JPH03178918A - Hair tonic - Google Patents

Abstract

PURPOSE:To obtain a hair tonic effective in preventing falling-off of hair and growing hair by using picolinic acid N-oxide as an active component. CONSTITUTION:The objective agent can be prepared by using 0.001-20wt.% (preferably 0.1-10wt.%) of picolinic acid N-oxide of formula as an essential component and properly compounding conventional additives for hair tonic. It may be compounded further with a vasodilator (e.g. carpronium chloride), amino acids, vitamins, skin function promoting agent, feminine hormones, etc. The conventional additives are an antibacterial agent, refreshing agent, oil, surfactant, perfumery, antioxidant, UV absorber, colorant, ethanol, water, etc. The agent is prepared in the form of an external drug such as milky lotion or ointment and directly applied or sprayed to the skin at a rate of 0.01-100mg/ kg/day in 1-4 divided doses.

Description

DETAILED DESCRIPTION OF THE INVENTION [Industrial Field of Application] The present invention relates to a hair nourishing agent that has excellent hair nourishing effects such as hair loss prevention and hair growth effects. The present invention is particularly useful in the fields of pharmaceuticals, quasi-drugs, and cosmetics.

[Prior Art] Traditionally, the causes of baldness and hair loss include activation of male hormones in organs such as hair roots and sebaceous glands, decreased blood flow to the hair, excessive secretion of sebum, and production of peroxide in the scalp. It is thought that this may be caused by an abnormality.

For this reason, conventional hair nourishing products remove the above causes,
or a compound that has a mitigating effect is generally included.

For example, vitamins such as vitamin B6 and vitamin E, amino acids such as serine and methionine, vasodilators such as Oriental japonica extract, acetylcholine derivatives, purple root extract, anti-inflammatory agents such as hinokitiol, female hormones such as estradiol, cephalanthine, etc. It is formulated with skin function enhancers, etc., and is used for the prevention and treatment of alopecia.

[Problem to be Solved by the Invention 1] However, despite various attempts as described above, conventional hair nourishing products have no effect on hair loss prevention or hair growth. The hair effect was not always sufficient.

This is probably because the causes of hair loss are various and the mechanism of hair growth is also very complex.

Purpose of the Invention In view of the insufficient hair-nourishing effect as described above, the present inventors have developed a method that is extremely effective and excellent in preventing hair loss.
As a result of searching for a substance that has a hair-growth effect and other hair-nourishing effects, it was discovered that picolinic acid N-oxide represented by the following general formula has a strong hair-nourishing effect, and the present invention was completed.

[Means for Solving the Problems] That is, the present invention provides a hair nourishing material containing picolinic acid N-oxide represented by the following general formula as an active ingredient.

Hereinafter, the configuration of the present invention will be explained in detail.

The picolinic acid N-oxide used in the present invention is obtained by a known method, and the amount thereof is 0.001 to 20% by weight, preferably 0.1 to 1% by weight in the hair nourishing material of the present invention.
It is 0% by weight.

In addition to picolinic acid N-oxide, the hair nourishing material according to the present invention includes carpronium chloride, Oriental japonica extract, vasodilators such as acetylcholine derivatives, amino acids such as serine and mediionine, vitamin B6, vitamin E and its derivatives, biotin, etc. vitamins, pantothenic acid and its derivatives,
Gliderrettic acid and its derivatives, nicotinic acid esters such as benzyl nicotinate, skin function enhancers such as cepharanthine, female hormones such as estradiol, etc. may be added at the same time. Furthermore, additives normally used in hair nourishing materials, such as antibacterial agents such as hinokitiol, hexachlorophene, benzalkonium chloride, cetylpyridinium chloride, undecylenic acid, trichlorocarbanilide and hinokitiol, and cooling agents such as menthol;
Drugs such as salicylic acid, zinc and its derivatives, lactic acid and its alkyl esters, organic acids such as citric acid, oils such as olive oil, squalane, liquid paraffin, isopropyl myristate, higher fatty acids and higher alcohols, and polypropylene such as glycerin and propylene glycol. alcohol, others, surfactants, fragrances, antioxidants, ultraviolet absorbers,
Pigments, ethanol, water, humectants, thickeners, and the like can be added as appropriate without losing the effects of the present invention.

The compound of the present invention also has low toxicity, and no side effects were observed even when 1000 mg/Kg was orally administered to SD rats. Therefore, the compound of the present invention is considered to be effective as a hair-nourishing material for hair loss and hair growth caused by various causes.

The hair nourishing material of the present invention can be administered in the form of external preparations such as liquids, emulsions, and ointments, and can be administered transdermally by applying or spraying directly onto the skin. In addition, the dosage of the hair nourishing material of the present invention cannot be clearly determined as it varies depending on age, individual differences, medical conditions, etc., but in general, when administered to humans, the dosage is 0.01 kg per kg of body weight and 0.01 kg per day. ~1
00 mg, preferably 0.1 to 1.0 mg,
This amount can be administered once a day or in 2 to 4 divided doses.

[Example] Next, the method for producing the hair nourishing material and the hair nourishing effect of the present invention will be explained in more detail with reference to Examples. The present invention is not limited thereby. The blending amount is in weight%.

(Manufacturing method) Picolinate N-oxide and hydrogenated castor oil ethylene oxide (40 mol) adduct were added to 95% ethanol, stirred and dissolved, and then ion exchanged water was added and mixed to produce the liquid hair nourishment of Example 1. I got it.

Examples 2 to 5 and Comparative Example 1 were also obtained in the same manner as Example 1.

[Hair Growth Test] The hair growth tests in Examples 1 to 5 and Comparative Example 1 were conducted using C3H/HeNCrJ mice in the resting phase of the hair cycle, using the method of Ogawa et al. (Normal and Abnormal).
Epidermal Difference [Norma
l and Abnormal Epidermal
Differentiation], M, 5eiji and 1. Edited by A. Bernstein, 159-17
0 page, 1982, University of Tokyo Press).

That is, 10 mice per group, no application, Example 1
The mice were divided into 7 groups of 5 to 5 and Comparative Example 1, their backs were pricked with hair clippers and a shaver, and 0.1 ml of each sample was applied once a day. The hair growth effect of each sample was compared by measuring the hair growth area on the back of the mouse and comparing the area ratio. Table 3 shows the number of days required for 50% hair growth rate for each sample.

As is clear from the mouse hair growth test results Table 3, the hair growth agent of the present invention has an excellent hair growth effect.

[Hair nourishing effect test] Next, in order to examine the hair nourishing effects of the hair nourishing agent of the present invention, such as hair loss prevention and hair growth effects, a tricogram test was conducted on humans. The tests were conducted on the hair nourishing products of Examples 1 to 5 and Comparative Example 1.

0 Nitricogram test: Observe the removed hair roots under a microscope before and after using the hair nourishing material, count the number of resting hair roots based on the morphology of the hair roots, and evaluate the hair nourishing effect of the hair nourishing material by increasing or decreasing the ratio. compared. Telogen hair roots are hair roots that have stopped growing, and it is recognized that people who complain of hair loss have a higher proportion of hair roots in the resting stage than normal people.

Each of the hair nourishing materials of Examples 1 to 5 and Comparative Example 1 was applied to the scalps of 10 male subjects twice a day at a rate of 2 ml at a time for 6 months, immediately before application and immediately after the end of application for 6 months. 1.00 hairs were removed from each subject and the roots of each hair were examined. The results are shown in Table-4.

table As is clear from Table 4, Hair nourishing material of the present invention Ba, It has an excellent hair nourishing effect.

Example 6 (Phase A) Picolinic acid N-oxide 1.0 Polyoxyethylene 2.0 (60 mol) Addition-hardened castor oil glycerin 10.0 Dipropylene glycol 10,01.3-Butylene glycol 5.0 Polyoxyethylene Ren glycol 1.500 5.0 (Phase B) Cedyl isooctane-1-10.0 Squalane 5.0 Vaseline 2.0 Propylparaben 2.0 (Phase C) To carboxyvinyl polymer 1% aqueous solution 30.0 Sodium xametaphosphate 0.03 ion exchange water
8.35 (Phase D) 3 Ion-exchanged water 4.5 (Phase E) Caustic potash 0.12 Ion-exchanged water 5.0 (Production method) Phases A and B are heated and dissolved at 60°C and mixed to form a homogeneous Process with a mixer to make a gel. Phase D was gradually added to this and emulsified with a homomixer to obtain O/W milk (night type hair nourishing material).

When this hair nourishing material was tested on humans in the same manner as in Example, it was confirmed that the hair nourishing effect was excellent.

Example 7 (Phase A) Picolinate N-oxide liquid paraffin cetostearyl alcohol glyceryl monostearate PEO (20 mol) -2-ocdildodecyl ether 5
．． 0 5.0 5.5 3.0 3.0 4 Propylparaben 0.3 Fragrance
0.1 (Phase B) Glycerin 8.0 Dipropylene glycol 20.0 Polyethylene glycol 4000 5.0 Sodium hexametaphosphate 0.005 Ion exchange water
45, 095 (Production method) Phase A and phase B were respectively heated and dissolved, mixed, and emulsified with a homomixer to obtain a cream-like hair nourishing agent.

When this hair nourishing agent was tested on humans in the same manner as in Example 1, it was confirmed that the hair nourishing effect was excellent.

[Effect of the invention] The hair nourishing agent of the present invention is a hair nourishing agent having an excellent hair nourishing effect.

Claims (1)

[Claims] (1) A hair nourishing agent characterized by containing picolinic acid N-oxide represented by the following general formula (numerical formula, chemical formula, table, etc.) as an active ingredient.