EP1448175A1 - Systeme therapeutique transdermique contenant des hormones steroides et du propylene glycol monocaprylate - Google Patents

Systeme therapeutique transdermique contenant des hormones steroides et du propylene glycol monocaprylate

Info

Publication number
EP1448175A1
EP1448175A1 EP02790390A EP02790390A EP1448175A1 EP 1448175 A1 EP1448175 A1 EP 1448175A1 EP 02790390 A EP02790390 A EP 02790390A EP 02790390 A EP02790390 A EP 02790390A EP 1448175 A1 EP1448175 A1 EP 1448175A1
Authority
EP
European Patent Office
Prior art keywords
transdermal therapeutic
therapeutic system
propylene glycol
glycol monocaprylate
styrene
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.)
Ceased
Application number
EP02790390A
Other languages
German (de)
English (en)
Inventor
Frank Theobald
René Eifler
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.)
LTS Lohmann Therapie Systeme AG
Original Assignee
LTS Lohmann Therapie Systeme AG
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 LTS Lohmann Therapie Systeme AG filed Critical LTS Lohmann Therapie Systeme AG
Publication of EP1448175A1 publication Critical patent/EP1448175A1/fr
Ceased legal-status Critical Current

Links

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
    • 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
    • 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
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/28—Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • 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
    • 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
    • A61P5/34—Gestagens

Definitions

  • Transdermal therapeutic systems are layered pharmaceutical dosage forms that have an active substance-impermeable backing layer, an active substance-containing reservoir layer and an adhesive layer, which ensures firm contact with the skin surface of a user.
  • TTS Transdermal therapeutic systems
  • transdermal therapeutic systems One of the most important areas of indication for transdermal therapeutic systems is hormone substitution therapy.
  • postmenopausal hormone substitution can advantageously be carried out using transdermal therapeutic systems.
  • Testosterone the male sex hormone, also belongs to the series of steroid hormones that are used in hormone replacement therapy (e.g. to treat hypogonadism). So-called penetration enhancers are often required to achieve the required plasma levels for the above-mentioned indications.
  • US Pat. No. 5,122,383 discloses the use of sorbitan esters and US Pat. No. 4,863,738 the use of glycerol monooleate, in each case as a penetration accelerator when steroids are used in transdermal therapeutic systems.
  • EP-A-279 977 describes the use of propylene glycol laurate and propylene glycol dipelarginate as a penetration accelerator for the transdermal administration of sex hormones (progesterone and estradiol).
  • EP-A-272 987 discloses the use of mono- and difatty acid esters of propylene glycol, in particular propylene glycol mono- and dilaurate, propylene glycol monopalmitate, propylene glycol monostearate and propylene glycol monooleate as percutaneous absorption enhancers in transdermal therapeutic systems, the active substances and fentanyl derivatives or other steroids could be.
  • estradiol ethinyl estradiol
  • progestogen as progestogen
  • medroxyprogesterone hydroxyprogesterone
  • levonorgestrel norethisterone acetate
  • norgestrel lynestrenol
  • ethynodiol diacetate allylestrenol
  • the progestogen (17 ⁇ -11-methyl-17-methyl-17-alpha-17-methyl-17-alpha-17-methyl-17-alpha-17-alpha-17-methyl-17-gestagen-17 ⁇ -17-methyl-17-n-19-gestagen) -4,15- dien-20-in-3-one (with the designation Org 30659, Fa. Organon, Oss, NL) and others, as well as testosterone as a male hormone (this list is not intended to be limiting).
  • Examples 1 and 2 below show that when 5% propylene glycol monocaprylate is used, an increase in the active substance flow of approximately 15% (gestagens) and approximately 20% (testosterone) can be achieved.
  • the measurements were carried out as follows: A modified Franz diffusion cell and in each case a transdermal therapeutic system with an effective diffusion area of 4.1 cm 2 were used.
  • the test temperature was 32 ° C.
  • the drug flow was measured on a human skin epidermis.
  • An aqueous solution of 0.1% hydroxypropyl- ⁇ -cyclodextrin + 0.1% NaN 3 was used as the acceptor; the acceptor volume was 9 ml (volume exchange after 32, 48, 56 and 72 hours).

Landscapes

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

Abstract

La présente invention concerne un système thérapeutique transdermique contenant au moins une hormone stéroïde et du propylène glycol monocaprylate en tant qu'accélérateur de pénétration dans le cadre de la thérapie de substitution hormonale et pour la contraception.
EP02790390A 2001-12-01 2002-11-16 Systeme therapeutique transdermique contenant des hormones steroides et du propylene glycol monocaprylate Ceased EP1448175A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10159120 2001-12-01
DE10159120A DE10159120B4 (de) 2001-12-01 2001-12-01 Steroidhormonhaltige transdermale therapeutische Systeme enthaltend Propylenglycolmonocaprylat und seine Verwendung
PCT/EP2002/012873 WO2003047555A1 (fr) 2001-12-01 2002-11-16 Systeme therapeutique transdermique contenant des hormones steroides et du propylene glycol monocaprylate

Publications (1)

Publication Number Publication Date
EP1448175A1 true EP1448175A1 (fr) 2004-08-25

Family

ID=7707752

Family Applications (1)

Application Number Title Priority Date Filing Date
EP02790390A Ceased EP1448175A1 (fr) 2001-12-01 2002-11-16 Systeme therapeutique transdermique contenant des hormones steroides et du propylene glycol monocaprylate

Country Status (17)

Country Link
US (1) US20050118244A1 (fr)
EP (1) EP1448175A1 (fr)
JP (1) JP2005531493A (fr)
KR (1) KR100908970B1 (fr)
CN (1) CN1596105A (fr)
AU (1) AU2002365624B2 (fr)
BR (1) BR0214634A (fr)
CA (1) CA2465395A1 (fr)
DE (1) DE10159120B4 (fr)
HU (1) HUP0402213A2 (fr)
IL (1) IL162196A0 (fr)
MX (1) MXPA04005211A (fr)
NZ (1) NZ533159A (fr)
PL (1) PL368734A1 (fr)
RU (1) RU2317813C2 (fr)
WO (1) WO2003047555A1 (fr)
ZA (1) ZA200403658B (fr)

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ES2712778T3 (es) 2007-05-30 2019-05-14 Ascensia Diabetes Care Holdings Ag Método y sistema para gestionar datos de salud
FR2924942B1 (fr) * 2007-12-14 2012-06-15 Pf Medicament Compositions pharmaceutiques transcutanees contenant une hormone steroidienne
JP2011121866A (ja) * 2008-03-31 2011-06-23 Rohto Pharmaceutical Co Ltd 皮膚外用組成物
KR101828619B1 (ko) 2010-03-28 2018-02-12 이브스트라, 인코포레이티드 질 내 약물 전달 장치
US9301920B2 (en) 2012-06-18 2016-04-05 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
HUE055562T2 (hu) 2011-11-23 2021-11-29 Therapeuticsmd Inc Természetes kombinációjú hormon helyettesítõ kiszerelések, és terápiák ezekkel
US10806697B2 (en) 2012-12-21 2020-10-20 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US20150196640A1 (en) 2012-06-18 2015-07-16 Therapeuticsmd, Inc. Progesterone formulations having a desirable pk profile
US20130338122A1 (en) * 2012-06-18 2013-12-19 Therapeuticsmd, Inc. Transdermal hormone replacement therapies
US10806740B2 (en) 2012-06-18 2020-10-20 Therapeuticsmd, Inc. Natural combination hormone replacement formulations and therapies
US11246875B2 (en) 2012-12-21 2022-02-15 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US11266661B2 (en) 2012-12-21 2022-03-08 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US9180091B2 (en) 2012-12-21 2015-11-10 Therapeuticsmd, Inc. Soluble estradiol capsule for vaginal insertion
US10471072B2 (en) 2012-12-21 2019-11-12 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10568891B2 (en) 2012-12-21 2020-02-25 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
US10537581B2 (en) 2012-12-21 2020-01-21 Therapeuticsmd, Inc. Vaginal inserted estradiol pharmaceutical compositions and methods
RU2016143081A (ru) 2014-05-22 2018-06-26 Терапьютиксмд, Инк. Натуральные комбинированные гормонозаместительные составы и терапии
WO2016018993A1 (fr) 2014-07-29 2016-02-04 Therapeuticsmd, Inc. Crème transdermique
US10328087B2 (en) 2015-07-23 2019-06-25 Therapeuticsmd, Inc. Formulations for solubilizing hormones
KR20180126582A (ko) 2016-04-01 2018-11-27 쎄러퓨틱스엠디, 인코퍼레이티드 스테로이드 호르몬 약제학적 조성물
US10286077B2 (en) 2016-04-01 2019-05-14 Therapeuticsmd, Inc. Steroid hormone compositions in medium chain oils
KR102024996B1 (ko) * 2017-12-27 2019-09-25 동아에스티 주식회사 도네페질을 함유하는 치매 치료용 경피흡수제제
JPWO2020184208A1 (fr) * 2019-03-14 2020-09-17
US11633405B2 (en) 2020-02-07 2023-04-25 Therapeuticsmd, Inc. Steroid hormone pharmaceutical formulations

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Also Published As

Publication number Publication date
DE10159120A1 (de) 2003-06-12
CN1596105A (zh) 2005-03-16
KR100908970B1 (ko) 2009-07-22
IL162196A0 (en) 2005-11-20
HUP0402213A2 (hu) 2005-02-28
JP2005531493A (ja) 2005-10-20
MXPA04005211A (es) 2004-08-19
AU2002365624B2 (en) 2007-11-22
PL368734A1 (en) 2005-04-04
DE10159120B4 (de) 2006-08-17
US20050118244A1 (en) 2005-06-02
ZA200403658B (en) 2004-09-01
RU2004120067A (ru) 2005-04-10
NZ533159A (en) 2005-12-23
KR20050044628A (ko) 2005-05-12
RU2317813C2 (ru) 2008-02-27
BR0214634A (pt) 2004-11-03
WO2003047555A1 (fr) 2003-06-12
CA2465395A1 (fr) 2003-06-12
AU2002365624A1 (en) 2003-06-17

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