WO2024242517A1 - Composition pharmaceutique ou de prévention de l'obésité comprenant un mélange de substances médicamenteuses orientales, et injection la comprenant - Google Patents

Composition pharmaceutique ou de prévention de l'obésité comprenant un mélange de substances médicamenteuses orientales, et injection la comprenant Download PDF

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WO2024242517A1
WO2024242517A1 PCT/KR2024/095440 KR2024095440W WO2024242517A1 WO 2024242517 A1 WO2024242517 A1 WO 2024242517A1 KR 2024095440 W KR2024095440 W KR 2024095440W WO 2024242517 A1 WO2024242517 A1 WO 2024242517A1
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pharmaceutical composition
preventing
treating obesity
obesity
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최진원
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    • 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)
    • A61K36/21—Amaranthaceae (Amaranth family), e.g. pigweed, rockwort or globe amaranth
    • 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)
    • A61K36/23—Apiaceae or Umbelliferae (Carrot family), e.g. dill, chervil, coriander or cumin
    • A61K36/232—Angelica
    • 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)
    • A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
    • A61K36/284—Atractylodes
    • 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)
    • A61K36/39—Convolvulaceae (Morning-glory family), e.g. bindweed
    • 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)
    • A61K36/46—Eucommiaceae (Eucommia family), e.g. hardy rubber tree
    • 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)
    • A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
    • A61K36/481—Astragalus (milkvetch)
    • 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)
    • A61K36/75—Rutaceae (Rue family)
    • A61K36/756—Phellodendron, e.g. corktree
    • 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)
    • A61K36/79—Schisandraceae (Schisandra family)
    • 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)
    • A61K36/80—Scrophulariaceae (Figwort family)
    • A61K36/804—Rehmannia
    • 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)
    • A61K36/81—Solanaceae (Potato family), e.g. tobacco, nightshade, tomato, belladonna, capsicum or jimsonweed
    • A61K36/815—Lycium (desert-thorn)
    • 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)
    • A61K36/88—Liliopsida (monocotyledons)
    • A61K36/894—Dioscoreaceae (Yam family)
    • A61K36/8945—Dioscorea, e.g. yam, Chinese yam or water yam

Definitions

  • the present invention relates to a pharmaceutical composition and injection for preventing obesity or containing a mixture of herbal medicines.
  • Obesity occurs when the supply of energy is much greater than the demand, resulting in excessive energy accumulation due to metabolic imbalance. It clinically causes or worsens various diseases, and diseases related to obesity include hypertension, atherosclerosis, diabetes, fatty liver, and gallstones.
  • endometrial cancer, gallbladder cancer, cervical cancer, ovarian cancer, and breast cancer are common in women, and the increase in incidence and mortality rate of endometrial cancer due to obesity is reported to be the most significant compared to other cancers.
  • the mortality rate is reported to be 1.3 times higher in obese people than in people of normal weight.
  • over-the-counter appetite suppressants such as caffeine, ephedrine and phenylpropanolamine (Acutrim, Dexatrim).
  • prescription medications including amphetamines, diethylpropion (Tenuate, mazindol (Mazanor, Sanorex), phentermine (Fastin, Ionamin), phenmetrazine (Preludin), phendimetrazine (Bontrol, Plegine, Adipost, Dital, Dyrexan, Melfiat, Prelu-2, Rexigen Forte), benzphetamines (Didrex), and fluoxetine (Prozac) are often used in the treatment of severely overweight and/or obese subjects or patients.
  • Topiramate (2,3,4,5-bis-O-(1-methylethylidene)- ⁇ -D-fructopyranose sulfamate) is a broad-spectrum neuroprotective agent approved by the FDA and regulatory agencies in many other countries for the treatment of certain seizure disorders and the prevention of migraine (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. C. Sachdeo (1998) Clin. Pharmacokinet.
  • topiramate is effective in the treatment of diabetes (U.S. Patent Nos. 7,109,174 and 6,362,220), neurological 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. 6,319,903), and hypertension (U.S. Patent No. 6,201,010).
  • diabetes U.S. Patent Nos. 7,109,174 and 6,362,220
  • neurological 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. 6,319,903
  • hypertension U.S. Patent No. 6,201,010
  • Fen-Phen containing 30 mg or 37.5 mg of phentermine hydrochloride
  • topiramate and phentermine which are included in Qsymia products, are also synthetic substances and are known to have side effects such as paresthesia, alopecia, parosmia, amenorrhea, and aphasia ([Korean J Obes 2015 March;24(1):17-27, Innov Clin Neurosci. 2011 Aug;8(8):14-16.]).
  • the inventors of the present invention have discovered a composition capable of eliminating or reducing the side effects of, and replacing, known conventional obesity prevention and treatment compositions, and thus aim to provide a pharmaceutical composition for obesity treatment and prevention that includes a natural substance capable of minimizing side effects as an active ingredient.
  • the pharmaceutical composition for preventing or treating obesity mentioned above is administered through intravenous injection with good absorbability, but in the case of intravenous injection, if air bubbles are included, embolism is also a problem.
  • One object of the present invention is to provide a pharmaceutical composition for preventing or treating obesity, comprising: an effective ingredient; a branched-chain amino acid (BCAA) comprising at least one selected from the group consisting of leucine, isoleucine, and valine; and a defoaming agent, wherein the effective ingredient comprises a mixture of herbal medicines, L-arginine, L-carnitine, and calcium pantothenate, the viscosity of the effective ingredient is 100 cPs or more and 1000 cPs or less, and the defoaming agent is 0.1 part by weight or more and 0.5 part by weight or less based on 100 parts by weight of the composition.
  • BCAA branched-chain amino acid
  • Another object of the present invention is to provide an injectable preparation for preventing or treating obesity comprising the above composition.
  • a pharmaceutical composition for preventing or treating obesity comprising: an active ingredient; a branched-chain amino acid (BCAA) comprising at least one selected from the group consisting of leucine, isoleucine, and valine; and a defoaming agent, wherein the active ingredient comprises a mixture of herbal medicines, L-arginine, L-carnitine, and calcium pantothenate, and the viscosity of the active ingredient is 100 cPs or more and 1000 cPs or less, and the defoaming agent is 0.1 part by weight or more and 0.5 part by weight or less based on 100 parts by weight of the composition.
  • BCAA branched-chain amino acid
  • a pharmaceutical composition for preventing or treating obesity wherein the defoaming agent comprises a non-polar oil or a polar oil.
  • a pharmaceutical composition for preventing or treating obesity wherein the non-polar oil includes at least one selected from mineral oil and silicone oil, and the polar oil includes at least one selected from the group consisting of fatty alcohols, fatty acids, and alkyl amines.
  • the herbal medicine mixture provides a pharmaceutical composition for preventing or treating obesity, which is prepared by processing and drying Schisandra chinensis and Tosa chinensis and then crushing them into a fine powder.
  • a pharmaceutical composition for preventing or treating obesity comprising: an active ingredient; a branched-chain amino acid (BCAA) comprising at least one selected from the group consisting of leucine, isoleucine, and valine; and a defoaming agent, wherein the active ingredient comprises a mixture of herbal medicines, L-arginine, L-carnitine, and calcium pantothenate, and the viscosity of the active ingredient is 100 cPs or more and 1000 cPs or less, and the defoaming agent is 0.1 part by weight or more and 0.5 part by weight or less based on 100 parts by weight of the composition.
  • BCAA branched-chain amino acid
  • the herbal medicine mixture can play a role in facilitating the basal metabolism of the human body and improving the absorption rate and function of ingested substances. By performing the said function, the basal metabolism of the human body is facilitated, and thereby the effect of preventing obesity is realized.
  • the herbal medicine mixture may be a mixture of at least one selected from the group consisting of Rehmannia glutinosa, Achyranthes root, Angelica gigas Nakai, Phellodendron amurense, Astragalus membranaceus, Astragalus membranaceus, Schisandra chinensis, White ginseng, White atractylodes, Sanyak root, Duzhong, Wolfberry and Tosa berry, ground into a fine powder after being processed and dried.
  • the herbal medicine mixture may be obtained by grinding Schisandra chinensis and Tosa chinensis into a fine powder after processing and drying them.
  • Schisandra chinensis (Turcz.) Baill.) belongs to the genus Schisandra and is one of the traditional medicinal plants with various therapeutic properties.
  • Schisandra chinensis fruit (Schisandrae Fructus) extracts and their components have various beneficial pharmacological effects, including anti-inflammation, anti-oxidation, neuroprotection, hepatoprotection, immunomodulation and antitumor effects.
  • Schisandra chinensis has the effect of facilitating human basal metabolism.
  • Cuscutae Semen is the seed of the annual climbing plant, ginseng, belonging to the Convolvulaceae family, which is sweet and very sweet and has a neutral nature. It contains resinous glycosides, amylase, about 40 mg% of provitamin A, and sugar. It is mainly known as a medicinal herb that protects the liver and kidneys, brightens the eyes, helps yang energy, and strengthens kidney function. Rather than having an effect of preventing obesity, it plays a role in supplementing kidney function when included as a medicinal herb.
  • L-carnitine has the chemical name ⁇ -hydroxy- ⁇ -N-trimethylaminobutyrate and is an amino acid-like substance structurally similar to choline.
  • L-carnitine is not a real vitamin because some of the body's requirements can be met through biosynthesis, and it can be said to be a nutrient in the form of vitamins, like choline, taurine, and inositol.
  • L-carnitine The most important biological mechanism of L-carnitine is its role as a transport molecule that smoothly transports fatty acids into mitochondria in the body and converts fat into cellular energy as an essential cofactor for fatty acid metabolism. This role improves intracellular fatty acid and sugar metabolism.
  • long-chain fatty acids are activated in the outer membrane of mitochondria and oxidized in the matrix of mitochondria. These long-chain fatty acids cannot pass through the inner membrane of mitochondria without a special transport mechanism, and L-carnitine acts as the transport mechanism. In this way, long-chain fatty acids activated in the outer membrane of mitochondria temporarily bind to the hydroxyl group of L-carnitine to form long-chain fatty acid acylcarnitine, which is transported into the mitochondria and metabolized.
  • L-carnitine has been proven to reduce lipid accumulation in the blood and tissues in various body conditions for weight loss, and it provides energy essential for muscles to work, thereby improving cardiac function, increasing oxygen intake, maintaining physical strength, and reducing fat.
  • the above L-carnitine may be L-carnitine tartrate, which has improved preservation properties by combining tartaric acid salt.
  • the pharmaceutical composition for preventing or treating obesity of the present invention comprises an active ingredient, and the active ingredient may comprise a mixture of herbal medicines, L-Arginine, L-Carnitine, and calcium pantothenate.
  • a pharmaceutical composition for preventing or treating obesity wherein the effective ingredients include a mixture of herbal medicines, L-Arginine, L-Carnitine, and calcium pantothenate in a weight ratio of 1:0.01 to 0.1:0.1 to 0.5:0.1 to 0.4.
  • the effective ingredient may be included in a weight ratio of the herbal medicine mixture, L-Arginine, L-Carnitine and calcium pantothenate of 1:0.01 to 0.1:0.1 to 0.5:0.1 to 0.4, preferably, a weight ratio of 1:0.015 to 0.05:0.25 to 0.3:0.2 to 0.3, for example, a weight ratio of 1:0.02:0.25:0.25.
  • the above herbal medicine mixture and the L-arginine may be included in a weight ratio of 1:0.01 to 0.1, and when the content of the L-arginine is less than 0.01 times the content of the herbal medicine mixture, the effect of inhibiting fat cell differentiation is reduced, and when it exceeds 0.1 times, the palatability is rapidly reduced due to a peculiar taste and smell, and problems such as stomachache, vomiting, diarrhea, and nausea may occur.
  • the above herbal medicine mixture and the L-carnitine may be included in a weight ratio of 1:0.1 to 0.5, and when the content of the L-carnitine is less than 0.1 times the content of the herbal medicine mixture, there is almost no effect of inhibiting adipocyte differentiation, and when it exceeds 0.5 times, the palatability is rapidly reduced due to a peculiar taste and odor, and problems such as stomachache, vomiting, diarrhea, and nausea may occur.
  • the viscosity of the effective ingredient may be 100 cPs or more and 1000 cPs or less, preferably 150 cPs or more and 800 cPs or less, and more preferably 200 cPs or more and 500 cPs or less.
  • the pharmaceutical composition of the present invention is characterized by including the above-mentioned effective ingredient in a premixed form. That is, premixing the effective ingredient does not simply mean mixing the composition included in the effective ingredient, but rather means adjusting the viscosity to the above-mentioned range through premixing.
  • a Garcinia cambogia extract obtained by extracting Garcinia cambogia with an extraction solvent may be further included.
  • compound as used in the present invention means a result obtained by performing fractionation to separate a specific component or a specific group of components from a mixture containing various components.
  • the separation method for obtaining the compound is not particularly limited, and can be performed according to a method commonly used in the relevant technical field.
  • a non-limiting example of the separation method may include a method of treating a natural substance extract with a predetermined solvent to obtain a compound from the extract.
  • extract includes the extract itself and all formulations that can be formed using the extract, such as an extract obtained by extraction treatment, a diluted or concentrated extract, a dried product obtained by drying the extract, a adjusted or purified product of the extract, or a mixture thereof.
  • the extract in this specification follows the dictionary definition and may mean a liquid substance extracted from a specific substance or state.
  • the extract in this specification follows the dictionary definition and means something obtained by concentrating a specific component in an extract liquid, separating a specific active ingredient with a suitable solvent, completely or mostly evaporating the solvent, and adjusting the remaining lump or powder according to a standard.
  • the extract can be used to mean all three forms, namely, a semi-fluid or syrupy form, a pill or solid form, and a dried powder.
  • drying of the extract can be carried out by a known method within a range where useful components are not destroyed from the collected natural material, and can be carried out, for example, by a method of natural drying in a shaded area.
  • crushing or pulverizing can be carried out by crushing or pulverizing to a degree that useful components of the plant can be sufficiently extracted during the subsequent extraction process to make it powdered.
  • the drying and crushing or pulverizing processes can be carried out in reverse order or repeatedly, as necessary.
  • the extraction method is not particularly limited, and extraction can be performed according to a method commonly used in the relevant technical field.
  • Non-limiting examples of the extraction method include hot water extraction, ultrasonic extraction, filtration, and reflux extraction, and these can be performed alone or in combination of two or more methods.
  • the above Garcinia cambogia extract is a powder form obtained by freeze-drying the peel of the Garcinia cambogia fruit, crushing it to 100 mesh or smaller, extracting it at a temperature of 80°C or higher with 70% extraction solvent, and then concentrating and freeze-drying it.
  • the extraction solvent for making the Garcinia cambogia according to the present application into an extract comprises a modified alkylene glycol; and a solvent having a boiling point of 90°C or lower, and the extraction solvent comprises 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 the solvent having a boiling point of 90°C or lower, thereby providing a pharmaceutical composition for preventing or treating obesity.
  • the alkylene group may include methylene, ethylene, propylene, butylene, etc.
  • the appropriate number of alkyl groups may include an alkylene group having 1 to 30 carbon atoms, more preferably an alkylene group having 1 to 20 carbon atoms, and 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 generally 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.
  • the organic solvent includes a modified alkylene glycol; and a solvent having a boiling point of 90°C or lower, and may include 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 the solvent having a boiling point of 90°C or lower.
  • the organic solvent includes a modified alkylene glycol; and a solvent having a boiling point of 90°C or lower, and may contain 80 parts by weight or more and 95 parts by weight or less of the modified alkylene glycol, preferably 85 parts by weight or more and 95 parts by weight or less, and more preferably 90 parts by weight or more and 95 parts by weight or less.
  • the organic solvent includes a modified alkylene glycol; and a solvent having a boiling point of 90°C or lower, and may be included in an amount of 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, and more preferably 5 parts by weight or more and 10 parts by weight or less, of the solvent having a boiling point of 90°C or lower.
  • a pharmaceutical composition for preventing or treating obesity wherein the defoaming agent comprises a non-polar oil or a polar oil, wherein the non-polar oil comprises at least one selected from mineral oil and silicone oil, and the polar oil comprises at least one selected from the group consisting of fatty alcohols, fatty acids, and alkyl amines.
  • the pharmaceutical composition of the present invention is used as an injection, not an oral administration, and particularly for intravenous injection.
  • intravenous injection since the effective ingredient is directly administered through the blood vessel, it is characterized by a high absorption rate compared to oral or other intramuscular injections, so the effect appears immediately.
  • the injection since the injection is administered into the vein, if air bubbles are included accordingly, serious side effects such as embolism may occur.
  • the pharmaceutical composition according to the present application since the content of the above-mentioned bubble removing agent is included, air bubbles can be removed when the injection is administered, thereby eliminating the problem of embolism, and also having the characteristic of ensuring the effect of preventing obesity.
  • composition of the present invention may further include at least one of Catechin, Cathinone, Tryptamine, P-Octopamine, P-Tyramine, Synephrine, and Ephedrine, which are norepinephrine releasing substances.
  • the norepinephrine acts as a neurotransmitter at the neural synapses between the brain and muscles, and as a hormone that regulates fuel metabolism in the liver and muscles.
  • catechin can be extracted from the tea tree ( Camellia sienesis ) and can act as a substance for preventing and treating obesity by inhibiting the COMT (catechol O-methyltransferase) enzyme, increasing norepinephrine in the synaptic gap, and thus being effective in energy activity ([Korean J Clin Pharm 2018;28(4):342-346, ARYA Atheroscler. 2014 Jan; 10(1): 55-58.]).
  • COMT catechol O-methyltransferase
  • the above cathinone can be extracted from Catha edulis (Khat), and like amphetamine, it releases catecholamines, such as dopamine, norepinephrine, and epinephrine, through TAAR1 activation, and acts on alpha and beta adrenergic receptors to exhibit an appetite suppressing effect.
  • the cathinone has a stronger CNS activating 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 above tryptamine can be extracted from Vachellia aroma , and can act as a substance for preventing and treating obesity with a complex mechanism that includes the effect of reducing fasting blood sugar in the liver by increasing insulin in the pancreas through the TAAR1 receptor, delaying the time of food emptying from the stomach, increasing GLP-1&PYY, and reducing glucose excretion from the body ([Pharmacology of human trace amine-associated receptors: Therapeutic opportunities and challenges], [Pharmacology & Therapeutics, Volume 180, December 2017, Pages 161-180]).
  • the above P-octopamine can be extracted from bitter orange ( Citrus aurantium ) and increases serotonin release through the TAAR1 receptor, thereby increasing satiety and reducing food intake, and thus can act as a substance for preventing and treating obesity.
  • P-octopamine acts on the Beta 3 Adrenergic receptor of adipocytes to activate the Beta 3 Adrenergic receptor, induces the conversion of white fat into brown fat through binding activation of norepinephrine and activation of UCP-1 protein of adipocytes, and increases energy consumption through thermogenesis by brown fat, so it can act as a substance for preventing and treating obesity ([Pharmacology of human trace amine-associated receptors: Therapeutic opportunities and challenges], [Pharmacology & Therapeutics, Volume 180, December 2017, Pages 161-180]).
  • the above P-tyramine can be extracted from Bitter Orange ( Citrus aurantium ) or Musa sapientum L , and can act as a substance for preventing and treating obesity with a complex mechanism that includes the effect of reducing fasting blood sugar in the liver by increasing insulin in the pancreas through the TAAR1 receptor, delaying the time of food emptying from the stomach, increasing GLP-1&PYY, and reducing glucose excretion from the body ([Pharmacology of human trace amine-associated receptors: Therapeutic opportunities and challenges], [Pharmacology & Therapeutics, Volume 180, December 2017, Pages 161-180]).
  • the above synephrine can be extracted from bitter orange ( Citrus aurantium ), and can act as a substance for preventing and treating obesity by releasing catecholamines through TAAR1 activation, activating lipolysis by binding to the ⁇ 3 adrenergic receptor, and increasing norepinephrine to be effective in energy activity ([Phytother Res. 2017 Oct; 31(10): 1463-1474.]).
  • the above ephedrine can be extracted from Ephedra sinica , and acts mainly on ⁇ and ⁇ adrenergic receptors, stimulates the sympathetic nerves, increases norepinephrine in the synaptic gap, and is effective in energy activity, so it can act as a substance for preventing and treating obesity ([Anesth Prog. 2012 Winter; 59(4): 159-169.]).
  • the pharmaceutical composition of the present invention contains catechin as a norepinephrine releasing substance.
  • the pharmaceutical composition for preventing or treating obesity of the present invention may contain the herbal medicine mixture, L-arginine, the L-carnitine, and the catechin in a weight ratio of 1:0.01 to 0.1:0.1 to 0.5:0.5 to 2.
  • the above herbal medicine mixture and the catechin may be included in a weight ratio of 1:0.5 to 1:2, and when the content of the catechin is less than 0.5 times the content of the herbal medicine mixture, the effect of inhibiting adipocyte differentiation is reduced, and when it exceeds 2 times, 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 to maximize the effect of inhibiting adipocyte differentiation while preventing or minimizing cytotoxicity.
  • the composition may include branched-chain amino acids (BCAA) including at least one selected from the group consisting of leucine, isoleucine and valine, calcium pantothenate, nicotinamide, crystalline cellulose, magnesium stearate, hydroxypropylmethylcellulose and calcium carboxymethylcellulose.
  • BCAA branched-chain amino acids
  • the above branched-chain amino acid is one of the essential amino acids that is closely related to muscles, and the above calcium pantothenate (molecular formula C 18 H 32 O 10 N 2 Ca) is a white powder that is odorless and slightly bitter in taste, a calcium salt fortifier that acts as a coenzyme in the body and is necessary for normalizing tissue function and maintaining physical growth and health.
  • the above nicotinic acid amide is a type of vitamin, and the above vitamins are added for obesity prevention and dieting, and refer to vitamins B1, B2, B6, B12, C, D3, and nicotinic acid amide.
  • Vitamins B, C, D, and nicotinic acid amide act as coenzymes of the TCA cycle, which breaks down glucose to create energy. If there are no vitamins, this process cannot proceed, and nutrients are not consumed as energy, but are converted to body fat and stored in the body. In other words, if there are not enough vitamins, the food you eat is not used as energy, but is stored in the body, which ultimately leads to obesity.
  • the above-mentioned crystalline cellulose is an additive used as an anti-caking agent, stabilizer, emulsifier, and dietary fiber agent in food
  • the above-mentioned magnesium stearate provides mineral components by supplying magnesium
  • the above-mentioned hydroxypropyl methyl cellulose (hypromellose, HPMC) and the above-mentioned carboxymethyl cellulose calcium act as viscosity regulators.
  • composition may further include additives such as zinc oxide and silicon dioxide.
  • the term “prevention” refers to any act of suppressing or delaying obesity
  • the term “treatment” refers to any act of improving or beneficially changing the symptoms of a subject suspected of obesity or developing obesity.
  • the pharmaceutical composition may be provided as a pharmaceutical composition containing an active ingredient alone, or including one or more pharmaceutically acceptable carriers, excipients or diluents.
  • pharmaceutically acceptable refers to a composition that is physiologically acceptable and does not typically cause an allergic reaction or similar reaction when administered to a human.
  • the pharmaceutical composition may be provided in combination with a conventionally known anti-obesity agent. That is, the pharmaceutical composition may be administered in combination with a known compound having an effect of preventing or treating obesity.
  • administration means introducing a given substance to an individual in an appropriate manner
  • individual means all animals, including rats, mice, and livestock, including humans, that have developed or may develop obesity.
  • a specific example may be a mammal, including humans.
  • obesity means something caused by energy imbalance, and the causes of obesity are complexly related to hormonal changes, genetics, mental health problems, and socioeconomic factors. Specifically, it means something that can be caused by energy imbalance, genetic factors, neuroendocrine factors, and environmental factors.
  • the route of administration of the above pharmaceutical composition is not limited to these, but in the case of the present application, it is used as an injection, and particularly for intravenous injection.
  • Non-aqueous solvents and suspensions may include propyleneglycol, polyethylene glycol, vegetable oils such as olive oil, and injectable esters such as ethyl oleate.
  • Suppository bases may include witepsol, macrogol, Tween 61, cacao butter, laurin butter, glycerogelatin, and the like.

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  • Health & Medical Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Alternative & Traditional Medicine (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Medical Informatics (AREA)
  • Medicinal Chemistry (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

La présente invention concerne une composition pharmaceutique ou de prévention de l'obésité et une injection comprenant un mélange de substances médicamenteuses orientales.
PCT/KR2024/095440 2023-05-19 2024-02-26 Composition pharmaceutique ou de prévention de l'obésité comprenant un mélange de substances médicamenteuses orientales, et injection la comprenant Ceased WO2024242517A1 (fr)

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KR1020230064716A KR102672768B1 (ko) 2023-05-19 2023-05-19 한약재 혼합물을 포함하는 비만 예방 또는 약학적 조성물 및 이를 포함하는 주사제
KR10-2023-0064716 2023-05-19

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Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20110121246A (ko) * 2010-04-30 2011-11-07 오숙자 비만개선 다이어트용 웰빙 한방식품 및 그 제조방법
KR20130075036A (ko) * 2011-12-27 2013-07-05 이강수 비만 억제 또는 개선용 식품 조성물 및 그의 제조 방법
KR20140074422A (ko) * 2012-12-07 2014-06-18 주식회사 대화약품 숫누에번데기를 주원료로 한 환(丸) 제품의 제조방법
KR20150128912A (ko) * 2013-03-15 2015-11-18 트레인 인터내셔날 인코포레이티드 윤활제 기포제거 첨가제 및 조성물
KR102461437B1 (ko) * 2022-05-02 2022-11-02 최진원 가르시니아 캄보지아 추출액을 포함하는 비만 예방 또는 약학적 조성물 및 건강기능성 식품

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20040097813A (ko) 2003-05-13 2004-11-18 (주)뉴로타이드 식욕억제, 체지방 감소 및 배변 활성화등 3가지 기능을 갖는 항비만 기능성 조성물

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20110121246A (ko) * 2010-04-30 2011-11-07 오숙자 비만개선 다이어트용 웰빙 한방식품 및 그 제조방법
KR20130075036A (ko) * 2011-12-27 2013-07-05 이강수 비만 억제 또는 개선용 식품 조성물 및 그의 제조 방법
KR20140074422A (ko) * 2012-12-07 2014-06-18 주식회사 대화약품 숫누에번데기를 주원료로 한 환(丸) 제품의 제조방법
KR20150128912A (ko) * 2013-03-15 2015-11-18 트레인 인터내셔날 인코포레이티드 윤활제 기포제거 첨가제 및 조성물
KR102461437B1 (ko) * 2022-05-02 2022-11-02 최진원 가르시니아 캄보지아 추출액을 포함하는 비만 예방 또는 약학적 조성물 및 건강기능성 식품

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