JP2003212752A - Sebum secretion-inhibitory cosmetic - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a cosmetic capable of sustainedly and topically inhibiting secretion of sebum in the skin and scalp, without adverse effects, highly safe and further having inhibitory actions on sebum synthesis. <P>SOLUTION: This sebum secretion-inhibitory cosmetic comprises a lipid ingredient obtained by treating skin surface lipids collected from a mammal with a silica gel column chromatogram, eluting a hexane/benzene mixture liquid (1:1 volume ratio) and a hexane/diethyl ether mixture liquid (1:1 volume ratio) and then eluting the resultant fraction with acetone as an active ingredient. <P>COPYRIGHT: (C)2003,JPO

Description

Detailed Description of the Invention

[0001]

TECHNICAL FIELD The present invention relates to suppressing secretion of sebum in the skin or scalp, rough skin, acne, seborrheic dermatitis,
The present invention relates to a cosmetic composition which prevents / ameliorates skin troubles due to excessive sebum secretion such as dandruff and hair loss, and further solves cosmetic problems caused by sebum such as skin shine and stickiness.

[0002]

2. Description of the Related Art Sebum secreted by the sebaceous glands of the skin and scalp keeps the skin soft and smooth, and is supplied to the hair as necessary and appropriate oil to improve the suppleness and beauty of the hair. It is an effective ingredient for keeping and is needed for skin and hair. Sebum also plays an important role in preventing various irritants from the outside from invading the skin or the scalp surface, while preventing the loss of water from the skin or the horny layer of the scalp.

However, if the activity of the sebaceous glands is excessively increased and sebum secretion is excessively increased, it may cause dermatitis such as acne and seborrheic skin disease, and various skin troubles, and dandruff on the scalp. And increase hair loss and cause hair loss.
In addition, excessive sebum is a factor that causes various skin abnormalities by promoting a cosmetically unfavorable condition on the skin and scalp (stickiness of skin and hair), promoting the growth of microorganisms and pathogens.

[0004] For the purpose of solving or preventing such dermatitis, skin troubles, cosmetic and cosmetic problems caused by excessive secretion of sebum, sebum has conventionally been removed by washing with soap or the like. In addition, attempts have been made to use sebum synthesis inhibitors in order to suppress the promotion of sebum secretion. Antiserum agents are generally well known as sebum synthesis inhibitors. An anti-androgen agent has an inhibitory effect on the activity of the 5α-reductase enzyme involved in the reduction of testosterone from dihydrotestosterone, and the binding of dihydrotestosterone to a specific receptor, or both. is there.
Vitamin A acid and the like are known as other sebum synthesis inhibitors.

[0005]

However, the effect of removing excess sebum by washing the skin or scalp with the above-mentioned soap or the like is temporary, and it is essential to suppress excessive secretion of sebum to fundamentally remove sebum. There is a problem that dermatitis and skin troubles caused by oversecretion cannot be improved.

On the other hand, the above anti-androgen is a substance involved in hormone metabolism, and vitamin A acid also has a hormone-like action. Even when applied to the skin or the like, these are organs or organs other than the sebaceous glands. There is a problem that the systemic side effects are larger than the local effects.

[0007] Therefore, an object of the present invention is to provide a cosmetic composition which continuously and locally suppresses the secretion of sebum in the skin and scalp, has no side effects, is highly safe, and has an inhibitory effect on sebum synthesis. is there.

[0008]

Under these circumstances, the present inventor has conducted extensive studies to solve the above-mentioned problems, and as a result, skin lipids have an inhibitory effect on sebum synthesis. Was derived from a lipid component (hereinafter referred to as "sebum synthesis inhibitor") present in a fraction of skin surface lipid components that is more polar than cholesterol, and the above-mentioned object was achieved by the sebum synthesis inhibitor component. The present invention has been completed based on the finding that they can be obtained.

That is, according to the present invention, skin surface lipids collected from mammals were subjected to a silica gel column chromatogram to obtain a hexane / benzene mixed solution (volume ratio 1: 1) and a hexane / diethyl ether mixed solution (volume ratio 1: 1). The present invention provides a sebum secretion-suppressing cosmetic composition comprising a lipid component, which is eluted with acetone and then eluted with acetone, as an active ingredient.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION The sebum synthesis inhibiting component used in the present invention is obtained by extracting mammalian skin surface lipids with an organic solvent. Examples of mammals include humans, pigs, cows, horses, sheep and goats. , Mouse, rat, rabbit, dog, guinea pig, cat, monkey and the like.

To extract skin surface lipids from these animals,
Solvents such as chloroform, ethanol, acetone, diethyl ether, petroleum ether, methanol, etc. alone or 2
It can be performed using a mixed liquid in which one or more kinds are mixed in an arbitrary ratio. The extraction is preferably carried out at a temperature of 5 to 40 ° C. for several seconds or longer, and particularly preferably for 1 to 3 minutes.

By further fractionating the skin surface lipid thus obtained, a sebum synthesis inhibiting component can be obtained. A method such as a column chromatogram, a liquid chromatogram, or a thin layer chromatogram is used for the fractionation.

To obtain the sebum synthesis-inhibiting component used in the present invention, for example, skin surface lipids are collected, subjected to silica gel column chromatogram, and sequentially mixed with hexane / benzene (volume ratio 1: 1) (fraction). 1) and a hexane / diethyl ether mixed solution (volume ratio 1: 1) (referred to as fraction 2) to collect each fraction. After that, the mixture is eluted with a solvent having a higher polarity than a hexane / diethyl ether mixed solution, and a fraction containing sebum synthesis-inhibiting components (referred to as fraction 3) is collected. As a solvent for obtaining this fraction (fraction 3), an ether solvent such as diethyl ether, a halogen solvent such as chloroform and methylene chloride, an ester solvent such as ethyl acetate, a ketone solvent such as acetone and methyl ethyl ketone, An alcohol-based solvent such as ethanol or methanol, a nitrile-based solvent such as acetonitrile, or the like may be used alone or as a mixed solution in which two or more kinds are mixed at an arbitrary ratio. Fraction 1 contains squalene, wax ester, sterol ester,
In fraction 2, triglyceride, free fatty acid, and cholesterol are recognized as main components, respectively, and in fraction 3, a lipid component having a higher polarity than cholesterol is present. Fraction 3 is used in the present invention.

The above-mentioned fraction 3 may be used alone as a sebum secretion suppressing cosmetic, but if necessary, a surfactant, an oil, a moisturizer, an astringent, a cooling agent, an antioxidant, an alcohol, a chelate. , PH regulators, preservatives, thickeners, pigments, fragrances, anti-inflammatory agents, keratolytic agents, antibacterial agents, bactericides, and other medicinal ingredients, as well as commonly used drugs, cosmetics, quasi drugs, etc. The components can be appropriately blended. The amount of the sebum synthesis inhibiting component in the cosmetic of the present invention is usually preferably 0.01 to 50% by weight (hereinafter simply referred to as "%") as a fraction 3 in the cosmetic, and 0.1 to 50% by weight.
20% is particularly preferred.

The cosmetics for suppressing sebum secretion of the present invention include external cosmetics for skin, cosmetics for hair-growth and hair-growth, and the dosage forms may be liquid, ointment, gel, aerosol and the like. Yes, specifically W / O emulsion cosmetics, O
/ W-type emulsified cosmetics, creams, lotions, lotions, oily lotions, packs, foundations, hair tonics, shampoos and the like.

[0016]

EXAMPLES Next, the present invention will be described more specifically by way of examples, but the present invention is not limited to these examples.

Test Example 1 (1) Preparation of skin surface lipid: 2 hours after washing the face, healthy human male 1
A cup with a diameter of 1.4 cm was placed on the forehead of 0 people, an acetone / diethyl ether mixture (volume ratio 1: 1) was poured, and the mixture was allowed to stand for 3 minutes to remove the skin lipids mainly containing fresh sebum after secretion. Extraction gave 1010 mg of dry weight lipid.

Next, this was dissolved in a small amount of an acetone / diethyl ether mixed solution (volume ratio 1: 1) and pretreated with a hexane / benzene mixed solution (volume ratio 1: 1) to produce a silica gel column (Analytichem Mega Bound Elut, manufactured by varian). ) And fractionated. First, 50 ml of a hexane / benzene mixture (volume ratio 1: 1) is flown, and the eluate is fraction 1
(Dry weight 360 mg). Hexane /
The eluate in 50 ml of a diethyl ether mixture (volume ratio 1: 1) was collected as fraction 2 (dry weight 587 mg), and the final eluate was collected in 50 ml of acetone as fraction 3 (dry weight 24 mg).

(2) Measurement of sebum synthesis inhibitory activity: The test samples were fraction 3 (polar fraction), fraction 2 (medium polar fraction), fraction 1 (nonpolar fraction) and pre-fractionated human sebum. Using the method of Hall et al. (Arch D
ermatol Res, 275; 1-7, 1983). That is, a piece of skin tissue (3 mm in diameter) containing sebaceous glands of the auricle of a male hamster was treated with Krebs-Ringer containing radioactive sodium acetate.
After culturing in a phosphate buffer for 3 hours, the tissue was hydrolyzed, extracted with hexane, and the amount of radiolabeled lipid in hexane was measured with a liquid scintillation counter to determine the amount of synthetic sebum in the sebaceous glands. This culture is performed in Krebs-Ringer phosphate buffer containing a test sample for skin tissue obtained from the right auricle of the same hamster,
The skin tissue obtained from the left auricle was subjected to Krebs-Ringer phosphate buffer containing no test sample, and the sebum synthesis inhibition rate was calculated by the following formula.

[0020]

[Equation 1]

The inhibition rate of sebum synthesis at each concentration of each fraction of human skin surface lipid is shown in FIG. As is clear from the results shown in FIG. 1, human skin surface lipids have an inhibitory effect on lipid biosynthesis in the sebaceous glands (D: 0.5% addition concentration in FIG. 1, about 40% sebum synthesis inhibition rate). It was shown that this inhibitory activity was the highest in the fraction 3 (polar fraction) obtained from human skin surface lipids (A in FIG. 1: sebum synthesis inhibition rate of about 50% at 0.06% addition concentration). From these results, it was confirmed that the sebum synthesis inhibiting component was present in the fraction 3. In addition, in order to clarify the sebum synthesis inhibitory component, the lipid biosynthesis inhibitory action of the major components of the skin surface lipids was examined and compared with the sebum synthesis inhibitory rate of each fraction (B: fraction 2, C: fraction 1). Is shown in FIG.

Test Example 2 Squalene, wax (palmitic acid palmitate), triglyceride (tripalmitin), free fatty acid (palmitic acid), cholesterol, sphingolipid (D-sphingosine) were used as lipids corresponding to the main components in the skin surface lipids. , The fraction 1 which is each fraction of skin surface lipid
3 to 3, the sebum synthesis inhibition rate was measured in the same manner as in Test Example 1. The results are shown in Table 1.

[0023]

[Table 1]

As shown in Table 1, the major components in the generally known skin surface lipids have almost no inhibitory effect on the lipid biosynthesis of the sebaceous glands, and the sebum synthesis inhibiting component is the polar lipid fraction of the skin surface lipids ( It is clear that it is a minor component present in fraction 3). As described above, it was confirmed that the skin surface lipids and the components derived from the skin surface lipids have an effect of suppressing sebum secretion. Since this polar lipid fraction is an in vivo component,
It is extremely safe to use externally over a long period of time.

Each of the above-mentioned fractions 3 was blended with each component to prepare a sebum secretion suppressing lotion (Example 1), sebum secretion suppressing cream (Example 2), sebum secretion suppressing pack (Example 3), anti-dandruff hair tonic ( Example 4), anti-dandruff shampoo (Example 5) and anti-dandruff rinse (Example 6) were produced according to a conventional method. All of them showed excellent stability.

Example 1 Skin lotion suppressing sebum secretion

[0027]

[Table 2]

Example 2 Sebum secretion inhibitory emollient cream

[0029]

[Table 3]

Example 3 Sebum secretion suppression pack

[0031]

[Table 4]

Example 4 Anti-dandruff hair tonic

[0033]

[Table 5]

Example 5 Anti-dandruff shampoo

[0035]

[Table 6]

Example 6 Anti-dandruff

[0037]

[Table 7]

[0038]

The cosmetic composition for suppressing sebum secretion of the present invention suppresses the secretion of sebum in the skin and scalp continuously and locally,
Furthermore, it has no side effects and has good safety. And, the sebum secretion-suppressing cosmetic composition of the present invention has almost no irritation to the skin or scalp, and has no hormone-like action, so that no overall side effect is observed and it is continuously applied for a long period of time. , There is no problem in safety.

[Brief description of drawings]

FIG. 1 is a graph showing the influence of human lipid fraction components on lipid synthesis.

─────────────────────────────────────────────────── ─── Continuation of front page (51) Int.Cl. ⁷ Identification code FI theme code (reference) A61K 7/00 A61K 7/00 Y 7/06 7/06 7/075 7/075 7/08 7/08 (72) Inventor Hiroshi Nojiri 2606, Akabane, Kai-cho, Haga-gun, Tochigi Prefecture Kao Institute of Stock Companies (72) Inventor Hiroyuki Nitta 2606, Akabane, Kai-cho, Haga-gun, Tochigi Institute (72) Inventor Noriko Sato 2606 Kabane-cho, Haga-gun, Tochigi Prefecture Kao Co., Ltd. Research Institute (72) Inventor Kimihiko Hori 2606 Kabaya-cho, Haga-gun, Tochigi Prefecture Kao Co., Ltd. F-term (reference) 4C083 AA081 AA082 AA112 AC012 AC072 AC082 AC102 AC122 AC182 AC242 AC402 AC422 AC442 AC482 AC642 AC692 AC782 AD042 AD112 AD132 AD272 AD532 AD552 AD662 CC04 CC05 CC07 CC33 CC38 CC39 DD22 DD23 DD27 DD31 EE06 EE07 EE12 EE14 EE22 EE23 EE29 FF01 FF05

Claims (2)

[Claims] 1. A skin surface lipid collected from a mammal is subjected to a silica gel column chromatogram and eluted with a hexane / benzene mixture (volume ratio 1: 1) and a hexane / diethyl ether mixture (volume ratio 1: 1). After that, a cosmetic composition for suppressing sebum secretion, which contains as an active ingredient a lipid component eluted with acetone. 2. A skin surface lipid is extracted from the skin of a mammal using a solvent selected from chloroform, ethanol, acetone, diethyl ether, petroleum ether and methanol, or a mixture of two or more solvents. A cosmetic composition for suppressing sebum secretion according to claim 1.