CN114601746A - 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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- CN114601746A CN114601746A CN202111104592.8A CN202111104592A CN114601746A CN 114601746 A CN114601746 A CN 114601746A CN 202111104592 A CN202111104592 A CN 202111104592A CN 114601746 A CN114601746 A CN 114601746A
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- microemulsion
- deionized water
- butanediol
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- 239000004530 micro-emulsion Substances 0.000 title claims abstract description 32
- 238000002360 preparation method Methods 0.000 title claims abstract description 10
- 238000000593 microemulsion method Methods 0.000 title description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 28
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 27
- 239000008367 deionised water Substances 0.000 claims abstract description 24
- 229910021641 deionized water Inorganic materials 0.000 claims abstract description 24
- 229920002385 Sodium hyaluronate Polymers 0.000 claims abstract description 23
- 229940010747 sodium hyaluronate Drugs 0.000 claims abstract description 23
- 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 23
- 229920001495 poly(sodium acrylate) polymer Polymers 0.000 claims abstract description 22
- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 claims abstract description 22
- 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 22
- 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 21
- 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 11
- RMGVATURDVPNOZ-UHFFFAOYSA-M potassium;hexadecyl hydrogen phosphate Chemical compound [K+].CCCCCCCCCCCCCCCCOP(O)([O-])=O RMGVATURDVPNOZ-UHFFFAOYSA-M 0.000 claims abstract description 11
- 229940032094 squalane Drugs 0.000 claims abstract description 11
- 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 10
- 239000002994 raw material Substances 0.000 claims description 26
- 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
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 claims description 10
- 239000011259 mixed solution Substances 0.000 claims description 10
- 230000003204 osmotic effect Effects 0.000 claims description 10
- 239000013543 active substance Substances 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 9
- 239000003961 penetration enhancing agent Substances 0.000 claims description 9
- 239000003995 emulsifying agent Substances 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 230000001815 facial effect Effects 0.000 claims description 6
- 229920000223 polyglycerol Polymers 0.000 claims description 6
- 239000003755 preservative agent Substances 0.000 claims description 6
- 230000002335 preservative effect Effects 0.000 claims description 6
- 238000002156 mixing Methods 0.000 claims description 5
- 238000001816 cooling Methods 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 3
- 239000002245 particle Substances 0.000 claims description 3
- 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 claims description 2
- 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 claims description 2
- AXTGDCSMTYGJND-UHFFFAOYSA-N 1-dodecylazepan-2-one Chemical compound CCCCCCCCCCCCN1CCCCCC1=O AXTGDCSMTYGJND-UHFFFAOYSA-N 0.000 claims description 2
- 230000002421 anti-septic effect Effects 0.000 claims description 2
- XXJWXESWEXIICW-UHFFFAOYSA-N diethylene glycol monoethyl ether Chemical compound CCOCCOCCO XXJWXESWEXIICW-UHFFFAOYSA-N 0.000 claims description 2
- 229960003639 laurocapram Drugs 0.000 claims description 2
- 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 claims description 2
- 229940094946 palmitoyl tetrapeptide-7 Drugs 0.000 claims description 2
- WCVRQHFDJLLWFE-UHFFFAOYSA-N pentane-1,2-diol Chemical compound CCCC(O)CO WCVRQHFDJLLWFE-UHFFFAOYSA-N 0.000 claims description 2
- 239000000839 emulsion Substances 0.000 abstract description 26
- 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 9
- 230000037303 wrinkles Effects 0.000 abstract description 9
- 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
- 229960005150 glycerol Drugs 0.000 abstract 1
- 230000000638 stimulation Effects 0.000 abstract 1
- 238000012423 maintenance Methods 0.000 description 12
- 239000000126 substance Substances 0.000 description 7
- 238000000265 homogenisation Methods 0.000 description 5
- 239000000047 product Substances 0.000 description 5
- 230000002829 reductive effect Effects 0.000 description 4
- 230000001502 supplementing effect Effects 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 3
- 230000007794 irritation Effects 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 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
- 230000035515 penetration Effects 0.000 description 2
- 230000001737 promoting effect Effects 0.000 description 2
- 230000037331 wrinkle reduction Effects 0.000 description 2
- RJZNPROJTJSYLC-LLINQDLYSA-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(=O)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](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(N)=O RJZNPROJTJSYLC-LLINQDLYSA-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
- 241000196324 Embryophyta Species 0.000 description 1
- 241000758706 Piperaceae Species 0.000 description 1
- 206010037660 Pyrexia Diseases 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
- 230000002776 aggregation Effects 0.000 description 1
- 238000004220 aggregation Methods 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
- 230000003247 decreasing effect Effects 0.000 description 1
- POULHZVOKOAJMA-UHFFFAOYSA-M dodecanoate Chemical compound CCCCCCCCCCCC([O-])=O POULHZVOKOAJMA-UHFFFAOYSA-M 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
- 229940070765 laurate Drugs 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 239000002357 osmotic agent Substances 0.000 description 1
- 230000037368 penetrate the skin Effects 0.000 description 1
- 230000007903 penetration ability Effects 0.000 description 1
- 239000012466 permeate Substances 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 238000012545 processing Methods 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
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 permeable microemulsion and a preparation method and application thereof, which are characterized in that polyglycerol-10 myristate, glycerol, squalane, potassium cetyl phosphate, tetrahydropiperine and deionized water are homogenized at high pressure, then mixed with the deionized water, 1, 3-butanediol, sodium hyaluronate, sodium polyacrylate and EDTA-2Na, and then acetyl hexapeptide-8 and phenoxyethanol are added to prepare the emulsion. The prepared emulsion is milder, has no stimulation 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 osmotic microemulsion, and a preparation method and application thereof.
Background
The polypeptide active substance has extremely high activity, can promote various functions such as organism regeneration, cell metabolism and the like, and is an important active substance in human bodies. The field of skin care products is usually added with polypeptide active substances to achieve the purpose of reviving the skin vitality.
Chinese patent CN110151597A discloses a polypeptide-containing emulsion, which is prepared by mixing multiple polypeptide substances, adding the mixture into a solution composed of propylene glycol, allantoin and other raw materials, and stirring uniformly. However, the polypeptide substance contained in the product is lack of substance for promoting penetration due to the limitation of the penetration capability of the polypeptide substance, and the polypeptide substance is difficult to penetrate the skin in the using process, thereby reducing the using effect of the emulsion. However, the use of the permeation enhancer in an increased amount damages the skin barrier layer, causes irritation, is not suitable for sensitive muscles, and does not provide satisfactory results when the use amount is decreased.
Based on the above, the application provides the high-efficiency osmotic microemulsion and the preparation method thereof, and the osmotic absorption effect of the polypeptide substance is improved in a mild, safe and healthy manner.
Disclosure of Invention
In the first aspect, the invention provides a high-efficiency osmotic microemulsion, which is prepared from a phase A containing an osmotic agent and a 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, and ethoxydiglycol.
In a preferred embodiment, the penetration enhancer in phase a is tetrahydropiperine.
The tetrahydropiperine is extracted from pepper family plants, is a safe and efficient natural plant extraction permeation-assisting substance, and drives functional active ingredients to permeate into cells by promoting the flow of cell phospholipid bilayers.
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, preservative and deionized water.
In a preferred embodiment, the butanediol is 1, 3-butanediol.
In a preferred embodiment, the polyglycerol ester emulsifier is selected from at least one of polyglycerol-10 myristate, polyglycerol-10 laurate, polyglycerol-10 stearate, polyglycerol-10 eicosadioate, and polyglycerol-10 tetradecadioate.
In a preferred embodiment, the polyglycerol ester emulsifier is polyglycerol-10 myristate.
In a preferred embodiment, the sum of the masses of the phases A and B is 100 parts by weight.
In a preferred embodiment, the phase A raw materials comprise, 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 potassium cetyl phosphate, 0.01-0.1 part of permeation promoter and 1-5 parts of deionized water.
In a preferred embodiment, the phase A raw materials comprise, by weight, 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of potassium cetyl phosphate, 0.01 part of tetrahydropiperine and 1.5 parts of deionized water.
In a preferred embodiment, the phase B raw material comprises, by weight, 5 parts of polypeptide active matter, 5-10 parts of butanediol, 0.01-0.08 part of sodium hyaluronate, 0.2-0.6 part of sodium polyacrylate, 0.05 part of EDTA-2Na0.05 part of preservative, 0.03-0.5 part of deionized water for supplementing the balance.
In a preferred embodiment, the phase B raw materials comprise, by weight, 85 parts of acetyl hexapeptide, 5 parts of butanediol, 0.05 part of sodium hyaluronate, 0.5 part of sodium polyacrylate, 0.05 part of EDTA-2Na, 0.5 part of preservative and the balance of deionized water.
In a preferred embodiment, the preservative is phenoxyethanol.
In a preferred embodiment, the acetyl hexapeptide-8 is purchased from Nanjing Bye Biochemical industries, Inc. at a mass concentration of 1000 ppm.
In a second aspect, the present invention provides a method for preparing a highly permeable microemulsion, comprising 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 a phase A mixed solution;
(2) and after the phase B is uniformly mixed, adding the phase A mixed solution, and homogenizing to obtain the high-efficiency osmotic 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 uniformly, adding premixed sodium polyacrylate, butanediol and sodium hyaluronate, stirring uniformly, adding A-phase mixed solution, homogenizing, adding antiseptic and polypeptide active substance, and stirring uniformly.
In the present application, the applicant found that the penetration ability of the polypeptide active substance can be improved by using specific raw materials and a specific preparation method, an emulsion with good wrinkle removing effect can be obtained, and the dosage of the penetration enhancer is only 20% of the dosage of the common emulsion. In the application, through a specific preparation method, an oil phase component formed by tetrahydropiperine, potassium cetyl phosphate, squalane and the like is added into a water phase formed by 1, 3-butanediol, sodium hyaluronate, deionized water and the like to form a small emulsion drop in an oil-in-water form, then the added acetyl hexapeptide-8 is adsorbed outside the emulsion drop, when the emulsion drop is broken in use, an internal oil phase component forms a layer of protective film on the surface of skin, the acetyl hexapeptide-8 and the tetrahydropiperine are locked, and the absorption of the acetyl hexapeptide-8 by the skin is promoted.
In addition, in the experimental process, the applicant finds that if the phase A raw material is directly added into the phase B raw material instead of being prepared into the mixed solution and then added into the phase B raw material, a complete emulsion drop structure cannot be formed, the tetrahydropiperine exists 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 homogenization pressure in step (1) is 600-800bar, and the number of homogenization times is 3-6.
In a preferred embodiment, the homogenization pressure in step (1) is 750bar and the number of homogenization times is 4.
In a preferred embodiment, the phase A raw material in the step (1) is mixed and heated to 70 ℃; and (2) cooling the A-phase mixed solution to 40 ℃ in the step (1).
In a preferred embodiment, the rotation speed for homogenization in step (2) is 3000 rpm/min.
In a third aspect, the invention provides an application of the microemulsion with high permeation efficiency, wherein the microemulsion is applied to facial maintenance, neck maintenance and hand maintenance.
Compared with the prior art, the invention has the following beneficial effects:
1. according to the emulsion prepared by the invention, through a specific preparation method, the aggregation and contact degrees of the raw materials such as the tetrahydropiperine, the acetyl hexapeptide-8, the squalane, the potassium cetyl phosphate and the like are improved, the permeation effect of the emulsion in the use process is improved, and the wrinkle removing capability of the emulsion is improved.
2. The emulsion prepared by the invention is added with the tetrahydropiperine as the penetration enhancer, and the wrinkle removing effect better than that of the common emulsion is achieved by only using 20 percent of the penetration enhancer in the common emulsion through the specific raw material proportion and the preparation method. And the dosage of the penetration enhancer is reduced, the irritation of the penetration enhancer to the skin is reduced, and the obtained emulsion is milder and has no irritation to the skin.
Detailed Description
Example 1
The invention provides a high-efficiency osmotic microemulsion, which comprises 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 phase A comprises the following raw materials in parts by weight: 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of potassium cetyl phosphate, 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 rest.
The mass concentration of the acetyl hexapeptide-8 is 1000ppm, and the acetyl hexapeptide-8 is purchased from Nanjing Sibaike Biochemical industry Co.
The tetrahydropiperine was purchased from Sabinsa, USA.
The sodium polyacrylate was purchased from basf, germany.
The sodium hyaluronate is purchased from Shandong focus Biotechnology Ltd and has a molecular weight of 80 w.
In a second aspect, the present invention provides a method for preparing a highly permeable microemulsion, comprising the following steps:
(1) mixing the A phase raw materials, heating to 70 deg.C, processing with a homogenizer at homogenizing pressure of 750bar for 4C times, homogenizing until the particle diameter is 200nm, and cooling to 40 deg.C to obtain A phase 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 finished product.
In a third aspect, the invention provides an application of the microemulsion with high permeation efficiency, wherein the microemulsion is applied to facial maintenance, neck maintenance and hand maintenance.
Example 2
The invention provides a high-efficiency osmotic microemulsion, which comprises the following raw materials in parts by weight: 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of potassium cetyl phosphate, 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 rest.
The mass concentration of the acetyl hexapeptide-8 is 1000ppm, and the acetyl hexapeptide-8 is purchased from Nanjing Sibaike Biochemical industry Co.
The tetrahydropiperine was purchased from Sabinsa, USA.
The sodium polyacrylate was purchased from basf, germany.
The sodium hyaluronate is purchased from Shandong focus Biotechnology Ltd and has a molecular weight of 80 w. In a second aspect, the present invention provides a method for preparing a highly permeable microemulsion, comprising 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 phase A, homogenizing at 3000rpm for 5 min, finally adding phenoxyethanol and acetyl hexapeptide-8, stirring for 10min, and uniformly stirring to obtain the finished product.
In a third aspect, the invention provides an application of the microemulsion with high permeation efficiency, wherein the microemulsion is applied to facial maintenance, neck maintenance and hand maintenance.
Example 3
The invention provides a high-efficiency osmotic microemulsion, which comprises 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 phase A comprises the following raw materials in parts by weight: 0.5 part of polyglycerol-10 myristate, 6 parts of glycerol, 2 parts of squalane, 0.05 part of potassium cetyl phosphate, 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 rest.
The mass concentration of the acetyl hexapeptide-8 is 1000ppm, and the acetyl hexapeptide-8 is purchased from Nanjing Sibaike Biochemical industry Co.
The tetrahydropiperine was purchased from Sabinsa, USA.
The sodium polyacrylate was purchased from basf, germany.
The sodium hyaluronate is purchased from Shandong focus Biotechnology Ltd and has a molecular weight of 80 w.
In a second aspect, the present invention provides a method for preparing a highly permeable microemulsion, comprising the following steps:
premixing sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, then uniformly stirring deionized water and EDTA-2Na, adding the premixed sodium polyacrylate, 1, 3-butanediol and sodium hyaluronate, stirring for 10min, after uniformly stirring, adding all the raw materials in phase A, homogenizing for 5 min at 3000rpm, finally adding phenoxyethanol and acetyl hexapeptide-8, stirring for 10min, and uniformly stirring to obtain the finished product.
In a third aspect, the invention provides an application of the microemulsion with high permeation efficiency, wherein the microemulsion is applied to facial maintenance, neck maintenance and hand maintenance.
Performance testing
The emulsions prepared in the examples were subjected to a wrinkle-removing efficacy test.
30 volunteers were selected for a 28-day wrinkle reduction efficacy test. Volunteers aged 18-60 years were randomly stratified into 3 groups of 10 volunteers each. Each panel used the emulsions prepared in the different examples. Each volunteer uses twice a day, continuously uses for four weeks, cleans the face before trying each time, sits still for at least 30min after using the lotion, does not drink water, and keeps the face relaxed. Wrinkle score tests were performed with a Visia 7 facial image analyzer on days 0, 7, 14, 21, and 28, respectively. The higher the wrinkle score, the more wrinkles the skin has, and the worse the wrinkles are. Wrinkle score is reported in Table 1
TABLE 1
| 7 days | 14 days | 21 days | 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 is superior in wrinkle-removing effect to the emulsion of example 2. The emulsion of example 3 was slightly less effective in wrinkle reduction than the emulsion of example 1. According to the use evaluation of the volunteers, 4 volunteers showed a phenomenon of skin fever and 2 volunteers showed a phenomenon of skin reddish after the emulsion of example 3 was used, and neither the emulsion of example 1 nor the emulsion of example 2 showed adverse phenomena.
Claims (10)
1. The efficient osmotic microemulsion is characterized in that the preparation raw materials comprise an A phase containing a permeation promoter and a B phase containing a polypeptide active substance.
2. The highly permeable microemulsion according to claim 1 wherein the permeation enhancer in phase a is selected from at least one of tetrahydropiperine, 1, 2-pentanediol, laurocapram, ethoxydiglycol.
3. The highly permeable microemulsion according to claim 1 wherein the polypeptide actives in phase B are selected from at least one of acetyl hexapeptide-8, acetyl hexapeptide-3, acetyl tetrapeptide-5, palmitoyl tetrapeptide-7, palmitoyl pentapeptide.
4. The highly permeable microemulsion according to claim 1 wherein phase a further comprises polyglycerol ester emulsifier, glycerol, squalane, potassium cetyl phosphate, deionized water; the phase B also comprises butanediol, sodium hyaluronate, sodium polyacrylate, EDTA-2Na, preservative and deionized water.
5. The highly permeable microemulsion according to claim 4 wherein the sum of the masses of phase A and phase B is 100 parts by weight.
6. The highly permeable microemulsion according to claim 4, wherein the phase A raw materials comprise, 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 potassium cetyl phosphate, 0.01-0.1 part of permeation promoter and 1-5 parts of deionized water.
7. The high-permeability microemulsion of claim 4, wherein the phase B raw material comprises, by weight, 5 parts of polypeptide active substances, 5-10 parts of butanediol, 0.01-0.08 part of sodium hyaluronate, 0.2-0.6 part of sodium polyacrylate, 0.05 part of EDTA-2Na, 0.03-0.5 part of preservative, and the balance of deionized water.
8. A method of preparing a highly permeable microemulsion according to any one of claims 4-7, comprising the 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 a phase A mixed solution;
(2) and uniformly mixing the phase B, adding the phase A mixed solution, and homogenizing to obtain the high-efficiency osmotic microemulsion.
9. The method according to claim 8, wherein the detailed steps of the step (2) are as follows: premixing sodium polyacrylate, butanediol and sodium hyaluronate, stirring deionized water and EDTA-2Na uniformly, adding premixed sodium polyacrylate, butanediol and sodium hyaluronate, stirring uniformly, adding A-phase mixed solution, homogenizing, adding antiseptic and polypeptide active substance, and stirring uniformly.
10. Use of a high permeation microemulsion according to any one of claims 1 to 7 for facial, neck and hand care applications.
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