WO1986001402A1 - Moyens de traitement du phenomene d'androgenisation et utilisation d'antiandrogenes pour leur production - Google Patents

Moyens de traitement du phenomene d'androgenisation et utilisation d'antiandrogenes pour leur production Download PDF

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Publication number
WO1986001402A1
WO1986001402A1 PCT/DE1985/000307 DE8500307W WO8601402A1 WO 1986001402 A1 WO1986001402 A1 WO 1986001402A1 DE 8500307 W DE8500307 W DE 8500307W WO 8601402 A1 WO8601402 A1 WO 8601402A1
Authority
WO
WIPO (PCT)
Prior art keywords
acetate
contraceptive
antiandrogenic
amounts
agent
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.)
Ceased
Application number
PCT/DE1985/000307
Other languages
German (de)
English (en)
Inventor
Souhail Abdulla
Friedmund Neumann
Michael Töpert
Hans Wendt
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.)
Bayer Pharma AG
Original Assignee
Schering AG
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
Priority claimed from DE19843432584 external-priority patent/DE3432584A1/de
Priority claimed from DE19843442857 external-priority patent/DE3442857A1/de
Application filed by Schering AG filed Critical Schering AG
Publication of WO1986001402A1 publication Critical patent/WO1986001402A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/008—Preparations for oily skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/63—Steroids; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth
    • A61Q7/02—Preparations for inhibiting or slowing hair growth
    • F—MECHANICAL ENGINEERING; LIGHTING; HEATING; WEAPONS; BLASTING
    • F02—COMBUSTION ENGINES; HOT-GAS OR COMBUSTION-PRODUCT ENGINE PLANTS
    • F02B—INTERNAL-COMBUSTION PISTON ENGINES; COMBUSTION ENGINES IN GENERAL
    • F02B1/00—Engines characterised by fuel-air mixture compression
    • F02B1/02—Engines characterised by fuel-air mixture compression with positive ignition
    • F02B1/04—Engines characterised by fuel-air mixture compression with positive ignition with fuel-air mixture admission into cylinder

Definitions

  • the invention relates to a new anti-androgen-containing agent for the treatment of androgenizing symptoms, in particular for the treatment of women with androgenizing symptoms.
  • the invention further relates to the use of antiandrogen for the preparation of an agent for the topical treatment of symptoms of androgenization.
  • Symptoms of androgenization are chronic diseases such as acne, seborrhea, alopecia and hirsutism. These symptoms can be combined or isolated.
  • Hormonal treatment can have a beneficial effect on acne disease.
  • contraceptives especially low-dose oral contraceptives
  • an improvement in acne is often observed.
  • oral contraceptives that have been specially developed for women who suffer from signs of androgenization.
  • These contraceptives contain an antiandrogenic progestogen, which counteracts the androgenic stimulating influences (Med. Monthly Bulletin 31, 9 (1977) 425). In all of these cases, the antiandrogen is administered orally.
  • the increased sebum gland function is considered one of the most important pathogenetic factors for acne and seborrhea. It is androgen dependent and is reduced by the antiandrogenic oral contraceptive.
  • the skin lipids decrease as early as 2-3 months after the start of therapy. Hirsutism and alopecia are signs of greater androgenization than acne and seborrhea. Significant improvements can only be expected after a longer treatment period of about 6 - 9 months with an antiandrogenic contraceptive.
  • cyproterone acetate in alcoholic solution is said to be a suitable topical agent for reducing sebum secretion.
  • alcoholic cyproterone acetate solution if at all, can only influence a slight form of a hormone disorder caused by androgens.
  • the concentration of antiandrogen used in the lipophilic preparation is about 0.1 to 10, preferably 0.5 to 5.0 percent by weight.
  • Particularly suitable antiandrogens are steroid compounds which, in addition to the antiandrogens, also have gestagenic and antigonadotropic activity.
  • These steroid compounds preferably include the progestogen-derived progestogens cyproterone acetate, chlormadinone acetate and megestrol acetate.
  • All progestogens of the progesterone and 19-nortestosterone series can occur in the contraceptive to be administered orally or parenterally. Particularly favorable results are achieved if the contraceptive is administered orally and contains an antiandrogenic gestagen as a gestagen component.
  • the same progestogens are particularly suitable as anti-androgen-acting progestogens, preferably in the topical preparations Cyproterone acetate, chlormadinone acetate and megestrol acetate.
  • Diane (R) In the form of the well-known preparations Diane (R) ,
  • Eun ⁇ min (R) , Gestamestrol (R) or the corresponding preparations containing megestrol can be used.
  • progestogen and estrogen can also be lower than with the known preparations, as long as it is ensured that adequate conception protection is guaranteed.
  • the topical preparation is produced in a customary manner by converting the active ingredients into the desired application form, for example solutions, lotions, creams, ointments or plasters, with suitable additives, lotions, creams and ointments being preferred.
  • the active substance concentration depends on the form of administration.
  • an active ingredient concentration of 0.1 percent by weight to 10 percent by weight is preferably used.
  • the lotions or creams (oil / water emulsions) and the ointments (water / oil emulsions) can be prepared in a conventional manner using conventional emulsifiers (Kirk Othmer: Encyclopedia of Chemical Technology, 3rd edition, 1979; John Wiley & Sons , New York, Vol. 8, pages 900 - 930, and Dr. Otto-Albrecht Neumüller: Römpps Chemie Lexikon, 7th edition, 1973; Franckh 'sche Verlags Stuttgart, pages 1009-1013),
  • the waxes used for these emulsions, Emulsifiers and other additives are the same as are used conventionally (Dr.
  • the topical preparation according to the invention in the form of an oil / water emulsion can consist of hydrophilic and / or lipophilic active substances, fat phase, oil / water emulsifier, aqueous phase and preservatives.
  • Suitable as an oily phase or as a fat phase in the oil / water emulsion are hydrocarbons, such as petroleum jelly, paraffins or stearin, or waxes, such as beeswax.
  • Suitable oil / water emulsifiers are, for example, stearyl alcohol, polyoxyethylene stearates (such as MYRJ (R) ), complex emulsifiers (such as amphoterin (R) ) and sorbitan fatty acid esters (such as Span (R) ) or carboxyvinyl polymers (such as Carbopol ( R) ).
  • the aqueous phase can additionally contain buffer substances, such as, for example, the disodium salt or ethylenediamine-N, N, N ', N'-tetraacetic acid and preservatives, such as chloroquinaldol, parabens or benzalkonium chloride.
  • the proportion of the inner emulsion in the oil / water emulsion is preferably 10 to 49 percent by weight, the particle size of the inner emulsion is preferably between 1 ⁇ m and 100 ⁇ m.
  • the topical preparation according to the invention in the form of a water / oil emulsion likewise consists of hydrophilic and / or lipophilic additives, as are also used in the 01 / water emulsion, fat phase, water / oil emulsifier and aqueous phase.
  • hydrocarbons for example paraffins and petroleum jelly, synthetic, vegetable and animal oils or waxes (such as, for example, olive oil, peanut oil, fine bone oil, almond oil, lanolin, beeswax or sunflower oil)
  • synthetic, vegetable and animal oils or waxes such as, for example, olive oil, peanut oil, fine bone oil, almond oil, lanolin, beeswax or sunflower oil
  • fatty alcohols such as cetyl alcohol, myristyl alcohol, stearyl alcohol or ceryl alcohol
  • fatty acid esters such as
  • the proportion of the inner emulsion in the water / oil emulsion is preferably 30 to 49 percent by weight, the particle size of the inner emulsion is preferably between 1 ⁇ m and 100 ⁇ m.
  • the finely dispersed system is additionally mixed with the micronized active ingredient (grain size preferably 1 to 20 ⁇ ) and optionally also with fragrances, such as that of the Crematest (R) series, and the same is stirred until uniform distribution.
  • the micronized active ingredient grain size preferably 1 to 20 ⁇
  • fragrances such as that of the Crematest (R) series
  • the agent can be prepared by mixing the active ingredient into the ointment base in an oily solution.
  • ointment bases Numerous, preferably lipophilic, water-absorbing ointments come into consideration as ointment bases. Examples include the products Unguentum emulsificans and Unguentum leniens specified in DAB 7 and preparations based on petroleum jelly containing wool wax alcohols such as Eucerinum anhydricum.
  • the active ingredient is incorporated into an ointment base containing 4 to 6% by weight of dexpanthenol.
  • an ointment base containing 4 to 6% by weight of dexpanthenol.
  • the resulting agent was administered to 20 women with a beard once or twice a day. Before treatment, the patients were forced to shave every day to remove the beard growth. After a total treatment period of 8 to 12 weeks, 15 out of 20 patients could not shave.
  • the agent prepared according to Example 1 was administered topically once or twice a day to 20 patients with severe facial acne. The first treatment successes appeared after 2 to 6 weeks. After a total of 8 weeks of treatment, the acne symptoms in 16 patients had essentially disappeared. At this point, treatment was reduced to one application three times a week and continued for two years. No significant acne symptoms reappeared in 14 treated patients during this period.
  • Example 1 The agent prepared according to Example 1 was administered to 5 male patients with severe facial acne as described in Example 2. The same therapeutic successes as described in Example 2 were achieved. No side effects were observed.
  • Emulsion with a particle size of 20 - 70 ⁇ m is created.
  • DAB 8 vascular venous line (DAB 8)
  • R Dehymuls
  • R g
  • the water / oil emulsion is introduced into the oil / water emulsion with vigorous stirring under a vacuum of 10 torr.
  • the mixture is stirred until a dispersion with a particle size of 10 to 50 ⁇ is formed, and the vacuum is removed.
  • Sucrose mixture (shell) is added to about 90 mg.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Dermatology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Birds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

Les moyens de traitement du phénomène d'androgénisation contiennent un antiandrogène dans une pommade servant de base et développent une action thérapeutique lorsqu'ils sont appliqués localement. L'effet thérapeutique est renforcé lorsqu'un contraceptif est utilisé en même temps.
PCT/DE1985/000307 1984-09-05 1985-08-30 Moyens de traitement du phenomene d'androgenisation et utilisation d'antiandrogenes pour leur production Ceased WO1986001402A1 (fr)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DEP3432584.0 1984-09-05
DE19843432584 DE3432584A1 (de) 1984-09-05 1984-09-05 Mittel zur behandlung von hirsutismus und akne
DE19843442857 DE3442857A1 (de) 1984-11-22 1984-11-22 Mittel zur behandlung von androgenisierungserscheinungen bei der frau
DEP3442857.7 1984-11-22

Publications (1)

Publication Number Publication Date
WO1986001402A1 true WO1986001402A1 (fr) 1986-03-13

Family

ID=25824455

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DE1985/000307 Ceased WO1986001402A1 (fr) 1984-09-05 1985-08-30 Moyens de traitement du phenomene d'androgenisation et utilisation d'antiandrogenes pour leur production

Country Status (2)

Country Link
AU (1) AU4805085A (fr)
WO (1) WO1986001402A1 (fr)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0330583A3 (fr) * 1988-02-26 1991-03-13 L'oreal Méthode pour améliorer l'aspect esthétique de la peau à l'aide de mélanges polyvitaminiques et compositions cosmétiques pour sa mise en oeuvre
WO1991006284A1 (fr) * 1989-10-27 1991-05-16 Schering Aktiengesellschaft Berlin Und Bergkamen Preparations pharmaceutiques
EP0566979A1 (fr) * 1992-04-23 1993-10-27 Ingeborg Zingraf Lotion capillaire et procédé de traitement pour réduire la chute des cheveux et favoriser leur pousse
WO1994006436A1 (fr) * 1992-09-12 1994-03-31 Lts Lohmann Therapie-Systeme Gmbh & Co. Kg Emplatre contenant du dexpanthenol pour application transcutanee d'hormones steroides
US5344651A (en) * 1993-07-23 1994-09-06 The Procter & Gamble Company Cyproterone acetate thioacetate
US5439901A (en) * 1993-07-23 1995-08-08 The Procter & Gamble Company Cyproterone thiopivalate
WO1996008231A1 (fr) * 1994-09-14 1996-03-21 Central Sheffield University Hospitals Nhs Trust Controle de la croissance des cheveux
WO1999046279A3 (fr) * 1998-03-11 2001-02-22 Endorech Inc INHIBITEURS DE LA 17β-HYDROXYSTEROIDE DESHYDROGENASE DU TYPE 5 ET DU TYPE 3 ET METHODES D'UTILISATION ASSOCIEES
WO2005115402A1 (fr) * 2004-05-28 2005-12-08 Grünenthal GmbH Utilisation d'une association d'ethinylestradiol et d'acetate de chlormadinone pour produire un medicament
WO2008077542A1 (fr) * 2006-12-22 2008-07-03 Grünenthal GmbH 3-hydroxy-chlormadinonacétate pour le traitement topique de maladies cutanées androgéno-dépendantes
US8580771B2 (en) 2004-05-28 2013-11-12 Richter Gedeon Nyrt. Dosage form for hormonal contraception
US9278072B2 (en) 2004-05-28 2016-03-08 Richter Gedeon Nyrt. Hormonal contraceptive containing a combination of ethinyloestradiol and chlormadinone acetate

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2218086A1 (fr) * 1973-02-21 1974-09-13 Schering Ag
DE2840144A1 (de) * 1978-09-15 1980-03-27 Goedecke Ag Topisch applizierbares arzneimittel mit antiandrogener wirkung
EP0033164A2 (fr) * 1980-01-29 1981-08-05 von Kistowski, Irmgard, Dr. Composition pour empêcher et inhiber la calvitie
US4396615A (en) * 1981-06-24 1983-08-02 Duke University Method of treating androgen-related disorders

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2218086A1 (fr) * 1973-02-21 1974-09-13 Schering Ag
DE2840144A1 (de) * 1978-09-15 1980-03-27 Goedecke Ag Topisch applizierbares arzneimittel mit antiandrogener wirkung
EP0033164A2 (fr) * 1980-01-29 1981-08-05 von Kistowski, Irmgard, Dr. Composition pour empêcher et inhiber la calvitie
US4396615A (en) * 1981-06-24 1983-08-02 Duke University Method of treating androgen-related disorders

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0330583A3 (fr) * 1988-02-26 1991-03-13 L'oreal Méthode pour améliorer l'aspect esthétique de la peau à l'aide de mélanges polyvitaminiques et compositions cosmétiques pour sa mise en oeuvre
WO1991006284A1 (fr) * 1989-10-27 1991-05-16 Schering Aktiengesellschaft Berlin Und Bergkamen Preparations pharmaceutiques
GR900100772A (el) * 1989-10-27 1992-03-20 Berlin Und Bergkamen Schering Μέ?οδος για την παρασκευή φαρμακευτικών σκευασμάτων.
EP0566979A1 (fr) * 1992-04-23 1993-10-27 Ingeborg Zingraf Lotion capillaire et procédé de traitement pour réduire la chute des cheveux et favoriser leur pousse
WO1994006436A1 (fr) * 1992-09-12 1994-03-31 Lts Lohmann Therapie-Systeme Gmbh & Co. Kg Emplatre contenant du dexpanthenol pour application transcutanee d'hormones steroides
US5344651A (en) * 1993-07-23 1994-09-06 The Procter & Gamble Company Cyproterone acetate thioacetate
US5439901A (en) * 1993-07-23 1995-08-08 The Procter & Gamble Company Cyproterone thiopivalate
US6020327A (en) * 1994-09-14 2000-02-01 The Central Sheffield University Hospitals Nhs Trust Control of hair growth
WO1996008231A1 (fr) * 1994-09-14 1996-03-21 Central Sheffield University Hospitals Nhs Trust Controle de la croissance des cheveux
WO1999046279A3 (fr) * 1998-03-11 2001-02-22 Endorech Inc INHIBITEURS DE LA 17β-HYDROXYSTEROIDE DESHYDROGENASE DU TYPE 5 ET DU TYPE 3 ET METHODES D'UTILISATION ASSOCIEES
US6541463B1 (en) 1998-03-11 2003-04-01 Endorecherche, Inc. Inhibitors of type 5 and type 3 17β-hydroxysteroid dehydrogenase and methods for their use
WO2005115402A1 (fr) * 2004-05-28 2005-12-08 Grünenthal GmbH Utilisation d'une association d'ethinylestradiol et d'acetate de chlormadinone pour produire un medicament
US8580771B2 (en) 2004-05-28 2013-11-12 Richter Gedeon Nyrt. Dosage form for hormonal contraception
US9278072B2 (en) 2004-05-28 2016-03-08 Richter Gedeon Nyrt. Hormonal contraceptive containing a combination of ethinyloestradiol and chlormadinone acetate
WO2008077542A1 (fr) * 2006-12-22 2008-07-03 Grünenthal GmbH 3-hydroxy-chlormadinonacétate pour le traitement topique de maladies cutanées androgéno-dépendantes
US8465763B2 (en) 2006-12-22 2013-06-18 Richter Gedeon Nyrt. 3-hydroxychlormadinone acetate for the topical treatment of androgen-dependent skin diseases

Also Published As

Publication number Publication date
AU4805085A (en) 1986-03-24

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