KR101019361B1 - 피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합 - Google Patents

피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합 Download PDF

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KR101019361B1
KR101019361B1 KR1020077013070A KR20077013070A KR101019361B1 KR 101019361 B1 KR101019361 B1 KR 101019361B1 KR 1020077013070 A KR1020077013070 A KR 1020077013070A KR 20077013070 A KR20077013070 A KR 20077013070A KR 101019361 B1 KR101019361 B1 KR 101019361B1
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ethynylestradiol
drospirenone
amount
daily dosage
range
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KR20070067248A (ko
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볼프강 하일
유르겐 힐만
랄프 리프
레나테 하이테커
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바이엘 쉐링 파마 악티엔게젤샤프트
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    • 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
    • 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
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • A61K31/585Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin containing lactone rings, e.g. oxandrolone, bufalin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P5/28Antiandrogens
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5084Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
KR1020077013070A 1999-08-31 2000-08-31 피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합 Expired - Lifetime KR101019361B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US38627499A 1999-08-31 1999-08-31
EP99202826 1999-08-31
EP99202826.6 1999-08-31
US09/386,274 1999-08-31

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
KR1020027002795A Division KR100857344B1 (ko) 1999-08-31 2000-08-31 피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합

Publications (2)

Publication Number Publication Date
KR20070067248A KR20070067248A (ko) 2007-06-27
KR101019361B1 true KR101019361B1 (ko) 2011-03-07

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KR1020077013070A Expired - Lifetime KR101019361B1 (ko) 1999-08-31 2000-08-31 피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합
KR1020027002795A Expired - Lifetime KR100857344B1 (ko) 1999-08-31 2000-08-31 피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합

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KR1020027002795A Expired - Lifetime KR100857344B1 (ko) 1999-08-31 2000-08-31 피임약으로서의 사용을 위한 에티닐에스트라디올과드로스피렌온의 약학적 조합

Country Status (26)

Country Link
EP (4) EP2044941A1 (https=)
JP (2) JP4354667B2 (https=)
KR (2) KR101019361B1 (https=)
AT (3) ATE254464T1 (https=)
AU (4) AU780330B2 (https=)
BG (1) BG66114B1 (https=)
BR (1) BR0014159A (https=)
CY (3) CY1108990T1 (https=)
CZ (1) CZ300514B6 (https=)
DE (5) DE60042089D1 (https=)
DK (3) DK1214076T3 (https=)
EE (1) EE05128B1 (https=)
ES (3) ES2211580T3 (https=)
HK (1) HK1047247B (https=)
HR (1) HRP20070188B1 (https=)
HU (1) HU227207B1 (https=)
IL (1) IL148339A0 (https=)
ME (2) MEP36008A (https=)
NO (1) NO326860B1 (https=)
NZ (1) NZ517845A (https=)
PL (1) PL199028B1 (https=)
PT (3) PT1214076E (https=)
RS (3) RS50262B (https=)
SI (3) SI1214076T1 (https=)
TW (1) TWI276436B (https=)
WO (1) WO2001015701A1 (https=)

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DE102008037025C5 (de) 2008-08-08 2016-07-07 Jesalis Pharma Gmbh Verfahren zur Herstellung kristalliner Wirkstoff-Mikropartikel bzw. einer Wirkstoffpartikel-Festkörperform
EP2398461A1 (en) 2009-02-18 2011-12-28 Bayer Pharma Aktiengesellschaft Formulation comprising drospirenone for subcutaneous or intramuscular administration
UY32836A (es) 2009-08-12 2011-03-31 Bayer Schering Pharma Ag Partículas estabilizadas que comprenden 5-metil-(6s)-tetrahidrofolato
US20130137664A1 (en) * 2010-04-15 2013-05-30 Bayer Intellectual Property Gmbh Low-dosed solid oral dosage forms for hrt
AR081670A1 (es) 2010-06-29 2012-10-10 Leon Farma Sa Lab Composicion farmaceutica que comprende drospirenona y kit anticonceptivo
US10849857B2 (en) 2010-07-28 2020-12-01 Laboratorios Leon Farma Sa Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same
US11351122B1 (en) 2010-07-28 2022-06-07 Laboratorios Leon Farma Sa Synthetic progestogens and pharmaceutical compositions comprising the same
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Patent Citations (1)

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WO1998004269A1 (en) * 1996-07-26 1998-02-05 American Home Products Corporation Monophasic contraceptive method and kit comprising a combination of a progestin and estrogen

Non-Patent Citations (1)

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Title
Contraception, Vol.54, pp.59-69(1996)*

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HK1047247A1 (en) 2003-02-14
PT1598069E (pt) 2009-07-20
HK1082432A1 (en) 2006-06-09
TWI276436B (en) 2007-03-21
CY1108990T1 (el) 2014-02-12
JP4354667B2 (ja) 2009-10-28
HU227207B1 (en) 2010-11-29
DE60006692D1 (de) 2003-12-24
SI1214076T1 (en) 2004-06-30
NO20020801D0 (no) 2002-02-19
EP1380301B1 (en) 2009-01-14
PL354406A1 (pl) 2004-01-12
CZ2002615A3 (cs) 2002-08-14
DE60006692T2 (de) 2004-09-23
ES2211580T3 (es) 2004-07-16
DE60042089D1 (de) 2009-06-04
EP1598069A3 (en) 2006-04-05
ES2319750T3 (es) 2009-05-12
DE122009000007I1 (de) 2009-05-07
HUP0202500A2 (en) 2002-10-28
BR0014159A (pt) 2002-05-07
EE05128B1 (et) 2009-02-16
ATE254464T1 (de) 2003-12-15
EP1598069A2 (en) 2005-11-23
AU2005202046B9 (en) 2008-12-11
KR20020040798A (ko) 2002-05-30
HRP20070188B1 (hr) 2015-06-19
CY2009015I1 (el) 2014-02-12
NO326860B1 (no) 2009-03-02
EP1214076A1 (en) 2002-06-19
EP1598069B1 (en) 2009-04-22
DK1214076T3 (da) 2004-02-23
JP2009143959A (ja) 2009-07-02
BG66114B1 (bg) 2011-05-31
JP2003508441A (ja) 2003-03-04
HK1061968A1 (en) 2004-10-15
DK1598069T3 (da) 2009-07-06
SI1380301T1 (sl) 2009-06-30
CY2009015I2 (el) 2014-02-12
SI1598069T1 (sl) 2009-10-31
EP2044941A1 (en) 2009-04-08
HUP0202500A3 (en) 2004-04-28
AU780330B2 (en) 2005-03-17
AU2005202046A1 (en) 2005-06-09
PL199028B1 (pl) 2008-08-29
DE122009000006I2 (de) 2012-03-22
CZ300514B6 (cs) 2009-06-03
NZ517845A (en) 2004-12-24
EP1380301A1 (en) 2004-01-14
AU6589500A (en) 2001-03-26
DE122009000007I2 (de) 2011-07-21
RS50262B (sr) 2009-07-15
MEP36008A (hr) 2011-02-10
EE200200110A (et) 2003-06-16
ME00329B (me) 2011-05-10
HK1047247B (en) 2004-07-23
IL148339A0 (en) 2002-09-12
AU2005202046B2 (en) 2008-11-20
DK1380301T3 (da) 2009-04-20
ATE420648T1 (de) 2009-01-15
CY1109252T1 (el) 2014-07-02
ES2325589T3 (es) 2009-09-09
AU2010226924A1 (en) 2010-10-28
NO20020801L (no) 2002-04-26
WO2001015701A1 (en) 2001-03-08
HRP20070188A2 (en) 2007-07-31
DE60041421D1 (de) 2009-03-05
KR100857344B1 (ko) 2008-09-05
ATE429231T1 (de) 2009-05-15
AU2009200247B2 (en) 2010-07-01
RS50262B2 (sr) 2018-10-31
AU2009200247A1 (en) 2009-02-19
RS20090134A (sr) 2009-11-10
PT1214076E (pt) 2004-04-30
YU14502A (sh) 2006-01-16
PT1380301E (pt) 2009-03-30
KR20070067248A (ko) 2007-06-27
DE122009000006I1 (de) 2009-05-07
EP1214076B1 (en) 2003-11-19

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