JPH09100242A - Emulsified composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain an emulsified composition having high cutaneous cell proliferative effect, and applicable as a skin care cosmetic or medicine such as an ointment for wound treatment or anti-inflammation. SOLUTION: This composition is obtained by emulsifying in O/W type an oily substance (e.g. a silicone oil) with saikosaponin b1 and/or saikosaponin b2 without using any surfactant followed by incorporating the resultant emulsion with 0.1-98wt.% of a liquid polyhydric alcohol (e.g. 1,3-butylene glycol). The content of the saikosaponin b1 and/or saikosaponin b2 is 0.0001-20wt.% in the final composition. This emulsified composition is excellent in long-term stability and promoted in percutaneous absorbability, and yields a cosmetic or medicine excellent in skin chapping preventive and remedying effect and skin aging preventive effect or wound curing effect, each inherent in saikccsaponin b1 and saikosaponin b2.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an emulsion composition. This emulsified composition has a high skin cell growth effect, and is applied to cosmetics for skin care and pharmaceuticals such as ointments for wound treatment and anti-inflammatory.

[0002]

2. Description of the Related Art Saikosaponin b1 and saikosaponin b2 extracted from plants such as Saiko have effects such as wound healing of skin, prevention and improvement of rough skin, and prevention of aging such as sagging and loss of skin. Blended into cosmetics.

[0003]

However, the composition containing the saikosaponin b1 and / or the saikosaponin b2 is improved in stability because the system becomes unstable and the above-mentioned effects are deteriorated when left standing for a long time. Therefore, it is necessary to mix an oily substance.

However, in order to emulsify an oily substance, a surface-active substance must be blended, and since this surface-active substance inhibits the percutaneous absorption of saikosaponin, the saikosaponin b1 and the saikosaponin b2 have the above-mentioned properties. There has been a problem that an emulsion composition that sufficiently exhibits the effect cannot be obtained.

The present invention has been completed as a result of intensive studies in view of the above problems, and stabilizes a system containing saikosaponin b1 and / or saikosaponin b2, and is excellent in transdermal absorbability thereof, It is an object of the present invention to provide an emulsified composition that can maintain the effects of saponin b1 and saikosaponin b2 for a long period of time.

[0006]

Means for Solving the Problems That is, the present invention provides an emulsified composition comprising an oily substance which is emulsified O / W with Psychosaponin b1 and / or Psychosaponin b2 and which contains no surfactant. It is provided.

The present invention also provides the emulsified composition described above, characterized in that the emulsified composition described above contains 0.1 to 98.0% by weight of a liquid polyhydric alcohol. is there.

Furthermore, the present invention provides 0.006 of the above-mentioned saikosaponin b1 and / or saikosaponin b2.
The emulsified composition is provided in an amount of 01 to 20% by weight.

Hereinafter, the present invention will be described in detail. The first gist of the present invention is to emulsify an oily substance by O / W with at least one of saikosaponin b1 and saikosaponin b2 without blending a surface-active substance, which is excellent in long-term stability and is transdermal. An emulsified composition having good absorbability and being able to sufficiently exhibit the above effects.

A second aspect of the present invention is characterized in that, in the first aspect, the liquid polyhydric alcohol is contained in an amount of 0.1 to 98.0% by weight, and that psychosaponin can be more effectively transdermally absorbed. In the emulsified composition.

A third aspect of the present invention is the emulsified composition according to the first or second aspect, which comprises 0.0001 to 20% by weight of at least one of saikosaponin b1 and saikosaponin b2. is there.

The oily substances used in the present invention include fats and oils, waxes, hydrocarbon oils, esters, silicones and the like. For example, liquid fats and oils include avocado oil, camellia oil, turtle oil, macadamia nut oil and corn oil. , Mink oil, olive oil, rapeseed oil, egg yolk oil, sesame oil, persic oil, wheat germ oil, southern oil, castor oil, linseed oil,
Safflower oil, cottonseed oil, eno oil, soybean oil, peanut oil, teaseed oil, kaya oil, rice bran oil, sinagiri oil, Japanese kiri oil,
Examples include jojoba oil, germ oil, triglycerin, glyceryl trioctanoate, glyceryl triisopalmitate and the like.
Examples of solid oils and fats include cacao butter, coconut oil, horse fat, hardened coconut oil, palm oil, beef tallow, sheep fat, hardened beef tallow, palm kernel oil, lard, beef bone fat, sorghum kernel oil, hardened oil, and beef tallow. , Owl, hydrogenated castor oil, etc. Examples of waxes include beeswax, candelilla wax, cotton wax, carnauba wax, bayberry wax, ivowa wax, whale wax, montan wax, nuka wax, lanolin, kapok wax, lanolin acetate, liquid lanolin, sugar cane wax, lanolin fatty acid isopropyl,
Hexyl laurate, reduced lanolin, jojoba wax,
Hard lanolin, shellac wax, etc. Hydrocarbon oils include liquid paraffin, ozokerite, squalene, pristane, paraffin, ceresin, squalene, petrolatum, microcrystalline wax and the like. Synthetic ester oils include isopropyl myristate, cetyl octanoate, octyldodecyl myristate, isopropyl palmitate, butyl stearate, hexyl laurate, myristyl myristate, decyl oleate, hexyldecyl dimethyloctanoate, cetyl lactate, myristyl lactate. , Lanolin acetate, isocetyl stearate, isocetyl isostearate, cholesteryl 12-hydroxystearyl acid, ethylene glycol di-2-ethylhexylate, dipentaerythritol fatty acid ester, N-alkyl glycol monoisostearate, neopentyl glycol dicaprate, malic acid Diisostearyl,
Glycerin di-2-heptylundecanoate, trimethylolpropane tri-2-ethylhexylate, trimethylolpropane triisostearate, pentaneerythritol tetra-2-ethylhexylate, glycerin tri-2-ethylhexylate, trimethylolpropane triisostearate, cetyl 2-ethylhexanoate, 2-ethylhexyl palmitate, glycerin trimyristate, tri-2-heptylundecanoic acid glyceride, castor oil fatty acid methyl ester, oleic acid oil, cetostearyl alcohol, acetoglyceride, palmitic acid 2-heptylunate Decyl, diisobutyl adipate, N-lauroyl-L-glutamic acid-2-octyldodecyl ester,
Di-2-heptylundecyl adipate, ethyl laurate, di-2-ethylhexyl sebacate, myristic acid 2-
Hexyldecyl, 2-hexyldecyl palmitate, 2-hexyldecyl adipate, diisopropyl sebacate,
2-ethylhexyl succinate, ethyl acetate, butyl acetate,
Examples include amyl acetate and triethyl citrate. Examples of the silicone include chain polysiloxanes such as dimethylpolysiloxane, methylphenylpolysiloxane, and methylhydrogenpolysiloxane, cyclic polysiloxanes such as decamethylpolysiloxane, dodecamethylpolysiloxane, and tetramethyltetrahydrogenpolysiloxane. Examples of the oil include silicone resin and silicone rubber that form a three-dimensional network structure.

Among the above oily substances, non-polar oils are preferable, and if silicone oil is used, they will be well spread and spread when applied to the skin.

The emulsion composition of the present invention contains at least one of saikosaponin b1 and saikosaponin b2. The compounding amount is 0.00 in the total amount of the emulsion composition.
01 to 20% by weight is preferable, 0.001 to 10% by weight
Is more preferred.

The present invention is characterized by O / W emulsification without using a surfactant, and the surfactant mentioned here means a cationic surfactant, an anionic surfactant, and a nonionic surfactant. It is a compound containing an active agent, an amphoteric surfactant and an amphipathic substance. Examples of the cationic surfactant include stearyltrimethylammonium chloride, alkyltrimethylammonium salts such as lauryltrimethylammonium chloride, distearyldimethylammonium dialkyldimethylammonium chloride, and poly (N, N'-dimethyl-3,5-methylene chloride). Piperidinium),
An alkylpyridinium salt such as cetylpyridinium chloride,
Alkyl quaternary ammonium salt, alkyl dimethyl benzyl ammonium salt, alkyl isoquinolinium salt, dialkyl morphonium salt, POE alkyl amine, alkyl amine salt, polyamine fatty acid derivative, amyl alcohol fatty acid derivative, benzalkonium chloride, benzethonium chloride, etc. Is. As the anionic surfactant, for example,
Base for soap, fatty acid soap such as sodium laurate, sodium palmitate, etc., higher alkyl sulfate ester salt such as sodium lauryl sulfate, lauryl sulfate K,
Alkyl ether sulfates such as POE lauryl sulfate triethanolamine and POE sodium lauryl sulfate;
N-acyl sarcosine acids such as sodium lauroyl sarcosine, N-myristoyl-N-methyltaurine sodium,
Higher fatty acid amide sulfonates such as coconut oil fatty acid sodium methyl tauride and sodium lauryl methyl tauride, POE sodium oleyl ether phosphate, POE
Phosphoric acid ester salts such as stearyl ether phosphoric acid, di-2
-Sulfosuccinates such as sodium ethylhexyl sulfosuccinate, monolauroyl monoethanolamide sodium polyoxyethylene sulfosuccinate, sodium lauryl polypropylene glycol sulfosuccinate, sodium linear dodecylbenzenesulfonate, triethanolamine linear dodecylbenzenesulfonate, and linear dodecylbenzenesulfone N-acyl glutamates such as alkylbenzene sulfonates such as acids, monosodium N-lauroylglutamate, disodium N-stearoylglutamate, monosodium N-myristoyl-L-glutamate, and higher fatty acids such as hydrogenated coconut oil fatty acid sodium glycerin sulfate Ester sulfates, sulfated oils such as funnel oils, POE alkyl ether carboxylic acids, PO
E Alkyl allyl ether carboxylate, α-olefin sulfonate, higher fatty acid ester sulfonate, secondary alcohol sulfate ester salt, higher fatty acid alkylolamide sulfate ester salt, lauroyl monoethanolamide sodium succinate, N-palmitoyl asparagine Examples thereof include acid ditriethanolamine and sodium caseinate. As the lipophilic nonionic surfactant, for example,
Sorbitan monooleate, sorbitan monoisostearate, sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan sesquioleate, sorbitan trioleate, penta
Sorbitan fatty acid esters such as -2-ethylhexylate diglycerol sorbitan, tetra-2-ethylhexylate diglycerol sorbitan, mono cottonseed oil fatty acid glycerin, glyceryl monoerucate, glyceryl sesquioleate, glyceryl monostearate, α, α'-olein Acid glyceryl pyroglutamate, glycerin polyglycerin fatty acid such as glycerin monostearate malic acid, propylene glycol fatty acid ester such as propylene glycol monostearate, hydrogenated castor oil derivative, glycerin alkyl ether and the like. Examples of hydrophilic nonionic surfactants include POE sorbitan monooleate, POE-sorbitan monostearate,
POE-sorbitan monooleate, POE-sorbitan tetraoleate and other POE sorbitan fatty acid esters, POE-sorbit monolaurate, POE-sorbit monooleate, POE-sorbit pentaoleate, POE-sorbit monostearate and other POE Sorbitol fatty acid esters, POE-glycerin monostearate, POE-glycerin monoisostearate, POE-glycerin triisostearate, and other POE glycerin fatty acid esters, POE monooleate, POE distearate, POE monodioleate, ethylene glycol cistearate, etc. POE fatty acid esters, POE lauryl ether, POE oleyl ether, POE stearyl ether, POE behenyl ether, POE2-octyldodecyl ether, POE cholestanol ether and other POE alkyl ethers, POE octyl ether Vinyl ether, POE nonylphenyl ether, PO
E POE alkyl phenyl ethers such as dinonyl phenyl ether, Pluronic types such as Bluronic, P
OE / POP cetyl ether, POE / POP2-decyl tetradecyl ether, POE / POP monobutyl ether, POE /
For POP hydrogenated lanolin, POE / POP glycerin ether, etc.
POE / POP alkyl ethers, Tetronic tetra POE / tetra POP ethylenediamine condensates, POE castor oil, POE hydrogenated castor oil, POE hydrogenated castor oil monoisostearate, POE hydrogenated castor oil triisostearate, POE hydrogenated Castor oil Monopyroglutamic acid monoisostearate diester, POE Hardened castor oil Maleic acid and other POE Castor oil Hardened castor oil derivative, POE Solbit beeswax and other POE beeswax lanolin derivatives, coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, fatty acid Alkanolamides such as isopropanolamide, POE Propylene glycol fatty acid ester, POE
Examples thereof include alkylamine, POE fatty acid amide, sucrose fatty acid ester, POE nonylphenylformaldehyde condensate, alkylethoxydimethylamine oxide, trioleylphosphoric acid and the like. Examples of the amphoteric surfactant include 2-undecyl-N, N, N- (hydroxyethylcarboxymethyl) -2-imidazoline sodium, 2-cocoyl-2-
Imidazolinium hydroxide-1-carboxyethyloxy disodium salt and other imidazoline-based amphoteric surfactants, 2-heptadecyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, lauryldimethylaminoacetic acid betaine, alkyl Examples thereof include betaine-based surfactants such as betaine, amidobetaine, and sulfobetaine. An amphipathic substance has a surface activity, but is itself highly hydrophobic and not as surface active as a general surfactant. For example, lauric acid, myristic acid, palmitic acid, stearic acid, behen ( Behenic acid), oleic acid, 12-hydroxystearic acid, undecylenic acid, tall acid, isostearic acid, linoleic acid, linoleic acid, eicosapentaenoic acid (EPA), docosahexaenoic acid (DHA) and other higher fatty acids, lauryl alcohol, cetyl alcohol , Linear alcohols such as stearyl alcohol, behenyl alcohol, myristyl alcohol, oleyl alcohol, and cetostearyl alcohol,
Higher aliphatic alcohols such as monostearyl glycerin ether (batyl alcohol), 2-decyltetradecinol, lanolin alcohol, cholesterol, phytosterols, hexyldecanol, isostearyl alcohol, octyldodecanol, etc., higher aliphatic alcohols, monoglycerides, glycerol Examples thereof include monoalkyl ethers, monoalkylamines, and compounds having a sterol skeleton (cholesterol, phytosterol).

Examples of the liquid polyhydric alcohol used in the second invention of the present invention include ethylene glycol and
Propylene glycol, trimethylene glycol, 1,
2-butylene glycol, 1,3-butylene glycol, tetramethylene glycol, 2,3-butylene glycol, pentamethylene glycol, 2-butene-1,
Dihydric alcohols such as 4-diol, hexylene glycol and octylene glycol, 3 such as glycerin, trimethylolpropane and 1,2,6-hexanetriol
Examples thereof include polyhydric alcohol polymers such as polyhydric alcohols, diethylene glycol, dipropylene glycol, triethylene glycol, polypropylene glycol, tetraethylene glycol, diglycerin, polyethylene glycol, triglycerin, tetraglycerin and polyglycerin. Among these, water-soluble liquid polyhydric alcohols are particularly preferable. The liquid polyhydric alcohol content is preferably 0.1 to 98.0% by weight, more preferably 1 to 40% by weight, based on the total weight of the emulsion composition.

The emulsified composition of the present invention contains, in addition to the above-mentioned essential components, components commonly used in cosmetics, pharmaceuticals, etc., such as an aqueous component, a powder component, a moisturizing agent, as long as the effects of the present invention are not impaired. A thickener, an antiseptic, an antioxidant, a percutaneous absorption enhancer, a fragrance, a coloring agent, a drug and the like can be added.

[0018]

EXAMPLES Next, the present invention will be described in detail with reference to examples, but it goes without saying that the technical scope of the present invention is not limited to these examples.

[Evaluation of transdermal absorbability] 50 microliters of the emulsified compositions of the following Examples and Comparative Examples were applied to 4 cm 2 of the back of male hairless mice aged 10 to 14 weeks. After 6 hours, they were sacrificed and the remaining emulsified composition was washed off with water. The skin was excised after tape stripping to completely remove the stratum corneum. Psychosaponin was extracted from the obtained epidermis and dermis layer and quantified by high performance liquid chromatography. The results were expressed as the concentration in skin (% by weight).

Example 1 Weight% (Phase A) Liquid paraffin 4.0 Psychosaponin b1 0.1 Purified water 3.5 (Phase B) Psychosaponin b1 1.0 Ethanol 10.0 Carboxyvinyl polymer 0.15 Potassium hydroxide 0.04 Methylparaben 0.2 Perfume 0.05 Purified water Residue (production method) Phase A was emulsified and added to the gel composition in which phase B was dissolved and stirred, and the mixture was uniformly mixed to obtain the emulsion composition of the present invention. Obtained. The transdermal absorbability of the emulsion composition of Example 1 is shown in "Table 1".

Example 2 Weight% (Phase A) Squalane 2.0 Psychosaponin b2 0.1 Purified water 1.0 (Phase B) Psychosaponin b2 1.0 1,3-butylene glycol 5.0 Glycerin 5 .0 Carboxyvinyl polymer 0.15 Potassium hydroxide 0.04 Methylparaben 0.2 Perfume 0.05 Purified water Residual (production method) Phase A was emulsified and added to the gel composition in which phase B was dissolved and stirred, and mixed uniformly. To obtain the emulsion composition of the present invention. The transdermal absorbability of the emulsion composition of Example 2 is shown in "Table 1".

Example 3 Weight% (Phase A) Dimethylpolysiloxane 2.0 Psychosaponin b2 0.05 Purified water 7.0 (Phase B) Psychosaponin b1 6.0 Glycerin 20.0 Ethanol 5.0 Carboxy Vinyl polymer 0.2 Potassium hydroxide 0.05 Butylparaben 0.1 Perfume 0.05 Purified water Residue (production method) Phase A was emulsified and added to the gel composition in which phase B was dissolved and stirred, and the mixture was uniformly mixed to form An emulsified composition of the invention was obtained. The transdermal absorbability of the emulsion composition of Example 3 is shown in "Table 1".

[Example 4] wt% (Phase A) Triglycerin 2.0 Psychosaponin b1 2.0 Purified water 7.0 (Phase B) Dipropylene glycol 20.0 Ethanol 5.0 Hydroxypyropyrcellulose 1. 0 Butylparaben 0.1 Perfume 0.05 Purified water Residue (production method) Phase A was emulsified and added to the gel composition in which phase B was dissolved and stirred, and the mixture was uniformly mixed to obtain the emulsion composition of the present invention. The transdermal absorbability of the emulsion composition of Example 4 is shown in "Table 1".

[Example 5] Weight% (Phase A) Beeswax 2.0 Psychosaponin b2 0.3 Purified water 1.0 (Phase B) Polyethylene glycol (Mw = 400) 47.0 Polyethylene glycol (Mw = 4000) 47.0 Methylparaben 0.1 Perfume 0.05 Ethanol Residue (production method) Phase B is heated to 65 ° C. while stirring to dissolve, and emulsified Phase A is added at room temperature and uniformly mixed to emulsify the present invention. A composition was obtained. The transdermal absorbability of the emulsion composition of Example 5 is shown in "Table 1".

[0025]

[Table 1] [Results of transdermal absorbability evaluation] The emulsified compositions of the present invention in Examples 1 to 5 are saikosaponin b.
1 and b2 have excellent transdermal absorbability.

Comparative Example 1 Weight% (Phase A) Psychosaponin b1 0.001 Fragrance 0.03 Ethanol 3.0 (Phase B) Stearic Acid 0.5 Cetyl Alcohol 1.5 Beeswax 2.0 Polyoxyethylene ( 10) Oleyl 2.0 Alcohol Ethylparaben 0.3 (Phase C) Propylene glycol 5.0 Quinceseed extract (5% aqueous solution) 20.0 Purified water Residue (Production method) 70 ° C phase C melted by heating at 70 ° C Phase B was added, preliminarily emulsified, and homogenized with a homomixer. While stirring this, the alcohol phase and the quince seed extract were added, and the mixture was cooled to 30 ° C. to obtain an emulsified composition. As a result of evaluating the transdermal absorbability of the emulsified composition of Comparative Example 1, the psychosaponin b1 was not detected in the skin.

“Comparative Example 2” wt% Saikosaponin b2 5.0 Vaseline 40.0 Stearyl alcohol 15.0 Mokurou 20.0 Polyoxyethylene (10) oleyl 0.5 alcohol Purified water Residual (manufacturing method) Purification at 70 ° C. Other components mixed and dissolved in water at 70 ° C. were added, and the mixture was uniformly emulsified with a homomixer, emulsified, and cooled to obtain an emulsified composition. As a result of evaluating the transdermal absorbability of the emulsified composition of Comparative Example 2, psychosaponin b2 was not detected in the skin.

Comparative Example 3 Weight% (Phase A) Triglycerin 2.0 Saikosaponin b1 2.0 Sorbitan monooleate 2.0 Purified water 7.0 (Phase B) Dipropylene glycol 20.0 Ethanol 5. 0 Hydroxypyropyrcellulose 1.0 Butylparaben 0.1 Perfume 0.05 Purified water Residual (production method) Phase A was emulsified and added to the gel composition in which phase B was dissolved and stirred, and the mixture was uniformly mixed to form an emulsified composition. Obtained. As a result of evaluating the transdermal absorbability of the emulsified composition of Comparative Example 3, saikosaponin b1 was not detected in the skin.

[0029]

INDUSTRIAL APPLICABILITY According to the present invention, an oily substance is O / W emulsified with at least one of saikosaponin b1 and saikosaponin b2 to provide an emulsified composition containing no surfactant, thereby providing saikosaponin b1. And the transdermal absorbability of saikosaponin b2 can be promoted, resulting in saikosaponin b1 and saikosaponin b2.
Cosmetics or pharmaceuticals having high skin roughening prevention and improvement effects, skin aging prevention effects or wound healing effects.

Further, by adding a liquid polyhydric alcohol to the emulsion composition of the present invention, it is possible to more efficiently transdermally absorb saikosaponin, and the above-mentioned effects of saikosaponin b1 and saikosaponin b2 are sufficiently exerted. A cosmetic or medicinal product that works is obtained.

Claims (3)

[Claims] 1. An emulsified composition, which is obtained by emulsifying an oily substance with a saikosaponin b1 and / or a saikosaponin b2 in an O / W manner and does not contain a surface-active substance. 2. The emulsion composition according to claim 1, wherein the emulsion composition contains 0.1 to 98.0% by weight of a liquid polyhydric alcohol. 3. The saikosaponin b1 and / or the above.
Or 0.0001 to 20% by weight of saikosaponin b2
The emulsified composition according to claim 1 or 2, comprising: