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WO1996028165A1 - Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause - Google Patents

Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause Download PDF

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Publication number
WO1996028165A1
WO1996028165A1 PCT/EP1996/001201 EP9601201W WO9628165A1 WO 1996028165 A1 WO1996028165 A1 WO 1996028165A1 EP 9601201 W EP9601201 W EP 9601201W WO 9628165 A1 WO9628165 A1 WO 9628165A1
Authority
WO
WIPO (PCT)
Prior art keywords
month
estradiol
replacement therapy
injectable
once
Prior art date
Application number
PCT/EP1996/001201
Other languages
German (de)
English (en)
Inventor
Ursula Lachnit-Fixson
Semiramis Aydinlik
Original Assignee
Schering Aktiengesellschaft
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 Schering Aktiengesellschaft filed Critical Schering Aktiengesellschaft
Priority to JP8527295A priority Critical patent/JPH11501649A/ja
Priority to PL96322202A priority patent/PL322202A1/xx
Priority to SK1239-97A priority patent/SK123997A3/sk
Priority to NZ304027A priority patent/NZ304027A/xx
Priority to CZ972896A priority patent/CZ289697A3/cs
Priority to AU51108/96A priority patent/AU713258B2/en
Priority to EP96907506A priority patent/EP0814811A1/fr
Priority to MX9707009A priority patent/MX9707009A/es
Publication of WO1996028165A1 publication Critical patent/WO1996028165A1/fr
Priority to NO974255A priority patent/NO974255L/no

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30Oestrogens

Definitions

  • the present invention relates to the use of a one-month injection (once-a-month injectable composition) containing an estrogenic and gestagenic component as active ingredients for the manufacture of a medicament for contraception and simultaneous hormone replacement therapy for peri- and premenopausal women.
  • a monthly injection in the sense of the present invention means a hormone preparation which is injected once a month for women of childbearing age for contraception.
  • This hormone preparation contains a gestagenic and an estrogenic component as active substances, each with a long enough effect to achieve a contraceptive effect for a period of one month.
  • progestogen-only injectables are also available, which ensure long-term contraceptive protection, albeit with poor cycle control.
  • US Pat. No. 4,826,831 already discloses a method for the hormonal treatment of menopausal, including perimenopausal and postmenopausal disorders (disorders), which relates in particular to treatment using a progestogen in conjunction with an estrogen.
  • the estrogen can also be continuous or cyclical, i.e. H. with breaks.
  • estrogens and progestogens are mentioned which are suitable for the purposes of this invention, including norethisterone acetate and medroxyprogesterone acetate as progestogens and estradiol valerate.
  • norethisterone acetate and medroxyprogesterone acetate as progestogens and estradiol valerate.
  • it should be possible to use all estrogens and progestogens that are also in oral contraceptives are conceivable. Adequate contraceptive protection is provided by the described
  • Norethisterone acetate / estradiol valerate is also disclosed as a possible combination.
  • progestogen and estrogen used are low: progestogen in a daily amount equivalent to 0.025 mg to 0.075 mg levonorgestrel and estrogen in a daily amount corresponding to 0.5 to 2.0 mg estradiol .
  • the amount to be administered daily is the amount to be administered daily.
  • estradiol valerate 20 mg to 100 mg estradiol valerate are given.
  • Gestagen depot formulation for 3 months should be 50 to 500 mg medroxyprogesterone acetate or 20 to
  • This patent also relates to pharmaceutical compositions for performing them
  • Premenopause begins, onset of ailments, such as hot flushes, dryness of the
  • US Pat. No. 4,826,831 expressly states that oral administration is not a method of contraception.
  • peri- and premenopause should have their conventional meaning as described in "The Controversial Cli acteric", P.A. van Keep et al., Ed., MTP Press (1981) on page 9 can be understood.
  • a one-month injection in the sense of the present invention should be understood to mean both the products already mentioned at the beginning and all other possible combinations of a natural estrogen with a progestogen.
  • the two active components must be present in a depot formulation, the depot effect being achieved either through the special type of pharmaceutical formulation (for example microcrystalline suspension) or rather through the chemical structure of the progestogen and / or estrogen (for example through the esterification of free hydroxyl groups).
  • the main estrogens here are 17 ⁇ -estradiol, estradiol-3-benzoate, estradiol-17-valerate, cypionate, undecylate, enanthate and or other estradiol esters (US Pat. No. 2,611,773, US Pat
  • the gestagen component is preferably selected from the group of compounds
  • Norethisterone acetate, norethisterone acetate, medroxyprogesterone acetate and cyproterone acetate Norethisterone acetate, norethisterone acetate, medroxyprogesterone acetate and cyproterone acetate.
  • Tables LA and 2A list selected estrogens or gestagens to be used according to the present invention, with an indication of the preferred amount range.
  • Tables 1B and 2B show the particularly preferred amounts of the respective estrogen or progestogen which are to be contained in a one-month syringe according to the present invention.
  • the combination of medroxyprogesterone acetate and estradiol cypionate is preferred for producing a one-month syringe for peri- and premenopausal contraception; the combination of norethisterone enanthate / estradiol valerate is particularly preferred.
  • the particularly preferred embodiment based on the progestogen / estrogen combination norethisterone enanthate / estradiol valerate not only offers a prophylactic effect with regard to osteoporosis, but in addition to the bone depletion-inhibiting effect of estrogen, a bone building effect caused by the norethis-terone enanthate is observed in this combination.

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne l'utilisation d'une injection mensuelle qui contient des composants ÷strogènes et gestagènes comme principes actifs pour préparer un médicament contraceptif utile en même temps en hormonothérapie substitutive pour femmes dans la périménopause et dans la préménopause. On obtient avec ce médicament un effet contraceptif fiable avec un ÷strogène 'naturel' (sans éthinyl÷stradiol), ainsi qu'une thérapie efficace des premiers symptômes d'insuffisance d'÷strogène, ainsi qu'une prophylaxie de l'ostéoporose.
PCT/EP1996/001201 1995-03-16 1996-03-15 Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause WO1996028165A1 (fr)

Priority Applications (9)

Application Number Priority Date Filing Date Title
JP8527295A JPH11501649A (ja) 1995-03-16 1996-03-15 閉経周辺期及び閉経前期にある女性に対する徐放性避妊薬としての及びホルモン補充療法に使用する1月用注射薬
PL96322202A PL322202A1 (en) 1995-03-16 1996-03-15 Monthly injections as a contraceptive measure for and in substitute hormonal therapy of pre- and in-menopausal female patients
SK1239-97A SK123997A3 (en) 1995-03-16 1996-03-15 Once-a-month-injectable useful as depot contraceptive and in hormone replacement therapy for perimenopausal and premenopausal women
NZ304027A NZ304027A (en) 1995-03-16 1996-03-15 Once a month injectable contraceptive comprising an estrogenic and gestagenic component for contraception and simultaneous hormone replacement therapy
CZ972896A CZ289697A3 (en) 1995-03-16 1996-03-15 Injection administered once a month as a depot contraception and for hormonal substitution therapy for women in perimenstrual and premenstrual pause
AU51108/96A AU713258B2 (en) 1995-03-16 1996-03-15 Once-a-month-injection as a depot contraceptive and for hormone replacement therapy for perimenopausal and premenopausal women
EP96907506A EP0814811A1 (fr) 1995-03-16 1996-03-15 Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause
MX9707009A MX9707009A (es) 1995-03-16 1996-03-15 Inyeccion de una vez al mes como un contraceptivo de base y para terapia de reemplazamiento hormonal para mujeres perimenopausicas y premenopausicas.
NO974255A NO974255L (no) 1995-03-16 1997-09-15 Preparat for injeksjon én gang pr. måned og som er anvendbart som depot-befruktningshemmende middel og i hormon-erstatningsterapi for perimenopausale og premenopausale kvinner

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19510861A DE19510861A1 (de) 1995-03-16 1995-03-16 Einmonatsspritze als Depot-Kontrazeptivum und für die Hormonersatztherapie für peri- und praemenopausale Frauen
DE19510861.2 1995-03-16

Publications (1)

Publication Number Publication Date
WO1996028165A1 true WO1996028165A1 (fr) 1996-09-19

Family

ID=7757668

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/001201 WO1996028165A1 (fr) 1995-03-16 1996-03-15 Injection mensuelle utile comme contraceptif retard et comme hormonotherapie substitutive pour femmes dans la perimenopause et dans la premenopause

Country Status (17)

Country Link
EP (1) EP0814811A1 (fr)
JP (1) JPH11501649A (fr)
KR (1) KR19980703058A (fr)
AR (1) AR002283A1 (fr)
AU (1) AU713258B2 (fr)
CA (1) CA2215382A1 (fr)
CZ (1) CZ289697A3 (fr)
DE (1) DE19510861A1 (fr)
HU (1) HUP9801691A3 (fr)
IL (1) IL117516A (fr)
MX (1) MX9707009A (fr)
NO (1) NO974255L (fr)
NZ (1) NZ304027A (fr)
PL (1) PL322202A1 (fr)
SK (1) SK123997A3 (fr)
WO (1) WO1996028165A1 (fr)
ZA (1) ZA962177B (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0000313D0 (en) 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0136011A2 (fr) * 1983-08-05 1985-04-03 Pre Jay Holdings Ltd. Méthode de traitement hormonal de troubles de la périménopause, ménopause et postménopause et emballage à préparations multiples dans ce but

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0136011A2 (fr) * 1983-08-05 1985-04-03 Pre Jay Holdings Ltd. Méthode de traitement hormonal de troubles de la périménopause, ménopause et postménopause et emballage à préparations multiples dans ce but

Also Published As

Publication number Publication date
DE19510861A1 (de) 1996-09-19
NO974255D0 (no) 1997-09-15
CA2215382A1 (fr) 1996-09-19
AR002283A1 (es) 1998-03-11
HUP9801691A3 (en) 1999-03-01
NO974255L (no) 1997-11-14
NZ304027A (en) 2000-05-26
MX9707009A (es) 1997-11-29
SK123997A3 (en) 1998-02-04
IL117516A0 (en) 1996-07-23
AU713258B2 (en) 1999-11-25
IL117516A (en) 2000-07-26
CZ289697A3 (en) 1997-12-17
PL322202A1 (en) 1998-01-19
AU5110896A (en) 1996-10-02
HUP9801691A2 (hu) 1998-11-30
ZA962177B (en) 1996-07-29
KR19980703058A (ko) 1998-09-05
JPH11501649A (ja) 1999-02-09
EP0814811A1 (fr) 1998-01-07

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