JP2017025002A - Hyperoxidation inhibitor for lipid, and cosmetic for scalp and hair - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a hyperoxidation inhibitor for lipid and a cosmetic for scalp and hair which stably and effectively inhibit hyperoxidation of lipid derived from scalp and/or hair which could cause dandruff, itch, and odor.SOLUTION: A hyperoxidation inhibitor for lipid derived from scalp and/or hair has 6-benzylaminopurine as an active ingredient, and a cosmetic for scalp and hair uses the hyperoxidation inhibitor for lipid.SELECTED DRAWING: None

Description

  The present invention relates to a lipid peroxidation inhibitor containing 6-benzylaminopurine as an active ingredient. Moreover, this invention relates to the cosmetics for scalp hair which use such a peroxidation inhibitor for lipids.

  Sebum prevents the entry of various stimulating substances from outside the body into the skin, and also has an effect of supplying an appropriate amount of oil to the hair in the scalp. However, sebum that exhibits such a significant action is easily oxidized and lipid peroxide is generated. This peroxidation reaction causes dandruff, itching and odor in the scalp. In order to solve the problems caused by sebum, washing with shampoo has been carried out, but since the sebum recovers quickly even after washing and removal, the scalp and hair immediately feel sticky. Causes dandruff, itching and odor.

  In vivo lipid peroxidation generally proceeds by a free radical chain reaction mechanism, giving hydroperoxide as the first product, which is further decomposed and enzymatically modified to oxidize epoxides, alcohols, ketones, aldehydes, etc. It is supposed to give a secondary product. And squalene monohydroperoxide has been detected from human calf, scalp surface lipids and dandruff lipids (Non-patent Document 1).

Tocopherol (vitamin E) has been conventionally known as an antioxidant that suppresses the formation of lipid peroxides, but there are problems such as limited prescription system and instability, which is more effective. Ingredients were desired.
Therefore, as techniques for solving such problems, for example, xanthophylls such as astaxanthin (Patent Document 1), a composition containing eucalyptus extract (Patent Document 2), and a composition containing 1,2-alkanediol (Patent Document 3). Cosmetics, etc., containing sucrose as an active ingredient have been developed.

  On the other hand, 6-benzylaminopurine (6-benzyladenine) and its derivatives are known as external preparations for the purpose of preventing skin aging and activating cells by external application to the scalp (for example, patents). Reference 4). However, it is not known to improve or inhibit lipid oxidation of the scalp by using 6-benzylaminopurine for the scalp.

JP 2008-273874 A JP 2005-206537 A Japanese Patent Laid-Open No. 2003-081801 JP-A-10-72321

Yoshiyuki Kono et al., Lipid Peroxidation in Human Epidermis. Soc. Cosmet. Chem. Japan. Vol. 27, no. 1,33-40 (1993)

  The present invention provides a lipid peroxidation inhibitor that stably and effectively inhibits peroxidation of lipids derived from the scalp and / or hair that cause dandruff, itching and odor. Moreover, this invention provides the cosmetics for scalp hair which use such a peroxidation inhibitor for lipids.

  As a result of intensive studies to solve the above problems, the present inventor has found that the following inventions meet the above object, and have reached the present invention.

That is, the present invention relates to the following inventions.
<1> A peroxidation inhibitor for lipids derived from the scalp and / or hair containing 6-benzylaminopurine as an active ingredient.
<2> A scalp hair cosmetic comprising the lipid peroxidation inhibitor described in <1> above.
<3> The scalp hair cosmetic according to <2>, wherein the scalp hair cosmetic is used for preventing dandruff, itching or odor.

  According to the lipid peroxidation inhibitor comprising 6-benzylaminopurine of the present invention as an active ingredient, a lipid peroxidation inhibitor that stably and effectively inhibits peroxidation of lipids derived from the scalp and / or hair is provided. be able to. The present invention also provides a scalp hair cosmetic for preventing dandruff, itching or odor by using such a lipid peroxidation inhibitor.

  DESCRIPTION OF EMBODIMENTS Embodiments of the present invention will be described in detail below. However, the description of the constituent elements described below is an example (representative example) of an embodiment of the present invention. It is not limited to the contents.

The present invention relates to a lipid peroxidation inhibitor containing 6-benzylaminopurine as an active ingredient. Here, the lipid is a general term for water-insoluble substances isolated from living organisms, and is generally defined as a molecule that exists or is derived from living organisms having long-chain fatty acids or hydrocarbon chains.
Among these lipids, the peroxidation inhibitor of the present invention is particularly suitable for lipids derived from the scalp and hair. In addition, the lipid (sebum) derived from hair refers to the thing which the lipid secreted from the sebaceous gland adhered to the hair.

The lipid peroxidation inhibitor of the present invention comprises 6-benzylaminopurine as an active ingredient. 6-Benzylaminopurine (molecular weight 225.26) is a crystalline white powder, also known as 6-benzyladenine, which is known as an active ingredient for hair growth, and is an active ingredient for inhibiting lipid peroxidation. As unknown. As a result of careful examination of other functionalities as a scalp and hair application material of 6-benzylaminopurine, the applicants found that it is suitable as an active ingredient of a peroxidation inhibitor of lipids derived from the scalp and hair. It was.
That is, 6-benzylaminopurine has an excellent lipid peroxidation-inhibiting action, and the present invention was completed by finding new knowledge that dandruff, itching and odor can be prevented by applying this to the scalp and hair. It is a thing.

  6-Benzylaminopurine lipid peroxidation-inhibiting effect is present in an optimal amount, but the form of the preparation is not particularly limited, but in order to effectively exhibit the effect, solubilization of a transparent system Mold type dosage forms are preferred. In practical terms, compatibility with water or ethanol is particularly important, but 6-benzylaminopurine is a material that is difficult to dissolve in both, and thus it is necessary to appropriately set conditions.

  In the present invention, 6-benzylaminopurine is 0.0001 to 2.0% by weight as a sufficient amount capable of exhibiting lipid peroxidation inhibitory effect, pharmacological effect (drug utilization) and stability in formulation formulation. In view of this, 0.0005 to 1.0% by weight, more preferably 0.0025 to 0.5% by weight, and most preferably 0.005 to 0.5% by weight is used. The solution can be prepared with a water / ethanol mixed solvent in an optimal ratio.

  The mixed solvent of water and ethanol can be configured such that the water and ethanol solvent ratio (weight ratio) is 65:35 to 10:90 with respect to the effective concentration of 6-benzylaminopurine.

  The lipid peroxidation inhibitor of the present invention includes a form acceptable as a category of pharmaceuticals, quasi-drugs, and cosmetics, and the dosage form is particularly limited as long as the object of the present invention is not impaired. Not constrained. For example, water / ethanol-based solution preparations, gels using the stock solution of the present invention regardless of whether they are liquid, solubilized preparations such as essences, and propellant mixed preparations such as aerosols. It may be a formulation to be washed away such as shampoo or rinse.

  Moreover, about the compounding base at the time of formulation design, the arbitrary liquid and solid raw material accept | permitted on hair application can be used widely. At that time, various additives such as preservatives, fragrances, stabilizers, colorants, ultraviolet absorbers / scattering agents, antioxidants, humectants, thickeners, and the like can be added as necessary.

  EXAMPLES Hereinafter, although an Example demonstrates this invention further in detail, this invention is not limited to a following example, unless the summary is changed.

Lipid peroxidation inhibition test
(A) Test method 100 mL / L linoleic acid ethanol solution 1.0 mL, 0.1 mol / L phosphate buffer (pH 7.0) 6.0 mL, ethanol 1.0 mL, water 1.0 mL, sample solution 1.0 mL The test solution was mixed. The test solution was incubated at 40 ° C., and after 3 days, 4 days, and 5 days, the peroxide value was measured by the rodan iron method to evaluate the antioxidant effect.
As the sample solution, the sample of the present invention was added so that the final concentration was 0.0025 to 0.01% by weight. Similarly, as a comparative example, α-tocopherol was added to 8 μmol / L. Moreover, what added water was made into control.
[Rodan Iron Method]:
To 0.1 mL of the test solution, 4.7 mL of 75% ethanol, 0.1 mL of 30% rhodanammonium, and 0.1 mL of a 3.5% hydrochloric acid solution of 0.02 mmol / L ferrous chloride were added, and the absorbance at 500 nm was added after 3 minutes. Was measured as the value of the peroxide value.

(B) Test results The test results are shown in Table 1. As is clear from the table, in the control, the peroxide value increased due to the decomposition of linoleic acid with the passage of days, but when 6-benzylaminopurine was added, the increase in the peroxide value was suppressed, and the antioxidant effect was observed. It was.

"Dander, itching, odor prevention effect test"
(A) Test method Ten men who suffered from dandruff, itching and odor of the scalp were targeted. Divided into 2 groups of 5 people each, using a 50% ethanol solution containing 0.0025 wt% and 0.5 wt% 6-benzylaminopurine, and a solvent not containing 6-benzylaminopurine as a control, half head Was evaluated. An appropriate amount of the sample was applied twice a day (2 mL per time). Two weeks and one month after the start of sample application, dandruff was observed with a microscope, and itching and odor were self-evaluated by each subject through sensory evaluation and wiping with absorbent cotton, respectively, and represented by the following score.

(Dandruff)
3: There are a lot of dandruff 2: There is a little dandruff 1: There is a slight dandruff 0: There is no dandruff (Itching)
3: Strong itching 2: Itching 1: Slightly itchy 0: No itching (odor)
3: Strong unpleasant odor 2: Unpleasant odor 1: Smell slightly 0: Smell but weak

(B) Test results The test results are shown in Tables 2 and 3. As is apparent from the table, 6-benzylaminopurine showed the effect of suppressing dandruff, itching and odor in a concentration range of 0.0025 wt% to 0.5 wt%. As described above, the present invention can not only prevent dandruff, itching and odor, but also prevent them simultaneously.

  Below, the formulation example of this invention is shown. In the formulation examples, “appropriate amount” means a value at which the entire formulation is 100% by weight.

<Prescription Example 1> Hair Tonic
(weight%)
6-Benzylaminopurine 0.5
Polyethylene glycol 400 2.0
Ethanol 60.0
Purified water Appropriate amount The ingredients were uniformly stirred to produce a hair tonic.

<Formulation example 2> Hair cream
(weight%)
A component:
6-Benzylaminopurine 1.0
Liquid paraffin 10.0
Squalane 7.0
Jojoba oil 3.0
Solid paraffin 3.0
Polyoxyethylene cetyl ether 2.0
Sorbitan sesquioleate 1.0
B component:
Glycerin 3.0
Ethyl paraoxybenzoate 0.1
Potassium hydroxide 0.15
Purified water appropriate amount Dissolve component A by heating. Separately, heat-dissolved component B was gradually added, and the mixture was stirred and emulsified uniformly, and then cooled to produce a hair cream.

<Prescription Example 3> Aerosol
(weight%)
A component:
6-Benzylaminopurine 0.5
Propylene glycol 2.0
Ethanol 48.0
Purified water appropriate amount B component:
Liquefied petroleum gas (propellant) 20.0
The component A was mixed and dissolved uniformly and placed in an aerosol container, and B was pressurized and filled into the container by a conventional method to produce an aerosol.

<Formulation example 4> Hair shampoo
(weight%)
A component:
6-Benzylaminopurine 0.05
N-coconut oil fatty acid-L-glutamic acid triethanolamine 40.0
Coconut oil fatty acid diethanolamide 3.0
Polyoxyethylene dioleic acid methyl glucoside 2.0
B component:
Ethyl paraoxybenzoate 0.3
Edetate disodium 0.1
Purified water Appropriate amount A component A was stirred and dissolved uniformly, and another component B that was uniformly heated and dissolved was gradually added and stirred uniformly to produce a hair shampoo.

<Prescription example 5> Hair treatment
(weight%)
A component:
6-Benzylaminopurine 0.01
Avocado oil 5.0
Squalane 5.0
Liquid paraffin 10.0
Stearic acid 3.0
Glycerol monostearate 3.0
Lanolin alcohol 5.0
B component:
1,3-butylene glycol 5.0
Triethanolamine 1.0
Methyl paraoxybenzoate 0.2
Purified water appropriate amount Dissolve component A by heating. Separately, heat-dissolved B component was gradually added, stirred uniformly, emulsified, and then cooled to produce a hair treatment.

  It was confirmed that all of these Formulation Examples 1 to 5 had the effect of achieving the object of the present invention, as confirmed in the test examples.

  The present invention relates to a lipid peroxidation inhibitor containing 6-benzylaminopurine as an active ingredient, and is useful for prevention of dandruff, itching and odor by applying it to the scalp.

Claims (3)

  A peroxidation inhibitor for lipids derived from scalp and / or hair, comprising 6-benzylaminopurine as an active ingredient.   A scalp hair cosmetic comprising the lipid peroxidation inhibitor according to claim 1.   The cosmetic for scalp hair according to claim 2, wherein the cosmetic for scalp hair is for preventing dandruff, itching or odor.