EP0464034A1 - Verwendung von spiroxazon zum induzieren und stimulieren des haarwuchses und zum verringern des haarausfalles - Google Patents

Verwendung von spiroxazon zum induzieren und stimulieren des haarwuchses und zum verringern des haarausfalles

Info

Publication number
EP0464034A1
EP0464034A1 EP19900903597 EP90903597A EP0464034A1 EP 0464034 A1 EP0464034 A1 EP 0464034A1 EP 19900903597 EP19900903597 EP 19900903597 EP 90903597 A EP90903597 A EP 90903597A EP 0464034 A1 EP0464034 A1 EP 0464034A1
Authority
EP
European Patent Office
Prior art keywords
composition according
spiroxasone
medium
composition
physiologically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP19900903597
Other languages
English (en)
French (fr)
Inventor
Robert Aron-Brunetiere
Gérard HABRIOUX
Jean-François Grollier
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LOreal SA
Original Assignee
LOreal SA
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by LOreal SA filed Critical LOreal SA
Publication of EP0464034A1 publication Critical patent/EP0464034A1/de
Withdrawn legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00Preparations for affecting hair growth
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63Steroids; Derivatives thereof

Definitions

  • the present invention relates to the application in cosmetics and pharmacy of 7- ⁇ - (acetylthio 4 ', 5'-dihydrospiro [androst 4-ene 17.2 , - (3'H) furan] 3-one or spiroxasone to induce and stimulate hair growth and reduce hair loss.
  • Hair growth and renewal is mainly determined by the activity of the hair follicles. Their activity is cyclical and essentially comprises three phases, namely the anagen phase, the catagen phase and the telogen phase.
  • the active anagen phase or growth phase which lasts several years during which the hair lengthens, is followed by a very short and transient catagen phase and a rest phase called the telogen phase of a few months.
  • hair loss occurs on genetically predisposed subjects and it affects men in particular. More particularly, it is androgenetic or androgenic or androgenogenetic alopecia.
  • This alopecia is essentially due to a disturbance of the capillary renewal which involves, initially, the acceleration of the frequency of the cycles at the expense of the quality of the hair then their quantity.
  • compositions which make it possible to suppress or reduce the effect of androgenetic alopecia and in particular to induce or stimulate the growth of hair or to reduce their fall.
  • pyrimidine derivatives such as minoxidil or retinoids such as all-trans retinoic acid have been proposed for this purpose;
  • spiroxasone when used, in topical application, had a surprising activity on regrowth of the hair and made it possible to induce and stimulate the growth of the latter and reduce their fall.
  • the trichogram or preferably the phototrichogram is used which makes it possible to determine inter alia the percentage of hair in the anagen phase compared to the hair in the telogen phase. Examination of the phototrichogram determined that spiroxasone was particularly effective in the treatment of androgenetic alopecia.
  • An object of the invention consists of cosmetic or pharmaceutical compositions used in topical application, with a view to inducing and stimulating hair growth and reducing their fall.
  • Another object of the invention consists of a cosmetic treatment process using said composition.
  • Other objects of the invention will appear on reading the description and the examples which follow.
  • compositions intended to be used in topical application to the scalp, with a view to inducing and stimulating hair growth and reducing hair loss are essentially characterized by the fact that they contain spiroxaisone in a physiologically acceptable solvent medium based alcohol.
  • [androst 4-ene 17.2 '(3'H) furan] 3-one can be used as it is or in the form of its salts or esters acceptable in cosmetics and in pharmacy. Mention may more particularly be made of acetate.
  • Spiroxasone is preferably used in proportions of between 0.1 and 15% by weight relative to the total weight of the composition and preferably between 1 and 10% by weight.
  • the physiologically acceptable alcohol-based solvent medium used in accordance with the invention is preferably an alcoholic or hydroalcoholic medium which may contain one or more other solvents acceptable in cosmetics or in pharmacy.
  • the alcoholic medium is preferably an anhydrous medium, that is to say containing less than 1% of water and containing one or more lower alcohols, C 1 -C 4 such as ethyl alcohol, isopropyl alcohol or alcohol. tert-butyl, a mixture of ethyl alcohol and isopropyl alcohol being particularly preferred.
  • the alcohols used in hydroalcoholic media are chosen from the lower C 1 -C 4 alcohols indicated above.
  • the other solvents which can be used in the compositions in accordance with the invention are in particular chosen from alkylene glycols such as propylene glycol, or in which the alkyl or alkylene group contains between 1 and 4 carbon atoms and more particularly the ethylene glycol monoethyl ether, propylene glycol monomethyl ether and diethylene glycol monoethyl ether.
  • thickening or gelling agents well known in the state of the art such as more particularly heterobiopolysaccharides.
  • xanthan gum and scleroglucans cellulose derivatives such as methylcellulose, hydroxymethylcellulose, carboxymethylcellulose, hydroxybutylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, methylhydroxyethylcellulose, hydroxyacylcellulose polyfunctional agent such as the products sold, under the name of "CARBOPOL" by the company GOODRICH.
  • the thickening agents are preferably used in the compositions in accordance with the invention in proportions of between 0.1 and 5% by weight, in particular between 0.4 and 3% by weight relative to the total weight of the composition.
  • the particularly preferred media consist of essentially anhydrous alcoholic, hydroalcoholic media preferably comprising less than 50% water.
  • a particularly preferred embodiment of the invention consists in using an alcoholic or hydroalcoholic medium containing at least one alcohol and one of the non-alcoholic solvents indicated above in proportions of between 85 and 99.9% by weight relative to the total weight of the composition.
  • compositions in accordance with the invention may contain other agents making it possible to induce and stimulate hair growth and to reduce their fall, such as for example Minoxidil and / or retinoids.
  • compositions in accordance with the invention may also contain other adjuvants usually used in the cosmetic or pharmaceutical field with a view to producing topical compositions such as more particularly surface-active agents, preserving agents, basifying or acidifying agents.
  • the pH of these compositions can vary between 3 and 9 and preferably between 5 and 8.
  • compositions are lotions, gels, emulsions, creams which may be pressurized in aerosols. These compositions can be applied by making them optionally follow their application with rinsing with water or optionally in the form of a shampoo in which case they necessarily contain a surfactant having detergent properties, well known in the art. technical.
  • the composition When the composition is prepared just at the time of use, it is possible to package it in the form of a device with several compartments or "kit" in which one of the compartments or one of the elements contains spiroxasone and the other the solvent medium.
  • the compartment or element containing the spiroxasone is preferably made of a photoprotective material.
  • the treatment for combating hair loss and promoting regrowth consists mainly in applying to the alopecic areas of the scalp and the individual's hair, a composition as defined above, for example after washing the scalp and hair using a shampoo or shortly after shampooing.
  • the preferred mode of application consists in applying 2 ml of the composition according to the invention to the alopecic area on a surface of 200 to 300 cm 2 of the scalp at a daily frequency.
  • the treatment can be continued for a few years.
  • the effectiveness of the treatment is preferably checked once a month by means of a phototrichogram. It was found that the composition according to the invention made it possible to obtain particularly surprising results by increasing the A / T ratio (anagen / telogen).
  • Another object of the invention is constituted by the use of spiroxasone for the preparation of a therapeutic composition intended for the treatment of alopecia, in particular androgenetic alopecia.
  • the treatment method according to the invention has the characteristics of a cosmetic treatment insofar as it makes it possible to treat the hair and the scalp in the cosmetic sense of the term, that is to say to provide them with the substances which missing and embellish them.
  • the method according to the invention also constitutes a therapeutic treatment insofar as the active substance acts on the biological mechanism of the hair cycle and allows in particular a therapeutic treatment of androgenetic alopecia.
  • the active lotion on hair growth and the reduction of hair loss of the following composition, is prepared:
  • This lotion is applied at the rate of 0.03 ml to an alopecic area of 3 cm 2 once a day for three months.
  • a lotion is prepared which makes it possible to halt hair loss and to promote their regrowth, of the following composition:
  • This lotion is applied once a day to the scalp. After two months of treatment there is a clear regrowth of hair.
  • a lotion is prepared which promotes hair regrowth and prevents hair loss, of the following composition:
  • composition for stimulating hair regrowth is evaluated in relation to a placebo, by applying 2 ml of this composition at the rate of one application per day to an alopecic area of 100 to 200 cm 2 of the scalp. In a few months of treatment, the composition effectively improves hair regrowth.
  • a lotion promoting hair regrowth and preventing hair loss is prepared, of the following composition:
  • This lotion is applied at the rate of 0.02 ml to an alopecic area of 2 cm 2 for three months.
  • An alcoholic gel having a positive action on the regrowth of hair and the reduction of their fall is prepared, of the following composition:
  • This lotion is applied at the rate of 0.04 ml to an alopecic area of 4 cm 2 once a day for three months.
  • a kit is prepared, the content of which is intended for use in a treatment which promotes hair regrowth and prevents hair loss.
  • a first element of the kit or component A is constituted by 1.5 g of spiroxazone in the form of powder stored in a container.
  • the second element of the kit or component B consists of 100 g of a solution comprising 93.5 g of isopropanol and 6.5 g of propylene glycol. Components A and B are mixed at the time of use. The resulting composition is applied in an amount of 0.02 ml to an alopecic area of 2 cm 2 for 3 months.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Cosmetics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EP19900903597 1989-02-13 1990-02-13 Verwendung von spiroxazon zum induzieren und stimulieren des haarwuchses und zum verringern des haarausfalles Withdrawn EP0464034A1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR8901824 1989-02-13
FR8901824A FR2642965B1 (fr) 1989-02-13 1989-02-13 Utilisation de la spiroxasone pour induire et stimuler la croissance des cheveux et diminuer leur chute

Publications (1)

Publication Number Publication Date
EP0464034A1 true EP0464034A1 (de) 1992-01-08

Family

ID=9378713

Family Applications (1)

Application Number Title Priority Date Filing Date
EP19900903597 Withdrawn EP0464034A1 (de) 1989-02-13 1990-02-13 Verwendung von spiroxazon zum induzieren und stimulieren des haarwuchses und zum verringern des haarausfalles

Country Status (5)

Country Link
EP (1) EP0464034A1 (de)
JP (1) JPH04505155A (de)
CA (1) CA2047169A1 (de)
FR (1) FR2642965B1 (de)
WO (1) WO1990009164A1 (de)

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4054563A (en) * 1975-04-25 1977-10-18 Ciba-Geigy Corporation Process for the manufacture of spiro compounds of the steroid series
FR2588755B3 (fr) * 1985-10-21 1988-01-22 Aron Brunetiere Robert Composition therapeutique a base de spironolactone destinee au traitement des alopecies androgenogenetiques

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9009164A1 *

Also Published As

Publication number Publication date
JPH04505155A (ja) 1992-09-10
FR2642965A1 (fr) 1990-08-17
CA2047169A1 (fr) 1990-08-14
WO1990009164A1 (fr) 1990-08-23
FR2642965B1 (fr) 1991-06-07

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