JPH10158141A - Sebum secretion-inhibiting cosmetic - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a sebum secretion-inhibiting cosmetic which is useful in inhibition of sebum secretion on the skin and scalp by using a lipid higher in the polarity than cholesterol. SOLUTION: Skin surface lipid of mammalian animals is extracted with an organic solvent, for example, chloroform, preferably at 5-40 deg.C for 1-3 minutes, subjected to chromatography and eluted sequentially with a hexane/diethyl ether 1:1 volume ratio mixture, a hexane/diethyl ether 1:1 volume ratio mixture, and further with a higher polar solvent than the hexane/diethyl ether mixture (for example, an ether such as diethyl ether) to collect the fraction containing a lipid component higher than cholesterol in polarity (sebum lipid synthesis inhibitor). This inhibitor is formulated to a cosmetic in an amount of 0.01-50wt.% and is used as a sebum secretion-inhibiting cosmetic (cosmetic of external use for skin or for hair growth and restoration).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention suppresses the secretion of sebum in the skin or scalp, and provides
The present invention relates to a cosmetic that prevents and ameliorates skin problems due to excessive sebum secretion such as dandruff and hair loss, and that solves cosmetic problems caused by sebum such as skin shine and stickiness.

[0002]

2. Description of the Related Art Sebum secreted from the sebaceous glands of the skin and scalp keeps the skin soft and smooth, and is supplied to the hair as a necessary and appropriate oil, thereby improving the suppleness and beauty of the hair. It is an effective ingredient for preserving and is required 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 water loss from the skin or the scalp stratum corneum.

[0003] However, if the activity of the sebaceous glands is excessively increased and secretion of sebum becomes excessive, dermatitis such as acne and seborrheic dermatosis and various skin troubles are caused, and dandruff is caused on the scalp. Causes increase in hair loss and hair loss.
In addition, excessive sebum is a cosmetically unfavorable condition on the skin and scalp (stickiness of skin and hair), promotes the growth of microorganisms and pathogenic bacteria, and becomes a factor that causes various skin abnormalities.

[0004] For the purpose of solving or preventing such dermatitis, skin troubles and cosmetic / cosmetic problems caused by excessive secretion of sebum, it has been customary to remove sebum by washing with soap or the like. In addition, attempts have been made to use sebum synthesis inhibitors in order to suppress the increase in sebum secretion. As sebum synthesis inhibitors, antiandrogens are generally well known. Antiandrogens have an inhibitory effect on the activity of 5α-reductase enzyme involved in the reduction of testosterone to dihydrotestosterone and / or on the binding of dihydrotestosterone to specific receptors. is there.
Also, as other sebum synthesis inhibitors, vitamin A acid and the like are known.

[0005]

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

On the other hand, the above-mentioned antiandrogens are substances involved in hormonal metabolism, and vitamin A acid also has a hormonal action, and these are organs and organs other than sebaceous glands even when applied to skin or the like. Also has the problem that systemic side effects are greater than local effects.

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

[0008]

Under such circumstances, the present inventors have conducted intensive studies to solve the above problems, and as a result, the epidermal lipid has an inhibitory effect on sebum synthesis, and this inhibitory effect has been demonstrated. Has been found to be derived from a lipid component present in a fraction having a higher polarity than cholesterol (hereinafter referred to as a “sebum synthesis inhibitory component”) among the skin surface lipid components. The inventors have found that the present invention can be obtained and completed the present invention.

[0009] That is, the present invention provides a sebum secretion suppressing cosmetic comprising, as an active ingredient, a lipid component having higher polarity than cholesterol among skin lipid components.

[0010]

BEST MODE FOR CARRYING OUT THE INVENTION The sebum synthesis-inhibiting component used in the present invention is obtained by extracting a skin epidermal lipid of a mammal with an organic solvent. Examples of the mammal include human, pig, cow, horse, sheep and goat. , Mice, rats, rabbits, dogs, guinea pigs, cats, monkeys and the like.

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

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

In order to obtain the sebum synthesis-inhibiting component used in the present invention, for example, a skin epidermal lipid is collected and subjected to a silica gel column chromatogram, and a hexane / benzene mixed solution (volume ratio of 1: 1) (fraction). 1), and eluted with a hexane / diethyl ether mixed solution (volume ratio 1: 1) (referred to as fraction 2) to collect each fraction. Further, thereafter, elution is performed with a solvent having a higher polarity than the hexane / diethyl ether mixed solution, and a fraction containing a sebum synthesis inhibitory component (referred to as fraction 3) is collected. Solvents for obtaining this fraction (fraction 3) include ether solvents such as diethyl ether, halogen solvents such as chloroform and methylene chloride, ester solvents such as ethyl acetate, ketone solvents 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 can be used alone or as a mixture of two or more kinds mixed at an arbitrary ratio. Fraction 1 contains squalene, wax ester and sterol ester,
Fraction 2 contains triglyceride, free fatty acid, and cholesterol as main components, respectively, and fraction 3 contains a lipid component that is more polar than cholesterol. In the present invention, fraction 3 is used.

The above-mentioned fraction 3 may be used alone as a sebum secretion suppressing cosmetic, but if necessary, a surfactant, oil, humectant, astringent, freshener, antioxidant, alcohol, chelate , PH adjusters, preservatives, thickeners, dyes, fragrances, anti-inflammatory agents, deflocculants, 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 0.1%.
20% is particularly preferred.

The cosmetics for inhibiting sebum secretion according to the present invention include cosmetics for external use on the skin, and cosmetics for hair restoration and hair growth. The dosage forms may be any of liquids, ointments, gels, aerosols and the like. And specifically, W / O type emulsified cosmetics, O
/ W type emulsified cosmetics, creams, emulsions, lotions, oily lotions, packs, foundations, hair tonics, shampoos and the like.

[0016]

EXAMPLES Next, the present invention will be described more specifically with reference to examples, but the present invention is not limited to these examples.

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

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

(2) Measurement of sebum synthesis inhibitory activity: The measurement was performed using, as test samples, fraction 3 (polar fraction), fraction 2 (medium-polar fraction), fraction 1 (non-polar fraction), and human sebum before fractionation. Using Hall's method (Arch D
ermatol Res, 275; 1-7, 1983). That is, a piece of skin tissue (diameter 3 mm) containing the auricular sebaceous gland 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 gland. This culture is performed in a Krebs-Ringer phosphate buffer containing a test sample for skin tissue obtained from the right pinna of the same hamster,
The skin tissue obtained from the left pinna was subjected to a Krebs-Ringer phosphate buffer containing no test sample, and the sebum synthesis inhibition rate was determined by the following formula.

[0020]

(Equation 1)

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

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

[0023]

[Table 1]

As shown in Table 1, the major components of the skin lipids that are generally known have almost no inhibitory effect on the lipid biosynthesis of the sebaceous glands, and the present sebum synthesis inhibitory component is a polar lipid fraction of skin lipids ( It is clear that this is a minor component present in fraction 3). As described above, it was confirmed that the skin surface lipid and the skin surface lipid-derived component exhibited a sebum secretion inhibitory effect. Since this polar lipid fraction is an in vivo component,
It is extremely safe even when used continuously for a long period of time.

The above-mentioned fraction 3 was blended with each component, and the sebum secretion suppressing lotion (Example 1), the sebum secretion suppressing cream (Example 2), the sebum secretion suppressing pack (Example 3), and the anti-dandruff hair tonic ( Example 4) An anti-dandruff shampoo (Example 5) and an anti-dandruff rinse (Example 6) were produced according to a conventional method. These all showed excellent stability.

Example 1 Sebum secretion inhibiting lotion

[0027]

[Table 2]

Example 2 Emollient cream for suppressing sebum secretion

[0029]

[Table 3]

Example 3 Sebum Secretion Inhibition Pack

[0031]

[Table 4]

Example 4 Anti-dandruff hair tonic

[0033]

[Table 5]

Example 5 Anti-dandruff shampoo

[0035]

[Table 6]

Example 6 Anti-fukerinse

[0037]

[Table 7]

[0038]

Industrial Applicability The sebum secretion suppressing cosmetic of the present invention suppresses sebum secretion in the skin and scalp continuously and locally,
Furthermore, it has no side effects and good safety. And the sebum secretion suppressing cosmetic of the present invention hardly irritates the skin and scalp, and has no hormonal action, so that no overall side effects are observed, and even if it is continuously applied for a long period of time, There is no problem with safety.

[Brief description of the drawings]

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

 ──────────────────────────────────────────────────の Continuing on the front page (72) Inventor Hiroyuki Nitta 2606 Kabane-cho, Akaga-cho, Haga-gun, Tochigi Pref. (72) Inventor Kimihiko Hori 2606 Akabane, Kaigamachi, Haga-gun, Tochigi Pref.

Claims (1)

[Claims] 1. A cosmetic composition for suppressing sebum secretion comprising, as an active ingredient, a lipid component having a polarity higher than that of cholesterol among skin surface lipid components.