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EA200601089A1 - TRANSDERMAL DELIVERY OF HORMONES WITHOUT THE NEED TO USE AGENTS, STRENGTHENING PENETRATION - Google Patents

TRANSDERMAL DELIVERY OF HORMONES WITHOUT THE NEED TO USE AGENTS, STRENGTHENING PENETRATION

Info

Publication number
EA200601089A1
EA200601089A1 EA200601089A EA200601089A EA200601089A1 EA 200601089 A1 EA200601089 A1 EA 200601089A1 EA 200601089 A EA200601089 A EA 200601089A EA 200601089 A EA200601089 A EA 200601089A EA 200601089 A1 EA200601089 A1 EA 200601089A1
Authority
EA
Eurasian Patent Office
Prior art keywords
patch
hormones
need
transdermal delivery
use agents
Prior art date
Application number
EA200601089A
Other languages
Russian (ru)
Other versions
EA011160B1 (en
Inventor
Штефан Брахт
Михаэль Диттген
Петра Хубер
Томас Ланггут
Дирк Шенк
Original Assignee
Шеринг Акциенгезельшафт
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34702342&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA200601089(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Шеринг Акциенгезельшафт filed Critical Шеринг Акциенгезельшафт
Publication of EA200601089A1 publication Critical patent/EA200601089A1/en
Publication of EA011160B1 publication Critical patent/EA011160B1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • 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
    • 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
    • A61K31/565—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
    • A61K31/567—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 position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
    • A61K9/7061—Polyacrylates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7076—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising ingredients of undetermined constitution or reaction products thereof, e.g. rosin or other plant resins
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Botany (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Reproductive Health (AREA)
  • Organic Chemistry (AREA)
  • Inorganic Chemistry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)

Abstract

Настоящее изобретение относится к пластырю, который включает слой, содержащий лекарственное средство, с низким содержанием гормонов, таких как гестоден, и необязательно эстроген (например, этинилэстрадиол). При использовании пластыря для женщины достигаются уровни концентрации гестодена в плазме крови по крайней мере 1,0 нг/мл при условиях устойчивого состояния, без необходимости введения в слой, содержащий лекарственное средство, агентов, способствующих всасыванию, или агентов, усиливающих проникновение. Удовлетворительные уровни гормонов в плазме крови также достигаются в течение периода по крайней мере 1 неделя, что делает пластырь приемлемым для применения при контрацепции у женщин при использовании пластыря один раз в неделю.The present invention relates to a patch, which includes a layer containing a drug, low in hormones, such as gestodene, and optionally estrogen (for example, ethinyl estradiol). When using a patch for a woman, plasma levels of gestodene are achieved at least 1.0 ng / ml under steady-state conditions, without the need for administration of absorption agents or penetration enhancing agents to the drug layer. Satisfactory plasma hormone levels are also achieved over a period of at least 1 week, which makes the patch suitable for contraception in women using the patch once a week.

EA200601089A 2003-12-12 2004-12-10 A composition for transdermal delivery of hormones without penetration enhancers and its use EA011160B1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US52871803P 2003-12-12 2003-12-12
EP03078881 2003-12-12
PCT/IB2004/052752 WO2005058287A2 (en) 2003-12-12 2004-12-10 Transdermal delivery system of hormones without penetration enhancers

Publications (2)

Publication Number Publication Date
EA200601089A1 true EA200601089A1 (en) 2006-12-29
EA011160B1 EA011160B1 (en) 2009-02-27

Family

ID=34702342

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200601089A EA011160B1 (en) 2003-12-12 2004-12-10 A composition for transdermal delivery of hormones without penetration enhancers and its use

Country Status (15)

Country Link
JP (1) JP4965263B2 (en)
KR (1) KR101168449B1 (en)
CN (1) CN1913878B (en)
AU (1) AU2004298930B2 (en)
BR (1) BRPI0417530B8 (en)
CA (1) CA2549916C (en)
CU (1) CU23868B1 (en)
EA (1) EA011160B1 (en)
EC (1) ECSP066694A (en)
IL (1) IL176112A (en)
MX (1) MXPA06006682A (en)
NO (1) NO341989B1 (en)
NZ (1) NZ548091A (en)
WO (1) WO2005058287A2 (en)
ZA (1) ZA200605713B (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MEP14008A (en) 2003-02-21 2010-06-10 Bayer Schering Pharma Ag Uv stable transdermal therapeutic plaster
US8962013B2 (en) 2005-05-02 2015-02-24 Bayer Intellectual Property Gmbh Multi-layered transdermal system with triazine UV absorber
DE102005050729A1 (en) * 2005-10-19 2007-04-26 Schering Ag Method of preventive on-demand hormonal contraception
FR2900048B1 (en) * 2006-04-21 2012-11-16 Oreal COMPOSITIONS COMPRISING A DIPHENYL-METHANE HYDROXYLATED DERIVATIVE
WO2012031999A2 (en) 2010-09-06 2012-03-15 Bayer Pharma Aktiengesellschaft Low-dose transdermal patches with high drug release
AU2015203180B2 (en) * 2010-09-06 2016-06-30 Bayer Intellectual Property Gmbh Transdermal therapeutic systems with crystallization-inhibiting protective film (release liner)
DE102010040299A1 (en) * 2010-09-06 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Transdermal therapeutic systems with crystallization-inhibiting protective film (release liner)
CA2861324A1 (en) * 2012-01-27 2013-08-01 Agile Therapeutics, Inc. Transdermal hormone delivery
AU2016264137B2 (en) * 2015-05-18 2021-08-19 Agile Therapeutics, Inc. Contraceptive compositions and methods for improved efficacy and modulation of side effects

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1990004397A1 (en) * 1988-10-27 1990-05-03 Schering Aktiengesellschaft Berlin Und Bergkamen Preparation for transdermal application containing gestodene
AU657502B2 (en) * 1990-10-29 1995-03-16 Alza Corporation Transdermal contraceptive formulations, methods and devices
US5512292A (en) * 1990-10-29 1996-04-30 Alza Corporation Transdermal contraceptive formulations methods and devices
DE4329242A1 (en) * 1993-08-26 1995-03-02 Schering Ag Agent for transdermal application containing gestodenester
DE4405898A1 (en) * 1994-02-18 1995-08-24 Schering Ag Transdermal therapeutic systems containing sex steroids
US5820878A (en) * 1994-11-18 1998-10-13 Hisamitsu Pharmaceutical Co., Inc. Percutaneously absorbable patch
WO1996040355A1 (en) * 1995-06-07 1996-12-19 Cygnus, Inc. Transdermal patch and method for administering 17-deacetyl norgestimate alone or in combination with an estrogen
JP4346696B2 (en) * 1996-05-28 2009-10-21 久光製薬株式会社 Transdermal therapeutic device
JP4167750B2 (en) * 1997-04-16 2008-10-22 久光製薬株式会社 Transdermal absorption base and percutaneous absorption preparation containing the base
JP4399044B2 (en) * 1998-10-14 2010-01-13 久光製薬株式会社 Absorption enhancer and transdermal absorption preparation comprising the absorption enhancer
DE19906152B4 (en) * 1999-02-10 2005-02-10 Jenapharm Gmbh & Co. Kg Active substance-containing laminates for transdermal systems
WO2001001990A1 (en) * 1999-07-01 2001-01-11 Hisamitsu Pharmaceutical Co., Inc. Adhesive preparation for percutaneous absorption
DE10053375C1 (en) * 2000-10-27 2002-01-24 Lohmann Therapie Syst Lts Transdermal therapeutic system with light-sensitive agent in polymer matrix and backing, useful for therapy with e.g. nicotine, nifedipine, lacidipine, gestagen, vitamin B 12 or antibiotic, contains colorless ultraviolet absorber
WO2002045701A2 (en) * 2000-12-05 2002-06-13 Noven Pharmaceuticals, Inc. Crystallization inhibition of drugs in transdermal drug delivery systems

Also Published As

Publication number Publication date
NZ548091A (en) 2009-12-24
JP2007513938A (en) 2007-05-31
KR101168449B1 (en) 2012-07-25
MXPA06006682A (en) 2006-08-11
CN1913878B (en) 2010-05-26
IL176112A0 (en) 2006-10-05
CU20100143A7 (en) 2011-10-31
CU23868B1 (en) 2013-03-27
WO2005058287A2 (en) 2005-06-30
JP4965263B2 (en) 2012-07-04
NO341989B1 (en) 2018-03-12
BRPI0417530B1 (en) 2018-01-23
KR20060128910A (en) 2006-12-14
BRPI0417530B8 (en) 2021-05-25
AU2004298930A1 (en) 2005-06-30
ECSP066694A (en) 2006-10-31
CN1913878A (en) 2007-02-14
WO2005058287A3 (en) 2006-03-02
ZA200605713B (en) 2008-01-08
BRPI0417530A (en) 2007-03-13
CA2549916A1 (en) 2005-06-30
NO20062594L (en) 2006-07-10
IL176112A (en) 2011-02-28
EA011160B1 (en) 2009-02-27
CA2549916C (en) 2013-09-17
AU2004298930B2 (en) 2009-11-26

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Legal Events

Date Code Title Description
PD4A Registration of transfer of a eurasian patent in accordance with the succession in title
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KZ KG MD TJ TM

TC4A Change in name of a patent proprietor in a eurasian patent
PC4A Registration of transfer of a eurasian patent by assignment