NZ298428A - Transdermal system to dispense (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazol or salt thereof - Google Patents
Transdermal system to dispense (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazol or salt thereofInfo
- Publication number
- NZ298428A NZ298428A NZ298428A NZ29842896A NZ298428A NZ 298428 A NZ298428 A NZ 298428A NZ 298428 A NZ298428 A NZ 298428A NZ 29842896 A NZ29842896 A NZ 29842896A NZ 298428 A NZ298428 A NZ 298428A
- Authority
- NZ
- New Zealand
- Prior art keywords
- administration form
- form according
- active substance
- matrix
- methyl
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title claims description 8
- 229940100640 transdermal system Drugs 0.000 title 1
- 239000013543 active substance Substances 0.000 claims description 38
- 239000011159 matrix material Substances 0.000 claims description 16
- 229920000642 polymer Polymers 0.000 claims description 15
- 239000010410 layer Substances 0.000 claims description 14
- 239000003961 penetration enhancing agent Substances 0.000 claims description 13
- 239000004014 plasticizer Substances 0.000 claims description 9
- 239000011241 protective layer Substances 0.000 claims description 9
- 239000004831 Hot glue Substances 0.000 claims description 8
- 239000004820 Pressure-sensitive adhesive Substances 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 7
- 239000012528 membrane Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 6
- 239000000463 material Substances 0.000 claims description 5
- -1 polyoxyethylene Polymers 0.000 claims description 5
- 150000001298 alcohols Chemical class 0.000 claims description 4
- 150000001412 amines Chemical class 0.000 claims description 4
- 150000001735 carboxylic acids Chemical class 0.000 claims description 4
- 150000002170 ethers Chemical class 0.000 claims description 4
- 239000004744 fabric Substances 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 229930195733 hydrocarbon Natural products 0.000 claims description 4
- 150000002430 hydrocarbons Chemical class 0.000 claims description 4
- 239000000203 mixture Substances 0.000 claims description 4
- 239000004753 textile Substances 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 230000009974 thixotropic effect Effects 0.000 claims description 4
- 229920001577 copolymer Polymers 0.000 claims description 3
- 230000007246 mechanism Effects 0.000 claims description 3
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 2
- 238000009472 formulation Methods 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 150000003097 polyterpenes Chemical class 0.000 claims description 2
- 229930004725 sesquiterpene Natural products 0.000 claims description 2
- 150000004354 sesquiterpene derivatives Chemical class 0.000 claims description 2
- 150000003626 triacylglycerols Chemical class 0.000 claims description 2
- UFTFJSFQGQCHQW-UHFFFAOYSA-N triformin Chemical compound O=COCC(OC=O)COC=O UFTFJSFQGQCHQW-UHFFFAOYSA-N 0.000 claims description 2
- 239000007788 liquid Substances 0.000 claims 3
- 238000005266 casting Methods 0.000 claims 2
- 238000001125 extrusion Methods 0.000 claims 2
- 238000007761 roller coating Methods 0.000 claims 2
- 238000010345 tape casting Methods 0.000 claims 2
- GXCLVBGFBYZDAG-UHFFFAOYSA-N N-[2-(1H-indol-3-yl)ethyl]-N-methylprop-2-en-1-amine Chemical compound CN(CCC1=CNC2=C1C=CC=C2)CC=C GXCLVBGFBYZDAG-UHFFFAOYSA-N 0.000 claims 1
- 239000000853 adhesive Substances 0.000 claims 1
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 150000002314 glycerols Chemical class 0.000 claims 1
- 229920001200 poly(ethylene-vinyl acetate) Polymers 0.000 claims 1
- 229920000058 polyacrylate Polymers 0.000 claims 1
- 150000004040 pyrrolidinones Chemical class 0.000 claims 1
- 229920003051 synthetic elastomer Polymers 0.000 claims 1
- 239000005061 synthetic rubber Substances 0.000 claims 1
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 description 4
- NIXOWILDQLNWCW-UHFFFAOYSA-M Acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 description 3
- 239000000654 additive Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 206010012289 Dementia Diseases 0.000 description 2
- 230000001270 agonistic effect Effects 0.000 description 2
- 229920005601 base polymer Polymers 0.000 description 2
- 230000036765 blood level Effects 0.000 description 2
- 230000001276 controlling effect Effects 0.000 description 2
- 239000003431 cross linking reagent Substances 0.000 description 2
- 239000011888 foil Substances 0.000 description 2
- 230000000474 nursing effect Effects 0.000 description 2
- 210000001002 parasympathetic nervous system Anatomy 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 description 1
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 1
- 229920002126 Acrylic acid copolymer Polymers 0.000 description 1
- 208000024827 Alzheimer disease Diseases 0.000 description 1
- 229920000298 Cellophane Polymers 0.000 description 1
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 description 1
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 description 1
- 229920002367 Polyisobutene Polymers 0.000 description 1
- 229920001328 Polyvinylidene chloride Polymers 0.000 description 1
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 description 1
- 230000036626 alertness Effects 0.000 description 1
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 1
- 229910052782 aluminium Inorganic materials 0.000 description 1
- 230000003930 cognitive ability Effects 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 150000001993 dienes Chemical class 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- OWMBTIRJFMGPAC-UHFFFAOYSA-N dimethylamino 2-methylprop-2-enoate Chemical compound CN(C)OC(=O)C(C)=C OWMBTIRJFMGPAC-UHFFFAOYSA-N 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 229920001971 elastomer Polymers 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 230000006870 function Effects 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 150000002734 metacrylic acid derivatives Chemical class 0.000 description 1
- 125000005397 methacrylic acid ester group Chemical group 0.000 description 1
- 239000000178 monomer Substances 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- 229920001343 polytetrafluoroethylene Polymers 0.000 description 1
- 239000004810 polytetrafluoroethylene Substances 0.000 description 1
- 239000005033 polyvinylidene chloride Substances 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 239000003381 stabilizer Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 230000036642 wellbeing Effects 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
- A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Description
New Zealand Paient Spedficaiion for Paient Number £98428 9 New Zealand No 298428 International No PCT/EP96/00074 TO BE ENTERED AFTER ACCEPTANCE AND PUBLICATION Priority dates 14 01 1995, Complete Specification Filed 10 01 1996 Classification (6) A61K9/70, A61K31/42 Publication date 28 October 1999 Journal No 1445 Title of Invention Transdermal therapeutic system for dispensing (s)-3-methyl-5-(1 -methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutical^ acceptable salts Name, address and nationality of applicant(s) as in international application form ABBOTT LABORATORIES, 100 Abbott Park Road, Abbott Park, Illinois 60064-3500, United States of America NEW ZEALAND PATENTS ACT 1953 COMPLETE SPECIFICATION \ 1 A transdermal therapeutic system for the administration of (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutical^ acceptable salts SPECIFICATION The present invention relates to an gdministration form for the administration of (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutical^ acceptable salts and to a process for its production The active substance (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazole stands out for a highly specific agonistic effect on the parasympathetic nervous system, in particular on the nicotinic receptors Based on recent studies of the Alzheimer's disease therapy, the application of this active substance seems to improve the cognitive abilities of diseased persons to a considerable extent In this connection, however, regular and quantitatively constant administration of the active substance is an important factor to ensure constantly effective blood levels over extended periods So far the active substance has been administered exclusively by the oral route However, the oral administration of drugs to patients suffering from dementia imposes unacceptable requirements on the nursing staff, since the patient - owing to his disease - is not able to control the intake on his own.
It is the object of the present invention to provide an administration form for the administration of the active substance (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazole to achieve a highly specific agonistic effect on the parasympathetic nervous system of patients suffering from dementia Replacing the hitherto required regular oral administration at short intervals, it can achieve a constantly effective blood level and - for the patients' well-being - relieves the nursing staff from the burden and alertness experienced as a disadvantage so far To achieve this object the present invention provides a new administration form to administer (s)-3-methyl-5- (1 -methyl-2-pyr-rolidenyU-isoxazole or one of its pharmaceutical^ acceptable salts, which consists in the fact that it is present in the form of a patch as a transdermal therapeutic system (TTS) Accordingly, the subject matter of the present invention is a TTS for the administration of (s)-3-methyl-5- (1-methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutical^ acceptable salts, which is present in the form of a patch and comprises a suitable backing layer, an active substance reservoir connected thereto, a membrane controlling the active substance release if other control mechanisms are absent, a pressure-sensitive adhesive facility to fix the system to the skin, and, if required, a protective layer removable prior to the application of the system The suitable backing layer may consist both of a flexible and inflexible material which is impermeable to active substances Substances suitable for its production include polymeric sheets or metallic foils, such as aluminum foils which may be used alone or coated with a polymeric substrate In addition, textile fabrics may also be used if the reservoir cannot penetrate through them owing to their physical property, or if penetration is prevented by an adequate layer The active substance reservoir may have either a layered or a bag-type structure.
The layered reservoir may optionally consist of a polymeric matrix and the pure active substance or of a suitable active substance formulation, wherein the cohesion of the system as such is 3 provided by the polymer properties The reservoir consists of a base polymer and conventional additives The choice of the polymer matrix and the base polymer depends on the physicochemical properties of the active substance on the one hand, and on the desired release from the system on 5 the other hand In principle, any polymei is suitable that is used in the production of pressure-sensitive adhesives and which is compatible with the active substance Examples thereof include rubber, rubber-like homo-, co- or block polymers, poiyacrylates and their copolymers, and hot-melt adhesives Particularly preferred are polymers based on styrene and 1,3-10 dienes, polyisobutylenes and polyterpenes, polymers based on conventional acrylate monomers and their derivatives, or ethylene-vinyl-a^etate copolymers Among the block polymers based on styrene and 1,3-dienes linear styrene-isoprene-block-polymers are preferably used Preferred polymers based on acrylate are acrylic acid copolymers of 2-ethylhexyl 1 5 acrylate, vinyl acetate and acrylic acid with or without cross-linking agents Methacrylates are primarily understood as copolymeis based on dimethylaminomethacrylate and neutral methacrylic acid esters with or without cross-linking agents Other preferred polymers include esters of the hydiogenated colophony, in particular methyl or glyercol esters of hydrogenated colophony The kind and amount of possible additives depends on the polymer matrix used and on the active substance According to their function they may be 25 classified into the following groups plasticizers, tackifiers, stabilizers, carrier substances, diffusion and penetration regulating additives, or fillers The physiologically acceptable substances suitable for this purpose are known to pharmacists The plasticizer may be present in concentration of 0-30%, preferably 5-20%, relative to the total weight of the matrix The plasticizer may comprise at least one component selected from the groups of hydrocarbons, alcohols, carboxylic acids and their derivatives, ethers, esters or amines Preferably, the plasticizer comprises a natural or partially synthetic triglyceride or a mixture of these triglycerides in a concentration ranging from 0-30%, preferably in the range 5-20%, relative to the total weight of the matrix The permeation enhancer, if present, may be in a concentration ranging from 0-30%, preferably in the range 5-20%, relative to the total weight of the matrix Preferably, the permeation enhancer comprises at least one component selected from the groups of hydrocarbons, alcohols, carboxylic acids and their derivatives, ethers, esters, or amines Alternatively the permeation enhancer comprises at least one component selected from the group consisting of mono-, di- or sesquiter- penes As a further alternative, the permeation enhancer comprises at least one component selected from the group consisting of polyoxyethylene derivatives Alternatively, the permeation enhancer comprises a component selected from the group consisting of nitrogen-containing heterocycles and their derivatives As a further alternative, the permeation enhancer comprises a component selected from the group consisting of pyrrohdone derivatives A bag-type reservoir system may consist of the pure active substance or of a highly viscous or semisolid or thixotropic active substance preparation Particularly suitable are oily or aqueous gels which are dosed into a bag made of suitable sheetings or membrane materials In this connection, production of the active substance preparation may be carried out on the basis of lipophilic or hydrophilic bases In this case, the back of the bag, which is averted from the skin, must be impermeable to the active @ substance Preferably, a membrane which is permeable to the active substance can control the active substance release In the absence of other control mechanisms, the reservoir may be 5 combined with a membrane controlling the active substance release and a pressure-sensitive adhesive device to fix the system to the skin A reservoir not sufficiently adhering to the skin represents a particular case, this is combined with a special pressure-sensitive adhesive layer ensuring permanent contact of the system to the skin In principle, the same 10 materials as those used for the polymer matrix of the reservoir are suitable for the pressure-sensitive adhesive facility The protective layer which, if required, is to be removed prior to application may consist of the same materials as those used for the backing layer of 1 5 the system provided that they have been rendered removable, e g , by a silicone treatment However, it is also possible to use other protective layers, such as paper treated with polytetrafluoroethylene, cellophane, polyvinyl chlorido, polyvinylidene chloride, and the like If the laminate according to the present invention is divided into formats adequate for 20 therapy (patches) prior to application of the protective layer, the formats of the protective layer to be applied then may have a projecting end to make their removal from the patch easier In accordance with the layered or bag-type construction of the transdermal 25 systems described hereinabove, two different production processes are described a The active substance is homogeneously mixed with the components of the active substance reservoir, optionally in solution or under heating and 30 cooling, and applied to the cover layer which is permeable to the active substances or to a textile fabric lying thereon, whereupon the solvent/s is/are removed, if necessary Depending on whether the reservoir layer is
Claims (2)
1. 10. 15. 20. 6. is/are removed, if necessary Depending on whether the reservoir layer is self-adhesive or not, a pressure-sensitive adhesive device for permanent attachment to the skin is introduced between the reservoir and the protective layer which is removed in case of need b Within an adequate device, the liquid active substance or the liquid or semisolid or thixotropic active substance formulation is dosed onto a membrane which is permeable to the active substance and coveted with a suitable sheeting, avoiding the formation of voids as far as possible, whereupon the membrane and the sheeting are tightly sealed to form a bag Optionally, dosage may be carried out into a textile fabric which can additionally serve as a support It is also possible to dose into preformed bags The reservoir bag filled with active substance is additionally combined with a pressure-sensitive adhesive device, which may also have a multilayered structure and be provided with a control function for active substance release, and is subsequently covered with a protective layer which is removed in the case of need Preferably, when a hot-melt adhesive is incorporated, the components of the hot-melt adhesive are incorporated prior to the addition of the active substance, under heating to preferably 11 0 to 1 70°C until a homogenous melt of 70 to 100°C is obtained Where appropriate, the homogenous, active-substance-containing hot- melt adhesive mass is applied by means of extrusion, casting, roller coating, knife coating or by a printing process 7. i (J CLAIMS 1 An administration form for the administration of (s)-3-methyl-5-(1 -methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutical^ acceptable 5 salts wherein it is present as a transdermal therapeutic system in the form of a patch, comprising a layered structure including a suitable backing layer, an active substance reservoir laminated thereon, in the absence of other control mechanisms, a membrane controlling the active substance release, a pressure-sensitive adhesive device to attach the system to the 10 skin, and, if required, a protective layer removable to prior to application, the active substance reservoir comprising a base material of at least one polymer selected from the groups of polyacrylates and their copolymers, polyisobutyienes, polyterpenes, ethylene-vinyl-acetate-copolymers, block polymers, synthetic rubbers, and hot-melt adhesives 15 2.The administration form according to claim 1 wherein the backing layer of the system is impermeable to moisture and active substar.rc 3.The administration form according to claim 1 wherein the backing layer 20 is permeable to the active substance 4 The administration form according to any one of claims 1-3 wherein the polymer layer comprises esters of the hydrogenated colophony 25. 5.The administration form according to claim 4 wherein the polymer layer comprises methyl or glycerol esters of hydrogenated colophony 6 The administration form according to any one of the preceding claims which comprises a plasticizer in a concentration of 0-30% relative to the 30 total weight of the matrix , .. ~ G c r *■ inn ";° *-c., 'TO 5 10 15 20 25 7.The administration form according to claim 6 which comprises a plasticizer in a concentration of 5-20% relative to the total weight of the matrix 8.The administration form according to claim 6 or claim 7 wherein the plasticizer comprises at least one component selected from the groups of hydrocarbons, alcohols, carboxylic acids and their derivatives, ethers, esters, or amines 9.The administration form according to claim 6 or claim 7 wherein the plasticizer comprises a natural or partially synthetic triglyceride or a mixture of triglycerides in a concentration ranging from 0-30% relative to the total weight of the matrix 10.The administration form according to claim 9 wherein the plasticizer is in a concentration ranging from 5-20% relative to the total weight of the matrix 11.The administration form according to any one of the preceding claims which comprises a permeation enhancer in a concentration ranging form 0-30% relative to the total weight of the matrix 12.
2 The administration form according to claim 11, wherein the permeation enhancer is in a concentration ranging from 5-20% relative to the total weight of the matrix 13. The administration form according to claim 11 or claim 12 wherern the permeation enhancer comprises at least one component selected from the groups of hydrocarbons, alcohols, carboxylic acids and their derivatives, ethers, esters or amines 9. 14. The administration form according to claim 11 or claim 1 2 wherein the permeation enhancer comprises at least one component selected from the group consisting of mono-, di- or sesquiter- penes 5 15.5 The administration form according to claim 11 or claim 1 2 wherein the permeation enhancer comprises at least one component selected from the group consisting of polyoxyethylene derivatives 16.6 The administration form according to claim 11 or claim 1 2 wherein the 10 permeation enhancer comprisies a component selected from the group consisting of nitrogen-containing heterocycles and their derivatives 17. The administration form according to claim 11 or claim 12 wherein the permeation enhancer comprises a component selected from the group 15 consisting of pyrrolidone derivatives 18. The administration form according to any one of the preceding claims which has a bag-type active substance reservoir filled with a liquid or semisolid or thixotropic matrix 20 19.The administration form according to claim 18 wherein a gel former is the base of the semisolid or thixotropic active substance reservoir 20 A process for the production of the administration form according to 25 any one of the preceding claims in which (s)-3-methyl-5-(1 -methyl-2- pyrrolidenylHsoxazole or its pharmaceutical^ acceptable salt is applied in solution on a textile fabric provided on a prefabricated matrix which is optionally provided with a protective layer, whereupon matrix and active substance depot are provided with a cover layer 30. m^Ecid]r -.. OF OrFfc "6 /3SS -5§cr/yeo 10 21.The process according to claim 20 in which components of a hot-melt adhesive are incorporated, prior to the addition of the active substance, under heating until a homogeneous malt of 70 to 100°C is obtained 22.The process according to claim 20 in which the components of the hot-melt adhesive are incorporated under heating to 110 to 170°C 23.The process according vo any one of claims 20 to 22 in which the homogeneous, active-substtince-oontaining hot-melt adhesive mass is applied by means of extrusion, casting, roller coating, knife coating, or by a printing process 24.An administration form according to any one of claims 1 to 19, substantially as herein described 25 A process according to any one of claims 20 to 23, substantially as herein < ^scribed SEE ALSO COMPLETE SPECIFICATION END OF CLAIMS .
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE19501022A DE19501022C1 (en) | 1995-01-14 | 1995-01-14 | Transdermal therapeutic system for the administration of (s) -3-methyl-5- (1-methyl-2-pyrrolidenyl) isoxazole or one of its pharmaceutically acceptable salts and process for its preparation |
| PCT/EP1996/000074 WO1996021434A1 (en) | 1995-01-14 | 1996-01-10 | Transdermal therapeutic system for dispensing (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazole or one of its pharmaceutically acceptable salts |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ298428A true NZ298428A (en) | 1999-10-28 |
Family
ID=7751534
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ298428A NZ298428A (en) | 1995-01-14 | 1996-01-10 | Transdermal system to dispense (s)-3-methyl-5-(1-methyl-2-pyrrolidenyl)-isoxazol or salt thereof |
Country Status (12)
| Country | Link |
|---|---|
| EP (1) | EP0802790B1 (en) |
| JP (1) | JPH10511972A (en) |
| KR (1) | KR19980701419A (en) |
| AR (1) | AR001070A1 (en) |
| AT (1) | ATE292458T1 (en) |
| BR (1) | BR9607488A (en) |
| CA (1) | CA2210341A1 (en) |
| DE (2) | DE19501022C1 (en) |
| IL (1) | IL116615A (en) |
| NZ (1) | NZ298428A (en) |
| WO (1) | WO1996021434A1 (en) |
| ZA (1) | ZA96260B (en) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9615628D0 (en) * | 1996-07-25 | 1996-09-04 | Smithkline Beecham Plc | Formulation |
| DE10004790B4 (en) * | 2000-02-01 | 2004-09-09 | Lts Lohmann Therapie-Systeme Ag | Method for producing sewn or embroidered three-dimensional textile structure utilized for e.g. table cloth, involves connecting points on lattice structure with threads to form thread arrangement under which lattice structure is not visible |
| DE10019067C1 (en) * | 2000-04-18 | 2001-10-04 | Lohmann Therapie Syst Lts | Transdermal plaster comprising dofetilide, is useful for treatment of cardiovascular disorders |
| DE10118282A1 (en) | 2001-04-12 | 2002-12-05 | Lohmann Therapie Syst Lts | Pressure sensitive adhesive based on ethylene-vinyl acetate copolymers and adhesive resins, for medical purposes |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69231557T2 (en) * | 1991-05-29 | 2001-06-21 | Abbott Laboratories, Abbott Park | ISOXAZOLE AND ISOTHIAZOLE COMPOUNDS THAT IMPROVE THE COGNITIVE FUNCTIONS |
| DE4313928C2 (en) * | 1993-04-28 | 1996-09-19 | Lohmann Therapie Syst Lts | Transdermal therapeutic system for the controlled delivery of pilocarpine to the skin, process for its production and its use |
| DE4336557C2 (en) * | 1993-05-06 | 1997-07-17 | Lohmann Therapie Syst Lts | Estradiol-containing transdermal therapeutic system, process for its preparation and its use |
| US5494680A (en) * | 1993-12-08 | 1996-02-27 | Minnesota Mining And Manufacturing Company | Transdermal delivery device |
-
1995
- 1995-01-14 DE DE19501022A patent/DE19501022C1/en not_active Expired - Fee Related
- 1995-12-29 IL IL11661595A patent/IL116615A/en not_active IP Right Cessation
-
1996
- 1996-01-10 CA CA002210341A patent/CA2210341A1/en not_active Abandoned
- 1996-01-10 WO PCT/EP1996/000074 patent/WO1996021434A1/en active IP Right Grant
- 1996-01-10 DE DE59611212T patent/DE59611212D1/en not_active Expired - Fee Related
- 1996-01-10 EP EP96900309A patent/EP0802790B1/en not_active Expired - Lifetime
- 1996-01-10 BR BR9607488A patent/BR9607488A/en not_active Application Discontinuation
- 1996-01-10 KR KR1019970704809A patent/KR19980701419A/en active IP Right Grant
- 1996-01-10 AT AT96900309T patent/ATE292458T1/en not_active IP Right Cessation
- 1996-01-10 JP JP8521426A patent/JPH10511972A/en not_active Ceased
- 1996-01-10 NZ NZ298428A patent/NZ298428A/en unknown
- 1996-01-12 AR AR33502496A patent/AR001070A1/en unknown
- 1996-01-12 ZA ZA96260A patent/ZA96260B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2210341A1 (en) | 1996-07-18 |
| DE59611212D1 (en) | 2005-05-12 |
| IL116615A (en) | 1999-09-22 |
| ZA96260B (en) | 1996-08-01 |
| ATE292458T1 (en) | 2005-04-15 |
| WO1996021434A1 (en) | 1996-07-18 |
| DE19501022C1 (en) | 1996-06-05 |
| AR001070A1 (en) | 1997-09-24 |
| JPH10511972A (en) | 1998-11-17 |
| IL116615A0 (en) | 1996-03-31 |
| EP0802790B1 (en) | 2005-04-06 |
| MX9705324A (en) | 1997-10-31 |
| BR9607488A (en) | 1997-12-23 |
| KR19980701419A (en) | 1998-05-15 |
| EP0802790A1 (en) | 1997-10-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RENW | Renewal (renewal fees accepted) |