CN104126801B - A kind of blood-fat reducing composition containing sterol - Google Patents

A kind of blood-fat reducing composition containing sterol Download PDF

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CN104126801B
CN104126801B CN201410394353.4A CN201410394353A CN104126801B CN 104126801 B CN104126801 B CN 104126801B CN 201410394353 A CN201410394353 A CN 201410394353A CN 104126801 B CN104126801 B CN 104126801B
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tea polyphenols
blood
food
phytosterol
chinese medicine
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CN104126801A (en
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曹玉平
周学晋
陈历水
徐永安
杨巍
武文华
梁广震
蒋一鸣
陈学兵
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COFCO TIANKE BIOENGINEERING (TIANJIN) Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/06Fungi, e.g. yeasts
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K36/00Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
    • A61K36/18Magnoliophyta (angiosperms)
    • A61K36/185Magnoliopsida (dicotyledons)
    • A61K36/82Theaceae (Tea family), e.g. camellia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/366Lactones having six-membered rings, e.g. delta-lactones

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Natural Medicines & Medicinal Plants (AREA)
  • Epidemiology (AREA)
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Abstract

The invention discloses a kind of blood-fat reducing composition containing sterol, formed by following component by quality: phytosterol 24%~35%, red colouring agent for food, also used as a Chinese medicine 17%~28%, Tea Polyphenols 3%~8%, lactose 18%~30%, dextrin 7%~12%, sodium carboxymethyl starch 5%~8%, dolomol 0.7%~1%; The purity of described phytosterol is >=90%, and the Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for described composition >=0.08%, and the Tea Polyphenols quality in Tea Polyphenols accounts for described composition >=3%. Its main component phytosterol of composition of the present invention, red colouring agent for food, also used as a Chinese medicine and Tea Polyphenols three compatibility play synergy, can suppress the absorption of cholesterol and triglycerides and synthesize, accelerate metabolism and the excretion of cholesterol and triglycerides, effectively reduce TC, TG, LDL-C level in blood, HDL-C level in rising blood, reaches effect of significant reduction blood fat.

Description

A kind of blood-fat reducing composition containing sterol
Technical field
The present invention relates to a kind of blood-fat reducing composition containing sterol.
Background technology
In modern medicine, hyperlipidemia be due to fat metabolism or running extremely make cholesterol (TC), triglycerides (TG) and (or)A kind of illness that low-density lipoprotein (LDL) is too high and (or) HDL (HDL) is too low and cause. Dyslipidemia is embodied inThe change of one or several index content such as TC, TG and LDL, HDL etc. To detect clinically blood fat project as the interior blood that disintegratesAn important means of fat metabolism status, lipids detection project mainly contains TC, TG, and apolipoprotein is serial as HDL, LDL etc.,These projects are synthetic, the metabolism situation of blood fat in ipsilateral antimer never, and clinical diagnosis, treatment and research are all had shouldBy value. Along with improving constantly of people's living standard, the incidence of disease of hyperlipidemia is obvious ascendant trend. Therefore find efficientNontoxic blood lipid-lowering medicine and health medicine have important realistic meaning.
The present invention relates to a kind of whole formula of blood-fat reducing composition containing sterol is mainly according to modern medical theory prescription, with plantSterol, red colouring agent for food, also used as a Chinese medicine, Tea Polyphenols are primary raw material. Phytosterol is that to utilize soybean wet goods vegetable oil cut or Tall oil be raw material,Making by explained hereafter such as saponification, extraction, crystallizations, is a kind of natural active matter being present in plant. Phytosterol canHinder competitively intestinal absorption cholesterol, promote that cholesterol excretes, can significantly reduce serum TC, LDL-C level, reachTo the effect of reducing blood lipid. Red colouring agent for food, also used as a Chinese medicine is taking rice as raw material, breeds a kind of aubergine rice song forming through monascus, and its taste is sweet, propertyTemperature, returns liver, spleen, large intestine channel, have promoting blood circulation and removing blood stasis, effect of reinforcing spleen to promote digestion, its active ingredient contestable suppresses cholesterolAn important rate-limiting enzyme in anabolism, thus the synthetic of cholesterol reduced, can effectively reduce TC, TG, LDL-C water in bloodFlat, HDL-C level in rising blood, effectively reduces blood fat. Tea Polyphenols is the class polyphenol chemical combination extracting from natural plants tealeavesThing complex, accounts for greatly 25% of dry weight of tea leaves, mainly comprises catechin, flavones and flavonols, flower by its chemical constitutionThe four large class materials such as pigment, phenolic acid and depside. Tea Polyphenols has plurality of health care functions and pharmacodynamics effect, and it can suppress intestinesThe absorption of exogenous cholesterol in road, accelerates the metabolism of cholesterol and the excretion of promotion cholesterol, can reduce the suction of exogenous TGThe metabolism of TG and the excretion of promotion aliphatic acid received, accelerated, thereby TC, TG metabolism regulated. Experiment showed, that Tea Polyphenols can reduceThe level of TG, TC and LDL-C in serum, rising HDL-C level. The mutual compatibility of three, synergy, can suppress cholesterolAnd the absorption of triglycerides and synthetic, accelerate metabolism and the excretion of cholesterol and triglycerides, effectively reduce TC in blood, TG, LDL-CLevel, HDL-C level in rising blood, reaches the effect that reduces blood fat.
Summary of the invention
The object of this invention is to provide blood-fat reducing composition a kind of determined curative effect, that contain efficiently sterol.
Technical scheme of the present invention is summarized as follows:
Containing the blood-fat reducing composition of sterol, formed by following component by quality: phytosterol 24%~35%, red colouring agent for food, also used as a Chinese medicine 17%~28%, Tea Polyphenols 3%~8%, lactose 18%~30%, dextrin 7%~12%, sodium carboxymethyl starch 5%~8%, dolomol 0.7%~1%; Purity >=90% of described phytosterol, the Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for described composition >=0.08%, in Tea PolyphenolsTea Polyphenols quality account for described composition >=3%.
Composition of the present invention can method routinely be made oral formulations, comprising: granule, tablet or pulvis etc.
Its main component phytosterol of composition of the present invention, red colouring agent for food, also used as a Chinese medicine and Tea Polyphenols three compatibility play synergy, can suppress courage solidThe absorption of alcohol and triglycerides and synthetic, accelerates metabolism and the excretion of cholesterol and triglycerides, effectively reduce TC in blood, TG,LDL-C level, HDL-C level in rising blood, reaches effect of significant reduction blood fat.
Detailed description of the invention
The following examples are in order to enable those skilled in the art to understand better the present invention, but the present invention are not appointedWhat restriction.
Phytosterol used in the present invention, its standard is Q/17A0772S-2011, sky section of China Oil and Food Import and Export Corporation bioengineering (Tianjin) hasLimit company sells, and the phytosterol that meets other enterprise of above-mentioned standard also can be for the present invention.
Tea Polyphenols: product standard " QB2154-1995 food additives Tea Polyphenols ", light industry professional standard.
Embodiment 1
Containing the blood-fat reducing composition of sterol, made by following component by weight percentage: phytosterol 28%, red colouring agent for food, also used as a Chinese medicine 22%,Tea Polyphenols 6%, lactose 28%, dextrin 8%, sodium carboxymethyl starch 7%, dolomol 1%; Wherein the purity of phytosterol is 90%,Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for 0.08% of described composition, and the Tea Polyphenols quality in Tea Polyphenols accounts for described composition 3%.
Embodiment 2
Containing the blood-fat reducing composition of sterol, made by following component by weight percentage: phytosterol 24%, red colouring agent for food, also used as a Chinese medicine 28%,Tea Polyphenols 8%, lactose 19.3%, dextrin 12%, sodium carboxymethyl starch 8%, dolomol 0.7%; The wherein purity of phytosterolBe 90.5%, the Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for 0.083% of described composition, and the Tea Polyphenols quality in Tea Polyphenols accounts for described groupCompound 3.1%.
Embodiment 3
Containing the blood-fat reducing composition of sterol, made by following component by weight percentage: phytosterol 29%, red colouring agent for food, also used as a Chinese medicine 17%,Tea Polyphenols 8%, lactose 30%, dextrin 7%, sodium carboxymethyl starch 8%, dolomol 1%; Wherein the purity of phytosterol is 90.5%,Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for 0.083% of described composition, and the Tea Polyphenols quality in Tea Polyphenols accounts for described composition 3.1%.
Embodiment 4
Containing the blood-fat reducing composition of sterol, made by following component by weight percentage: phytosterol 35%, red colouring agent for food, also used as a Chinese medicine 18%,Tea Polyphenols 3%, lactose 30%, dextrin 8%, sodium carboxymethyl starch 5%, dolomol 1%; Wherein the purity of phytosterol is 90.5%,Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for 0.083% of described composition, and the Tea Polyphenols quality in Tea Polyphenols accounts for described composition 3.1%.
Embodiment 5
Containing the blood-fat reducing composition of sterol, made by following component by weight percentage: phytosterol 30%, red colouring agent for food, also used as a Chinese medicine 27%,Tea Polyphenols 6%, lactose 18%, dextrin 10%, sodium carboxymethyl starch 8%, dolomol 1%; Wherein the purity of phytosterol is 90.5%,Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for 0.083% of described composition, and the Tea Polyphenols quality in Tea Polyphenols accounts for described composition 3.1%.
Embodiment 6
Preparation method:
1) sieve: by phytosterol, red colouring agent for food, also used as a Chinese medicine, Tea Polyphenols, lactose, dextrin, sodium carboxymethyl starch, dolomol mistake respectively80 mesh sieves, each component takes by each Example formulations amount respectively, for subsequent use;
2) mix: phytosterol, red colouring agent for food, also used as a Chinese medicine, Tea Polyphenols, lactose, dextrin and sodium carboxymethyl starch are put in mixer and mixed 30Minute, mix, obtain total mixed powder;
3) granulate: be 50% ethanol water to adding appropriate volumetric concentration in total mixed powder, stir, softwood processed;Cross 18 mesh sieves with oscillating granulator again and granulate, obtain wet granular. Wet granular is with HighefficientFluidbeddrier dry (approximately 50 DEG C), dryThe whole grain of dry rear mistake 18 orders, obtains dry particle;
4) compressing tablet: dry particle and dolomol are put in mixer and mixed 5 minutes, mix, obtain always mixed particle; Total mixedGrain use high speed tablet press compressing tablet, trimmer is heavily 1.0g/ sheet, rejects defective, obtains plain sheet;
5) dressing: take coating powder, adding volumetric concentration is 70% ethanol water, stirs, and makes quality denseDegree is 8% coating powder solution. Sugar coating machine dressing for the sheet heart (increasing weight approximately 2%), obtains coating tablet.
Can also be prepared into according to a conventional method granule or pulvis etc.
Embodiment 7
The present invention is containing auxiliary lipid-lowering function zoopery (foundation " the health food inspection and evaluation skill of the blood-fat reducing composition of sterolArt specification (2003 editions) " content tests).
Auxiliary lipid-lowering function zoopery
1 materials and methods
1.1 samples: press step 4 in the composition of embodiment 1 and the preparation method of embodiment 6) (the abbreviation lipopenicillinase of the rear plain sheet obtainingSheet).
1.2 animals used as test: select body weight 152~175g, 40 of SPF level male Wistar rats, by Beijing, dimension tonneau China is realTesting animal Science and Technology Ltd. provides, the quality certification number: SCXK (capital) 2006-00090191366.
1.3 animal used as test high lipid foods: feed is provided by the feed corporation,Ltd that pulls together of Beijing Australia of section, the feed quality certification number: SCXK (capital)2009-00120193842, filling a prescription is: basal feed 78.8%, cholesterol 1%, lard 10%, yolk powder 10%, 0.2%Cholate.
1.4 experimental animal feeding environment: SPF level experimental animal room, 20~25 DEG C of temperature, relative humidity 40~70%RH is qualifiedCard number: SYXK (Tianjin) 2008-0004.
1.5 dosage groupings: tablets of reducing blood fat, people intend with dosage be 6.0g/60kgBW day, specifically dosage is designed to: 0.5g/kgBW,1.0g/kgBW, 2.0g/kgBW, be equivalent to respectively people and intend 5 times, 10 times, 20 times with dosage. Take respectivelyTested material 20.0g, 40.0g, 80.0g, each adding distil water is to 400ml, and per os gavage, all vibrates and mixes before each gavage,Gavage amount 1.0ml/100gBW, model control group gives equivalent distilled water, every day 1 time, carries out continuously 30 days. AnimalSingle cage is fed.
1.6 experimental techniques: employing hyperlipoidemia method-preventative given the test agent of giving, under experimental situation, feed with basal feedRaise rat and observe after 5 days, angular vein clump is got blood, enzymatic assays serum total cholesterol (TC), triglycerides (TG) andHDL-C (HDL-C), is divided into 4 groups according to TC level at random by animal: model control group and 3 are subject toExamination thing group, every group of 10 animals, from formal experiment, each treated animal is fed and is raised high lipid food, except model control group,Per os gavage gives the tested material of various dose simultaneously. Experiment finishes rear fasting 16h, and angular vein clump is got blood, measures serumTC, TG and HDL-C.
1.7 key instruments and reagent: TOSHIBATBA-40FR automatic clinical chemistry analyzer. T-CHOL (TC), triglycerides(TG) and HDL-C (HDL-C) kit, carry by Beijing Zhong Shengbei control Bioisystech Co., LtdSupply.
1.8 statistical methods: respectively organize data and all adopt variance analysis in SPSS11.5FORWINDOWS to carry out statistical analysis, variance is notNeat person adopts data transaction, adopts nonparametric statistics as still uneven after conversion.
2 results
The impact of 2.1 tablets of reducing blood fat on rat body weight
From table 1, with the tablets of reducing blood fat gavage rat of various dose 30 days, each treated animal growth, movable normal. Each doseThe weightening finish of amount treated animal and model control group comparison, the equal not statistically significant of difference (P > 0.05).
The impact (g, means standard deviation) of table 1 tablets of reducing blood fat on rat body weight
Experiment showed, embodiment 2-5 the preparation method of composition embodiment 6 in the plain sheet that the obtains impact on rat body weightThe result of result and embodiment 1 is approximate.
The impact of 2.2 tablets of reducing blood fat on rat fat
From table 2~4, test latter stage, high dose group animal blood serum T-CHOL (TC) and triglyceride (TG) are equalLower than model control group, high dose group HDL (HDL-C) is higher than model control group, and difference has statistics meaningJustice (P<0.05); All the other each dosage groups, indices and model control group comparison, difference not statistically significant (P>0.05).
The impact (means standard deviation) of table 2 tablets of reducing blood fat on Serum TC
* with control group comparison, difference has statistical significance (P < 0.05)
The impact (means standard deviation) of table 3 tablets of reducing blood fat on rat blood serum TG
* with control group comparison, difference has statistical significance (P < 0.05)
The impact (means standard deviation) of table 4 tablets of reducing blood fat on rat blood serum HDL-C
* with control group comparison, difference has statistical significance (P < 0.05)
Experiment showed, embodiment 2-5 the preparation method of composition embodiment 6 in the impact of the plain sheet rat fat that obtainsResult and the result of embodiment 1 approximate.
3 brief summaries
With 0.5g/kgBW, 1.0g/kgBW, 2.0g/kgBW dosage (be equivalent to respectively people intend with 5 times of dosage,10 times, 20 times) tablets of reducing blood fat gavage rat 30 days, each treated animal vegetative activity is good, each dosage treated animal weightening finish and mouldType control group is compared, difference not statistically significant (P > 0.05); High dose group animal blood serum T-CHOL (TC) and glycerineThree esters (TG) are all lower than model control group, and difference has statistical significance (P < 0.05); High dose group HDL(HDL-C) higher than model control group, and difference has statistical significance (P < 0.05). According to " health food is checked and commentedValency technical specification " (version in 2003) auxiliary lipid-lowering function result criterion, prompting tablets of reducing blood fat has the auxiliary animal that reducesBlood fat function.

Claims (1)

1. containing the blood-fat reducing composition of sterol, it is characterized in that the following method of described composition makes:
1) sieve: by phytosterol, red colouring agent for food, also used as a Chinese medicine, Tea Polyphenols, lactose, dextrin, sodium carboxymethyl starch, dolomol mistake respectively80 mesh sieves, each component takes by quality respectively: phytosterol 24%~35%, red colouring agent for food, also used as a Chinese medicine 17%~28%, Tea Polyphenols 3%~8%, breastSugar 18%~30%, dextrin 7%~12%, sodium carboxymethyl starch 5%~8%, dolomol 0.7%~1%; Described phytosterol pureDegree is for >=90%, and the Lovastatin quality in red colouring agent for food, also used as a Chinese medicine accounts for described composition >=0.08%, and the Tea Polyphenols quality in Tea Polyphenols accounts for described groupCompound >=3%; For subsequent use;
2) mix: phytosterol, red colouring agent for food, also used as a Chinese medicine, Tea Polyphenols, lactose, dextrin and sodium carboxymethyl starch are put in mixer and mixed 30Minute, mix, obtain total mixed powder;
3) granulate: be 50% ethanol water to adding volumetric concentration in total mixed powder, stir, softwood processed; Again with shakingPendulum-type granulator is crossed 18 mesh sieves and is granulated, and obtains wet granular; Wet granular is dry with 50 DEG C of HighefficientFluidbeddriers, dry rear 18 orders of crossingWhole grain, obtains dry particle;
4) compressing tablet: dry particle and dolomol are put in mixer and mixed 5 minutes, mix, obtain always mixed particle; Total mixedGrain use high speed tablet press compressing tablet, trimmer is heavily 1.0g/ sheet, rejects defective, obtains plain sheet;
5) dressing: take coating powder, adding volumetric concentration is 70% ethanol water, stirs, and makes quality denseDegree is 8% coating powder solution; Element sheet sheet heart sugar coating machine dressing, obtains coating tablet.
CN201410394353.4A 2014-08-12 2014-08-12 A kind of blood-fat reducing composition containing sterol Active CN104126801B (en)

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CN105124569A (en) * 2015-07-13 2015-12-09 北京世纪合辉医药科技股份有限公司 Blood-fat-reducing health-caring food and preparation method of same
CN105494812A (en) * 2015-12-29 2016-04-20 中粮集团有限公司 Beverage capable of lowering blood lipid and application of beverage
CN105535601A (en) * 2015-12-30 2016-05-04 徐州市铜山区生命科学研究院 Medicinal and edible dual-purpose compound red yeast rice phytosterol health protection medicine for preventing and treating cardio-cerebrovascular disease and preparation method thereof
CN105533747A (en) * 2015-12-31 2016-05-04 哈药集团技术中心 Health food capable of assisting in reduction of blood fat
CN106620344A (en) * 2016-12-27 2017-05-10 南京圣诺生物科技实业有限公司 Composition with blood lipid lowering effect and preparation method thereof
CN109596844A (en) * 2018-12-18 2019-04-09 江苏大学附属医院 It is a kind of to detect the drug and application that metabolic syndrome is fallen ill
CN109619571A (en) * 2019-02-20 2019-04-16 吉林大学 A kind of panax ginseng plant sterol chewable tablets and preparation method thereof with hypolipemic function
CN113730547A (en) * 2021-09-17 2021-12-03 江苏协合转化医学研究院有限公司 Composition for reducing blood fat and dissolving thrombus, preparation method and application thereof

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