JPH04364109A - Hair tonic - Google Patents

Abstract

PURPOSE:To provide a tonic containing an alkoxycarbonylpyridine N-oxides as the active component and excellent in hair-growing effects such as prevention of falling hair and trichogenous effect. CONSTITUTION:One or two or more kinds of compounds represented by the formula (R is 2-17C straight or branched chain alkyl), e.g. 4- ethoxycarbonylpyridine N-oxide and 3-isobutoxycarbonylpyridine N-oxides are blended in a hair tonic in an amount of 0.001-20wt.%, preferably 0.1-10wt.%. The above-mentioned hair tonic is applied by percutaneous administration, i.e., spreading directly on the skin or spraying and the dosage is within a range of 0.01-100mg/day, preferably 0.1-10mg/day per kg.

Description

[Detailed description of the invention]

0001

BACKGROUND OF THE INVENTION 1. Field of the Invention 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.

0002

[Prior Art] Conventionally, 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 hair follicles, excessive secretion of sebum, and production of peroxides. Scalp abnormalities are suspected. For this reason, conventional hair nourishing products generally contain compounds that have the effect of eliminating or alleviating the above-mentioned causes.

[0003] For example, vitamins such as vitamin B and vitamin E, amino acids such as serine and methionine, vasodilators such as Oriental japonica extract and acetylcholine derivatives, purple root extract, anti-inflammatory agents such as hinokitiol, and female hormones such as estradiol. It is used to prevent and treat alopecia, and is used to prevent and treat alopecia.

0004

[Problems to be Solved by the Invention] Problems with the Prior Art However, conventional hair nourishing agents are said to be effective in preventing and improving dandruff, itching, hair loss, etc. and to promote hair growth. The mechanism of hair is extremely complex, and it has not been possible to achieve sufficient hair loss prevention or hair growth effects simply by inhibiting the activation of male hormones or increasing blood flow to hair follicles using conventional hair tonics.

Purpose of the Invention In view of the above circumstances, the present inventor has searched for a substance that is effective against hair loss and has excellent hair growth prevention and hair growth effects, and has found the following general formula: The present inventors have discovered that alkoxycarbonylpyridine N-oxide represented by formula I has a strong hair-nourishing effect, and have completed the present invention.

[0006]

[Chemical formula I] (wherein, R represents a straight chain or branched alkyl group having 2 to 17 carbon atoms.)

[0007]

[Means for Solving the Problems] That is, the present invention is a hair nourishing agent characterized by containing one or more alkoxycarbonylpyridine N-oxides represented by the following general formula and formula I as an active ingredient. .

[0008]

[Formula I] (In the formula, R represents a straight chain or branched alkyl group having 2 to 17 carbon atoms.) The structure of the present invention will be explained in detail below.

The alkoxycarbonylpyridine N-oxide used in the present invention has the following general formula:

0010

[Chemical formula I] (wherein, R represents a straight chain or branched alkyl group having 2 to 17 carbon atoms.)

The chemical name of the compound is 2-
Methoxycarbonylpyridine N-oxide, 3-methoxycarbonylpyridine N-oxide, 4-methoxycarbonylpyridine N-oxide, 2-ethoxycarbonylpyridine N-oxide, 3-ethoxycarbonylpyridine N-oxide, 4-ethoxycarbonylpyridine N- oxide, 2-n-propoxycarbonylpyridine N-oxide, 3-iso-propoxycarbonylpyridine N-oxide, 4-tert-butoxycarbonylpyridine N-oxide, 2-n-butoxycarbonylpyridine N-oxide, 3-iso- Butoxycarbonylpyridine N-oxide, 2-tert
-butoxycarbonylpyridine N-oxide, 2-is
o-pentyloxycarbonylpyridine N-oxide, 4-neopentyloxycarbonylpyridine N-oxide, 2-n-pentyloxycarbonylpyridine N
-oxide, 2-neopentyloxycarbonylpyridine N-oxide, 2-n-hexyloxycarbonylpyridine N-oxide, 2-n-heptyloxycarbonylpyridine N-oxide, 2-octyloxycarbonylpyridine N-oxide, 4- Octyloxycarbonylpyridine N-oxide, 4-(1-methylheptyloxycarbonyl)pyridine N-oxide,
2-n-nonyloxycarbonylpyridine N-oxide, 2-(2-methyloctyloxycarbonyl)pyridine N-oxide, 2-(1-butylpentyloxycarbonyl)pyridine N-oxide, 4-n-nonyloxycarbonylpyridine N-oxide, 4-(1-butylpentyloxycarbonyl)pyridine N-oxide, 2-n-decylpyridine N-oxide, 3-n-
Decyloxycarbonylpyridine N-oxide, 4-n
-decyloxycarbonylpyridine N-oxide, 2
-n-undecyloxycarbonylpyridine N-oxide, 4-n-dodecyloxycarbonylpyridine N
-oxide, 2-n-tridecyloxycarbonylpyridine N-oxide, 3-n-tridecyloxycarbonylpyridine N-oxide, 4-n-tridecyloxycarbonylpyridine N-oxide, 2-n-heptadecyloxycarbonyl Pyridine N-oxide, 4-
These include n-heptadecyloxycarbonylpyridine N-oxide, 2-(1-octylnonyloxycarbonyl)pyridine N-oxide, and the like.

[0012] The alkoxycarbonylpyridine N-oxide used in the present invention is obtained by a known method, and the amount of the alkoxycarbonylpyridine N-oxide contained in the hair nourishment of the present invention is 0.001 to 20
% by weight, preferably from 0.1 to 10% by weight.

[0013] In addition to alkoxycarbonylpyridine N-oxide, the hair nourishment according to the present invention contains vasodilators such as carpronium chloride, Oriental japonica extract, and acetylcholine derivatives, amino acids such as serine and methionine, and vitamin B.
vitamins such as vitamin E and its derivatives, biotin, pantothenic acid and its derivatives, glycyrrhetinic acid and its derivatives, nicotinic acid esters such as benzyl nicotinate, skin function enhancers such as cephalanthine, and female hormones such as estradiol. etc. may be blended at the same time. Furthermore, additives normally used in hair nourishing agents, such as hinokitiol, hexachlorophene, benzalkonium chloride, cetylpyridinium chloride, antibacterial agents such as undecylenic acid, trichlorocarbanilide and bithionol, cooling agents such as menthol, salicylic acid, Zinc and its derivatives, drugs such as lactic acid and its alkyl esters, organic acids such as citric acid, protease inhibitors such as tranexamic acid, amino acids such as arginine, olive oil, squalane, liquid paraffin, isopropyl myristate, higher fatty acids , oils such as higher alcohols, polyhydric alcohols such as glycerin and propylene glycol, other surfactants, fragrances, antioxidants, ultraviolet absorbers, pigments, ethanol, water, humectants, thickeners, etc., have the effects of the present invention. It can be blended as appropriate within a range that does not impair the properties.

The hair nourishment of the present invention may be in any form as long as it can be applied to the skin, such as liquid, milky lotion, or ointment. The hair growth agent of the present invention is administered by transdermal administration, in which it is directly applied or sprayed onto the skin. Furthermore, the dosage of the hair nourishment of the present invention cannot be clearly determined as it varies depending on age, individual differences, medical conditions, etc., but in general, the dosage when administered to humans is 0.01 to 100 mg per kg of body weight and per day.
, preferably 0.1 to 10 mg, and this amount is administered once a day.
It can be administered once or in 2 to 4 divided doses.

[0015]

Effects of the Invention The hair nourishing agent of the present invention has excellent hair nourishing effects such as hair loss prevention and hair growth effects.

[0016]

EXAMPLES Next, the method for producing the hair nourishing agent 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%. (Production method) Add alkoxycarbonylpidiline N-oxide and hydrogenated castor oil ethylene oxide (40 mol) adduct to 95% ethanol, stir and dissolve, then add ion-exchanged water and mix to prepare the liquid of Example 1. I got hair nourishment. Examples 2 to 15 and Comparative Example 1 were also obtained in the same manner as Example 1.

[0017]

[Table 1]

[0018]

[Table 2]

[0019]

[Table 3]

[Hair growth test] The hair growth tests of Examples 1 to 28 and Comparative Example 1 were conducted using C3H/HeNC in the resting phase of the hair cycle.
Using rJ mice, Ogawa et al.'s method (normal and
Abnormal Epidermal Difference Normal and Abnormal E
Pidermal Differentiation
,M. Seiji and I. A. Bernstein (ed., pages 159-170, 1982, University of Tokyo Press)
This was done by That is, 10 mice per group,
The mice were divided into 30 groups: no application, Examples 1 to 15, and Comparative Example 1, and the backs of the mice were shaved with clippers and a shaver.
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. 5 for each sample
Table 4 shows the number of days required for 0% hair growth rate.

[0021]

[Table 4]

As mentioned above, the hair nourishment according to the present invention is
It 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 test was performed on the hair nourishing products of Examples 1 to 15 and Comparative Example 1. (Trichogram test) Observe the removed hair roots under a microscope before and after using the hair nourishing agent, count the number of resting hair roots based on the shape of the hair root, and compare the hair nourishing effect of the hair nourishing agent by increasing or decreasing the ratio. did. 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 telogen phase than normal people. Examples 1-15
Each hair nourishing agent of 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 consecutive months.
100 hairs per person were removed and the root of each hair was examined. The results are shown in Table 5.

[0023]

[Table 17] As described above, the hair nourishing agent according to the present invention has an excellent hair nourishing effect.

Example 16

Weight% (Phase A) 3-phytoxycarboxylic acid N-oxyto
1.0 Polyoxyethylene (60 mol) addition-hardened castor oil
2.0
glycerin

10.0 Dipropylene glycol

10.0 1,3-butylene glycol
5.0 Polyethylene glycol 1500
5.0
(Phase B) Cetyl isooctanate

10.0 Squalane

5.0 Vaseline


2.0 Propylparaben

2.0 (C phase) 1% carboxyvinyl polymer aqueous solution
30.0
Sodium hexametaphosphate

0.03 Ion exchange water

8.35 (D phase) Ion exchange water

4.5 (E phase) Caustic potash

0.12 Ion exchange water

5.0 (Manufacturing method) Phase A and phase B are heated and dissolved at 60°C, mixed and treated with a homomixer to form a gel. Phase D is gradually added to this and dispersed using a homomixer. Next, the dissolved phase C was added thereto, and finally the dissolved phase E was added and emulsified with a homomixer to obtain an o/w emulsion type hair nourishment. When this hair nourishing agent was tested on humans in the same manner as in Example 1, it was confirmed that its hair nourishing effect was excellent.

Example 17

Weight % (Phase A) 4-Isopropyrooxycarboxylic acid N-oxyto
2.0 Liquid paraffin

5.0 Cetostearyl alcohol

5.5 Glyceryl monostearate

3.0 EO (20 mol)-2-
Octyl dodecyl ether
3.0 Propylparaben
0.
3 Fragrance

0.1 (B phase) Glycerin

8.0 Dipropylene glycol
20.0 Polyethylene glycol 4000
5.0
Sodium hexametaphosphate

0.005 Ion exchange water

48.095 (Manufacturing method) Phase A, B
The phases were dissolved and mixed by heating, and the mixture was emulsified using a homomixer to obtain a creamy 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.

[Chemical formula 1]

[Table 5]

Claims (1)

[Claims] 1. A hair nourishing composition comprising one or more alkoxycarbonylpyridine N-oxides represented by the following general formula and formula I as an active ingredient. [Chemical formula I] (wherein, R represents a straight chain or branched alkyl group having 2 to 17 carbon atoms.)