NL2029794B1 - Application of three yellows and two fragrances powder in the preparation of drugs for preventing and treating uv damage, extract of three yellows and two fragrances powder and cream for preventing and treating uv damage - Google Patents

Application of three yellows and two fragrances powder in the preparation of drugs for preventing and treating uv damage, extract of three yellows and two fragrances powder and cream for preventing and treating uv damage Download PDF

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NL2029794B1
NL2029794B1 NL2029794A NL2029794A NL2029794B1 NL 2029794 B1 NL2029794 B1 NL 2029794B1 NL 2029794 A NL2029794 A NL 2029794A NL 2029794 A NL2029794 A NL 2029794A NL 2029794 B1 NL2029794 B1 NL 2029794B1
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extract
cream
yellows
fragrances
powder
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NL2029794A
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Zhu Junbo
Gu Wenqi
Duan Yabin
La Linli
Yang Jianxin
Qu Ning
Zheng Yongbiao
Li Hailin
Bai Xue
Wang Yafeng
Liu Guiqin
Zhou Yang
Su Xiaodong
Duo Delong
Wang Qian
Li Xiangyang
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Univ Qinghai
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/18Antioxidants, e.g. antiradicals
    • 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)
    • A61K36/32Burseraceae (Frankincense family)
    • A61K36/324Boswellia, e.g. frankincense
    • 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)
    • A61K36/32Burseraceae (Frankincense family)
    • A61K36/328Commiphora, e.g. mecca myrrh or balm of Gilead
    • 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)
    • A61K36/70Polygonaceae (Buckwheat family), e.g. spineflower or dock
    • A61K36/708Rheum (rhubarb)
    • 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)
    • A61K36/71Ranunculaceae (Buttercup family), e.g. larkspur, hepatica, hydrastis, columbine or goldenseal
    • A61K36/718Coptis (goldthread)
    • 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)
    • A61K36/75Rutaceae (Rue family)
    • A61K36/756Phellodendron, e.g. corktree

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  • Natural Medicines & Medicinal Plants (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Biochemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
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  • Cosmetics (AREA)

Abstract

The present disclosure provides an application of Three Yellows and Two Fragrances Powder in the preparation of drugs for preventing and treating UV damage, an extract of Three Yellows and Two Fragrances Powder, and a cream for preventing and treating UV 5 damage, belonging to the field of sunscreen technology. The Three Yellows and Two Fragrances Powder of the present disclosure is originated from the book “Detailed Analysis of Epidemic Warm Diseases ° Upper—jiao” by Wu Tang in the Qing Dynasty. The cream for preventing and treating UV damage provided by the present 10 disclosure utilizes a cream extract and a volatile oil extracted from Three Yellows and Two Fragrances Powder. Because of the high content of active ingredients in the cream extract and the volatile oil, the cream for preventing and treating UV damage has a better effect of preventing and treating UV damage. 15 (+ Fig. l)

Description

P799/NLpd
APPLICATION OF THREE YELLOWS AND TWO FRAGRANCES POWDER IN THE
PREPARATION OF DRUGS FOR PREVENTING AND TREATING UV DAMAGE,
EXTRACT OF THREE YELLOWS AND TWO FRAGRANCES POWDER AND CREAM FOR
PREVENTING AND TREATING UV DAMAGE
TECHNICAL FIELD
The present disclosure relates to the field of sunscreen technology, more particularly to an application of Three Yellows and Two Fragrances Powder in the preparation of drugs for prevent- ing and treating UV damage, an extract of Three Yellows and Two
Fragrances Powder, and a cream for preventing and treating UV dam- age.
BACKGROUND ART
The natural environment in the plateau areas is harsh. Spe- cial environmental factors such as low oxygen, cold, dry, strong wind and strong UV radiation have caused great harm people who live in the plateau areas and affected their quality of life and physical and mental health. Studies have shown that the incidence of skin diseases in plateau areas is much higher than that in plain areas. Among them, sunlight-related skin diseases are the most common skin diseases in plateau areas, which are related to the strong UV irradiation on the plateau.
Presently, there are two strategies for the prevention and treatment of UV damage:reducing UV irradiation and treating UV damage. The measures to reduce UV irradiation include wearing sun- screen clothing, avoiding the sun during peak UV periods, and ap- plying sunscreen creams appropriately. The application of sun- screen creams can effectively protect the skin from UV damage.
Common sunscreen creams are mainly physical shielding agents and chemical absorbents. Physical shielding agents mainly include ti- tanium dioxide, zinc oxide, etc., which mainly utilize particles with a diameter of about 100 nm to form a uniform barrier layer on the surface of the skin to scatter or reflect ultraviolet light, to protect the skin from sunburns. This type of sun-screening agents are stable, but excessive use of them will leave a solid sticky substance on the skin surface that affects the sensory and visual effects, and the particles can penetrate into the skin to block pores, affecting the normal respiration of the epidermis, easily causing skin problems and new skin diseases and other unde- sirable consequences. Chemical absorbents mainly include p- aminobenzoic acid (PABA) and its derivatives, salicylate and its derivatives, cinnamic acid, etc. They utilize the n-n* transition of the conjugated system in the aromatic compound that binds to the carbonyl group to absorb ultraviolet rays, and resonant duan- tum is generated through molecular resonance, which converts ul- traviolet light energy into harmless visible light to play a pro- tective role. This type of sun-screening agents has the advantages of wide UV absorption spectrum, high absorption intensity, and significant sun protection effect, but they will decompose under the light to produce free radicals or intermediate products that are harmful to the human body; moreover, they are prone to oxida- tive deterioration, leading to skin allergies and causing damage to the skin or the body for a long-term use.
Currently, there are several kinds of treatment methods and drugs for the skin damage caused by UV rays. Retinoids are used to treat UV damage. Tretinoin and tazarotene are two topical vitamin
A derivatives approved by the FDA for the treatment of UV-induced photoaging, which can increase the production of collagen and up- regulate the proliferation of fibroblasts and block the degrada- tion of dermal matrix after sun exposure, therefore, they can sig- nificantly improve the pigmentation and rough skin surface caused by UV rays. However, long-term use of this cream may cause retin- oid dermatitis characterized by erythema and peeling. Oral or top- ical antioxidants are also an effective way to treat UV damage.
Commonly used antioxidants include vitamin C, vitamin E, lipoic acid, and coenzyme 9, etc. Vitamin C is a popular antioxidant, which has been proven to up-regulate the synthesis of skin colla- gen, prevent erythema after UV irradiation, reduce facial wrin- kles. However, vitamin C has poor permeability after topical use and is easily oxidized with poor stability, leading to its short half-life. Vitamin E has good anti-oxidation ability, and has ex-
cellent moisturizing and anti-inflammatory ability. It can be used as a preservative, so it is present in many skin care products.
Lipoic acid also has antioxidant and anti-inflammatory properties, and its anti-inflammatory effect is mainly achieved by down- regulating the production of transcription factors related to the production of inflammatory cytokines. Coenzyme Q derivatives re- duce skin roughness and fine lines by inhibiting the production of reactive oxygen species, and increase skin hydration to treat UV damage. The combination of antioxidants or combination of antioxi- dants and sunscreen creams can enhance their protective effect and exert a greater effect of anti-UV damage
Traditional Chinese medicine preparations have huge ad- vantages over western medicines in treatment of diseases. Tradi- tional Chinese medicines are safer than western medicines and can exert therapeutic effects through multiple mechanisms to achieve the best therapeutic effect. Studies have shown that some tradi- tional Chinese medicines have a certain UV protection effect, such as Chinese medicine monomers astragaloside IV, gypenosides, cordyceps polysaccharides, etc., single Chinese herbs rhodiola, astragalus, aloe, etc. Aloe vera gels made from aloe have a wide range of applications in the clinical treatment of skin damage caused by UV rays, which have both sun blocking effect and post- sun repairing effect. In addition, studies have shown that the compound medicines Yupingfeng powder, Danggui Shaoyao powder, and
Shenlingbaizhu powder also have a certain UV protection effect.
Although studies have shown that traditional Chinese medicines have the effect of anti-UV damage, there are nearly no traditional
Chinese medicine preparations available for the treatment of UV damage in the clinical practices.
SUMMARY
The object of the present disclosure is to provide an appli- cation of Three Yellows and Two Fragrances Powder in the prepara- tion of drugs for preventing and treating UV damage, an extract of
Three Yellows and Two Fragrances Powder, and a cream for prevent- ing and treating UV damage. Frankincense and myrrh contained in
Three Yellows and Two Fragrances Powder have the effects of detu-
mescence and promoting granulation, and invigorating blood circu- lation and alleviating pain; rhubarb, coptis and phellodendron have the effects of eliminating dampness and detoxification; thus, it indicates that Three Yellows and Two Fragrances Powder is suit- able for the prevention and treatment of UV damage.
In order to achieve the foregoing object, the present adopts the following technical solution:
The present disclosure provides an application of Three Yel- lows and Two Fragrances Powder in the preparation of drugs for preventing and treating UV damage, wherein the Three Yellows and
Two Fragrances Powder is a mixture of frankincense, myrrh, rhu- barb, coptis and phellodendron at a mass ratio of 1:1:2:2:2.
Preferably, the Three Yellows and Two Fragrances Powder is used in the form of an extract of Three Yellows and Two Fragrances
Powder.
The present disclosure further provides an extract of Three
Yellows and Two Fragrances Powder, the extract comprises a cream extract and a volatile oil; the cream extract comprises a water extract and an alcohol extract; the water extract, the alcohol ex- tract and the volatile oil are prepared by the following steps: mixing frankincense, myrrh and water, and sequentially per- forming leaching and steam distillation extraction to obtain the volatile oil, a water extracting solution and a residue; performing ethanol precipitation of the water extracting so- lution to obtain the water extract; performing ethanol heating reflux extraction of the residue, rhubarb, coptis and phellodendron, to obtain the alcohol extract.
Preferably, the ratio of the total mass of frankincense and myrrh to the volume of water is 1 g: (6-10) mL.
Preferably, the time for the leaching is 0.01-2 h;
Preferably, the time for the steam distillation extraction time is 3-10 h.
Preferably, the reagent for the ethanol heating reflux ex- traction is ethanol solution; the volume concentration of the eth- anol solution is 60-80%; the ratio of the total mass of the resi- due, rhubarb, coptis and phellodendron to the volume of the etha- nol solution is 1 g: (8-12) mL.
Preferably, the ethanol heating reflux extraction is per- formed for 1-3 times, and the time for each ethanol heating reflux extraction is 1-3 h.
The present disclosure further provides a cream for prevent- 5 ing and treating UV damage, comprising the following components in percentage by weight: stearic acid 4.5-6%, glyceryl monostearate 2.5-5.5%, liquid paraffin 7.5-12.5%, vaseline 2.5-7.0%, emulsifier 4-6%, Span-60 2- 3%, glycerol 7.5 -12.5%, ethylparaben 0.1-1%, transdermal enhancer 1-5%, cream extract 0.3-5%, volatile oil 0.3-5%, and water; the cream extract and volatile oil are the cream extract and volatile oil in the extract of the Three Yellows and Two Fragrances Powder described in the foregoing technical solution.
The present disclosure further provides a method for prepar- ing the cream for preventing and treating UV damage described in the foregoing technical solution, comprising the following steps: mixing the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 with the volatile oil to obtain an oil phase; mixing the emulsifier, the glycerol, the ethylparaben, the cream extract, the transdermal enhancer with the water to obtain an water phase; pouring the water phase into the oil phase and emulsifying, to obtain the cream for preventing and treating UV damage.
The present disclosure provides an application of Three Yel- lows and Two Fragrances Powder in the preparation of drugs for preventing and treating UV damage. The three yellows and two Fra- grances powder is a mixture of frankincense, myrrh, rhubarb, coptis and phellodendron at a mass ratio of 1:1:2:2:2. The Three
Yellows and Two Fragrances Powder of the present disclosure is originated from the book “Detailed Analysis of Epidemic Warm Dis- eases « Upper-jiao” by Wu Tang in the Qing Dynasty, according to the book, frankincense and myrrh contained in Three Yellows and
Two Fragrances Powder have the effects of detumescence and promot- ing granulation, and invigorating blood circulation and alleviat- ing pain; rhubarb, coptis and phellodendron have the effects of eliminating dampness and detoxification; thus, it indicates that
Three Yellows and Two Fragrances Powder is suitable for the pre- vention and treatment of UV damage.
The present disclosure further provides an extract of Three
Yellows and Two Fragrances Powder. The preparation method of the extract of Three Yellows and Two Fragrances Powder not only re- tains the active ingredients and auxiliary ingredients of the
Three Yellows and Two Fragrances Powder to the greatest extent, but also reduces inactive ingredients; moreover, it can maximize the dissolution and penetration of the active ingredients of the drug, so that the Three Yellows and Two Fragrances Powder has a better therapeutic effect; in addition, the obtained extract of
Three Yellows and Two Fragrances Powder can be used to prepare other novel topical Chinese medicine preparations with stable and reliable quality, thus promoting the secondary development and utilization of ancient prescriptions.
The present disclosure further provides a cream for prevent- ing and treating UV damage, comprising the following components in percentage by weight: stearic acid 4.5-6%, glyceryl monostearate 2.5-5.5%, liquid paraffin 7.5-12.5%, vaseline 2.5-7.0%, emulsifier 4-6%, Span-60 2-3%, glycerol 7.5-12.5%, ethylparaben 0. 1-1%, transdermal enhancer 1-5%, cream extract 0.3-5%, volatile oil 0.3- 5%, and water; the cream extract and volatile oil are the cream extract and volatile oil in the extract of the Three Yellows and
Two Fragrances Powder described in the foregoing technical solu- tion. The cream for preventing and treating UV damage of the pre- sent disclosure utilizes the cream extract that is extracted from the Three Yellows and Two Fragrances Powder (of which, the content of berberine hydrochloride in alcohol extract is up to 32.36 mg/g) and the volatile oil. Since the cream extract includes anthraqui- none compounds and alkaloid compounds, the anthraguinone compounds are mainly the active ingredients of rhubarb, mainly including emodin, rhein, chrysophanol, etc., which can resist UV damage through anti-oxidation, anti-inflammatory and other pharmacologi- cal mechanisms. Alkaloid compounds are mainly the active ingredi- ents of coptis and phellodendron, which can reduce the expression of inflammatory factors and MMP induced by UV rays, increase the expression of collagens, thus exerting the effect of resisting UV damage. The volatile oil mainly includes monoterpenes, sesquiter- penes, enols and esters, which can treat UV damage through anti- inflammatory and analgesic effects, increase the interactions be- tween skin keratin and lipids and promote the absorption of drugs.
BRIEF DESCRIPTION OF THE DRAWINGS
FIG.1 is a flow chart for the preparation of an extract of
Three Yellows and Two Fragrances Powder.
DETAILED DESCRIPTION OF THE EMBODIMENTS
The present disclosure provides an application of Three Yel- lows and Two Fragrances Powder in the preparation of drugs for preventing and treating UV damage, wherein the Three Yellows and
Two Fragrances Powder is a mixture of frankincense, myrrh, rhu- barb, coptis and phellodendron at a mass ratio of 1:1:2:2:2.
In the present disclosure, the Three Yellows and Two Fra- grances Powder is preferably used in the form of an extract of
Three Yellows and Two Fragrances Powder.
The Three Yellows and Two Fragrances Powder of the present disclosure is originated from the book “Detailed Analysis of Epi- demic Warm Diseases »« Upper-jiao” by Wu Tang in the Qing Dynasty, according to the book, frankincense and myrrh contained in Three
Yellows and Two Fragrances Powder have the effects of detumescence and promoting granulation, and invigorating blood circulation and alleviating pain; rhubarb, coptis and phellodendron have the ef- fects of eliminating dampness and detoxification; thus, it indi- cates that Three Yellows and Two Fragrances Powder is suitable for the prevention and treatment of UV damage.
The present disclosure further provides an extract of Three
Yellows and Two Fragrances Powder, the extract comprises a cream extract and a volatile oil; the cream extract comprises a water extract and an alcohol extract; the water extract, the alcohol ex- tract and the volatile oil are prepared by the following steps: mixing frankincense, myrrh and water, and sequentially per- forming leaching and steam distillation extraction to obtain the volatile oil, a water extracting solution and a residue; performing ethanol precipitation of the water extracting so-
lution to obtain the water extract; performing ethanol heating reflux extraction of the residue, rhubarb, coptis and phellodendron, to obtain the alcohol extract.
In the present disclosure, unless otherwise specified, the raw materials used herein are preferably commercially available products.
In the present disclosure, frankincense, myrrh and water are mixed, and leaching and steam distillation extraction are per- formed sequentially, to obtain the volatile oil, the water ex- tracting solution and the residue.
In the present disclosure, the frankincense is preferably used in the form of frankincense coarse powder. In the present disclosure, the myrrh is preferably used in the form of myrrh coarse powder. In the present disclosure, the water is preferably deionized water.
In the present disclosure, the ratio of the total mass of the frankincense and the myrrh to the volume of water is preferably lg: (6-10) mL, specifically preferably lg: 6 mL.
In the present disclosure, the time for the leaching is pref- erably 0.01-2 h, specifically preferably 1 h. In the present dis- closure, the leaching temperature is preferably a room tempera- ture, namely, neither additional heating nor additional cooling is required.
In the present disclosure, the time for the steam distilla- tion extraction time is preferably 3-10 h, further preferably 7 h.
In the present disclosure, a volatile oil and an extracting solution are collected directly in the process of the steam dis- tillation extraction. In the present disclosure, the yield of the volatile oil reaches 1.3%. In the present disclosure, the volatile oil mainly includes monoterpenes, sesquiterpenes, enols and es- ters, etc., which can treat UV damage through anti-inflammatory and analgesic effects, increase the interactions between skin ker- atin and lipids and promote the absorption of drugs. In the pre- sent disclosure, the extracting solution is subjected to solid- liquid separation to obtain a water extracting solution and a res- idue. In the present disclosure, the solid-liquid separation meth- od is preferably filtration.
After obtaining the water extracting solution, ethanol pre- cipitation of the water extracting solution is performed in the present disclosure, to obtain the water extract.
In the present disclosure, the water extracting solution is preferably concentrated before ethanol precipitation to obtain a concentrated solution, and subsequent ethanol precipitation of the concentrated solution is performed. In the present disclosure, the operation for concentration is not specifically limited, as long as the specific gravity of the concentrated solution is 1.1 to 1.2.
In the present disclosure, the reagent for the ethanol pre- cipitation is preferably ethanol; the volume content of ethanol in the ethanol precipitation system is preferably 60-70%. In the pre- sent disclosure, the time for the ethanol precipitation is prefer- ably 24 h.
After the ethanol precipitation, the present disclosure pref- erably further includes filtering the obtained water precipitation solution to obtain the water extract. In the present disclosure, the operation for filtration is not specifically limited as long as solid-liquid separation can be achieved. In the present disclo- sure, the mode of concentration is preferably concentration under reduced pressure; and the temperature of the concentration under reduced pressure is preferably 40-55°C. In the present disclosure, the pressure and time of the concentration under reduced pressure are not specifically limited as long as the solvent in the fil- trate can be basically removed. In the present disclosure, the drying preferably includes evaporative drying or freeze drying. In the present disclosure, the temperature of the evaporative drying is preferably 80-85°C. In the present disclosure, the time of the evaporative drying is not specifically limited as long as it can be dried to a constant weight. In the present disclosure, the tem- perature of the freeze-drying is preferably -40 to -50°C. In the present disclosure, the time of the freeze-drying is not specifi- cally limited as long as it can be dried to a constant weight.
In the present disclosure, after a residue is obtained, etha- nol heating reflux extraction of the residue, rhubarb, coptis and phellodendron is performed to obtain the alcohol extract.
In the present disclosure, the rhubarb, coptis and phelloden- dron are preferably APIs that have not been crushed and processed.
In the present disclosure, the reagent for the ethanol heat- ing reflux extraction is preferably an ethanol solution; the vol- ume concentration of the ethanol solution is preferably 60-80%, specifically preferably 60%; the ratio of the total mass of the residue, rhubarb, coptis and phellodendron to the volume of the ethanol solution is 1 g: (8-12) mL, specifically preferably 1 g :12 mL.
In the present disclosure, preferably, the ethanol heating reflux extraction is performed for 1 to 3 times, specifically preferably 3 times; and the time for each ethanol heating reflux extraction is preferably 1-3 h, more preferably 2 h.
In the present disclosure, alcohol extracting solution is collected directly through the ethanol heating reflux extraction, and the alcohol extracting solution is filtered, then the obtained filtrate is sequentially concentrated and dried to obtain the al- cohol extract. In the present disclosure, the mode of filtration is not specifically limited as long as solid-liquid separation can be achieved. In the present disclosure, the concentration is pref- erably concentration under reduced pressure; the temperature of the concentration under reduced pressure is preferably 40-55°C. In the present disclosure, the pressure and time of the concentration under reduced pressure are not specifically limited as long as the solvent in the filtrate can be basically removed. In the present disclosure, the drying preferably includes evaporative drying or freeze drying. In the present disclosure, the temperature of the evaporative drying is preferably 80-85°C. In the present disclo- sure, the time of the evaporative drying is not specifically lim- ited as long as it can be dried to a constant weight. In the pre- sent disclosure, the temperature of the freeze-drying is prefera- bly -40 to -50°C. In the present disclosure, the time of the freeze-drying is not specifically limited as long as it can be dried to a constant weight.
In the present disclosure, the volatile oil, water extract and alcohol extract constitute the extract of the Three Yellows and Two Fragrances Powder; the mass ratio of the water extract to the alcohol extract in the extract of Three Yellows and Two Fra- grances Powder is preferably 1: (9-11); the water extract and the alcohol extract in the extract of Three Yellows and Two Fragrances
Powder constitute a cream extract. In the present disclosure, the content of berberine hydrochloride in the alcohol extract reaches 32.36 mg/g; at the same time, the extraction rate of the alcohol extract is 35%.
In the present disclosure, the cream extract includes anthra- quinone compounds and alkaloid compounds. The anthraguinone com- pounds are mainly the active ingredients of rhubarb, mainly in- cluding emodin, rhein, chrysophanol, etc., which can resist UV damage through anti-oxidation, anti-inflammatory and other pharma- cological mechanisms. Alkaloid compounds are mainly the active in- gredients of coptis and phellodendron, which can reduce the ex- pression of inflammatory factors and MMP induced by UV rays, in- crease the expression of collagens, thus exerting the effect of resisting UV damage.
FIG.1 shows a flow chart for the preparation of an extract of
Three Yellows and Two Fragrances Powder. Steam distillation ex- traction of frankincense and myrrh is performed to obtain a vola- tile oil, a water extracting solution and a residue; and ethanol precipitation of the water extracting solution is performed to ob- tain a water precipitation solution, and then the water precipita- tion solution is filtered and concentrated, to obtain a water ex- tract; ethanol heating reflux extraction of the residue, rhubarb, coptis and phellodendron is performed, to obtain an alcohol ex- tracting solution, and the alcohol extracting solution is filtered and concentrated, to obtain an alcohol extract.
The present disclosure provides a cream for preventing and treating UV damage, including the following components in percent- age by weight: stearic acid 4.5-6%, glyceryl monostearate 2.5-5.5%, liquid paraffin 7.5-12.5%, vaseline 2.5-7.0%, emulsifier 4-6%, Span-60 2- 3%, glycerol 7.5 -12.5%, ethylparaben 0.1-1%, transdermal enhancer 1-5%, cream extract 0.3-5%, volatile oil 0.3-5%, and water; the cream extract and volatile oil are the cream extract and volatile oil in the extract of the Three Yellows and Two Fragrances Powder described in the foregoing technical solution. In the present dis- closure, the cream extract is a mixture of water extract and alco- hol extract; the mass ratio of the water extract and the alcohol extract in the cream extract is 1: (9-11).
The cream for preventing and treating UV damage provided by the present disclosure includes 4.5-6% of stealic acid by weight, preferably 4.7-5.2% by weight. In the present disclosure, the stearic acid can increase the lubricity of the cream, adjust the consistency of the cream, and make the drug to be uniformly dis- persed.
The cream for preventing and treating UV damage provided by the present disclosure includes 2.5-5.5% of glyceryl monostearate by weight, preferably 3.4-5.0% by weight, and more preferably 4.0- 4.5% by weight. In the present disclosure, the glyceryl monos- tearate can increase the water absorption capacity of the oil phase while stabilizing the base, and in addition, it can adjust the consistency of the cream to make the cream base to be delicate and bright.
The cream for preventing and treating UV damage provided by the present disclosure includes 7.5-12.5% of liquid paraffin by weight, preferably 8.0-12.0% by weight, and more preferably 9.0- 10.5% by weight. In the present disclosure, the liquid paraffin can adjust the consistency and spreadability of the cream.
The cream for preventing and treating UV damage provided by the present disclosure includes 2.5-7.0% of vaseline by weight, preferably 3.0-6.0% by weight, and more preferably 3.5-5.0% by weight. In the present disclosure, the vaseline can prevent the base moisture from evaporating and facilitate the hydration of the stratum corneum; in addition, vaseline has a suitable viscosity and ductility, so the cream is easy to apply.
The cream for preventing and treating UV damage provided by the present disclosure includes 4-6% of emulsifier by weight, preferably 4.2-5.8% by weight. In the present disclosure, the emulsifier preferably includes Tween-80 and/or triethanolamine, and more preferably Tween-80. In the present disclosure, the emul- sifier can cause the oil phase and the water phase in the base to undergo an emulsification reaction to promote the formation of a cream.
The cream for preventing and treating UV damage provided by the present disclosure includes 2-3% of Span-60 by weight, more preferably 2.1-2.9% by weight. In the present disclosure, the
Span-60 can be used as an auxiliary emulsifier to promote occur- rence of the emulsification reaction.
The cream for preventing and treating UV damage provided by the present disclosure includes 7.5-12.5% of glycerol by weight, preferably 7.7-12.1% by weight, and more preferably 8-12% by weight, and still more preferably 9-11% by weight. In the present disclosure, the glycerol can be used as a humectant to prevent the cream from hardening due to the loss of water; in addition, glyc- erol has a certain lubricating and protective effect on the skin and mucous membranes.
The cream for preventing and treating UV damage provided by the present disclosure includes 0.1-1% of ethylparaben by weight, preferably 0.2-0.93 by weight, more preferably 0.3-0.8% by weight, still more preferably 0.4-0.7% by weight. In the present disclo- sure, the ethylparaben is a main preservative, which can prevent the deterioration and corruption of cream caused by microbial con- tamination such as bacteria and molds, etc.
The cream for preventing and treating UV damage provided by the present disclosure includes 1-5% of transdermal enhancer by weight, preferably 2-4% by weight. In the present disclosure, the transdermal enhancer preferably includes one or more of azone, menthol, and propylene glycol, more preferably 2% azone, 2% men- thol, 2% propylene glycolazone, 2% azone-2% propylene glycol mix- ture or 2%menthol-2%propylene glycol mixture, still more prefera- bly 2%propylene glycol. In the present disclosure, the transdermal enhancer can make the skin stratum corneum interact with lipids, reduce the phase transition temperature of the effective substance to the lipids in the stratum corneum gap, reduce the diffusion re- sistance of the drug in the stratum corneum, and promote the drug absorption.
The cream for preventing and treating UV damage provided by the present disclosure includes 0.3-5% of cream extract by weight, preferably 0.5-4.5% by weight, more preferably 1.0-4.0% by weight,
still more preferably 2.0-3.0% by weight. In the present disclo- sure, the cream extract includes anthraquinone compounds and alka- loid compounds, the anthragquinone compounds are mainly the active ingredients of rhubarb, mainly including emodin, rhein, chrysopha- nel, etc., which can resist UV damage through anti-oxidation, an- ti-inflammatory and other pharmacological mechanisms. Alkaloid compounds are mainly the active ingredients of coptis and phel- lodendron, which can reduce the expression of inflammatory factors and MMP induced by UV rays, increase the expression of collagens, thus exerting the effect of resisting UV damage.
The cream for preventing and treating UV damage provided by the present disclosure includes 0.3-5% of volatile oil by weight, preferably 0.5-4.5% by weight, more preferably 1.0-4.0% by weight, still more preferably 2.0-3.0% by weight. In the present disclo- sure, the volatile oil mainly includes monoterpenes, sesquiter- penes, enols and esters, which can treat UV damage through anti- inflammatory and analgesic effects, increase the interactions be- tween skin keratin and lipids and promote the absorption of drugs.
The cream for preventing and treating UV damage provided by the present disclosure includes water; the water is preferably de- ionized water.
The present disclosure further provides a method for prepar- ing a cream for preventing and treating UV damage described in the foregoing technical solution, comprising the following steps: mixing the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 with the volatile oil to obtain an oil phase; mixing the emulsifier, the glycerol, the ethylparaben, the cream extract, the transdermal enhancer with the water to obtain an water phase; pouring the water phase into the oil phase and emulsifying, to obtain the cream for preventing and treating UV damage.
In the present disclosure, the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 are mixed with the volatile oil to obtain an oil phase.
In the present disclosure, the mixing is preferably carried out under the conditions of a water bath and stirring, and the temperature of the water bath is preferably 80°C; in the present disclosure, the stirring speed is not specifically limited; in the present disclosure, the time of mixing is not specifically limited as long as the raw materials can be sufficiently mixed.
In the present disclosure, the emulsifier, the glycerol, the ethylparaben, the cream extract, the transdermal enhancer are mixed with the water to obtain an water phase.
In the present disclosure, the mixing is preferably carried out under the conditions of a water bath and stirring, and the temperature of the water bath is preferably 80°C; in the present disclosure, the stirring speed is not specifically limited; in the present disclosure, the time of mixing is not specifically limited as long as the raw materials can be sufficiently mixed.
In the present disclosure, when the transdermal enhancer is added to the water phase, the transdermal enhancer is preferably propylene glycol; when the transdermal enhancer is preferably azone and/or menthol, the transdermal enhancer is preferably added to the oil phase.
In the present disclosure, after obtaining the water phase and the oil phase, the water phase is added to the oil phase for emulsification to obtain the cream for preventing and treating UV damage.
In the present disclosure, the water phase is preferably add- ed to the oil phase within 1-5 s.
In the present disclosure, the emulsification is preferably carried out in a homogenizer, and the speed of the homogenizer is preferably 2500-3000 r/min, more preferably 2700-2800 r/min; the time for the emulsification is preferably 20-120 s, more prefera- bly 60 s.
After the emulsification, the present disclosure preferably further includes taking out the obtained emulsification system and continuing to stir in a magnetic stirrer until a rotor stops, and finally stirring to room temperature with a glass rod, to obtain the cream for preventing and treating UV damage.
The application of the Three Yellows and Two Fragrances Pow- der provided in the present disclosure, the extract of the Three
Yellows and Two Fragrances Powder and the cream for preventing and treating UV damage will be described in detail below in conjunc- tion with embodiments, but the description cannot be understood as limiting the scope of protection of the present disclosure.
Example 1
A cream for preventing and treating UV damage comprised the following components in percentage by weight: stearic acid 5%, glyceryl monostearate 5.5%, liquid paraffin 8.5%, vaseline 6%, tween-80 4.0%, Span-60 2.0%, glycerol 12%, ethylparaben 0. 1%, propylene glycol 2%, cream extract 1%, volatile oil 1%, and water added to 100%.
The above raw materials were weighed according to the above percentages by weight, and the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 were mixed with the volatile oil evenly in a water bath at 80°C to obtain an oil phase; the tween-80, the glycerol, the ethylparaben, the cream extract, the propylene glycol were mixed with the water evenly in a water bath at 80°C to obtain a water phase; the water phase was added to the oil phase, and emulsified in a homogenizer at 2800 r/min for 60 s, then taken out, stirred in a magnetic stirrer un- til the rotor was stopped, and finally stirred to room temperature with a glass rod, to obtain a cream for preventing and treating UV damage.
A method for preparing an extract of the Three Yellows and
Two Fragrances Powder comprised the following steps: weighing the five medicinal materials (frankincense, myrrh, rhubarb, coptis, and phellodendron) at a mass ratio of 1:1:2:2:2, crushing the frankincense and the myrrh to obtain coarse powdered frankincense and myrrh; the rhubarb, the coptis and the phelloden- dron were APIs that were not crushed and processed.
Step 1: mixing the frankincense coarse powder, the myrrh coarse powder with water (the ratio of the total mass of frankin- cense coarse powder and myrrh coarse powder to the volume of water was 1 g: 6 mL), soaking for 1 h, heating and performing steam dis- tillation extraction for 7 h, to obtain a volatile oil and an ex- tracting solution; filtering the extracting solution to obtain a water extracting solution and a residue.
Step 2: concentrating the water extracting solution obtained in the step 1 to a specific gravity of 1.2, adding 95% ethanol precipitation (the volume concentration of ethanol in the ethanol precipitation system was 65%) equivalent to 2 times the volume of the obtained concentrated solution for 24 h, filtering; concen- trating the filtrate and recovering the ethanol, then drying in a water bath at 80°C to a constant weight to obtain the water ex- tract.
Step 3: mixing the residue obtained in the step 1 with rhu- barb, coptis and phellodendron, and adding an ethanol solution with a volume concentration of 60% (the ratio of the total mass of residue, rhubarb, coptis and phellodendron to the volume of the ethanol solution was 1g:12 mL), performing ethanol heating reflux extraction for 3 times, 2 h each time, filtering, and taking the filtrate and concentrating to recover ethanol, and then drying in a water bath at 80°C to a constant weight to obtain the alcohol extract;
Mixing the water extract obtained in the step 2 and the alco- hol extract obtained in the step 3 as a cream extract.
Example 2
A cream for preventing and treating UV damage comprised the following components in percentage by weight: stearic acid 4.5%, glyceryl monostearate 4.8%, liquid paraffin 12.5%, vaseline 2.5%, tween-80 4%, Span-60 2%, glycerol 10.9%, ethylparaben 0. 1%, pro- pylene glycol 2%, cream extract 1%, volatile oil 1%, and water added to 100%.
The above raw materials were weighed according to the above percentages by weight, and the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 were mixed with the volatile oil evenly in a water bath at 80°C to obtain an oil phase; the tween-80, the glycerol, the water, the ethylpara- ben, the propylene glycol and the cream extract were mixed evenly in a water bath at 80°C to obtain a water phase; the water phase was added to the oil phase, and emulsified in a homogenizer at 2800 r/min for 60 s, then taken out, stirred in a magnetic stirrer until the rotor was stopped, and finally stirred to room tempera- ture with a glass rod, to obtain a cream for preventing and treat- ing UV damage.
The method of obtaining the cream extract and the volatile oil in this example was the same as that in Example 1.
Example 3
A cream for preventing and treating UV damage comprised the following components in percentage by weight: stearic acid 4.5%, glyceryl monostearate 4.8%, liquid paraffin 12.5%, vaseline 2.5%, tween-80 4%, Span-60 2%, glycerol 10.9%, ethylparaben 0. 1%, pro- pylene glycol 2%, cream extract 1%, volatile oil 1%, and water added to 100%.
The above raw materials were weighed according to the above percentages by weight, and the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 were mixed with the volatile oil evenly in a water bath at 80°C to obtain an oil phase; the tween-80, the glycerol, the water, the ethylpara- ben, the propylene glycol and the cream extract were mixed evenly in a water bath at 80°C to obtain a water phase; the water phase was added to the oil phase, and emulsified in a homogenizer at 2800 r/min for 60 s, then taken out, stirred in a magnetic stirrer until the rotor was stopped, and finally stirred to room tempera- ture with a glass rod, to obtain a cream for preventing and treat- ing UV damage.
The method of obtaining the cream extract and the volatile oil in this example was the same as that in Example 1.
Example 4
A cream for preventing and treating UV damage comprised the following components in percentage by weight: stearic acid 4.55, glyceryl monostearate 5.5%, liquid paraffin 10. 1%, vaseline 4.7%, tween-80 5.8%, Span-60 2.9%, glycerol 7.7%, ethylparaben 0. 1%, propylene glycol 2%, cream extract 1%, volatile oil 1%, and water added to 100%.
The above raw materials were weighed according to the above percentages by weight, and the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 were mixed with the volatile oil evenly in a water bath at 80°C to obtain an oil phase; the tween-80, the glycerol, the water, the ethylpara- ben, the propylene glycol and the cream extract were mixed evenly in a water bath at 80°C to cbtain a water phase; the water phase was added to the oil phase, and emulsified in a homogenizer at 2800 r/min for 60 s, then taken out, stirred in a magnetic stirrer until the rotor was stopped, and finally stirred to room tempera- ture with a glass rod, to obtain a cream for preventing and treat- ing UV damage.
The method of obtaining the cream extract and the volatile oil in this example was the same as that in Example 1.
Example 5
A cream for preventing and treating UV damage comprised the following components in percentage by weight: stearic acid 6%, glyceryl monostearate 3.4%, liquid paraffin 7.5%, vaseline 3.3%, tween-80 6%, Span-60 3%, glycerol 12. 1%, ethylparaben 0. 1%, pro- pylene glycol 2%, cream extract 1%, volatile oil 1%, and water added to 100%.
The above raw materials were weighed according to the above percentages by weight, and the vaseline, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 were mixed with the volatile oil evenly in a water bath at 80°C to obtain an oil phase; the tween-80, the glycerol, the water, the ethylpara- ben, the propylene glycol and the cream extract were mixed evenly in a water bath at 80°C to obtain a water phase; the water phase was added to the oil phase, and emulsified in a homogenizer at 2800 r/min for 60 s, then taken out, stirred in a magnetic stirrer until the rotor was stopped, and finally stirred to room tempera- ture with a glass rod, to obtain a cream for preventing and treat- ing UV damage.
The method of obtaining the cream extract and the volatile oil in this example was the same as that in Example 1.
The above description is merely preferred embodiments of the present disclosure. It should be noted that for those of ordinary skill in the art, several improvements and modifications can be made without departing from the principle of the present disclo- sure, and these improvements and modifications shall also fall within the scope of protection of the present disclosure.

Claims (10)

CONCLUSIESCONCLUSIONS 1. Toepassing van Three Yellows and Two Fragrances-poeder bij de bereiding van geneesmiddelen voor het voorkomen en behandelen van UV-schade, waarbij het Three Yellows en Two Fragrances-poeder een mengsel is van wierook, mirre, rabarber, coptis en phellodendron in een massaverhouding van 1:1:2:2:2.1. Application of Three Yellows and Two Fragrances powder in the preparation of drugs for the prevention and treatment of UV damage, where the Three Yellows and Two Fragrances powder is a mixture of frankincense, myrrh, rhubarb, coptis and phellodendron in a mass ratio of 1:1:2:2:2. 2. Toepassing volgens conclusie 1, waarbij het Three Yellows and Two Fragrances-poeder wordt gebruikt in de vorm van een extract van Three Yellows en Two Fragrances-poeder.Use according to claim 1, wherein the Three Yellows and Two Fragrances powder is used in the form of an extract of Three Yellows and Two Fragrances powder. 3. Extract van Three Yellows and Two Fragrances-poeder, waarbij het extract een crème-extract en een vluchtige olie omvat; waarbij het crème-extract een waterextract en een alcoholextract omvat; waarbij het waterextract, het alccholextract en de vluchtige olie worden bereid door de volgende stappen: het mengen van wierook, mirre en water, en het achtereenvolgens uitvoeren van uitloging en stoomdestillatie-extractie om de vluch- tige olie, een waterextractie-oplossing en een residu te verkrij- gen; het uitvoeren van ethanolprecipitatie van de waterextractie- oplossing om het waterextract te verkrijgen; het uitvoeren van extractie met ethanol onder terugvloeikoeling van het residu, rabarber, coptis en phellodendron, om het alcohol- extract te verkrijgen.3. Extract of Three Yellows and Two Fragrances powder, wherein the extract comprises a cream extract and a volatile oil; wherein the cream extract comprises a water extract and an alcohol extract; wherein the water extract, the alcohol extract and the volatile oil are prepared by the following steps: mixing frankincense, myrrh and water, and performing leaching and steam distillation extraction sequentially to obtain the volatile oil, a water extraction solution and a residue to obtain; performing ethanol precipitation of the water extraction solution to obtain the water extract; performing extraction with ethanol under reflux of the residue, rhubarb, coptis and phellodendron, to obtain the alcohol extract. 4. Extract van Three Yellows and Two Fragrances-poeder volgens conclusie 3, waarbij de verhouding van de totale massa van wierook en mirre tot het volume water 1 g: (6-10) ml is.The extract of Three Yellows and Two Fragrances powder according to claim 3, wherein the ratio of the total mass of frankincense and myrrh to the volume of water is 1 g : (6-10) ml. 5. Extract van Three Yellows and Two Fragrances-poeder volgens conclusie 3 of 4, waarbij de uitloogtijd 0,01-2 uur is.The extract of Three Yellows and Two Fragrances powder according to claim 3 or 4, wherein the leaching time is 0.01-2 hours. 6. Extract van Three Yellows and Two Fragrances-poeder volgens conclusie 3 of 4, waarbij de tijd voor de extractietijd door stoomdestillatie 2-10 uur is.The extract of Three Yellows and Two Fragrances powder according to claim 3 or 4, wherein the time for the extraction time by steam distillation is 2-10 hours. 7. Extract van Three Yellows and Two Fragrances-poeder volgens conclusie 3, waarbij het reagens voor de extractie met ethanol on- der terugvloeikoeling een ethanoloplossing is; waarbij de volume- concentratie van de ethanoloplossing 60-80% is; de verhouding van de totale massa van het residu, rabarber, coptis en phellodendron tot het volume van de ethanoloplossing 1 g: (8-12) ml is.The extract of Three Yellows and Two Fragrances powder according to claim 3, wherein the reagent for the refluxing ethanol extraction is an ethanol solution; wherein the volume concentration of the ethanol solution is 60-80%; the ratio of the total mass of the residue, rhubarb, coptis and phellodendron to the volume of the ethanol solution is 1 g: (8-12) ml. 8. Extract van Three Yellows and Two Fragrances-poeder volgens conclusie 3 of 7, waarbij de extractie met ethanol onder terug- vloeikoeling 1-3 keer wordt uitgevoerd, en de tijd voor elke ex- tractie met ethanol onder terugvloeikoeling 1-3 uur is.The extract of Three Yellows and Two Fragrances powder according to claim 3 or 7, wherein the refluxing ethanol extraction is performed 1-3 times, and the time for each refluxing ethanol extraction is 1-3 hours . 9. Crème voor het voorkomen en behandelen van UV-schade, omvatten- de de volgende bestanddelen in gewichtspercentage: stearinezuur 4,5-6%, glycerylmonostearaat 2,5-5,5%, vloeibare pa- raffine 7,5-12,5%, vaseline 2,5-7,0%, emulgator 4-6%, Span-60 2- 3%, glycerol 7,5 -12,5%, ethylparabeen 0,1- 15, transdermale ver- sterker 1-5%, crème-extract 0,3-5%, vluchtige olie 0,3-5% en wa- ter; waarbij het crème-extract en de vluchtige olie het crème- extract en de vluchtige olie in het extract van het Three Yellows and Two Fragrances-poeder volgens een van de conclusies 3 tot 8 zijn.A cream for preventing and treating UV damage, comprising the following ingredients by weight: stearic acid 4.5-6%, glyceryl monostearate 2.5-5.5%, liquid paraffin 7.5-12, 5%, petroleum jelly 2.5-7.0%, emulsifier 4-6%, Span-60 2-3%, glycerol 7.5-12.5%, ethyl paraben 0.1-15, transdermal enhancer 1- 5%, cream extract 0.3-5%, volatile oil 0.3-5% and water; wherein the cream extract and the volatile oil are the cream extract and the volatile oil in the extract of the Three Yellows and Two Fragrances powder according to any one of claims 3 to 8. 10. Werkwijze voor het bereiden van de crème voor het voorkomen en behandelen van UV-schade volgens conclusie 9, die de volgende stappen omvat: het mengen van de vaseline, het stearinezuur, de vloeibare paraf- fine, het glycerylmonostearaat, de Span-60 met de vluchtige olie om een oliefase te verkrijgen; het mengen van de emulgator, de glycerol, de ethylparabeen, het crème-extract, de transdermale versterker met het water om een wa- terfase te verkrijgen; het gieten van de waterfase in de oliefase en emulgeren, om de crème voor het voorkomen en behandelen van UV-schade te verkrij-The method for preparing the cream for preventing and treating UV damage according to claim 9, comprising the steps of: mixing the petroleum jelly, the stearic acid, the liquid paraffin, the glyceryl monostearate, the Span-60 with the volatile oil to obtain an oil phase; mixing the emulsifier, the glycerol, the ethyl paraben, the cream extract, the transdermal enhancer with the water to obtain a water phase; pouring the water phase into the oil phase and emulsifying to obtain the cream for preventing and treating UV damage gen.gene.
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