JP6661292B2 - Peroxidation inhibitors for lipids and cosmetics for scalp hair - Google Patents

Description

  The present invention relates to a peroxidation inhibitor for lipids containing 6-benzylaminopurine as an active ingredient. The present invention also relates to a cosmetic for scalp hair using such a peroxidation inhibitor for lipids.

  Sebum acts to prevent various irritants from entering the skin from the outside of the body and to supply a moderate amount of oil to hair on the scalp. However, sebum that exhibits such a significant effect is easily oxidized to produce lipid peroxide. This peroxidation reaction causes dandruff, itching and odor on the scalp. Washing with shampoo, etc. is performed to eliminate the trouble caused by this sebum, but the sebum recovers immediately after washing and removal, so the scalp and hair immediately feel sticky. It causes dandruff, itching and odor.

  The peroxidation of lipids in vivo generally proceeds by a free-radical chain reaction mechanism, giving hydroperoxide as the first product, which is further degraded and enzymatically modified to oxidize epoxides, alcohols, ketones, aldehydes, etc. It is said to give a secondary product. In addition, squalene monohydroperoxide has been detected in human scalp, scalp skin lipids and dandruff lipids (Non-Patent Document 1).

Tocopherol (vitamin E) has been conventionally known as an antioxidant that suppresses the production of lipid peroxide, but there are problems such as the restriction of the prescription system and instability. Ingredients were desired.
Therefore, as a technique for solving such a problem, 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 and the like containing an active ingredient 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, see Patents). Reference 4). However, it has not been known that the use of 6-benzylaminopurine in the scalp improves and suppresses scalp lipid oxidation.

JP 2008-273874 A JP 2005-206537 A JP-A-2003-081801 JP-A-10-72321

Kono, Y. et al., Lipid peroxidation in human epidermis. Soc. Cosmet. Chem. Japan. Vol. 27, no. 1, 33-40 (1993)

  The present invention has been made in view of the above prior art, and provides a peroxidation inhibitor for lipids that stably and effectively suppresses peroxidation of lipids derived from the scalp and / or hair which cause dandruff, itching, and odor. The present invention also provides a cosmetic for scalp hair using such a peroxidation inhibitor for lipids.

  The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, have found that the following inventions meet the above objects, and have accomplished the present invention.

That is, the present invention relates to the following inventions.
<1> A peroxidation inhibitor for lipids derived from scalp and / or hair containing 6-benzylaminopurine as an active ingredient.

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

  Hereinafter, embodiments of the present invention will be described in detail. However, the description of the constituent requirements described below is an example (representative example) of the embodiment of the present invention, and the present invention is described below unless it exceeds the gist thereof. It is not limited to the content of.

The present invention relates to a lipid peroxidation inhibitor containing 6-benzylaminopurine as an active ingredient. Here, lipid is a general term for water-insoluble substances isolated from living organisms, and is generally defined as molecules that exist in living organisms or have biological origin having long-chain fatty acids or hydrocarbon chains.
The peroxidation inhibitor of the present invention is suitably used especially for lipids derived from the scalp or hair among these lipids. The lipid (sebum) derived from the hair refers to lipids secreted from the sebaceous glands adhered to the hair.

The lipid peroxidation inhibitor of the present invention is characterized by using 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 an active ingredient for suppressing peroxidation of lipids. As unknown. As a result of detailed examination of other functionalities of 6-benzylaminopurine as a material for application to the scalp and hair, the applicants have found that 6-benzylaminopurine is suitable as an active ingredient of a peroxidation inhibitor for lipids derived from the scalp and hair. Was.
That is, 6-benzylaminopurine was found to have an excellent lipid peroxidation inhibitory action, and by applying it to the scalp and hair, it was possible to prevent dandruff, itch and odor, and completed the present invention. It was done.

  Although the optimal amount of 6-benzylaminopurine for inhibiting lipid peroxidation is present, the formulation is not particularly limited. However, in order to exert the effect efficiently, the transparent system must be solubilized. Formulation forms of the type are preferred. Practically, compatibility with water or ethanol is particularly important, but since 6-benzylaminopurine is a material that is difficult to dissolve in both, it is necessary to appropriately set conditions.

  In the present invention, 6-benzylaminopurine has a sufficient amount of 0.0001 to 2.0% by weight to exhibit the effect of inhibiting lipid peroxidation, and has a medicinal pharmacology (drug utilization rate) and stability in the formulation. From the viewpoint, 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. A solution can be prepared with an optimal ratio of a water / ethanol mixed solvent.

  The mixed solvent of water and ethanol can be composed of, for example, a water / ethanol solvent ratio (weight ratio) of 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 for the category of pharmaceuticals, quasi-drugs, and cosmetics, and its dosage form is not particularly limited as long as the object of the present invention is not impaired. Not restricted. Examples thereof include water / ethanol-based solution preparations, solubilized preparations such as gels and essences using the stock solution of the present invention irrespective of whether they are liquid or mixed propellant preparations such as aerosols. A wash-off preparation such as shampoo or rinse may be used.

  Further, as the compounding base at the time of designing the formulation, any liquid or solid raw material that is acceptable for hair application can be used widely. At this time, various additives such as preservatives, fragrances, stabilizers, coloring agents, ultraviolet absorbers / scatterers, antioxidants, humectants, and thickeners can be added as necessary.

  Hereinafter, the present invention will be described in more detail with reference to examples, but the present invention is not limited to the following examples unless the gist 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 mixture was mixed to prepare a test solution. The test solution was incubated at 40 ° C., and after 3 days, 4 days, and 5 days, the peroxide value was measured by the rhodane iron method, and the antioxidant action was evaluated.
The sample solution was added so that the final concentration of the sample of the present invention was 0.0025 to 0.01% by weight. Similarly, as a comparative example, α-tocopherol was added at 8 μmol / L. A control to which water was added was used as a control.
[Rodan iron method]:
4.7 mL of 75% ethanol, 0.1 mL of 30% rhodammonium, 0.1 mL of 0.02 mmol / L ferrous chloride in 3.5% hydrochloric acid were added to 0.1 mL of the test solution, and the absorbance at 500 nm was added after 3 minutes. Was measured and used 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. Was.

"Test for dandruff, itching and odor prevention effect"
(A) Test method Ten men were concerned with dandruff, itch and odor on the scalp. Half-head using only 50% ethanol solution containing 0.0025% by weight and 0.5% by weight of 6-benzylaminopurine and a solvent containing no 6-benzylaminopurine alone as a control. Was evaluated. The sample was applied in an appropriate amount twice a day (2 mL per time). Two weeks and one month after the start of the sample application, dandruff was observed with a microscope, and itching and odor were subjected to a self-evaluation by each subject by sensory evaluation and wiping with absorbent cotton, respectively, and expressed by the following scores.

(Dandruff)
3: Very many dandruff 2: Slight dandruff 1: Slight dandruff 0: No dandruff (itch)
3: Strong itching 2: Itching 1: Slight itching 0: No itching (odor)
3: Strong unpleasant odor 2: Unpleasant odor 1: Slightly odorless 0: Smell but weak

(B) Test results The test results are shown in Tables 2 and 3. As is clear from the table, 6-benzylaminopurine exhibited an effect of suppressing dandruff, itch and odor in a concentration range of 0.0025% by weight to 0.5% by weight. As described above, the present invention not only can prevent dandruff, itching and odor, but also can prevent them at the same time.

  In the following, formulation examples of the present invention are shown. In the formulation examples, “appropriate amount” means a value at which the entire formulation becomes 100% by weight.

<Prescription example 1> Hair tonic
(weight%)
6-benzylaminopurine 0.5
Polyethylene glycol 400 2.0
Ethanol 60.0
Appropriate amount of purified water The components were uniformly stirred to produce a hair tonic.

<Prescription 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
Appropriate amount of purified water Heat and dissolve component A. Separately, the B component heated and dissolved was gradually added, uniformly stirred and emulsified, and then cooled to produce a hair cream.

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

<Prescription 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
Amount of purified water A component was uniformly stirred and dissolved, and separately heated and dissolved component B was gradually added thereto, followed by uniform stirring 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
Glycerin monostearate 3.0
Lanolin alcohol 5.0
B component:
1,3-butylene glycol 5.0
Triethanolamine 1.0
Methyl paraoxybenzoate 0.2
Purified water qs Dissolve component A by heating. Separately, the heat-dissolved B component was gradually added, uniformly stirred and emulsified, and then cooled to produce a hair treatment.

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

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

Claims (1)

  A peroxidation inhibitor for lipids derived from scalp and / or hair, comprising 6-benzylaminopurine as an active ingredient.