans and garcinia cambogia, the composition can be made into, for example, liquid, solid, granular, powdery, paste Processed product in the form of a gel or a gel. The processed product of the composition can be matched with an excipient or flavoring agent as an additive to enhance the flavor and ease of consumption.

Excipients are, for example, starches such as wheat starch, rice starch, corn starch, potato starch, dextrin, and cyclodextrin; crystalline celluloses; lactose, glucose, granulated sugar, reduced maltose, caramel, fructooligosaccharides, and emulsified oligosaccharides And other sugars; sorbitol, erythritol, xylitol, lactitol, mannitol and other sugar alcohols.

Flavoring agents are, for example, various fruit extracts such as longan extract, lychee extract, grapefruit extract; various fruit juices such as apple juice, orange juice, and lemon juice; various spices such as peach flavor, plum flavor, and yogurt flavor; acesulfame Various sweeteners such as potassium acid, sucralose, erythritol, oligosaccharides, mannose, xylitol, isomerized sugars; various acidifiers such as citric acid, malic acid, tartaric acid, gluconic acid; green tea, oolong tea, Various tea ingredients such as Banaba Tea, Eucommia Tea, Tieguanyin Tea, 薏苡 Tea, Aescinate Tea, White Tea, Kumbu Tea; Coffee Arabica, Coffee Robusta, Various coffee ingredients such as Coffee Liberica.

Furthermore, the composition can also be coated in capsules to facilitate oral ingestion of Glycyrrhizae extract. The composition may be coated in a hard capsule in the form of a dry powder, or the composition may be Solution, suspension, paste, powder or granule forms are coated in soft capsules.

The fats and oils used to dissolve or disperse the licorice extract in soft capsules are e.g. pear oil, almond oil, linseed oil, cumin oil, white perilla oil, olive oil, olive squalene, sweet orange oil, chestnut Orange roughy oil, sesame oil, garlic oil, cocoa butter, pumpkin seed oil, chamomile oil, carrot oil, courgette oil, tallow fatty acids, Hawaiian stone oil, bilberry oil, brown rice germ oil, rice oil, wheat germ Oil, safflower oil, shea oil, liquid shea oil, perilla oil, soybean oil, evening primrose oil, camellia oil, corn oil, rapeseed oil, saw palmetto extract oil, emu oil, Peach kernel oil, parsley oil, castor oil, sunflower oil, grape seed oil, borage oil, Australian walnut oil, meadowfoam oil, cottonseed oil, peanut oil, turtle oil, mink oil, egg butter, Fish oil, palm oil, palm kernel oil, wood wax, coconut oil, long chain / medium chain / short chain fatty acid triglycerides, diglycerides, tallow, lard, squalene, squalane, tincture Alkanes, and hydrides of these oils and fats. Among them, borage oil and evening primrose oil contain a large amount of Gamma-Linolenic Acid (GLA). Gamma-linolenic acid is an essential fatty acid of the human body, which has moisturizing, promotes cell regeneration, and promotes brown fat activity. Degree to promote fat burning function.

In addition, colorants, preservatives, tackifiers, binding agents, disintegrating agents, dispersants, stabilizers, gelling agents, antioxidants, surfactants, preservatives, pH adjusters, etc. are added in accordance with government regulations. The product can also be added to the processed product according to the dosage standard prescribed by the government unit and the needs of processing production.

In the following, the method for adjusting the body shape disclosed in the present invention will be described by the examples, comparative examples 1, two and control examples of the present invention, and experimental tests will be performed to illustrate the efficacy of the method for adjusting the body shape disclosed in the present invention.

The experimental method was a single-blind test. The subjects were 40 male and female members aged 35 to 60 years. The experiment was conducted for 30 consecutive days. The weight of each subject is greater than the ideal weight of each subject by 5 to 20 kg, and the subject's height and body mass index (BMI) is greater than 30. The subjects were randomly divided into control group, experimental group, comparison group one and comparison group two. The subjects who were divided into the control group, the experimental group, the comparison group 1 and the comparison group 2 had a normal daily diet and exercised for 30 minutes a day. The subjects' daily calorie intake was 2200 to 3000 calories.

The subjects assigned to the control group consumed the beverages brewed by the control powder once a day. The control powder contained a placebo made of corn dextrin. The subjects assigned to the experimental group consumed the drink brewed by the powder of the example once a day. The powder of the example contained 200 mg of ganko extract, 300 mg of white kidney bean extract, and 300 mg of Garcinia cambogia extract. . The subjects classified as Comparative Group 1 consumed the beverage brewed by the powder of Comparative Example 1 once a day. The powder of Comparative Example 1 contained 1500 mg of kidney kidney bean extract. The subjects classified as Comparative Group 2 consumed the beverage brewed by the powder of Comparative Example 2 once a day. The powder of Comparative Example 2 contained 2500 mg of Garcinia Cambogia extract. Among the powders of the control examples, examples, comparative examples 1 and 2, the coffee powder was used as a flavoring agent.

The powder composition ratios of the examples, comparative examples 1, comparative examples 2 and control examples and the measurement results of the subjects in the corresponding experimental group, comparative group 1, comparative group 2 and control group are shown in Table 1 and Figures 4 to 4. 7 is shown. FIG. 4 is a schematic diagram showing the effects of the examples, comparative examples 1, comparative examples 2 and control examples on the amount of weight loss. FIG. 5 is a schematic diagram showing the influence of the embodiment, the comparative example 1, the comparative example 2 and the control example on the amount of body fat reduction. FIG. 6 is a schematic diagram showing the influence of the embodiment, the comparative example 1, the comparative example 2 and the control example on the waist circumference drop amount. FIG. 7 is a schematic diagram showing the influence of the embodiment, the comparative example 1, the comparative example 2 and the control example on the amount of decrease in height and body mass index.

As shown in FIG. 4, the weight loss of the subjects in the experimental group is greater than that in the control group, the comparison group 1 and the comparison group 2, indicating that the weight adjustment effect of the embodiment is better than that of the comparison example 1 and Comparative Example 2 weight adjustment effect. As shown in FIG. 5, the decrease in the body fat percentage of the subjects in the experimental group was greater than the decrease in the body fat percentage of the subjects in the control group, the comparison group 1 and the comparison group 2, which illustrates the effect of adjusting the body fat ratio of the embodiment. It is better than the body fat percentage adjustment effect of Comparative Examples 1 and 2. As shown in FIG. 6, the waist circumference drop of the subjects in the experimental group is greater than the waist circumference drop of the subjects in the control group, the comparison group 1 and the comparison group 2, which shows that the waist adjustment effect of the embodiment is better than that of the comparison example 1. Comparative example 2 waist adjustment effect. As shown in FIG. 7, the decrease in the body height and body mass index of the subjects in the experimental group is greater than that in the control group, the comparison group 1, and the comparison group two, which illustrates the adjustment of the height and body mass index in the embodiment. The effect was better than the height and body mass index adjustment effects of Comparative Examples 1 and 2.

According to the results of the above experiment, the composition of the example containing 200 mg of Gan Ganzi extract, 300 mg of white kidney bean extract, and 300 mg of Garcinia cambogia extract passed through Gan Gan extract, white kidney bean extract and Garcinia cambogia The combined effect of the extracts makes the composition better than the 1500 mg white kidney bean extract in Comparative Example 1 and the 2500 mg Garcinia Cambogia extract in Comparative Example 2.

Furthermore, the total weight of the ganko extract, white kidney bean extract, and garcinia cambogia extract in the examples is 800 mg, which is much lower than the weight of the white kidney bean extract in comparative example 1 or the garcinia cambogia in comparative example 2. Fruit extract weight. According to the feedback from the test subjects, The total weight of white kidney bean extract and garcinia cambogia extract is low, which has less influence on the flavor of the flavoring agent and has better palatability. In contrast, the white kidney bean extract of Comparative Example 1 or the Garcinia Cambogia extract of Comparative Example 2 has a higher weight, which has a greater influence on the flavor of the flavoring agent and has poor palatability.

According to the use of the extract combination disclosed in the present invention for preparing a pharmaceutical composition for reducing triglyceride production, edible Glycyrrhizae extract, kidney kidney bean extract, and Garcinia cambogia extract can reduce triglyceride in the body. Ester production. In this way, the amount and rate of triglyceride accumulation in the body can be further reduced, thereby achieving the effect of reducing the body fat rate, weight, waist circumference, or height and body mass index of the human body.

Although the present invention is disclosed in the foregoing embodiments, it is not intended to limit the present invention. Changes and modifications made without departing from the spirit and scope of the present invention belong to the patent protection scope of the present invention. For the protection scope defined by the present invention, please refer to the attached patent application scope.

Claims (8)

An extract combination is used for preparing a medicinal composition for reducing triglyceride production, wherein the extract combination comprises a licorice extract, a white kidney bean extract and a garcinia cambogia extract. The use of the extract combination as described in claim 1 for preparing a pharmaceutical composition for reducing triglyceride production, wherein the licorice extract is obtained by extracting licorice fruit with water as a solvent. The use of the extract combination according to any one of claim 1 and claim 2 for preparing a pharmaceutical composition for reducing triglyceride production, wherein the licorice extract contains 35% to 55% by weight of Emblicanin -A mixture with Emblicanin-B, 4% to 15% by weight of Punigluconin, 10% to 20% by weight of Pedunculagin, 5% to 15% by weight of Rutin and 10% to 30% by weight of Gallo-ellagitannoids. The use of the extract combination as described in claim 1 for the preparation of a pharmaceutical composition for reducing triglyceride production, wherein the effective dose of the licorice extract is 150 milligrams (mg) to 300 milligrams (mg), and the white The effective dose of kidney bean extract is more than 250 milligrams (mg) and less than 1500 milligrams (mg), and the effective dose of the Garcinia cambogia extract is more than 250 milligrams (mg) and less than 2500 milligrams (mg). The use of the extract combination as described in claim 4 for the preparation of a pharmaceutical composition for reducing triglyceride production, wherein the effective dose of the Glycyrrhizae extract is 200 milligrams (mg), and the effective amount of the white kidney bean extract is The dose is 300 milligrams (mg) and the effective dose of the Garcinia cambogia extract is 300 milligrams (mg). The use of the extract combination according to claim 4 for preparing a pharmaceutical composition for reducing triglyceride production, wherein the pharmaceutical composition is added to a beverage when the pharmaceutical composition is consumed. Use of the combination of extracts according to claim 1, claim 2, and any one of claims 4 to 6 to prepare a pharmaceutical composition for reducing triglyceride production, wherein the pharmaceutical composition is consumed to reduce Waist size, body fat or weight. The use of the combination of the extracts described in claim 1, claim 2 and any one of claims 4 to 6 for the preparation of a pharmaceutical composition for reducing triglyceride production, wherein the pharmaceutical composition is consumed to reduce Height Body Mass Index (BMI).