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
  • 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
  • A61L—METHODS 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
  • A61L15/00—Chemical aspects of, or use of materials for, bandages, dressings or absorbent pads
  • A61L15/16—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons
  • A61L15/20—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons containing organic materials
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS 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
  • A61L15/00—Chemical aspects of, or use of materials for, bandages, dressings or absorbent pads
  • A61L15/16—Bandages, dressings or absorbent pads for physiological fluids such as urine or blood, e.g. sanitary towels, tampons
  • A61L15/42—Use of materials characterised by their function or physical properties
  • A61L15/58—Adhesives
• • 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

• 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)
• Chemical & Material Sciences (AREA)
• Veterinary Medicine (AREA)
• Public Health (AREA)
• General Health & Medical Sciences (AREA)
• Animal Behavior & Ethology (AREA)
• Epidemiology (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Medicinal Chemistry (AREA)
• Pharmacology & Pharmacy (AREA)
• Dermatology (AREA)
• Hematology (AREA)
• Materials Engineering (AREA)
• Organic Chemistry (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• General Chemical & Material Sciences (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Endocrinology (AREA)
• Diabetes (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)
• Steroid Compounds (AREA)

Priority Applications (8)

Applications Claiming Priority (2)

Publications (1)

Family

ID=7875612

Family Applications (1)

Country Status (14)

Families Citing this family (2)

Citations (3)

Family Cites Families (3)

• 1998
  • 1998-07-29 DE DE19834006A patent/DE19834006A1/de not_active Ceased
• 1999
  • 1999-07-16 EP EP99938276A patent/EP1100478A1/de not_active Withdrawn
  • 1999-07-16 PL PL99345696A patent/PL345696A1/xx unknown
  • 1999-07-16 BR BR9912688-5A patent/BR9912688A/pt not_active Application Discontinuation
  • 1999-07-16 AU AU52842/99A patent/AU762589B2/en not_active Ceased
  • 1999-07-16 CN CN99808853A patent/CN1310615A/zh active Pending
  • 1999-07-16 JP JP2000561985A patent/JP2002521426A/ja active Pending
  • 1999-07-16 WO PCT/EP1999/005084 patent/WO2000006130A1/de not_active Application Discontinuation
  • 1999-07-16 KR KR1020017001312A patent/KR20010072071A/ko not_active Application Discontinuation
  • 1999-07-16 CA CA002338861A patent/CA2338861A1/en not_active Abandoned
  • 1999-07-16 TR TR2001/00290T patent/TR200100290T2/xx unknown
  • 1999-07-16 IL IL14103299A patent/IL141032A0/xx unknown
  • 1999-07-28 AR ARP990103731A patent/AR019948A1/es not_active Application Discontinuation
• 2001
  • 2001-01-25 ZA ZA200100721A patent/ZA200100721B/en unknown

Patent Citations (3)

Non-Patent Citations (1)

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