CN108814995A - A kind of non-aqueous multiple self-emulsifying systems of rutin and its preparation method and application - Google Patents
A kind of non-aqueous multiple self-emulsifying systems of rutin and its preparation method and application Download PDFInfo
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- CN108814995A CN108814995A CN201810685669.7A CN201810685669A CN108814995A CN 108814995 A CN108814995 A CN 108814995A CN 201810685669 A CN201810685669 A CN 201810685669A CN 108814995 A CN108814995 A CN 108814995A
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
- A61K8/04—Dispersions; Emulsions
- A61K8/06—Emulsions
- A61K8/066—Multiple emulsions, e.g. water-in-oil-in-water
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
- A61K8/25—Silicon; Compounds thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/342—Alcohols having more than seven atoms in an unbroken chain
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
- A61K8/34—Alcohols
- A61K8/345—Alcohols containing more than one hydroxy group
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
- A61K8/922—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof of vegetable origin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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Abstract
A kind of non-aqueous multiple self-emulsifying systems of rutin and its preparation method and application, the system load have rutin active constituent, by its mass fraction, are made of following raw materials according：0.8 ~ 2.0 part of rutin；20 ~ 40 parts of glycerol；45.5 ~ 73.4 parts of vegetable oil；4 ~ 8 parts of cetostearyl alcohol；0.8 ~ 1.2 part of hydrophobic silica；1 ~ 3 part of hydrophobic surfactant；4 ~ 6 parts of hydrophilic surfactant active.The non-aqueous multiple self-emulsifying systems of rutin of the invention are with good stability；The dissolubility for improving the awkward property ingredient Rutin of grease, to improve its bioavilability；Each component has very high safety in formula, nonirritant to body, non-toxic, can be used as intermediate-type and is used in compounding with cosmetic formulations, compatibility is good, can be widely used for cosmetic field；The preparation method is simply controllable, reproducible.
Description
Technical field
The invention belongs to the carrier system technical field in cosmetics technology of preparing, it is related to a kind of the non-aqueous more of package rutin
Weight self-emulsifying systems and its preparation method and application.
Background technique
Rutin（Rutin）Also known as citrin, rutin sophorin etc., chemical name are Luteolin -3-
Rutin sophorin, No. CAS：153-18-4, molecular formula C27H30O16, and molecular weight is 610.52, is widely present in plant
Flavonols carbohydrate ligands, character are the crystallization of yellow powder sample.
Ultraviolet light is divided into three sections：The area A（320 ~ 400 nm）Can go directly corium and have irreversible cumulative bad, B
Area（290 ~ 320 nm）Lead to the root of skin sunburn, the area C（200 ~ 280 nm）Also known as sterilizing area does not produce human skin
Raw harm.Rutin has very strong removing free radical, oxidation resistant function.Rutin is in 200 ~ 240 nm and 330 ~ 380 nm
Range of wavelengths have very strong absorbability, can effectively absorb the area A ultraviolet light, the suncream containing rutin can also effectively be inhaled simultaneously
The area B and the area A ultraviolet light are received, the effect of the integrated protections such as anti-, anti-oxidant, anti-inflammatory can be played.In addition, as natural sun-screening agents, rutin
It can be used to do Red blood streak dispelling frost.The active oxygen radical that the obvious scavenger-cell of rutin energy generates is added in cosmetics, to make skin
Skin is moist, fine and smooth, crease-resistant.
Rutin is both insoluble in water, is also insoluble in most greases, belongs to two refractory components of grease, two indissoluble characteristic of grease
Cause its skin bioavilability very low, also greatly limit its application for absorbing field in cosmetics, this patent aims to solve the problem that
Problem of the above rutin in cosmetic applications field.
Under normal conditions, the lotion being widely studied and applied at present, either oil-in-water（O/W）Lotion, or oil
Bao Shui（W/O）Lotion, a phase therein contain water, i.e. aqueous emulsion.However, two kinds of liquid immiscible in lotion can also
Not include water, i.e. nonaqueous emulsion under specific condition, also referred to as oil packet is oily（O/O）Lotion is directed to degradable in water
Ingredient or two refractory components of grease all have good advantage.Meanwhile it being directed to load water soluble active constituent in recent years
Multiple self-emulsifying systems（Self-double-emulsifying drug delivery system, SDEDDS）It is got over
Carry out more concerns.Traditional SDEDDS generally refers to Aquo System, and is mainly used for the load of water soluble ingredient, reports at present
The preparation process about SDEDDS mostly use the two-step method of improvement to prepare, unlike multiple emulsion preparation process, if
Hydrophilic emulsifier is added directly into W/O colostrum in the second step process, rather than is pre-dispersed in outer aqueous phase, it is special
Sign shows as the homogeneous mixture that the system original state is W/O lotion and hydrophilic emulsifier, in an aqueous medium through external light
After micro- stirring can self-emulsifying formed W/O/W multiple emulsion, wherein water soluble ingredient is mainly distributed（Or dissolution）In inner aqueous phase.So
And on the basis ofs nonaqueous emulsion and tradition SDEDDS etc., by the inner aqueous phase organic solvent of traditional SDEDDS（Such as glycerol, propylene glycol
Deng）Instead of rear, it can design and non-aqueous multiple self-emulsifying systems are prepared（Non-aqueous SDEDDS）, which is oil packet oil
（O/O）The homogeneous mixture of lotion and hydrophilic emulsifier, wherein two refractory components of grease may be dissolved in interior oily phase.The body
In an aqueous medium, stable O/O/W multiple emulsion can be spontaneously formed by giving lower energy, can significantly improve grease two for system
The dissolubility of refractory components improves the load capacity and bioavailability of two refractory components of grease, enhances the anti-oxidant of skin
Ability and protective effect.The some disadvantages of rutin in application process can be improved by non-aqueous multiple self-emulsifying systems, to make
It preferably moves towards commercialization process.
This patent carries out package processing to rutin using non-aqueous multiple self-emulsifying systems, can be good at solving above retouched
The rutin stated is applying upper problem, and the present invention comes therefrom.
Summary of the invention
The technical issues of solution：The present invention provides non-aqueous multiple self-emulsifying systems and its preparation of a kind of rutin high load amount
Methods and applications produce a kind of rutin applied in skin sparing cosmetics, solve the grease in cosmetics in the prior art
In place of the dissolubility of soluble bioactive compound, the load capacity of facing a difficult choice and the shortcoming and defect such as skin bioavilability is low.
Technical solution：A kind of non-aqueous multiple self-emulsifying systems of rutin, the system load has rutin active constituent, by its matter
Number is measured, is made of following raw materials according：0.8 ~ 2.0 part of rutin；20 ~ 40 parts of glycerol；45.5 ~ 73.4 parts of vegetable oil；Ten
Six 4 ~ 8 parts of octadecyl alcolols；0.8 ~ 1.2 part of hydrophobic silica；1 ~ 3 part of hydrophobic surfactant；Hydrophily table
4 ~ 6 parts of face activating agent.
Above-mentioned vegetable oil is selected as camellia seed oil, evening primrose oil, olive oil, corn oil, peanut oil, at least one in soybean oil
Kind.
Above-mentioned hydrophobic silica be WACKER HDKH20, WACKER HDKH30, EVONIK AerosilR106,
Any one in EVONIK AerosilR972, Cabot TS-610.
Above-mentioned hydrophobic surfactant is span 40, sorbester p18, sorbester p17, polyglycerol polyricinoleate, the poly- second of cetyl
Any one in -10/1 dimethyl siloxane of glycol/polypropylene glycol, -30 dimerization hydroxy stearic acid ester of polyethylene glycol.
Above-mentioned hydrophilic surfactant active is polysorbas20, polysorbate40, polysorbate60, Tween 80, ten polyglycereol monolaurates
In any one.
The preparation method of the above-mentioned non-aqueous multiple self-emulsifying systems of rutin, includes the following steps：（1）Rutin and glycerol are mixed
It is stirred afterwards to solution to become at room temperature and be clarified, as interior oily phase；（2）By hydrophobic silica be added into vegetable oil and in
30 ~ 50 min of high-speed stirred under 3000 ~ 5000 rpm micro- thick liquid of pellucidity is presented to dispersion, by this
Micro- thick liquid is ultrasonically treated 5 ~ 10 min resulting dispersion systems；（3）Hydrophobic surfactant and cetostearyl alcohol are added
To step（2）In dispersions obtained system, and it is thoroughly mixed to form homogeneous phase in 65 DEG C ~ 70 DEG C waters bath with thermostatic control, obtains outer oily phase；
（4）Interior oily phase is added dropwise in outside oil phase under the stirring of 800 ~ 1500 rpm, continuing 10 ~ 20 min of stirring fills it
Divide emulsification, obtains oil packet oil（O/O）Colostrum；（5）Hydrophilic surfactant active is directly added to step（4）Gained oil packet oil is just
In cream, 10 ~ 15 min are stirred at low speed in 200 ~ 300 rpm at 48 DEG C ~ 52 DEG C.
The above-mentioned non-aqueous multiple self-emulsifying systems of rutin are preparing the application in skin protection cosmetics.
Beneficial effect：（1）The non-aqueous multiple self-emulsifying systems of rutin of the invention are with good stability；（2）It improves
The dissolubility of the awkward property ingredient Rutin of grease, to improve its bioavilability；（3）Each component has very high safety in formula
Property, nonirritant to body, non-toxic, can be used as intermediate-type is used in compounding with cosmetic formulations, and compatibility is good, can be extensive
For cosmetic field；（4）The preparation method is simply controllable, reproducible.
Detailed description of the invention
Fig. 1 is the preparation method flow chart of the non-aqueous multiple self-emulsifying systems of rutin of the present invention.
Specific embodiment
The invention will be further described with reference to embodiments.These embodiments are not limited to for illustrating the present invention
It limits the scope of the invention.Implementation condition used in the examples can do further adjustment according to the condition of specific producer.
Embodiment 1
It weighs 1.6 g rutins to be added into 40.0 g glycerol, until magnetic agitation to solution becomes clarification at room temperature, as interior oil
Phase；It weighs 1.0 g WACKER HDKH20 to be added in the mixture of 20.4 g evening primrose oil and 30.0 g olive oil, in 3000
Micro- thick liquid of pellucidity is presented to dispersion by 30 min of high-speed stirred under rpm, which is ultrasonically treated
1.0 g polyglycerol polyricinoleates, 6.0 g cetostearyl alcohols are then added into above-mentioned dispersion in 5 min resulting dispersion systems,
It is thoroughly mixed to form homogeneous phase in 65 DEG C of waters bath with thermostatic control, outer oily phase is obtained, then to above-mentioned 58.4 under the stirring of 1000 rpm
Oil-phase solution in 41.6 g is added dropwise in the outer oily phase of g, continuing 15 min of stirring keeps its fully emulsified, obtains oil and wraps oily colostrum；
5.0 g polysorbas20s are added in colostrum, it is non-aqueous up to rutin high load amount in 250 rpm to stir at low speed 12 min at 50 DEG C
Multiple self-emulsifying systems.The non-aqueous multiple self-emulsifying systems of 1.0 g rutins are added in 100 g deionized waters, after evenly dispersed,
Average grain diameter is 17.5 ± 3.5 μm after obtaining the non-aqueous multiple self-emulsifying systems water dispersion of rutin using laser light scattering instrument, and 25 DEG C
Its average grain diameter is 19.3 ± 3.5 μm after being placed at room temperature for 1 month, and change of size no significant difference shows that its stability is good
It is good.
Embodiment 2
It weighs 1.6 g rutins to be added into 35.0 g glycerol, until magnetic agitation to solution becomes clarification at room temperature, as interior oil
Phase；It weighs 1.0 g EVONIK AerosilR106 and 0.2 g WACKER HDKH30 is added in 54.4 g corn oils, in
Micro- thick liquid of pellucidity is presented to dispersion, which is surpassed by 30 min of high-speed stirred under 3500 rpm
1.8 g sorbester p17s, 6.0 g cetostearyl alcohols are then added into above-mentioned dispersion in 5 min resulting dispersion system of sonication,
It is thoroughly mixed to form homogeneous phase in 65 DEG C of waters bath with thermostatic control, outer oily phase is obtained, then to above-mentioned 63.4 g under the stirring of 1000 rpm
Oil-phase solution in 36.6 g is added dropwise in outer oil phase, continuing 15 min of stirring keeps its fully emulsified, obtains oil and wraps oily colostrum；It will
6.0 g Tween 80s are added in colostrum, and it is non-aqueous more up to rutin high load amount in 250 rpm to stir at low speed 12 min at 50 DEG C
Weight self-emulsifying systems.The non-aqueous multiple self-emulsifying systems of 1.0 g rutins are added in 100 g deionized waters, after evenly dispersed, benefit
Average grain diameter is 12.3 ± 2.8 μm after obtaining the non-aqueous multiple self-emulsifying systems water dispersion of rutin with laser light scattering instrument, and 25 DEG C of rooms
Its average grain diameter is 14.5 ± 3.0 μm after temperature is placed 1 month, and change of size no significant difference shows that its stability is good
It is good.
Embodiment 3
It weighs 2.0 g rutins to be added into 40.0 g glycerol, until magnetic agitation to solution becomes clarification at room temperature, as interior oil
Phase；It weighs 1.0 g Cabot TS-610 and 0.4 g WACKER HDKH20 is added in 49.6 g evening primrose oil, in 3500
Micro- thick liquid of pellucidity is presented to dispersion by 30 min of high-speed stirred under rpm, which is ultrasonically treated
It is poly- that -10/1 dimethyl siloxane of 1.0 g cetyl polyethylene/polypropylene glycol, 0.5 g is then added in 5 min resulting dispersion systems
Glycerol polyricinoleate, 6.0 g cetostearyl alcohols are thoroughly mixed to form uniform into above-mentioned dispersion in 65 DEG C of waters bath with thermostatic control
Phase obtains outer oily phase, oil in 42.0 g then is added dropwise in oily phase to outside above-mentioned 58.0 g under the stirring of 1000 rpm and mixes
Liquid, continuing 15 min of stirring keeps its fully emulsified, obtains oil and wraps oily colostrum；6.0 g polysorbas20s are added in colostrum, at 50 DEG C
Under in 250 rpm stir at low speed 12 min up to the non-aqueous multiple self-emulsifying systems of rutin high load amount.1.0 g rutins are non-aqueous more
Weight self-emulsifying systems are added in 100 g deionized waters, and after evenly dispersed, it is non-aqueous multiple from cream to obtain rutin using laser light scattering instrument
After change system water dispersion average grain diameter be 15.6 ± 3.2 μm, and 25 DEG C be placed at room temperature for 1 month after its average grain diameter be 17.0
± 3.7 μm, change of size no significant difference shows that it has good stability.
The foregoing examples are merely illustrative of the technical concept and features of the invention, its object is to allow professional and technical personnel in the field can
Understand the contents of the present invention and implement accordingly, it is not intended to limit the scope of the present invention.All spirit according to the present invention is real
The changes, modifications, substitutions, combinations, simplifications that matter is done should be equivalent substitute mode, be included in protection model of the invention
Within enclosing.
Claims (7)
1. a kind of non-aqueous multiple self-emulsifying systems of rutin, the system load has rutin active constituent, it is characterised in that presses its matter
Number is measured, is made of following raw materials according：0.8 ~ 2.0 part of rutin；20 ~ 40 parts of glycerol；45.5 ~ 73.4 parts of vegetable oil；Ten
Six 4 ~ 8 parts of octadecyl alcolols；0.8 ~ 1.2 part of hydrophobic silica；1 ~ 3 part of hydrophobic surfactant；Hydrophily table
4 ~ 6 parts of face activating agent.
2. the non-aqueous multiple self-emulsifying systems of rutin according to claim 1, it is characterised in that the vegetable oil is selected as tea seed
At least one of oil, evening primrose oil, olive oil, corn oil, peanut oil, soybean oil.
3. the non-aqueous multiple self-emulsifying systems of rutin according to claim 1, it is characterised in that the hydrophobic silica is
WACKER HDKH20、WACKER HDKH30、EVONIK AerosilR106、EVONIK AerosilR972、Cabot TS-
Any one in 610.
4. the non-aqueous multiple self-emulsifying systems of rutin according to claim 1, it is characterised in that the hydrophobic surfactant
For span 40, sorbester p18, sorbester p17, polyglycerol polyricinoleate, -10/1 dimethyl silica of cetyl polyethylene/polypropylene glycol
Any one in alkane, -30 dimerization hydroxy stearic acid ester of polyethylene glycol.
5. the non-aqueous multiple self-emulsifying systems of rutin according to claim 1, it is characterised in that the hydrophilic surfactant active
For any one in polysorbas20, polysorbate40, polysorbate60, Tween 80, ten polyglycereol monolaurates.
6. the preparation method of any non-aqueous multiple self-emulsifying systems of rutin of claim 1 ~ 5, it is characterised in that including following
Step：
（1）It is stirred at room temperature to solution to become after rutin and glycerol are mixed and be clarified, as interior oily phase；
（2）Hydrophobic silica is added into vegetable oil and the high-speed stirred 30 ~ 50 under 3000 ~ 5000 rpm
Micro- thick liquid of pellucidity is presented to dispersion by min, which, which is ultrasonically treated 5 ~ 10 min, to disperse
System；
（3）Hydrophobic surfactant and cetostearyl alcohol are added to step（2）In dispersions obtained system, and 65 DEG C ~
It is thoroughly mixed to form homogeneous phase in 70 DEG C of waters bath with thermostatic control, obtains outer oily phase；
（4）Interior oily phase is added dropwise in outside oil phase under the stirring of 800 ~ 1500 rpm, continuing 10 ~ 20 min of stirring makes
Its is fully emulsified, obtains oil packet oil（O/O）Colostrum；
（5）Hydrophilic surfactant active is directly added to step（4）In gained oil packet oil colostrum, at 48 DEG C ~ 52 DEG C in
200 ~ 300 rpm stir at low speed 10 ~ 15 min.
7. any one of the claim 1 ~ 5 non-aqueous multiple self-emulsifying systems of rutin are preparing the application in skin protection cosmetics.
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109924491A (en) * | 2019-04-01 | 2019-06-25 | 东南大学 | A kind of dihydromyricetin solid-state self-emulsifying material and its preparation method and application |
| CN113546009A (en) * | 2021-07-30 | 2021-10-26 | 上海应用技术大学 | Water-in-oil type rutin microemulsion and preparation method thereof |
| CN114452227A (en) * | 2022-01-20 | 2022-05-10 | 江南大学 | Method for preparing alcohol-in-water-in-oil-in-water multiple pickering emulsion by anti-solvent recrystallization method |
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| CN102697672A (en) * | 2012-06-05 | 2012-10-03 | 东南大学 | Multiple emulsion of arbutin and preparation method thereof |
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2018
- 2018-06-28 CN CN201810685669.7A patent/CN108814995A/en active Pending
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102697672A (en) * | 2012-06-05 | 2012-10-03 | 东南大学 | Multiple emulsion of arbutin and preparation method thereof |
Non-Patent Citations (2)
| Title |
|---|
| QIANG WANG等: "Oil-in-oil-in-water pre-double emulsions stabilized by nonionic surfactants and silica particles: A new approach for topical application of rutin", 《COLLOIDS AND SURFACES A: PHYSICOCHEMICAL AND ENGINEERING ASPECTS》 * |
| QIANG WANG等: "Stabilization of a non-aqueous self-doubleemulsifying delivery system of rutin by fat crystals and nonionic surfactants: preparation and bioavailability study", 《FOOD & FUNCTION》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109924491A (en) * | 2019-04-01 | 2019-06-25 | 东南大学 | A kind of dihydromyricetin solid-state self-emulsifying material and its preparation method and application |
| CN113546009A (en) * | 2021-07-30 | 2021-10-26 | 上海应用技术大学 | Water-in-oil type rutin microemulsion and preparation method thereof |
| CN114452227A (en) * | 2022-01-20 | 2022-05-10 | 江南大学 | Method for preparing alcohol-in-water-in-oil-in-water multiple pickering emulsion by anti-solvent recrystallization method |
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Application publication date: 20181116 |