JPS63305930A - Emulsion composition - Google Patents

Abstract

PURPOSE:To stabilize emulsion and to enable a pH region to be freely controlled by blending higher fatty acid and its salt or the like with bile acid and its salt. CONSTITUTION:Bile acid and/or its salt (component A) such as deoxycholic acid, sterol (component B) such as cholesterol, higher fatty acid and/or its salt (component C) such as caprylic acid and glycerin monofatty acid ester such as glyceryl monostearate and/or glycerin difatty acid ester (component D) are blended and the amount of the component A to be blended is regulated to 0.05-5wt.% and the amounts of the components B, C and D to be blended are regulated respectively to 0.1-3, 0.01-3 and 0.1-3 by weight ratio when the amount of the component A to be blended is regulated to 1. Thereby the stability of emulsion is made excellent. Further the pH region can be freely controlled to weak basicity from weak acidity by controlling the amounts to be blended of bile acid and/or its salt and higher acid and/or its salt.

Description

Detailed Description of the Invention [Industrial Field of Application] The present invention uses bile acid and/or its salt, which is known as a highly safe natural surfactant, as an emulsifier to produce cosmetics,
Application to pharmaceuticals is ``one purpose.''

[Prior Art] In recent years, much research has been conducted on emulsification, and a large number of emulsifiers have been developed. However, many general consumers have concerns about safety, and the use of biologically derived substances with surface activity is also being considered.

Natural surfactants such as bile salts are highly hydrophilic;
Generally, it has been difficult to use it as an emulsifier. Therefore, an emulsification method has been proposed in which bile acids and/or their salts are dissolved in a water-soluble polyhydric alcohol having two or more hydroxyl groups in the molecule, oil is added thereto, and water is further added ( (Japanese Unexamined Patent Publication No. 141510/1983).

[Problems to be Solved by the Invention] However, the oil-in-water emulsion composition disclosed in JP-A-59-141510 requires extensive use of water-soluble polyhydric alcohol due to its manufacturing method, and as seen from the examples. Ba,
More than 20% by weight should preferably be used. For this reason, emulsified compositions have been sensory-limited.

Moreover, it was not preferable in terms of safety for the skin and the like.

In addition, if bile acids and bile salts are not sufficiently converted into salts, their solubility in water may be insufficient, and crystal precipitation may occur over time. In addition, when bile acids are applied to emulsified compositions in the form of salts, in most cases the pH of the emulsified composition is
is in the neutral to alkaline range, making it difficult to apply it in the weakly acidic range.

[Means for solving the problems] In view of the above points, the present inventors aimed to effectively utilize bile acids and bile salts, which are highly safe natural surfactants, as emulsifiers, and to overcome the above drawbacks. As a result of intensive research to obtain an emulsified composition, we found that bile acids and/or their salts, styrene, higher fatty acids and/or their salts,
A stable emulsion can be obtained by emulsifying an oily component and an aqueous component at a specific ratio with chrycerin monofatty acid ester and/or glycerin difatty acid ester, and
The present invention was completed based on the discovery that an emulsified composition in which the H region can also be freely controlled can be obtained.

The configuration of the present invention will be described below.

The bile acid used in the present invention is one of the carboxylic acids having a steroid skeleton, and is an acid that exists as a component of animal bile. It also includes so-called conjugated bile acids which are amide-bound with glycine or taurine.

For example, cholicocholic acid, taurocholic acid, cholic acid,
Examples include deoxycholic acid, lithocholic acid, and chenodeoxycholic acid, and these can be used alone or in combination of two or more.

When the bile acid is used as a salt, the salt-forming substances include inorganic bases such as sodium hydroxide, potassium hydroxide, and ammonium hydroxide, sodium ions,
Basic inorganic salts and basic organic salts containing potassium ions, ammonium ions, etc., basic amino acids such as arginine, lysine, histidine, ornithine, and basic oligopeptides having these as residues, monoethanolamine, jetanolamine, Basic amines such as triethanolamine, aminomethylpropatool, amizmedelpropanediol, etc. are used singly or in combination of two or more. The salt may be reacted in advance to form a salt and then added, or may be added separately and reacted during the manufacturing process of the emulsion composition to form a salt.

Styrene used in the present invention is a type of steroid, and is a steroid alcohol widely distributed in the animal and plant kingdoms.

Examples of animal styrol include cholestyrol, plant styrol includes cytostyrene, and fungal styrol includes ergosterin. Cholestyol is particularly advantageous economically. These may be one or more types.
Used in combination with L.

The higher fatty acids used in the present invention have 8 to 26 carbon atoms, and can be either natural fatty acids or synthetic fatty acids, straight chain saturated fatty acids, straight chain unsaturated fatty acids, branched saturated fatty acids, or branched unsaturated fatty acids. It's okay. For example, examples of straight chain saturated fatty acids include caprylic acid, pelargonic acid, capric acid, lauric acid, myristic acid, valmitic acid, margaric acid, stearic acid, arachidic acid, behenic acid, lignoceric acid, and cerotic acid. In addition, as linear unsaturated fatty acids, caproleic acid, lindelic acid, lauroleic acid, tuzunic acid, myristoleic acid, palmitoleic acid, petroselic acid, oleic acid, elaidic acid, basenic acid, linoleic acid, linoelaidic acid, eleostearin Examples of the acid include lyrinic acid, lyrunelaidic acid, pseudoeleostearic acid, valinaric acid, bondoic acid, arachidonic acid, erucic acid, curbanodonic acid, and the like. Furthermore, examples of branched fatty acids include 2-ethylhexanoic acid, invalmitic acid, isostearic acid, neodecanoic acid, neotridecanoic acid, and lanolin fatty acid. These can be used alone or in combination of two or more.

When the above-mentioned higher fatty acids are used as salts, the substances forming the salts include inorganic bases such as sodium hydroxide, potassium hydroxide, and ammonium hydroxide, and basic inorganic salts containing sodium ions, potassium ions, ammonium ions, etc. and basic organic salts, arginine, lysine,
Basic amino acids such as bistidine and ornithine, basic oligopeptides having them as residues, basic amines such as monoethanolamine, jetanolamine, triethanolamine, aminomethyl propatool, amizmedel propanediol, etc. It is used either as a species or as a combination of two or more species. The salt may be added after being subjected to a caustic reaction to form a salt, or may be added separately and reacted during the manufacturing process of the emulsion composition to form a salt.

The glycerin monofatty acid ester and glycerin difatty acid ester used in the present invention are obtained by partially esterifying glycerin with a higher fatty acid. The constituent higher fatty acids have 8 to 26 carbon atoms, and may be any of linear saturated fatty acids, linear unsaturated fatty acids, branched saturated fatty acids, and branched unsaturated fatty acids.

Preferred glycerin monofatty acid esters and glycerin difatty acid esters include, for example, glyceryl monocaprylate, glyceryl monomyristate, glyceryl monostearate, glyceryl monooleate, glyceryl monoisostearate, glyceryl monopalmitate, and glyceryl monostearate. Palmitooleate, chryceryl monolinoate, glyceryl monoarachitoate, glyceryl monolisinate, glyceryl monodocosahexaate, chryceryl monopentadecanate, chryceryl distearate, glyceryl dioleate, chryceryl dipalmitate , glyceryl dioxystearate, glyceryl dipalmitoleate, glyceryl silidinoate, glyceryl diisopalmitate, chryceryl diisostearate, glyceryl dialachinate, glyceryl dilinoate, and the like. These can be used alone or in combination of two or more.

The amount of bile acid and/or its salt is preferably 0.05 to 5% by weight, and within this range, an emulsified composition can be obtained that makes full use of its emulsifying power.

Styrene (component B), higher fatty acid and/or its salt (component C), glycerin monofatty acid ester and/or
Alternatively, the amount of glycerin difatty acid ester (component D) is within the range shown below in terms of weight ratio to the amount of bile acid and/or its salt (component A). B component, C component, and D component are respectively 0.1 to 3, 0, and O for A component 1.
2N2.0.1 to 3 are preferred. Within this range, each component will have a favorable effect on each other, and the oily component and aqueous component will be emulsified well, and no crystal precipitation of bile acids will be observed over time. It seems that each component forms an interfacial complex compound at the interface of the emulsion to stabilize the emulsion.

The method for producing an emulsified composition of the present invention involves heating bile acid and/or its salt, styrene, higher fatty acid and/or its salt, glycerin monofatty acid ester and/or glycerin difatty acid ester, and oily component. The heated aqueous component may be added to the dissolved and uniformly mixed mixture to emulsify it. After that, the process is completed by cooling to about room temperature. Also, during emulsification, reverse the order of addition.
An oil-based component may be added to the water-based component.

In addition, in the emulsified composition of the present invention, the pH of the emulsified composition can be freely controlled to be weakly acidic, neutral, or weakly alkaline by adjusting the blending amounts of bile salts and higher fatty acid salts. In particular, it is possible to obtain an emulsified composition with a pH of 4 to 6, which is close to the pH of the skin, which has been difficult to apply in the past. Also, the stability of the emulsified composition is determined at any pH.
It is also good in terms of

Bile acids and/or their salts, styrene, higher fatty acids and/or their salts, glycerin monofatty acid esters and/or glycerin difatty acid esters, which are essential components of the present invention, are all biologically related substances. The safety of the emulsified composition is also high.

Since the present invention is an emulsified composition, the oily component used is an oily agent commonly used in the cosmetics, pharmaceutical, and other industries. The blending amounts of the oily component and the aqueous component may be appropriately selected depending on the intended emulsified composition.

In addition to the above ingredients, the emulsified composition of the present invention further includes pigments, dyes, burrs, fragrances, moisturizing agents, etc. commonly used in cosmetics and pharmaceuticals, within a range that does not impede the effects of the present invention. Preservatives, beauty agents, drugs, antioxidants, ultraviolet absorbers, water-soluble polymers, oil-soluble polymers, alcohol, powder, and the like can be blended as appropriate.

[Example] Next, the present invention will be further explained with reference to Examples.

These do not limit the invention in any way.

Examples [1] to [12], Comparative Examples [1] to [6] Examples [1] to [12], Comparative Examples [1] to [6]
Table 1 also shows the prescription. The blending amounts in the table are weight %. For each Example and Comparative Example, the pH at room temperature and the particle size of the emulsion were measured on the day of production. Furthermore, the stability over time was checked after one month at 40°C.

The results are also shown in Table 1.

(Margin below) Table 1 Table 1 (continued) Table 1 attached) (Manufacturing method) A(1) to (7) are heated and dissolved at 75°C.

Heat B(8) at 75°C.

Add B to CA and emulsify.

Finish by cooling the DC to 35°C.

As is clear from the results in Table 1, Examples [11
- [12], emulsified compositions having various pH values from weakly acidic to weakly alkaline and having fine particle sizes were obtained. Furthermore, the stability over time after one month at 40°C was also good.

On the other hand, the product that does not contain styrene, which is an essential component of the present invention (Comparative Example [1]), has poor stability over time. Furthermore, in the case where higher fatty acids and/or their salts are not blended (Comparative Example [2]), not only is it not possible to obtain an emulsion with a fine particle size, but the stability over time is also poor. The one containing a small amount of bile acid (Comparative Example [3]) not only does not provide an emulsion with a uniform particle size, but also has poor stability over time.

Comparative example [4]) with a small blending ratio of styrene is
Although an emulsion with a fine particle size can be obtained, the stability over time is poor. Furthermore, those containing a small blending ratio of higher fatty acid salts (Comparative Example [5]) also have poor stability over time. Those with a low blending ratio of glycerin monofatty acid ester (Comparative example [6]
), it is not possible to obtain an emulsion with a fine particle size, and the stability over time is also poor.

Example [13] Emulsion (formulation) (wt%) (1)
Dehydrocholic acid 1.0 (2) Cholestyrol 0.4 (3) Potassium oleate 0.1 (4) Glyceryl monooleate 1.0 (5) Macadamian nut oil
l000 (6) Lecithin
0.5 (7) Estradiol
0.001(8) Retinol Valmitate 0
．． 1 (9) Fragrance 0.1 (
10) Sodium chondroitin sulfate 0.2 (11
) Preservative 0.1 (12) Grain ice making Remaining amount (manufacturing method) A Heat and melt (1) to (9) at 75°C.

B. Heat and dissolve (10) to (12) at 75°C.

Add A to CB and emulsify.

Cool the DC to 35°C to obtain an emulsion.

The emulsion obtained as described above has an emulsion particle size of 0.
It was extremely fine and uniform with a thickness of 5 μm, had a rich feel on use, and had a good texture that blended well with the skin. The pH of the emulsion is 5.
It was weakly acidic with a rating of 7 and had excellent stability over time.

Example [14] Cream (prescription) (wt%) (1)
Deoxycholic acid 2.5 (2) Cholestyrol 1.0 (3) Stearic acid 20 (4) Glyceryl monostearate 5.0 (5) Squalane
2.0(6) Cetyl 2-ethylhexanoate
6.0 (7) Glyceryl Triinstear 12.
0 rate (8) stearyl alcohol 3, 0 (9)
Ethinyl estradiol 0.05 (10) d1-α-tocopherol acetate 0.2 (11) Fragrance 0.2 (12) Glycerin 1O90 (13) Sodium hydroxide 0.04 (14) Potassium hydroxide 0.04 (15) Preservative
0.1 (+6) Bantothenyl ethyl ether 0.05 (17) Sodium chondroitin sulfate 0.1 (18) Glycine
0.25 (19) Purified water
Remaining amount (manufacturing method) A (+) to (11) are heated and dissolved at 70°C.

B. Heat and melt (+2) to (19) at 70°C.

Add B to CA and emulsify.

Cool the DC to 35°C to obtain the cream.

The cream obtained as described in I- below has an emulsion particle size of 0.5 μm, is extremely fine and uniform, and has a glossy, fine-grained and beautiful appearance. When applied to the skin, it applied lightly and smoothly, felt rich, and had a good L/X feel to the skin. Cream 10% aqueous dispersion p
H is neutral at 7.2 and has excellent stability over time, reaching 1.
/)is.

Example [15] Lotion (prescription) (wt%) (1)
Cholic acid 0.2 (2) Cholestirol 0.1 (3) Glyceryl monostearate 0.2 (4) Avocado oil
0.2 (5) Fragrance
0.1(6) Potassium stearate 0
．． 2 (7) Glycerin 5.0 (8
) Pigment Appropriate amount (9) Purified water Remaining amount (manufacturing method) Dissolve A(1) to (5) by heating at 70°C.

B(6) to (9) are heated and dissolved at 70°C.

Add B to CA and emulsify.

Cool the DC to 35°C to obtain the lotion.

The lotion thus obtained had a uniform emulsion particle size of 1 μm, had good staining on the skin, and had a moist skin effect. The pH of the lotion is 7.
It was neutral with a rating of 5 and had excellent stability over time.

[Effects of the Invention] As detailed above, the emulsified composition of the present invention is an emulsified composition in which bile acids and bile salts, which are highly safe natural surfactants, are used as emulsifiers. A uniform emulsion can be obtained and its stability over time is also excellent. In addition, by adjusting the blending amounts of bile salts and higher fatty acid salts, the pH of the emulsified composition can be freely controlled from weakly acidic to weakly alkaline.
Furthermore, sufficient stability is maintained in any pH range.

that's all

Claims (1)

[Claims] (1) Bile acid and/or its salt (A component), styrene (B component), higher fatty acid and/or its salt (C component), glycerin monofatty acid ester and/or
or glycerin difatty acid ester (component D), and the blending amount of component A is 0.05 to 5% by weight, and further, when the blending amount of component A is 1, component B, C
The amount of component D is 0.1 to 3 by weight, respectively.
0.01-3, an emulsified composition characterized in that it is 0.1-3.