JP2003212751A - Gel composition and oil-in-water (o/w) composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a composition having a high gel-forming ability, a high forming ability of an oil-in-water (O/W) composition, excellent retention of an oil, capable of forming fine vesicles by regulating the amount of the oil, highly safe for living bodies, having excellent stability of the composition with time and preventing effects on skin roughening and assuming various forms of a gel, a cream having a transparent to a clouded appearance, a low- to a high-viscosity solution, etc. <P>SOLUTION: This composition comprises a compound represented by general formula 1 (R<SB>1</SB>and R<SB>2</SB>are one or more selected from hydrogen, an alkyl group, an acyl group, ethylene oxide, an alkali metal, an alkaline earth metal or the like, respectively) and/or its salt. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to a gel composition and an oil-in-water (O / W) type composition characterized by containing a compound represented by the general formula 1 and / or a salt thereof. More specifically, by containing the compound represented by the general formula 1 and / or a salt thereof, it is possible to form an oil-containing gel composition, and further by diluting the gel composition with water. It relates to being able to obtain a homogeneous and stable emulsion composition. In addition, various oil-in-water (O / W) compositions such as micelles, vesicles and emulsions can be prepared according to the purpose by adjusting the type and amount of oil to be blended.

[0002]

2. Description of the Related Art In recent years, from the viewpoint of human safety, studies have been made to reduce the amount of the surface-active substance used as an emulsifier in a preparation or to use a milder one. Under such circumstances, studies have been conducted to make substances having beneficial physiological activity, so-called active ingredients, even play a role of emulsifiers.

Further, regarding a preparation to be applied externally to humans,
In addition to excellent stability over time, low irritation to the skin and high safety, it is also required to improve percutaneous absorption of the active ingredient and improvement in the pharmacokinetics of the active ingredient, including skin intracellular enrichment. Has been.

[0004]

[Problems to be Solved by the Invention] In such a situation,
What is required of external preparations for skin such as cosmetics is that a gel composition can be formed by a component having a beneficial physiological activity, and further, by adding water to the gel composition, it is possible to efficiently use a physically weak stirring force. The formation of fine emulsified particles that are stable over time, and at the same time, low irritation to the skin.

[0005]

Means for Solving the Problems The inventors of the present invention have made extensive studies in view of such circumstances, and as a result, by containing the compound represented by the general formula 1 and / or a salt thereof, the self-organizing ability is high, Excellent stability over time, high oil emulsifying ability, low irritation to the skin and high safety,
The invention of a gel composition and an oil-in-water (O / W) type composition was completed.

That is, the gel composition and the emulsified composition of the present invention contain the compound represented by the general formula 1 and / or a salt thereof and have high self-organizing ability.
The composition is excellent in stability over time, has a high oil emulsifying ability, has low irritation to the skin, and is highly safe.

The structure of the present invention will be described in detail below.

The substance represented by the general formula 1 used in the present invention is a compound having a chroman skeleton and having a very effective protective effect against rough skin. These compounds have excellent antioxidant ability, prevent the harmful effects of active oxygen in the body, lipid peroxides and free radicals derived from them, and exert a hair growth and hair growth effect by a physiologically active action represented by blood circulation promotion. Or, for example, coexistence with vitamins and their derivatives can synergistically improve each other's effectiveness.

Specifically, each of R ₁ and R ₂ is selected from one or more of hydrogen, an alkyl group, an acyl group, ethylene oxide, an alkali metal, an alkaline earth metal and the like, and may be combined if necessary. Physical properties such as solubility, gel-forming property and self-association property can be changed by these selections.

In the compound represented by the general formula 1 used in the present invention, at least one of R ₁ and R ₂ is preferably sodium. Further, the content is not particularly limited, but is preferably 0.1 to 25% by weight, and if less than 0.1% by weight, a stable gel composition having poor physiological activity, gel forming ability and emulsifying ability and An oil-in-water (O / W) type composition may not be obtained in some cases, and the content of more than 25% by weight is possible, but it is not economical as a gel composition and an emulsion composition.

Further, the role of glycerin in the present invention is very important. The compound represented by the general formula 1 has the ability to form a gel or an oil-in-water (O / W) type composition alone, but the addition of glycerin improves its dispersibility. It will be possible to fully utilize the potential of the. The blending amount is not particularly limited, but is preferably 0.5 to 60%,
If it is less than 0.5%, a remarkable effect may not be recognized in some cases, and if it exceeds 60%, it may be blended, but it may be disadvantageous because it feels sticky in use.

The preparation of the gel is not particularly limited, but a method of forming a gel by thoroughly mixing General Formula 1 with glycerin and adding oil to this state while stirring little by little is preferable. It is possible to form a gel by other methods as well, but since it requires treatment at high temperature or mechanical shearing share, it is easy and safe to use the above method. It becomes possible to produce a gel.

In addition to the above-mentioned essential components, the composition of the present invention may contain various components such as cosmetics, quasi drugs, pharmaceuticals and the like which are commonly used in external preparations for skin, and components which are used in foods. . For example, oily ingredients, lipids, humectants, thickeners, medicinal ingredients, bactericidal / preservatives, pigments, powders, pH adjusters, UV absorbers, antioxidants, plasticizers, fragrances, amino acids, sweeteners, colorants. Etc. can be blended appropriately. Further, other surfactants can be blended in the role of assisting gel forming ability and emulsifying ability.

Specific examples of the oily component include hydrocarbons, plant-derived oils, insect-derived oils, animal fats and oils, triglycerides, higher alcohols, fatty acids, esters of higher alcohols and fatty acids, silicone oils and the like. Examples of the moisturizer include polyhydric alcohols, high molecular polysaccharides, plant extracts, and metabolites of microorganisms. Examples of the thickener include carboxyvinyl polymers, xanthan gum, methylcellulose, polyvinylpyrrolidone, gelatin, clay minerals such as bentonite, and the like. Examples of the medicinal component include various vitamins and their derivatives, allantoin, glycyrrhizic acid and its derivatives, various animal and plant extracts, and the like. Further, as the emulsifier, for example, polyoxyethylene alkyl ether,
Polyoxyethylene fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sorbitan fatty acid ester, glycerin fatty acid ester, polyglycerin fatty acid ester, nonionic surfactant such as polyoxyethylene hydrogenated castor oil, anionic surfactant such as sodium stearoyl lactylate, Examples thereof include amphoteric surfactants such as phospholipids and cationic surfactants such as alkyltrimethylammonium chloride.

The gel composition of the present invention and oil-in-water (O /
The W) type composition can be produced by a known method,
It can be used regardless of the fields of cosmetics, quasi drugs, external medicines, foods, etc., and its dosage form can be arbitrarily selected according to the purpose, and creams, emulsions, lotions, gels, ointments, packs, sticks can be used. And the like.

[0016]

The gel composition of the present invention and the oil-in-water (O /
The W) type composition contains a compound represented by the general formula 1 and / or a salt thereof, and has a beneficial physiological activity as compared with a conventionally generally used surfactant. It has excellent gelling ability and oil retaining ability, and it forms micelles, vesicles, and emulsified particles by adjusting the compounding ingredients, and it has excellent stability over time. Furthermore, it has low irritation to the skin and high transdermal absorbability. Therefore, it is highly safe and can be enriched in the cells of the skin.

In order to demonstrate these effects, Examples 1 to 1
16 was prepared and evaluated.

Prior to the examples, the gelation method and the emulsification method used in the present invention will be described.

(Gelification method) The following formula was used to formula 1
After thoroughly stirring the compound shown in (1) and glycerin (part A) at room temperature, the oil phase (part B) which was heated to 60 ° C. and also heated to 60 ° C. was gradually added to part A while stirring. Then, it cooled to room temperature and obtained the gel composition.

A compound represented by the general formula 1 Glycerin B Glyceryl trioctanoate

[Results] As shown in Table 1, the compound represented by the general formula 1 was shown to have a good gel-forming ability. It was also shown that this gel-forming ability was further improved by the addition of glycerin.

[0022]

[Table 1]

(Emulsification Method) In the following formulation, the compound represented by the general formula 1 and an appropriate amount of glycerin (part A) were thoroughly stirred at room temperature, and then heated to 60 ° C. and also to 60 ° C. The oil phase (part B) is gradually added to part A with stirring. Thereafter, an aqueous phase (part C) heated to 70 ° C. was added, the rest of glycerin was added, and the mixture was cooled to room temperature with stirring and oil-in-water (O /
A W) type emulsion composition was obtained.

A compound represented by the general formula 1 Glycerin B Neopentyl glycol dicaprate C Propylene glycol Preservative purified water

[Results] As shown in Table 2, it was shown that the compound represented by the general formula 1 had a good oil-in-water (O / W) type composition forming ability. It was also shown that this gel-forming ability was further improved by the addition of glycerin.

[0026]

[Table 2]

As described above, according to the present invention, by containing the compound represented by the general formula 1 and / or a salt thereof, a gel composition having a high oil emulsifying ability and excellent stability over time and It becomes possible to provide an oil-in-water (O / W) type composition. Furthermore, it has been found that a better composition can be obtained by adding glycerin.

[0028]

EXAMPLES The present invention will now be described with reference to examples, but the present invention is not limited thereto.

Example 13 Moisturizing Gel Cream A Compound represented by General Formula 1 (sodium for R ₁ and R ₂ ) 2.0% by weight Glycerin 5.0 B Squalane 40.0 Octyldodecyl myristate 59.5 Stearyl alcohol 2 0.0 Cetanol 1.0 Ascorbic acid dipalmitate Suitable amount Perfume Suitable amount

A gel composition is obtained by gradually adding, with stirring, Part B, which is completely and uniformly dissolved, to Part A that has been well mixed. The obtained gel composition was excellent in stability over time, had low irritation to the skin, and was a good moisturizing gel cream.

Example 14 Lotion 1 A Compound represented by the general formula 1 (either R ₁ or R ₂ is sodium, the other is hydrogen) 2.0% by weight B glycerin 30.0 C propylene glycol 5.0 ascorbic acid Glucoside 0.5 Hydrogenated lecithin 1.0 Pentylene glycol 5.0 Fragrance D Sodium hydroxide pH adjustment Purified water Residual

Part A is dissolved in part B. Add part of part D to part C and dissolve uniformly. After they are uniformly dissolved, they are mixed and the total amount is adjusted to 100% in part D. The obtained lotion is a slightly turbid oil-in-water (O / W) type suspension lotion containing fine vesicles having a particle size of several tens to several μm.
It has excellent stability over time and penetration into the skin, and prevents skin roughening.

Example 15 Lotion 2 A Compound represented by the general formula 1 (both R ₁ and R ₂ are sodium) 2.0% by weight B propylene glycol 5.0 C retinol palmitate 0.1 preservative proper amount perfume proper amount D Purified water Residual

After dissolving part A in part B, part C which has been uniformly mixed is added, and finally part D is added. The mixed liquid is treated with an ultra-high pressure jet flow inversion type emulsification device (trade name: DeBee2000). The obtained lotion is a slightly turbid oil-in-water (O / W) type suspension lotion containing fine vesicles having a particle size of 0.1 to several tens of μm, and has excellent stability over time and skin permeability. , Well prevented the skin.

Example 16 Lotion 3 A Compound represented by General Formula 1 (both R ₁ and R ₂ are sodium) 2.0 wt% B glycerin 10.0 C propylene glycol 5.0 retinol palmitate 0.1 preservative Agent Suitable amount Perfume Suitable amount D Purified water Residual

After dissolving the A part in the B part, the uniformly mixed C part is added, and finally the D part is added. The mixed liquid is treated under the same conditions as in Example 15 in an ultrahigh pressure jet flow inversion type emulsification device (trade name: DeBee2000). The obtained lotion contains finer vesicles than the particle size obtained in Example 15, such as a particle size of several tens nm, and is a slightly turbid oil-in-water (O / W) type suspension lotion, which has a permeability to the skin. Excellent in preventing the skin from getting rough. However, the stability over time was superior to that of Example 15, showing the merit of incorporating glycerin.

   ─────────────────────────────────────────────────── ─── Continued front page    (72) Inventor Jiro Kitahara             2-7 Torimicho, Nishi-ku, Nagoya-shi, Aichi Japan             Nard Cosmetics Co., Ltd. (72) Inventor Satoru Nakata             2-7 Torimicho, Nishi-ku, Nagoya-shi, Aichi Japan             Nard Cosmetics Co., Ltd. F-term (reference) 4C083 AB032 AB051 AB052 AC022                       AC072 AC121 AC122 AC352                       AC901 AC902 AD572 AD622                       AD642 CC05 DD33 DD41                       EE01 EE10 EE12 EE22 FF05

Claims (7)

[Claims] 1. A compound containing a chroman skeleton represented by the general formula 1 (R ₁ and R ₂ are each selected from hydrogen, an alkyl group, an acyl group, ethylene oxide, an alkali metal, an alkaline earth metal and the like) and And / or a salt thereof. [Chemical 1] 2. The gel composition according to claim 1, which contains 0.5 to 60% by weight of glycerin. 3. A compound containing a chroman skeleton represented by the general formula 1 (R ₁ and R ₂ are each selected from hydrogen, an alkyl group, an acyl group, ethylene oxide, an alkali metal, an alkaline earth metal and the like) and The gel composition according to claim 2, which is prepared by a method of mixing // its salt and glycerin, and then adding oil with stirring. 4. An emulsified composition obtained by adding water to the gel composition according to claim 1 to emulsify it. 5. A compound containing a chroman skeleton represented by the general formula 1 (R ₁ and R ₂ are each selected from hydrogen, an alkyl group, an acyl group, ethylene oxide, an alkali metal, an alkaline earth metal and the like) and And / or an oil-in-water (O / W) type composition containing a salt thereof. 6. The oil-in-water (O / W) type composition according to claim 4, wherein glycerin is added in an amount of 0.5 to 60% by weight. 7. The composition according to claim 1, wherein the compound of the general formula 1 and / or its salt is compounded in an amount of 0.1 to 25% by weight.