CN114601746B - Efficient-permeation microemulsion and preparation method and application thereof - Google Patents
Efficient-permeation microemulsion and preparation method and application thereof Download PDFInfo
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- 239000004530 micro-emulsion Substances 0.000 title claims abstract description 24
- 238000002360 preparation method Methods 0.000 title claims abstract description 11
- 238000000593 microemulsion method Methods 0.000 title description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 25
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 24
- 229920002385 Sodium hyaluronate Polymers 0.000 claims abstract description 22
- 239000008367 deionised water Substances 0.000 claims abstract description 22
- 229910021641 deionized water Inorganic materials 0.000 claims abstract description 22
- 229940010747 sodium hyaluronate Drugs 0.000 claims abstract description 22
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 claims abstract description 22
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 claims abstract description 21
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 claims abstract description 21
- AJLNZWYOJAWBCR-OOPVGHQCSA-N (4s)-4-acetamido-5-[[(2s)-1-[[(2s)-1-[[(2s)-5-amino-1-[[(2s)-1-[[(2s)-1-amino-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-car Chemical compound OC(=O)CC[C@H](NC(C)=O)C(=C)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O AJLNZWYOJAWBCR-OOPVGHQCSA-N 0.000 claims abstract description 20
- PRAKJMSDJKAYCZ-UHFFFAOYSA-N squalane Chemical compound CC(C)CCCC(C)CCCC(C)CCCCC(C)CCCC(C)CCCC(C)C PRAKJMSDJKAYCZ-UHFFFAOYSA-N 0.000 claims abstract description 20
- 229940095094 acetyl hexapeptide-8 Drugs 0.000 claims abstract description 19
- 108010006338 acetyl-glutamyl-glutamyl-methionyl-glutaminyl-arginyl-argininamide Proteins 0.000 claims abstract description 19
- APZYKUZPJCQGPP-UHFFFAOYSA-N Tetrahydropiperine Chemical compound C=1C=C2OCOC2=CC=1CCCCC(=O)N1CCCCC1 APZYKUZPJCQGPP-UHFFFAOYSA-N 0.000 claims abstract description 18
- JXTPJDDICSTXJX-UHFFFAOYSA-N n-Triacontane Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCC JXTPJDDICSTXJX-UHFFFAOYSA-N 0.000 claims abstract description 10
- 229940032094 squalane Drugs 0.000 claims abstract description 10
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims abstract description 8
- CNXJITYCNQNTBD-UHFFFAOYSA-L dipotassium;hexadecyl phosphate Chemical compound [K+].[K+].CCCCCCCCCCCCCCCCOP([O-])([O-])=O CNXJITYCNQNTBD-UHFFFAOYSA-L 0.000 claims abstract description 6
- 239000002994 raw material Substances 0.000 claims description 29
- 238000003756 stirring Methods 0.000 claims description 22
- 229920001184 polypeptide Polymers 0.000 claims description 18
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 18
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 18
- 239000013543 active substance Substances 0.000 claims description 11
- 239000011259 mixed solution Substances 0.000 claims description 10
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 claims description 9
- 238000002156 mixing Methods 0.000 claims description 7
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 230000001815 facial effect Effects 0.000 claims description 6
- 239000003995 emulsifying agent Substances 0.000 claims description 5
- 150000002148 esters Chemical class 0.000 claims description 5
- 230000000149 penetrating effect Effects 0.000 claims description 5
- 239000003755 preservative agent Substances 0.000 claims description 5
- 230000002335 preservative effect Effects 0.000 claims description 5
- 238000001816 cooling Methods 0.000 claims description 4
- 229920000223 polyglycerol Polymers 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 3
- 239000002245 particle Substances 0.000 claims description 3
- 230000002421 anti-septic effect Effects 0.000 claims description 2
- 230000035515 penetration Effects 0.000 claims 1
- 239000000839 emulsion Substances 0.000 abstract description 28
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 abstract description 24
- 235000019437 butane-1,3-diol Nutrition 0.000 abstract description 12
- 230000000694 effects Effects 0.000 abstract description 11
- 230000037303 wrinkles Effects 0.000 abstract description 10
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 abstract description 8
- 229960005323 phenoxyethanol Drugs 0.000 abstract description 8
- 229940105132 myristate Drugs 0.000 abstract description 7
- TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 abstract description 7
- 230000007794 irritation Effects 0.000 abstract description 4
- 229960005150 glycerol Drugs 0.000 abstract 1
- 238000000034 method Methods 0.000 description 7
- 239000000126 substance Substances 0.000 description 6
- 239000003961 penetration enhancing agent Substances 0.000 description 5
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 4
- 230000001502 supplementing effect Effects 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 241000274177 Juniperus sabina Species 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 241001220680 Sibiraea Species 0.000 description 3
- 239000012467 final product Substances 0.000 description 3
- 230000003204 osmotic effect Effects 0.000 description 3
- RMGVATURDVPNOZ-UHFFFAOYSA-M potassium;hexadecyl hydrogen phosphate Chemical compound [K+].CCCCCCCCCCCCCCCCOP(O)([O-])=O RMGVATURDVPNOZ-UHFFFAOYSA-M 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 241000196324 Embryophyta Species 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- POJWUDADGALRAB-UHFFFAOYSA-N allantoin Chemical compound NC(=O)NC1NC(=O)NC1=O POJWUDADGALRAB-UHFFFAOYSA-N 0.000 description 2
- 238000000265 homogenisation Methods 0.000 description 2
- 239000012466 permeate Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- IHRKJQSLKLYWBQ-QKDODKLFSA-N (2s)-2-[[(2s)-1-[(2s)-5-amino-2-[[2-(hexadecanoylamino)acetyl]amino]-5-oxopentanoyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid Chemical compound CCCCCCCCCCCCCCCC(=O)NCC(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(O)=O IHRKJQSLKLYWBQ-QKDODKLFSA-N 0.000 description 1
- ROTFCACGLKOUGI-JYJNAYRXSA-N (2s)-2-[[(2s)-2-[[(2s)-2-(3-acetamidopropanoylamino)-3-(1h-imidazol-5-yl)propanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1h-imidazol-5-yl)propanoic acid Chemical compound C([C@H](NC(=O)CCNC(=O)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=1NC=NC=1)C(O)=O)C1=CN=CN1 ROTFCACGLKOUGI-JYJNAYRXSA-N 0.000 description 1
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 description 1
- POJWUDADGALRAB-PVQJCKRUSA-N Allantoin Natural products NC(=O)N[C@@H]1NC(=O)NC1=O POJWUDADGALRAB-PVQJCKRUSA-N 0.000 description 1
- PAHWROPPWOVREG-UHFFFAOYSA-N P(=O)(O)(O)O.C(CCCCCCCCCCCCCCC)[K] Chemical compound P(=O)(O)(O)O.C(CCCCCCCCCCCCCCC)[K] PAHWROPPWOVREG-UHFFFAOYSA-N 0.000 description 1
- 241000758706 Piperaceae Species 0.000 description 1
- 238000001604 Rao's score test Methods 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 229960000458 allantoin Drugs 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000019522 cellular metabolic process Effects 0.000 description 1
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 description 1
- 239000003651 drinking water Substances 0.000 description 1
- 235000020188 drinking water Nutrition 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 238000000605 extraction Methods 0.000 description 1
- 230000003993 interaction Effects 0.000 description 1
- 229960003639 laurocapram Drugs 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 229940094946 palmitoyl tetrapeptide-7 Drugs 0.000 description 1
- WCVRQHFDJLLWFE-UHFFFAOYSA-N pentane-1,2-diol Chemical compound CCCC(O)CO WCVRQHFDJLLWFE-UHFFFAOYSA-N 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 229940097941 polyglyceryl-10 laurate Drugs 0.000 description 1
- 229940061570 polyglyceryl-10 stearate Drugs 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 230000008929 regeneration Effects 0.000 description 1
- 238000011069 regeneration method Methods 0.000 description 1
- 230000008591 skin barrier function Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- HQHCYKULIHKCEB-UHFFFAOYSA-N tetradecanedioic acid Chemical compound OC(=O)CCCCCCCCCCCCC(O)=O HQHCYKULIHKCEB-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- A61K8/64—Proteins; Peptides; Derivatives or degradation products thereof
-
- 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
-
- 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
- A61K8/31—Hydrocarbons
-
- 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
-
- 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
-
- 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
-
- 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
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
- A61K8/73—Polysaccharides
- A61K8/735—Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
-
- 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
- A61Q19/08—Anti-ageing preparations
-
- 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
- A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
- A61K2800/805—Corresponding aspects not provided for by any of codes A61K2800/81 - A61K2800/95
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Birds (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Dispersion Chemistry (AREA)
- Gerontology & Geriatric Medicine (AREA)
- Dermatology (AREA)
- Cosmetics (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicinal Preparation (AREA)
Abstract
The invention provides a high-efficiency permeation microemulsion and a preparation method and application thereof, wherein polyglycerol-10 myristate, glycerol, squalane, cetyl phosphate potassium, tetrahydropiperine and deionized water are homogenized under high pressure, and then mixed with deionized water, 1, 3-butanediol, sodium hyaluronate, sodium polyacrylate and EDTA-2Na, and acetyl hexapeptide-8 and phenoxyethanol are added to prepare the emulsion. The emulsion is milder, has no irritation to skin, and has good wrinkle removing effect.
Description
Technical Field
The invention belongs to the field of A61Q19/08, and particularly relates to a high-efficiency permeation microemulsion, and a preparation method and application thereof.
Background
The polypeptide active substance has extremely high activity, can promote the regeneration of organisms, the metabolism of cells and other functions, and is an important active substance in human bodies. The field of skin care products is often achieved by adding polypeptide active substances to achieve the purpose of skin vitality.
Chinese patent CN110151597A discloses a polypeptide emulsion, which is prepared by mixing various polypeptide substances, adding into a solution composed of raw materials such as propylene glycol, allantoin and the like, and uniformly stirring to obtain the polypeptide emulsion. However, the polypeptide substances contained in the product are limited by the self-permeation capacity and lack permeation promoting substances, so that the polypeptide substances are difficult to permeate the skin in the use process, and the use effect of the emulsion is reduced. However, the skin barrier layer is damaged by the increased amount of the permeation enhancer, which causes irritation, is not suitable for sensitive muscle, and the satisfactory effect is not achieved by the reduced amount.
Based on the above, the application provides a high-efficiency osmotic microemulsion and a preparation method thereof, and the osmotic absorption effect of polypeptide substances is improved in a mild, safe and healthy manner.
Disclosure of Invention
In a first aspect, the invention provides a high-efficiency osmotic microemulsion prepared from phase A containing an permeation enhancer and phase B containing a polypeptide active substance.
In a preferred embodiment, the permeation enhancer in phase a is selected from at least one of tetrahydropiperine, 1, 2-pentanediol, laurocapram, ethoxydiglycol.
In a preferred embodiment, the permeation enhancer in phase a is tetrahydropiperine.
Tetrahydropiperine is extracted from plants of Piperaceae, is a safe and efficient natural plant extraction permeation-assisting substance, and drives effective active ingredients to permeate cells by promoting the flow of a cell phospholipid bilayer.
In a preferred embodiment, the polypeptide active in phase B is selected from at least one of acetyl hexapeptide-8, acetyl hexapeptide-3, acetyl tetrapeptide-5, palmitoyl tetrapeptide-7, palmitoyl pentapeptide.
In a preferred embodiment, the polypeptide active in phase B is acetyl hexapeptide-8.
In a preferred embodiment, the phase a further comprises a polyglycerol ester emulsifier, glycerol, squalane, potassium cetyl phosphate, deionized water; the phase B also comprises butanediol, sodium hyaluronate, sodium polyacrylate, EDTA-2Na, a preservative and deionized water.
In a preferred embodiment, the butanediol is 1, 3-butanediol.
In a preferred embodiment, the polyglyceryl ester emulsifier is selected from at least one of polyglyceryl-10 myristate, polyglyceryl-10 laurate, polyglyceryl-10 stearate, polyglyceryl-10 eicosadioate, polyglyceryl-10 tetradecanedioate.
In a preferred embodiment, the polyglycerol ester emulsifier is polyglycerol-10 myristate.
In a preferred embodiment, the mass sum of the phases A and B is 100 parts by weight.
In a preferred embodiment, the phase A raw material comprises, by weight, 0.1-0.8 part of a polyglycerol ester emulsifier, 5-10 parts of glycerol, 1.5-3.5 parts of squalane, 0.01-0.1 part of potassium cetyl phosphate, 0.01-0.1 part of a permeation enhancer and 1-5 parts of deionized water.
In a preferred embodiment, the A phase raw material comprises 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of cetyl phosphate potassium, 0.01-part of tetrahydropiperine and 1.5 parts of deionized water according to parts by weight.
In a preferred embodiment, the B phase raw material comprises 5 parts by weight of polypeptide active substance, 5-10 parts by weight of butanediol, 0.01-0.08 part by weight of sodium hyaluronate, 0.2-0.6 part by weight of sodium polyacrylate, 0.05 part by weight of EDTA-2Na0.05 part by weight of preservative, and the balance of deionized water.
In a preferred embodiment, the B phase raw material comprises, by weight, acetyl hexapeptide-85 parts, butanediol 5 parts, sodium hyaluronate 0.05 parts, sodium polyacrylate 0.5 parts, EDTA-2Na0.05 parts, preservative 0.5 parts, and deionized water for supplementing the balance.
In a preferred embodiment, the preservative is phenoxyethanol.
In a preferred embodiment, the acetyl hexapeptide-8 is present at a concentration of 1000ppm by mass and is purchased from the company Biochemical industries, inc. of the Nanj family.
The second aspect of the invention provides a method for preparing a high-efficiency permeable microemulsion, which comprises the following steps:
(1) Mixing and heating the phase A raw materials, homogenizing by a homogenizer until the particle size is 150-200nm, and cooling to obtain phase A mixed solution;
(2) And (3) after uniformly mixing the phase B, adding the phase A mixed solution, and homogenizing to obtain the high-efficiency permeable microemulsion.
In a preferred embodiment, the detailed steps of step (2) are as follows: premixing sodium polyacrylate, butanediol and sodium hyaluronate, stirring deionized water and EDTA-2Na, adding the premixed sodium polyacrylate, butanediol and sodium hyaluronate, stirring, adding phase A mixed solution, homogenizing, adding antiseptic and polypeptide active substance, and stirring.
In the application, the applicant finds that the specific raw materials and the specific preparation method can improve the permeability of the polypeptide active substances to obtain emulsion with good wrinkle removal effect, and the dosage of the permeation assisting agent is only 20% of that of the common emulsion. In the application, through a specific preparation method, oil phase components formed by tetrahydropiperine, potassium cetyl phosphate, squalane and the like are added into water phases formed by 1, 3-butanediol, sodium hyaluronate, deionized water and the like to form small emulsion drops in the form of oil-in-water, then the added acetyl hexapeptide-8 is adsorbed on the outer sides of the emulsion drops, when the emulsion drops are broken during use, a protective film is formed on the surface of the skin by the inner oil phase components, so that the acetyl hexapeptide-8 and tetrahydropiperine are locked, and the absorption of the acetyl hexapeptide-8 by the skin is promoted.
In the experimental process, the applicant finds that if the A phase raw material is not prepared into the mixed solution firstly and then added into the B phase raw material, but the A phase raw material is directly added into the B phase raw material, a complete emulsion drop structure cannot be formed, tetrahydropiperine can exist in the water phase, the interaction between the tetrahydropiperine and the acetyl hexapeptide-8 is reduced, and the permeation effect is reduced.
In a preferred embodiment, the homogenizing pressure in step (1) is 600-800bar and the number of homogenizing times is 3-6.
In a preferred embodiment, the homogenization pressure in step (1) is 750bar and the number of homogenization is 4.
In a preferred embodiment, the phase a feedstock in step (1) is heated to 70 ℃ with mixing; and (3) cooling the phase A mixed solution in the step (1) to 40 ℃.
In a preferred embodiment, the homogenizing speed in step (2) is 3000rpm/min.
In a third aspect, the present invention provides the use of a high-efficiency penetrating microemulsion for facial, neck and hand care.
Compared with the prior art, the invention has the beneficial effects that:
1. the emulsion prepared by the invention improves the agglomeration and contact degree of raw materials such as tetrahydropiperine, acetyl hexapeptide-8, squalane, cetyl potassium phosphate and the like through a specific preparation method, improves the permeation effect in the use process of the emulsion, and improves the wrinkle removing capability of the emulsion.
2. The emulsion prepared by the invention is added with tetrahydropiperine as the permeation assisting agent, and the better wrinkle removing effect than the common emulsion is achieved by only 20 percent of the permeation assisting agent in the common emulsion through the specific raw material proportion and the preparation method. The dosage of the permeation assisting agent is reduced, the irritation of the permeation assisting agent to the skin is reduced, and the obtained emulsion is milder and has no irritation to the skin.
Detailed Description
Example 1
The first aspect of the invention provides a high-efficiency permeable microemulsion, which comprises a raw material including a phase A and a phase B, wherein the total mass of the phase A and the phase B is 100 parts by weight, and the raw material of the phase A comprises the following components in parts by weight: 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of cetyl phosphate potassium, 0.01 part of tetrahydropiperine and 1.5 parts of deionized water; the phase B raw materials comprise the following components in parts by weight: comprises acetyl hexapeptide-85 parts, 1, 3-butanediol 5 parts, sodium hyaluronate 0.05 parts, sodium polyacrylate 0.5 parts, EDTA-2Na0.05 parts, phenoxyethanol 0.5 parts and deionized water for supplementing the balance.
The mass concentration of the acetyl hexapeptide-8 is 1000ppm, and the acetyl hexapeptide-8 is purchased from Nanjing Sibiraea Biochemical industry Co.
The tetrahydropiperine is purchased from sabina corporation, usa.
The sodium polyacrylate is purchased from basf, germany.
The sodium hyaluronate was purchased from Shandong focus Biotechnology Inc. and had a molecular weight of 80w.
The second aspect of the invention provides a method for preparing a high-efficiency permeable microemulsion, which comprises the following steps:
(1) Mixing and heating the phase A raw materials to 70 ℃, treating by a homogenizer under the homogenizing pressure of 750bar for 4C times, homogenizing until the particle size is 200nm, and cooling to 40 ℃ to obtain phase A mixed solution;
(2) Premixing sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, uniformly stirring deionized water and EDTA-2Na, adding the premixed sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, stirring for 10min, uniformly stirring, adding the phase A mixed solution, homogenizing at 3000rpm for 5 min, finally adding phenoxyethanol and acetyl hexapeptide-8, stirring for 10min, and uniformly stirring to obtain the final product.
In a third aspect, the present invention provides the use of a high-efficiency penetrating microemulsion for facial, neck and hand care.
Example 2
The first aspect of the invention provides a high-efficiency permeable microemulsion, which comprises a raw material including a phase A and a phase B, wherein the total mass of the phase A and the phase B is 100 parts by weight, and the raw material of the phase A comprises the following components in parts by weight: 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of cetyl phosphate potassium, 0.01 part of tetrahydropiperine and 1.5 parts of deionized water; the phase B raw materials comprise the following components in parts by weight: comprises acetyl hexapeptide-85 parts, 1, 3-butanediol 5 parts, sodium hyaluronate 0.05 parts, sodium polyacrylate 0.5 parts, EDTA-2Na0.05 parts, phenoxyethanol 0.5 parts and deionized water for supplementing the balance.
The mass concentration of the acetyl hexapeptide-8 is 1000ppm, and the acetyl hexapeptide-8 is purchased from Nanjing Sibiraea Biochemical industry Co.
The tetrahydropiperine is purchased from sabina corporation, usa.
The sodium polyacrylate is purchased from basf, germany.
The sodium hyaluronate was purchased from Shandong focus Biotechnology Inc. and had a molecular weight of 80w. The second aspect of the invention provides a method for preparing a high-efficiency permeable microemulsion, which comprises the following steps:
premixing sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, uniformly stirring deionized water and EDTA-2Na, adding the premixed sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, stirring for 10min, uniformly stirring, adding all the raw materials in the phase A, homogenizing at 3000rpm for 5 min, finally adding phenoxyethanol and acetyl hexapeptide-8, stirring for 10min, and uniformly stirring to obtain the final product.
In a third aspect, the present invention provides the use of a high-efficiency penetrating microemulsion for facial, neck and hand care.
Example 3
The first aspect of the invention provides a high-efficiency permeable microemulsion, which comprises a raw material including a phase A and a phase B, wherein the total mass of the phase A and the phase B is 100 parts by weight, and the raw material of the phase A comprises the following components in parts by weight: 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of cetyl phosphate potassium, 0.05 part of tetrahydropiperine and 1.5 parts of deionized water; the phase B raw materials comprise the following components in parts by weight: comprises acetyl hexapeptide-85 parts, 1, 3-butanediol 5 parts, sodium hyaluronate 0.05 parts, sodium polyacrylate 0.5 parts, EDTA-2Na0.05 parts, phenoxyethanol 0.5 parts and deionized water for supplementing the balance.
The mass concentration of the acetyl hexapeptide-8 is 1000ppm, and the acetyl hexapeptide-8 is purchased from Nanjing Sibiraea Biochemical industry Co.
The tetrahydropiperine is purchased from sabina corporation, usa.
The sodium polyacrylate is purchased from basf, germany.
The sodium hyaluronate was purchased from Shandong focus Biotechnology Inc. and had a molecular weight of 80w.
The second aspect of the invention provides a method for preparing a high-efficiency permeable microemulsion, which comprises the following steps:
premixing sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, uniformly stirring deionized water and EDTA-2Na, adding the premixed sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, stirring for 10min, uniformly stirring, adding all the raw materials in the phase A, homogenizing at 3000rpm for 5 min, finally adding phenoxyethanol and acetyl hexapeptide-8, stirring for 10min, and uniformly stirring to obtain the final product.
In a third aspect, the present invention provides the use of a high-efficiency penetrating microemulsion for facial, neck and hand care.
Performance testing
The emulsion prepared in the example was subjected to a wrinkle-removing efficacy test.
30 volunteers were selected for 28 days of wrinkle removal efficacy test. The volunteers were 18-60 years old, and 3 groups of 10 volunteers each were randomized. Each panel tested the emulsion prepared in the different examples. Each volunteer used twice daily for four weeks continuously, cleaned the face before each trial, and rested for at least 30min after using the emulsion without drinking water, keeping the face relaxed. Wrinkle score tests were performed with a Visia 7 facial image analyzer on day 0, day 7, day 14, day 21, and day 28, respectively. The higher the score of the wrinkles, the more wrinkles in the skin and the worse the condition of the wrinkles. The wrinkle scores are recorded in Table 1
TABLE 1
For 7 days | 14 days | 21 days | For 28 days | |
Example 1 | -7.23% | -12.43% | -16.03% | -18.59% |
Example 2 | -3.64% | -8.33% | -12.26% | -14.72% |
Example 3 | -5.33% | -10.92% | -14.68% | -17.78% |
The test results show that the emulsion of example 1 has a better wrinkle-removing effect than the emulsion of example 2. The emulsion of example 3 showed slightly weaker wrinkle-removing effect than the emulsion of example 1. And according to the use evaluation of volunteers, the emulsion of example 3 had a phenomenon that 4 volunteers had skin heat after use, and 2 volunteers had a phenomenon that skin was reddish, and neither the emulsion of example 1 nor the emulsion of example 2 had adverse phenomena.
Claims (3)
1. A high-efficient permeable microemulsion is characterized in that the preparation raw material comprises an A phase containing a permeation assisting agent and a B phase containing polypeptide active substances;
the permeation aid in the phase A is selected from tetrahydropiperine;
the mass sum of the phase A and the phase B is 100 parts by weight;
the phase A raw material comprises, by weight, 0.1-0.8 part of polyglycerol ester emulsifier, 5-10 parts of glycerol, 1.5-3.5 parts of squalane, 0.01-0.1 part of cetyl phosphate potassium, 0.01-0.1 part of permeation aid and 1-5 parts of deionized water; the phase B raw material comprises 5 parts by weight of polypeptide active substances, 5-10 parts by weight of butanediol, 0.01-0.08 part by weight of sodium hyaluronate, 0.2-0.6 part by weight of sodium polyacrylate, 0.05 part by weight of EDTA-2Na, 0.03-0.5 part by weight of preservative and the balance of deionized water;
the polypeptide active substance in the phase B is acetyl hexapeptide-8;
the preparation method of the high-efficiency permeable microemulsion is characterized by comprising the following steps of:
(1) Mixing and heating the raw materials in the phase A, homogenizing by a homogenizer until the particle size is 150-200nm, and cooling to obtain phase A mixed solution;
(2) And (3) after uniformly mixing the phase B, adding the phase A mixed solution, and homogenizing to obtain the high-efficiency permeable microemulsion.
2. The high-efficiency penetration microemulsion of claim 1, wherein the detailed steps of step (2) are as follows: premixing sodium polyacrylate, butanediol and sodium hyaluronate, stirring deionized water and EDTA-2Na, adding the premixed sodium polyacrylate, butanediol and sodium hyaluronate, stirring, adding phase A mixed solution, homogenizing, adding antiseptic and polypeptide active substance, and stirring.
3. Use of a high-efficiency penetrating microemulsion according to any one of claims 1-2, wherein said microemulsion is applied for facial care, neck care, hand care.
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