CN109966202A - Purposes of the precious Rogor in Transdermal absorption - Google Patents

Purposes of the precious Rogor in Transdermal absorption Download PDF

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Publication number
CN109966202A
CN109966202A CN201910242076.8A CN201910242076A CN109966202A CN 109966202 A CN109966202 A CN 109966202A CN 201910242076 A CN201910242076 A CN 201910242076A CN 109966202 A CN109966202 A CN 109966202A
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purposes
rogor
precious rogor
skin
precious
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焦红
刘博�
潘滔
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Guangzhou Boroho Biotechnology Co Ltd
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Guangzhou Boroho Biotechnology Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60Sugars; Derivatives thereof
    • A61K8/602Glycosides, e.g. rutin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783Angiosperms [Magnoliophyta]
    • A61K8/9789Magnoliopsida [dicotyledons]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00Preparations for care of the skin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/10General cosmetic use

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Birds (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Botany (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Cosmetics (AREA)

Abstract

The present invention relates to a kind of new applications of substance to belong to skin-protection type cosmetic technical field more particularly, to purposes of the precious Rogor in percutaneously experiment Transdermal absorption.The present invention also provides purposes of the precious Rogor in the skin care item for Transdermal absorption.Precious Rogor of the invention has the effect of Transdermal absorption, and active constituent penetrates keratoderma, penetrates into deep skin and participates in metabolism and plays efficacy effect, can be used to prepare efficacy effect can transdermal absorption skin-protection type cosmetics.

Description

Purposes of the precious Rogor in Transdermal absorption
Technical field
The present invention relates to purposes of the precious Rogor in percutaneous Transdermal absorption, belong to the cosmetic technical field of skin care.
Background technique
Precious Rogor (Borojoa sorbilis Cuter.) is that Rubiaceae woods fruit belongs to plant Borojoa patinoi Cuatrec. with the ripening fruits of Borojoa sorbilis Cuatrec., the torrid zone of Latin America Ecuador weather is originated in Rainforest is in sepia.The local precious Rogor of civil title, which has, eliminates fatigue, and stabilizing blood sugar is horizontal, maintains normal arterial pressure, and enhancing is exempted from Epidemic disease, it is anti-inflammatory and anti-oxidant and other effects.Polysaccharide, protein, potassium, sodium, calcium, phosphorus, iron, magnesium and the water that precious Rogor fruit concentration powder is rich in The substances such as dissolubility B family vitamin play the role of enhancing cell viability;The linoleic acid and Asia that precious Rogor cannot also be synthesized containing human body Numb acid, can be used as the important substance for maintaining cell membrane flow, be conducive to the enzymatic reaction of cell membrane, while to reduction lipid peroxy Change plays the role of positive.Sesquiterpenoids (iridoid glycoside), Polyphenols and the VE that powder is rich in is concentrated in precious Rogor fruit The one of the major reasons that its antioxidation generates.The precious Rogor fruit concentration middle and high dosage group of powder can significantly improve mice serum With SOD in liver, reduction MDA content;Precious Rogor fruit concentration powder high dose group can significantly improve mouse aging serum and GSH-Px vigor in liver.Currently, there is not yet document makees in-depth study to the transdermal situation of precious Rogor.
Skin is the human body barriers for the natural resistance foreign substance invasion that the mankind have, and having has specific protective to skin Energy, good transdermal effect, transdermal dosage compositions appropriate and effect are the basic conditions of effect skin-protection type cosmetics.In percutaneous dosing In the exploitation of system, it is drug, percutaneously through sorbefacient and high molecular material etc. that the research of drug transdermal rate, which is crucial, The foundation of prescription screening.The main method that percutaneous drug administration preparation In vitro penetration test reported in the literature uses at present is to expand Dissipate pond method.The method is after isolated skin is removed subcutaneous fat, to be cut into suitable size and be clipped in diffusion cell, and isolated skin will be spread Pond is isolated into supply chamber and receiving chamber, and for cuticula towards supply chamber, skin corium makes the acceptable solution in acceptance pool towards receiving chamber Just it is contacted with skin corium.Medicinal application is close to cuticula in supply chamber, then takes connecing for certain volume at the time point of setting Concentration of the different time points drug in acceptable solution is analyzed by liquid, to analyze the percutaneous absorbtion situation of drug.Application at present In In vitro penetration test diffusion cell be mainly modified form franz diffusion cell (also referred to as Keshary-Chien diffusion cell), by Using simplicity and there is good application in the pond K-C, become in the research of percutaneous drug administration preparation In vitro penetration most often Instrument.Human skin is the optimum skin of In vitro penetration test, but more difficult acquisition, therefore document report at home at present In, In vitro penetration research skin used largely comes from healthy rat, mouse and rabbit etc..In the selection of receiving liquid On, it is largely water in blood of human body, only substances such as fraction electrolyte and protein.Ideal acceptable solution should be leaked meeting As close possible to human skin microenvironment on the basis of groove bar part.At present the common acceptable solution in home and abroad have physiological saline (NS), Ringer's solution, isotonic phosphate buffer liquid (IPBS).
Percutaneous penetration is the important method for investigating drugs through skin, is to guarantee curative effect and weight stable and controllable for quality Means are wanted, present inventor selects rat skin as medium, and physiological saline is receiving liquid, with modified form Frans diffusion cell Method carries out the transdermal experiment containing precious Rogor skin care item, with activity specific substance treasured Rogor 8,9- iridoid glycoside in precious Rogor It is protected as reference marker with the transdermal release amount of UPLC-MS/MS method detection active matter percutaneous absorbtion to study precious Rogor The transdermal situation of skin product.
Summary of the invention
It is an object of the invention to overcome the shortcomings of that above-mentioned existing skin care item technology cannot play efficacy effect through skin Place and purposes of the precious Rogor in Transdermal absorption is provided.
To achieve the above object, the technical scheme adopted by the invention is as follows: purposes of the precious Rogor in Transdermal absorption.
As the preferred embodiment of purposes of the present invention, transdermal experiment and its active matter of the precious Rogor in skin care item The purposes of percutaneous absorbtion.
As the preferred embodiment of purposes of the present invention, the Transdermal absorption refers to that the active constituent in precious Rogor is saturating Keratoderma is crossed, deep skin is penetrated into and participates in skin metabolism and play efficacy effect.
As the preferred embodiment of purposes of the present invention, the significant active constituent is precious Rogor 8,9- cyclenes ether Terpene glycosides.
Second aspect, the present invention provides purposes of the precious Rogor in the skin-protection type cosmetics for transdermal absorption.
As the preferred embodiment of purposes of the present invention, the Transdermal absorption refers to that the active constituent of precious Rogor penetrates Keratoderma penetrates into deep skin and plays efficacy effect.
As the preferred embodiment of purposes of the present invention, the significant active constituent is precious Rogor 8,9- cyclenes ether Terpene glycosides.
As the preferred embodiment of purposes of the present invention, the cosmetics are sunscreen, suncream, sun water, essence Magnificent liquid, toner, facial mask, eye cream, face cream or lotion.The cosmetics are generally resident skin care item.
As the preferred embodiment of purposes of the present invention, the dosage form of the cosmetics is aqua, emulsion, paste, powder Agent or creme.
As the preferred embodiment of purposes of the present invention, mass percentage of the treasured Rogor powder in cosmetics It is 0.01~5%.
As the preferred embodiment of purposes of the present invention, the transdermal effect of the treasured Rogor is the same as Rogor precious in skin care item The amount of addition is in dose-effect relationship.That is: the amount that precious Rogor is added in skin care item is more, through the precious Rogor -8 in subcutaneous mucus, The amount of 9- iridoid glycoside is just more;On the contrary, the amount for adding precious Rogor in skin care item is few, through the precious Rogor -8 in subcutaneous mucus, The amount of 9- iridoid glycoside is just few.Precious Rogor 8,9- iridoid glycoside can penetrate into deep skin in a short time and play drug effect, and It can continue for 24 hours in subcutaneous action time.
Compared with prior art, the invention has the benefit that precious Rogor of the invention has the effect of Transdermal absorption, Active constituent can penetrate keratoderma, penetrate into deep skin and play efficacy effect, can be used to prepare the skin care of transdermal absorption Type cosmetics.
Detailed description of the invention
Fig. 1 is in vitro transdermal test device figure;Wherein, A is vitro penetration instrument figure, and B is Franz diffusion cell figure;
Fig. 2 is the penetration curve figure of 8,9- iridoid glycoside in the sample;Wherein, 8 A, 9- iridoid glycoside are happy in treasured Penetration curve figure in fruit sunscreen, B 8, penetration curve figure of the 9- iridoid glycoside in precious Rogor whitening essence cream, C are Penetration curve figure of 8, the 9- iridoid glycosides in precious Rogor maintenance sleep mask, D 8,9- iridoid glycoside are soft in precious Rogor Penetration curve figure in skin water.
Specific embodiment
Purposes, technical schemes and advantages in order to better illustrate the present invention, below in conjunction with the drawings and specific embodiments pair The present invention is described further.It should be pointed out that the component content for the skin care item used in embodiment, those skilled in the art It can according to need carry out conventional selection, the application only studies the Transdermal absorption effect of precious Rogor.
The effect test of the precious Rogor Transdermal absorption of embodiment 1
1, test material
(1) test sample material
The present embodiment is with precious Rogor active material 8, and 9- iridoid glycoside is as marker, to the cosmetics without precious Rogor Matrix, precious Rogor sunscreen, precious Rogor whitening essence cream, precious Rogor maintenance sleep mask, the Transdermal absorption of precious Rogor smoothing toner Effect is tested.Each test sample relevant information is as shown in table 1, and the result in table 1 represents what groups of animals use was accordingly formulated After skin care item, the amount of contained active matter index in subcutaneous mucus.
Table 1
Each test sample at be grouped as and the preparation method is as follows:
Cosmetic base:
Water, glycerol, Phenylbenzimidazolesulfonic acid, magnesium sulfate, dipotassium glycyrrhizinate, titanium dioxide/aluminium hydroxide/zinc oxide/ Triethoxy octyl silane, Polydimethylsiloxane PEG-10/15 Crosslinked Polymer/dimethyl silicone polymer, etc..
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;Raw material is added respectively Enter in agitated kettle, stirs;Vacuum is opened, material in agitated kettle is pumped into vacuum emulsification pot, mixing is stirred evenly Raw material in pot, emulsifying stir after 2~3 minutes, and constant temperature stirring defoaming cools down after ten minutes.To standard specimen qualification mistake The discharging of 100 mesh, it is filling after detection is qualified;It is inspected by random samples again after filling, detects qualified storage.
Precious Rogor sunscreen:
At being grouped as: water, glycerol, Phenylbenzimidazolesulfonic acid, arginine, magnesium sulfate, dipotassium glycyrrhizinate, hyaluronic acid Sodium, titanium dioxide/aluminium hydroxide/triethoxy octyl silane, ethylhexyl methoxy cinnamate, octyl polymethyl siloxane, Ring five dimethyl silicone polymer, butyl octanol salicylate, ethylhexyl salicylate, zinc oxide/triethoxy octyl silane gather Dimethyl siloxane PEG-10/15 cross-linked polymer/dimethyl silicone polymer, two octanoic acids of butanediol/dicaprate, ring five poly- two Methylsiloxane/Dimethicone/Vinyl Dimethicone cross-linked polymer, ring five dimethyl silicone polymer/ Distearyl dimethylammonium hectorite/propylene glycol carbonate, bis-ethylhexoxyphenol methoxyphenyl triazine, poly-methyl methacrylate Ester, acrylic acid (ester) class/polydimethylsiloxanecopolymer copolymer/ring five dimethyl silicone polymer, PEG-10 Polydimethylsiloxane, Polymethylsilsesquioxane, trimethyl silicane alkoxy esters of silicon acis, bismuth oxychloride, HDI/ trihydroxy methyl hexyl lactone cross-linked polymeric Object/silica, poly- hydroxy stearic acid, dimetylsilyl SiClx stone, precious Rogor fruit juice, -1/ fucose of biological carbohydrate gum/water, water/ Purslane (PORTULACA OLERACEA) extract/butanediol, Phenoxyethanol/Sensiva SC50, water/xylitol/dehydration Xylitol/Xylitol-based glucoside, 3-o- ethylascorbyl.
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;Raw material is added respectively Enter in agitated kettle, after stirring is warming up to 80~85 DEG C, stir, keeps the temperature spare;Vacuum is opened, by material in agitated kettle It is pumped into vacuum emulsification pot, stirs evenly raw material in mixing kettle, emulsifying stirs after 2~3 minutes, constant temperature stirring Defoaming cools down after ten minutes;When being cooled to 45 DEG C or less, the precious Rogor fruit juice being pre-dissolved in advance is added by 0.5~5% allocation ratio (precious Rogor juice first uses dissolved in purified water at liquid before addition, according to the content in total system, is then then added to system In), it discharges, stand after stirring;The discharging of 100 mesh is crossed to standard specimen qualification, it is filling after detection is qualified;It is taken out again after filling Inspection detects qualified storage.
Precious Rogor whitening essence cream:
At being grouped as: water, dipropylene glycol, ethoxy urea, erythrite, acrylic acid (ester) class/C10-30 alkylol acrylamide acid esters Cross-linked polymer, carbomer, methyl hydroxybenzoate, Sodium Hyaluronate, panthenol, sodium hydroxide, water/purslane (PORTULACA OLERACEA) extract/butanediol, precious Rogor fruit juice, niacinamide, alpha-arbutin, flavonoids of Glycyrrhiza/dipropylene glycol, PEG-40 Rilanit special, propylene glycol, essence, Cer NS/Natrulon H-10 oleate/butanediol/Phenoxyethanol, water, benzyl alcohol/second Base hexyl glycerol, water/butanediol/Phenoxyethanol, CI 40800.
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;It adds raw materials into and stirs It mixes and is warming up to 85~90 DEG C after stirring in pot, cool down within insulated and stirred 15~30 minutes;Discharge after stirring, It stands;Hereinafter, the precious Rogor fruit juice being pre-dissolved is added by 0.2~3% allocation ratio in advance when being cooled to 45 DEG C, stir It discharges, stand afterwards;After the assay was approved, filling, packaging, coding, storage.
Precious Rogor smoothing toner:
At being grouped as: water, propylene glycol, dipropylene glycol, erythrite, panthenol, precious Rogor fruit juice, isononanoic acid ethylhexyl, third Olefin(e) acid (ester) analog copolymer sodium, Nexbase 2004, PPG-1 tridecanol polyethers -6, hydrolysis glycosaminoglycan, glycerol, acrylic acid/ MA copolymer sodium, butanediol, pungent glycol, 1,6-HD, EDETATE SODIUM, acrylic acid (ester) class/C10-30 alkylol acrylamide acid esters Cross-linked polymer, triethanolamine, golden yellow chamomile (CHRYSANTHELLUM INDICUM) extract, Sodium Hyaluronate, oat (AVENA SATIVA) benevolence extract, tremella (TREMELLA FUCIFORMIS) extract turn round thorn cactus (OPUNTIA STREPTACANTHA) stem extraction, hexylene glycol, Caesalpinia spinosaKuntze (CAESALPINIA SPINOSA) glue, potassium sorbate, benzyl alcohol, Sensiva SC50, methyl hydroxybenzoate, Phenoxyethanol, essence, CI40800.
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;It adds raw materials into true It in empty emulsion pot, after stirring is warming up to 80~85 DEG C, stirs, keeps the temperature spare;The precious Rogor fruit being pre-dissolved in advance is added Juice presses 0.01~0.5% allocation ratio, opens vacuum, and emulsifying stirs after 5~8 minutes, constant temperature stirring defoaming Cool down after ten minutes;It when being cooled to 45 DEG C or less, discharges, stand after stirring;The discharging of 100 mesh is crossed to standard specimen qualification, It is filling after detection is qualified;It is inspected by random samples again after filling, detects qualified storage.
Precious Rogor maintenance sleep mask:
At being grouped as: water, glycerol, propylene glycol, erythrite, ethoxy urea, polyacrylate cross-linked polymer -6, ripple angle Pitch dish (CHONDRUS CRISPUS) extract, butanediol, multiflora rose (ROSA MULTIFLORA) fruit oil, tocopherol acetate, Hydroxy-ethyl acrylate/sodium acryloyldimethyl taurate copolymers, triethanolamine, carbomer, cetearyl glucoside, sorb Smooth stearate, stearine, cetostearyl alcohol, acrylic acid (ester) analog copolymer sodium, Nexbase 2004, PPG-1 13 Alcohol polyethers -6, precious Rogor) fruit juice, acrylic acid (ester) class/C10-30 alkylol acrylamide acid esters cross-linked polymer, allantoin, acrylic acid/ MA copolymer sodium, pungent glycol, 1,6-HD, pyrenomycetes (SCLEROTIUM ROLFSSII) glue, Sodium Hyaluronate, oat (AVENA SATIVA) benevolence extract, tremella (TREMELLA FUCIFORMIS) extract turn round thorn cactus (OPUNTIA STREPTACANTHA) stem extraction, hexylene glycol, benzyl alcohol, Sensiva SC50, methyl hydroxybenzoate, Phenoxyethanol, essence, CI 40800。
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;It adds raw materials into true It in empty emulsion pot, after stirring is warming up to 80~85 DEG C, stirs, keeps the temperature spare;The precious Rogor fruit being pre-dissolved in advance is added Juice presses 0.1~2% allocation ratio, opens vacuum, and emulsifying stirs after 5~8 minutes, and 10 points of defoaming of constant temperature stirring Cool down after clock;It when being cooled to 45 DEG C or less, discharges, stand after stirring;The discharging of 100 mesh, detection are crossed to standard specimen qualification It is filling after qualification;It is inspected by random samples again after filling, detects qualified storage.
(2) instrument
Ultra high efficiency liquid phase tandem mass spectrum (UPLC-MS/MS, U.S. Waters, XEVO TQ-S, quaternary pump);ACQUICTY UPLC HSS T3 chromatographic column (2.1 × 100mm, 1.8 μm);5804R type refrigerated centrifuge (German Eppendorf company);Analysis Balance (model: BT-125D);The intelligent transdermal diffusion apparatus of TP-6 (Tianjin Jing Tuo instrument Science and Technology Ltd.).
(3) drug and reagent
8,9- iridoid glycoside reference substances (self-control), apiolin standard items (National Institute for Food and Drugs Control, purity >= 99%, lot number: 111901-201603);Acetonitrile, methanol, formic acid (chromatographic grade, Moke Stock Limited Partnership, 4L);Ultrapure water is (silent Ke Milibo Co., Ltd, ELIX ultrapure water system).
(4) animal
SPF grades male SD rat 15, weight (250 ± 20) g is provided by Guangdong Medical Lab Animal Center, qualified Card SCXK (Guangdong) 2013-0002;Raising and experimental implementation, humidity (40%~70%), temperature are in the laboratory SPF (20 DEG C~24 DEG C).All experimental implementations are carried out according to the requirement of the Guangdong Provincial TCM Hospital animal welfare committee.
2, test method
After SD rat anesthesia, belly shaving removes skin of abdomen, rejects subcutaneous fat, carries out penetrating absorption immediately.Receive Physiological saline is added in room, and each 1g of sample described in table 1 is added in supply chamber, then preservative film is covered on supply chamber, in vitro transdermal test The skin handled well as shown in Figure 1, is placed between receiving chamber and supply chamber that (transdermal area is 3.14cm by device2, receiving chamber appearance Product is 15ml, and experimental temperature remains 37 ± 0.5 DEG C, and mixing speed is 300 ± 10r/min).Respectively at 1,2,4,6,8,10, 12,1mL is sampled from receiving liquid for 24 hours, while supplementing the receiving liquid of same volume, obtained sample takes out 400 μ L in EP pipe, And 100 μ L apiolin inner mark solutions are added, vortex 3min, 14000rpm are centrifuged 30min, and taking supernatant, sample introduction is analyzed, calculates activity Object: the content of precious Rogor 8,9- iridoid glycoside.
3, test result
According to 1 unit of account area Percutaneous permeability of formula:
C in formula 1nFor the corrected concentrations of n-th of sample point drug;
CiIt is the drug concentration that i-th of sample point measures;
VnAnd ViIt is the volume (15mL) and sample volume (1mL) of reception tank respectively;
A is the diffusion area (A=3.14cm of diffusion cell2)。
It is mapped with Qn to time t, and to the straight line portion linear regression in curve, obtains straight slope That is steady-state permeation rate Js (μ gcm-2·h-1).Linear intercept is lag time tlag, (Cd is infiltration coefficient (P)=Js/Cd The mass concentration of drug in test solution).
Precious Rogor 8, the permeability parameters of 9- iridoid glycoside in the sample are as shown in table 1, and penetration curve is as shown in Figure 2.
Table 1
By table 1 and Fig. 2 it is found that precious Rogor 8,9- iridoid is not detected in the cosmetic base sample without precious Rogor Glycosides.Steady-state permeation rate (6.37 ± 2.35ng.cm of precious Rogor sunscreen-2.h-1) it is significantly higher than precious Rogor whitening essence cream (3.69±1.01ng.cm-2.h-1), precious Rogor maintenance sleep mask (0.56 ± 0.12ng.cm-2.h-1) and precious Rogor toner (0.32±0.11ng.cm-2.h-1).Four test samples of precious Rogor have Transdermal absorption effect, wherein precious Rogor sunscreen is saturating The amount for crossing keratoderma is most, is higher than other precious Rogor cosmetics.As can be seen that the transdermal effect of precious Rogor is the same as in skin care item The amount of precious Rogor is in dose-effect relationship.That is: the amount that precious Rogor is added in skin care item is more, through the precious Rogor-in subcutaneous mucus The amount of 8,9- iridoid glycoside is just more.It is less used in toner, therefore precious Rogor -8,9- iridoid glycoside in subcutaneous mucus Amount it is just few.Precious Rogor 8,9- iridoid glycoside can penetrate into deep skin in a short time and play drug effect, and, in subcutaneous effect Time can continue for 24 hours.
Embodiment 2
1, test material
(1) test sample material
The present embodiment is using precious Rogor active material iridoid glycoside as marker, to the antiallergic essence used without precious Rogor Magnificent liquid, positive anti-allergic essence control, the anti-allergic essence containing precious Rogor, the anti-allergic essence containing precious Rogor and masculine principle Four groups of animals carry out Transdermal absorption measure of merit.Each test sample at be grouped as and the preparation method is as follows:
Anti-allergic essence without precious Rogor:
Water, glycerol, Phenylbenzimidazolesulfonic acid, magnesium sulfate, dipotassium glycyrrhizinate, titanium dioxide/aluminium hydroxide/zinc oxide/ Triethoxy octyl silane, Polydimethylsiloxane PEG-10/15 Crosslinked Polymer/dimethyl silicone polymer, etc..
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;Raw material is added respectively Enter in agitated kettle, stirs;Vacuum is opened, material in agitated kettle is pumped into vacuum emulsification pot, mixing is stirred evenly Raw material in pot, emulsifying stir after 2~3 minutes, and constant temperature stirring defoaming cools down after ten minutes.To standard specimen qualification mistake The discharging of 100 mesh, it is filling after detection is qualified;It is inspected by random samples again after filling, detects qualified storage.
Anti-allergic essence positive control:
Water, glycerol, Phenylbenzimidazolesulfonic acid, magnesium sulfate, dipotassium glycyrrhizinate, titanium dioxide/aluminium hydroxide/zinc oxide/ Triethoxy octyl silane, Polydimethylsiloxane PEG-10/15 Crosslinked Polymer/dimethyl silicone polymer, 4-aminopyridine 0.02% (positive control): etc..
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;Raw material is added respectively Enter in agitated kettle, stirs;Vacuum is opened, material in agitated kettle is pumped into vacuum emulsification pot, mixing is stirred evenly Raw material in pot, emulsifying stir after 2~3 minutes, and constant temperature stirring defoaming cools down after ten minutes.To standard specimen qualification mistake The discharging of 100 mesh, it is filling after detection is qualified;It is inspected by random samples again after filling, detects qualified storage.
Anti-allergic essence containing precious Rogor:
Water, glycerol, Phenylbenzimidazolesulfonic acid, magnesium sulfate, dipotassium glycyrrhizinate, titanium dioxide/aluminium hydroxide/zinc oxide/ Triethoxy octyl silane, Polydimethylsiloxane PEG-10/15 Crosslinked Polymer/dimethyl silicone polymer, precious Rogor powder 2%, etc..
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;Raw material is added respectively Enter in agitated kettle, stir, when temperature drops to 40 DEG C, precious Rogor powder is added, stirs evenly.Vacuum is opened, it will Material is pumped into vacuum emulsification pot in agitated kettle, stirs evenly raw material in mixing kettle, emulsifying is sufficiently stirred after 2~3 minutes Uniformly, constant temperature stirring defoaming cools down after ten minutes.The discharging of 100 mesh is crossed to standard specimen qualification, it is filling after detection is qualified;It is taken out again after filling Inspection detects qualified storage.
Anti-allergic essence containing precious Rogor and masculine principle:
Water, glycerol, Phenylbenzimidazolesulfonic acid, magnesium sulfate, dipotassium glycyrrhizinate, titanium dioxide/aluminium hydroxide/zinc oxide/ Triethoxy octyl silane, Polydimethylsiloxane PEG-10/15 Crosslinked Polymer/dimethyl silicone polymer, 4-aminopyridine 0.02% (positive control), precious Rogor powder 2%, etc..
Preparation method: various raw materials in precise formula are held with vessel that are clean and disinfecting;Raw material is added respectively Enter in agitated kettle, stir, when temperature drops to 40 DEG C, precious Rogor powder is added, stirs evenly.Vacuum is opened, it will Material is pumped into vacuum emulsification pot in agitated kettle, stirs evenly raw material in mixing kettle, emulsifying is sufficiently stirred after 2~3 minutes Uniformly, constant temperature stirring defoaming cools down after ten minutes.The discharging of 100 mesh is crossed to standard specimen qualification, it is filling after detection is qualified;It is taken out again after filling Inspection detects qualified storage.
Instrument, reagent material
1.1.1 experimental animal SPF grades of KM mouse, 60, half male and half female, by Zhongshan University (university city) Experimental Animal Center It provides, 19.0 ± 1.7g of weight, quality certification number are as follows: SCXK (Guangdong) -2011-0029.
1.1.2 key instrument BSA224S electronic analytical balance (Sai Duolisi scientific instrument (Beijing) Co., Ltd), constant temperature Water-bath (Shanghai precision experimental facilities Co., Ltd), microplate reader Model680 (Bole's life medical product Co., Ltd) are high Fast refrigerated centrifuge KDC-140HR (intermediate range scientific instrument Co., Ltd, section in Anhui), FJ200-S digital display high speed disperser (on This model of seamark factory), CP-8000 shaver Shenzhen Codos Electrical Appliances Co., Ltd., Seriesn170 shaver Germany BRAUN.
1.1.3 drug and reagent
1.1.3.1 test specimen:
1. C13738 cosmetic base;2. C13737 treasured Rogor;3. C13739 masculine principle;4. C13740 treasured Rogor+sun Property ingredient.
1.1.3.2 mouse positive sensitizer
4-aminopyridine: Merck Products, lot number: 54914223.With physiological saline to be made into 0.02% molten using preceding Liquid 0.01mL/g.
1.1.3.3 histamine tests kit
Mouse HIS Elisa kit, the production of the Beijing E-20451 Yong Hui Science and Technology Ltd., lot number: 201306.
2, test method
1.2 method
1.2.1 experimental method
A mouse skin 4-AP cause itches model to itch-threshold influence experiment
Mouse is randomly divided into blank control, matrix group, precious Rogor group, positive controls by weight, positive control+treasured is happy Fruit group.2cm × 3cm area hair is shaved at its back using shaver, is uniformly applied on shaving area skin by test solution, daily 1 Secondary, 100 μ L/ only, continuously smear 7d, blank control group does not give any drug.In the nape of the neck coating position after last dose 40min Subcutaneous injection 4-aminopyridine (physiological saline is made into 0.02%) solution 0.01mL/g, blank control group injecting normal saline. Record each group licks body number in 10min, and calculates response inhabitation rate.
B mouse skin 4-AP cause is itched subcutaneous mucus transdermal experiment after experiment
Cause is itched after experiment, respectively puts to death each group mouse, is opened a kerf at back shaving position, is opened skin surface, is used Syringe extracts subcutaneous mucus to test tube, and cold chain send precision instrument room to do HPLC-MS/MS experiment immediately, tests precious in cutaneous permeable agent The content of -8,9 iridoid glycoside of Rogor.
3, test result
The transmitance difference of precious Rogor -8,9 iridoid glycoside ingredient, polyphenol in each sample is as shown in Table 2,3.
Table 2
Table 3
As shown in Table 2, iridoid is not detected in the anti-allergic essence and anti-allergic essence positive control without precious Rogor Glycosides ingredient, and table ring is detected in the anti-allergic essence containing precious Rogor and the anti-allergic essence containing precious Rogor and masculine principle The Transdermal absorption of alkene ether terpene glycosides;From table 3 it can be seen that anti-allergic essence containing precious Rogor and anti-containing precious Rogor and masculine principle There is also Transdermal absorption effects for polyphenol in quick Essence in precious Rogor nutritional ingredient.
Finally, it should be noted that the above embodiments are merely illustrative of the technical solutions of the present invention rather than protects to the present invention The limitation of range is protected, although the invention is described in detail with reference to the preferred embodiments, those skilled in the art should Understand, it can be with modification or equivalent replacement of the technical solution of the present invention are made, without departing from the essence of technical solution of the present invention And range.

Claims (10)

1. purposes of the precious Rogor in Transdermal absorption.
2. purposes as described in claim 1, which is characterized in that the Transdermal absorption refers to the active constituent of precious Rogor through skin Skin cuticula penetrates into deep skin and participates in metabolism performance efficacy effect.
3. purposes as claimed in claim 2, which is characterized in that the active constituent is precious Rogor 8,9- iridoid glycoside.
4. precious Rogor is for can purposes in the skin-protection type cosmetics of transdermal absorption.
5. purposes as claimed in claim 4, which is characterized in that transdermal absorb refers to that the active constituent of precious Rogor can be thoroughly Keratoderma is crossed, deep skin is penetrated into and participates in metabolism performance efficacy effect.
6. purposes as claimed in claim 5, which is characterized in that the active constituent is precious Rogor 8,9- iridoid glycoside.
7. purposes as claimed in claim 4, which is characterized in that the cosmetics are sunscreen, suncream, sun water, essence Liquid, toner, facial mask, eye cream, face cream or lotion.
8. purposes as claimed in claim 4, which is characterized in that the dosage form of the cosmetics is aqua, emulsion, paste, pulvis Or creme.
9. such as the described in any item purposes of claim 4~8, which is characterized in that quality hundred of the treasured Rogor in cosmetics Dividing content is 0.01~5%.
10. such as the described in any item purposes of claim 4~8, which is characterized in that the same skin care item of transdermal effect of the treasured Rogor The amount of middle treasured Rogor addition is in dose-effect relationship.
CN201910242076.8A 2019-03-27 2019-03-27 Purposes of the precious Rogor in Transdermal absorption Pending CN109966202A (en)

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CN101129300A (en) * 2007-08-16 2008-02-27 峰胜集团有限公司 Anti-dandruff relieve itching hair rinsing lotion composition
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