JPS5959606A - Remedy for senile, seborrheic and diabetic apopecia - Google Patents

Abstract

PURPOSE:To provide the titled remedy for apopecia, containing oxendolone as a main component, free from undesirable side effects such as actions of hormones, etc., and having high safety and excellent remedying effect. CONSTITUTION:The titled remedy for apopecia contains oxendolone (chemical name: 16beta-ethyl-17beta-hydroxy-4-estren-3-one) as a main component. The remedy has three effects in combination, i.e. inhibition of the uptake of blood testosterone in the cells of the sebaceous gland, inhibition of reductase activity, and inibition of bonding of 5alpha-dihydrotestosterone with receptor protein, and is effective for the remedy of senile, seborrheic and diabetic apopecia. Dose: about 0.1-100mg of oxedolone daily for adult.

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention is excellent in that it does not have the problems of -1 Lumo/Sakukawa et al. Elderly people with rf lle effect ↑′1, fat I notification ↑t1 and desk board hair removal! +
'＋Enter the therapeutic agent. Senile hair loss 1111 according to the present invention
41: (I) is a general term for hair loss or hair loss that becomes noticeable in each year, and also includes those that are classified separately as alopecia in the old year.

The so-called male-pattern alopecia, such as ``hair loss'' in the elderly and IIFT leakage, is caused by an increase in male t'l, 1 lmono stimulation, which is based on an overload of male↑11 hormones. Recently, it has been said that the main body of this male, 1 lumo/active substance in organs such as hair roots and sebaceous glands is an enzyme named testosderone or i-stoste 11-5a-reductase (hereinafter referred to as F reductase) in these target lids. Omitted.

5α-11', + 5α-1 (hereinafter abbreviated as 5α-1) II T. ) is becoming well known. In other words, Komaru and sub7"f
The y-stosuge 11 no (male, 1 ru (/) made from 1'l, 1 ru (/) enters the bloodstream and becomes -1 in the sebaceous glands, and is made more powerful by the reductase in the sebaceous gland cells. 5α-1) is converted to II T. This 5 a
-1) HT binds to intracellular receptors, acts on coughing, and does not promote the proliferation of sebaceous gland cells; on the other hand, HT itself exits the sebaceous gland cells and enters the bloodstream, acting on hair G) cells and stimulating the growth of hair G). ．． J, is said to suppress the division of hair 1 cona cells and increase hair growth IQ.

iI'L prevents so-called male-pattern hair loss caused by aging, oiliness, and senility.In order to promote hair growth, it is incorporated into the destoblast 117 in the blood or into the sebaceous gland cells. It also inhibits the activity of sebum, which is present in the skin, and inhibits the activity of the powerful man ↑ 11 hormone / hair 1 inch. and Moni, 5a-l) The binding of II T to receptor proteins must be inhibited. Several substances have been discovered so far based on this viewpoint. However, these substances cannot be used as reductases.
Even if the inhibition rate is large, it is good.
3:5α-1) The inhibition rate of binding between II T and receptor protein is as low as 17.
It had the disadvantage that it was inferior to the therapeutic effect of fl.

In view of the circumstances of the -1- article, Akina Kinai is an unfavorable subtitle of 51βshinoi'1kawa'η゛ ('+ use 1, safe, and in the song) ``stosno [1 no sebaceous gland cell] 1t11'11;, Inhibition of reductase activity, O, l,
and 5α-1) Exploring the effect of inhibiting the binding between IIT and receptor protein 0114-t', 'it thing f no), and using IIT as one of the ingredients, 111 with excellent therapeutic effects on the elderly.
, seborrheic, J, and RP+ hair removal treatment 11 therapeutic agents 91
We are doing a lot of research.1. 2♀11. Fruit, -A-'l
・By using SET/TOI+NO, 1. After discovering that the above objectives could be achieved, I was able to complete the present invention.

That is, the present invention is a therapeutic agent for senile, seborrheic and alopecia alopecia, which contains Oxent 11 as a main ingredient.

The configuration of the present invention will be explained in detail.

Oxent 11 used in the present invention has the chemical name 1
It is called 6β-ethyl-1β-human 1x-4-estreno-3-one, and is a white or pale yellowish-white powder, and is odorless.

Use of Monthly 1-cent 11 as a therapeutic agent for alopecia in the elderly, seborrheic acne and castorum ↑11 according to the present invention: 11
is about 01 to 1100 I1 per 111 adults. (
The Kuwa IJ dosage form is available in external preparations such as JFi lIk% soft tablets, and injectables (71), which are manufactured by the I+j method. The method is 200 mH 1 =) seven nodes 1 + 7 I OOc:c
O) ll'l iij Kawa Asiaru (11 Konoha Station〆);) to obtain transparency i1k, and this solution (k) was dissolved in the peripheral scalp 1 (0.05 cc per barb to -11). It is said that the f5 mucus is washed twice.As is clear from the examples described below, all the clinical cases showed good f5 mucus.7.
(IJ is progressing, and no side effects have been observed.

Next, the acute toxicity of OxenoFr+one will be described.

Next, A xenol used in the present invention? The harmful effect of ++7 on l/ductase, 1-1111 and the binding-inhibiting effect on receptor tan/<5α-1) II T will be explained by giving comparative examples.

Reductase activity inhibition effect Takayasu's method (Nishi 11 Honkin J:: Academic journal, 121
5-12+7. Based on +qs+>, using the sebaceous glands on the back of the pigeon star, Bustosderon or 5 a l)
The amount reduced to IIT was measured. The sample used for the experiment [
1 concentration is 10-' and 10-5 molar concentration. The inhibition rate was determined from the obtained data using the following formula. The results are shown in Table 1.

Inhibition rate (%) = (C-1/·C) xlO.

C: Amount of 5α-D II T produced in control t: Amount of 5α-1) IjT produced when the sample was added.
l) crmatol, Ras, , 2 (i4.50-5
1, I4179), the receptor tan/< 5α
-The amount of binding with D II T was measured. Sample 1' used in the experiment: [Concentration is 10 molar]. ? The inhibition rate was determined from the data obtained using the following formula. The results are shown in Table 2.

Inhibition rate (%) = (C-c/C) The combination of [,1 personl and person2: Aru)l.

II 7 is the conventional public 211 4-at-11th "Inl"
-4717β Nonol, the inhibitory effect of Retakuchi activity + 1 compared to the monoacid is 1J''/i', or the receptor protein, J=5α-1) 1.1□ with II T Combine μ
m1 harmful effect is great, the present invention o111 (1!J can be expressed as a substance that achieves J.?;t-,te,;4), the set I+7 is the I゛ component. h)↑
It was expected that the therapeutic effect of dj treatment for alopecia 11 and desk plate alopecia would be significant.

Next, we will give examples of clinical trials to further explain the present invention. Y' will be explained in detail.

Clinical trial example 1 (1/1 male with senile alopecia) 40
I was concerned about the increase in hair loss around the age of 1, so I had tried some over-the-counter products or received treatment at a local doctor.
No significant effect was obtained. During that time, hair loss was occurring from the forehead to the mid-section of the head, and I had given up on hair removal. The main rules from nJ1 in 1981: [1-] Approximately 5cc
After application, new vellus hair was observed on the forehead after about one row, and after about 1 row, vellus hair had increased on the fff of the head compared to before. We are currently monitoring the progress of 11 days. The version for sub A'1 has not been seen.

Clinical Case 31 (Experimental Example 2 (Elderly t'l de-flooding nj; 48-year-old male i!1) 1: I +: r' + rr J- Hair loss progressed rapidly, between 4 and 15 years. +iii l(/i
The hair from the part to the yjl I:rt part is the system, ) ("
kaj7 tesata. is 1. The hair or vellus hair on the t-shirt is rough. For this reason, I used a ``wig'' once seven or eight years ago. I also tried Yamasaka medicine, but it had no effect.

For this reason, I visited the Department of Dermatology, Kyoto University Hospital, and was prescribed a treatment. Approximately 2 months later, vellus hair appeared on the forehead, and after about 3 months, vellus hair appeared on the forehead (7 degrees).

Clinical trial example 3 (Seborrheic alopecia: 12 years old male) approx. 2
Head power from year 111f; 1. I noticed that my skin and sebum increased, so I used two devices. After a while, redness appeared on the forehead and hair loss increased. Because the hairline on my forehead had increased to 157 cm, I panicked and started using Fuwa once in December 1939. After about one row, I noticed redness, curly hair, and decreased hair loss. After about 3 months, terminal hair began to appear.

After that, do you continue to use the main rule? Vice A'1 River is 1\(
do not have. This is Kinoe Machina's own case.

Clinical trial example 4 (senile alopecia 52:J' 17↑
11) Approximately +2<r ago, after losing a relative, I started to notice 2ial fφ↑11 hair loss. For this reason, the patient visited the Department of Dermatology, Department of Dermatology, 7th Division, Fukuku Hospital, Kyoto University, and used the prescribed patch, but no improvement was observed. After that, 15% for hair removal! I 1. I had given up on it, but next year it will be 5 ft 3 Jl, 7'l' ljJ:
2 years ago, I visited the Department of Dermatology, Department of Dermatology, Faculty Affiliated Hospital, and was prescribed a treatment for the condition. Head strength in about a week, -
Although 1mm was lost, there was no change in hair loss 11F. Approximately 2 weeks later, hair loss fiiH was reduced to 1', shavings were reduced, and new vellus hair was observed. After about a month and a half, hair all over the head ■11-
There is a lot of hair loss, and the hair loss is still the same.
1, te21). When he visited the hospital about 4 months later, the hair on his forehead had become noticeably thicker.

Clinical trial example 5 (37-year-old male with desk plate alopecia) + <
+2 months ago 1jii I noticed that I was losing a lot of hair.

It was accompanied by the power of Jl Mi and the pretending of Ta H1. There was no mental stress, and for this reason, in February 1980, he visited Kyoto University Hospital Pediatrics 1#f:I, where he was prescribed a treatment. When she visited the hospital about a month later, her symptoms had decreased by 1°, her tsuku had decreased, and the threat of hair loss had also decreased somewhat.

In a clinical trial, (51) male + 1+) hair loss increased in the forehead area and ``rJnrrt area'' for about 5 years, and hair loss increased in the same period.Mental (For this reason, I started using a water solution from April 1930. After about a month, I noticed a decrease in caries and hair loss, and at the same time, I noticed 7J of new vellus hair.) Perhaps because I continue to use the liquid medication, the hair on one section of my head is now darkened to the extent that it is thin or 11 times black.There are no particular side effects.

Clinical test example 7 (senile alopecia 520-male t'l
) Childhood (1!f) He had suffered an injury to his head, and due to the scars, the hair on the rf! part of his head had thinned and he was using a ``wig.'' Approximately 5
From 2011, rtif hair on the forehead and top of the head! It's all over the place.

Soi: 417 (Nari Kyoto University Hospital Skin T1■
I visited the department. I prescribed a liquid medication and looked at the situation. (Also, after about 2 weeks, hair loss decreased and vellus hair started to grow.Currently, progress is being monitored.

Most of the following clinical test examples are based on the present invention 11 or S:It v
#Y treated at the dermatology department of J.
i:3.

Claims (1)

[Claims] Old man whose main ingredient is 1 hit "I" ↑ 11, fat Kj
1'1 and alopecia therapeutic agent