NO20062594L - Transdermal delivery system of hormones without penetration enhancers - Google Patents
Transdermal delivery system of hormones without penetration enhancersInfo
- Publication number
- NO20062594L NO20062594L NO20062594A NO20062594A NO20062594L NO 20062594 L NO20062594 L NO 20062594L NO 20062594 A NO20062594 A NO 20062594A NO 20062594 A NO20062594 A NO 20062594A NO 20062594 L NO20062594 L NO 20062594L
- Authority
- NO
- Norway
- Prior art keywords
- hormones
- patch
- penetration enhancers
- delivery system
- transdermal delivery
- Prior art date
Links
- 239000003623 enhancer Substances 0.000 title abstract 3
- 229940088597 hormone Drugs 0.000 title abstract 3
- 239000005556 hormone Substances 0.000 title abstract 3
- 230000035515 penetration Effects 0.000 title abstract 2
- 230000037317 transdermal delivery Effects 0.000 title 1
- 229940079593 drug Drugs 0.000 abstract 2
- 239000003814 drug Substances 0.000 abstract 2
- 230000036470 plasma concentration Effects 0.000 abstract 2
- BFPYWIDHMRZLRN-UHFFFAOYSA-N 17alpha-ethynyl estradiol Natural products OC1=CC=C2C3CCC(C)(C(CC4)(O)C#C)C4C3CCC2=C1 BFPYWIDHMRZLRN-UHFFFAOYSA-N 0.000 abstract 1
- BFPYWIDHMRZLRN-SLHNCBLASA-N Ethinyl estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 BFPYWIDHMRZLRN-SLHNCBLASA-N 0.000 abstract 1
- 229940011871 estrogen Drugs 0.000 abstract 1
- 239000000262 estrogen Substances 0.000 abstract 1
- 229960002568 ethinylestradiol Drugs 0.000 abstract 1
- 238000010348 incorporation Methods 0.000 abstract 1
- 230000003442 weekly effect Effects 0.000 abstract 1
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)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Botany (AREA)
- Gynecology & Obstetrics (AREA)
- Endocrinology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Reproductive Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Steroid Compounds (AREA)
Abstract
Den foreliggende oppfinnelsen angår et plaster som omfatter et legemiddelinneholdende lag med lavt innhold av hormon, slik som gestoden, og eventuelt et østrogen (f.eks. etiny-lestradiol). Ved administrasjon av plasteret til en kvinne, oppnås plasmanivåer på minst 1,0 ng/ml av gestoden ved steady-state-betingelser uten behov for inkorporering av penetrasjonsenhancere eller permeasjonsenhancere i det legemiddelinneholdende laget. Tilfredsstillende plasmanivaer i hormonene oppnås også gjennom en periode på minst 1 uke, idet plasteret gjøres anvendelig til bruk ved svangerskapsforebygging hos kvinner med et prinsipp om administrasjon av plastrene én gang ukentlig.The present invention relates to a patch comprising a low-hormone drug-containing layer, such as the gestod, and optionally an estrogen (e.g., ethinylestradiol). When administering the patch to a woman, plasma levels of at least 1.0 ng / ml of the gestode are achieved under steady-state conditions without the need for incorporation of penetration enhancers or permeation enhancers into the drug-containing layer. Satisfactory plasma levels of the hormones are also achieved over a period of at least 1 week, the patch being made usable for use in contraception in women with a principle of administering the patches once weekly.
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 |
|---|---|
| NO20062594L true NO20062594L (en) | 2006-07-10 |
| NO341989B1 NO341989B1 (en) | 2018-03-12 |
Family
ID=34702342
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NO20062594A NO341989B1 (en) | 2003-12-12 | 2006-06-06 | Transdermal administration of hormones without the need for penetration enhancers. |
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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004073696A1 (en) | 2003-02-21 | 2004-09-02 | Schering 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 |
| SI2613772T1 (en) | 2010-09-06 | 2017-03-31 | Bayer Intellectual Property Gmbh | 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) |
| HK1204287A1 (en) * | 2012-01-27 | 2015-11-13 | 敏捷治疗公司 | Transdermal hormone delivery |
| WO2016187269A1 (en) * | 2015-05-18 | 2016-11-24 | Agile Therapeutics, Inc. | Contraceptive compositions and methods for improved efficacy and modulation of side effects |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU210549B (en) * | 1988-10-27 | 1995-05-29 | Schering Ag | Process for producing transdermally applicable pharmaceutical composition containing gestodene |
| MX9101787A (en) * | 1990-10-29 | 1992-06-05 | Alza Corp | 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 |
| CA2222133C (en) * | 1995-06-07 | 2002-12-24 | 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 |
| US20020106402A1 (en) * | 2000-12-05 | 2002-08-08 | Hartwig Rod Lawson | Crystallization inhibition of drugs in transdermal drug delivery systems and methods of use |
-
2004
- 2004-12-10 CA CA2549916A patent/CA2549916C/en not_active Expired - Fee Related
- 2004-12-10 NZ NZ548091A patent/NZ548091A/en not_active IP Right Cessation
- 2004-12-10 AU AU2004298930A patent/AU2004298930B2/en not_active Ceased
- 2004-12-10 MX MXPA06006682A patent/MXPA06006682A/en active IP Right Grant
- 2004-12-10 CN CN2004800413210A patent/CN1913878B/en not_active Expired - Lifetime
- 2004-12-10 BR BRPI0417530A patent/BRPI0417530B8/en not_active IP Right Cessation
- 2004-12-10 EA EA200601089A patent/EA011160B1/en not_active IP Right Cessation
- 2004-12-10 WO PCT/IB2004/052752 patent/WO2005058287A2/en not_active Ceased
- 2004-12-10 JP JP2006543709A patent/JP4965263B2/en not_active Expired - Fee Related
- 2004-12-10 KR KR1020067013923A patent/KR101168449B1/en not_active Expired - Fee Related
-
2006
- 2006-06-05 IL IL176112A patent/IL176112A/en active IP Right Grant
- 2006-06-06 NO NO20062594A patent/NO341989B1/en not_active IP Right Cessation
- 2006-07-11 ZA ZA2006/05713A patent/ZA200605713B/en unknown
- 2006-07-11 EC EC2006006694A patent/ECSP066694A/en unknown
-
2010
- 2010-07-05 CU CU20100143A patent/CU23868B1/en active IP Right Grant
Also Published As
| Publication number | Publication date |
|---|---|
| CN1913878A (en) | 2007-02-14 |
| JP2007513938A (en) | 2007-05-31 |
| CA2549916C (en) | 2013-09-17 |
| EA011160B1 (en) | 2009-02-27 |
| BRPI0417530B8 (en) | 2021-05-25 |
| NO341989B1 (en) | 2018-03-12 |
| WO2005058287A2 (en) | 2005-06-30 |
| IL176112A0 (en) | 2006-10-05 |
| NZ548091A (en) | 2009-12-24 |
| CN1913878B (en) | 2010-05-26 |
| AU2004298930B2 (en) | 2009-11-26 |
| KR101168449B1 (en) | 2012-07-25 |
| CU20100143A7 (en) | 2011-10-31 |
| CA2549916A1 (en) | 2005-06-30 |
| BRPI0417530B1 (en) | 2018-01-23 |
| CU23868B1 (en) | 2013-03-27 |
| IL176112A (en) | 2011-02-28 |
| MXPA06006682A (en) | 2006-08-11 |
| EA200601089A1 (en) | 2006-12-29 |
| WO2005058287A3 (en) | 2006-03-02 |
| JP4965263B2 (en) | 2012-07-04 |
| ECSP066694A (en) | 2006-10-31 |
| KR20060128910A (en) | 2006-12-14 |
| ZA200605713B (en) | 2008-01-08 |
| AU2004298930A1 (en) | 2005-06-30 |
| BRPI0417530A (en) | 2007-03-13 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| CHAD | Change of the owner's name or address (par. 44 patent law, par. patentforskriften) |
Owner name: BAYER INTELLECTUAL PROPERTY GMBH, DE |
|
| MM1K | Lapsed by not paying the annual fees |