JP2010024180A - Oil-in-water emulsion composition for promoting recovery of skin barrier function - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a preparation promptly recovering skin barrier function which is one of the various functions of the skin and is deteriorated by external stimuli or stresses such as exposure to UV or chemicals or internal factors such as aging. <P>SOLUTION: The oil-in-water emulsion composition for recovering skin barrier function is an emulsion which comprises an oil-soluble component containing ≥70% sterol ester, at least one surfactant and a water-soluble component and has an average particle size of ≤300 nm. The composition comprising at least one chosen from lecithin, polyglyceryl fatty acid ester and ceramide saccharide as the surfactant is particularly effective. <P>COPYRIGHT: (C)2010,JPO&INPIT

Description

  The present invention relates to an oil-in-water emulsion composition used as a cosmetic or pharmaceutical product. More specifically, the present invention relates to an oil-in-water emulsion composition effective for promoting the recovery of skin barrier function.

Although there are various skin functions, one of them has a barrier function, but the skin barrier function is also lowered by internal factors such as ultraviolet rays and chemical external stimuli, stress and aging.
Ceramide, nicotinic acids (see Patent Document 1), glycyrrhizin or its derivatives, asparagus, butcher's bloom extract (see Patent Document 2), and the like are known for recovery of the skin barrier function.
In fields such as cosmetics, sterol esters are used as raw materials. One example is a liquid crystal structure, which is used as a cosmetic product with high aesthetics and high moisture retention. (See Patent Document 3)
JP 11-292765 A JP 2000-053533 A Japanese Patent Laid-Open No. 01-246209

  Although cosmetics already exist for the purpose of restoring the skin barrier function, it is to find a cosmetic having a better ability to restore the skin barrier function.

  An oil-in-water emulsion comprising an oil-soluble component containing 70% or more of a sterol ester, one or more surfactants, and a water-soluble component, and having an average particle size of 300 nm or less, the skin barrier function A preparation with very good recovery ability could be obtained. (In this application, “%” means “% by weight”)

First, the sterol ester used in the present invention is a sterol such as cholesterol, dihydrocholesterol, lanosterol, dihydrolanosterol, desmosterol, stigmasterol, sitosterol, campesterol, brassicasterol, ergosterol, etc. It is an ester with a carboxylic acid which may have an unsaturated branch and may further have a hydroxy group. One or more of these are used.
These sterol esters are blended so as to occupy 70% or more of the oil-soluble component. Other oil-soluble components are not particularly limited.

The surfactant may be any of an anionic surfactant, an amphoteric surfactant, and a nonionic surfactant. However, depending on the type and amount of sterol ester, other oil-soluble components, and types and amounts of water-soluble components, the surfactant may be used. The type and amount are selected, but the nonionic surfactant is mainly selected.
In particular, lecithin, polyglycerin fatty acid ester, and sugar ceramide are preferable from the viewpoint of safety, utilization of natural products, effectiveness on skin, and the like.
Lecithin includes not only lecithin extracted from egg yolk and plants, but also lecithin or hydrogenated product obtained by further purifying these, and lysolecithin.
Polyglycerol fatty acid ester is an ester of polyglycerol having a polymerization degree of glycerin of 5 to 15 and linear, branched, saturated or unsaturated fatty acid having 16 to 22 carbon atoms and having an average esterification degree of 2 or less. Often used.
As the sugar ceramide, galactosylceramide, glucosylceramide, animal sphingolipids containing these, plant sphingolipids and the like are most often used.

The water-soluble component contains water, a polyhydric alcohol, a water-soluble drug, etc., but it is particularly preferable to add a polyhydric alcohol.
Polyhydric alcohols include ethylene glycol, diethylene glycol, triethylene glycol, higher polyethylene glycols, propylene glycol, dipropylene glycol, higher polypropylene glycols, 1,3-butylene glycol, 1,4-butylene glycol, etc. Butylene glycols, glycerol, diglycerol, higher polyglycerols, sugar alcohols such as sorbitol, mannitol, xylitol, maltitol, ethylene oxide of glycerol (hereinafter abbreviated as EO), propylene oxide (hereinafter abbreviated as PO) ) Adducts, sugar alcohols EO, PO adducts, saccharides such as galactose, glucose, fructose and their EO, PO adducts, polysaccharides such as maltose, lactose and their EO, with PO Polyhydric alcohol such as object are exemplified. Among these, glycerin is in accordance with the gist of the present invention and varies depending on various conditions, but 20% or more of the water-soluble components are preferably glycerin.
Since the polyhydric alcohol affects the particle size, the blending amount and type are selected so as to meet the purpose.
Although water can be blended to some extent, it is necessary to make fine particles, so strong emulsification is necessary in the subsequent process, so it is also possible to mix water, water-soluble drugs, water-soluble polymers, etc. after fine particle formation. is there.

  The blending ratio of the oil-soluble component, surfactant, and water-soluble component varies greatly depending on the type and use of the formulation, and the components and amount added after micronization as described below. The amount of the surfactant is preferably 0.01 to 100, and the water-soluble component is preferably 1 to 1000.

These raw materials are emulsified using an emulsifier to an average particle size of 300 nm or less, more preferably 150 nm or less.
Depending on the ingredients, propeller stirrer, homomixer, etc. may be possible, but Manton-Gorin type, Microfluidizer (trade name, manufactured by Microfluidic), Ultimateizer (trade name, manufactured by Tau Technology), It is necessary to use a high-pressure emulsifier such as Nanomizer (trade name, manufactured by Nanomizer).

After emulsification, if necessary, a water-soluble component or an oil-in-water emulsion composition is added and stirred to obtain a necessary preparation.
The water-soluble component or the oil-in-water emulsion composition may contain an oil component, a humectant, a surfactant, vitamins, a pigment, a fragrance, various drugs, water, and the like.

  Examples are olive oil, mink oil, castor oil, palm oil, beef tallow, evening primrose oil, palm oil, castor oil, cacao oil, macadamia nut oil, jojoba oil, beeswax, lanolin, carnauba wax, candelilla wax, lauryl alcohol, Stearyl alcohol, cetyl alcohol, oleyl alcohol, lauric acid, palmitic acid, stearic acid, solid paraffin, squalane, petrolatum, ceresin, microcrystalline wax, butyl stearate, hexyl laurate, diisopropyl adipate, diisopropyl sebacate, octyldodecyl myristate , Isopropyl myristate, isopropyl palmitate isopropyl myristate, cetyl isooctanoate, neopentyl glycol dicaprate, methyl silicone Methyl phenyl silicone, elastin, collagen, triclosan, trichlorocarban, methyl paraben, butyl paraben, deoxyribonucleic acid and its salts, adenylic acid derivatives such as adenosine triphosphate, adenosine diphosphate, adenosine monophosphate and their salts, ribonucleic acid And salts thereof, cyclic AMP, cyclic GMP, flavin adenine nucleotide, guanine, adenine, cytosine, thymine, xanthine and their derivatives caffeine, theophylline, calf blood extract, serum deproteinized extract, spleen extract , Egg components such as birds, poultry extract, fish meat extract, mollusc extract such as squid, royal jelly, silk protein and its degradation product or their derivatives, hemoglobin or its degradation product, lactoferrin or its degradation product, etc. Extracts from animals such as milk, birds, fish, mollusks, crustaceans, shellfish, insects; extracts from microorganisms such as yeast extract, lactic acid bacteria extract, bifidobacteria extract, fermentation metabolites; α- and γ-linolenic acid, eicosapentaenoic acid and derivatives thereof, hormones such as estradiol, etenyl estradiol, glycolic acid, citric acid, lactic acid, malic acid, tartaric acid, succinic acid, glycyrrhizic acid, glycyrrhetinic acid and their Derivatives and their salts, mefenamic acid, phenylbutazone, indomethacin, ibuprofen, ketoprofen, allantoin, guaiazulene, panthenol and their derivatives and their salts, ε-aminocaproic acid, diclofenac sodium, tranexamic acid or antioxidants are vitamins Class A and their induction Bodies and salts thereof, vitamins B and derivatives thereof, and salts thereof, vitamins D and derivatives thereof, and salts thereof, vitamins E and derivatives thereof, and salts thereof, dibutylhydroxytoluene and butylhydroxyanisole, Ferulic acid and caffeic acid, carotenoids, flavonoids, tannins and gallic acid and salts thereof and esters, tocopherol and derivatives thereof, nonyl acid vanillamide, capsaicin, gingerone, cantalis tincture, ictamol, α-borneol, inositol hexa Nicotinate, cyclandrate, cinnarizine, trazoline, acetylcholine, verapamil, cephalanthin, γ-oryzanol, ascorbic acid and derivatives thereof, and salts thereof, N, N′-diacetylsilane Cysteine such as tin dimethyl and its derivatives and salts thereof, grabridine, glabrene, liquiritin, isoliquiritin, placenta extract, hydroquinone and derivatives thereof such as arbutin, resorcin and derivatives thereof, ferulic acid and caffeic acid and derivatives thereof and salts thereof, Glutathione, deciduous extract, licorice extract, chamomile extract, animal and plant extract containing carotenoids, asparagus extract, pea extract, age extract, oxon extract, onionis extract, seaweed extract, Raspberry extract, Kujin extract, Caiquet extract, Gokahi extract, Coffee extract, Rice bran extract, Wheat germ extract, Saisin extract, Hawthorn extract, Sunpens extract, Shirayuri extract, Peonies extract, Sempukuka Extract, soy Extract, tea extract, molasses extract, tomato extract, beechlen extract, beech bud extract, grape extract, flow demanita extract, hop extract, micaika extract, mokka extract, yukinoshita extract And Eucalyptus extract, Yokuinin extract, and Luohan fruit extract. (The polyhydric alcohol and the surfactant are omitted because they are described above.)

  It does not specifically limit as a form of a formulation, For example, arbitrary dosage forms, such as a milky lotion, cream, aqueous solution, a pack, can be selected.

Example 1 Part A by weight
Hydrogenated lecithin 0.500
Glycerin 13.200
1,3-butylene glycol 3.300
B part dihydrocholesteryl oleate 0.761
Cholesteryl nonanoate 0.761
Cholesteryl butyrate 0.453
Dihydrocholesteryl butyrate 0.305
Phytostearyl oleate 0.120
Long-chain branched fatty acid cholesteryl 0.600
Preparation method Part A and part B were dissolved at 85 ° C. with stirring. While adding part B to part A, the mixture was stirred at 5000 rpm for 1 minute with a homogenizer (Model No. TK Robotics, manufactured by Primics).
This was treated once with a microfluidizer (model number M-110-EH manufactured by Microfluidic Corporation) of 124 MPa.
This was gradually cooled to 35 ° C.
The hydrogenated lecithin (SLP-PC70HS manufactured by Sakai Oil Co., Ltd.) was used, and the long-chain branched fatty acid cholesteryl used was Nippon Seika Co., Ltd. YOFCO CLE-NE.

Example 2 parts by weight Example 1 20.0
Purified water 58.4
1,3 butylene glycol 4.7
1,2 pentanediol 3.0
Methyl paraoxybenzoate 0.1
Glycerin 1.8
2% carboxyvinyl polymer aqueous solution (neutralized) 12.0
Production method These were mixed.

Example 3 Part by weight Part A squalane 15.0
Olive oil 1.0
Mink oil 1.0
Jojoba oil 2.0
Beeswax 2.0
Cetostearyl alcohol 2.0
Glycerol monostearate 1.0
Sorbitan monostearate 2.0
Part B
Purified water 37.9
Polyoxyethylene (20E.O.) sorbitan monostearate 2.0
Polyoxyethylene (60E.O.) hydrogenated castor oil 1.0
Glycerin 5.0
1.0% sodium hyaluronate aqueous solution 5.0
Methyl paraoxybenzoate 0.1
Part C Example 1 20.0
Part A and part B were weighed and heated to 70 ° C., part A was gradually added to part B with stirring, and then cooled to 30 ° C. with slow stirring. To this, part C was gradually added with stirring.

Comparative Example 1
Example 2 using Example 1 in which only the microfluidizer process is omitted, the others are the same

Skin barrier function recovery promotion test The following tests were carried out by 6 healthy men (34 to 54 years old).
A glass cylinder with an inner diameter of 2 cm was pressed against the three inner parts of the left forearm. This was carried out twice a day for 3 days.
Specimen 1 (Example 2) and Specimen 2 (Comparative Example 1) were applied twice a day for 25 days to the site of rough skin caused by sodium lauryl sulfate. (No application at one place)
Before causing skin irritation with sodium lauryl sulfate (initial), after applying sodium lauryl sulfate 6 times, 4 days, 11 days, 18 days, and 25 days after applying the sample, the amount of water evaporation (TEWL) from the skin was measured as follows. It was measured.
After washing the inner part of the left forearm with a commercially available facial cleansing foam, the amount of water evaporation (TEWL) was measured after 30 minutes in a constant temperature and humidity chamber at a temperature of 21 ° C. ± 2 ° C. and a humidity of 45% ± 5%.
For measurement, VAPOSCAN AS-VT100RS manufactured by Asahi Biomed Co., Ltd. was used.
As a result, an average of 6 persons was taken and the initial value was shown as 1. (Table 1)

Measurement of particle diameter As a result of measuring the particle diameter of a 1% aqueous solution of the same prescription part as in Example 1 in which microfluidizer treatment used in Example 1 and Comparative Example 1 is omitted with Zetasizer Nano manufactured by Malvern, the average particle diameter Was 133 nm in Example 1 and 2970 nm in the same prescription part as Example 1 in which the microfluidizer treatment used in Comparative Example 1 was omitted.

  Thus, although Example 2 and Comparative Example 1 were the same composition, it turned out that an average particle diameter differs and the rough skin improvement, ie, the recovery | restoration of a skin barrier function, is performed rapidly.

Claims (5)

  An oil-in-water emulsified emulsion for promoting the recovery of skin barrier function having an average particle size of 300 nm or less, comprising an oil-soluble component containing 70% or more of a sterol ester, one or more surfactants, and a water-soluble component. Composition    The oil-in-water emulsion composition for promoting skin barrier function recovery according to claim 1, wherein the surfactant is one or more selected from lecithin, polyglycerin fatty acid ester and sugar ceramide.   The oil-in-water emulsion composition for promoting the recovery of skin barrier function according to claim 1 or 2, wherein a part of the sterol ester is an ester of a branched fatty acid (12 to 31 carbon atoms) and cholesterol.   4. The oil-in-water emulsion composition for promoting the recovery of skin barrier function according to claim 1, wherein the average particle size is 150 nm or less.   A composition for promoting the recovery of skin barrier function, wherein a water-soluble component and / or an oil-in-water emulsion composition is added to the oil-in-water emulsion composition of claims 1 to 3.