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WO1995022332A1 - Procede et produit de substitution hormonale postmenopausique - Google Patents

Procede et produit de substitution hormonale postmenopausique Download PDF

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Publication number
WO1995022332A1
WO1995022332A1 PCT/EP1995/000498 EP9500498W WO9522332A1 WO 1995022332 A1 WO1995022332 A1 WO 1995022332A1 EP 9500498 W EP9500498 W EP 9500498W WO 9522332 A1 WO9522332 A1 WO 9522332A1
Authority
WO
WIPO (PCT)
Prior art keywords
daily
substitution
units
composition according
estrogen
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/EP1995/000498
Other languages
German (de)
English (en)
Inventor
Rolf-Dieter Hesch
Marika Ehrlich
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.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to AU17070/95A priority Critical patent/AU1707095A/en
Publication of WO1995022332A1 publication Critical patent/WO1995022332A1/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
    • 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
    • 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

Definitions

  • the invention relates to an agent for postmenopausal hormone substitution, with a number spatially separated and individually removable in a packaging unit, for oral administration without a free interval of certain substitution daily units, each as a first hormone component, a progestogen in constant dosage and as a second Hormone component contain a natural estrogen, and a method for postmenopausal hormone treatment, in which a number of daily substitution units, each containing progestogen as a first hormone component and estrogen as a second hormone component, are administered consecutively for long-term treatment without a free interval.
  • estrogen hormones which are combined with progestogen hormones in the second half of the cycle in order to produce a stopping bleeding and thus to counteract the proliferative and potentially carcinogenic effect of an estrogen medication alone.
  • progestogen hormones in women without a womb, estrogen can be applied alone.
  • the combined sequential substitution by means of estrogen and progestogen thus protects the woman from endo etriu carcinoma.
  • a disadvantage of the combined sequential administration of estrogen / progestogen described above is that tied monthly withdrawal bleeding in the form of a menstrual bleeding. Many postmenopausal women perceive this as such a nuisance that they want to forego hormone replacement despite the health benefits.
  • the invention is therefore based on the object of further developing the generic agent and the generic method in such a way that undesired intermediate bleeding is avoided.
  • this object is achieved in a further development of the agent in that the estrogen content of the daily substitution units increases from the first daily substitution unit to be taken to the last daily substitution unit to be taken. It can be provided that the estrogen content of the daily substitution units changes essentially continuously.
  • the invention also proposes that the estrogen content of the daily substitution units change essentially linearly.
  • the estrogen content is different from two successive daily substitution units.
  • the invention also proposes that at least two consecutive daily substitution units have the same estrogen content and the two adjoining daily substitution units have a different but different estrogen content from the two preceding daily substitution units.
  • the invention also proposes that three successive groups are provided, each with an essentially constant estrogen content per daily substitution unit.
  • the invention also proposes that 84 daily substitution units be provided. It can be provided that the gestagen content of the daily substitution units corresponds to 0.25 to 1.5 mg NETA.
  • the invention also proposes that the gestagen content of the daily substitution units corresponds in each case to approximately 5 mg of NETA.
  • gestagen content of the daily substitution units corresponds in each case to approximately 2.5 mg MPA.
  • the invention also proposes that the estrogen content of the lowest-dose daily substitution unit corresponds to 0.25 to 1.0 mg of estradiol and that of the highest-dose daily substitution units corresponds to up to 4 mg of estradiol.
  • the estrogen content of the lowest daily substitution unit corresponds to approximately 0.5 mg estradiol and that of the highest daily substitution unit corresponds to approximately 2.5 mg estradiol.
  • the invention provides that at least one of the daily substitution units contains at least one component from the progesterone, chloromadinone acetate, norethisterone acetate, cyproterone acetate, desogestrel, levonorgestrel, other natural and / or synthetic gestagens and at least one of the aforementioned hormone components after taking hormone compounds which rapidly release having.
  • At least one of the daily substitution units at least one component from the estradiol, estrone, conjugated estrogens and / or other natural estrogens and at least one of the aforementioned hormone components rapidly cleaving after ingestion Group containing hormone compounds.
  • the method according to the invention is characterized in that, before the start of the long-term treatment with the daily substitution units, a number of daily substitution units with a low dose of the first daily substitution unit to a higher final dose of last substitution daily unit increasing estrogen content, whereupon the final permanent treatment with daily substitution units with constant progestogen and estrogen content follows.
  • the duration of the treatment with daily substitution units with increasing estrogen content extends over a period of 1 to 4 months.
  • the invention is based on the surprising finding that it is possible to significantly increase acceptance in postmenopausal hormone substitution by means of progestogen / estrogen combination preparations by largely suppressing unwanted bleeding by not immediately starting the administration of the daily dose of estrogen intended for long-term therapy , but a pre-therapy takes place, in which insignificant small amounts of estrogen are initially administered per day, before then after a period of preferably three months, the final daily estrogen dose z. B. 3 months the final daily estrogen dose for long-term treatment is achieved.
  • the risk of undesirable bleeding can be significantly reduced, particularly in the case of older women, in whom hormone substitution only begins at a long distance after the start of postmenopause. You can increase the daily estrogen dose Carry out both continuously and discontinuously, i.e. gradually.
  • the invention is particularly suitable for use following progestogen therapy, as is the subject of German patent application P 44 05 590.0 (attorney file EM1294) of the same date.

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

Abstract

Un produit de substitution hormonale postménopausique comprend un nombre d'unités quotidiennes de substitution séparées dans l'espace et prélevables individuellement d'une unité d'emballage, destinées à être oralement administrées sans périodes d'arrêt de prise. Ces unités quotidiennes contiennent comme premier composant hormonal un gestagène à dose constante et comme deuxième composant hormonal un ÷strogène naturel. Ce produit se caractérise en ce que la teneur en ÷strogène des unités quotidiennes de substitution augmente de l'unité quotidienne de substitution à administrer en premier à l'unité quotidienne de substitution à administrer en dernier. L'invention concerne également un procédé de substitution hormonale postménopausique impliquant l'utilisation du produit décrit.
PCT/EP1995/000498 1994-02-22 1995-02-10 Procede et produit de substitution hormonale postmenopausique Ceased WO1995022332A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU17070/95A AU1707095A (en) 1994-02-22 1995-02-10 Postmenopausal hormone substitution product and process

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP4405591.9 1994-02-22
DE19944405591 DE4405591C1 (de) 1994-02-22 1994-02-22 Mittel zur postmenopausalen Hormonsubstitution

Publications (1)

Publication Number Publication Date
WO1995022332A1 true WO1995022332A1 (fr) 1995-08-24

Family

ID=6510837

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1995/000498 Ceased WO1995022332A1 (fr) 1994-02-22 1995-02-10 Procede et produit de substitution hormonale postmenopausique

Country Status (3)

Country Link
AU (1) AU1707095A (fr)
DE (1) DE4405591C1 (fr)
WO (1) WO1995022332A1 (fr)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001026640A3 (fr) * 1999-10-15 2001-10-18 Orion Corp Traitement de l'osteoporose
US6846496B1 (en) 1999-10-15 2005-01-25 Orion Corporation Treatment of osteoporosis
US7871994B2 (en) 2001-01-11 2011-01-18 Bayer Schering Pharma Ag Hormone replacement therapy method and its administration form

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19739916C2 (de) * 1997-09-11 2001-09-13 Hesch Rolf Dieter Verwendung einer Kombination aus einem Gestagen und einem Estrogen zur kontinuierlichen Ovulationshemmung und ggf. gleichzeitigen Behandlung und/oder Prophylaxe von Tumoren der Brustdrüsen

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4962098A (en) * 1987-06-15 1990-10-09 Warner-Lambert Company Graduated estrogen contraceptive

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0559240B1 (fr) * 1987-09-24 2001-12-05 Jencap Research Limited Packages contraceptives contenant de l'estrogen et du progestin
DE4104385C1 (fr) * 1991-02-09 1992-08-13 Marika Dr.Med. 6509 Framersheim De Ehrlich

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4962098A (en) * 1987-06-15 1990-10-09 Warner-Lambert Company Graduated estrogen contraceptive

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001026640A3 (fr) * 1999-10-15 2001-10-18 Orion Corp Traitement de l'osteoporose
US6846496B1 (en) 1999-10-15 2005-01-25 Orion Corporation Treatment of osteoporosis
US7871994B2 (en) 2001-01-11 2011-01-18 Bayer Schering Pharma Ag Hormone replacement therapy method and its administration form

Also Published As

Publication number Publication date
AU1707095A (en) 1995-09-04
DE4405591C1 (de) 1995-07-20

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