JP2002012518A - Hair cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a new solubilizing means for a sparingly water-soluble active ingredient in a skin care preparation in a solubilized form, especially a skin care preparation for the hair. SOLUTION: This skin care preparation for the hair in the solubilized form is obtained by solubilizing the sparingly water-soluble active ingredient with a nonionic surfactant and a phospholipid.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a skin external preparation suitable for cosmetics, and more particularly to a solubilized form of a skin external preparation containing a poorly water-soluble active ingredient.

[0002]

2. Description of the Related Art In the field of external preparations for skin such as cosmetics and external preparations for skin, many of those active ingredients have poor water solubility. For this reason, in formulating skin external preparations, the greatest challenge is to uniformly disperse or solubilize them. In preparing such a formulation, when such a poorly water-soluble active ingredient is contained, an emulsified formulation such as an emulsion or cream is used, but depending on the formulation characteristics, such an emulsified system may be used. It may be difficult.
Examples of such preparations include hair growth cosmetics and hair growth skin external medicine. In these, when the emulsifying agent form is used, the hair may become sticky, or the hair may be wet with an oily component. However, there has been no choice but to use a solubilizing agent type system. However, in such a solubilizing system, the amount of the active ingredient solubilized is limited, and further improvement of the solubilizing means has been desired. Furthermore, in recent years, the amount of ethanol used as a solubilizing aid has also tended to be limited from the viewpoint of environmental conservation, and it is desired to improve solubilizing means with a small amount of ethanol-containing system. I was This improvement was particularly evident in systems with a high ethanol content, such as hair tonics.

On the other hand, in a solubilized form of a skin external preparation,
No formulation containing a poorly water-soluble active ingredient, a nonionic surfactant and a phospholipid has been known at all.

[0004]

DISCLOSURE OF THE INVENTION The present invention has been made under such circumstances, and in a solubilized form of a skin external preparation, a novel water-insoluble active ingredient for a skin external preparation for hair. It is an object to provide a solubilizing means.

[0005]

In view of such circumstances, the present inventors have sought a new means for solubilizing a poorly water-soluble active ingredient in a skin external preparation, particularly for a solubilized form of a skin external preparation. As a result of diligent research efforts, they have found that such a solubilization can be achieved by adding a poorly water-soluble active ingredient, a nonionic surfactant and a phospholipid to a skin external preparation, and have developed the invention. It was completed. That is, the present invention relates to the following technology. (1) A solubilized form of a skin external preparation comprising a sparingly water-soluble active ingredient, a nonionic surfactant and a phospholipid. (2) The skin external preparation according to (1), wherein the content of ethanol is 40% by weight or less. (3) The skin external preparation according to (1) or (2), wherein the content of the nonionic surfactant is 1% by weight or less. (4) the poorly water-soluble substance is a hair restorer;
(1) The external preparation for skin according to any one of (1) to (3). (5) (1) to (4) characterized by being a cosmetic.
An external preparation for skin according to any one of the preceding claims. (6) (1) to (5) characterized by being for hair
An external preparation for skin according to any one of the preceding claims. Hereinafter, the present invention will be described in detail focusing on embodiments.

[0006]

DESCRIPTION OF THE PREFERRED EMBODIMENTS (1) Phospholipid as an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention is characterized by containing a phospholipid as an essential component. The phospholipids that can be used in the external preparation for skin of the present invention can be used without any particular limitation as long as they are usually used in external preparations for skin.
Preferred examples thereof include lecithin, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, and lyso forms thereof. These may be used alone or in combination of two or more. Among them, particularly preferred is lecithin which has been used frequently. Lecithin may originate from a plant like soybeans or from an animal like egg yolk. In the skin external preparation of the present invention, these phospholipids work together with a nonionic surfactant described later, and have an action of solubilizing a poorly water-soluble active ingredient.
Here, solubilization in the present invention means forming small micelles that do not scatter light and forming a one-phase system having a transparent appearance, and does not include preparations such as liposomes and niosomes. The preferred content of these phospholipids in the skin external preparation of the present invention is 0.05 to the total amount of the skin external preparation.
To 2% by weight, more preferably 0.1 to 1% by weight. This is because if the amount of the phospholipid is too large, it may deviate from the solubilization zone, and if it is too small, the solubilization may not be possible.

(2) Nonionic surfactant which is an essential component of the external preparation for skin of the present invention The external preparation for skin of the present invention is also characterized by containing a nonionic surfactant. Here, as the nonionic surfactant that can be used in the skin external preparation of the present invention, HLB is 10 to 2
A hydrophilic nonionic surfactant of 0 is preferred, for example,
Polyoxyethylene alkyl ether, polyoxyethylene fatty acid ester, polyoxyethylene polyoxypropylene alkyl ether, polyoxyethylene polyoxypropylene fatty acid ester, polyoxyethylene hardened castor oil, polyoxyethylene castor oil, polyoxyethylene polyoxypropylene alkyl ether, Preferred examples include sorbitan fatty acid esters. Of these, particularly preferred are polyoxyethylene / polyoxypropylene-2-decyltetradecyl ether,
Polyoxyethylene phytostanol and sorbitan monolaurate. Taking into account the addition mole number of the alkylene oxide, polyoxyethylene (20) polyoxypropylene (6) -2-decyltetradecyl ether, polyoxyethylene (5) phytostanol, and polyoxyethylene (10) phytostanol are preferable. Can be illustrated. These nonionic surfactants may contain only one kind, or may contain two or more kinds in combination. The preferred content of these nonionic surfactants in the skin external preparation of the present invention is 0.05 to 2% by weight, more preferably 0.1 to 1% by weight.
This is because if it is too small, it cannot be solubilized, and if it is too large, the effect will reach a plateau and the feeling of use may be impaired. In particular, the content of the nonionic surfactant is particularly preferably 1% by weight or less from the viewpoint of safety.

(3) Poorly water-soluble active ingredient, which is an essential component of the skin external preparation of the present invention, is also characterized in that it contains a poorly water-soluble active ingredient. Here, the term "poorly water-soluble" in the present invention means:
A component having a solubility in water of 0.01% by weight or less. The effects of such active ingredients include, for example, phytostesides, glycosphingolipids, moisturizing action or skin protecting action by sphingolipids, antibacterial by preservatives such as parabens and antifungal agents such as terbinafine and butenafine. Action or antiseptic action, anti-inflammatory action or analgesic action by anti-inflammatory agents such as steroids, indomethacin, and suprofen; hair-growth action by hair restorer such as minoxidil and phytosteide; astringent action by medicinal plant extracts such as witch hazel , Benzophenones and cinnamic acid esters, such as UV-absorbing action of UV-absorbing agents such as aminobenzoic acid esters,
Of these, active ingredients having a hair-growth effect are particularly preferred. This is because the skin cosmetic for hair growth is particularly often used in a solubilizing system due to its formulation characteristics such as feeling of use and ease of use. Specific active ingredients for hair growth include, for example, minoxidil, phytosteide, tocopherol nicotinate, ethinylestradiol,
Preferred examples include polyporsterone and ecdysteroids. Of these, phytosteide is particularly preferred,
Particularly preferred as phytosteside are glycosides of stigmasterol and stigmasterol,
Among them, stigmasterol maltoside and stigmasteranol maltoside are preferable, and stigmasterol maltoside is particularly preferable. The content of these active ingredients in the cosmetic of the present invention may be determined by the effective amount, but is preferably about 0.01 to 1% by weight.

(4) External preparation for skin of the present invention The external preparation for skin of the present invention comprises the above-mentioned essential ingredients, a poorly water-soluble active ingredient, a nonionic surfactant and a phospholipid, and is a solubilizing agent. It is characterized by being. Here, the external preparation for skin referred to in the present invention is a general term for a composition in the form of percutaneous administration to the skin, and specific examples thereof include cosmetics, external skin medicines, and disinfectants and disinfectants for skin. it can. Of these, cosmetics are particularly preferred. This is because, in cosmetics, the amount of solvent such as ethanol is limited to some extent, moreover, there are many solubilizers in dosage form, and many cases contain many types of poorly water-soluble active ingredients. Under such circumstances, there have been many troubles in which crystals and oily substances are precipitated with time in the form of a solubilizing agent. This is because such a trouble can be greatly improved by applying the technology of the present invention, and there is a base material that can fully utilize the effects of the present invention. In such cosmetics, the external preparation for skin of the present invention is preferably applied as an active ingredient to a cosmetic for hair in which a hair restorer is solubilized. This is because, in such hair cosmetics, the amount of ethanol used tends to be restricted from the viewpoint of environmental science, and the solubilizing means is particularly strongly required in recent years.

The external preparation for skin of the present invention may contain, in addition to the above-mentioned essential components, any components usually used in external preparations for skin. Such optional components include, for example, hydrocarbons such as squalane, petrolatum, and microcrystalline wax, jojoba oil, carnauba wax, esters such as octyldodecyl oleate,
Triglycerides such as olive oil, beef tallow, and coconut oil; fatty acids such as stearic acid, oleic acid, and ritinoleic acid;
Higher alcohols such as oleyl alcohol, stearyl alcohol and octyl dodecanol; anionic surfactants such as sulfosuccinates and sodium polyoxyethylene alkyl sulfate; amphoteric surfactants such as alkyl betaine salts; cationic interfaces such as dialkyl ammonium salts. Activators, sorbitan fatty acid esters, fatty acid monoglycerides, nonionic surfactants such as polyoxyethylene adducts, polyoxyethylene alkyl ethers, polyoxyethylene fatty acid esters, etc., polyethylene glycol, glycerin, 1,3-butanediol And the like, polyhydric alcohols such as, for example, thickening / gelling agents, antioxidants, ultraviolet absorbers, coloring agents, preservatives, and powders. The external preparation for skin of the present invention can be produced by treating these essential components and optional components according to a conventional method.

[0011]

EXAMPLES Hereinafter, the present invention will be described in more detail with reference to Examples, but it goes without saying that the present invention is not limited to only these Examples.

<Examples 1 to 3> Cosmetics for hair, which is an external preparation for skin of the present invention, were prepared according to the following formulations. That is, the ingredients were stirred and solubilized at 80 ° C., and cooled by stirring to obtain a cosmetic. This is one week at 5 ℃, 20 ℃,
After storage at 40 ° C., the solubilized state was observed. The standard of observation is
：: no abnormality, Δ: slight turbidity or precipitation of crystals, x: clear turbidity or precipitation of crystals. The feeling of use was also examined by a specialized panelist. The items of feeling of use were "non-stickiness" and "non-greasy after use", and were ○: good, Δ: slightly difficult, and ×: bad. Comparative Example 1 contained only a phospholipid (lecithin) and Comparative Example 2 contained a nonionic surfactant (polyoxyethylene (10) phytostanol; BP
SH10) alone. Table 1 shows the results. This indicates that the cosmetic for hair, which is an external preparation for skin of the present invention, has excellent solubilizing properties and a feeling of use.
It should also be noted that despite the low ethanol content of 20% by weight, it has such excellent properties. Stigmatanol maltoside 0.1 part by weight Phospholipid / nonionic surfactant * 1 part by weight 1,3-butanediol 5 parts by weight Methyl paraben 0.1 part by weight Ethanol 20 parts by weight Water 73.8 parts by weight * Details in the table It is shown in FIG.

[0013]

[Table 1]

<Examples 4 to 8> Cosmetics for hair, which is an external preparation for skin of the present invention, were prepared according to the following formulations. That is, the ingredients were stirred and solubilized at 80 ° C., and cooled by stirring to obtain a cosmetic. This was evaluated in the same manner as in Examples 1 to 3. Table 2 shows the results. This indicates that the cosmetic for hair, which is an external preparation for skin of the present invention, has excellent solubilizing properties and a feeling of use. It should also be noted that despite the low ethanol content of 20% by weight, it has such excellent properties. Stigmasteranol maltoside 0.1 part by weight Lecithin 0.5 part by weight Nonionic surfactant ** 0.5 part by weight 1,3-butanediol 5 parts by weight Methylparaben 0.1 part by weight Ethanol 20 parts by weight Water 73.8 Parts by weight ** Details are shown in Table 2.

[0015]

[Table 2]

<Examples 9 to 12> Cosmetic products for skin, which are external preparations for skin of the present invention, were prepared according to the following formulations. That is, the ingredients were stirred and solubilized at 80 ° C., and cooled by stirring to obtain a cosmetic. This was evaluated for stability only in the same manner as in Examples 1 to 3. Table 3 shows the results. Than this,
It can be seen that the cosmetic for skin, which is an external preparation for skin of the present invention, has excellent solubilizing properties. It should also be noted that despite having no ethanol, it has such excellent properties. Active ingredient *** 0.1 parts by weight Lecithin 0.5 parts by weight POE (10) phytostanol 0.5 parts by weight 1,3-butanediol 5 parts by weight Glycerin 5 parts by weight 1,2-pentanediol 5 parts by weight Methylparaben 0.1 parts by weight Water 83.8 parts by weight *** Details are shown in Table 3.

[0017]

[Table 3]

<Examples 13 to 16> According to the following formulation, a skin pharmaceutical composition, which is an external preparation for skin of the present invention, was prepared. That is, the ingredients are stirred and solubilized at 80 ° C.
The cosmetic was obtained by stirring and cooling. This was evaluated for stability only in the same manner as in Examples 1 to 3. Table 4 shows the results. From this, it is understood that the pharmaceutical composition for skin, which is an external preparation for skin of the present invention, has excellent solubilizing properties. It should also be noted that despite having only 10% by weight of ethanol, it has such excellent properties. Active ingredient **** 0.1 part by weight Lecithin 0.5 part by weight POE (10) phytostanol 0.5 part by weight 1,3-butanediol 5 parts by weight Glycerin 5 parts by weight 1,2-pentanediol 5 parts by weight Ethanol 10 parts by weight Methyl paraben 0.1 parts by weight Water 83.8 parts by weight **** Details are shown in Table 4.

[0019]

[Table 4]

<Examples 17 to 19> Cosmetics for hair were prepared according to the following recipe in the same manner as described above. Table 5 shows the results of evaluating the stability and feeling of use in the same manner as in Examples 1 to 3. These are 5 ° C, 20 ° C, 4
It was extremely stable even under the condition of storage at 0 ° C. for one month, and the feeling of use was extremely excellent. Stigmastanol maltoside 0.1 parts by weight Lecithin / PEN4620 **** 1 part by weight Sorbitan monolaurate 0.2 parts by weight 1,3-butanediol 1 part by weight Ethanol 30 parts by weight Water 67.7 parts by weight ** **** Details are shown in Table 5. PEN4620 represents POE (20) POP (6) 2-decyltetradecyl ether.

[0021]

[Table 5]

[0022]

According to the present invention, it is possible to provide a novel means for solubilizing a poorly water-soluble active ingredient in a solubilized form of a skin external preparation, especially for a skin external preparation for hair.

Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat II (reference) A61P 17/16 A61P 17/16 // A61K 45/00 A61K 45/00 F term (reference) 4C076 AA11 BB31 CC05 CC18 CC30 DD09 DD37 DD38 DD45 DD63 DD69 DD70 FF15 4C083 AC101 AC102 AC112 AC122 AC442 AC482 AD391 AD491 AD571 AD572 BB04 BB53 CC01 CC31 CC37 DD23 DD27 DD38 EE22 4C084 AA17 AA27 NA02 ZA892 ZA922

Claims (6)

[Claims] 1. A solubilized form of a skin external preparation comprising a poorly water-soluble active ingredient, a nonionic surfactant and a phospholipid. 2. The external preparation for skin according to claim 1, wherein the content of ethanol is 40% by weight or less. 3. The external preparation for skin according to claim 1, wherein the content of the nonionic surfactant is 1% by weight or less. 4. The external preparation for skin according to claim 1, wherein the poorly water-soluble substance is a hair restorer. 5. The external preparation for skin according to claim 1, which is a cosmetic. 6. The external preparation for skin according to any one of claims 1 to 5, which is used for hair.