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WO2023214716A1 - Composition pharmaceutique et aliment fonctionnel de santé pour la prévention de l'obésité comprenant un extrait de garcinia cambogia - Google Patents

Composition pharmaceutique et aliment fonctionnel de santé pour la prévention de l'obésité comprenant un extrait de garcinia cambogia Download PDF

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WO2023214716A1
WO2023214716A1 PCT/KR2023/005272 KR2023005272W WO2023214716A1 WO 2023214716 A1 WO2023214716 A1 WO 2023214716A1 KR 2023005272 W KR2023005272 W KR 2023005272W WO 2023214716 A1 WO2023214716 A1 WO 2023214716A1
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pharmaceutical composition
preventing
weight
treating obesity
obesity
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Korean (ko)
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최진원
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Choice Medicare Co Ltd
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Choice Medicare Co Ltd
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
    • A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/353—3,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18—Magnoliophyta (angiosperms)
    • A61K36/185—Magnoliopsida (dicotyledons)
    • A61K36/38—Clusiaceae, Hypericaceae or Guttiferae (Hypericum or Mangosteen family), e.g. common St. Johnswort
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38—Cellulose; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Definitions

  • the present invention relates to an obesity prevention or pharmaceutical composition and health functional food containing Garcinia cambogia extract.
  • Obesity occurs when excessive energy accumulation occurs due to metabolic imbalance when the supply of energy is much greater than the demand for energy. Clinically, it is involved in the development of various diseases or worsens them. Diseases related to obesity include high blood pressure and camellia sclerosis. , diabetes, fatty liver, and cholelithiasis. In particular, endometrial cancer, gallbladder cancer, cervical cancer, ovarian cancer, and breast cancer occur frequently in women, and in the case of endometrial cancer, the increase in incidence and mortality due to obesity is reported to be the most significant compared to other cancer diseases. Additionally, the mortality rate of obese people is reported to be 1.3 times higher than that of normal weight people.
  • the treatment can be enhanced by the controlled use of over-the-counter appetite suppressants such as caffeine, ephedrine and phenylpropanolamine (Acutrim, Dexatrim).
  • over-the-counter appetite suppressants such as caffeine, ephedrine and phenylpropanolamine (Acutrim, Dexatrim).
  • over-the-counter appetite suppressants
  • Topiramate (2,3,4,5-bis-O-(1-methylethylidene)- ⁇ -D-fructopyranose sulfamate) is approved by the FDA and many others for the treatment of certain seizure disorders and for the prevention of migraines. It is a broad-spectrum neurotherapeutic agent approved by national regulatory agencies (E. Faught et al. (1996) Neurology 46:1684-90]; [Karim et al. (1995) Epilepsia 36 (S4):33]; [ S. K. Sachdeo et al. (1995) Epilepsia 36(S4):33]; [T. A. Glauser (1999) Epilepsia 40 (S5):S71-80]; [R.
  • topiramate is effective in treating diabetes (U.S. Patent Nos. 7,109,174 and 6,362,220), nervous system disorders (U.S. Patent No. 6,908,902), depression (U.S. Patent No. 6,627,653), psychosis (U.S. Patent No. 6,620,819), headache (U.S. Patent No. No. 6,319,903) and high blood pressure (U.S. Patent No. 6,201,010).
  • diabetes U.S. Patent Nos. 7,109,174 and 6,362,220
  • nervous system disorders U.S. Patent No. 6,908,902
  • depression U.S. Patent No. 6,627,653
  • psychosis U.S. Patent No. 6,620,819
  • headache U.S. Patent No. No. 6,319,903
  • high blood pressure U.S. Patent No. 6,201,010
  • Phentermine was approved by the FDA as an appetite suppressant in 1959, and phentermine hydrochloride has been used as a weight loss agent since the 1970s, for example, Adipex-P®, Fastin® , Zantril® It has been used under brand names such as.
  • topiramate and phentermine included in Qsymia products are also synthetic substances and are known to have side effects such as paresthesia, alopecia, parosmia, amenorrhea, and aphasia. There is ([Korean J Obes 2015 March;24(1):17-27, Innov Clin Neurosci. 2011 Aug; 8(8): 14-16.]).
  • the present inventor discovered a composition that can eliminate or reduce the side effects of conventional obesity prevention and treatment compositions and replace them, and thus treat and prevent obesity containing natural substances that can minimize side effects as active ingredients.
  • the purpose is to provide a pharmaceutical composition for.
  • Garcinia cambogia which is known to be effective in suppressing obesity, is a tropical fruit tree of the Guttiferae family and is obtained by extracting the pericarp of Garcinia cambogia fruit. It is known that the resulting product is used to prevent or treat obesity.
  • This Garcinia cambogia extract contains HCA (hydroxy citric acid).
  • the HCA is a compound that is very similar to citric acid but has a hydroxyl group attached to it. It inhibits the process of converting citrate to acetyl-Co-A in vivo, inhibiting the synthesis of fatty acids, promoting oxidation, and converting to glucogen synthesis. increases energy production.
  • HCA is known to have various physiologically active functions, such as suppressing appetite and promoting fat decomposition.
  • One object of the present invention is to provide a pharmaceutical composition for preventing or treating obesity containing Garcinia cambogia extract, L-Arginine, and L-Carnitine.
  • Another object of the present invention is to provide a health functional food for preventing or treating obesity containing the above composition.
  • a combination preparation Branched chain amino acids (BCAAs) containing at least one selected from the group consisting of leucine, isoleucine and valine; Calcium pantothenate; Nicotinic acid amide; crystalline cellulose; Magnesium stearate; hydroxypropylmethylcellulose; and carboxymethylcellulose calcium; a pharmaceutical composition for preventing or treating obesity, wherein the combination preparation includes an active ingredient, the combination preparation has a structure of a core and a shell formed on the core, and the active ingredient is Garcinia cambogia extract obtained by extracting Garcinia cambogia with an extraction solvent, contains L-Arginine and L-Carnitine in a weight ratio of 1:0.01 to 0.1:0.1 to 0.5, and the core contains the Garcinia cambogia.
  • BCAAs Branched chain amino acids
  • It contains the extract and the L-Carnitine, the shell contains the L-Arginine, and the ratio of the outer diameter of the composite preparation to the outer diameter of the core is 1:0.6 to 1:0.95.
  • a pharmaceutical composition for preventing or treating obesity that satisfies the above.
  • Catechin, Cathinone, Tryptamine, P-Octopamine, P-Tyramine, Synephrine and Ephedrine It provides a pharmaceutical composition for preventing or treating obesity further comprising at least one selected from the group consisting of.
  • the present invention provides a pharmaceutical composition for preventing or treating obesity, comprising the Garcinia cambogia extract, L-Arginine, and L-Carnitine in a weight ratio of 1:0.017:0.25. .
  • a pharmaceutical composition for preventing or treating obesity comprising 40 parts by weight or more and 70 parts by weight or less of the combination preparation based on 100 parts by weight of the pharmaceutical composition for preventing or treating obesity.
  • the pharmaceutical composition for preventing or treating obesity contains the L-arginine ( L-Arginine) is in the range of 40 to 45% of the total weight of the active ingredient after 1 hour, and the Garcinia Cambogia extract and L-Carnitine are in the range of 5 to 15% of the total weight of the active ingredient after 1 hour.
  • L-arginine L-Arginine
  • Garcinia Cambogia extract and L-Carnitine are in the range of 5 to 15% of the total weight of the active ingredient after 1 hour.
  • a pharmaceutical composition for preventing or treating obesity that satisfies a dissolution profile.
  • the extraction solvent is water, C1-C4 alcohol, n-hexane, ether, glycerol, propylene glycol, butylene glycol, ethyl acetate, methyl acetate, dichloromethane, chloroform, ethyl acetate, benzene, and mixtures thereof.
  • a pharmaceutical composition for preventing or treating obesity which is selected from the group consisting of solvents.
  • the extraction solvent is modified alkylene glycol; and a solvent having a boiling point of 90°C or lower, wherein the extraction solvent includes 80 parts by weight or more and 95 parts by weight or less of the modified alkylene glycol; and 5 parts by weight or more and 20 parts by weight or less of a solvent having a boiling point of 90°C or lower.
  • the pharmaceutical composition for preventing or treating obesity provided by the present invention contains Garcinia cambogia extract, L-Arginine, and L-Carnitine, and exhibits effects in preventing and treating obesity.
  • the pharmaceutical composition of the present invention reduces the side effects caused by conventional synthetic drugs and contains natural substances that can replace them, such as garcinia cambogia extract, L-arginine, and L-carnitine, as active ingredients to minimize side effects and reduce obesity. It has excellent efficacy in the prevention and treatment of.
  • the pharmaceutical composition of the present invention has a composite preparation containing the above-mentioned active ingredients, and the composite preparation is composed of a core and shell structure, and the ratio of the outer diameter of the composite preparation to the outer diameter of the core is 1:0.6 to 1: It is characterized by satisfying 0.95.
  • the outer diameter ratio of the core satisfies a certain range (i.e., by adjusting the ratio of the core and shell), so it has the feature of effectively controlling the amount of active ingredient dissolved within a certain time. do.
  • the three substances included as active ingredients are not eluted at once, but are prepared in the form of a complex preparation to satisfy the specific structure of the core-shell, so the required composition is eluted in high content within a certain period of time and the 3 substances are continuously released thereafter. It was confirmed that it showed superior obesity prevention and treatment effects by eluting with .
  • the pharmaceutical composition of the present invention has anti-obesity and anti-inflammatory properties as well as antioxidant and toxin removal, that is, detox effects.
  • Figure 1 is a diagram schematically showing a combination preparation according to an embodiment of the present invention.
  • Figure 2 is a graph showing cell survival rate treated with compositions according to one embodiment of the present invention.
  • Figures 3 to 10 show images taken under a microscope at 20x magnification showing the results of inhibiting intracellular adipocyte differentiation when 3T3-L1 cells were treated with compositions according to embodiments of the present invention.
  • Figure 11 is a graph schematically illustrating the results of inhibiting intracellular adipocyte differentiation when treated with compositions according to embodiments of the present invention.
  • a combination preparation Branched chain amino acids (BCAAs) containing at least one selected from the group consisting of leucine, isoleucine and valine; Calcium pantothenate; Nicotinic acid amide; crystalline cellulose; Magnesium stearate; hydroxypropylmethylcellulose; and carboxymethylcellulose calcium; a pharmaceutical composition for preventing or treating obesity, wherein the combination preparation includes an active ingredient, the combination preparation has a structure of a core and a shell formed on the core, and the active ingredient is Garcinia cambogia extract obtained by extracting Garcinia cambogia with an extraction solvent, contains L-Arginine and L-Carnitine in a weight ratio of 1:0.01 to 0.1:0.1 to 0.5, and the core contains the Garcinia cambogia.
  • BCAAs Branched chain amino acids
  • It contains the extract and the L-Carnitine, the shell contains the L-Arginine, and the ratio of the outer diameter of the composite preparation to the outer diameter of the core is 1:0.6 to 1:0.95. It relates to a pharmaceutical composition for preventing or treating obesity that satisfies the above.
  • the term “compound” refers to a result obtained by performing fractionation to separate a specific component or specific group of components from a mixture containing various various components.
  • the separation method for obtaining the above compound in the present invention is not particularly limited and may be performed according to methods commonly used in the art.
  • a non-limiting example of the separation method may be a method of obtaining a compound from a natural substance extract by treating it with a predetermined solvent.
  • extract refers to an extract obtained by extraction treatment, a diluted or concentrated liquid of the extract, a dried product obtained by drying the extract, a crude product or purified product of the extract, or a mixture thereof. etc., includes the extract itself and all formulations of the extract that can be formed using the extract.
  • the extract in this specification follows the dictionary definition and may mean a liquid substance extracted from a specific substance or condition.
  • extract of this specification follows the dictionary definition and is obtained by concentrating a specific component in the extract.
  • the specific active ingredient is separated with an appropriate solvent, the solvent is completely or mostly evaporated, and the remaining lump or powder is adjusted according to the standard.
  • extract can be used to include all three types: semifluid or syrup, pill dealer or solid, dried powder, etc. there is.
  • drying of the extract can be done by a known method as long as useful components from the collected natural material are not destroyed, for example, by natural drying in the shade.
  • crushing or pulverization can be performed to a degree that the useful components of the plant can be sufficiently extracted during the subsequent extraction process.
  • the drying and crushing or pulverizing processes can be performed in reverse order or repeatedly as needed.
  • the extraction method is not particularly limited, and extraction may be performed according to a method commonly used in the art.
  • Non-limiting examples of the extraction method include hot water extraction, ultrasonic extraction, filtration, and reflux extraction, which may be performed alone or by combining two or more methods.
  • the type of extraction solvent used to extract natural substances in the present invention is not particularly limited, and any solvent known in the art can be used.
  • Garcinia cambogia is known to be effective in suppressing obesity, and it is known that the result obtained by extracting the pericarp of Garcinia cambogia fruit, a tropical fruit tree of the Guttiferae family, is used for the prevention or treatment of obesity.
  • the Garcinia cambogia extract contains hydroxycitric acid (HCA), an inhibitor of enzymes involved in fatty acid and cholesterol synthesis, and provides the function of inhibiting fat synthesis, suppressing appetite, and promoting fat decomposition.
  • HCA hydroxycitric acid
  • the HCA is a compound that is very similar to citric acid but has a hydroxyl group attached. It inhibits the process of converting citrate to acetyl-coenzyme A (acetyl-coenzyme A) in vivo, thereby inhibiting the synthesis of fatty acids. It promotes oxidation and conversion to glycogen synthesis, increasing energy production.
  • HCA is known to have various physiologically active functions, such as suppressing appetite and promoting fat decomposition.
  • Garcinia Cambogia extract acts as a factor that blocks the synthesis of excess carbohydrates in the spleen and interferes with fat synthesis, thereby prolonging energy production in the body and increasing total energy production.
  • Garcinia cambogia extract reduces acetyl-Co-A in the human body, resulting in increased liver and glycogen synthesis rates.
  • the Garcinia cambogia extract is in powder form by freeze-drying the peel of the Garcinia cambogia fruit, pulverizing it to 100 mesh or less, extracting it at a temperature of 80°C or higher with 70% extraction solvent, concentrating and freeze-drying.
  • Garcinia cambogia extract obtained by extracting Garcinia cambogia with an extraction solvent is used.
  • the extraction solvent is water, C1-C4 alcohol, n-hexane, ether, glycerol, propylene glycol, butylene glycol, ethyl acetate, methyl acetate, dichloromethane, chloroform, ethyl acetate, benzene, and mixed solvents thereof.
  • a pharmaceutical composition for preventing or treating obesity which is selected from the group consisting of.
  • the extraction solvent for making the Garcinia cambogia extract according to the present application includes modified alkylene glycol; and a solvent having a boiling point of 90°C or lower, wherein the extraction solvent includes 80 parts by weight or more and 95 parts by weight or less of the modified alkylene glycol; and 5 parts by weight or more and 20 parts by weight or less of a solvent having a boiling point of 90°C or lower.
  • glycol refers to a compound having two hydroxy groups (-OH)
  • alkylene glycol refers to a substance having two hydroxy groups (-OH) functional groups in a straight-chain or branched alkyl group. it means.
  • modified alkylene glycol as in the present application, it may refer to a substance obtained by reacting at least one of the hydroxy groups to replace another compound.
  • the alkylene group may include methylene, ethylene, propylene, butylene, etc., and the appropriate number of alkyl groups may include an alkylene group having 1 to 30 carbon atoms, more preferably may be an alkylene group having 1 to 20 carbon atoms, most preferably an alkylene group having 1 to 5 carbon atoms.
  • the modified alkylene glycol may include propylene glycol monomethyl ether.
  • the solvent having a boiling point of 90° C. or lower may be used without limitation as long as the boiling point range among widely known solvents satisfies the above range.
  • the solvent having a boiling point of 90°C or lower may include at least one selected from the group consisting of acetone and ethyl acetate.
  • modified alkylene glycols In the case of organic solvents according to the present application, modified alkylene glycols; and a solvent having a boiling point of 90°C or lower, wherein 80 parts by weight or more and 95 parts by weight or less of the modified alkylene glycol; And it may include 5 parts by weight or more and 20 parts by weight or less of a solvent having a boiling point of 90°C or lower.
  • modified alkylene glycols and a solvent having a boiling point of 90°C or lower, including 80 parts by weight or more and 95 parts by weight or less of modified alkylene glycol, preferably 85 parts by weight or more and 95 parts by weight or less, more preferably 90 parts by weight or more and 95 parts by weight or less. may be included.
  • modified alkylene glycols In the case of organic solvents according to the present application, modified alkylene glycols; and a solvent having a boiling point of 90°C or lower, wherein the amount of the solvent having a boiling point of 90°C or lower is 5 parts by weight or more and 20 parts by weight or less, preferably 5 parts by weight or more and 15 parts by weight or less, more preferably 5 parts by weight or more and 10 parts by weight or less. may be included.
  • the inventor of the present application discovered that the extraction solvent for making Garcinia cambogia into an extract as described above has the above composition, and that when it satisfies the above extraction solvent composition, it is effective in extracting Garcinia cambogia extract from the skin of Garcinia cambogia fruit.
  • the L-Arginine is one of the amino acids that make up protein and belongs to the protein protamine present in fish sperm. As a semi-essential amino acid required for the growth of children and animals, it has been reported that ingestion of L-arginine promotes the secretion of glucagon, which directly accelerates the decomposition of fat tissue in the human body (Kalkhoff RK, et al. , N Engl J Med 289: 465-467).
  • L-carnitine has the chemical name of ⁇ -hydroxy- ⁇ -N-trimethylaminobutyrate, and is an amino acid-like substance structurally similar to choline.
  • L-carnitine is not an actual vitamin because part of the body's requirements can be met through biosynthesis, but it can be said to be a nutrient in the form of a vitamin such as choline, taurine, inositol, etc.
  • L-carnitine The most important biological mechanism of L-carnitine is its role as an essential cofactor in fatty acid metabolism and as a transport molecule that smoothly transports fatty acids into mitochondria in the body and converts fat into cellular energy. This role improves intracellular fatty acid and sugar metabolism.
  • long-chain fatty acids are activated in the mitochondrial outer membrane and oxidized in the mitochondrial matrix.
  • the long-chain fatty acids cannot pass through the inner membrane of mitochondria without a special transport mechanism, and in this case, the transport mechanism is L-carnitine.
  • long-chain fatty acids activated in the mitochondrial outer membrane temporarily bind to the hydroxyl group of L-carnitine to form long-chain fatty acid acyl-carnitine, which is transported into the mitochondria and metabolized.
  • L-carnitine has been proven to reduce lipid accumulation in the blood and tissues in various conditions in the body for weight loss, and improves cardiac function and oxygen intake by supplying energy essential for muscle work. It provides effects such as increasing body weight, maintaining physical strength, and reducing fat.
  • the L-carnitine may be L-carnitine tartrate, which has improved preservability by combining tartrate.
  • the pharmaceutical composition for preventing or treating obesity of the present invention includes a combination preparation, and the combination preparation includes an active ingredient, and the active ingredient is Garcinia cambogia extract, L-Arginine (L-Arginine) and L-carnitine ( L-Carnitine) may be included in a weight ratio of 1:0.01 to 0.1:0.1 to 0.5.
  • the Garcinia cambogia extract, the L-arginine and the L-carnitine are used at a weight ratio of 1:0.015 to 0.05:0.05 to 0.4, preferably, 1:0.015 to 0.05:0.25 to 0.3, for example , may be included in a weight ratio of 1:0.017:0.25.
  • the Garcinia cambogia extract and the L-arginine may be included in a weight ratio of 1:0.01 to 0.1, and if the content of the L-arginine is less than 0.01 times that of the Garcinia cambogia extract, the effect of inhibiting adipocyte differentiation is reduced, If it exceeds twice the amount, palatability decreases rapidly due to the unique taste and smell, and problems such as stomach pain, vomiting, diarrhea, and nausea may occur.
  • the Garcinia cambogia extract and the L-carnitine may be included in a weight ratio of 1:0.1 to 0.5, and if the content of the L-carnitine is less than 0.1 times the content of the Garcinia cambogia extract, there is almost no effect of inhibiting adipocyte differentiation, and 0.5 If it exceeds twice the amount, palatability decreases rapidly due to the unique taste and smell, and problems such as stomach pain, vomiting, diarrhea, and nausea may occur.
  • the first feature of the present invention is that the combination preparation contains an active ingredient and the active ingredient satisfies the above composition and content, resulting in a more effective obesity prevention effect.
  • the composite preparation according to the present application has a structure of a core and a shell formed on the core, wherein the core contains the Garcinia cambogia extract and the L-Carnitine (L-Carnitine), and the shell contains the L-arginine (L -Arginine).
  • the above-described composite preparation satisfies the above-described composition and content and is formed in a core-shell structure, each containing a specific composition in the core and shell parts.
  • the ratio of the outer diameter of the composite preparation to the outer diameter of the core may satisfy 1:0.6 to 1:0.95.
  • the ratio of the outer diameter of the composite preparation to the outer diameter of the core is 1:0.6 to 1:0.95, preferably 1:0.65 to 1:0.85, more preferably 1.0.70 to 1:0.80. can be satisfied, and more preferably, the range of 1:0.75 can be satisfied.
  • Figure 1 is a diagram schematically showing a combination preparation according to an exemplary embodiment of the present invention.
  • the outer diameter of the combination preparation may be indicated by B, and in this case, the outer diameter of the core may be indicated by A. That is, the outer diameter can be expressed as the radius of a sphere or circle.
  • the pharmaceutical composition for preventing or treating obesity contains the above-mentioned composition contained in the water eluate at 37°C, pH 4.0, and water according to the Korean Pharmacopoeia Dissolution Test Method 2 (Paddle Method).
  • L-Arginine accounts for 40 to 45% of the total weight of the active ingredient after 1 hour
  • the Garcinia Cambogia extract and L-Carnitine account for 5 to 15% of the total weight of the active ingredient after 1 hour.
  • the dissolution profile dissolving in the range of % is satisfied.
  • the composite preparation satisfies a certain outer diameter range, and specifically, the outer diameter ratio of the core and the shell satisfies a certain range. Accordingly, in the early stages after administration, the content of L-Arginine contained in the shell is high, and the Garcinia Cambogia extract and L-Carnitine contained in the core are eluted to a minimum extent, especially It is effective in managing obesity.
  • the second feature of the present invention is that the dissolution amount of the three components can be adjusted over time by satisfying the outer diameter range as described above, maximizing the effect, even without including a separate release control mechanism.
  • composition of the present invention contains Catechin, Cathinone, Tryptamine, P-Octopamine, P-Tyramine, Synephrine and Ephedrine ( Ephedrine) may further include any one or more of these substances, which are norepinephrine releasing substances.
  • Norepinephrine acts as a neurotransmitter in the nerve junctions of the brain and muscles and regulates fuel metabolism in the liver and muscles. It means acting as a hormone.
  • the pharmaceutical composition for preventing or treating obesity may be a compound that stimulates the hypothalamus to increase norepinephrine secretion. Specifically, it increases the concentration of norepinephrine at the synapse and activates hypothalamic POMC neurons to suppress appetite and provide energy. It may be a compound that increases consumption.
  • the catechin can be extracted from Camellia sienesis and inhibits COMT (catechol O-methyltransferase) enzyme to increase norepinephrine in the synaptic gap, thereby increasing energy activity, thereby preventing and treating obesity. It can act as a substance ([Korean J Clin Pharm 2018;28(4):342-346, ARYA Atheroscler. 2014 Jan; 10(1): 55-58.]).
  • COMT catechol O-methyltransferase
  • the cathinone can be extracted from Catha edulis (Khat) and, like amphetamine, catecholamines such as dopamine and norepinephrine through TAAR1 activation. ), releases epinephrine, and acts on ⁇ and beta adrenergic receptors (Alpha, beta Adrenergic receptors), showing an appetite suppressing effect.
  • the cathinone has a greater CNS activation effect than amphetamine ([Cathinone (Khat) and Methcathinone (CAT)in Urine Specimens: A Gas Chromatographic-Mass Spectrometric Detection Procedure], [MECHANISM OF ACTION OF CATHINONE: THE ACTIVE INGREDIENT OF KHAT (CATHA EDULIS)]).
  • the tryptamine can be extracted from Vachellia aroma , and increases insulin in the pancreas through the TAAR1 receptor, thereby reducing fasting blood sugar in the liver and delaying food evacuation time from the stomach.
  • GLP-1&PYY By increasing GLP-1&PYY, it can act as a substance for the prevention and treatment of obesity through a complex mechanism including the effect of reducing the extracorporeal excretion of glucose ([Pharmacology of human trace amine-associated receptors: Therapeutic opportunities and challenges], [ Pharmacology & Therapeutics, Volume 180, December 2017, Pages 161-180]).
  • the P-Octopamine can be extracted from Bitter Orange ( Citrus aurantium ), and has the effect of increasing the feeling of satiety by increasing the release of Serotonin through the TAAR1 receptor, thereby reducing food intake. As a result, it can act as a substance for the prevention and treatment of obesity.
  • P-octopamine acts on the Beta 3 Adrenergic receptor in adipocytes to activate Beta 3 Adrenergic receptor, and induces the conversion of white fat into brown fat through the binding activation of Norepinephrine and activation of UCP-1 protein in adipocytes.
  • the P-Tyramine can be extracted from Bitter Orange ( Citrus aurantium ) or Musa sapientum L , and increases insulin in the pancreas through the TAAR1 receptor, thereby increasing fasting blood sugar level in the liver. It can act as a substance for the prevention and treatment of obesity through a complex mechanism including the effect of reducing the extracorporeal excretion of glucose by increasing GLP-1&PYY by delaying the gastric food excretion time ([Pharmacology of human trace amine -associated receptors: Therapeutic opportunities and challenges], [Pharmacology & Therapeutics, Volume 180, December 2017, Pages 161-180]).
  • the synephrine can be extracted from Bitter Orange ( Citrus aurantium ), releases catecholamines through TAAR1 activation, binds to the ⁇ 3 adrenergic receptor, activates lipolysis, and It can act as a substance for the prevention and treatment of obesity by increasing epinephrine (norepinephrine) and showing efficacy in energy activation ([Phytother Res. 2017 Oct; 31(10): 1463-1474.]).
  • the ephedrine is ephedra sinica ), it mainly acts on ⁇ and ⁇ adrenergic receptors, stimulates sympathetic nerves, increases norepinephrine in the synaptic gap, and is effective in energy activation, thereby acting as a substance for the prevention and treatment of obesity. ([Anesth Prog. 2012 Winter; 59(4): 159-169.]).
  • the pharmaceutical composition of the present invention preferably contains catechin as a norepinephrine release substance.
  • the pharmaceutical composition for preventing or treating obesity of the present invention may include the Garcinia cambogia extract, L-arginine, L-carnitine, and catechin in a weight ratio of 1:0.01 to 0.1:0.1 to 0.5:0.5 to 2.
  • the Garcinia cambogia extract and the catechin may be included in a weight ratio of 1:0.5 to 1:2, and if the content of the catechin is less than 0.5 times that of the Garcinia cambogia extract, the effect of inhibiting adipocyte differentiation is reduced, and if the content of the catechin is more than 2 times. In this case, a problem of cytotoxicity occurs.
  • the composition may be included in a weight ratio of 1:0.015 to 0.05:0.05 to 0.4:0.1 to 0.2 in order to maximize the effect of inhibiting adipocyte differentiation while preventing or minimizing cytotoxicity.
  • the composition includes branched-chain amino acids (BCAA) containing at least one selected from the group consisting of leucine, isoleucine, and valine, calcium pantothenate, nicotinic acid amide, crystalline cellulose, magnesium stearate, hydroxypropylmethylcellulose, and It may contain calcium carboxymethylcellulose.
  • BCAA branched-chain amino acids
  • the branched-chain amino acid is one of the essential amino acids that is closely related to muscles, and the calcium pantothenate (molecular formula C 18 H 32 O 10 N 2 Ca) is a white powder with an odor. It is a calcium salt fortifier with a slightly bitter taste that acts as a coenzyme in the body and is necessary for normalizing tissue function, physical growth, and maintaining health.
  • the nicotinic acid amide is a type of vitamin, which is added to suppress obesity and diet, and includes vitamins B1, B2, B6, B12, C, D3, and nicotinic acid amide.
  • Vitamins B, C, D, and nicotinic acid amide act as coenzymes in the TCA cycle, which breaks down glucose to create energy. At this time, if there are no vitamins, this process cannot proceed and the nutrients cannot be consumed as energy and are converted to body fat and accumulated in the body. In other words, if you do not have enough vitamins, the food you eat cannot be used as energy and accumulates in the body, ultimately leading to obesity.
  • the crystalline cellulose is an additive used as an anti-caking agent, stabilizer, emulsifier, and dietary fiber in foods, and the magnesium stearate provides mineral components by supplying magnesium, and the hydroxypropylmethylcellulose (hypromellose, HPMC),
  • HPMC hydroxypropylmethylcellulose
  • the carboxymethylcellulose calcium serves as a viscosity regulator.
  • composition may further include additives such as zinc oxide and silicon dioxide.
  • the term “prevention” refers to all actions that suppress or delay obesity
  • the term “treatment” refers to all actions that improve or beneficially change the symptoms of an individual suspected of or suffering from obesity.
  • the pharmaceutical composition may contain the active ingredient alone or may be provided as a pharmaceutical composition including one or more pharmaceutically acceptable carriers, excipients, or diluents.
  • 'pharmacologically acceptable' refers to a composition that is physiologically acceptable and does not usually cause allergic reactions or similar reactions when administered to humans.
  • the pharmaceutical composition may be provided by mixing with conventionally known obesity treatment substances. That is, the pharmaceutical composition can be administered in combination with a known compound that has the effect of preventing or treating obesity.
  • administration means introducing a predetermined substance into an individual by an appropriate method
  • individual refers to all animals such as rats, mice, and livestock, including humans, that have or may develop obesity. As a specific example, it may be a mammal, including humans.
  • obesity refers to something caused by energy imbalance, and the causes of obesity are complexly related to hormonal changes, genetics, mental health problems, socioeconomic factors, etc. Specifically, it means that it can be caused by energy imbalance, genetic factors, neuroendocrine factors, and environmental factors.
  • the route of administration of the pharmaceutical composition is not limited to these, but is oral, intravenous, intramuscular, intraarterial, intramedullary, intrathecal, intracardiac, transdermal, subcutaneous, intraperitoneal, intranasal, enteral, topical, sublingual, or Includes workplace.
  • the pharmaceutical composition can be administered orally or parenterally, and when administered parenterally, it is preferable to select the injection method by external injection through the skin or intraperitoneal injection, intrarectal injection, subcutaneous injection, intravenous injection, intramuscular injection, or intrathoracic injection. , but is not limited to this, and oral administration may be preferably selected from the viewpoint of selecting a more effective absorption route.
  • the composition of the present invention can be formulated into powder, granule, tablet, pill, powder, sugar-coated tablet, capsule, solution, gel, syrup, slurry, suspension, etc. using methods known in the art. It can get angry.
  • oral preparations can be prepared by combining the active ingredient with solid excipients, grinding them, adding suitable auxiliaries and processing them into a granule mixture to obtain tablets or dragees.
  • excipients examples include sugars including lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol and maltitol, starches including corn starch, wheat starch, rice starch and potato starch, cellulose, Fillers such as cellulose, including methyl cellulose, sodium carboxymethylcellulose, and hydroxypropylmethyl-cellulose, gelatin, polyvinylpyrrolidone, calcium carbonate, etc. may be included. In addition to simple excipients, lubricants such as magnesium stearate and talc are also used. Liquid preparations for oral use include suspensions, oral solutions, emulsions, syrups, etc.
  • composition of the present invention may further include anti-coagulants, lubricants, fragrances, emulsifiers, and preservatives.
  • Non-aqueous solvents and suspensions include propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate.
  • injectable ester such as ethyl oleate.
  • a base for suppositories witepsol, macrogol, tween 61, cacao, laurel, glycerogeratin, etc. can be used.
  • the preferred dosage of the pharmaceutical composition varies depending on the patient's condition and weight, degree of disease, drug form, administration route and period, but can be appropriately selected by a person skilled in the art.
  • the pharmaceutical composition of the present invention may vary the content of the active ingredient depending on the severity of the disease.
  • a preferred total dosage of the composition of the present invention may be about 0.01 ⁇ g to 1,000 mg per kg of patient body weight per day, most preferably 0.1 ⁇ g to 100 mg per kg of patient body weight per day.
  • the dosage of the composition is determined by considering various factors such as the route of administration and number of treatments of the pharmaceutical composition, as well as the patient's age, weight, health status, gender, severity of the disease, diet, and excretion rate.
  • the pharmaceutical composition according to the present invention is not particularly limited in its formulation, administration route, and administration method as long as it exhibits the effects of the present invention.
  • the pharmaceutical composition When formulating the pharmaceutical composition, it is prepared using diluents or excipients such as commonly used fillers, extenders, binders, wetting agents, disintegrants, and surfactants.
  • composition of the present invention can be used not only in the form of a medicine for humans, but also in the form of an animal medicine.
  • animals are a concept that includes livestock and pets.
  • a health functional food containing the pharmaceutical composition for preventing or treating obesity according to the present application is provided.
  • the health functional food may be formulated with one selected from the group consisting of tablets, pills, powders, granules, powders, capsules, and liquid formulations, further including one or more of carriers, diluents, excipients, and additives.
  • Foods to which the above acteoside or its foodologically acceptable salt can be added include various foods, powders, granules, tablets, capsules, syrups, beverages, gum, tea, vitamin complexes, nutritional supplements, health functional foods, and Food additives, etc.
  • Additives that may be further included in the health functional food include natural carbohydrates, flavors, nutrients, vitamins, minerals (electrolytes), flavors (synthetic flavors, natural flavors, etc.), colorants, fillers (cheese, chocolate, etc.) , pactic acid and its salts, alginic acid and its salts, organic acids, protective colloidal thickeners, pH adjusters, stabilizers, preservatives, antioxidants, glycerin, alcohol, carbonating agents and pulp. there is.
  • natural carbohydrates examples include monosaccharides such as glucose, fructose, etc.; Disaccharides such as maltose, sucrose, etc.; and polysaccharides, such as common sugars such as dextrin and cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol.
  • natural flavoring agents thaumatin, stevia extract (e.g., rebaudioside A, glycyrrhizin, etc.) and synthetic flavoring agents (saccharin, aspartame, etc.) can be advantageously used.
  • Nutrients vitamins, minerals (electrolytes), flavoring agents such as synthetic and natural flavors, colorants and thickening agents (cheese, chocolate, etc.), pectic acid and its salts, alginic acid and its salts, organic acids, protective colloidal thickeners, It may contain pH adjusters, stabilizers, preservatives, glycerin, alcohol, carbonating agents used in carbonated drinks, etc.
  • the health functional food may contain pulp for the production of natural fruit juice and vegetable drinks. These ingredients can be used independently or in combination.
  • the carriers, excipients, diluents and additives include, but are not limited to, lactose, dextrose, sucrose, sorbitol, mannitol, erythritol, starch, gum acacia, calcium phosphate, alginate, gelatin, calcium phosphate, calcium.
  • the health functional food When formulating the health functional food, it is prepared using diluents or excipients such as commonly used fillers, extenders, binders, wetting agents, disintegrants, and surfactants.
  • diluents or excipients such as commonly used fillers, extenders, binders, wetting agents, disintegrants, and surfactants.
  • Garcinia cambogia extract was obtained by freeze-drying the peel of the Garcinia cambogia fruit, pulverizing it to 100 mesh or less, and extracting it at a temperature of 80°C or higher with 70% extraction solvent. At this time, the extraction solvent below was used, Accordingly, Garcinia Cambogia Extract-1 and Garcinia Cambogia Extract-2 were prepared.
  • Garcinia cambogia extract-1 was extracted using extraction solvent 1
  • Garcinia cambogia extract-2 was extracted using extraction solvent 2.
  • Extraction solvent 1 An extraction solvent was prepared to satisfy 5 parts by weight of acetone, 5 parts by weight of ethyl acetate, and 90 parts by weight of propylene glycol monomethyl ether based on 100 parts by weight of the total extraction solvent.
  • Extraction solvent 2 An extraction solvent was prepared to satisfy 75 parts by weight of acetone, 20 parts by weight of ethyl acetate, and 5 parts by weight of propylene glycol monomethyl ether based on 100 parts by weight of the total extraction solvent in an Erlenmeyer flask.
  • a core-shell structure was formed with a composite preparation that satisfied the composition, content, and outer diameter of Table 1 below.
  • Example 1 Extract - 160g 1.02g 30nm 15g 40nm
  • Example 2 Extract - 160g 1.02g 38nm 15g 40nm
  • Example 3 Extract - 160g 1.02g 24nm 15g 40nm
  • Example 4 Extract - 260g 1.02g 30nm 15g 40nm Comparative Example 1 Extract - 160g 10g 24 nm 15g 40nm Comparative Example 2 Extract - 160g 1.02g 24nm 40g 40nm Comparative Example 3 Extract - 160g 1.02g 22nm 15g 40nm Comparative Example 4 Extract - 160g 1.02g 39.5nm 15g 40nm
  • composition containing the above complex preparation As additional mixing ingredients in the composition containing the above complex preparation, 0.1 g of BCAA mix, 0.1 g of calcium pantothenate, 0.1 g of nicotinic acid amide, 18 g of crystalline cellulose, 2 g of magnesium stearate, 1 g of hydroxypropyl methyl cellulose, and 3 g of calcium carboxymethyl cellulose are added.
  • the final compositions were prepared by mixing.
  • Rat pancreatic ⁇ -cells purchased from Biohermes (Shanghai, China) were supplemented with 11mM D-glucose, 10% fetal bovine serum, and 1% penicillin/streptomycin. Penicillin/streptomycin (Invitrogen Co., Grand Island, NY, USA), 0.05mM2-mercaptoethanol, 2mM L-glutamine, 10mM hydroxyethylpiperazineethane The cells were cultured in RPMI-1640 (Cellgro, Manassas, VA, USA) containing sulfonic acid (HEPES) and 1 mM sodium pyruvate at 37°C, 5% CO 2 and 95% humidity.
  • RPMI-1640 Cellgro, Manassas, VA, USA
  • 3T3-L1 preaidpocyte cells purchased from ATCC (American Type Culture Collection, USA) are subcultured in DMEM (containing 10% Bovine Serum, 100 units/ml penicillin, 100ug/ml streptomycin) medium and used to induce adiocyte differentiation and adipogenesis. .
  • DMEM containing 10% Bovine Serum, 100 units/ml penicillin, 100ug/ml streptomycin
  • Preadipocyte cells were used as a normal group, and as a control group, preadipocyte cells cultured to a post-confluent state after seeding were induced to differentiate for 3 days using Zenbio DM medium according to Zenbio manual, and then cultured once every two days using Zenbio AM medium. The adipocytes were exchanged and maintained for 4 days.
  • the experimental group was treated with Hispidulin, Synephrine, and P-Octopamine (Octopamine hydrochloride) at concentrations of 0, 5, 10, 20, or 40 ⁇ M each time DM and AM medium were treated, respectively, under the same culture conditions as the control group.
  • 3T3-L1 cells which are adipogenic cells derived from mice, we evaluated whether Hispidulin, Synephrine, and P-Octopamine (Octopamine hydrochloride) affect cell viability as follows.
  • 3T3-L1 preadipocyte cells of the preparation example were dispensed into a 96-well plate at 1 ⁇ 10 4 per well and cultured under the same conditions for 24 hours to stabilize the cells.
  • compositions of Examples 1 to 4 and Comparative Examples 1 to 4 were cultured under the same conditions for 24 hours after each treatment.
  • EZ-Cytox cell viability assay solution 100 ⁇ L; Daeil Lab Service Co., Ltd., Seoul
  • absorbance of the samples in the well plate was measured using a PowerWave
  • Figure 2 is a graph showing cell survival rate treated with compositions according to one embodiment of the present invention.
  • Figure 2 is a graph showing the survival rate results of 3T3-L1 cells treated with the compositions of Examples 1 to 4 and Comparative Examples 1 to 4 at a concentration of 200ug/ml.
  • Example Cell survival rate (%) Example 1 97.2 ⁇ 3.1 Example 2 96.5 ⁇ 2.5 Example 3 98.1 ⁇ 2.7 Example 4 95.2 ⁇ 4.2 Comparative Example 1 95.6 ⁇ 1.9 Comparative Example 2 98.2 ⁇ 2.3 Comparative Example 3 94.5 ⁇ 3.4 Comparative Example 4 96.9 ⁇ 2.3
  • 3T3-L1 cells were treated with the compositions of Examples 1 to 4 and Comparative Examples 1 to 4 each time they were treated with DM medium and AM medium under the same culture conditions as the control group in the preparation example. Then, to confirm the effect of the compositions of Examples 1 to 4 and Comparative Examples 1 to 4 on fat accumulation, the culture medium of each group of cells was removed and the amount of fat accumulated in the cells was compared and confirmed through the Oil red O test.
  • Figures 3 to 10 show images taken under a microscope at 20x magnification showing the results of intracellular fat accumulation (adipocyte differentiation inhibition rate) when 3T3-L1 cells cultured in a post confluent state were treated with compositions according to embodiments of the present invention. admit.
  • Figure 11 is a graph schematically illustrating the results of inhibiting intracellular adipocyte differentiation when treated with compositions according to embodiments of the present invention.
  • Figures 3 to 10 are images of 3T3-L1 cells treated with the compositions of Examples 1 to 4 and Comparative Examples 1 to 4 of the present invention at a concentration of 200ug/ml
  • Figure 11 is an image of Figures 3 to 10. This is a graph showing the results of intracellular fat accumulation (adipocyte differentiation inhibition rate), and Table 3 below shows the results of the graph in Figure 11 in a table.
  • Example Oil Red O (%) Example 1 38.1 ⁇ 3.6
  • Example 2 42.3 ⁇ 2.8
  • Example 3 38.9 ⁇ 4.1
  • Example 4 42.7 ⁇ 1.9 Comparative Example 1 68.2 ⁇ 2.4 Comparative Example 2 71.5 ⁇ 3.5 Comparative Example 3 65.8 ⁇ 1.5 Comparative Example 4 65.2 ⁇ 2.3
  • Example 1 of the present invention satisfies the weight ratio of the Garcinia cambogia extract, L-Arginine and L-Carnitine of 1:0.017:0.25, and the outer diameter: core of the composite preparation It was confirmed that the ratio of the outer diameter satisfied the ratio of 1:0.75, which was the most effective.
  • Example 4 Although evaluated better than Comparative Examples 1 to 4, in Example 4, the extraction solvent was changed to a different composition, so less effective substances were extracted into the extracted Garcinia cambogia extract, and Example 4 among Examples 1 to 4 was The inhibition rate of adipocyte differentiation was the poorest.
  • Comparative Example 1 and Comparative Example 2 each satisfied the outer diameter ratio of the present invention, but did not satisfy the composition ratio, and it was confirmed that the effect of inhibiting adipocyte differentiation was only insignificant, about 30%.
  • Comparative Examples 3 and 4 correspond to cases where the composition ratio of the present invention is satisfied but the external diameter ratio is not satisfied. That is, in Comparative Example 3, the outer diameter of the core is less than the range of the present invention, and in Comparative Example 4, the outer diameter of the core is greater than the range of the present invention.
  • Garcinia cambogia extract, L-Arginine, and L-Carnitine are included in the eluate at 37°C, pH 4.0, and water according to the Korean Pharmacopoeia Dissolution Test Method 2 (Paddle Method) After 1 hour, the L-Arginine accounts for 40 to 45% of the total weight of the active ingredient, and the Garcinia Cambogia extract and the L-Carnitine account for 5% of the total weight of the active ingredient after 1 hour. Since the range of ⁇ 15% was not satisfied, it was confirmed that the effect of inhibiting adipocyte differentiation was only minimal, around 30%.
  • the main purpose of the present invention is to discover a composition that has an excellent obesity suppression rate when the combination preparation satisfies a certain outer diameter ratio and at the same time satisfies a specific composition and content range.

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Abstract

La présente invention concerne une composition pharmaceutique et un aliment fonctionnel de santé pour la prévention de l'obésité, comprenant un extrait de Garcinia cambogia. En particulier, la composition pharmaceutique et l'aliment fonctionnel de santé comprennent, en tant que principe actif, un extrait de Garcinia cambogia, de la L-arginine, de la L-carnitine, ou similaire, qui sont des substances naturelles qui réduisent les effets secondaires provoqués par des médicaments synthétiques classiques et peuvent remplacer ces médicaments, et présentant ainsi une excellente efficacité dans la prévention et le traitement de l'obésité tout en réduisant au minimum les effets secondaires.
PCT/KR2023/005272 2022-05-02 2023-04-19 Composition pharmaceutique et aliment fonctionnel de santé pour la prévention de l'obésité comprenant un extrait de garcinia cambogia Ceased WO2023214716A1 (fr)

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KR102896033B1 (ko) 2022-12-22 2025-12-04 연세대학교 산학협력단 N-벤질퀴나졸린-4-아민 화합물을 포함하는, 비만 및 지질 관련 대사성 질환의 예방 또는 치료용 조성물
KR20240139645A (ko) 2023-03-14 2024-09-24 이화여자대학교 산학협력단 레바우디오사이드 a 및 네오헤스페리딘 디하이드로칼콘을 유효 성분으로 포함하는, 비만 및 지질 관련 대사성 질환의 예방 또는 치료용 조성물
KR102563745B1 (ko) * 2023-03-17 2023-08-07 원영국 가르시니아 캄보지아 추출액을 포함하는 비만 예방 또는 약학적 조성물 및 건강기능성 식품
KR20240149483A (ko) 2023-04-05 2024-10-15 연세대학교 산학협력단 Usp10 억제제를 유효성분으로 포함하는, 비만 및 지질 관련 대사성 질환의 예방 또는 치료용 조성물
KR102672768B1 (ko) * 2023-05-19 2024-06-07 최진원 한약재 혼합물을 포함하는 비만 예방 또는 약학적 조성물 및 이를 포함하는 주사제

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