JPH05255102A - Testosterone-5-alpha-reductase inhibitor - Google Patents

Abstract

PURPOSE:To provide an inhibitor, hair grower, or dermatic external preparation, each having excellent testosterone-5-alpha-reductase-inhibitory activity, thus outstanding in the promotive effects for depilation prevention, hair growing, or sebum suppression (e.g. pimple suppression). CONSTITUTION:The objective inhibitor, hair grower, or dermatic external preparation containing, as active ingredient, at least one kind of extract of plant selected from Quercus spp., Asparagi radix, Ophipogonis tuber, Corydalis tuber, Cyperi rhizoma, Jateorhiza columba, Marsdenia cundurango, Achillea millefolium, Cephaelis ipecacuanha, Corni fructus, Sophorae subprostratae radix, Gynura japonica, Faeces leporum, and Menyanthes trifoliata.

Description

Detailed Description of the Invention

[0001]

INDUSTRIAL APPLICABILITY The present invention has a novel and safe testosterone-5α-reductase inhibitor, which is excellent in promoting hair loss prevention, hair growth, hair growth, sebum suppression, and the like. The present invention relates to a hair nourishing agent and a skin external preparation. The present invention is particularly used in the fields of medicines, quasi drugs, and cosmetics.

[0002]

2. Description of the Related Art Conventionally, physiological signs such as male pattern baldness, baldness, and seborrhea are based on an increase in androgen stimulation caused by excessive accumulation of androgen in the metabolic system. It is known. Recently, the main body of androgen activity in several organs such as hair root and sebaceous gland is 5α-dihydrotestosterone (hereinafter 5α).
-Abbreviated as DHT. ), Which is well known to be produced by the reduction of testosterone by testosterone-5α-reductase (hereinafter abbreviated as reductase) in the target organ. for that reason,
Signs of androgenetic baldness, baldness, and seborrhea caused by increased androgen stimulation may be reduced or prevented by inhibiting reductase, and specifically inhibit reductase. Several inhibitors have been found and have been synthesized. However, the newly synthesized inhibitors so far have a drawback that they have a steroid structure or a steroid-like structure and have some undesirable hormone-like action.

[0003]

DISCLOSURE OF INVENTION Problems to be Solved by the Invention As a result of diligent studies by the present inventors of a naturally derived drug that is effective in preventing hair loss, hair growth, hair growth, seborrhea, etc. The inventors have found that this problem can be solved and completed the present invention.

[0004]

[Means for Solving the Problems] That is, claim 1 of the present invention is, oak, tenmondou, bakumondou, corydalis, kobushi, colombo, conzulango, sanshuyu,
It is a testosterone-5-α-reductase inhibitor containing one or more plant extracts selected from sandscon, citrus japonicus, yarrow, turmeric and honeywort. Claim 2 is oak, Tenmondou, Bakumondou, Engosaku, Kobushi, Colombo,
A skin external preparation characterized by containing one or two or more plant extracts selected from Condulango, Sanshuyu, Sansukon, Sanchisou, Yarrows, konjac, and honeywort. Claim 3 contains one or more kinds of plant extracts selected from oak, Tenmondou, Bakumondou, Engosaku, Kobushi, Colombo, Conzulango, Sanyuyu, Sunzukon, Sanchisou, Achillea millefolium, Tokon and Mitsugasiwa. It is a hair nourishing agent.

The structure of the present invention will be described in detail below. The following plant extracts are used as the plant extract used in the present invention. Oak [Terminalia cheb
ula Retzius] fruit, Tenmondou (Chrysanthemum japonicum, Tenmon winter) [Asparagus coch
inchinensis Merrill), Bakumondou (Janohige, Bakumon Fuyu) [Ophiopogo
n japonicus Ker-Gawler] roots, Engosaku (Cornelus tu)
tuber of rtschaninovii Besser],
Rhododendron (Cyperus ro)
tundus L. ] Rhizome, Colombo [Jateor
hizacolumba Miers] root, Conzurango [Marsdenia cundurango R
eichenbach] bark, Sanshuyu (Yamatake)
[Corunus officinalis Sieb
old] seeds, Sandscon (wild bean root) [Sophor
a subprostrata Chen et T. ]
Rhizomes and roots of Cyprinus japonica [Cynura japo
nica Juel. ] Leaves, Achillea millefolium [Achillea millefolium
L. ], Tokon [Cephaelis ipe]
cacuanhaA. Richard] roots, Menyanthes trifolia
L. ] Leaves are used.

The method for producing the plant extract used in the present invention includes a plant (dried product such as crude drug or raw plant) as a solvent, for example, hot water or lower alcohol such as methanol or ethanol.
Or water-containing lower alcohol or propylene glycol, 1-3 butylene glycol or other polyvalent alcohol or water-containing polyvalent alcohol or other water-containing alcohol.

The blending amount of the plant extract in the present invention is 0.00 as a dry product in the total amount of the hair nourishing agent or the skin external preparation.
5 to 20% by weight is preferable, more preferably 0.01
10 to 10% by weight. When it is less than 0.005% by weight,
The effect of the present invention is not sufficiently exerted, which is not preferable.
If it exceeds 20% by weight, it is not preferable in terms of formulation.

The hair nourishing agent and external preparation for skin of the present invention may have any properties such as liquid, emulsion, ointment, etc. so long as they can be applied to the outer skin. In addition to the above-mentioned essential components, the effects of the present invention can be obtained. Incorporating various components commonly used in cosmetics, quasi-drugs, pharmaceuticals, etc., aqueous components, moisturizers, thickeners, preservatives, antioxidants, fragrances, coloring agents, drugs, etc. be able to. Further, the dosage form of the hair nourishing agent and the external skin preparation of the present invention is arbitrary, and examples thereof include a hair restorer, tonic, hair cream, mousse, shampoo,
The dosage form can be a rinse, cream, emulsion, lotion, or pack.

[0009]

EXAMPLES Next, the present invention will be described more specifically with reference to examples. The present invention is not limited to this. The blending amount is% by weight.

(Method for measuring 5α reductase inhibitory effect) Takayasu et al. (S. Takayasu, K. Adachi, J. Clin. End
ocrinol.Metab. , 34, 1098-1101 (1972)), the amount of testosterone reduced to 5α-DHT was measured using human hair roots, and 0.1% and 70% ethanol solutions of each plant extract methanol extract dried product were measured. The inhibitory effect on testosterone-5-α-reductase was examined, and the results are shown in Table 1.

[0011]

[Table 1]

As is clear from Table 1, the testosterone-5α-reductase inhibitor according to the present invention has an excellent inhibitory effect.

Table 2 shows Examples 1 to 5 and Comparative Example 1. The manufacturing method is as follows. Each plant extract and hydrogenated castor oil ethylene oxide (40 mol) adduct were added to 95% ethanol, dissolved by stirring, and then ion-exchanged water was added and mixed to obtain a liquid hair nourishing agent of Example 1. Examples 2 to 5 and Comparative Example 1 were also obtained in the same manner as in Example 1.

[0014]

[Table 2]

Next, in order to examine the hair-retaining effects such as hair loss prevention and hair growth effect of the hair nourishing agent of the present invention, a trichogram test was conducted on humans. The hair nourishing agents of Examples 1 to 5 and Comparative Example 1 were used.

(Trichogram test) The hair roots of the removed hair before and after the use of the hair nourishing agent are observed under a microscope, and the number of resting hair roots is counted from the morphology of the hair nourishing agent. The effects were compared. Resting hair roots are hair roots of hairs that have stopped growing, and it has been recognized that people who complain of hair loss have a higher proportion of resting hair roots than normal people. Each of the hair nourishing agents of Examples 1 to 5 and Comparative Example 1 was applied to the scalp of 10 male subjects twice a day, 2 ml each, continuously for 6 months, immediately before and immediately after the application for 6 months. 100 hairs were removed from each subject, and each hair root was examined. The results are shown in Table 3.

[0017]

[Table 3]

As described above, the hair nourishing agent according to the present invention has an excellent hair nourishing action.

Next, the method for producing the skin external preparation of the present invention and the acne improving action will be described in more detail with reference to examples.

Example 6 (Phase A) Sorbitol 3.0 Glycerin 5.0 Resorcinol 0.02 Ion-exchanged water balance (Phase B) Methanol extract dried product of Sandscon 0.08 Methanol extract dried product of Sanshuyu 1.2 Methanol extract dried product of Kobushi 0.5 Polyoxyethylene (60) ) Hardened castor oil 0.5 95% ethanol 20.3 Fragrance Suitable amount The ingredients of phase A were mixed and dissolved, and the mixed solution of phase B was added thereto with stirring to obtain a lotion as a uniform solution.

Example 7 (Phase A) Sorbitol 3.0 Glycerin 5.0 Resorcinol 0.02 Ion-exchanged water 68.0 (Phase B) Oak propanol extract dry matter 0.5 Colombo methanol extract dry matter 0.5 Polyoxyethylene (60) hydrogenated castor oil 0.5 95% Ethanol 20.3 Fragrance Appropriate amount The ingredients of phase A were mixed and dissolved, and the mixed solution of phase B was added thereto with stirring to obtain a lotion as a uniform solution.

Example 8 (Phase A) Beeswax 10.0 Paraffin wax 6.0 Lanolin 3.0 Isopropyryl myristate 6.0 Squalane 8.0 Liquid paraffin 26.0 Dried mannmond extract methanol extract 0.5 Conzulango propanol extract 0.1 Mitsugasiwa Ethanol extract dried product 0.05 Polyoxyethylene sorbitan stearate 2.0 Sorbitan monostearate 4.2 Preservative proper amount (Phase B) Prolene glycol 2.0 Polyoxyethylene (60) hydrogenated castor oil 1.0 Water 29.0 Mix Phase A ingredients The mixture was heated and dissolved at 75 ° C, and the mixed solution of phase B heated to 75 ° C was added thereto with stirring, cooled, and stirred at 45 ° C and left to obtain a cream.

Example 9 (Phase A) Sorbitol 3.0 Glycerin 5.0 Resorcinol 0.02 Ion-exchanged water 70.0 (Phase B) Methanol extract dry matter of Sanchisou 1.0 1.0 Bakumondou methanol extract dry matter 0.5 Polyoxyethylene (60) hydrogenated castor oil 0.5 95% Ethanol 20.3 Fragrance Appropriate amount The ingredients of phase A were mixed and dissolved, and the mixed solution of phase B was added thereto with stirring to obtain a lotion as a uniform solution.

Example 10 (Phase A) Sorbitol 3.0 Glycerin 5.0 Resorcin 0.02 Ion-exchanged water 70.0 (Phase B) Dried ethanol extract of Engozag 0.5 Dried ethanol extract of Astragalus sinensis 0.4 Polyoxyethylene (60) hydrogenated castor oil 0.5 95% ethanol 20.3 Fragrance Suitable amount Phase A ingredients were mixed and dissolved, and the phase B mixed solution was added thereto with stirring to obtain a lotion as a uniform solution.

(Acne symptom improvement effect test) Examples 6 to 8
Each of the external preparations for skin of Comparative Example 2 (lotion without addition of a plant extract) was tested by 40 males and 30 females aged 15 to 21 years old twice a day, and a small amount of lotion was applied after washing the face. After a week, the effect of improving the acne symptoms was tested and evaluated. (Evaluation) The degree of each symptom was divided into the following four categories. Zenji: All symptoms disappeared. Remarkable effect: Remarkably effective. Effective: All lighter. Invalid: No change before and after use. The results are shown in Table-4.

[0026]

[Table 4]

As described above, the external preparation for skin according to the present invention is
It was confirmed to have an excellent effect.

[0028]

The testosterone-5-α-reductase inhibitor of the present invention is a hair nourishing agent having an excellent hair nourishing effect,
It is an external preparation for skin that has an excellent acne treatment effect.

Claims (3)

[Claims] 1. A testosterone comprising, as an active ingredient, one or two or more kinds of plant extracts selected from oak, Tenmondou, Bakumondou, Engosaku, Kobushi, Colombo, Conzurango, Sanshuyu, Sunzukon, Sanshiso, Achillea millefolium, Tokon and Mitsugasiwa. 5-α
-Reductase inhibitors. 2. One or more kinds of plant extracts selected from oak, Tenmondou, Bakumondou, Engosaku, Kobushi, Colombo, Conzulango, Sanshuyu, Sunzukon, Sanchisou, Achillea millefolium, Tokon and Mitsugasiwa. Hair nourishing agent. 3. One or more kinds of plant extracts selected from oak, Tenmondou, Bakumondou, Engosaku, Kobushi, Colombo, Conzurango, Sanshuyu, Sunzukon, Sanchisou, Achillea millefolium, Tokon, and Mitsugasiwa. External preparation for skin.