JPH04505155A - How to use siloxane to induce and promote hair growth and inhibit hair loss - Google Patents

Abstract

(57) [Summary] This bulletin contains application data before electronic filing, so abstract data is not recorded.

Description

[Detailed description of the invention] The present invention provides 7-α-( acetylthio)4',5'-cybadrospiro[androst-4-ene 17.2 '-(3'H)furan)3-one or spiroxacin in cosmetics or drugs and apply it.

Hair growth or regeneration depends primarily on the activity of hair follicles.

The activity of hair follicles is cyclical, consisting essentially of an anadiene phase, a catadiene phase and a telodiene phase. It consists of periods.

Growth is stimulated during the anadiene phase, which lasts for several years, during which the hair grows longer. Following this The catadiene phase is very short and temporary, and the telodiene phase, which lasts several months, is the body breath phase. It is.

At the end of the breathing period, the hair on the head falls out and a new cycle begins. Therefore, human hair It regenerates constantly, and about lθ% of the 150,000 hairs on the head are in the breathing phase, and after several months. It is something that is supposed to be regenerated within.

Hair loss is often hereditary and occurs primarily in men.

This is particularly true for androgenic, androgenic, and even androgenic hormonal alopecia. means.

This alopecia mainly causes abnormalities in hair regeneration, and the first stage is It starts with shortening the cycle, on which the quality and quantity of hair depends. due to hair loss The quality of downy hair gradually deteriorates to the point where it is said to be in the "late stage" state. Range of hair removal It is most common in the temporal region or frontal region in men, and in the parietal region in women.

The cosmetics and pharmaceutical industries have been trying to stop hair loss caused by androgenic hormones for quite some time. or reduce, in particular compositions that induce or promote hair growth or reduce hair loss. I've been researching things. Traditionally, pyrimidine derivatives such as minoxidil have been used for this purpose. Retinoids such as conductor and retinol acid have been proposed.

The present invention shows that today, when spiroxacin is applied topically, it has little effect on hair regrowth. This fact indicates that it can induce and promote hair growth and suppress hair loss. That's what I saw.

Spiroxacin (DCI) or 7-α (acetylthio) 4', 5' Cibadro Spiro(androst4-ene17,2'-(3'H)furan)3-one is , is a known compound, especially known for its diuretic properties.

In order to clarify the potency and quick-acting effect of the composition of the present invention, trichogram method, preferably a phototrichogram, to target hair in the telogen stage. The percentage of hair in the nadien stage was determined. Trichogram test is a It has been clarified that loxacin is particularly effective against androgenic alopecia.

One subject of the present invention is a method for inducing or promoting hair growth and suppressing hair loss. , consisting of topically applied cosmetic or medicinal compositions.

Another subject of the invention is a method of cosmetic treatment using the aforementioned composition. It consists of

Other subjects of the invention will become clear from the detailed description of the invention and the examples that follow. Probably.

Eyes applied topically on the scalp to induce and promote hair growth and inhibit hair loss The composition used in the It is characterized by containing spiroxacin.

Spiroxacin or further 7-α(acetylthio)-4',5'-cibide Rospiro [androst4-ene17.2'-(3'H)furan)3-one may be used as such in a cosmetically or pharmaceutically acceptable form, or in its salts or Can be used as an ester. In particular, I mention that acetate here.

Spiroxacin is used in an amount of 0.1 to 15% by weight of the total composition, preferably 1 to 10% by weight. It is preferable to use % by weight.

The alcohol-based physiologically acceptable solvent used in the present invention is preferably Preferably, it contains one or more other cosmetically or pharmaceutically acceptable solvents. alcohol or hydroalcohol.

The alcoholic medium is preferably an anhydrous medium, i.e. with a water content of 1% or less, and one or two or more lower alcohols of 01 to 04, such as ethyl alcohol, Sopropyl alcohol or quaternary butyl alcohol, particularly preferably ethyl alcohol It consists of a mixture of alcohol and isopropyl alcohol. Used in hydroalcoholic medium The alcohol used is selected from the C3 to C4 lower alcohols mentioned above. Ru.

Other solvents that can be used in the compositions of the invention include propylene glycol, among others. alkylene glycol, or an alkyl group or an alkylene group having 1 to 4 carbon atoms Alkylene glycols, particularly preferably ethylene glycol monoethyl ether , propylene glycol monoethyl ether, and diethylene glycol mono It is ethyl ether.

These different media can be thickened using well-known thickening or gelling agents. You can. For example, especially heterobiopolysaccharides: for example xane Sun gum, scleroglucan, methylcellulose, hydroxymethylcellulose carboxymethyl cellulose, hydroxybutyl cellulose, hydroxy Dimethyl cellulose, hydroxypropylene cellulose, methyl hydroxy Cellulose derivatives such as ethyl cellulose and methyl hydroxypropyl cellulose Conductor, multifunctional conductor such as rcARBOPOLJ sold by GOODRICH Polyacrylic acid etc. that have been reticulated with a functional agent are fried. used in the present invention The amount of the thickening agent used is 0.1 to 3% by weight, particularly preferably 0.1 to 3% by weight, based on the total amount of the composition. It accounts for 4 to 3% by weight.

Particularly preferred media include absolute alcohol and aqueous alcohol with a water content of 50% or less. Consisting of le cole.

One particularly preferred embodiment of the invention provides at least one alcohol and the aforementioned Contains 85 to 99.9% by weight of one non-alcoholic solvent based on the total composition using an alcoholic or hydroalcoholic medium.

It is of course also possible to mix spiroxacin into the solvent body at the time of application.

The composition according to the invention may also be used to induce or promote hair growth and to inhibit hair loss. substances such as minoxidil and/or retinoids can of course also be present. Ru.

The compositions of the present invention are not commonly used in cosmetics or pharmaceuticals in carrying out suitable compositions. It also contains other additives, especially surfactants, preservatives, alkalinizing agents and acidifying agents. It can contain. The pH of this composition is between 3 and 9, preferably between 5 and 8. be.

Preferred forms of these compositions include lotions, gels, emulsions, creams, creams, creams, etc. In some cases, it is an aerosol.

These compositions are suitable for shampoos containing surfactants with cleaning properties in the composition. When taking a shape, rinsing with water is inevitably involved.

If the composition is prepared at the time of application, several compartments or a [kit]-like device and and the first compartment contains spiroxacin and the second compartment contains the solvent. Can be done. The partitions or elements containing spiroxacin should be made of light-resistant materials. It is preferable that Treatments for hair loss and regrowth include shampoos, After washing the scalp and hair with a shampoo or immediately after shampooing, apply the above-mentioned composition. Apply mainly to the bald areas of the scalp and on the hair. The preferred usage is 200 The composition according to the present invention was applied to the depilated areas of the scalp from 300 cm to 300 cm. - Consists of daily application. This treatment may last several years Ru.

It is recommended to monitor the effectiveness of this treatment monthly using phototricrograms. Yes. The composition according to the present invention increases the A/T (anadiene/telodiene) ratio. It was found that it showed a more significant effect.

Another subject of the invention is a preparation for the treatment of alopecia, in particular androgenic alopecia. spiroxacin in a composition containing spiroxacin.

The treatment method according to the present invention treats hair and scalp within the scope of cosmetic use, that is, non-treatment. It is characterized by treatment in the sense of not supplementing the added ingredients but making them beautiful. do.

The treatment method according to the invention is based on the fact that the active ingredients act on biological mechanisms. Within the scope of use, there is one additional treatment method, especially the treatment of androgenic alopecia. constitute therapy.

The examples given below are illustrative of the invention and are not intended to impose any limitations.

Example 1 Preparing an active lotion that promotes hair growth and inhibits hair loss.

Composition: in 100g Spiroxacin 1.5g Propylene glycol 6.45g Ethyl alcohol remaining amount Apply 0.03-mL of this lotion to the depilated area once a day for 3 months.

A reduction in hair loss and hair regeneration was observed.

Example 2 A lotion is prepared that inhibits hair fall and aids in hair regeneration.

Composition + 100g Spiroxacin 0.95g Remaining amount of mixture consisting of three components Ethyl alcohol 81.6g Isopropyl alcohol 13.6g Propylene glycol 4.7g Apply this lotion on your scalp once a day. Two months later, hair regrowth was observed.

Example 3 Preparing a lotion that aids hair regeneration and inhibits hair fall Composition: in 100g Spiroxacin 1g Ethyl alcohol (l/3 weight) and Remaining amount of isopropyl alcohol (2/3 weight) mixture Apply this lotion once a day to the 100" to 200" scalp area where hair loss has occurred. 2-Activity of the composition for application to promote hair regrowth versus placebo Evaluate.

After several months of treatment, this composition can thoroughly promote hair regrowth. found.

Example 4 A lotion is prepared that aids hair regeneration and inhibits hair loss.

Composition: in 100g Spiroxacin 0.1g Propylene glycol 22.8g Ethyl alcohol 55.1g Water remaining amount I used this lotion for 3 months and lost 2 cal on the area where I lost hair! Apply 0.02- Ru.

Observe hair loss and regrowth.

Example 5 To prepare an alcohol-containing gel that promotes hair regeneration and suppresses hair fall.

Composition: in 100g Spiroxacin 1.2g Hydroxypropylcellulose 3g (product name: UCEL G, HERCU (manufactured by LES) Propylene glycol 6.45g Ethyl alcohol remaining amount Apply this lotion at a dose of 0.0.4 mN on the hair removed area Jan' every day for 3 months. Applied once.

A decrease in hair fall and regeneration was observed.

Example 6 Prepare kits for treatments to aid hair regeneration and reduce hair fall. Ru.

1. Kit or component A consists of 1.5g of powdered spiroxacin kept in a container. It is preserved.

The second kit or component B contains 93.5 g of isopropyl alcohol and 93.5 g of propylene. Consists of 100g liquid containing 6.5g glycol.

Mix components A and B at the time of use. Apply the mixed ingredients to 0.0 cm on the hair removal area. Apply 2- each for 3 months.

As a result of the phototricrogram test, a reduction in hair shedding and regeneration were observed. .

Procedural amendment (voluntary) September 6, 1991

Claims (14)

[Claims] 1. At least 7-α-(acetylthio)4',5'-dihydrospiro[an Drost-4-ene 17,2'-(3'H)furan]3-one or spiroxazo or any of their salts or their esters based on alcohol hair growth inducing or A topically used composition that promotes and inhibits hair loss. 2. Spiroxazone is present in the composition in an amount of 0.1 to 15% by weight, preferably 1 to 10% by weight. A composition according to claim 1, characterized in that it contains % by weight. 3. If the physiologically acceptable alcohol-based solvent is absolute alcohol or The composition according to claim 1 or 2, which is a hydroalcohol. 4. The solvent whose main component is alcohol is a mixture of C1 to C4 lower alcohols. The composition according to claim 3, characterized in that it consists of: 5. In this solvent, further alkylene glycol or monoalkylene glycol is added. and an alkyl ether of dialkylene glycol. 4. The composition described in 4. 6. The solvent containing hydrous alcohol contains 50% or less water, and one or two types The above C1 to C4 lower alcohols and one or more alkylene groups The composition according to claim 3, characterized in that it contains a recall. 7. The solvent may contain a thickening agent in an amount of 0.1 to 5% by weight based on the total weight of the composition. 4. A composition according to claim 3, characterized in that it is concentrated by. 8. Physiologically acceptable media include ethyl alcohol and isopropyl alcohol. The composition according to claim 4, comprising: 9. The physiologically acceptable medium is lower alcohol, alkyl, consisting of C1 to C4. lene glycol, any alkyl ether of mono- or diethylene glycol according to claim 3, characterized in that it is selected from among these and contains 85 to 99.9% by weight. Composition. 10. A claim further comprising minoxidil and/or a retinoid. Compositions according to items 1 to 9. 11. Any of claims 1 to 10, wherein the applicable method is the treatment of androgenic alopecia. The composition according to crab. 12. The composition according to any one of claims 1 to 10 may be used in patients suffering from alopecia. A treatment method using hair cosmetics for the scalp, which is characterized by applying it on the scalp. . 13. For the preparation of compositions intended for the treatment of androgenetic alopecia The use of spiroxazone. 14. Spiroxazone in the first compartment and alcohol in the second compartment Contains primarily a physiologically acceptable vehicle for spiroxazone, and upon use contains 2 characterized in that the contents of the first compartment are mixed with the contents of the first compartment. A device consisting of several compartments or "kits".