WO1996028165A1 - Einmonatsspritze als depot-kontrazeptivum und für die hormonersatztherapie für peri- und praemenopausale frauen - Google Patents

Einmonatsspritze als depot-kontrazeptivum und für die hormonersatztherapie für peri- und praemenopausale frauen 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)
French (fr)
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 PL96322202A priority Critical patent/PL322202A1/xx
Priority to AU51108/96A priority patent/AU713258B2/en
Priority to SK1239-97A priority patent/SK123997A3/sk
Priority to JP8527295A priority patent/JPH11501649A/ja
Priority to EP96907506A priority patent/EP0814811A1/de
Priority to MX9707009A priority patent/MX9707009A/es
Priority to CZ972896A priority patent/CZ289697A3/cs
Priority to NZ304027A priority patent/NZ304027A/xx
Publication of WO1996028165A1 publication Critical patent/WO1996028165A1/de
Priority to NO974255A priority patent/NO974255L/no

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
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/30—Oestrogens

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.
PCT/EP1996/001201 1995-03-16 1996-03-15 Einmonatsspritze als depot-kontrazeptivum und für die hormonersatztherapie für peri- und praemenopausale frauen WO1996028165A1 (de)

Priority Applications (9)

Application Number Priority Date Filing Date Title
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
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
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
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
EP96907506A EP0814811A1 (de) 1995-03-16 1996-03-15 Einmonatsspritze als depot-kontrazeptivum und für die hormonersatztherapie für peri- und praemenopausale frauen
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.
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
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
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
DE19510861.2 1995-03-16
DE19510861A DE19510861A1 (de) 1995-03-16 1995-03-16 Einmonatsspritze als Depot-Kontrazeptivum und für die Hormonersatztherapie für peri- und praemenopausale Frauen

Publications (1)

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

Family

ID=7757668

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1996/001201 WO1996028165A1 (de) 1995-03-16 1996-03-15 Einmonatsspritze als depot-kontrazeptivum und für die hormonersatztherapie für peri- und praemenopausale frauen

Country Status (17)

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

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 (en) * 1983-08-05 1985-04-03 Pre Jay Holdings Ltd. A method of hormonal treatment of peri-menopausal, menopausal and post-menopausal disorders and multi-preparation pack therefor

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0136011A2 (en) * 1983-08-05 1985-04-03 Pre Jay Holdings Ltd. A method of hormonal treatment of peri-menopausal, menopausal and post-menopausal disorders and multi-preparation pack therefor

Also Published As

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

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