WO2018177340A1 - 用于减少体重及减少体脂肪的组合物及其医药品与应用 - Google Patents
用于减少体重及减少体脂肪的组合物及其医药品与应用 Download PDFInfo
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- WO2018177340A1 WO2018177340A1 PCT/CN2018/080968 CN2018080968W WO2018177340A1 WO 2018177340 A1 WO2018177340 A1 WO 2018177340A1 CN 2018080968 W CN2018080968 W CN 2018080968W WO 2018177340 A1 WO2018177340 A1 WO 2018177340A1
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- polyoxyethylene
- stearate
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- fat
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Definitions
- the invention relates to a composition, in particular a composition comprising epigallocatechin gallate, curcumin, and an excipient; the invention relates to the use of a composition, in particular by said combination
- the invention relates to a medicament for preparing a medicament for reducing body weight and body fat; the invention relates to a medicament comprising the composition, in particular to a medicament for reducing body weight and reducing body fat; the invention relates to a The use of the pharmaceutical product, in particular, for the use of an effective amount of the medicament for reducing body weight, reducing body fat, treating fatty liver, or treating nonalcoholic steatohepatitis.
- Obesity is a state of the body that has accumulated too much body fat and has a negative impact on health, which may lead to shortened life spans and various health problems.
- body mass index (BMI) greater than 25 is defined as overweight
- BMI greater than 30 is defined as obesity
- some East Asian countries adopt more stringent standards, such as Taiwan health benefits.
- Taiwanese adults had a BMI of 27, which was obese, and 24, BMI ⁇ 27, was overweight.
- Taiwan health benefits In April 2002, the Ministry of Health announced that Taiwanese adults had a BMI of 27, which was obese, and 24, BMI ⁇ 27, was overweight.
- Taiwan Health In April 2002, the Ministry of Health announced that Taiwanese adults had a BMI of 27, which was obese, and 24, BMI ⁇ 27, was overweight.
- the World Health Organization, the US Food and Drug Administration (FDA), the National Institutes of Health (NIH), and the American Medical Association now treat obesity as a Chronic diseases caused by environmental and genetic factors.
- FDA US Food and Drug
- Synthetic drugs currently used for weight loss or weight loss still have varying degrees of cardiovascular risk and safety concerns.
- plant extracts used for weight loss or weight loss often have low bioavailability and are ineffective. problem. Therefore, there is still a lack of a weight loss or weight loss drug with higher safety, low side effects, no cardiovascular risk concerns, high bioavailability, effective weight loss and body fat, and reduced cardiovascular risk.
- the present invention provides a plant extract composition for reducing body weight and body fat comprising green tea extract and turmeric extract, based on the total weight of the plant extract composition, green tea extract
- the weight percentages with the turmeric extract are 30% to 75% and 20% to 55%, respectively.
- the weight percentage of the green tea extract and the turmeric extract is 20% to 91% and 9% to 80%, respectively, based on the total weight of the plant extract composition.
- the weight percentage of the green tea extract and the turmeric extract is 40% to 67% and 33% to 60%, respectively.
- the weight ratio of the green tea extract to the turmeric extract in the plant extract composition is from 1:4 to 10:1.
- the weight ratio of the green tea extract to the turmeric extract is from 2:3 to 2:1.
- the plant extract composition of the present invention further comprises resveratrol, and the resveratrol comprises from greater than 0% to 30% by weight of the total composition.
- the turmeric extract refers to a turmeric component mixture extracted by any solvent and any extraction method, a commercially available turmeric extract, and any one containing at least 75% by weight of turmeric.
- resveratrol refers to resveratrol obtained from natural plant extract or commercially available.
- the resveratrol has a purity of from 90% to 100% by weight.
- the green tea extract refers to a mixture of green tea ingredients extracted from any solvent and any extraction method or a commercially available green tea extract, preferably, at least 45% ( Percent by weight of a mixture of epigallocatechin gallate (EGCG), any mixture comprising at least 90% by weight of total catechins, or a commercially available epigal canthus Camelliate gallate.
- EGCG epigallocatechin gallate
- the total percentage of total catechins and curcumin is from 20% to 91% and from 9% to 80%, based on the total weight of the plant extract composition.
- the weight percentages of total catechins and curcumin are 40% to 67% and 33% to 60%, respectively.
- the weight ratio of total catechin to curcumin in the plant extract composition is from 1:4 to 10:1.
- the weight ratio of total catechin to curcumin is from 2:3 to 2:1.
- the invention further provides a composition for reducing body weight or body fat comprising:
- a weight loss or fat loss active ingredient composition comprises epigallocatechin gallate (EGCG) and curcumin;
- EGCG epigallocatechin gallate
- curcumin curcumin
- the excipient comprises glyceryl dibehenate, polyoxyethylene stearates, polysorbate 80 mixture, vitamin E polyethylene glycol succinate, At least one or a combination of glyceryl monostearate and Oleoyl polyoxyl-6 glycerides; moreover, the polysorbate 80 mixture comprises polysorbate Alcohol ester 80 and magnesium aluminometasilicate.
- the composition for reducing body weight or body fat further comprises at least one of Glyceryl Palmitostearate, polysorbate 20, poloxamer, and polyethylene glycol, or a combination thereof.
- the composition for reducing body weight or body fat further comprises piperine.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and based on the total weight of the composition for reducing body weight or body fat, the polyoxyethylene (32) The weight percentage of stearate is from 0.1% to 20%; or, based on the total weight of the composition for reducing body weight or body fat, the weight percentage of the polysorbate 80 mixture is from 0.5% to 20% %; or alternatively, the polyoxyethylene stearate is polyoxyethylene (40) stearate, and based on the total weight of the composition for reducing body weight or body fat, the polyoxyethylene (40) The weight percentage of stearate is from 0.005% to 6.7%.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and based on the total weight of the composition for reducing body weight or body fat, the polyoxyethylene (32) The percentage by weight of stearate is from 1% to 15%; or, based on the total weight of the composition for reducing body weight or body fat, the weight percentage of the polysorbate 80 mixture is from 1% to 15%. %; or alternatively, the polyoxyethylene stearate is polyoxyethylene (40) stearate, and based on the total weight of the composition for reducing body weight or body fat, the polyoxyethylene (40) The weight percentage of stearate is from 0.01% to 3.3%.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and based on the total weight of the composition for reducing body weight or body fat, the polyoxyethylene (32)
- the percentage by weight of stearate is from 1% to 10%; or, based on the total weight of the composition for reducing body weight or body fat, the weight percentage of the polysorbate 80 mixture is from 3% to 10% %; or alternatively, the polyoxyethylene stearate is polyoxyethylene (40) stearate, and based on the total weight of the composition for reducing body weight or body fat, the polyoxyethylene (40)
- the weight percentage of stearate is 0.05% to 1%.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate, and the ratio of the weight of the curcumin to the weight of the polyoxyethylene (32) stearate is 5.3 to 26.7. Or the ratio of the weight of the curcumin to the weight of the polysorbate 80 mixture is from 2 to 8.9; or the polyoxyethylene stearate is polyoxyethylene (40) stearate, and The ratio of the weight of the curcumin to the weight of the polyoxyethylene (40) stearate is 40 to 533.3; or alternatively, the polyoxyethylene stearate is polyoxyethylene (32) stearate, and The ratio of the weight of the weight loss or fat-reducing active ingredient composition and the weight of the polyoxyethylene (32) stearate is 9.5 to 47.5; or is the weight of the weight-reducing or fat-reducing active ingredient composition and The ratio of the weight of the polysorbate 80 mixture is 3.6 to 15.8; or alternatively, the polyoxyethylene stearate is polyoxyethylene (40) stearate, and
- the composition for reducing body weight or body fat further comprises at least one of mannitol, microcrystalline cellulose, sodium lauryl sulfate, and crosslinked methylcellulose, or a combination thereof.
- the ratio of the weight of the curcumin to the weight of the epigallocatechin gallate is from 3.2 to 0.32; or, based on the total weight of the weight loss or fat-reducing active ingredient composition, the table
- the weight percentage of gallocatechin gallate is 23.8% to 75.8% and the weight percentage of curcumin is 24.2% to 76.2%.
- the ratio of the weight of the curcumin to the weight of the epigallocatechin gallate is from 3.2 to 0.4; or, based on the total weight of the weight loss or fat-reducing active ingredient composition, the table
- the weight percentage of gallocatechin gallate is 23.8% to 71.4% and the weight percentage of curcumin is 28.6% to 76.2%.
- the weight loss or fat reducing active ingredient composition further comprises resveratrol.
- the active pharmaceutical ingredients of the present invention refer to a combination of at least two "ingredients which are applied to an individual to reduce the body weight or visceral fat of the individual".
- the invention further provides a method of reducing body weight or body fat comprising applying a composition to a body, wherein the composition comprises:
- a weight loss or fat loss active ingredient composition comprises an epigallocatechin gallate (EGCG) and a curcumin;
- EGCG epigallocatechin gallate
- curcumin curcumin
- the excipient comprises glyceryl dibehenate, polyoxyethylene stearates, polysorbate 80 mixture, vitamin E polyethylene glycol succinate, At least one or a combination of glyceryl monostearate and Oleoyl polyoxyl-6 glycerides; moreover, the polysorbate 80 mixture comprises polysorbate Alcohol ester 80 and magnesium aluminometasilicate.
- the composition further comprises at least one of Glyceryl Palmitostearate, polysorbate 20, poloxamer, and polyethylene glycol, or a combination thereof.
- the composition further comprises piperine.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and the weight percent of the polyoxyethylene (32) stearate is based on the total weight of the composition. 0.1% to 20%; or, based on the total weight of the composition, the polysorbate 80 mixture is 0.5% to 20% by weight; or alternatively, the polyoxyethylene stearate is polyoxyl Ethylene (40) stearate, and the weight percent of the polyoxyethylene (40) stearate is from 0.005% to 6.7%, based on the total weight of the composition.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and the weight percent of the polyoxyethylene (32) stearate is based on the total weight of the composition. 1% to 15%; or, based on the total weight of the composition, the polysorbate 80 mixture is 1% to 15% by weight; or alternatively, the polyoxyethylene stearate is polyoxyl Ethylene (40) stearate, and the weight percent of the polyoxyethylene (40) stearate is from 0.01% to 3.3% based on the total weight of the composition.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and the weight percent of the polyoxyethylene (32) stearate is based on the total weight of the composition. 1% to 10%; or, based on the total weight of the composition, the polysorbate 80 mixture is 3% to 10% by weight; or alternatively, the polyoxyethylene stearate is polyoxyl Ethylene (40) stearate, and the weight percent of the polyoxyethylene (40) stearate is from 0.05% to 1%, based on the total weight of the composition.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate, and the ratio of the weight of the curcumin to the weight of the polyoxyethylene (32) stearate is 5.3 to 26.7. Or the ratio of the weight of the curcumin to the weight of the polysorbate 80 mixture is from 2 to 8.9; or the polyoxyethylene stearate is polyoxyethylene (40) stearate, and The ratio of the weight of the curcumin to the weight of the polyoxyethylene (40) stearate is 40 to 533.3; or alternatively, the polyoxyethylene stearate is polyoxyethylene (32) stearate, and The ratio of the weight of the weight loss or fat-reducing active ingredient composition and the weight of the polyoxyethylene (32) stearate is 9.5 to 47.5; or is the weight of the weight-reducing or fat-reducing active ingredient composition and The ratio of the weight of the polysorbate 80 mixture is 3.6 to 15.8; or alternatively, the polyoxyethylene stearate is polyoxyethylene (40) stearate, and
- the composition further comprises at least one of mannitol, microcrystalline cellulose, sodium lauryl sulfate, and crosslinked methylcellulose, or a combination thereof.
- the ratio of the weight of the curcumin to the weight of the epigallocatechin gallate is from 3.2 to 0.32; or, based on the total weight of the weight loss or fat-reducing active ingredient composition, the table
- the weight percentage of gallocatechin gallate is 23.8% to 75.8% and the weight percentage of curcumin is 24.2% to 76.2%.
- the ratio of the weight of the curcumin to the weight of the epigallocatechin gallate is from 3.2 to 0.4; or, based on the total weight of the weight loss or fat-reducing active ingredient composition, the table
- the weight percentage of gallocatechin gallate is 23.8% to 71.4% and the weight percentage of curcumin is 28.6% to 76.2%.
- the weight loss or fat reducing active ingredient composition further comprises resveratrol.
- the composition is administered to the subject in an oral manner.
- the individual is a normal-weight individual, an overweight individual, an obese individual, an individual with fatty liver, or an individual having non-alcoholic steatohepatitis (NASH).
- NASH non-alcoholic steatohepatitis
- the present invention further provides a method of treating fatty liver or nonalcoholic steatohepatitis comprising administering a composition to an individual having fatty liver or having nonalcoholic steatohepatitis, wherein the composition comprises:
- a weight loss or fat-reducing active ingredient composition comprises an epigallocatechin gallate (EGCG) and a curcumin;
- EGCG epigallocatechin gallate
- curcumin curcumin
- the excipient comprises glyceryl dibehenate, polyoxyethylene stearates, polysorbate 80 mixture, vitamin E polyethylene glycol succinate, At least one or a combination of glyceryl monostearate and Oleoyl polyoxyl-6 glycerides; moreover, the polysorbate 80 mixture comprises polysorbate Alcohol ester 80 and magnesium aluminometasilicate.
- the composition further comprises at least one of Glyceryl Palmitostearate, polysorbate 20, poloxamer, and polyethylene glycol, or a combination thereof.
- the composition further comprises piperine.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate and the weight percent of the polyoxyethylene (32) stearate is based on the total weight of the composition. 0.1% to 20%; or, based on the total weight of the composition, the polysorbate 80 mixture is 0.5% to 20% by weight; or alternatively, the polyoxyethylene stearate is polyoxyl Ethylene (40) stearate, and the weight percent of the polyoxyethylene (40) stearate is from 0.005% to 6.7%, based on the total weight of the composition.
- the polyoxyethylene stearate is polyoxyethylene (32) stearate, and the ratio of the weight of the curcumin to the weight of the polyoxyethylene (32) stearate is 5.3 to 26.7. Or the ratio of the weight of the curcumin to the weight of the polysorbate 80 mixture is from 2 to 8.9; or the polyoxyethylene stearate is polyoxyethylene (40) stearate, and The ratio of the weight of the curcumin to the weight of the polyoxyethylene (40) stearate is 40 to 533.3; or alternatively, the polyoxyethylene stearate is polyoxyethylene (32) stearate, and The ratio of the weight of the weight loss or fat-reducing active ingredient composition and the weight of the polyoxyethylene (32) stearate is 9.5 to 47.5; or is the weight of the weight-reducing or fat-reducing active ingredient composition and The ratio of the weight of the polysorbate 80 mixture is 3.6 to 15.8; or alternatively, the polyoxyethylene stearate is polyoxyethylene (40) stearate, and
- the composition further comprises at least one of mannitol, microcrystalline cellulose, sodium lauryl sulfate, and crosslinked methylcellulose, or a combination thereof.
- the ratio of the weight of the curcumin to the weight of the epigallocatechin gallate is from 3.2 to 0.32; or, based on the total weight of the weight loss or fat-reducing active ingredient composition, the table
- the weight percentage of gallocatechin gallate is 23.8% to 75.8% and the weight percentage of curcumin is 24.2% to 76.2%.
- the ratio of the weight of the curcumin to the weight of the epigallocatechin gallate is from 3.2 to 0.4; or, based on the total weight of the weight loss or fat-reducing active ingredient composition, the table
- the weight percentage of gallocatechin gallate is 23.8% to 71.4% and the weight percentage of curcumin is 28.6% to 76.2%.
- the composition is administered orally to the individual having fatty liver or having nonalcoholic steatohepatitis.
- the present invention further provides a method of producing a plant extract composition comprising green tea extract and turmeric extract, comprising: a plant extract composition comprising green tea extract and turmeric extract and a pharmaceutically acceptable salt composition
- a pharmaceutically acceptable stabilizer or pharmaceutically acceptable excipient is mixed into a capsule, a lozenge or a coated ingot or an infusion.
- the method further comprises adding resveratrol to form a plant extract composition comprising green tea extract, turmeric extract and resveratrol.
- the stabilizer includes, but is not limited to, xylitol, sorbitol, polydextrose, isomalt, and dextrose.
- the present invention further provides the use of the plant extract composition for reducing body weight and body fat in the preparation of a medicament for reducing body weight and body fat.
- the present invention further provides a pharmaceutical for reducing body weight and body fat comprising an effective amount of the plant extract composition for reducing body weight and body fat, and a pharmaceutically acceptable excipient.
- the pharmaceutical product further comprises resveratrol effective to reduce body weight and body fat dosage.
- the "pharmaceutically acceptable excipient” or “excipient” includes, but is not limited to, a disintegrant, a binder, a filler, a lubricant (lubricant). ), a suspending agent, a solubilizer, and a glidant.
- the pharmaceutically acceptable excipient or excipient includes, but is not limited to, piperine, Glyceryl dibehenate (also known as glycerol mono docate) Glyceryl monobehenate), the main component of Compritol 888 ATO, Oleoyl polyoxyl-6 glycerides (also known as Oleoyl Macrogolglycerides, the main component of Labrafil M 1944 CS), Glyceryl Palmitostearate Precirol ATO 5 main component), Magnesium Stearate, Poloxamer 188, Labrasol, Poloxamer 407, Polyethylene glycol 6000 (PEG 6000), glyceryl monostearate (IMWITOR) 491 main component), Sodium dodecyl sulfate, Sepitrap 80 (a polysorbate 80 mixture, comprising polysorbate 80 and magnesium aluminometasilicate), polyethylene glycol 400 ( PEG 400), polysorbate 20, polyoxyethylene stearates, poly
- the addition of glyceryl dioxalate in the embodiment of the present invention refers to, for example, direct addition of glyceryl disorbate or addition of Compritol 888 ATO; in the embodiment of the present invention, oleic acid polyethylene glycol-6 glyceride is added.
- the addition of Glyceryl Palmitostearate in the examples of the invention refers, for example, to the direct addition of Glyceryl Palmitostearate or the addition of Precirol ATO 5;
- the addition of glyceryl monostearate refers, for example, to the direct addition of glyceryl monostearate or the addition of IMWITOR 491;
- the addition of a mixture of polysorbate 80 in the examples of the invention means, for example, the addition of any of the polysorbate 80 and Mixture of magnesium aluminum silicate or addition of Sepitrap 80;
- addition of polyoxyethylene (32) stearate in the examples of the present invention means, for example, direct addition of polyoxyethylene (32) stearate or addition 48/16;
- the addition of vitamin E polyethylene glycol succinate in the examples of the present invention refers to, for example, direct addition of vitamin E polyethylene glycol succinate or
- the excipient is present in an amount of from 10 to 60% by weight based on the total weight of the composition.
- the weight percentage of piperine is from 0.1 to 1% based on the total weight of the composition.
- the weight percentage of glycerol dioxalate is from 1 to 10% based on the total weight of the composition.
- the weight percentage of glyceryl dibehenate is from 1 to 3%.
- the weight percentage of Oleoyl Macrogolglycerides is from 10 to 99%, based on the total weight of the composition.
- Glyceryl Palmitostearate is present in an amount of from 1 to 3% by weight based on the total weight of the composition.
- the weight percentage of magnesium stearate is from 0 to 2% based on the total weight of the composition.
- the weight percentage of magnesium stearate is from 0 to 0.5%.
- the weight percentage of Poloxamer 188 is from 0.01 to 10% based on the total weight of the composition.
- the weight percentage of Poloxamer 407 is from 0.01 to 10% based on the total weight of the composition.
- the weight percentage of Labrasol is from 10 to 99% based on the total weight of the composition.
- the Labrasol is 10 to 35% by weight.
- the weight percent of PEG 6000 is from 0 to 5%, based on the total weight of the composition.
- the IMWITOR 491 is 0.5 to 2% by weight based on the total weight of the composition.
- the weight percent of Sodium dodecyl sulfate is from 0.5 to 2.5%, based on the total weight of the composition.
- Sepitrap 80 is present in an amount of from 0 to 20% by weight based on the total weight of the composition.
- the disintegrant comprises agar, algionic acid, calcium carbonate, carboxymethylcellulose, cellulose, clay, Colloidal silica, croscarmellose sodium, cross-linked povidone, gum, magnesium aluminum silicate, methyl fiber Methyl cellulose, polacrilin potassium, sodium alginate, low substituted hydroxypropyl cellulose, crosslinked polyvinylpyrrolidone hydroxypropyl cellulose (crosslinked Polyvinylpyrrolidone hydroxypropylcellulose), sodium starch glycolate, starch, cross-linked polyvinyl carboxymethyl cellulose, cross-linked polyvinylpyrrolidone (also known as cross-linked polyvinylpyrrolidone) Polyvinyl polypyrrolidone (PVPP for short) and low-substituted hydroxypropyl cellulose (L-hydroxypropyl cellulose) At least one or a combination of L-HPC) in.
- L-HPC low-substituted hydroxypropyl
- the binder includes, but is not limited to, microcrystalline cellulose (MCC), hydroxymethyl cellulose, hydroxypropyl cellulose, and polyvinyl pyrrolidone. ), water, alcohol, hydroxypropyl methylcellulose, povidone (PVP-K series), carboxymethyl cellulose, Tween series, SPAN series, Vitamin E TPGS, 48/16, polyethylene glycol (PEG), propylene glycol (Propylene glycol), hydroxypropyl methyl fiber, cyclodextrin series (cyclodextrin).
- the filler comprises calcium carbonate, calcium phosphate, dibasic calcium phosphate, tribasic calcium sulfate, calcium carboxymethylcellulose, Cellulose, dextrin, salt, dextrose, fructose, lactitol, lactose, carbonate, magnesium oxide , maltitol, maltodextrin, maltose, sorbitol, starch, sucrose, sugar, xylitol, mannitol At least one or a combination of glucose, powdered cellulose, and microcrystalline cellulose.
- the lubricant includes, but is not limited to, agar, calcium stearate, ethyl oleate, ethyl laurate, glycerin, stearic acid.
- Glyceryl palmitostearate hydrogenated vegetable oil, magnesium oxide, magnesium stearate, mannitol, poloxamer, ethylene glycol, sodium benzoate , sodium lauryl sulfate, sodium stearoyl acid, sorbitol, stearic acid, talc, zinc stearate, silica (silicon dioxide), and talc powder.
- the suspending agent includes, but is not limited to, mannitol, carboxymethyl cellulose (CMC), and sodium carboxymethyl cellulose (CMC-Na).
- the co-solvent comprises, but is not limited to, hydroxypropyl-beta-cyclodextrin, tween 80, castor oil, polyethylene glycol (PEG). , Poloxame, polysorbate, sorbitan fatty acid ester (Sorbitan fatty acid esters, which is the main component of the commercial Span), vitamin E polyethylene glycol succinate (vitamin E Polyethylene glycol succinate, which is a main component of TPGS, polyoxyethylene stearates, propylene glycol, glyceryl stearate, and Sepitrap 80, or a combination thereof.
- PEG polyethylene glycol
- Poloxame polysorbate
- sorbitan fatty acid ester Sorbitan fatty acid esters, which is the main component of the commercial Span
- vitamin E polyethylene glycol succinate vitamin E Polyethylene glycol succinate, which is a main component of TPGS, polyoxyethylene stearates, propylene glycol, glyce
- the glidant includes, but is not limited to, magnesium stearate, silica, magnesium trisilicate, powdered cellulose, starch, talc, tribasic calcium phosphate, Materials such as calcium silicate, magnesium silicate, colloidal silica, and silicon hydrogel.
- the pharmaceutical products of the present invention may exist in various forms. These forms include, but are not limited to, liquid, semi-solid, and solid pharmaceutical forms such as liquid solutions (eg, injectable and infusible solutions), dispersions or suspensions, lozenges, pills, powders, liposomes, and suppositories.
- liquid solutions eg, injectable and infusible solutions
- dispersions or suspensions lozenges
- pills pills
- powders powders
- liposomes suppositories.
- suppositories a pharmaceutical composition
- the preferred form depends on the intended mode of administration and therapeutic application; preferably, the pharmaceutical of the present invention is in the form of an orally or infusible solution.
- a pharmaceutical composition for reducing body weight and body fat comprises an effective amount of a combination of a green tea extract and a turmeric extract, which is administered orally, and the plant extract composition according to the present invention is suitable for and subjected to Preferred oral dosage forms are tablets, granules, coated tablets, capsules, lozenges and other solid oral dosage forms which are also encompassed within the scope of the invention.
- the soft capsule preparation step of the present invention is as follows: the green tea extract and the turmeric extract are mixed with an appropriate oil-based excipient (eg, lecithin, beeswax, coconut oil, palm) In oil or the like, an oily solution containing a content is formed.
- the oily solution containing the content is filled into a capsule membrane material in a liquid form (such as gelatin, glycerin, water, etc.) and formed by a soft capsule filling and pressing step; or, the animal gelatin is sliced.
- the outer membrane of the capsule is made by using a stainless steel mold, and then the oily solution containing the content is poured into the outer membrane. After the soft capsules are dried, they are packaged.
- the present invention further provides an application of the pharmaceutical product for reducing body weight and body fat, which is administered to a recipient by an effective amount of a pharmaceutical extract comprising a green tea extract and a plant extract composition of turmeric extract.
- a pharmaceutical extract comprising a green tea extract and a plant extract composition of turmeric extract.
- the body is human or animal to achieve the effect of reducing body weight and body fat.
- the administration mode is oral administration or injection administration.
- the effective dose refers to a pharmaceutical product which is administered from 1.8 mg to 145 mg per kilogram of the recipient per day, wherein the receptor is human or animal, preferably human.
- the effective dose means 5.4 mg to 70 mg of the drug per kilogram of the recipient per day, where the receptor is human or animal, preferably human.
- the "effective dose” can be estimated herein according to the “Food and Drug Administration” (FDA) "estimating the maximum safe starting dose in initial clinical trials (estimating the maximum safe starting dose in initial Table 1 (Table 1) of clinical trials for therapeutics in adult healthy volunteers)” extrapolates the effective dose of different receptors.
- FDA Food and Drug Administration
- reducing body weight and body fat means administering an effective amount of a composition comprising green tea extract and turmeric extract, or further comprising a composition of resveratrol, such that the individual, for example, or The body fat index is less than the obese control group; the reduction of body fat can be measured by administering a specific range of the composition of the green tea extract and the turmeric extract, or a composition further comprising resveratrol, and measuring in a specific time range. For example, the amount of fat in the epididymis, the amount of fat in the kidney, the amount of fat in the mesenteric area, the amount of fat in the groin and the peritoneal cavity are changed.
- the various components of the plant extracting composition of the present invention are obtained by plant extraction, and the experimental results show that the plant extracting composition of the present invention does not affect appetite or food intake, and does not affect other serum biochemical safety indexes. Therefore, the safety is higher, and it is safer and has no obvious side effects compared with other weight-reducing drugs currently on the market.
- the plant extracting composition of the present invention not only reduces body weight, but also reduces the body weight by reducing the heat absorption by suppressing appetite or blocking the absorption of intestinal fat by the prior art.
- the plant extracting composition of the present invention can provide a safer and more effective method for reducing body weight and body fat in response to the current global obesity and overweight problem, and can be applied to related medicines or health care in the future. Food and other uses.
- Figure 1 is a bar graph showing the effect of each group on the growth inhibition of precursor fat cells by the cell viability assay (MTT assay).
- Figure 2 is a bar graph showing the effect of each group on the growth inhibition of differentiated adipocytes in a cell viability assay (MTT assay).
- Figure 3 is a bar graph showing the amount of lipolytic enzyme expression in each group of mature adipocytes by reverse transcription-polymerase chain reaction (RT-PCR) according to the present invention.
- Figure 4 is a bar graph of the present invention for detecting changes in body weight gain of mice in each group by simultaneously inducing obesity and administration.
- Figure 5 is a bar graph of the effect of different excipients on the dissolution rate of curcumin in the compositions of the present invention by a dissolution test of the present invention.
- Figure 6 is a bar graph of the effect of different concentrations of polyoxyethylene (40) stearate on the dissolution rate of curcumin in the compositions of the present invention by a dissolution test of the present invention.
- Figure 7 is a bar graph of the effect of a mixture of polysorbate 80 mixtures at various concentrations on the dissolution rate of curcumin in the compositions of the present invention by a dissolution test of the present invention.
- Figure 8 is a bar graph of the effect of different concentrations of polyoxyethylene (32) stearate on the dissolution rate of curcumin in the compositions of the present invention by a dissolution test of the present invention.
- Figure 9 is a bar graph of the effect of the ratio of curcumin and polyoxyethylene (40) stearate in the composition of the present invention on the dissolution rate of curcumin by the dissolution test of the present invention.
- Figure B is a graph showing the effect of the ratio of the weight loss or fat-reducing active ingredient composition and the polyoxyethylene (40) stearate on the dissolution rate of curcumin in the composition of the present invention by a dissolution test. Histogram.
- Figure 10 is a bar graph of the effect of the ratio of curcumin and polysorbate 80 mixture in the composition of the present invention on the dissolution rate of curcumin by the dissolution test of the present invention.
- Figure B is a bar graph of the effect of the ratio of the weight loss or reduced fat active ingredient composition and the polysorbate 80 mixture in the composition of the present invention on the dissolution rate of curcumin by the dissolution test of the present invention.
- Figure 11 is a bar graph of the effect of the ratio of curcumin and polyoxyethylene (32) stearate in the composition of the present invention on the dissolution rate of curcumin by the dissolution test of the present invention.
- Figure B is a graph showing the effect of the ratio of the weight loss or fat-reducing active ingredient composition and the polyoxyethylene (32) stearate on the dissolution rate of curcumin in the composition of the present invention by a dissolution test. Histogram.
- Figure 12A is a bar graph of the effect of simultaneous induction of obesity and administration to detect total body weight gain in groups of rats by simultaneous induction of obesity and administration of a composition comprising three different excipients.
- Figure 12B is a bar graph of the effect of simultaneous induction of obesity and administration to detect the effect of a composition comprising three different excipients on body fat percentage in each group of rats.
- Figure 13A is a bar graph of the effect of simultaneous induction of obesity and administration to detect different ratios of composition for total body weight gain in each group of rats.
- Figure 13B is a bar graph of the effect of simultaneous induction of obesity and administration to detect the effect of different ratios of composition on body fat percentage in each group of rats.
- Figure 14A is a bar graph of the effect of the composition of the present invention on total body weight gain in rats with fatty liver and nonalcoholic steatohepatitis by first inducing obesity re-administration.
- Figure 14B is a bar graph of the effect of the composition of the present invention on body fat percentage in rats with fatty liver and nonalcoholic steatohepatitis by first inducing obesity re-administration.
- Figure 15A is a bar graph of the effect of the composition of the present invention on the liver weight of rats with fatty liver and nonalcoholic steatohepatitis by first inducing obesity re-administration.
- Figure 15B is a bar graph of the effect of the composition of the present invention on liver fat mass in rats with fatty liver and nonalcoholic steatohepatitis by first inducing obesity re-administration.
- Figure 15C is a bar graph of the effect of the composition of the present invention on total liver cholesterol in rats with fatty liver and nonalcoholic steatohepatitis by first inducing obesity re-administration.
- Figure 15D is a bar graph of the effect of the composition of the present invention on liver triglyceride in rats with fatty liver and nonalcoholic steatohepatitis by first inducing obesity re-administration.
- 3T3-L1 adipocyte precursor per well of 1 ⁇ 10 4 cells (1 ⁇ 10 4 cells / well ) concentration of the present embodiment will be cultured in 96-well plates, in addition to the control group (i.e., DMSO solvent control group), in 50 ppm resveratrol, 50 ppm turmeric extract, 80 ppm green tea extract and 100 ppm of the plant extract compositions ME008A, ME008D, ME001, ME00C1 and ME00D1 of the present invention were added to the different wells, and a total of 9 experiments were performed and 3 replicates were performed for each set of experiments. .
- the control group i.e., DMSO solvent control group
- the plant extract composition ME008A of the present invention comprises 50 wt% green tea extract, 25 wt% green coffee bean extract and 25 wt% resveratrol;
- ME008D comprises 40 wt% green tea extract, 45 wt% green coffee bean extract and 15 wt% chalk Resver;
- ME001 comprises 60wt% green tea extract, 10wt% turmeric extract and 30wt% resveratrol;
- ME00C1 comprises 40wt% green tea extract, 50wt% turmeric extract and 10wt% resveratrol;
- ME00D1 contains 75wt% green tea Extract with 25 wt% turmeric extract.
- the plant extracting compositions ME00C1, ME001 and ME008D of the present invention can significantly inhibit the growth of the precursor fat cells (p ⁇ 0.05), and the growth of the precursor fat cells by ME00C1.
- the inhibitory effect was optimal (p ⁇ 0.05), and the growth inhibition effect of the composition ME00C1 on the precursor fat cells was significantly better than that of the resveratrol, turmeric extract or green tea extract alone (p ⁇ 0.05).
- 3T3-L1 adipocytes precursor per well in 1 ⁇ 10 5 cells (1 ⁇ 10 5 cells / well ) concentration of the present embodiment will be cultured in 12-well plates, containing culture to use the fourth day 5 micrograms per milliliter ( 5 ⁇ g/ml) differentiation agent insulin, 1 micromolar ( ⁇ M) dexamethasone (dexmethasone), 0.5 millimolar (mM) 3-isobutyl-1-methylxanthine (3-isobutyl-1) -methylxanthine) culture medium to induce adipocyte differentiation.
- ⁇ M micromolar
- dexmethasone dexamethasone
- mM 3-isobutyl-1-methylxanthine 3-isobutyl-1) -methylxanthine
- each group was separately added with 50 ppm resveratrol, 50 ppm turmeric extract, 80 ppm green tea extract, and 100 ppm of the plant extract compositions ME008A, ME008D, ME001, ME00C1, ME00D1 of the present invention.
- 50 ppm resveratrol 50 ppm turmeric extract
- 80 ppm green tea extract 100 ppm of the plant extract compositions ME008A, ME008D, ME001, ME00C1, ME00D1 of the present invention.
- MTT assay cell viability assay
- the plant extract compositions of the present invention can significantly inhibit the growth of adipocytes during differentiation (p ⁇ 0.05), wherein ME00C1 has the best inhibitory effect on the growth of adipocytes during differentiation. (p ⁇ 0.05), and the effect of composition ME00C1 on the growth inhibition of differentiated adipocytes was significantly better than that of resveratrol, turmeric extract or green tea extract alone (p ⁇ 0.05).
- 3T3-L1 cells were cultured in a 12-well plate at a concentration of 3 ⁇ 10 4 cells/well. The culture was cultured until the fourth day, and cultured in DMEM medium (Gibco Inc, Germany) containing 5 ⁇ g/ml insulin, 1 ⁇ M dexamethasone, and 0.5 mM 3-isobutyl-1-methylxanthine, and replaced with two days later. The culture medium of 5 ⁇ g/ml insulin was continuously cultured for six days. After the differentiation of 3T3-L1 cells, except for the control group (ie, the DMSO solvent control group), each group was separately added with 50 ppm turmeric extract, 50 ppm green tea extract, and 50 ppm of the present invention.
- the control group ie, the DMSO solvent control group
- the plant extract composition C15 of the present invention comprises 20 wt% green tea extract and 80 wt% turmeric extract
- C14 comprises 33 wt% green tea extract and 67 wt% turmeric extract
- C13 comprises 40 wt% green tea extract and 60 wt% turmeric extract
- C12 comprises 50 wt% green tea extract and 50 wt% turmeric extract
- C11 comprises 60 wt% green tea extract and 40 wt% turmeric extract
- D11 comprises 67 wt% green tea extract and 33 wt% turmeric extract
- D12 comprises 75 wt% green tea extract and 25 wt% turmeric extract
- D13 comprises 80 wt% green tea extract and 20 wt% turmeric extract
- D14 comprises 83 wt% green tea extract and 17 wt% turmeric
- RNA from mature adipocytes was extracted with Trizol Reagent (Thermo Fisher Scientific Inc, USA), and then reverse transcription kit (Reverse Transcription Kit; Thermo Fisher Scientific Inc, USA) and polymerase chain reaction.
- a reverse transcription-polymerase chain reaction was performed using a kit (Polymerase chain reaction Kit; Thermo Fisher Scientific Inc, USA) to detect the amount of Hormone sensitive lipase (HSL) expression in mature adipocytes.
- the primers used in the polymerase chain reaction are 5'-GAATATCACGGAGATCGAGG-3' and 5'-CCGAAGGGACACGGTGATGC-3'.
- the plant extract compositions C11, C12, C13, C14, D11, D12 and D13 of the present invention can significantly increase the performance of lipolytic enzymes.
- the amount (p ⁇ 0.05), and synergistic effect on the efficacy of increasing the amount of lipolytic enzyme, has an unpredictable effect. It can be seen that when the ratio of the weight of the green tea extract and the weight of the turmeric extract is 1:2 to 4:1, a synergistic effect occurs; that is, the ratio of the weight of the green tea extract to the weight of the turmeric extract is 0.5. At ⁇ 4, synergy will occur.
- the turmeric extract used in the examples of the present invention contains at least 80% of curcumin, and the green tea extract used contains at least 50% of epigallocatechin gallate, and thus, via the present embodiment
- the result shows that when the ratio of the weight of curcumin and the weight of epigallocatechin gallate is 0.4-3.2, a synergistic effect occurs, and the weight percentage of curcumin is 28.57%-76.19%.
- the weight percentage of gallocatechin gallate is 23.81% to 71.43%.
- 8-week old B6 female mice were used and divided into normal control group, obese control group and resveratrol group (resorrel was administered at a dose of 61.5 mg/kg BW) and green tea extract group ( The green tea extract was applied at a dose of 123 mg/kg BW), the plant extract composition ME001 of the present invention (the application dose of ME001 was 676.5 mg/kg BW), and each group was tested with 5 female animals, during the test, except The normal control group was fed with normal feed, and the other groups were fed with high-fat diet for 8 weeks to induce obesity symptoms. At the same time, the test substance was administered daily for 8 weeks, and the obese control group was fed with equal volume of sterile water.
- mice To assess the difference in body weight of each group of mice. The body weight and average food intake of each animal were recorded weekly during the experiment, and the mice were sacrificed after the test was completed. There was no statistical difference in the average weekly food intake between the groups fed the high fat diet during the experimental trials (p>0.05).
- the data of each group were expressed as mean ⁇ SD (Mean ⁇ SD).
- the English letters a, b, and c indicate statistical results. Different letters indicate statistical differences between groups (p ⁇ 0.05), and the same letters indicate no between groups. There is a statistical difference (p>0.05).
- the test results are shown in Fig. 4.
- the total weight gain of the mice fed the plant extract composition ME001 of the present invention was significantly reduced (p ⁇ 0.05), and the decrease was 47.2%. Therefore, the present invention
- the plant extract composition ME001 was effective in achieving weight loss (p ⁇ 0.05).
- the total weight gain of mice administered with resveratrol alone was not statistically different (p>0.05) compared with the obese control group.
- the plant extracting composition ME001 of the present invention not only can effectively reduce body weight, but also has better efficacy than the single plant extract group (p ⁇ 0.05), and has better weight-reducing effect than other groups.
- test substances were prepared in the following manner.
- Formulation of a tablet containing 1% polyoxyethylene (32) stearate 250 mg of green tea extract, 200 mg of turmeric extract, polyoxyethylene (32) stearate, filler, and disintegrant are sequentially placed A mixture containing 1% polyoxyethylene (32) stearate was prepared by mixing in a mixer and then performing a dry powder compressing into tablets. Each tablet containing 1% polyoxyethylene (32) stearate weighs 600 mg, and each tablet containing 1% polyoxyethylene (32) stearate contains 250 mg of green tea extract, 200 mg. Turmeric extract, and 1% by weight of polyoxyethylene (32) stearate.
- Formulation of a 5% polysorbate 80 mixture The formulation method is approximately the same as that of the polyoxyethylene (32) stearate-containing tablet, the only difference being that 5% polysorbate 80 The mixture replaced the polyoxyethylene (32) stearate such that each tablet contained a 5% by weight mixture of polysorbate 80. Wherein, the polysorbate 80 mixture is Sepitrap 80.
- the formulation method is almost the same as that of the tablet containing 1% polyoxyethylene (32) stearate, the only difference being that Polyoxyethylene (40) stearate, vitamin E polyethylene glycol succinate, polysorbate 20, polyethylene glycol (400), polyethylene glycol (6000), glyceryl monostearate Replacing polyoxyethylene (32) stearate with oleic acid polyethylene glycol-6 glyceride or glyceryl dibenzoate, so that each tablet contains 0.
- Formulation of the control tablet The formulation method was approximately the same as that of the tablet containing polyoxyethylene (32) stearate, the only difference being that no polyoxyethylene (32) stearate was added.
- Each of the above-mentioned various tablets contains 250 mg of green tea extract and 200 mg of turmeric extract, each of which has a weight of 600 mg, and a filler, a disintegrating agent, and a disintegrating agent used in the preparation of each tablet. And the binders are all identical to each other.
- the filler described in this embodiment includes at least one of mannitol, starch, glucose, lactose, maltodextrin, dextrin, microcrystalline cellulose, sucrose, maltose, calcium carbonate, and powdered cellulose or combination.
- the disintegrating agent described in this embodiment includes at least one of or a combination of Cross-Linked Sodium Carboxymethyl Cellulose, cross-linked polyvinylpyrrolidone, and low-substituted hydroxypropylcellulose. .
- the eluent was hydrochloric acid (Hydrochloric acid) with a concentration of 0.1N. That is, HCl), the volume of the eluate was 900 ml, which contained 4% SDS and the temperature was 37 ⁇ 0.5 °C.
- the dissolution test was carried out at a rotation speed of 100 rpm, and samples were taken at 30 minutes and 60 minutes after the start of the dissolution test, and the concentration of curcumin in the sample was measured by high performance liquid chromatography (HPLC). And calculate the dissolution rate of curcumin in the following manner:
- the amount of slowly dissolved or poorly soluble water in the dissolution test should not be less than 85% of the marker content. Therefore, if the dissolution rate of curcumin in the tablet is at least 85% if the dissolution test is carried out for 30 minutes or 60 minutes, the tablet conforms to the specifications of the oral preparation. Among them, if the dissolution test is carried out for 30 minutes, the dissolution rate of curcumin in the tablet is at least 85%, which is called rapid dissolving.
- a control tablet a tablet containing 1% polyoxyethylene (32) stearate, a tablet containing 0.5% polyoxyethylene (40) stearate, and 5%.
- the elution rates of curcumin in the lozenges of glyceryl bismuthate were 54.48%, 80.35%, 79.36%, 61.36%, 53.12%, 41.57%, 79.75%, 63.46%, 80.50%, 76.62%, respectively.
- polyoxyethylene (32) stearate, polyoxyethylene (40) stearate, polyethylene glycol (400), and glyceryl monostearate can all make the present invention contain epigallocate
- the combination of the tea catechin and curcumin achieves a near-rapid dissolving standard.
- a control tablet a tablet containing 1% polyoxyethylene (32) stearate, a tablet containing 0.5% polyoxyethylene (40) stearate, and a 5% polysorbate.
- the dissolution rates of curcumin in the 60-minute curcumin were 69.50%, 89.01%, 86.97%, 85.30%, 86.41%, 71.67%, 87.68%, 80.52%, 89.14%, 86.50%, respectively. 85.89%.
- the lozenges of the alcohol-6 glyceride and the lozenges containing 1% glyceryl disorbate had a dissolution rate of 85% of curcumin at 60 minutes.
- polyoxyethylene (32) stearate, polyoxyethylene (40) stearate, 5% polysorbate 80 mixture, vitamin E polyethylene glycol succinate, polyethylene glycol ( 400), glyceryl monostearate, polyethylene glycol-6 glyceryl oleate, and glyceryl dioxalate can make the composition containing epigallocatechin gallate and curcumin of the present invention conform to oral administration Formulation of the formulation and increase bioavailability.
- Example 6-1 Effect of different concentrations of polyoxyethylene (40) stearate on the dissolution rate of curcumin
- a lozenge containing 0.5% polyoxyethylene (40) stearate was formulated in the same manner as the formulation of the lozenge containing 0.5% polyoxyethylene (40) stearate in Example 5.
- Formulation of lozenges containing 0.05% polyoxyethylene (40) stearate or lozenges containing 0.1% polyoxyethylene (40) stearate formulation method and 0.5% polyoxygenation in Example 5 Tablets of ethylene (40) stearate were formulated in substantially the same manner, except that each tablet contained 0.05% or 0.1% by weight of polyoxyethylene (40) stearate in each tablet.
- test results are shown in Fig. 6.
- a tablet containing 0.05% polyoxyethylene (40) stearate, a tablet containing 0.1% polyoxyethylene (40) stearate, and 0.5% polyoxyethylene ( 40) The dissolution rates of the stearate lozenges in 30 minutes were 83.13%, 84.71%, and 79.36%, respectively.
- a tablet containing 0.05% polyoxyethylene (40) stearate a tablet containing 0.1% polyoxyethylene (40) stearate, and 0.5% polyoxyethylene (40).
- the dissolution rates of the stearate lozenges in the 60 minutes of curcumin were 89.54%, 90.88%, and 86.97%, respectively, both of which were 85%.
- the polyoxyethylene (40) stearate having a weight percentage of 0.05% to 0.5% can make the composition containing epigallocatechin gallate and curcumin of the present invention conform to the specification and improvement of the oral preparation. Bioavailability, and low concentration can make the dissolution rate of curcumin better.
- Example 6-2 Effect of different concentrations of polysorbate 80 mixture on the dissolution rate of curcumin
- a tablet containing a mixture of 5% polysorbate 80 was prepared in the same manner as the formulation of the tablet containing 5% polysorbate 80 in Example 5.
- a lozenge containing a mixture of 3% polysorbate 80, or a lozenge containing a mixture of 10% polysorbate 80 a formulation of a lozenge containing a mixture of 5% polysorbate 80 in Example 5
- the formulation method is about the same, the only difference being that each tablet contains a mixture of polysorbate 80 in a percentage by weight of 3% or 10%.
- test results are shown in Figure 7, a tablet containing a mixture of 3% polysorbate 80, a tablet containing a mixture of 5% polysorbate 80, and a tablet containing a mixture of 10% polysorbate 80 in 30 minutes.
- the dissolution rates of curcumin were 71.76%, 61.36%, and 32.41%, respectively.
- a tablet containing 3% polysorbate 80 mixture, a tablet containing 5% polysorbate 80 mixture, and a lozenge containing 10% polysorbate 80 mixture in 60 minutes of turmeric The dissolution rates of the primes were 87.77%, 85.30%, and 49.98%, respectively.
- the lozenges containing a mixture of 3% polysorbate 80 and the lozenge containing a mixture of 5% polysorbate 80 in 60 minutes of curcumin The dissolution rate is 85%. It can be seen that the polysorbate 80 mixture of 3% to 5% by weight can make the composition containing epigallocatechin gallate and curcumin of the present invention meet the specifications of the oral preparation and improve the bioavailability. And the low concentration can make the dissolution rate of curcumin better.
- Example 6-3 Effect of different concentrations of polyoxyethylene (32) stearate on the dissolution rate of curcumin
- a tablet containing 1% polyoxyethylene (32) stearate was prepared in the same manner as in the formulation of the tablet containing 1% polyoxyethylene (32) stearate in Example 5.
- Formulation of a tablet containing 3% polyoxyethylene (32) stearate or a tablet containing 5% polyoxyethylene (32) stearate the formulation method is the same as that of Example 5 containing 1% polyoxyl Tablets of ethylene (32) stearate are formulated in substantially the same manner, except that each tablet contains 3% or 5% by weight of polyoxyethylene (32) stearate in each tablet.
- test results are shown in Fig. 8.
- the dissolution rate of the stearate tablet in 30 minutes of curcumin was 80.35%, 65.41%, and 44.74%, respectively.
- the dissolution rate of the stearate tablet in 60 minutes of curcumin was 89.01%, 88.11%, and 77.34%, respectively, and the tablet containing 1% polyoxyethylene (32) stearate, and containing 3
- the lozenges of % polyoxyethylene (32) stearate had an elution rate of 85% in 60 minutes of curcumin.
- the polyoxyethylene (32) stearate having a weight percentage of 1% to 3% can make the composition containing epigallocatechin gallate and curcumin of the present invention conform to the specification and improvement of the oral preparation. Bioavailability, and low concentration can make the dissolution rate of curcumin better.
- Example 7-1 Effect of the ratio of drug to polyoxyethylene (40) stearate on the dissolution rate of curcumin
- a tablet having a weight ratio of curcumin to polyoxyethylene (40) stearate of 53.3:1: a formulation method and a tablet containing 0.5% polyoxyethylene (40) stearate in Example 5 The preparation method is the same.
- the lozenge containing 0.5% polyoxyethylene (40) stearate in Example 5 contained 200 mg of turmeric extract, and the turmeric extract used in the present invention contained at least 80% of curcumin, and thus Examples
- the test results are shown in Fig. 9A.
- the weight ratio of curcumin to polyoxyethylene (40) stearate in the tablet containing polyoxyethylene (40) stearate is 40, 48, 53.3, 200, respectively.
- the dissolution rates of the curcumin in the 30 minutes were 89.57%, 78.56%, 79.36%, 89.00%, 84.71%, and 83.13%, respectively.
- the weight ratio of curcumin to polyoxyethylene (40) stearate in a tablet containing polyoxyethylene (40) stearate is 40, 48, 53.3, 200, 266.7.
- the dissolution rates of the curcumin in the 60 minutes were 92.40%, 85.75%, 86.97%, 90.72%, 90.88%, and 89.54%, respectively, both of which were 85%.
- the weight ratio of curcumin to polyoxyethylene (40) stearate in the tablet is 40, 48, 53.3, 200, 266.7, or 533.3
- the present invention can be made to contain epigallocatechin.
- the combination of gallic acid ester and curcumin meets the specifications of oral preparations and enhances bioavailability.
- Figure 9B is a graph showing the "weight ratio of curcumin to polyoxyethylene (40) stearate" in Figure 9A to "weight loss or fat-reducing active ingredient composition and polyoxyethylene (40) stearate Weight ratio".
- the weight loss or fat-reducing active ingredient composition is a general term for the epigallocatechin gallate in the green tea extract and the curcumin in the turmeric extract.
- the preparation method is the same as the preparation method of the tablet containing 0.5% polyoxyethylene (40) stearate in Example 5), the ingot containing 0.5% polyoxyethylene (40) stearate in Example 5.
- the agent contained 160 mg of curcumin and 3 mg of polyoxyethylene (40) stearate.
- the tablet containing 0.5% of polyoxyethylene (40) stearate in Example 5 contained 250 mg of green tea extract, and the turmeric extract used in the present invention contained at least 50% of epigal tea.
- the test results are shown in Fig. 9B, and the weight ratio of the weight loss or fat-reducing active ingredient composition to the polyoxyethylene (40) stearate in the tablet containing polyoxyethylene (40) stearate is sequentially At 71.3, 85.5, 95, 356.3, 475, and 950, the dissolution rates of the curcumin in the 30 minutes were 89.57%, 78.56%, 79.36%, 89.00%, 84.71%, and 83.13%, respectively.
- the weight ratio of the weight loss or fat-reducing active ingredient composition to the polyoxyethylene (40) stearate in the tablet containing polyoxyethylene (40) stearate is 71.3, At 85.5, 95, 356.3, 475, or 950, the dissolution rates of the curcumin in the 60 minutes were 92.40%, 85.75%, 86.97%, 90.72%, 90.88%, and 89.54%, respectively, which were 85%. It can be seen that the weight ratio of the weight loss or fat-reducing active ingredient composition in the tablet to the polyoxyethylene (40) stearate is 71.3, 85.5, 95, 356.3, 475, or 950.
- the composition containing the epigallocatechin gallate and curcumin meets the specifications of the oral preparation and improves the bioavailability.
- Example 7-2 Effect of the ratio of drug to polysorbate 80 mixture on the dissolution rate of curcumin
- a tablet having a weight ratio of curcumin to polysorbate 80 in a ratio of 5.3:1 was prepared: the formulation method was the same as that of the tablet containing 5% polysorbate 80 in Example 5.
- the tablet containing the 5% polysorbate 80 mixture in Example 5 contained 200 mg of turmeric extract, and the turmeric extract used in the present invention contained at least 80% of curcumin, so the content of Example 5 was contained.
- the formulation of the tablet is about the same, the only difference being that the weight ratio of the mixture of curcumin and polysorbate 80 is in the order of 2, 6.7, 8, or 8.9.
- Fig. 10A The test results are shown in Fig. 10A.
- the weight ratio of the mixture of curcumin and polysorbate 80 in the tablet containing the polysorbate 80 mixture is sequentially 2, 5.3, 6.7, 8, and 8.9, the tablet is in the form of a tablet.
- the dissolution rates of curcumin for 30 minutes were 60.64%, 61.36%, 73.31%, 72.30%, and 71.76%, respectively.
- the weight ratio of the mixture of curcumin and polysorbate 80 in the tablet containing the polysorbate 80 mixture is sequentially 2, 5.3, 6.7, 8, and 8.9, and the tablet is in 60 minutes.
- the dissolution rates of curcumin were 86.16%, 85.30%, 91.66%, 85.25%, and 87.77%, respectively, both of which were 85%. It can be seen that when the weight ratio of the mixture of curcumin and polysorbate 80 in the tablet is 2, 5.3, 6.7, 8, or 8.9, the present invention can be made to contain epigallocatechin gallate and curcumin.
- the composition meets the specifications of the oral preparation and improves the bioavailability.
- Figure 10B is a graph showing the "weight ratio of curcumin to polysorbate 80 mixture" in Figure 10A to "weight ratio of the weight loss or reduced fat active ingredient composition to polysorbate 80 mixture".
- the weight loss or fat-reducing active ingredient composition is a general term for the epigallocatechin gallate in the green tea extract and the curcumin in the turmeric extract.
- the preparation method and the preparation method in Example 5 The tablet containing 5% polysorbate 80 mixture was prepared in the same manner), the tablet containing 5% polysorbate 80 mixture in Example 5 contained 160 mg of curcumin and 30 mg of polysorbate 80 mixture. . Further, the tablet containing the mixture of 5% polysorbate 80 in Example 5 contained 250 mg of green tea extract, and the turmeric extract used in the present invention contained at least 50% of epigallocatechin gallate.
- the test results are shown in Fig. 10B, and the weight ratio of the weight loss or fat-reducing active ingredient composition to the polysorbate 80 mixture in the tablet containing the polysorbate 80 mixture is 3.6, 9.5, 11.9, 14.3, respectively.
- the dissolution rates of the curcumin in the 30 minutes were 60.64%, 61.36%, 73.31%, 72.30%, and 71.76%, respectively.
- the weight ratio of the weight loss or fat-reducing active ingredient composition to the polysorbate 80 mixture in the tablet containing the polysorbate 80 mixture is 3.6, 9.5, 11.9, 14.3, and 15.8, respectively.
- the dissolution rates of the curcumin in the 60 minutes were 86.16%, 85.30%, 91.66%, 85.25%, and 87.77%, respectively, which were 85%.
- the weight ratio of the weight loss or fat-reducing active ingredient composition in the tablet to the polysorbate 80 mixture is 3.6, 9.5, 11.9, 14.3, and 15.8, respectively.
- the combination of catechin gallate and curcumin meets the specifications of oral preparations and enhances bioavailability.
- Example 7-3 Effect of the ratio of drug to polyoxyethylene (32) stearate on the dissolution rate of curcumin
- the test results are shown in Fig. 11A.
- the weight ratio of curcumin to polyoxyethylene (32) stearate in the tablet containing polyoxyethylene (32) stearate was 5.3, 8.9, or 26.7.
- the dissolution rates of the curcumin in the lozenge at 30 minutes were 44.74%, 65.41%, and 80.35%, respectively.
- the weight ratio of curcumin to polyoxyethylene (32) stearate in the tablet containing polyoxyethylene (32) stearate is 5.3, 8.9, or 26.7, respectively.
- the dissolution rate of curcumin in the 60 minutes was 77.34%, 88.11%, and 89.01%, respectively, and the ratio of the weight ratio of curcumin to polyoxyethylene (32) stearate was 8.9, or 26.7. Both are 85%. From this, it can be seen that when the weight ratio of curcumin to polyoxyethylene (32) stearate in the tablet is 8.9 or 26.7, the present invention can contain a combination of epigallocatechin gallate and curcumin. The substance meets the specifications of the oral preparation.
- Figure 11B is a graph showing the "weight ratio of curcumin to polyoxyethylene (32) stearate" in Figure 11A to "weight loss or fat-reducing active ingredient composition and polyoxyethylene (32) stearate Weight ratio”.
- the test results are shown in Fig. 11B, and the weight ratio of the weight loss or fat-reducing active ingredient composition to the polyoxyethylene (32) stearate in the tablet containing polyoxyethylene (32) stearate is sequentially At 9.5, 15.8, or 47.5, the dissolution rates of the curcumin in the 30 minutes were 44.74%, 65.41%, and 80.35%, respectively.
- the weight ratio of the weight loss or fat-reducing active ingredient composition to the polyoxyethylene (32) stearate in the tablet containing polyoxyethylene (32) stearate is 9.5.
- the dissolution rates of the curcumin in the 60 minutes were 77.34%, 88.11%, and 89.01%, respectively, wherein the weight loss or fat-reducing active ingredient composition and the polyoxyethylene (32) stearic acid were used.
- the dissolution ratio of the ester weight ratio of 15.8, or 47.5 was 85%.
- the present invention can be used to contain epigallocatechin gallate.
- the composition of the acid ester and curcumin meets the specifications of the oral preparation and improves the bioavailability.
- test substances were prepared in the following manner.
- the ME00R5 composition was prepared by mixing ME00C1A and an appropriate amount of sterile water so that the total concentration of the green tea extract and the turmeric extract was 108.5 mg/mL, which is the ME00R5 composition. Among them, based on the total weight of ME00C1A, the weight percentage of the green tea extract was 55.5 wt%, and the weight percentage of the turmeric extract was 44.5 wt%.
- the ME00R composition was prepared by mixing ME00C1A, piperine, and an appropriate amount of sterile water so that the total concentration of the green tea extract and the turmeric extract was 108.5 mg/mL, which is the ME00R composition. Among them, the content of the green tea extract and the content of the turmeric extract were respectively the same as those in the ME00R5 composition.
- the weight percentage of piperine is 0.1 to 0.5% based on the total weight of the ME00R composition.
- the concentration of piperine is 0.525 to 2.625 mg/mL (milligrams solute per milliliter of solution) based on the total volume of the ME00R composition.
- the ME00C1B composition was prepared by mixing ME00C1A, piperine, glyceryl diammonate, and an appropriate amount of sterile water so that the total concentration of the green tea extract and the turmeric extract was 108.5 mg/mL, which is the ME00C1B composition.
- the content of the green tea extract and the content of the turmeric extract were respectively the same as those in the ME00R5 composition.
- the weight percentage of piperine is 0.1 to 0.5%
- the weight percentage of glyceryl dibelide is 0.5 to 1.2%.
- the concentration of piperine is 0.525 to 2.625 mg/mL
- the concentration of glyceryl dibelide is 2.625 to 6.3 mg/mL (milligrams solute per milliliter of solution).
- Formulation of ME00C2B composition Mix ME00C1A, piperine, polyoxyethylene (32) stearate, and appropriate amount of sterile water to make the total concentration of green tea extract and turmeric extract 108.5mg/mL, which is ME00C2B combination.
- the content of the green tea extract and the content of the turmeric extract were respectively the same as those in the ME00R5 composition.
- the weight percentage of piperine is 0.1 to 0.5%
- the weight percentage of polyoxyethylene (32) stearate is 0.5 to 1.2%.
- the concentration of piperine is 0.525 to 2.625 mg/mL
- the concentration of polyoxyethylene (32) stearate is 2.625 to 6.3 mg/mL (milligrams solute per milliliter of solution).
- the ME00C3B composition was prepared by mixing ME00C1A, piperine, polysorbate 80 mixture, and an appropriate amount of sterile water so that the total concentration of the green tea extract and the turmeric extract was 108.5 mg/mL, which is the ME00C3B composition.
- the content of the green tea extract and the content of the turmeric extract were respectively the same as those in the ME00R5 composition.
- the weight percentage of piperine is 0.1 to 0.5% based on the total weight of the ME00C3B composition, and the weight percentage of the polysorbate 80 mixture is 0.5 to 1.2%.
- the concentration of piperine is 0.525 to 2.625 mg/mL
- the concentration of the mixture of polysorbate 80 is 2.625 to 6.3 mg/mL (milligrams solute per milliliter of solution).
- the polysorbate 80 mixture is a mixture comprising polysorbate 80 and magnesium aluminum metasilicate.
- the concentrations of piperine in the ME00R composition, the ME00C1B composition, the ME00C2B composition, and the ME00C3B composition are the same.
- the weight percent concentration of glyceryl behenate in the ME00C1B composition is the same as the weight percent concentration of polyoxyethylene (32) stearate in the ME00C2B composition.
- HFD group 7-week old SD strain male rats were used, and were divided into an obese control group (i.e., HFD group), a composition ME00R group, a ME00R5 group, a ME00C1B group, a ME00C2B group, and a ME00C3B group.
- Each group was tested with 4 rats, fed with high-fat diet for 8 weeks to induce obesity, and the test substance was administered daily (the Dosing volume was 3 mL/kg per administration).
- the body weight of the rats; the dose of the test substance administered daily (Dosage) was 325.5 mg/kg rat body weight/day), and the obese control group was given an equal volume of sterile water to evaluate the difference in body weight and visceral fat between the groups.
- the body weight and average food intake of each animal were recorded weekly during the experiment, and the rats were fasted for 8 to 12 hours one night before the completion of the test. Then, the rats were sacrificed, the fasting body weight was weighed, and the visceral fat mass was calculated by weighing the peri-testosterone, the peripheral fat of the kidney, and the fat around the mesentery, and then calculating the relative body fat percentage (%) by the following method.
- the total weight gain of the rats administered with ME00C1B, ME00C2B, or ME00C3B was significantly decreased (p ⁇ 0.05) as compared with the ME00R5 group.
- glyceryl di-antimonate and piperine can significantly improve the weight-reducing effect of the composition of the present invention
- polyoxyethylene (32) stearate and piperine can significantly improve the weight-reducing effect of the composition of the present invention
- the polysorbate 80 mixture and piperine can also significantly enhance the weight reduction effect of the compositions of the present invention.
- glyceryl dibehenate and piperine can significantly improve the fat-reducing effect of the composition of the present invention; polyoxyethylene (32) stearate and piperine can significantly improve the fat-reducing effect of the composition of the present invention;
- the polysorbate 80 mixture and piperine can also significantly enhance the reduced fatening effect of the compositions of the present invention.
- the excipients can significantly enhance the weight-reducing effect and the fat-reducing effect of the composition of the present invention and increase the bioavailability of the composition of the present invention.
- test substances were prepared in the following manner.
- Formulation of ME00C1B composition The formulation method was the same as the ME00C1B composition in Example 8. The ratio of turmeric extract to green tea extract in the ME00C1B composition was 4:5.
- Formulation of ME00C14 composition The formulation method was the same as the ME00C1B composition of Example 8, except that the ratio of turmeric extract to green tea extract in the ME00C14 composition was 2:1.
- Formulation of ME00D11 composition The formulation method was the same as the ME00C1B composition of Example 8, except that the ratio of the turmeric extract to the green tea extract in the ME00D11 composition was 1:2.
- Formulation of ME00D14 composition The formulation method was the same as the ME00C1B composition of Example 8, except that the ratio of the turmeric extract to the green tea extract in the ME00D14 composition was 1:5.
- HFD group a composition of the present invention ME00C14 group, a ME00D11 group, a ME00D14 group, and a ME00C1B group.
- Each group was tested with 4 rats, fed with high-fat diet for 8 weeks to induce obesity, and the test substance was administered daily (the Dosing volume was 3 mL/kg per administration).
- the body weight of the rats; the dose of the test substance administered daily (Dosage) was 325.5 mg/kg rat body weight/day), and the obese control group was given an equal volume of sterile water to evaluate the difference in body weight and visceral fat between the groups.
- the body weight and average food intake of each animal were recorded weekly during the experiment, and the rats were fasted for 8 to 12 hours one night before the completion of the test. Then, the rats were sacrificed, the weight of the fasting stomach was weighed, and the amount of visceral fat was calculated by weighing the peri-testosterone, the fat around the kidney, and the fat around the mesentery. The calculation is the same as in the eighth embodiment.
- test substances were prepared in the following manner.
- ME00C4A composition Mixing 250 mg of green tea extract, 200 mg of turmeric extract, piperine, polyoxyethylene (40) stearate, and an appropriate amount of sterile water is the ME00C4A composition.
- the weight percentage of piperine is 0.1 to 0.5%
- the weight percentage of polyoxyethylene (40) stearate is 0.5 to 1.2%.
- the concentration of piperine is 0.525 to 2.625 mg/mL
- the concentration of polyoxyethylene (40) stearate is 2.625 to 6.3 mg/mL (milligrams solute per milliliter of solution).
- mice Male SD rats were used, which were divided into normal diet control group (ie, NFD-C group), high-fat and high-cholesterol diet control group (ie, HFD-C group), and ME00C4A group.
- rats in other groups were fed with high-fat and high-cholesterol diet for 8 weeks to induce obesity, fatty liver, and non-alcoholic steatohepatitis.
- the ME00C4A composition of the ME00C4A group was administered daily (the dose of the ME00C4A composition (Dosage) was 372 mg/kg rat body weight/day) for 8 weeks, and the normal diet control group (ie, the NFD-C group).
- High-fat, high-cholesterol diet control group ie, the HFD-C group
- High-fat, high-cholesterol diet control group ie HFD-C group
- ME00C4A group rats were given high-fat and high-cholesterol diet during the experiment.
- the body weight and average food intake of each animal were recorded daily, and the rats were fasted for 8 to 10 hours after the test was completed. Then, the rats were sacrificed, the fasting body weight was weighed, and the visceral fat mass was calculated by weighing the peri-testosterone, the peripheral fat of the kidney, and the fat around the mesentery, and the calculation method was the same as that in Example 8.
- NAS non-alcoholic fatty liver disease inflammatory system
- the relative weight gain and body fat percentage of the rats administered ME00C4A were significantly decreased (p ⁇ 0.05) compared with the high fat and high cholesterol diet control group (i.e., the HFD-C group).
- composition of the present invention added with an excipient can achieve a significant weight loss effect and a fat loss effect in rats with fatty liver and nonalcoholic steatohepatitis.
- liver weight was significantly reduced (p ⁇ 0.05).
- composition of the present invention added with an excipient can make liver weight, liver fat mass, total liver cholesterol, and liver triglyceride amount in rats with fatty liver and nonalcoholic steatohepatitis. They are significantly reduced to achieve the effect of treating fatty liver and non-alcoholic steatohepatitis.
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Abstract
Description
Claims (33)
- 一种用于减少体重或体脂肪的组合物,包含:一赋形剂;以及一减重或减脂活性成分组合物,且该减重或减脂活性成分组合物包含表没食子儿茶素没食子酸酯(epigallocatechin gallate,EGCG)以及姜黄素;其中,该赋形剂包含甘油二山俞酸酯、聚氧乙烯硬脂酸酯(polyoxyethylene stearates)、聚山梨醇酯80混合物、维生素E聚乙二醇琥珀酸酯(vitamin E polyethylene glycol succinate)、单硬脂酸甘油酯(glyceryl monostearate)、以及油酸聚乙二醇-6甘油酯(Oleoyl polyoxyl-6glycerides)中的至少一种或其组合;而且,该聚山梨醇酯80混合物包含聚山梨醇酯80以及偏硅酸镁铝(magnesium aluminometasilicate)。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中更包含Glyceryl Palmitostearate、聚山梨醇酯20(polysorbate 20)、泊洛沙姆(poloxamer)、以及聚乙二醇(polyethylene glycol)中的至少一种或其组合。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中更包含胡椒碱。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该用于减少体重或体脂肪的组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为0.1%~20%;抑或是,以该用于减少体重或体脂肪的组合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为0.5%~20%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该用于减少体重或体脂肪的组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.005%~6.7%。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该用于减少体重或体脂肪的组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为1%~15%;抑或是,以该用于减少体重或体脂肪的组合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为1%~15%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该用于减少体重或体脂肪的组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.01%~3.3%。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该用于减少体重或体脂肪的组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为1%~10%;抑或是,以该用于减少体重或体脂肪的组 合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为3%~10%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该用于减少体重或体脂肪的组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.05%~1%。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且该姜黄素的重量以及该聚氧乙烯(32)硬脂酸酯的重量的比值为5.3~26.7;抑或是,该姜黄素的重量以及该聚山梨醇酯80混合物的重量的比值为2~8.9;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且该姜黄素的重量以及该聚氧乙烯(40)硬脂酸酯的重量的比值为40~533.3;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且该减重或减脂活性成分组合物的重量以及该聚氧乙烯(32)硬脂酸酯的重量的比值为9.5~47.5;抑或是,该减重或减脂活性成分组合物的重量以及该聚山梨醇酯80混合物的重量的比值为3.6~15.8;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且该减重或减脂活性成分组合物的重量以及该聚氧乙烯(40)硬脂酸酯的重量的比值为71.3~950。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中更包含甘露醇(mannitol)、微晶纤维素、十二烷基硫酸钠(sodium dodecyl sulfate,SDS)、以及交联甲基纤维素中的至少一种或其组合。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中,该姜黄素的重量以及该表没食子儿茶素没食子酸酯的重量的比值为3.2~0.32;抑或是,以该减重或减脂活性成分组合物的总重量为基础,该表没食子儿茶素没食子酸酯的重量百分比为23.8%~75.8%且该姜黄素的重量百分比为24.2%~76.2%。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,其中,该姜黄素的重量以及该表没食子儿茶素没食子酸酯的重量的比值为3.2~0.4;抑或是,以该减重或减脂活性成分组合物的总重量为基础,该表没食子儿茶素没食子酸酯的重量百分比为23.8%~71.4%且该姜黄素的重量百分比为28.6%~76.2%。
- 如权利要求1所述的用于减少体重或体脂肪的组合物,该减重或减脂活性成分组合物更包含白藜芦醇。
- 一种减少个体体重或体脂肪的方法,包括将一组合物施用于一个体,其中,该组合物包含:一赋形剂;以及一减重或减脂活性成分组合物,且该减重或减脂活性成分组合物包含一表没食子儿茶素没食子酸酯(epigallocatechin gallate,EGCG)以及一姜黄素;其中,该赋形剂包含甘油二山俞酸酯、聚氧乙烯硬脂酸酯(polyoxyethylene stearates)、聚山梨醇酯80混合物、维生素E聚乙二醇琥珀酸酯(vitamin E polyethylene glycol succinate)、单硬脂酸甘油酯(glyceryl monostearate)、以及油酸聚乙二醇-6甘油酯(Oleoyl polyoxyl-6glycerides)中的至少一种或其组合;而且,该聚山梨醇酯80混合物包含聚山梨醇酯80以及偏硅酸镁铝(magnesium aluminometasilicate)。
- 如权利要求12所述的方法,该组合物中更包含Glyceryl Palmitostearate、聚山梨醇酯20(polysorbate 20)、泊洛沙姆(poloxamer)、以及聚乙二醇(polyethylene glycol)中的至少一种或其组合。
- 如权利要求12所述的方法,该组合物中更包含胡椒碱。
- 如权利要求12所述的方法,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为0.1%~20%;抑或是,以该组合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为0.5%~20%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.005%~6.7%。
- 如权利要求12所述的方法,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为1%~15%;抑或是,以该组合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为1%~15%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.01%~3.33%。
- 如权利要求12所述的方法,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为1%~10%;抑或是,以该组合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为3%~10%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.05%~1%。
- 如权利要求12所述的方法,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且该姜黄素的重量以及该聚氧乙烯(32)硬脂酸酯的重量的比值为5.3~26.7;抑或是,该姜黄素的重量以及该聚山梨醇酯80混合物的重量的比值为2~8.9;抑或是,该聚氧乙烯硬脂 酸酯为聚氧乙烯(40)硬脂酸酯,且该姜黄素的重量以及该聚氧乙烯(40)硬脂酸酯的重量的比值为40~533.3;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且该减重或减脂活性成分组合物的重量以及该聚氧乙烯(32)硬脂酸酯的重量的比值为9.5~47.5;抑或是,该减重或减脂活性成分组合物的重量以及该聚山梨醇酯80混合物的重量的比值为3.6~15.8;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且该减重或减脂活性成分组合物的重量以及该聚氧乙烯(40)硬脂酸酯的重量的比值为71.3~950。
- 如权利要求12所述的方法,其中该组合物中更包含甘露醇(mannitol)、微晶纤维素(microcrystalline cellulose)、十二烷基硫酸钠(sodium dodecyl sulfate,SDS)、以及交联甲基纤维素中的至少一种或其组合。
- 如权利要求12所述的方法,该姜黄素的重量以及该表没食子儿茶素没食子酸酯的重量的比值为3.2~0.32;抑或是,以该减重或减脂活性成分组合物的总重量为基础,该表没食子儿茶素没食子酸酯的重量百分比为23.8%~75.8%且该姜黄素的重量百分比为24.2%~76.2%。
- 如权利要求12所述的方法,该姜黄素的重量以及该表没食子儿茶素没食子酸酯的重量的比值为3.2~0.4;抑或是,以该减重或减脂活性成分组合物的总重量为基础,该表没食子儿茶素没食子酸酯的重量百分比为23.8%~71.4%且该姜黄素的重量百分比为28.6%~76.2%。
- 如权利要求12所述的方法,该减重或减脂活性成分组合物更包含白藜芦醇。
- 如权利要求12所述的方法,为以口服方式将该组合物施用于该个体。
- 如权利要求12所述的方法,该个体为一体重正常的个体、体重过重的个体、肥胖的个体、具有脂肪肝的个体、或具有非酒精性脂肪性肝炎(Non-alcoholic steatohepatitis;NASH)的个体。
- 一种治疗脂肪肝或非酒精性脂肪性肝炎的方法,包括将一组合物施用于一具有脂肪肝或具有非酒精性脂肪性肝炎的个体,其中,该组合物包含:一赋形剂;以及一减重或减脂活性成分组合物,且该减重或减脂活性成分组合物包含一表没食子儿茶素没食子酸酯(epigallocatechin gallate,EGCG)以及一姜黄素;其中,该赋形剂包含甘油二山俞酸酯、聚氧乙烯硬脂酸酯(polyoxyethylene stearates)、 聚山梨醇酯80混合物、维生素E聚乙二醇琥珀酸酯(vitamin E polyethylene glycol succinate)、单硬脂酸甘油酯(glyceryl monostearate)、以及油酸聚乙二醇-6甘油酯(Oleoyl polyoxyl-6glycerides)中的至少一种或其组合;而且,该聚山梨醇酯80混合物包含聚山梨醇酯80以及偏硅酸镁铝(magnesium aluminometasilicate)。
- 如权利要求25所述的方法,该组合物中更包含Glyceryl Palmitostearate、聚山梨醇酯20(polysorbate 20)、泊洛沙姆(poloxamer)、以及聚乙二醇(polyethylene glycol)中的至少一种或其组合。
- 如权利要求25所述的方法,该组合物中更包含胡椒碱。
- 如权利要求25所述的方法,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(32)硬脂酸酯的重量百分比为0.1%~20%;抑或是,以该组合物的总重量为基础,该聚山梨醇酯80混合物的重量百分比为0.5%~20%;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且以该组合物的总重量为基础,该聚氧乙烯(40)硬脂酸酯的重量百分比为0.005%~6.7%。
- 如权利要求25所述的方法,其中,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且该姜黄素的重量以及该聚氧乙烯(32)硬脂酸酯的重量的比值为5.3~26.7;抑或是,该姜黄素的重量以及该聚山梨醇酯80混合物的重量的比值为2~8.9;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且该姜黄素的重量以及该聚氧乙烯(40)硬脂酸酯的重量的比值为40~533.3;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(32)硬脂酸酯,且该减重或减脂活性成分组合物的重量以及该聚氧乙烯(32)硬脂酸酯的重量的比值为9.5~47.5;抑或是,该减重或减脂活性成分组合物的重量以及该聚山梨醇酯80混合物的重量的比值为3.6~15.8;抑或是,该聚氧乙烯硬脂酸酯为聚氧乙烯(40)硬脂酸酯,且该减重或减脂活性成分组合物的重量以及该聚氧乙烯(40)硬脂酸酯的重量的比值为71.3~950。
- 如权利要求25所述的方法,其中该组合物中更包含甘露醇(mannitol)、微晶纤维素(microcrystalline cellulose)、十二烷基硫酸钠(sodium dodecyl sulfate,SDS)、以及交联甲基纤维素中的至少一种或其组合。
- 如权利要求25所述的方法,该姜黄素的重量以及该表没食子儿茶素没食子酸酯的重量的比值为3.2~0.32;抑或是,以该减重或减脂活性成分组合物的总重量为基础,该表没食子儿茶素没食子酸酯的重量百分比为23.8%~75.8%且该姜黄素的重量百分比为24.2%~76.2%。
- 如权利要求25所述的方法,该姜黄素的重量以及该表没食子儿茶素没食子酸酯的重量的比值为3.2~0.4;抑或是,以该减重或减脂活性成分组合物的总重量为基础,该表没食子儿茶素没食子酸酯的重量百分比为23.8%~71.4%且该姜黄素的重量百分比为28.6%~76.2%。
- 如权利要求25所述的方法,为以口服方式将该组合物施用于该具有脂肪肝或具有非酒精性脂肪性肝炎的个体。
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CN103717224A (zh) * | 2011-06-07 | 2014-04-09 | 独立行政法人科学技术振兴机构 | 一氧化碳(co)对脂肪酸和胆固醇摄取的抑制 |
WO2017037594A2 (zh) * | 2015-08-28 | 2017-03-09 | 康霈生技股份有限公司 | 用于减少局部脂肪的医药组成物及其用途 |
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US9731015B2 (en) * | 2012-08-04 | 2017-08-15 | Eric Hauser Kuhrts | Water-soluble lipophilic natural compound formulations |
CN103784421B (zh) * | 2014-02-27 | 2016-04-27 | 哈尔滨医科大学 | 载姜黄素和胡椒碱的固体脂质纳米粒及其制备方法 |
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CN103717224A (zh) * | 2011-06-07 | 2014-04-09 | 独立行政法人科学技术振兴机构 | 一氧化碳(co)对脂肪酸和胆固醇摄取的抑制 |
WO2017037594A2 (zh) * | 2015-08-28 | 2017-03-09 | 康霈生技股份有限公司 | 用于减少局部脂肪的医药组成物及其用途 |
WO2017049157A1 (en) * | 2015-09-18 | 2017-03-23 | Duke University | Methods and compositions for the treatment of steatosis-associated disorders |
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CN109498616A (zh) * | 2018-12-29 | 2019-03-22 | 中国医科大学附属第医院 | Egcg在制备改善肝脏炎症及胰岛素抵抗药物中的应用 |
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TW201836602A (zh) | 2018-10-16 |
EP3603628A1 (en) | 2020-02-05 |
EP3603628A4 (en) | 2020-12-02 |
AU2018241639B2 (en) | 2020-10-15 |
CN110446492A (zh) | 2019-11-12 |
CA3055451C (en) | 2021-10-12 |
CA3055451A1 (en) | 2018-10-04 |
AU2018241639A1 (en) | 2019-11-14 |
AU2020277116A1 (en) | 2020-12-24 |
JP2020515552A (ja) | 2020-05-28 |
TWI676476B (zh) | 2019-11-11 |
KR20190134671A (ko) | 2019-12-04 |
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