AU762589B2 - Estradiol-containing patch for transdermal administration of hormones - Google Patents
Estradiol-containing patch for transdermal administration of hormones Download PDFInfo
- Publication number
- AU762589B2 AU762589B2 AU52842/99A AU5284299A AU762589B2 AU 762589 B2 AU762589 B2 AU 762589B2 AU 52842/99 A AU52842/99 A AU 52842/99A AU 5284299 A AU5284299 A AU 5284299A AU 762589 B2 AU762589 B2 AU 762589B2
- Authority
- AU
- Australia
- Prior art keywords
- active substance
- containing patch
- pressure
- patch according
- reservoir
- 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.)
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- VOXZDWNPVJITMN-ZBRFXRBCSA-N 17β-estradiol Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 VOXZDWNPVJITMN-ZBRFXRBCSA-N 0.000 title claims description 16
- 229960005309 estradiol Drugs 0.000 title claims description 16
- 229930182833 estradiol Natural products 0.000 title claims description 16
- 229940088597 hormone Drugs 0.000 title claims description 3
- 239000005556 hormone Substances 0.000 title claims description 3
- 239000013543 active substance Substances 0.000 claims description 50
- 239000010410 layer Substances 0.000 claims description 19
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 17
- 239000000853 adhesive Substances 0.000 claims description 11
- 230000001070 adhesive effect Effects 0.000 claims description 11
- 239000000583 progesterone congener Substances 0.000 claims description 11
- 239000012528 membrane Substances 0.000 claims description 9
- 239000011241 protective layer Substances 0.000 claims description 7
- 230000001225 therapeutic effect Effects 0.000 claims description 7
- 229920002261 Corn starch Polymers 0.000 claims description 6
- 239000008120 corn starch Substances 0.000 claims description 6
- 238000010521 absorption reaction Methods 0.000 claims description 5
- 238000002425 crystallisation Methods 0.000 claims description 4
- 230000008025 crystallization Effects 0.000 claims description 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 241001465754 Metazoa Species 0.000 claims description 3
- 238000013270 controlled release Methods 0.000 claims description 3
- 239000003223 protective agent Substances 0.000 claims description 3
- 239000003963 antioxidant agent Substances 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 239000002537 cosmetic Substances 0.000 claims description 2
- 239000006185 dispersion Substances 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003623 enhancer Substances 0.000 claims description 2
- 239000004831 Hot glue Substances 0.000 claims 1
- 238000002360 preparation method Methods 0.000 claims 1
- 229920005989 resin Polymers 0.000 claims 1
- 239000011347 resin Substances 0.000 claims 1
- 210000003491 skin Anatomy 0.000 description 11
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 10
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 8
- 238000004519 manufacturing process Methods 0.000 description 5
- 239000011159 matrix material Substances 0.000 description 5
- 238000000034 method Methods 0.000 description 5
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 4
- 235000012000 cholesterol Nutrition 0.000 description 4
- 239000000126 substance Substances 0.000 description 4
- ZVVGLAMWAQMPDR-WVEWYJOQSA-N (8r,9s,13s,14s,17s)-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol;hydrate Chemical compound O.OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1.OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 ZVVGLAMWAQMPDR-WVEWYJOQSA-N 0.000 description 3
- IMONTRJLAWHYGT-ZCPXKWAGSA-N Norethindrone Acetate Chemical compound C1CC2=CC(=O)CC[C@@H]2[C@@H]2[C@@H]1[C@@H]1CC[C@](C#C)(OC(=O)C)[C@@]1(C)CC2 IMONTRJLAWHYGT-ZCPXKWAGSA-N 0.000 description 3
- 229960003851 estradiol hemihydrate Drugs 0.000 description 3
- 229940011871 estrogen Drugs 0.000 description 3
- 239000000262 estrogen Substances 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000000203 mixture Substances 0.000 description 3
- 229960001652 norethindrone acetate Drugs 0.000 description 3
- 230000035515 penetration Effects 0.000 description 3
- 239000004014 plasticizer Substances 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- 229920001296 polysiloxane Polymers 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 239000002313 adhesive film Substances 0.000 description 2
- 229920000058 polyacrylate Polymers 0.000 description 2
- 229920006267 polyester film Polymers 0.000 description 2
- 238000001953 recrystallisation Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 238000003756 stirring Methods 0.000 description 2
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 description 1
- 229920002367 Polyisobutene Polymers 0.000 description 1
- 239000012790 adhesive layer Substances 0.000 description 1
- 239000004840 adhesive resin Substances 0.000 description 1
- 229920006223 adhesive resin Polymers 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 150000001875 compounds Chemical class 0.000 description 1
- 239000003433 contraceptive agent Substances 0.000 description 1
- 230000002254 contraceptive effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 238000005516 engineering process Methods 0.000 description 1
- 210000002615 epidermis Anatomy 0.000 description 1
- 230000007717 exclusion Effects 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000000155 melt Substances 0.000 description 1
- 239000003961 penetration enhancing agent Substances 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000002994 raw material Substances 0.000 description 1
- 239000002356 single layer Substances 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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
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)
- Hematology (AREA)
- Materials Engineering (AREA)
- Dermatology (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)
Description
Estradiol-containing patch for transdermal application of hormones The invention relates to an active substance-containing patch for controlled release of estradiol or its pharmaceutically acceptable derivatives, alone or in combination with gestagens, to the human or animal skin.
Estrogen- and/or gestagen-containing patches are already known. They do, however, have disadvantages in that they either contain ethanol or involve the potential danger of the active substance recrystallizing in the course of time.
From DE-OS 32 05 258 and EP 0 285 563 it is known to simultaneously administer estradiol and ethanol in a patch formulation. The production of this patch is, however, very complicated, and the patches have little wearing comfort after they have been applied, since they lack flexibility.
EP 0 285 563 describes a transdermal therapeutic system for the combined application of estrogens and gestagens. The reservoir contains the active substance formulation and optionally a membrane, as well as ethanol as percutaneous, absorption-enhancing agent. Since the release of active substance is mainly controlled by the membrane, this transdermal therapeutic system is fundamentally different from the active substance patch according to the present invention. In the patch described by this document, the adhesive merely has the function of fixing the patch on the skin. The fact that it is capable of contributing to the control of the active substance release does not constitute its main task, but is merely a possibly even unwanted side effect. The patch is a so-called "pouch patch", since the active substance formulation is present within a pouch, consisting of an impermeable backing layer and a membrane with adhesive layer. As a consequence of its complicated structure, the production of this patch requires great expenditure since the individual components must be prepared separately and then, in a further process step, combined to form a patch.
EP 0 275 716 describes a transdermal two-layer system in contrast to the mono-layer system of the present invention for simultaneous administration of one or more estrogens, which are dissolved or microdispersed in the polymer layer.
Here, the pressure-sensitive layer contains, apart from the active compounds, substances which enhance transdermal absorption. Polymer and pressure-sensitive layers may 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, its derivatives and combinations thereof.
WO 87/07138 describes an estradiol patch comprising a backing layer, a matrix containing the active substance, and a pressure-sensitive adhesive, which adhesive is covered by a removable protective layer. The production of the matrix and pressure-sensitive adhesive is carried out in process steps requiring a great expenditure in terms of the technology to be applied, by homogenizing, degasifying, coating, drying and separating into individual pieces. In one embodiment, the backing layer must even be coated with a pressure-sensitive adhesive, which means a further process step. The combining of the individual parts takes place in a separate process step. The overall production of the patch thus involves great expenditure and is complicated.
From US 4 624 665, systems are known which contain the active substance in microencapsuled form in the reservoir. The reservoir is embedded between a backing layer and a membrane.
The outer margin of the system is provided with a pressuresensitive adhesive. The structure and production of this system is very complicated since the active substance must be microencapsulated and distributed in a homogenous phase, which then, in further process steps, must be embedded between backing layer and membrane. In addition, the system must then be provided with an adhesive margin and covered with a protective layer.
Further, from EP 0 186 019 active substance patches are known wherein to a rubber/adhesive resin mass are added waterswellable polymers, and from which patches estradiol can be released. It has, however, emerged that the release of estradiol from these active substance patches is too low by far and does not meet therapeutic requirements.
In DE-OS 20 06 969 a patch or an adhesive bandage is described which has systemic action and wherein contraceptive substances are incorporated in the adhesive component or the adhesive film. The adhesive film may be an acrylate.
Thus the present invention seeks to avoid the abovementioned disadvantages and to provide a stable, i.e.
recrystallization-free estrogen- and/or gestagen-containing patch having sufficient active substance release, whose release is not subject to change by storage.
Surprisingly, it has emerged that this may be achieved by an estrogen- and/or gestagen-containing pressure-sensitive adhesive which contains cholesterol or corn starch.
According to one aspect, the present invention provides an active substance-containing patch according to the main claim. The oo subclaims relate to especially preferred embodiments of the subject matter of the invention.
As now claimed, according to one aspect, the present invention provides active substance-containing patch for controlled release of estradiol or its pharmaceutically acceptable derivatives in combination with gestagens to the human or animal skin, consisting of a backing layer, an active substance-containing reservoir connected thereto which is suitable for combined active substance release and has been produced using pressure-sensitive adhesives and comprises a crystallization inhibitor, and of a detachable protective layer, characterized in that the hormonecontaining pressure-sensitive adhesive of the active substance-containing reservoir contains 1-20%-wt. of corn starch as crystallization inhibitor.
Cholesterol is known as a pharmaceutical raw material and is described as such by the pharmacopoeias. Cholesterol acts as a swelling-regulating substance and as protective substance.
It is used by reason of its being well tolerated by the skin since it makes the epidermis soft and smooth. In addition, it increases the water absorption capability.
Corn starch is also described in the pharmacopoeias. Corn starch is used because of its adhesive power and absorption capacity, and because of its swelling capacity.
The active substance patch according to the invention can be used for cosmetic as well as therapeutic purposes in human and veterinary medicine.
S The recrystallization-free estrogen- and/or gestagencontaining patch having sufficient active substance release contains in its reservoir estradiol and its pharmaceutically acceptable derivatives, alone or in combination with gestagens, in a concentration of a total of 1 relative to the totality of the reservoir components, in fact in a molar ratio of 1:1 to 1:10.
The estradiol-containing reservoir may contain at least one component belonging to the- group comprising age-protecting agents, plasticizers, antioxidants and absorption enhancers.
Suitable plasticizers are known to those skilled in the art, and are described, for example, in DE 37 43 946. The estradiol-containing reservoir usually contains plasticizers in a portion of up to Furthermore, the reservoir contains age-protecting agents in a concentration of up to l%-wt. These are known to those *e
C
.e 0 skilled in the art and are described, for example, in DE 37 43 946.
The materials for the impermeable backing layer and the detachable protective layer are also known to those skilled in the art.
The estradiol-containing reservoir may be made from the solution, dispersion and from the melt.
In case the reservoir has no sufficient inherent tack on the skin, it can be provided with an additional active substancefree pressure-sensitive adhesive or with a circumferential pressure-sensitive adhesive margin. In this way it is ensured that the transdermal patch adheres on the skin over the entire period of application.
A particularly preferred structure of the transdermal estradiol-containing patch is a matrix system, wherein, as is known, the matrix takes over the control of the active substance release and is subject to the 4t-law according to Higuchi. This does not mean, however, that a membrane system is not of advantage in special cases. In membrane systems, an active substance release-controlling membrane is located between reservoir and pressure-sensitive adhesive layer.
The thickness of the transdermal patch is dependent on the therapeutic requirements and can be adjusted accordingly.
Usually, it ranges from 0.03 0.6 mm.
In the following, the invention will be illustrated by way of embodiment examples.
EXAMPLE 1: 131.91 g 3.2 55.89 of Durotak 387-2287 solution (67.8 g of solid matter) of cholesterol of ethanol/acetic acid ethyl ester (2:1 g/g) are homogenized by stirring at room temperature.
Subsequently, of estradiol hemihydrate and norethindrone acetate are added and this is stirred for about 2 hours.
The resultant active substance-containing adhesive mass is coated on the detachable protective layer (Hostaphan RN 100, coated on one side with silicone by Hoechst Diafoil) such that an active substance-containing reservoir having a weight per unit area of approximately 80 g/m 2 results. On this reservoir is laminated the impermeable backing layer (polyester film, 19 upm-thick). Subsequently, active substance patches of 16 cm 2 are punched out.
EXAMPLE 2: 131.91 3.2 55.89 of Durotak 387-2287 solution (67.8 g of solids) of corn starch of ethanol/acetic acid ethyl ester (2:1 g/g) are homogenized by stirring at room temperature.
Subsequently, of estradiol hemihydrate and norethindrone acetate are added and this is stirred for about 2 hours.
The resultant active substance-containing adhesive mass is coated on the detachable protective layer (Hostaphan RN 100, coated on one side with silicone by Hoechst Diafoil) such that an active substance-containing reservoir having a weight per unit area of approximately 80 g/m 2 results. On this reservoir is laminated the impermeable backing layer (polyester film, 19 mn-thick). Subsequently, active substance patches of 16 cm 2 are punched out.
For measuring the human skin penetration, the skin is clamped into the Franz cell. An estrogen- and/or gestagen-containing patch having a surface of 1.539 cm 2 is stuck on this skin and the active substance release is measured at 37 oC (acceptor medium: 0.9% sodium chloride solution 0.1% NaN 3 The examination on recrystallization phenomena is carried through in counterlight.
The results are listed in Table 1.
TABLE 1: Analysis results Active substance Human skin Example content penetration Recrystalug/16 cm 2 pg/16 cm 2 lisation (24-48 Std.) Es NeA Es NeA 1 3.200 11.200 97 131 none 2 3.200 11.200 173 163 none Comparison product 3.200 11.200 33 46 consider- Evorel able Conti Es: Estradiol hemihydrate NeA: Norethindrone acetate 8 As is shown by the Table, with the patch according to the invention one obtains a clearly increased penetration through the human skin as compared to the comparison product. At the same time it can be ascertained that in the examples according to the invention no recrystallization occurs.
Throughout this specification and the claims which follow, unless the context requires otherwise, the word "comprise", or variations such as "comprises" or "comprising", will be understood to imply the inclusion of a stated integer or step or group of integers or steps but not the exclusion of any other integer or step or group of integers or steps.
The reference to any prior art in this specification is not, and should not be taken as, an acknowledgment or any form of suggestion that the prior art forms part of the common general knowledge in Australia.
oo **e oo* *oo
Claims (12)
1. Active substance-containing patch for controlled release of estradiol or its pharmaceutically acceptable derivatives in combination with gestagens to the human or animal skin, consisting of a backing layer, an active substance-containing reservoir connected thereto which is suitable for combined active substance release and has been produced using pressure-sensitive adhesives and comprises a crystallization inhibitor, and of a detachable protective layer, characterized in that the hormone-containing pressure- sensitive adhesive of the active substance-containing reservoir contains 1-20%-wt. of corn starch as crystal- lization inhibitor.
2. Active substance-containing patch according to Claim 1, characterized in that the reservoir contains estradiol or its pharmaceutically acceptable derivatives, alone or in combination with gestagens, in a portion of 1 preferably 1.5
3. Active substance-containing patch according to Claim 1 or 2, characterized in that the reservoir contains estradiol or its pharmaceutically acceptable derivatives, alone or in combination with gestagens, in a molar ratio of 1:1 to 1:10.
4. Active substance-containing patch according to any one of Claims 1 to 3, characterized in that the pressure- sensitive adhesive contains tackifying resins in a concentration of 1 Active substance-containing patch according to one or more of Claims 1 to 4, characterized in that the reservoir contains at least one component belonging to the group of age-protecting agents, antioxidants and absorption enhancers. *o.
6. Active substance-containing patch according to one or more of Claims 1 to 5, characterized in that the pressure- sensitive adhesive is a pressure-sensitive solution adhesive, a pressure-sensitive dispersion adhesive or a pressure- sensitive hot-melt adhesive.
7. Active substance-containing patch according to one or more of Claims 1 to 6, characterized in that the backing layer is impermeable to the components of the reservoir.
8. Active substance-containing patch according to one or more of Claims 1 to 7, characterized in that the reservoir consists of several layers and is provided with an additional active substance-containing pressure-sensitive adhesive layer.
9. Active substance-containing patch according to one or more of Claims 1 to 8, characterized in that an active substance release-controlling membrane is provided between the reservoir and the pressure-sensitive adhesive layer. Active substance-containing patch according to one or more of Claims 1 to 9, characterized in that the reservoir is provided with a circumferential, pressure-sensitive adhesive margin.
11. Active substance-containing patch according to one or more of Claims 1 to 10, characterized in that the thickness of the active substance-containing patch is in the range of 0.03 0.6 mm.
12. Use of the active substance-containing patch according to Claims 1 to 11 for cosmetic purposes.
13. Use of the active substance-containing patch according to one of Claims 1 to 11 as a preparation for therapeutic purposes in human or veterinary medicine. 11
14. Active substance-containing patch and use thereof substantially as hereinbefore described with reference to examples 1 and 2. DATED THIS 30th day of April, 2003. LTS LOHMANN THERAPIE-SYSTEME AG By Its Patent Attorneys DAVIES COLLISON CAVE 99* *9 9** *9
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19834006 | 1998-07-29 | ||
| DE19834006A DE19834006A1 (en) | 1998-07-29 | 1998-07-29 | Estradiol-containing patch for the transdermal application of hormones |
| PCT/EP1999/005084 WO2000006130A1 (en) | 1998-07-29 | 1999-07-16 | Estradiol-containing patch for transdermal administration of hormones |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU5284299A AU5284299A (en) | 2000-02-21 |
| AU762589B2 true AU762589B2 (en) | 2003-06-26 |
Family
ID=7875612
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU52842/99A Ceased AU762589B2 (en) | 1998-07-29 | 1999-07-16 | Estradiol-containing patch for transdermal administration of hormones |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1100478A1 (en) |
| JP (1) | JP2002521426A (en) |
| KR (1) | KR20010072071A (en) |
| CN (1) | CN1310615A (en) |
| AR (1) | AR019948A1 (en) |
| AU (1) | AU762589B2 (en) |
| BR (1) | BR9912688A (en) |
| CA (1) | CA2338861A1 (en) |
| DE (1) | DE19834006A1 (en) |
| IL (1) | IL141032A0 (en) |
| PL (1) | PL345696A1 (en) |
| TR (1) | TR200100290T2 (en) |
| WO (1) | WO2000006130A1 (en) |
| ZA (1) | ZA200100721B (en) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2005047906A (en) * | 2003-07-16 | 2005-02-24 | Taisho Pharmaceut Co Ltd | Anti-inflammatory analgesic composition for external use |
| KR100689534B1 (en) * | 2005-05-18 | 2007-03-02 | 삼성전자주식회사 | Handheld terminal |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993008795A1 (en) * | 1991-10-31 | 1993-05-13 | Schering Aktiengesellschaft | Transdermal therapeutic systems containing crystallization inhibitors |
| EP0737477A1 (en) * | 1993-12-27 | 1996-10-16 | Akzo Nobel N.V. | Percutaneously absorbable preparation |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CH674618A5 (en) * | 1987-04-02 | 1990-06-29 | Ciba Geigy Ag | |
| US5676968A (en) * | 1991-10-31 | 1997-10-14 | Schering Aktiengesellschaft | Transdermal therapeutic systems with crystallization inhibitors |
| DE4229820C2 (en) * | 1992-09-07 | 1998-12-03 | Jenapharm Gmbh | Progestogen-based pharmaceutical preparation |
| DE4416927C1 (en) * | 1994-05-13 | 1995-08-31 | Lohmann Therapie Syst Lts | Device for release of active agents from melt-type adhesive |
-
1998
- 1998-07-29 DE DE19834006A patent/DE19834006A1/en not_active Ceased
-
1999
- 1999-07-16 JP JP2000561985A patent/JP2002521426A/en active Pending
- 1999-07-16 BR BR9912688-5A patent/BR9912688A/en not_active Application Discontinuation
- 1999-07-16 PL PL99345696A patent/PL345696A1/en unknown
- 1999-07-16 KR KR1020017001312A patent/KR20010072071A/en not_active Withdrawn
- 1999-07-16 IL IL14103299A patent/IL141032A0/en unknown
- 1999-07-16 CN CN99808853A patent/CN1310615A/en active Pending
- 1999-07-16 EP EP99938276A patent/EP1100478A1/en not_active Withdrawn
- 1999-07-16 WO PCT/EP1999/005084 patent/WO2000006130A1/en not_active Ceased
- 1999-07-16 AU AU52842/99A patent/AU762589B2/en not_active Ceased
- 1999-07-16 CA CA002338861A patent/CA2338861A1/en not_active Abandoned
- 1999-07-16 TR TR2001/00290T patent/TR200100290T2/en unknown
- 1999-07-28 AR ARP990103731A patent/AR019948A1/en not_active Application Discontinuation
-
2001
- 2001-01-25 ZA ZA200100721A patent/ZA200100721B/en unknown
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1993008795A1 (en) * | 1991-10-31 | 1993-05-13 | Schering Aktiengesellschaft | Transdermal therapeutic systems containing crystallization inhibitors |
| EP0737477A1 (en) * | 1993-12-27 | 1996-10-16 | Akzo Nobel N.V. | Percutaneously absorbable preparation |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20010072071A (en) | 2001-07-31 |
| IL141032A0 (en) | 2002-02-10 |
| ZA200100721B (en) | 2002-05-27 |
| BR9912688A (en) | 2001-11-27 |
| PL345696A1 (en) | 2002-01-02 |
| EP1100478A1 (en) | 2001-05-23 |
| JP2002521426A (en) | 2002-07-16 |
| AR019948A1 (en) | 2002-03-27 |
| AU5284299A (en) | 2000-02-21 |
| WO2000006130A1 (en) | 2000-02-10 |
| DE19834006A1 (en) | 2000-02-24 |
| TR200100290T2 (en) | 2001-07-23 |
| CA2338861A1 (en) | 2000-02-10 |
| CN1310615A (en) | 2001-08-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FGA | Letters patent sealed or granted (standard patent) |