CN106726643A - A kind of many vesicles for coating water-soluble glabridin and preparation method thereof - Google Patents
A kind of many vesicles for coating water-soluble glabridin and preparation method thereof Download PDFInfo
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- CN106726643A CN106726643A CN201710050471.7A CN201710050471A CN106726643A CN 106726643 A CN106726643 A CN 106726643A CN 201710050471 A CN201710050471 A CN 201710050471A CN 106726643 A CN106726643 A CN 106726643A
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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
- A61K8/14—Liposomes; Vesicles
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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
- A61K8/40—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing nitrogen
- A61K8/44—Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts; Esters or N-acylated derivatives 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
- A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
- A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
- A61K8/498—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom having 6-membered rings or their condensed derivatives, e.g. coumarin
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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
- A61K8/55—Phosphorus compounds
- A61K8/553—Phospholipids, e.g. lecithin
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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
- A61K8/63—Steroids; Derivatives thereof
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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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/10—General cosmetic use
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
- A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
- A61K2800/41—Particular ingredients further characterized by their size
- A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns
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Abstract
A kind of many vesicles for coating water-soluble glabridin, are made up of phosphatide, neutral lipid, cholesterol, organic solvent, hydrophilic emulsifier, water-soluble glabridin, amino acid, osmotic pressure regulator and deionized water.Be dissolved in organic solvent for phosphatide, cholesterol and neutral lipid by the present invention, used as organic phase;Water-soluble glabridin, amino acid, osmotic pressure regulator and deionized water are mixed as interior water phase;By in the interior water phase components organic phase component of addition, w/o type colostric fluid is obtained;Hydrophilic emulsifier, amino acid, osmotic pressure regulator and deionized water are mixed as outer water phase;The outer water phase components of homogeneous, add w/o type colostric fluid component, and ultrasound is carried out after homogeneous, are stirred for being cooled into W/O/W type multiple emulsions;Multiple emulsion is scattered in Freamine Ⅲ again, is passed through nitrogen and is removed organic solvent, obtain final product many vesicles suspension of the water-soluble glabridin of cladding.The present invention improves the stability of water-soluble glabridin.
Description
Technical field
The invention belongs to cosmetic field, it is related to a kind of liposome, specifically wraps a kind of water-soluble light Radix Glycyrrhizae of cladding
Fixed many vesicles and preparation method thereof.
Background technology
Glabridin is a kind of efficiency natural whitening factor, and its white-skinned face function is higher by 232 than common ingredients Vitamin C
Times, be described as " whitening gold ", with strong antibacterial, it is anti-oxidant, prevent ultraviolet stimulate cause inflammation, pigmentation and
Pachylosis etc. is acted on, and it can coordinate the skin repair process of self, strengthens whitening effect, and deep layer moistens skin after shining.Light is sweet
The application that grass is scheduled in cosmetics mainly has three broad aspects:Whitening, suppresses melanogen;Anti-inflammatory;It is anti-oxidant.Due to glabridin
Water insoluble property, be typically modified as water solubility to expand range of application, but water-soluble glabridin is in climax ring
Border stability inferior is poor, it is therefore desirable to improve stability to its suitable carrier of offer, and exploitation has that functionality is strong, good stability
Water-soluble glabridin liposome class cosmetics will have broad prospects and application value.
Multivesicular liposome (multivesieularliposomes, MVLs), is a kind of structure also known as many vesicles
Special novel lipid body preparation, its discontinuous aqueous inner chamber is separated by nonconcentric(al) lipoid and immobilized artificial membrane, and formation is permitted
More trickle vesica.MVLS particles are in honeycomb, and particle size is typically between 1-100 μm.The structure of many vesicas of MVLs makes it
Volume is encapsulated with more water-soluble substanceses, hydroecium volume accounts for the 95% of particle overall volume, the load active matter of its water-soluble substances
Amount is more much higher than traditional unilamellar liposome and multilamellar liposome;When certain capsules rupture, active material from rupture vesica
Disengage, complete vesica still can maintain the original state, thus have good slowly releasing effect;The non-concentric structure of lipid layer makes lipid
The stability of body increases, and the release time of active matter extends.
Cladding for hydroaropic substance is needed by means of many vesicles, and water-soluble glabridin is coated on into interior water
Phase, forms a kind of coated carrier structure for being directed to water-soluble glabridin.To improve the stability of water-soluble glabridin, promote
Enter permeability, and then improve the activity of water-soluble glabridin.
At present, the research on many vesicles carrier techniques has had a lot, and mostly coating medicine is applied to medical treatment
Industry, its preparation technology is more complicated, but coats many vesicles of water-soluble glabridin and be applied in cosmetics
There is not yet open.
The content of the invention
For above-mentioned technical problem of the prior art, the invention provides a kind of many capsules for coating water-soluble glabridin
Bubble liposome and preparation method thereof, described many vesicles of this cladding water solubility glabridin and preparation method thereof will
Solve the technical problem of water-soluble glabridin stability difference of the prior art.
The invention provides a kind of many vesicles for coating water-soluble glabridin, count by weight percentage, its
Raw material is constituted and content is as follows:
Phosphatidase 1 .0 ~ 20.0%;
Neutral lipid 1.0 ~ 10.0%;
Cholesterol 1.0 ~ 10.0%;
Organic solvent 5.0 ~ 20.0%;
Water-soluble glabridin 0.01 ~ 5.0%;
Hydrophilic emulsifier 0.1 ~ 12.0%;
Amino acid 0.1 ~ 1.0%;
Osmotic pressure regulator 2.0 ~ 8.0%;
Deionized water surplus;
Described phosphoric acid is lecithin, hydrolecithin, soybean lecithin, phosphatidyl-ethanolamine, DSPC, two
In dimyristoylphosphatidycholine, DOPE or DPPG one or two with
On the mixture that is constituted;
Described neutral lipid is olein, glyceric acid, glyceryl laurate ester, decanoin, three sad glycerine
One or more mixtures for being constituted in ester or vitamin E;
Described organic solvent is by one or more mixing for constituting in ether, ethanol, butanol or ethyl acetate
Thing;
Described hydrophilic emulsifier is hydrophilic Tween 80, polyox-yethylene-polyoxypropylene block copolymer, peptides bimolecular oleophylic
Table work, PEG-100 stearates, stearine, arachidic alcohol and docosyl alcohol and arachidic alcohol glucoside, cetostearyl alcohol and whale
Wax stearyl glucoside, AEO(21EO), in Compritol 888 ATO or cetearyl glucoside one
Plant or two or more constituted mixtures;
Described amino acid is lysine, asparatate, serine, L-arginine, alanine, L-aminobutanedioic acid, glutamic acid, sweet
One or more mixture in propylhomoserin, histidine, tryptophan, tyrosine, proline, leucine or valine;
Described osmotic pressure regulator is one or more the mixture in glucose, sucrose or physiological saline.
Further, a kind of many vesicles of above-mentioned cladding water solubility glabridin, count by weight percentage,
Its raw material is constituted and content is as follows:
Phosphatidase 1 .0%;
Neutral lipid 1.0%;
Cholesterol 1.0%;
Organic solvent 5.0%;
Water-soluble glabridin 0.01%;
Hydrophilic emulsifier 0.1%;
Amino acid 0.1%;
Osmotic pressure regulator 2.0%;
Deionized water surplus;
Described phosphatide is lecithin;
Described neutral grease is olein;
Described organic solvent is ether;
Described hydrophilic emulsifier is Tween 80;
Described amino acid is lysine;
Described osmotic pressure regulator is glucose.
Further, a kind of many vesicles of above-mentioned cladding water solubility glabridin, count by weight percentage,
Its raw material is constituted and content is as follows:
Phosphatidase 1 0.0%;
Neutral lipid 5.0%;
Cholesterol 5.0%;
Organic solvent 12.5%;
Water-soluble glabridin 2.5%;
Hydrophilic emulsifier 6.0%;
Amino acid 0.5%;
Osmotic pressure regulator 5.0%;
Deionized water surplus;
Described phosphatide is the mixture of one or two compositions in hydrolecithin or soybean lecithin;
Described neutral substance is glyceric acid;
Described organic solvent is ethanol;
Described hydrophilic emulsifier is in polyox-yethylene-polyoxypropylene block copolymer or PEG-100 stearates
Plant or two kinds of mixtures for being constituted;
Described amino acid is asparatate;
Described osmotic pressure regulator is sucrose.
Further, a kind of many vesicles of above-mentioned cladding water solubility glabridin, count by weight percentage,
Its raw material is constituted and content is as follows:
Phosphatidase 2 0.0%
Neutral lipid 10.0%
Cholesterol 10.0%
Organic solvent 20.0%
Water-soluble glabridin 5.0%
Hydrophilic emulsifier 12.0%
Amino acid/11 .0%
Osmotic pressure regulator 8.0%
Deionized water surplus;
Described phosphoric acid is phosphatidyl-ethanolamine;
Described neutral lipid is by one or two mixtures for constituting in tricaprylin or vitamin E;
Described organic solvent is butanol;
Described hydrophilic emulsifier is that the hydrophilic table of peptides bimolecular oleophylic is lived or cetostearyl alcohol and cetearyl glucose
One or two mixtures for being constituted in glycosides;
Described amino acid is L-arginine;
Described osmotic pressure regulator is physiological saline.
Present invention also offers a kind of preparation method of many vesicles of above-mentioned cladding water solubility glabridin, bag
Include following steps:
1) phosphatide, neutral lipid, cholesterol, organic solvent, hydrophilic emulsifier, water-soluble light Radix Glycyrrhizae are weighed by weight percentage
Fixed, amino acid, osmotic pressure regulator and deionized water;
2) phosphatide, cholesterol and neutral lipid are dissolved in organic solvent, as organic phase;
3) Freamine Ⅲ of 1 ~ 100mmol/L is configured, by water-soluble glabridin, 30 ~ 60% Freamine Ⅲ, 30 ~ 60%
Osmotic pressure regulator and 30 ~ 60% deionized water mixing, as interior water phase;
4) by step 3)Water is added in organic phase in middle gained, with homogeneous speed 7200~30000rpm homogeneous organic phase groups
Point, while interior water phase components are added thereto, 1~15min of homogeneous, w/o type colostric fluid is obtained;
5) by hydrophilic emulsifier, the Freamine Ⅲ of remaining content, the osmotic pressure regulator of remaining content and remaining content
Deionized water mixes, used as outer water phase;
6) with the outer water phase components of homogeneous 7200~30000rpm of speed homogeneous, while by step 4)Obtained w/o type colostric fluid group
Point be added thereto, after 1~15min of homogeneous, select ultrasonic power 20%~30%, ultrasound stops 5 seconds in 5 seconds, to emulsion ultrasound 1~
20min, to system, natural cooling is down to room temperature in the lump for stirring, is made W/O/W type multiple emulsions;
7) configuration and step 3) in concentration identical Freamine Ⅲ, the amino acid that the multiple emulsion that will be obtained is scattered in configuration is molten
In liquid, wherein multiple emulsion and the volume ratio of Freamine Ⅲ is 5:1~1:5, be passed through nitrogen remove multiple emulsion in it is organic
Solvent, is obtained many vesicles suspension of the water-soluble glabridin of cladding.
The step 7) in Freamine Ⅲ effect be influence the aqueous solution pH, adjust oil-water interfaces phosphatide surface electricity
Lotus, improves the electrostatic stability of many vesicles, reduces many vesicles and blows down breaking during removing organic solvent in nitrogen
Newborn phenomenon, and the forming process of many vesicles is not involved in, therefore the content of amino acid does not include this part in formula.
Be dissolved in organic solvent for phosphatide, cholesterol and neutral lipid by the present invention, used as organic phase;By water-soluble light Radix Glycyrrhizae
Fixed, amino acid, osmotic pressure regulator and deionized water are well mixed as interior water phase;The organic phase component of homogeneous, by interior water phase group
Divide and add, w/o type colostric fluid is obtained;Hydrophilic emulsifier, amino acid, osmotic pressure regulator and deionized water are mixed, dispersion
Uniformly as outer water phase;The outer water phase components of homogeneous, the w/o type colostric fluid component prepared before addition carries out ultrasound after homogeneous, then
Stirring is cooled to room temperature, forms W/O/W type multiple emulsions;Multiple emulsion is scattered in Freamine Ⅲ again, is passed through nitrogen and is removed
The organic solvent gone in multiple emulsion, obtains final product many vesicles suspension of the water-soluble glabridin of cladding.
Present invention employs suitable phosphatide, neutral lipid, cholesterol, organic solvent, amino acid, osmotic pressure regulator and
The compound scheme of deionized water.Using two step emulsion processes, and ultrasound is carried out, therefore, many vesicles of final gained
The particle diameter of dispersed phase particles is more uniform, and its preparation process is simple, energy consumption are low, the emulsion system stabilization of formation, not only feeds water
Dissolubility glabridin provides suitable carrier, improves the stability of water-soluble glabridin, and it is gentle to skin, absorbs
Hurry up, have feature and esthetics concurrently.
The present invention is compared with prior art, and its technological progress is significant.The water-soluble glabridin of cladding of the invention
Many vesicles, for the cladding of water-soluble glabridin provides suitable carrier, while improving the steady of water-soluble glabridin
It is qualitative, promote permeability, and then improve the activity of water-soluble glabridin, develop with functionality is strong, good stability, nontoxic
The cosmetics of harmless containing water-soluble glabridin active matter.
Brief description of the drawings
Fig. 1 is the microphotograph of many vesicles of the water-soluble glabridin of cladding of the gained of embodiment 1.
Specific embodiment
The present invention is expanded on further below by specific embodiment and with reference to accompanying drawing, but is not intended to limit the present invention.
Embodiment 1
A kind of many vesicles for coating water-soluble glabridin, count by weight percentage, its raw material composition and content are such as
Under:
Phosphatidase 1 .0%;
Neutral lipid 1.0%;
Cholesterol 1.0%;
Organic solvent 5.0%;
Water-soluble glabridin 0.01%;
Hydrophilic emulsifier 0.1%;
Amino acid 0.1%;
Osmotic pressure regulator 2.0%;
Deionized water surplus;%
Described phosphatide is lecithin;
Described neutral grease is olein;
Described organic solvent is ether;
Described hydrophilic emulsifier is Tween 80;
Described amino acid is lysine;
Described osmotic pressure regulator is glucose;
A kind of preparation method of many vesicles of above-mentioned cladding water solubility glabridin, specifically includes following steps:
1) phosphatide, neutral lipid, cholesterol, organic solvent, hydrophilic emulsifier, water-soluble light Radix Glycyrrhizae are weighed by weight percentage
Fixed, amino acid, osmotic pressure regulator and deionized water;
2) phosphatide, cholesterol and neutral lipid are dissolved in organic solvent, as organic phase;
3) Freamine Ⅲ of 1 ~ 100mmol/L is configured, by water-soluble glabridin, 30 ~ 60% Freamine Ⅲ, 30 ~ 60%
Osmotic pressure regulator and 30 ~ 60% deionized water mixing, as interior water phase;
4) by step 3)Water is added in organic phase in middle gained, with homogeneous speed 7200~30000rpm homogeneous organic phase groups
Point, while interior water phase components are added thereto, 1~15min of homogeneous, w/o type colostric fluid is obtained;
5) by hydrophilic emulsifier, the Freamine Ⅲ of remaining content, the osmotic pressure regulator of remaining content and remaining content
Deionized water mixes, used as outer water phase;
6) with the outer water phase components of homogeneous 7200~30000rpm of speed homogeneous, while by step 4)Obtained w/o type colostric fluid group
Point be added thereto, after 1~15min of homogeneous, select ultrasonic power 20%~30%, ultrasound stops 5 seconds in 5 seconds, to emulsion ultrasound 1~
20min, to system, natural cooling is down to room temperature in the lump for stirring, is made W/O/W type multiple emulsions;
7) configuration and step 3) in concentration identical Freamine Ⅲ, the amino acid that the multiple emulsion that will be obtained is scattered in configuration is molten
In liquid, wherein multiple emulsion and the volume ratio of Freamine Ⅲ is 5:1~1:5, be passed through nitrogen remove multiple emulsion in it is organic
Solvent, is obtained many vesicles suspension of the water-soluble glabridin of cladding.
Embodiment 2
A kind of many vesicles for coating water-soluble glabridin, count by weight percentage, its raw material composition and content are such as
Under:
Phosphatidase 1 0.0%;
Neutral lipid 5.0%;
Cholesterol 5.0%;
Organic solvent 12.5%;
Water-soluble glabridin 2.5%;
Hydrophilic emulsifier 6.0%;
Amino acid 0.5%;
Osmotic pressure regulator 5.0%;
Deionized water 53.5%;
Described phosphatide is the mixture of one or two compositions in hydrolecithin, soybean lecithin;
Described neutral substance is glyceric acid;
Described organic solvent is ethanol;
Described hydrophilic emulsifier be polyox-yethylene-polyoxypropylene block copolymer, PEG-100 stearates in one kind or
Two kinds of mixtures for being constituted;
Described amino acid is asparatate;
Described osmotic pressure regulator is sucrose;
A kind of preparation method of many vesicles of above-mentioned cladding water solubility glabridin, specifically includes following steps:
1) phosphatide, neutral lipid, cholesterol, organic solvent, hydrophilic emulsifier, water-soluble light Radix Glycyrrhizae are weighed by weight percentage
Fixed, amino acid, osmotic pressure regulator and deionized water;
2) phosphatide, cholesterol and neutral lipid are dissolved in organic solvent, as organic phase;
3) Freamine Ⅲ of 1 ~ 100mmol/L is configured, by water-soluble glabridin, 30 ~ 60% Freamine Ⅲ, 30 ~ 60%
Osmotic pressure regulator and 30 ~ 60% deionized water mixing, as interior water phase;
4) by step 3)Water is added in organic phase in middle gained, with homogeneous speed 7200~30000rpm homogeneous organic phase groups
Point, while interior water phase components are added thereto, 1~15min of homogeneous, w/o type colostric fluid is obtained;
5) by hydrophilic emulsifier, the Freamine Ⅲ of remaining content, the osmotic pressure regulator of remaining content and remaining content
Deionized water mixes, used as outer water phase;
6) with the outer water phase components of homogeneous 7200~30000rpm of speed homogeneous, while by step 4)Obtained w/o type colostric fluid group
Point be added thereto, after 1~15min of homogeneous, select ultrasonic power 20%~30%, ultrasound stops 5 seconds in 5 seconds, to emulsion ultrasound 1~
20min, to system, natural cooling is down to room temperature in the lump for stirring, is made W/O/W type multiple emulsions;
7) configuration and step 3) in concentration identical Freamine Ⅲ, the amino acid that the multiple emulsion that will be obtained is scattered in configuration is molten
In liquid, wherein multiple emulsion and the volume ratio of Freamine Ⅲ is 5:1~1:5, be passed through nitrogen remove multiple emulsion in it is organic
Solvent, is obtained many vesicles suspension of the water-soluble glabridin of cladding.
Embodiment 3
A kind of many vesicles for coating water-soluble glabridin, count by weight percentage, its raw material composition and content are such as
Under:
Phosphatidase 2 0.0%;
Neutral lipid 10.0%;
Cholesterol 10.0%;
Organic solvent 20.0%
Water-soluble glabridin 5.0%;
Hydrophilic emulsifier 12.0%;
Amino acid/11 .0%;
Osmotic pressure regulator 8.0%;
Deionized water 14.0%;
Described phosphoric acid is phosphatidyl-ethanolamine;
Described neutral lipid is by one or two mixtures for constituting in tricaprylin, vitamin E;
Described organic solvent is butanol;
Described hydrophilic emulsifier is in the hydrophilic table work of peptides bimolecular oleophylic, cetostearyl alcohol and cetearyl glucoside
One or two composition mixtures;
Described amino acid is L-arginine;
Described osmotic pressure regulator is physiological saline;
A kind of preparation method of many vesicles of above-mentioned cladding water solubility glabridin, specifically includes following steps:
1) phosphatide, neutral lipid, cholesterol, organic solvent, hydrophilic emulsifier, water-soluble light Radix Glycyrrhizae are weighed by weight percentage
Fixed, amino acid, osmotic pressure regulator and deionized water;
2) phosphatide, cholesterol and neutral lipid are dissolved in organic solvent, as organic phase;
3) Freamine Ⅲ of 1 ~ 100mmol/L is configured, by water-soluble glabridin, 30 ~ 60% Freamine Ⅲ, 30 ~ 60%
Osmotic pressure regulator and 30 ~ 60% deionized water mixing, as interior water phase;
4) by step 3)Water is added in organic phase in middle gained, with homogeneous speed 7200~30000rpm homogeneous organic phase groups
Point, while interior water phase components are added thereto, 1~15min of homogeneous, w/o type colostric fluid is obtained;
5) by hydrophilic emulsifier, the Freamine Ⅲ of remaining content, the osmotic pressure regulator of remaining content and remaining content
Deionized water mixes, used as outer water phase;
6) with the outer water phase components of homogeneous 7200~30000rpm of speed homogeneous, while by step 4)Obtained w/o type colostric fluid group
Point be added thereto, after 1~15min of homogeneous, select ultrasonic power 20%~30%, ultrasound stops 5 seconds in 5 seconds, to emulsion ultrasound 1~
20min, to system, natural cooling is down to room temperature in the lump for stirring, is made W/O/W type multiple emulsions;
7) configuration and step 3) in concentration identical Freamine Ⅲ, the amino acid that the multiple emulsion that will be obtained is scattered in configuration is molten
In liquid, wherein multiple emulsion and the volume ratio of Freamine Ⅲ is 5:1~1:5, be passed through nitrogen remove multiple emulsion in it is organic
Solvent, is obtained many vesicles suspension of the water-soluble glabridin of cladding.
The above is only the basic explanation under present inventive concept, and according to technical scheme made it is any etc.
Effect conversion, all should belong to protection scope of the present invention.
Claims (5)
1. a kind of many vesicles for coating water-soluble glabridin, it is characterised in that count by weight percentage, its raw material
Composition and content are as follows:
Phosphatidase 1 .0 ~ 20.0%;
Neutral lipid 1.0 ~ 10.0%;
Cholesterol 1.0 ~ 10.0%;
Organic solvent 5.0 ~ 20.0%;
Water-soluble glabridin 0.01 ~ 5.0%;
Hydrophilic emulsifier 0.1 ~ 12.0%;
Amino acid 0.1 ~ 1.0%;
Osmotic pressure regulator 2.0 ~ 8.0%;
Deionized water surplus;
Described phosphoric acid is lecithin, hydrolecithin, soybean lecithin, phosphatidyl-ethanolamine, DSPC, two
In dimyristoylphosphatidycholine, DOPE or DPPG one or two with
On the mixture that is constituted;
Described neutral lipid is olein, glyceric acid, glyceryl laurate ester, decanoin, three sad glycerine
One or more mixtures for being constituted in ester or vitamin E;
Described organic solvent is by one or more mixing for constituting in ether, ethanol, butanol or ethyl acetate
Thing;
Described hydrophilic emulsifier is hydrophilic Tween 80, polyox-yethylene-polyoxypropylene block copolymer, peptides bimolecular oleophylic
Table work, PEG-100 stearates, stearine, arachidic alcohol and docosyl alcohol and arachidic alcohol glucoside, cetostearyl alcohol and whale
Wax stearyl glucoside, AEO(21EO), in Compritol 888 ATO or cetearyl glucoside one
Plant or two or more constituted mixtures;
Described amino acid is lysine, asparatate, serine, L-arginine, alanine, L-aminobutanedioic acid, glutamic acid, sweet
One or more mixture in propylhomoserin, histidine, tryptophan, tyrosine, proline, leucine or valine;
Described osmotic pressure regulator is one or more the mixture in glucose, sucrose or physiological saline.
2. a kind of many vesicles for coating water-soluble glabridin as claimed in claim 1, it is characterised in that by weight
Percentage is calculated, and its raw material composition and content are as follows:
Phosphatidase 1 .0%;
Neutral lipid 1.0%;
Cholesterol 1.0%;
Organic solvent 5.0%;
Water-soluble glabridin 0.01%;
Hydrophilic emulsifier 0.1%;
Amino acid 0.1%;
Osmotic pressure regulator 2.0%;
Deionized water surplus;
Described phosphatide is lecithin;
Described neutral grease is olein;
Described organic solvent is ether;
Described hydrophilic emulsifier is Tween 80;
Described amino acid is lysine;
Described osmotic pressure regulator is glucose.
3. a kind of many vesicles for coating water-soluble glabridin as claimed in claim 1, it is characterised in that by weight
Percentage is calculated, and its raw material composition and content are as follows:
Phosphatidase 1 0.0%;
Neutral lipid 5.0%;
Cholesterol 5.0%;
Organic solvent 12.5%;
Water-soluble glabridin 2.5%;
Hydrophilic emulsifier 6.0%;
Amino acid 0.5%;
Osmotic pressure regulator 5.0%;
Deionized water surplus;
Described phosphatide is the mixture of one or two compositions in hydrolecithin or soybean lecithin;
Described neutral substance is glyceric acid;
Described organic solvent is ethanol;
Described hydrophilic emulsifier is in polyox-yethylene-polyoxypropylene block copolymer or PEG-100 stearates
Plant or two kinds of mixtures for being constituted;
Described amino acid is asparatate;
Described osmotic pressure regulator is sucrose.
4. a kind of many vesicles for coating water-soluble glabridin as claimed in claim 1, it is characterised in that by weight
Percentage is calculated, and its raw material composition and content are as follows:
Phosphatidase 2 0.0%
Neutral lipid 10.0%
Cholesterol 10.0%
Organic solvent 20.0%
Water-soluble glabridin 5.0%
Hydrophilic emulsifier 12.0%
Amino acid/11 .0%
Osmotic pressure regulator 8.0%
Deionized water surplus;
Described phosphoric acid is phosphatidyl-ethanolamine;
Described neutral lipid is by one or two mixtures for constituting in tricaprylin or vitamin E;
Described organic solvent is butanol;
Described hydrophilic emulsifier is that the hydrophilic table of peptides bimolecular oleophylic is lived or cetostearyl alcohol and cetearyl glucose
One or two mixtures for being constituted in glycosides;
Described amino acid is L-arginine;
Described osmotic pressure regulator is physiological saline.
5. a kind of preparation method of many vesicles of the water-soluble glabridin of cladding described in claims 1,2,3 or 4,
It is characterized in that comprising the following steps:
1)Phosphatide, neutral lipid, cholesterol, organic solvent, hydrophilic emulsifier, water-soluble light Radix Glycyrrhizae are weighed by weight percentage
Fixed, amino acid, osmotic pressure regulator and deionized water;
2)Phosphatide, cholesterol and neutral lipid are dissolved in organic solvent, as organic phase;
3)The Freamine Ⅲ of 1 ~ 100mmol/L is configured, by water-soluble glabridin, 30 ~ 60% Freamine Ⅲ, 30 ~ 60%
Osmotic pressure regulator and 30 ~ 60% deionized water mixing, as interior water phase;
4)By step 3)Water is added in organic phase in middle gained, with homogeneous speed 7200~30000rpm homogeneous organic phase groups
Point, while interior water phase components are added thereto, 1~15min of homogeneous, w/o type colostric fluid is obtained;
5)By going for water emulsifier, the Freamine Ⅲ of remaining content, the osmotic pressure regulator of remaining content and remaining content
Ionized water mixes, used as outer water phase;
6)With the outer water phase components of homogeneous 7200~30000rpm of speed homogeneous, while by step 4)Obtained w/o type colostric fluid group
Point be added thereto, after 1~15min of homogeneous, select ultrasonic power 20%~30%, ultrasound stops 5 seconds in 5 seconds, to emulsion ultrasound 1~
20min, to system, natural cooling is down to room temperature in the lump for stirring, is made W/O/W type multiple emulsions;
7)Configuration and step 3) in concentration identical Freamine Ⅲ, the amino acid that the multiple emulsion that will be obtained is scattered in configuration is molten
In liquid, wherein multiple emulsion and the volume ratio of Freamine Ⅲ is 5:1~1:5, be passed through nitrogen remove multiple emulsion in it is organic
Solvent, is obtained many vesicles suspension of the water-soluble glabridin of cladding.
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CN113893191A (en) * | 2021-11-12 | 2022-01-07 | 湖北省麦诗特生物科技有限公司 | Whitening essence based on phospholipid-coated glabridin nanoemulsion and preparation method thereof |
US11617706B2 (en) | 2020-06-29 | 2023-04-04 | The Procter & Gamble Company | Hair conditioning composition free of fatty alcohol |
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CN103432009A (en) * | 2013-09-12 | 2013-12-11 | 广东轻工职业技术学院 | Whitening agent liposome coating micro-capsule composition as well as preparation method and application thereof |
CN105581911A (en) * | 2014-11-27 | 2016-05-18 | 无限极(中国)有限公司 | Glabridin-cladded nano solid lipid carrier and preparation method and application thereof |
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CN103432009A (en) * | 2013-09-12 | 2013-12-11 | 广东轻工职业技术学院 | Whitening agent liposome coating micro-capsule composition as well as preparation method and application thereof |
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US11617706B2 (en) | 2020-06-29 | 2023-04-04 | The Procter & Gamble Company | Hair conditioning composition free of fatty alcohol |
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