EP1248627A2 - Orale anwendung von dehydroepiandrosterone, ihre vorläufer und derivate als feuchthaltemittel mit direkter wirkung - Google Patents

Orale anwendung von dehydroepiandrosterone, ihre vorläufer und derivate als feuchthaltemittel mit direkter wirkung

Info

Publication number
EP1248627A2
EP1248627A2 EP01907605A EP01907605A EP1248627A2 EP 1248627 A2 EP1248627 A2 EP 1248627A2 EP 01907605 A EP01907605 A EP 01907605A EP 01907605 A EP01907605 A EP 01907605A EP 1248627 A2 EP1248627 A2 EP 1248627A2
Authority
EP
European Patent Office
Prior art keywords
use according
group
precursors
derivatives
composition
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Withdrawn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
EP01907605A
Other languages
English (en)
French (fr)
Inventor
Olivier De La Charriere
Stéphanie Nouveau
Françoise FORETTE
Etienne-Emile Baulieu
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.)
Assistance Publique Hopitaux de Paris APHP
Original Assignee
Assistance Publique Hopitaux de Paris APHP
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 Assistance Publique Hopitaux de Paris APHP filed Critical Assistance Publique Hopitaux de Paris APHP
Publication of EP1248627A2 publication Critical patent/EP1248627A2/de
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/5685—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone having an oxo group in position 17, e.g. androsterone
    • 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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/16—Emollients or protectives, e.g. against radiation
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
    • A61K2800/92—Oral administration
    • 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
    • A61Q19/007—Preparations for dry skin

Definitions

  • the present invention relates to the use of dehydroepiandrosterone, its precursors and its derivatives, for the manufacture of a composition suitable for oral administration and intended to be used for directly increasing the water content of the skin.
  • DHEA Dehydroepiandrosterone
  • DHEA at least one of its chemical precursors, of its chemical derivatives, of its biological precursors, or its metabolic derivatives, administered orally, are capable of acting directly on the water content of the skin, and this independently of their action on seborrhea.
  • a subject of the present invention is therefore the use of at least one compound chosen from the group consisting of dehydroepiandrosterone, its chemical precursors, its chemical derivatives, its biological precursors and its metabolic derivatives, for the preparation of a composition suitable for oral administration and intended to be used to directly increase the water content of the skin.
  • the biological precursor is chosen from the group comprising cholesterol, pregnenolone, 17 ⁇ -hydroxy pregnenolone, 5-androstenediol, dehydroepiandrosterone sulfate, sulfate of 17 ⁇ -hydroxy pregnenolone and 5-androstenediol sulfate.
  • the chemical precursor is chosen from the group comprising sapogenins, such as for example diosgenin (or spirost-5-en-3- ⁇ -ol) and the natural extracts containing them , especially fenugreek and extracts from Dioscorea such as Wild Yam (or wild yam root).
  • the metabolic derivative is chosen from the group comprising:
  • the chemical derivative is chosen from the group comprising the salts of DHEA, in particular the water-soluble salts of DHEA, such as for example DHEA sulphate and DHEA esters , including DHEA salicylate.
  • the composition may be a cosmetic composition or a dermatological composition, being in all the galenical forms normally used for oral administration, in particular in the form of breakable tablets or not, of granules, of capsules , capsules, solutes, suspensions or solutions, and comprising at least one compound chosen from the group consisting of dehydroepiandrosterone, its precursors and its derivatives as active principle, in association with any suitable excipient.
  • the compounds are present in the composition in an amount allowing their administration at a dose between 1 and 100 mg per day, preferably between 25 and 75 mg per day, said dosage being carried out in one or more doses, for example with a unit dose of 50 mg.
  • the DHEA which can be used according to the invention is for example available from the company SIGMA or from the company AKZO NOBEL.
  • the evaluation was carried out in a randomized double-blind clinical study in 280 subjects (140 men and 140 women).
  • the inclusion criteria were as follows: healthy volunteers, of both sexes, free from any serious pathology and aged 60 to 80 years.
  • the treatment consisted, for 12 months, in a daily intake in the morning, of DHEA at the dose of 50 mg, in the form of a scored tablet, for half of the subjects, or a placebo for the other half of the topics.
  • the hydration of the skin on the ventral forearm is measured blind at the start of treatment (T0) and at the end of treatment (T12), by the same clinician, using a Dermodiag®, device described in patent US5, 001,436.
  • the device features are as follows: output impedance: 1.4 kOhms and working frequency 10 MHz. The method used is that described by Lévêque J.L., Soc. Cosmet. Chem. (1983), 34, 419-428.
  • This device makes it possible to evaluate the state of hydration (water content of the surface layers of the epidermis) by measuring the electrical conductance.
  • Conductance is measured using an electrode applied to the skin for 10 seconds.
  • the conductance value is the result of the average of 6 individual measurements per measurement time.
  • the sebum production is measured at the start of the treatment (T0) and at the end of the treatment (T12) according to the techniques described by Kligman AM et al, J. Soc. Cosmet. Chem. (1986), 37, 369-373 and by Nordstrom KM et al, J. Invest. Dermatol (1986), 87, 260-264.
  • White adhesive microporous patches (Sebutape®, Cuderm Corporation Dallas, Texas USA,) described in US Pat. No. 4,532,937 are used; the patches are applied in a standardized way to the skin, previously degreased with 10 cotton swabs soaked in alcohol at 70 ° C.
  • the lipids which are passively absorbed on the stamps are visualized by the presence of transparent spots, themselves measured by image analysis.
  • Each spot represents an active sebaceous gland.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Birds (AREA)
  • Toxicology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Cosmetics (AREA)
  • Medicines Containing Plant Substances (AREA)
EP01907605A 2000-01-17 2001-01-17 Orale anwendung von dehydroepiandrosterone, ihre vorläufer und derivate als feuchthaltemittel mit direkter wirkung Withdrawn EP1248627A2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR0000551 2000-01-17
FR0000551A FR2803751B1 (fr) 2000-01-17 2000-01-17 Utilisation par voie orale de la dehydroepiandrosterone,de ses precurseurs et de ses derives comme agents hydratants a action directe
PCT/FR2001/000138 WO2001052856A2 (fr) 2000-01-17 2001-01-17 Utilisation par voie orale de la dehydroepiandrosterone, de ses precurseurs et de ses derives comme agents hydratants a action directe

Publications (1)

Publication Number Publication Date
EP1248627A2 true EP1248627A2 (de) 2002-10-16

Family

ID=8845991

Family Applications (1)

Application Number Title Priority Date Filing Date
EP01907605A Withdrawn EP1248627A2 (de) 2000-01-17 2001-01-17 Orale anwendung von dehydroepiandrosterone, ihre vorläufer und derivate als feuchthaltemittel mit direkter wirkung

Country Status (6)

Country Link
US (1) US20030050293A1 (de)
EP (1) EP1248627A2 (de)
JP (1) JP2003520238A (de)
AU (1) AU2001235528A1 (de)
FR (1) FR2803751B1 (de)
WO (1) WO2001052856A2 (de)

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3326901A (en) * 1965-04-16 1967-06-20 Irwin I Lubowe Pregnenolone salts of allantoin
US4542129A (en) * 1982-08-16 1985-09-17 Norman Orentreich DHEA Formulations and methods for treating dry skin
US4496556A (en) * 1982-08-16 1985-01-29 Norman Orentreich Topical applications for preventing dry skin
EP0319638A1 (de) * 1987-12-08 1989-06-14 Estee Lauder Inc. Liposome enthaltende Kosmetika und Arzneimittel sowie Verfahren zur Anwendung solcher Mittel
US5215759A (en) * 1991-10-01 1993-06-01 Chanel, Inc. Cosmetic composition
US6093706A (en) * 1992-03-04 2000-07-25 Bioresponse, L.L.C. Combined dehydroepiandrosterone and retinoid therapy for epithelial disorders
JPH07196467A (ja) * 1993-12-28 1995-08-01 Kanebo Ltd 表皮角質化促進剤
US5736537A (en) * 1995-09-12 1998-04-07 Estee Lauder, Inc. Dehydroep:androsterone sailcylate useful against skin atrophy
EP0908183A1 (de) * 1997-10-08 1999-04-14 Institute For Advanced Skin Research Inc. Dehydroepiandrosterone oder ihre Derivate zur Erhöhung des Hyaluronische Saüre-Gehalts der Haut
FR2803519B1 (fr) * 2000-01-12 2002-03-22 Assist Publ Hopitaux De Paris Utilisation par voie orale de la dehydroepiandrosterone, de ses precurseurs et de ses derives pour ameliorer l'aspect papyrace de la peau

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0152856A2 *

Also Published As

Publication number Publication date
FR2803751B1 (fr) 2004-03-12
AU2001235528A1 (en) 2001-07-31
JP2003520238A (ja) 2003-07-02
WO2001052856A2 (fr) 2001-07-26
US20030050293A1 (en) 2003-03-13
FR2803751A1 (fr) 2001-07-20
WO2001052856A3 (fr) 2002-06-06

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