JP2001097811A - Lipid complex and external application composition containing the complex - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a lipid complex having excellent moisture-keeping action and protecting action on the skin and hair and capable of including an agent and slowly releasing the agent and provide an external application composition containing the complex. SOLUTION: The objective lipid complex contains (A) a surfactant, (B) an amphiphilic substance and (C) sterol as constituent components and takes the form of a vesicular lipid membrane capable of including a water phase, more preferably takes the form of a aqueous dispersion. The external application composition contains the lipid complex.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to a lipid complex which is useful as a component of a composition for external use such as cosmetics.

[0002]

2. Description of the Related Art It is well known that in emulsified compositions such as emulsions and creams, a surfactant and an amphiphile form an aggregate with a certain composition and thicken and solidify the composition. ing. This phenomenon is based on a thickening effect by a surfactant and an amphiphile forming an aggregate having a lamellar structure in an aqueous phase, which further forms a three-dimensional network structure. The aggregate formed by the surfactant and the amphiphile increases the emulsification stability of the emulsion composition by thickening and solidifying the emulsion composition, and exerts a moisturizing action on skin and hair. You can also.

[0003] On the other hand, certain amphiphiles swell in an amphiphile-water system to form lamellar liquid crystals, and when they are agitated, the bilayer film of the lamellar liquid crystals overlaps one or more layers. It is also known that this forms vesicles containing an aqueous phase.

[0004]

However, for the purpose of protecting and moisturizing the skin and hair, a combination of a surfactant and an amphipathic substance used in emulsions and creams is used, for example, with a low viscosity such as lotion. Incorporation into a formulation causes poor dispersion and causes problems such as aggregation and viscosity increase over time. To solve this problem, see, for example,
As described in JP-A-71421, in the oil-in-water emulsion composition, the total amount of the amphiphilic substance and the surfactant capable of forming a gel in the aqueous phase is substantially added to the boundary between the oil phase and the aqueous phase. A preparation method has been developed which makes it possible to maintain a low viscosity over a long period of time by allowing the presence of the compound to be present. In the preparation obtained by this method, an association formed by the surfactant and the amphipathic substance is reformed in the middle of application, and a high moisturizing effect can be exerted on skin and hair. However, when the oil is not blended or the amount of the oil blended is small, a stable base cannot be obtained by this preparation method.

On the other hand, as a means for forming vesicles, a method using phospholipid as an amphipathic substance is known.
By using this means, the drug can be retained in the aqueous phase in the lipid bilayer membrane or in the vesicle. When the base on which vesicles are formed using this means is applied on the skin,
These vesicles are gradually broken down on the skin, and it is possible to control the release of the drug contained in the vesicles. That is, by using the vesicle forming means using this phospholipid,
It is also possible to control the release of a water-soluble drug or a fat-soluble drug that can be contained in a lipid membrane. However, phospholipids are generally unstable and expensive.

[0006]

In such a situation, the present inventors stably dispersed a surfactant-amphiphile combination effective for the skin in an aqueous phase, and furthermore they contained an aqueous phase. In order to form vesicles, the inventors investigated the physical properties of the aggregate formed by the surfactant and the amphiphile. As a result, it was found that, in a combination of a surfactant and an amphiphile that forms a gel at normal temperature or higher, by mixing sterol in the gel, the gel can be stably dispersed as vesicles in an aqueous phase. . Further, the external composition containing vesicles formed by this means has a function of moisturizing and further protecting the skin and hair, and can further contain fat-soluble drugs and water-soluble drugs in the vesicles. The inventors have found that the present invention has been completed.

That is, in the present application, the present inventor:
Provided is a lipid complex containing (A) a surfactant, (B) an amphiphilic substance, and (C) a sterol as components (hereinafter, also referred to as the lipid complex of the present invention). Usually, the lipid complex of the present invention is in the form of a vesicular lipid membrane capable of enclosing the aqueous phase (D). And most preferably, it is present as a lipid complex in the form of an aqueous dispersion.
The inventor also provides an external composition containing the lipid complex of the present invention (hereinafter, also referred to as an external composition of the present invention) in the present application.

[0008]

Embodiments of the present invention will be described below. As described above, the lipid complex of the present invention is a lipid complex containing at least (A) a surfactant, (B) an amphipathic substance, and (C) a sterol as its components. In addition, the lipid complex of the present invention usually takes the form of a vesicular lipid membrane capable of containing (D) an aqueous phase.

Furthermore, the lipid complex of the present invention is characterized in that the constituent components (A) to (C) satisfy predetermined conditions,
(D) It can be provided as an aqueous dispersion of a vesicular lipid membrane capable of containing an aqueous phase.

[0010] The surfactant which is the component (A) constituting the lipid complex of the present invention is not particularly limited, and may be a cationic surfactant, an anionic surfactant, an amphoteric surfactant or a nonionic surfactant. Any type of surfactant can be used alone or in combination of two or more. In particular,
As anionic surfactants, for example, fatty acid soaps such as sodium laurate and sodium palmitate; higher alkyl sulfates such as sodium lauryl sulfate and potassium cetyl sulfate; alkyl ethers such as POE lauryl sulfate triethanolamine and POE sodium lauryl sulfate N-acyl sarcosine acids such as sodium lauroyl sarcosine; N-myristoyl-N
-Higher fatty acid amide sulfonates such as sodium methyltaurine, coconut fatty acid sodium methyltauride and sodium laurylmethyltauride; phosphate esters such as sodium cetyl phosphate and POE stearyl ether phosphoric acid; di-2-ethylhexyl sulfosuccinic acid Sodium sulfo succinates such as sodium monolauroyl monoethanolamide polyoxyethylene sodium sulfosuccinate, sodium lauryl polypropylene glycol sulfosuccinate; alkyl benzene sulfones such as sodium linear dodecylbenzene sulfonate, triethanolamine linear benzene sulfonate, and linear dodecyl benzene sulfonate Acid salts: monosodium N-lauroylglutamate, disodium N-stearoylglutamate, N-myris N-acyl glutamates such as monosodium lyl-L-glutamate; higher fatty acid ester sulfates such as hydrogenated coconut fatty acid sodium glycerin sulfate; sulfated oils such as funnel oil; POE alkyl ether carboxylic acid; POE alkyl allyl ether carboxylate Acid salt, α-olefin sulfonate, higher fatty acid ester sulfonate, secondary alcohol sulfate,
Higher fatty acid alkylolamide sulfates, sodium lauroyl monoethanolamide succinate, N-palmitoyl aspartate ditriethanolamine, hydroxyalkyl ether carboxylate, and the like.

Examples of the cationic surfactant include alkyltrimethylammonium salts such as stearyltrimethylammonium chloride and behenyltrimethylammonium chloride; dialkyldimethylammonium salts such as distearyldimethylammonium chloride; alkylpyridinium salts such as cetylpyridinium chloride; Secondary ammonium salts, alkyldimethylbenzylammonium salts, alkylisoquinolinium salts, dialkylmorphonium salts, POE alkylamines, alkylamine salts, amyl alcohol fatty acid derivatives, benzalkonium chloride, benzethonium chloride, fatty acid dimethylamine propylamide, Fatty acid diethylamine diethylamide and the like can be mentioned.

Examples of the amphoteric surfactant include 2-undecyl-N, N, N- (hydroxyethylcarboxymethyl) -2-imidazoline sodium and 2-cocoyl-
Imidazoline amphoteric surfactants such as 2-imidazolinium hydroxide-1-carboxyethyloxy-2-sodium salt; 2-heptadecyl-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, lauryl dimethylaminoacetic acid betaine , Betaine surfactants such as alkylbetaine, amidobetaine and sulfobetaine.

As the nonionic surfactant, for example, PO
POE such as E sorbitan monooleate, POE sorbitan monostearate, POE sorbitan monooleate
Sorbitan fatty acid esters; POE sorbite monooleate, POE
E sorbitol fatty acid esters; POE glycerin fatty acid esters such as POE glycerin monostearate, POE glycerin monoisostearate; POE fatty acid esters such as POE monooleate, POE distearate, POE monodioleate, ethylene glycol distearate; POE oleyl ether; POE stearyl ether, POE behenyl ether, POE2-
POE alkyl ethers such as octyl dodecyl ether and POE cholestanol ether; POE octyl phenyl ether, POE nonyl phenyl ether, POE
POE alkyl phenyl ethers such as E dinonyl phenyl ether; POE / POP cetyl ether, POE
・ POP2-decyltetradecyl ether, POE ・ P
POE / POP alkyl ethers such as OP hydrogenated lanolin, POE / POP glycerin ether; POE castor oil, POE hardened castor oil, POE hardened castor oil monoisostearate, POE hardened castor oil triisostearate, POE hardened castor oil Monopyroglutamic acid monostearic acid diester, POE castor oil, such as maleic acid POE castor oil, hydrogenated castor oil derivatives; POE beeswax, lanolin derivatives, such as POE sorbitol beeswax; coconut oil fatty acid diethanolamide, lauric acid monoethanolamide, fatty acid isopropanolamide Alkanolamides such as POE propylene glycol fatty acid ester, POE alkylamine, POE fatty acid amide, sucrose fatty acid ester, POE nonylphenylformaldehyde condensate, Le ethoxy dimethylamine oxide, trioleyl phosphate and the like.

In particular, typically selected components (A) include monosodium N-stearoylglutamate,
N-long-chain acyl acidic amino acid salts such as monosodium palmitoylglutamate; fatty acid soaps such as potassium behenate, potassium stearate and triethanolamine stearate; monoalkyl phosphates such as sodium cetyl phosphate; polyoxyethylene (4 ) POE alkyl ether carboxylates such as sodium lauryl ether carboxylate; acylmethyl taurine salts such as coconut oil fatty acid sodium methyl taurine; sodium lauryl sulfate;
Alkyl sulfates such as sodium cetyl sulfate; hydroxyalkyl ether carboxylate such as sodium dodecane-1,2-diol acetate; quaternary ammonium salts such as behenyltrimethylammonium chloride and stearyltrimethylammonium chloride; polyoxyethylene (30 ) Behenyl ether, polyoxyethylene (20) behenyl ether, polyoxyethylene (2
0) Stearyl ether, polyoxyethylene (15)
It is particularly preferable to select and use one or more nonionic surfactants having an HLB value of 10 or more, such as oleyl ether.

The amphiphile, which is also the component (B),
"Although having surface activity, itself is strongly hydrophobic,
"Substance that does not have the same surface activity as a general surfactant." In the present invention, as the component (B),
Higher alcohols such as behenyl alcohol, stearyl alcohol and cetyl alcohol; higher fatty acids such as behenic acid, stearic acid, palmitic acid and isostearic acid;
It is preferable to select and use one or more of monoglycerides such as glycerin monostearate; and glycerol monoalkyl ethers such as glycerol monostearyl ether. Among these, the particularly preferred component (B) is a higher alcohol having 16 or more carbon atoms in the alkyl chain.

The sterol, which is also the component (C), comprises 3
As long as it is a steroid alcohol having a hydroxyl group at the position,
It is not particularly limited, and specifically, in addition to phytosterols such as stigmasterol and sitosterol, one or more cholesterols and mycosterols can be selected and used. Particularly preferred sterols are phytosterols. And cholesterol.

[0017] is an essential component in the present invention lipid complex, (A) ~ (D) component described above, in principle, the following conditions 1. ~ 3 . Obey. 1 . The surfactant as the component (A) and the amphipathic substance as the component (B) are selected from combinations capable of forming a gel at room temperature or higher in a surfactant-amphiphile-water system.

"Normal temperature" generally refers to a temperature range assumed when an external composition is used. Specifically, it is about 15 to 25 ° C. However, the present invention is not limited to this. The transition temperature of the gel formed in the above surfactant-amphiphile-water system is 6
It is preferable that the temperature is 0 ° C. or higher in order to satisfy the gel forming conditions described above.

The formation of a gel in the surfactant-amphiphile-water system indicates that in the lipid complex of the present invention,
This is a prerequisite for obtaining vesicles having the desired properties. In a surfactant-amphiphile-water system, an aggregate formed in a specific composition behaves similarly to a phospholipid having a two-chain type hydrocarbon chain which alone forms a vesicle,
It is thought that a vesicle is formed by forming a bimolecular membrane and closing it. Further, in consideration of the dispersion stability of vesicles that can be formed as the lipid complex of the present invention, the surfactant-amphiphile-aqueous gel in the aqueous system has a surfactant and an amphiphile alkyl in the gel. It is preferable that the chains are α-type, which is a structure arranged in a hexagonal system.
When the gel is other than the α-type, it is also assumed that the structure of the above-mentioned bilayer membrane becomes rigid, dispersibility is reduced, and formation of vesicles is hindered.

It should be noted that whether or not the gel is α-type
For example, it is possible to determine whether a single strong peak is observed around 21.4 ° by X-ray diffraction of the gel.
These conditions 1 . The combination of the components (A) and (B) to be selected can be satisfied by appropriately combining the preferred embodiments of the components (A) and (B) specifically listed above. is there.

[0021] 2. The weight ratio of the surfactant (A) and the amphiphile (B) is as follows:
(B) = 1: 5 to 5: 1 and the components (A) and (B)
It is preferable that the sum of the components and the weight ratio of the sterol as the component (C) be (A) + (B) :( C) = 10: 1 to 1: 1.

The weight ratio of the components (A) and (B) in the lipid complex of the present invention [(A) :( B) = 1: 5
If the weight ratio of the surfactant (A) is larger than 5: 1], the moisturizing effect and the protective effect of the lipid complex on the skin and hair are impaired. Conversely, if the weight ratio of the amphiphilic substance as the component (B) is large, the dispersion stability of the vesicle as the lipid complex decreases.

The weight ratio of the sum of the components (A) and (B) and the sterol (C) is [(A) +
Outside the range of (B) :( C) = 10: 1 to 1: 1], the sterol-stabilizing action of vesicles is impaired.

3 . When the sum of the components (A), (B) and (C) and the weight ratio of the component (D) (aqueous phase) are [(A)
+ (B) + (C) :( D) = 0.1: 99.9-30:
70]. When the weight ratio of the sum of the components (A), (B), and (C), which are lipid dispersions, to the component (D), which is an aqueous phase, is lower than the above range, the moisturizing action and the protective action due to the blending of lipids are reduced. I do. Conversely, if the weight ratio of the sum of the components (A), (B) and (C) to the component (D) is higher than the above range, it becomes difficult to disperse the vesicles in the aqueous phase.

In the components (A) to (D), in principle, these conditions 1 . ~ 3 . The production method of the lipid complex of the present invention according to the present invention is not particularly limited, for example, as shown in `` Colloid Science IV Colloid Science Experimental Method, edited by The Chemical Society of Japan, Tokyo Kagaku Dojin, p343-346 (1992) '' After dissolving the components in a solvent and premixing and evaporating and removing the solvent, a method of adding an aqueous phase or a method of adding an aqueous phase to the melted lipid component may be used. Further, a lipid complex and a composition containing the same can be easily obtained by dissolving a film-forming component in a water-soluble solvent such as ethanol or dipropylene glycol and adding the resulting solution to an aqueous phase. Further, the lipid complex or the composition obtained by these production methods is further processed by a high-speed mixer or a high-pressure emulsifier to produce a lipid complex or the composition in which finer vesicles are dispersed. It is also possible.

The lipid complex or the composition of the present invention which can be produced in this manner can exert a moisturizing effect and a protective effect on skin and hair by itself, but it is effective for the vesicles constituting the lipid complex. , By encapsulating various drugs,
After stabilizing these drugs, it becomes possible to release them slowly on the skin and hair.

The drug to be included is not particularly limited.
It may be water-soluble or oil-soluble. In particular,
Whitening agents such as, for example, ascorbic acid and its derivatives, hydroxy acids, kojic acid, arbutin and its derivatives;
Anti-inflammatory agents such as tranexamic acid and its derivatives, glycyrrhizin and its derivatives, allantoin, azulene, ε-aminocaproic acid, hydrocortisone; zinc oxide, zinc sulfate, allantoin hydroxyaluminum, aluminum chloride, aluminum sulfate, zinc sulfocarbonate, tannic acid, citric acid Astringents such as acid and lactic acid; cooling agents such as menthol and camphor; retinol, vitamin A derivatives, pyridoxine hydrochloride and its derivatives, nicotinic acid derivatives, vitamin D ₂ , vitamin E and its derivatives, calcium pantothenate, ethyl pantothenate Vitamins such as ether and biotin; amino acids such as serine, cystine, glycine, arginine, cysteine, methionine, leucine, tryptophan; thiotaurine, hypotaurine, butylhydroxytoluene Hormones such as estradiol and its esters, estrone, ethinylestradiol, cortisone and its esters, hydrocortisone and its esters, presonisone and prednisolone; antihistamines such as diphenhydramine hydrochloride and chlorpheniramine maleate; aloe extract and carrot extract And plant extracts such as licorice extract, oak extract, chamomile extract and loquat extract; and horny layer peeling agents such as sulfur, salicylic acid and resorcinol.

When the water-soluble drug is encapsulated in the vesicle, for example, the water-soluble drug is contained in the aqueous phase in the above-mentioned production method, so that the desired water-soluble drug is contained in the vesicle. The lipid complex of the present invention or the composition contained in the aqueous phase can be obtained.

The lipid complex of the present invention or the same composition in which the desired lipid-soluble drug is encapsulated in the vesicle wall can be obtained by incorporating the lipid-soluble drug into the above-mentioned lipid component.

The drug contained in the vesicles of the lipid complex of the present invention is water-soluble or fat-soluble and differs only in handling at the time of manufacture.
The whitening effect and the skin aging prevention effect are not limited at all.

The lipid complex or the composition of the present invention can exert a moisturizing effect, a protective effect, and an individual effect of the contained drug by applying itself to the skin or hair. Topical compositions containing the lipid complex of the present invention processed into various dosage forms (for example, cosmetics, pharmaceuticals,
Quasi-drugs, etc.) (composition for external use of the present invention).

In the composition for external use of the present invention, in addition to the lipid complex of the present invention, components which are blended in a general external composition, for example, as long as the excellent effects of the lipid complex on skin and hair are not impaired, for example, , An oil, a surfactant, a humectant, an ultraviolet absorber, a chelating agent, a pH adjuster, a preservative, a thickener, a pigment, a fragrance, a drug, and the like can be appropriately compounded.

The dosage form of the composition for external use of the present invention is arbitrary, and may be any of a solution type, a solubilizing type, an emulsifying type, a powder dispersing type, a water-powder two-phase type, a water-oil-powder three-phase type, etc. It is possible to choose the dosage form. Furthermore, the use of the composition for external use of the present invention is arbitrary, and it can be used for any of facial, body, and hair.

The abundance of the lipid complex of the present invention in the composition for external use of the present invention, that is, the abundances of the components (A), (B) and (C) in the composition for external use of the present invention are as follows:
In that the intended effect of the present invention is exhibited,
Preferably, it is 0.1% by weight or more of the whole external use composition, and in terms of exhibiting good usability, it is 20.0% by weight or less, preferably 1% or less of the whole external use composition.
0.0% by weight or less.

[0035]

The present invention will be described more specifically with reference to the following examples. However, the technical scope of the present invention is not limited by the description of these examples. Composition and Physical Properties of Surfactant, Amphiphilic Substance, and Sterol As described above, the weight ratio of the surfactant (A) to the amphiphilic substance (B) in the present invention,
And the sum of the surfactant and the amphiphilic substance, and the weight ratio of the sterol as the component (C) have a great effect on the dispersion stability of the lipid complex in an aqueous solvent and on the moisturizing action on the skin and hair. give.

Therefore, first, the relationship between the composition of the lipid complex composed of the components (A) to (C) and the dispersion stability and the skin moisturizing effect was examined. The components (A) and (B) are, as described above,
It is necessary to form a gel having a phase transition temperature of room temperature or higher. Therefore, Test Examples 1 and 2 described in Table 1 below were used.
A gel was manufactured based on the formulation shown in FIG. 2, and its phase transition temperature was measured. The measurement of the phase transition temperature was performed using a differential scanning calorimeter (DSC), specifically, DSC120 (manufactured by Seiko Instruments Inc.), and the endothermic peak observed in the obtained DSC heating curve was obtained. The temperature at the top was taken as the phase transition temperature.

As is clear from Test Examples 1 and 2, the combination of sodium N-stearoyl-L-glutamate and behenyl alcohol, and the combination of sodium N-stearoyl-L-glutamate and POE (30) behenyl ether and behenyl alcohol were mixed in the aqueous phase. As a result, it was found that a gel having a transition temperature higher than room temperature was formed.

[0038]

[Table 1]

Using the combinations shown in Table 1, the compositions of the above components (A) to (C) were examined. That is, a lipid complex was produced based on the formulation shown in Table 2,
The dispersion stability and the skin moisturizing effect were examined by the following test methods. Each lipid complex was prepared by dissolving (1) to (5) shown in Table 2 at 80 ° C, adding (6) to (8) to an aqueous phase heated to 80 ° C, and stirring. It was prepared by dispersing.

After the dispersion stability test sample was left at 40 ° C. for one month, it was placed in a 1 cm quartz cell,
The absorbance at 600 nm was measured with a spectrophotometer and compared with the same absorbance of the sample immediately after preparation, and at the same time, the appearance of the sample was visually evaluated. The evaluation criteria are as follows.

A: The absorbance after one month at 40 ° C./the absorbance immediately after preparation was less than 1.5, and the appearance was good. ：: Absorbance after one month at 40 ° C./absorbance immediately after preparation is less than 1.5 to less than 2.0, and the appearance is good. Δ: Absorbance after one month at 40 ° C./absorbance immediately after preparation was 2.0 or more, and haze and haze were observed in appearance. ×: Precipitation or creaming is observed in appearance.

Moisturizing Effect Test After washing the inner part of the forearm of a female professional panel of 10 women with soap, the moisture content in the stratum corneum at the above site after 30 minutes in a constant temperature and humidity room at 23 ° C. and 50% was determined. It was measured with a high-frequency impedance meter (SKICON200: manufactured by IBS). Next, 1 μl / cm ^{2 of the} sample was placed on the site of the panel.
6 hours after the application, the sample was removed by washing with soap, and the water content in the stratum corneum was measured under the same conditions as before the application of the sample. The moisturizing action of the skin of the sample was evaluated by the ratio of the amount of keratin water before and after applying the sample (after application / before application: average value of 10 persons) according to the following criteria. The larger the value, the better the moisturizing effect of the sample on the skin.

A: The ratio of keratin water content is 1.5 or more. ：: The ratio of keratin water content is less than 1.2 to less than 1.5. Δ: The ratio of keratin water content is 1 to less than 1.2. X: The ratio of keratin water content is less than 1.

Skin Tactile Test A sample was applied to the face of a panel of 10 female professionals, and an actual use test for skin feel was performed, and evaluated according to the following criteria.

A: Eight or more panels evaluated that the feeling of use was good. ：: 6 to 7 panels evaluated that the use feeling was good. Δ: Four to five panels evaluated that the use feeling was good. X: Three or less panels evaluated that the use feeling was good.

[0046]

[Table 2] From Table 2, it can be seen that the composition having both good moisturizing effect and dispersion stability on skin and hair is in the region where the weight ratio of component (A) to component (B) is 1: 5 to 5: 1. It has been clarified that when the composition of the surfactant (component) is high, the effect on the skin and hair is impaired, and when the composition of the amphipathic substance (component (B)) is high, the dispersion stability is reduced.

The preferred weight ratio of the sum of the components (A) and (B) to the sterol as the component (C) is 1
The results in Table 2 also show that the vesicles cannot be sufficiently stabilized if the ratio of the component (C) in this weight ratio is out of this range. Was.

Further, a lipid complex was produced based on the formulation shown in Table 3. Each lipid complex has a low-viscosity liquid appearance, dispersion stability over time, and moisturizing effect on the skin (test methods and evaluation methods are the same as those in the above test).
Was good, and the feel upon use was also good.

[0049]

[Table 3]

Incorporation test of water-soluble drug An inclusion test of a water-soluble drug using the lipid complex of the present invention was performed.

Specifically, based on the prescription shown in Table 4,
A lipid complex containing arbutin was produced. That is, a surfactant, 97 g of a 2% by weight aqueous solution of arbutin,
An amphiphilic substance, phytosterol, was added after melting at 110 ° C, and the mixture was stirred and dispersed at 80 ° C. After the preparation, the sample was cooled to room temperature and separated by a gel filtration into a lipid complex containing arbutin and arbutin in an external aqueous phase.

Sephadex G-50 was used for gel filtration. The eluent used was a 1.32% by weight aqueous glucose solution (isotonic with a 2% by weight aqueous solution of arbutin). The total amount of the lipid complex fraction was mixed with twice as much ethanol,
Filtration using 2μm filter, UV absorption (282nm)
The total amount of arbutin encapsulated in the lipid complex was determined by measuring.

The sum of both quantitative values corresponded to the total amount of arbutin blended. From this, the capture rate = a _in / (a _out
+ A _in ) × 100 (%), the incorporation rate was 37.96%.

[0054]

[Table 4]

Hereinafter, the composition for external use of the present invention containing the lipid complex of the present invention was produced by the following formulation according to a conventional method unless otherwise specified.

[Example 25] Amount of blending component of toner (wt%) Lipid complex described in Example 11 10.0 Ethanol 8.0 Glycerin 8.0 EDTA-3Na 0.01 Preservative Appropriate amount Perfume Appropriate amount Purified Water Residual The lotion of Example 25 was excellent in the moisturizing effect on the skin and also had good usability.

Example 26 Cream Component Ingredient Content (% by Weight) Lipid complex described in Example 14 20.0 Polyethylene glycol 4000 1.0 1,3-butylene glycol 5.0 Glycerin 7.0 Squalane 20. 0 Vaseline 5.0 Cetostearyl alcohol 3.0 Polyoxyethylene (20 mol) Oleyl alcohol ether 1.5 Glyceryl monostearate 1.5 Urea 2.0 Sodium lactate 1.0 Xanthan gum 0.05 Preservative Suitable amount Caustic potash 0 0.01 EDTA-3Na 0.01 Perfume Appropriate Amount Purified Water Residue The cream of Example 26 was excellent in the moisturizing effect on the skin and good in usability.

Example 27 Emulsion Formulation Component Content (% by Weight) Lipid complex described in Example 15 30.0 Dipropylene glycol 7.0 Glycerin 5.0 Sodium pyrrolidonecarboxylate 0.5 Squalane 5.0 Vaseline 1.0 setostearyl alcohol 0.3 polyoxyethylene (20 mol) oleyl alcohol ether 1.5 sodium polyacrylate 0.03 preservative 0.2 caustic potash 0.1 EDTA-3Na 0.03 fragrance appropriate amount purified water residue Amount The emulsion of Example 27 was excellent in moisturizing effect on the skin and good in usability.

[Example 28] Hair treatment compounding ingredients (% by weight) Lipid complex described in Example 7 10.0 1,3-butylene glycol 10.0 cetostearyl alcohol 3.0 stearyltrimethylammonium chloride 0 Dimethyl silicone (20 mP · s) 10.0 Preservatives Appropriate amount Perfume Appropriate amount Purified water remaining amount The hair treatment of Example 28 was excellent in the moisturizing action of the hair and was excellent in usability.

Example 29 Amount of Cream Ingredients (% by Weight) (1) Residual amount of purified water (2) Lipid complex described in Example 11 10.0 (3) Sodium lactate 1.0 (4) 1 , 3-butylene glycol 4.0 (5) liquid paraffin 5.0 (6) cetyl-2-ethylhexanoate 5.0 (7) pentaerythritol tetra-2-ethylhexanoate 3.0 (8) methyl Phenylpolysiloxane 3.0 (9) Decamethylcyclopentasiloxane 10.0 (10) Silicone oil rubber powder * 1 2.0 (11) Dimethylsilylated silicic anhydride * 2 2.0 (12) Polyether-modified silicone * 3 2.0 (13) Zinc stearate 2.0 (14) Vitamin E-acetate suitable amount (15) Methylparaben proper amount * 1: Toray Dow Corning Silicone Co., Ltd. Trefil E-505C (trade name) * 2: Japan Aeroge Aerosil R-972 (trade name) * 3: Silicon SC9450N (trade name) manufactured by Shin-Etsu Silicone Co., Ltd. <Process> An oil obtained by mixing (5) to (9) and (12) to (16) at room temperature. The powder was uniformly dispersed while gradually adding the powders (10) and (11) to the phase. After that, (1) plus (3) is added to (2)
An aqueous phase obtained by adding (15) to (4) was gradually added to the oil phase and uniformly dispersed with a homomixer. Then, emulsified particles were prepared to obtain a cream. The cream of Example 29 was excellent in usability and drug stability.

Example 30 Cream Blending Amount (% by Weight) (1) Remaining Purified Water (2) Glycerin 5.0 (3) 1,3-butylene glycol 4.0 (4) Described in Example 11 50.0 (5) Water-swelled clay mineral * 1 2.0 (6) Benzyldimethylstearylammonium chloride 1.0 (7) Isostearic acid 1.0 (8) Decamethylcyclopentasiloxane 22.0 ( 9) Carboxymethylcellulose 1.0 (10) Citric acid 0.05 (11) Sodium citrate 0.5 (12) Methylparaben 0.1 (13) Flavoring appropriate amount * 1: Vegum (Vegum Bilt) (brand name) < Production method> (5) was dispersed in ethanol, (6) was added thereto, and the mixture was heated to 50 ° C. and dispersed with a disper. This was sufficiently dried to remove the ethanol to obtain an organically modified clay mineral. Next, (7) was added to this organically modified clay mineral, kneaded twice with a roller having a pressure of 15 kg / cm, and then (8) and (13) were added to prepare an oil phase. 1) ~
A cream was obtained by gradually adding the aqueous phase obtained by mixing (4) and (9) to (12) under stirring with a homomixer. The cream of Example 30 was excellent in usability and drug stability.

[0062]

According to the present invention, it has an excellent moisturizing and protective effect on skin and hair, and further contains a drug,
Provided are a lipid complex capable of sustained release of this drug, and an external composition containing the same.

 ──────────────────────────────────────────────────続 き Continued on the front page F term (reference) 4C083 AB032 AB172 AB442 AC012 AC022 AC071 AC072 AC102 AC122 AC172 AC182 AC242 AC302 AC352 AC422 AC532 AC612 AC662 AC682 AC692 AC782 AC792 AD042 AD152 AD162 AD172 AD272 AD352 AD392 AD491 AD492 AD662 AD702 BB01 CC01 CC04 CC05 CC31 DD23 DD31 EE01 EE06 EE12 EE28 FF05

Claims (7)

[Claims] 1. A lipid complex comprising (A) a surfactant, (B) an amphipathic substance and (C) a sterol as constituents. 2. The lipid complex according to claim 1, wherein the lipid complex is a vesicular lipid membrane capable of containing (D) an aqueous phase. 3. A surfactant, (B) an amphiphile,
(C) a sterol and (D) the aqueous phase, the following 1. ~ 3 . According to claim 2, wherein the lipid complexes: 1. (A) and (B) are surfactants-amphiphiles-
It is selected from combinations capable of forming a gel at a temperature not lower than room temperature in an aqueous system. 2 . When the weight ratio of (A) and (B) is (A) :( B) =
1: 5 to 5: 1, and the sum of (A) and (B) and the weight ratio of (C) are (A) + (B) :( C) = 10: 1
１1: 1. 3 . The sum of (A), (B) and (C) and the weight ratio of (D) are (A) + (B) + (C) :( D) = 0.1: 9
9.9 to 30:70. (A) a surfactant comprising an N-long-chain acyl acid amino acid salt, a fatty acid soap, a monoalkyl phosphate, a quaternary alkyl ammonium salt, a POE alkyl ether carboxylate, an acylmethyltaurine salt;
One or more surfactants selected from the group consisting of alkyl sulfate salts, hydroxyalkyl ether carboxylate salts and nonionic surfactants having a linear alkyl chain and an HLB value of 10 or more, Claim 1
The lipid complex according to claim 3. 5. The (B) amphiphilic substance contains a higher alcohol having at least 16 carbon atoms in the alkyl chain.
The lipid complex according to any one of claims 1 to 4. 6. The lipid complex according to claim 1, wherein (C) the sterol is cholesterol and / or phytosterol. 7. An external composition comprising the lipid complex according to any one of claims 1 to 6.