EP1100478A1 - Estradiolhaltiges pflaster zur transdermalen applikation von hormonen - Google Patents

Estradiolhaltiges pflaster zur transdermalen applikation von hormonen

Info

Publication number
EP1100478A1
EP1100478A1 EP99938276A EP99938276A EP1100478A1 EP 1100478 A1 EP1100478 A1 EP 1100478A1 EP 99938276 A EP99938276 A EP 99938276A EP 99938276 A EP99938276 A EP 99938276A EP 1100478 A1 EP1100478 A1 EP 1100478A1
Authority
EP
European Patent Office
Prior art keywords
active substance
reservoir
sensitive adhesive
containing plaster
plaster according
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.)
Withdrawn
Application number
EP99938276A
Other languages
German (de)
English (en)
French (fr)
Inventor
Elvira Kirstgen
Reinhold Meconi
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 EP1100478A1 publication Critical patent/EP1100478A1/de
Withdrawn legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703Transdermal 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
    • A61K9/7038Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • A61K9/7053Transdermal 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
    • A61K9/7061Polyacrylates
    • 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
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L15/00Chemical aspects of, or use of materials for, bandages, dressings or absorbent pads
    • A61L15/16Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons
    • A61L15/20Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons containing organic materials
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61LMETHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
    • A61L15/00Chemical aspects of, or use of materials for, bandages, dressings or absorbent pads
    • A61L15/16Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons
    • A61L15/42Use of materials characterised by their function or physical properties
    • A61L15/58Adhesives
    • 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
    • A61P5/34Gestagens

Definitions

  • the invention relates to an active substance-containing patch for the controlled release of estradiol or its pharmaceutically acceptable derivatives, alone or in combination with gestagens, on the human or animal skin.
  • Patches containing estrogen and / or gestagen are already known. However, they have the disadvantages that they either contain ethanol or carry the potential risk that the active ingredient recrystallizes over time.
  • EP 0 285 563 describes a transdermal therapeutic system for the combined application of estrogens and gestagens.
  • the reservoir receives the active ingredient formulation and, if appropriate, a membrane and ethanol as a percutaneous absorption-improving agent. Since the release of the active ingredient is mainly controlled by the membrane, this transdermal therapeutic system differs fundamentally from the active ingredient patch according to the present invention.
  • the adhesive With the patch described there, the adhesive only has the function of attaching the patch to the skin. It is not his main task that he is able to contribute to the control of the active ingredient release, but only a - possibly even undesirable - side effect.
  • EP 0 275 716 describes - in contrast to the single-layer system according to the invention - a two-layer transdermal system for the simultaneous administration of one or more estrogens which are dissolved or microdispersed in the polymer layer.
  • the adhesive layer contains substances that improve transdermal absorption.
  • Polymer and adhesive layers can consist of polyacrylates, silicones or polyisobutylenes.
  • EP 0 328 806 describes a membrane-free transdermal therapeutic system, the matrix of which consists of a polyacrylate adhesive, a solvent, a penetration enhancer and estrogens, their derivatives and combinations thereof.
  • WO 87/07138 describes an estradiol patch with a backing layer, a matrix containing the active ingredient and a pressure-sensitive adhesive which is covered with a removable protective layer.
  • the matrix and pressure sensitive adhesive are produced in technologically very complex work processes by homogenizing, degassing, coating, drying and separating.
  • the back layer must even be coated with a pressure sensitive adhesive, which requires a further operation.
  • the individual parts are assembled in a separate operation. The production of the patch is therefore very complex and complex.
  • Active ingredient plasters are also known from EP 0 186 019, in which polymers which are swellable in water are added to a rubber / adhesive resin composition and from which estradiol can be released. However, it has been shown that the release of estradiol from these active substance patches is far too low and does not meet the therapeutic requirements.
  • DE-OS 20 06 969 describes a plaster or adhesive dressing with a systemic effect, in which contraceptive substances are incorporated in the adhesive component or the adhesive film.
  • the adhesive film can be an acrylate.
  • Cholesterol is known as a pharmaceutical raw material and is described as such in the pharmacopoeias. Cholesterol acts as a swelling regulator and protective substance. It is used because of its good skin tolerance, because it makes the epidermis soft and tender. It also increases water absorption.
  • Corn starch is also described in the pharmacopoeias. Corn starch is used because of its adherence and absorbency and its swelling ability.
  • the active ingredient-containing plaster according to the invention can be used for cosmetic and therapeutic purposes in human and veterinary medicine.
  • the recrystallization-free, estrogen- and / or progestin-containing plaster with sufficient active ingredient release contains estradiol and its pharmaceutically acceptable derivatives in the reservoir alone or in combination with gestagens in a concentration of 1-20% by weight, based on the totality of the reservoir components in a molar ratio of 1: 1 to 1:10.
  • the estradiol-containing reservoir can contain at least one component from the group comprising anti-aging agents, plasticizers, antioxidants and absorption improvers. Suitable plasticizers are known to the person skilled in the art and are described, for example, in DE 37 43 946.
  • the estradiol-containing reservoir usually contains plasticizers in a proportion of up to 5% by weight.
  • anti-aging agents are also present in the active substance-containing reservoir in a concentration of up to 1% by weight. contain. These are known to the person skilled in the art and are described, for example, in DE 37 43 946.
  • the materials for the impermeable backing layer and the removable protective layer are also known to the person skilled in the art.
  • the estradiol-containing reservoir can be generated from solution, from dispersion and also from the melt.
  • the reservoir can consist of several layers.
  • the reservoir is not sufficiently sticky to the skin, it can be provided with an additional active substance-free adhesive layer or with a circumferential adhesive edge. In this way it is ensured that the transdermal patch adheres to the skin over the entire application period.
  • a particularly preferred structure of the transdermal estradiol-containing patch is a matrix system in which, as is known, the matrix takes over the control for the active ingredient release and obeys the Vt law according to Higuchi.
  • a membrane system is not an advantage in special cases.
  • a membrane controlling the release of the active ingredient is attached between the reservoir and the pressure-sensitive adhesive layer.
  • the thickness of the transdermal patch depends on the therapeutic requirements and can be adjusted accordingly. It is usually in the range of 0.03-0.6 mm. The invention is explained below on the basis of exemplary embodiments.
  • the adhesive composition obtained in this way is coated on the removable protective layer (Hostapan RN 100, coated on one side with silicone - Hoechst-Diafoil) in such a way that an active ingredient-containing reservoir with a basis weight of approx. 80 g / m 2 results.
  • the impermeable backing layer (polyester film, 19 ⁇ m thick) is laminated on from this reservoir. Then 16 cm 2 large patches of active ingredient are punched out.
  • the adhesive substance obtained in this way is thus applied to the removable protective layer (Hostapan RN 100, coated on one side with silicone - Hoechst-Diafoil) coated that results in a drug-containing reservoir with a basis weight of approx. 80 g / m 2 .
  • the impermeable backing layer (polyester film, 19 ⁇ m thick) is laminated on from this reservoir. Then 16 cm 2 large patches of active ingredient are punched out.
  • the recrystallization phenomenon is checked visually in backlight.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Materials Engineering (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Endocrinology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
EP99938276A 1998-07-29 1999-07-16 Estradiolhaltiges pflaster zur transdermalen applikation von hormonen Withdrawn EP1100478A1 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19834006A DE19834006A1 (de) 1998-07-29 1998-07-29 Estradiolhaltiges Pflaster zur transdermalen Applikation von Hormonen
DE19834006 1998-07-29
PCT/EP1999/005084 WO2000006130A1 (de) 1998-07-29 1999-07-16 Estradiolhaltiges pflaster zur transdermalen applikation von hormonen

Publications (1)

Publication Number Publication Date
EP1100478A1 true EP1100478A1 (de) 2001-05-23

Family

ID=7875612

Family Applications (1)

Application Number Title Priority Date Filing Date
EP99938276A Withdrawn EP1100478A1 (de) 1998-07-29 1999-07-16 Estradiolhaltiges pflaster zur transdermalen applikation von hormonen

Country Status (14)

Country Link
EP (1) EP1100478A1 (pt)
JP (1) JP2002521426A (pt)
KR (1) KR20010072071A (pt)
CN (1) CN1310615A (pt)
AR (1) AR019948A1 (pt)
AU (1) AU762589B2 (pt)
BR (1) BR9912688A (pt)
CA (1) CA2338861A1 (pt)
DE (1) DE19834006A1 (pt)
IL (1) IL141032A0 (pt)
PL (1) PL345696A1 (pt)
TR (1) TR200100290T2 (pt)
WO (1) WO2000006130A1 (pt)
ZA (1) ZA200100721B (pt)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005047906A (ja) * 2003-07-16 2005-02-24 Taisho Pharmaceut Co Ltd 外用消炎鎮痛剤組成物
KR100689534B1 (ko) * 2005-05-18 2007-03-02 삼성전자주식회사 휴대 단말기

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH674618A5 (pt) * 1987-04-02 1990-06-29 Ciba Geigy Ag
DE4210711A1 (de) * 1991-10-31 1993-05-06 Schering Ag Berlin Und Bergkamen, 1000 Berlin, De Transdermale therapeutische systeme mit kristallisationsinhibitoren
US5676968A (en) * 1991-10-31 1997-10-14 Schering Aktiengesellschaft Transdermal therapeutic systems with crystallization inhibitors
DE4229820C2 (de) * 1992-09-07 1998-12-03 Jenapharm Gmbh Pharmazeutische Zubereitung auf Gestagen-Basis
WO1995017896A1 (fr) * 1993-12-27 1995-07-06 Akzo Nobel N.V. Preparation pour absorption par voie percutanee
DE4416927C1 (de) * 1994-05-13 1995-08-31 Lohmann Therapie Syst Lts Vorrichtung zur Abgabe von Wirkstoffen aus Haftschmelzklebern, Verfahren zu ihrer Herstellung und ihre Verwendung

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO0006130A1 *

Also Published As

Publication number Publication date
AR019948A1 (es) 2002-03-27
AU762589B2 (en) 2003-06-26
WO2000006130A1 (de) 2000-02-10
CA2338861A1 (en) 2000-02-10
BR9912688A (pt) 2001-11-27
TR200100290T2 (tr) 2001-07-23
KR20010072071A (ko) 2001-07-31
CN1310615A (zh) 2001-08-29
IL141032A0 (en) 2002-02-10
AU5284299A (en) 2000-02-21
JP2002521426A (ja) 2002-07-16
PL345696A1 (en) 2002-01-02
ZA200100721B (en) 2002-05-27
DE19834006A1 (de) 2000-02-24

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