JPS6011884B2 - Cosmetics for hair and skin care - Google Patents

Description

DETAILED DESCRIPTION OF THE INVENTION The present invention relates to hair and skin care cosmetics which are highly suitable for obtaining strong hair growth and healthy and well-groomed skin, especially the scalp.

It has long been said that cosmetic changes in hair and skin are caused by hormonal imbalance2. Cosmetic disorders such as extreme hair loss and pimples have therefore been attempted to be treated with cosmetic agents supplemented with certain hormones and/or vitamins. They found that a series of natural and synthetic female hormones (oestrone, estradiol, and stilbestrol) are similar in their hormonal and skin tissue effects. Therefore, it was natural to utilize the effects of these sex hormones for cosmetic purposes. Treatment with hormonal creams, for example creams containing estrogen, transforms aging skin into a fresh and youthful phenotype. Since these female hormones are thought to stimulate hair growth, ostrogens and extracts containing estrogen are used in biological hair lotions. These cosmetic agents are mainly used by men, who are said to experience more hair loss than women, so it cannot be said that there are problems with the use of these cosmetic agents.Hormonal Even if the amount is very small, it is effective, and ``its effects are not localized only to the place where it is used, but some of it penetrates deep into the skin layer, reaching the blood vessels.'' Therefore, even a small amount of the hormone entering the bloodstream produces distinct physical or psychological effects.

The use of hormonally active agents in cosmetic preparations therefore has the disadvantage that they may give rise to unintended systemic effects and must be very limited for cosmetic use. A search has been made for agents that can avoid the above-mentioned operational disadvantages, have the desired cosmetic effect reliably, and have little hormonal effect. Progesterone and a series of similar steroids have come to be known as such agents that are chemically similar to the above-mentioned estrogen. However, since these active agents also always act as sex hormones, their use as cosmetic agents must be extremely limited. For example, cosmetic changes caused by male hormones, such as androgenetic alopecia, are mostly due to the production of testosterone by male reproductive hormones.

Therefore, hair loss on the forehead and crown occurs when the blood reaches a certain dangerous level of testosterone concentration. In women, only a slight excess of normal plasma levels of testosterone is sufficient to cause excessive hair growth, especially beard growth (abnormal hair growth). The contradictory effects of testosterone, such as promoting hair loss on the forehead and top of the head on the one hand, and promoting beard growth on the other, are based on the same mechanism.

These are well understood, and experiments have been conducted to reduce or prevent the above-mentioned modulations due to the influence of this mechanism. In order to prevent the action of the enzyme 5Q-reductase, which transforms testosterone into dihydrotestosterone within cells,
For example, the progesterone progesterone was added.
Dihydrotestosterone is more effective than testosterone and binds to proteins (receptors). This complex is transported to the intracellular plasma where it influences genetic information. Efforts have therefore also been made to prevent the formation of receptor complexes, for which cip-3 roterone acetate has also proven to be a suitable agent. Despite the fact that hair loss is observed in men with androgenetic alopecia when cosmetic agents are used locally in this way, pure cosmetic treatment is not possible because these agents have their own hormonal effects4. However, there are still problems when using these drugs for medical purposes, and some of them do not act locally, so they are not satisfactory. It is an object of the present invention to exhibit excellent effects in overcoming the above-mentioned cosmetic changes, and to provide an agent that does not have hormonal effects and that can be used locally for a long period of time. To provide a locally usable cosmetic for hair and skin care that does not cause side effects.

The above object is to provide a cosmetic for hair and skin care characterized by containing 11Q-hydroxyprosterone as an active agent in a mixture of additives commonly used for hair and skin care. achieved.

The active agent 11Q-hydroxyprogesterone used in the present invention is well known and was already synthesized and manufactured in 1952, but no significant hormonal action has been shown in animal experiments.

[Proc. Soc. Expert. Biol. &Med
．． 82 (1953) pages 243-247]. 11
Q-hydroxyprogesterone is not present in human tissues and has a special inhibitory effect on the 5Q-reductase of testosterone.

The 11Q-hydroxyprogesterone used in the present invention is highly suitable for treating the cosmetic abnormalities mentioned above, and this agent also has the advantage of having no hormonal or other undesirable side effects. Therefore, there is no problem with using it in cosmetic drugs.

In particular, the cosmetic composition according to the invention containing this active agent is suitable for local hair and skin care;
After a relatively short period of time (8-12 days), fat production is significantly reversed in the case of oily hair, and with continued use, hair loss is noticeably reduced. Even in the case of treating colds, the symptoms in question recede or in many cases disappear after only a short period of action. Hair abnormalities such as androgenic alopecia, excessive hair fat generation "11Q-hydroxyprogesterone's excellent cosmetic effect when applied locally with common wipes is 16
This was proven through months of clinical experiments on men and women aged 7 to 54.

Ten men with excessive hair fat and alopecia were treated with 1% 11Q-hydroxyp in 60% ethanol for 4 to 6 months.

Approximately 1 dose per day for topical treatment with gesterone solution
Rub the solution of 0-15 secretion into the scalp, the result is about 5-15
A marked regression of hair loss was observed after 6 weeks, which returned to a completely normal state with further treatment.
No side effects were observed during the entire treatment. Next, 14 women with similar severe hair fat and/or androgenetic alopecia were given the same treatment.
In this case, the first effects appeared in 12 people within 8-12 days in the form of a clear reduction in hair fat development, and after 5-6 weeks a marked regression of hair loss was observed. Some of the people who did the experiment didn't like the fact that their hair became dry. However, by further reducing the alcohol content with certain additives and/or taking care of the skin, or by using another suitable alcohol, such as isopropanol, this may occur occasionally or in people with particularly sensitive skin layers. This kind of incidental phenomenon that only occurs can be suppressed. Other than this, even in the case of women, no local or general side effects appeared during the treatment. In the next experiment, we tested five women and four men who had pimples on their faces and upper bodies.
Approximately 1.4% by weight of 11 in normal fat-containing ○/W emulsion
Treated with a special night cream containing Q-hydroxyprogesterone.

I rubbed this cream once a day into the affected areas of my skin that were covered with flakes. In all cases, a marked regression of the pimple rash was observed already after 8-10 days. Further, by applying local treatment, permanent improvement of the condition was observed after about 15 to 20 days. There were no local or global side effects during or after the treatment. In a parallel experiment, 11Q-hydroxyprogesterone acetate was added to a 1% alcohol solution for 1.
A 4% amount of night cream was used by men and women suffering from severe hair fat formation, hair loss, and pimples.

In either case, the same effect as in the case of 11Q-hydroxybrogesteroso was obtained. The table below shows 11Q
- Presented individual results regarding the cosmetic effects of hydroxyprogesterone.

Each effect is expressed by the following symbols. 10: Effective 10: Quite effective 100: Very effective −: No effect ±: The effect is doubtful Table 2 60
Table 3: Treatment of men with excessive hair steatosis and androgenic alopecia with 1% 11a-hydroquine brogesterone solution in % ethanol. The wipes were treated with a cosmetically applied fat-containing night cream (0/W emulsion) in the usual manner and amounts containing % 11a-hydroquine progesterone.

(Notes) a) Experimenter No. 6 made a full recovery and was discharged from the hospital after 5 months of treatment. In the next experiment, a 1% solution of 11Q-hydroxyprogesterone in ~60% ethanol was applied once daily to the forehead skin of two healthy men. J. at the stage before treatment and at the stage after 14 and 15 days respectively. S. Stra order s and P. E. PocHI's J. IN
VEST. Dennis. 36chi 293-298 (1961
) The sebum content of the forehead skin layer was measured by weight. The results are shown in Table 4. Table 4: 1% of 60% ethanol
Effect of sebum content on forehead skin by treatment with 11a-hydroxy-11 brogesterone solution. 11 from the above 4 tables
It is clearly seen that a relatively short treatment with Q-hydroxyprogesterone significantly lowers the sebaceous line movement.

This shows that the active agent according to the invention penetrates the cortical layer and produces an effect on the skin area to be treated. These observations are consistent with the results obtained when treating excessive hair steatosis, androgenetic alopecia, and pimples. The above experimental results show that 11Q-hydroxyprogesterone used according to the present invention can be used locally without causing hormonal or other local or general side effects, especially in the case of hair abnormalities and flakes caused by male hormones. This indicates that the product is a cosmetic for hair and skin care that produces cosmetic effects when used.

It can therefore be seen that this relates to purely cosmetic care cosmetics. The invention furthermore relates to the use of the active agents for producing hair and skin care cosmetics. The hair and skin care cosmetics according to the present invention contain, in addition to the above-mentioned active agents, additives to be used depending on the respective cosmetic purpose.

Therefore, the cosmetics according to the present invention can be commercialized as hair tonics, hair oils, oils for skin layer function, skin nourishing emulsions, aerosol sprays, shampoos, and hairdressing agents. The above agents for use in the present invention also include other general and specialized skin and hair care formulations. The active agents used according to the invention are incorporated into the preparation in amounts that, when used regularly, ensure reliable action.

According to experiments, the amount of the active agent is approximately 0.5% based on the total amount of cosmetics.
~2. A concentration of 0.8 to 1.4% by weight, in particular, falls within the above-mentioned guaranteed amount. Next, each example is an example of the invention using 11Q-hydroxyprogesterone, as well as one of the pharmaceutically acceptable esters of 11Q-hydroxyprogesterone, to produce hair and skin care cosmetics. Example 1 Production of hair tonic Isopropyl alcohol extra 529 ethyl polyglycol acetate 2911Q-hydroxyprogesterone 1.2 Perfume oil
0.8 evening distilled water
44.09100-0 antidepressant,
Perfume oil, ethyl polyglycol acetate, is mixed with inpropyl alcohol and the mixture is soaked in water for 100 minutes.

Example 2 Preparation of hair oil Isopropyl palmitate 30.0 Tysopropyl myristate 20.0 Tavaserin oil 47.0 1
1Q-Acetoxyprogesterone 1.8T Perfume Oil 0.7T Dichlorophene 0.5T 100-
0 Example 3 Manufacture of skin cream Fantang oil (fat) 10.0 Tacetin oil (mixture consisting of esters of unsaturated C,2-C,8 fatty acids) 12.0 Tacetyl alcohol and stearyl alcohol 12.0 Tacetyl alcohol Sodium salt of stearyl sulfate 3.0% glycerin 6.0% 11Q-acetoxyprogesterone 1.4% perfume oil
0.6 Yusui
55.0 evening 100-0 evening Example 4 Production of shampoo Fatty acid-protein aggregate (“Lamepon 60'') 25.
0 tag glycerin monolaurate monozulfart 20
．． 0 Glycerin 7.
0 evening 11Q-Hydroxyprogesterone 0.
5 ta perfume oil 0.5 Yumi 47.0 Yu1
The preferred embodiments of the present invention described above are summarized below.

{1' 11Q for producing hair and skin care cosmetics based on any of claims 1 to 5;
-Hydroxyprogesterone and/or the 11Q
- Using one of the esters of hydroxyprogesterone.

[21] Use of 11Q-acetoxyprogesterone to produce a hair and skin care cosmetic according to claim 1.

Claims (1)

[Scope of Claims] 1. A cosmetic for hair and skin care, characterized in that it contains 11α-hydroxyprogesterone as an active agent in a mixture with common additives. 2. The cosmetic according to claim 1, characterized in that the active agent is added to a hair tonic or hair oil. 3. The cosmetic according to claim 1, characterized in that the active agent is added to a skin cream. 4 Claim 1 characterized in that the active agent is added to the shampoo
Cosmetics listed in section. 5. The cosmetic according to any one of claims 1 to 4, wherein the active agent is added at a concentration of about 0.5 to 2.0% by weight based on the total amount of the cosmetic. . 6. The cosmetic according to any one of claims 1 to 5, characterized in that the active agent is added at a concentration of about 0.8 to 1.4% by weight based on the total amount of the cosmetic. .