CA2549916C - Administration transdermique d'hormones sans utilisation d'un agent facilitant la penetration - Google Patents

Administration transdermique d'hormones sans utilisation d'un agent facilitant la penetration Download PDF

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Publication number
CA2549916C
CA2549916C CA2549916A CA2549916A CA2549916C CA 2549916 C CA2549916 C CA 2549916C CA 2549916 A CA2549916 A CA 2549916A CA 2549916 A CA2549916 A CA 2549916A CA 2549916 C CA2549916 C CA 2549916C
Authority
CA
Canada
Prior art keywords
drug
gestodene
containing layer
weight
ester
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.)
Expired - Fee Related
Application number
CA2549916A
Other languages
English (en)
Other versions
CA2549916A1 (fr
Inventor
Stefan Bracht
Michael Dittgen
Petra Huber
Thomas Langguth
Dirk Schenk
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.)
Luye Pharma Switzerland AG
Original Assignee
Bayer Intellectual Property GmbH
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=CA2549916(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bayer Intellectual Property GmbH filed Critical Bayer Intellectual Property GmbH
Publication of CA2549916A1 publication Critical patent/CA2549916A1/fr
Application granted granted Critical
Publication of CA2549916C publication Critical patent/CA2549916C/fr
Anticipated expiration legal-status Critical
Expired - Fee Related 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
    • 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
    • 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
    • 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)
  • Reproductive Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Organic Chemistry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)

Abstract

La présente invention se rapporte à un timbre comportant une couche renfermant un médicament à faible teneur en hormones, par exemple un gestodène, et éventuellement un oestrogène (par exemple éthinyloestradiol). Lorsqu'une femme reçoit ce timbre, son taux de gestodène plasmatique est porté à 1,0 ng/ml dans des conditions constantes, l'adjonction à la couche renfermant le médicament d'agents facilitant la pénétration ou la perméation étant superflue. Des taux plasmatiques satisfaisants des hormones sont également obtenus pendant au moins une semaine, ce timbre étant ainsi utilisable à des fins de contraception chez la femme sur la base d'une fréquence d'administration hebdomadaire du timbre.
CA2549916A 2003-12-12 2004-12-10 Administration transdermique d'hormones sans utilisation d'un agent facilitant la penetration Expired - Fee Related CA2549916C (fr)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US52871803P 2003-12-12 2003-12-12
EP03078881.4 2003-12-12
US60/528,718 2003-12-12
EP03078881 2003-12-12
PCT/IB2004/052752 WO2005058287A2 (fr) 2003-12-12 2004-12-10 Administration transdermique d'hormones sans utilisation d'un agent facilitant la penetration

Publications (2)

Publication Number Publication Date
CA2549916A1 CA2549916A1 (fr) 2005-06-30
CA2549916C true CA2549916C (fr) 2013-09-17

Family

ID=34702342

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2549916A Expired - Fee Related CA2549916C (fr) 2003-12-12 2004-12-10 Administration transdermique d'hormones sans utilisation d'un agent facilitant la penetration

Country Status (15)

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

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100704825B1 (ko) 2003-02-21 2007-04-09 바이엘 쉐링 파마 악티엔게젤샤프트 Ｕｖ 안정성 경피 치료 플라스터
US8962013B2 (en) 2005-05-02 2015-02-24 Bayer Intellectual Property Gmbh Multi-layered transdermal system with triazine UV absorber
DE102005050729A1 (de) * 2005-10-19 2007-04-26 Schering Ag Verfahren zur präventiven bedarfsweisen hormonalen Kontrazeption
FR2900048B1 (fr) * 2006-04-21 2012-11-16 Oreal Compositions comprenant un derive diphenyl-methane hydroxyle
AU2015203180B2 (en) * 2010-09-06 2016-06-30 Bayer Intellectual Property Gmbh Transdermal therapeutic systems with crystallization-inhibiting protective film (release liner)
DE102010040299A1 (de) * 2010-09-06 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Transdermale therapeutische Systeme mit kristallisationsinhibierender Schutzfolie (Release Liner)
WO2012031999A2 (fr) 2010-09-06 2012-03-15 Bayer Pharma Aktiengesellschaft Timbres transdermiques faiblement dosés avec une libération élevée de médicament
EP2806862A2 (fr) * 2012-01-27 2014-12-03 Agile Therapeutics, Inc. Administration d'hormones par voie transdermique
HK1251938A1 (zh) * 2015-05-18 2019-05-03 敏捷治疗公司 避孕组合物及提高效能和调节副作用的方法

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0394429B1 (fr) * 1988-10-27 1996-01-10 Schering Aktiengesellschaft Preparation pour application transcutanee renfermant du gestodene
US5512292A (en) * 1990-10-29 1996-04-30 Alza Corporation Transdermal contraceptive formulations methods and devices
NZ240358A (en) * 1990-10-29 1994-09-27 Alza Corp Transdermal contraceptive device comprising (as active agents) an estrogen and a gestodene together with a skin permeation enhancer
DE4329242A1 (de) * 1993-08-26 1995-03-02 Schering Ag Mittel zur transdermalen Applikation enthaltend Gestodenester
DE4405898A1 (de) * 1994-02-18 1995-08-24 Schering Ag Transdermale therapeutische Systeme enthaltend Sexualsteroide
KR970706805A (ko) * 1994-11-18 1997-12-01 나까토미 히로타카 경피흡수첩부제(percutaneously absorbable patch)
CN1188189C (zh) * 1995-06-07 2005-02-09 奥瑟－麦内尔制药公司 基质层含有17－脱乙酰基诺孕酯的经皮贴片及基质的用途
JP4346696B2 (ja) * 1996-05-28 2009-10-21 久光製薬株式会社 経皮治療用装置
JP4167750B2 (ja) * 1997-04-16 2008-10-22 久光製薬株式会社 経皮吸収用基剤及び該基剤を含有する経皮吸収製剤
JP4399044B2 (ja) * 1998-10-14 2010-01-13 久光製薬株式会社 吸収促進剤及び該吸収促進剤を有してなる経皮吸収製剤
DE19906152B4 (de) * 1999-02-10 2005-02-10 Jenapharm Gmbh & Co. Kg Wirkstoffhaltige Laminate für Transdermalsysteme
WO2001001990A1 (fr) * 1999-07-01 2001-01-11 Hisamitsu Pharmaceutical Co., Inc. Preparation adhesive pour absorption percutanee
DE10053375C1 (de) * 2000-10-27 2002-01-24 Lohmann Therapie Syst Lts Transdermale therapeutische Systeme mit lichtempfindlichen Wirkstoffen
AU2002235155A1 (en) * 2000-12-05 2002-06-18 Noven Pharmaceuticals, Inc. Crystallization inhibition of drugs in transdermal drug delivery systems

Also Published As

Publication number Publication date
CN1913878A (zh) 2007-02-14
EA011160B1 (ru) 2009-02-27
NO341989B1 (no) 2018-03-12
KR20060128910A (ko) 2006-12-14
BRPI0417530B8 (pt) 2021-05-25
JP2007513938A (ja) 2007-05-31
NO20062594L (no) 2006-07-10
EA200601089A1 (ru) 2006-12-29
CU20100143A7 (es) 2011-10-31
ECSP066694A (es) 2006-10-31
IL176112A0 (en) 2006-10-05
CA2549916A1 (fr) 2005-06-30
AU2004298930B2 (en) 2009-11-26
CN1913878B (zh) 2010-05-26
CU23868B1 (es) 2013-03-27
MXPA06006682A (es) 2006-08-11
KR101168449B1 (ko) 2012-07-25
AU2004298930A1 (en) 2005-06-30
WO2005058287A2 (fr) 2005-06-30
JP4965263B2 (ja) 2012-07-04
IL176112A (en) 2011-02-28
ZA200605713B (en) 2008-01-08
NZ548091A (en) 2009-12-24
BRPI0417530A (pt) 2007-03-13
WO2005058287A3 (fr) 2006-03-02
BRPI0417530B1 (pt) 2018-01-23

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CA2549916C (fr) Administration transdermique d'hormones sans utilisation d'un agent facilitant la penetration
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MKLA Lapsed

Effective date: 20211210