DK200500030U3 - Transdermalt plaster til indgivelse af fentanyl - Google Patents
Transdermalt plaster til indgivelse af fentanyl Download PDFInfo
- Publication number
- DK200500030U3 DK200500030U3 DK200500030U DKBA200500030U DK200500030U3 DK 200500030 U3 DK200500030 U3 DK 200500030U3 DK 200500030 U DK200500030 U DK 200500030U DK BA200500030 U DKBA200500030 U DK BA200500030U DK 200500030 U3 DK200500030 U3 DK 200500030U3
- Authority
- DK
- Denmark
- Prior art keywords
- fentanyl
- patch according
- reservoir
- patch
- phase
- Prior art date
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- PJMPHNIQZUBGLI-UHFFFAOYSA-N fentanyl Chemical compound C=1C=CC=CC=1N(C(=O)CC)C(CC1)CCN1CCC1=CC=CC=C1 PJMPHNIQZUBGLI-UHFFFAOYSA-N 0.000 title description 26
- 229960002428 fentanyl Drugs 0.000 title description 21
- 239000000853 adhesive Substances 0.000 description 12
- 230000002779 inactivation Effects 0.000 description 11
- 239000000470 constituent Substances 0.000 description 8
- 239000012071 phase Substances 0.000 description 8
- GGCSSNBKKAUURC-UHFFFAOYSA-N sufentanil Chemical compound C1CN(CCC=2SC=CC=2)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 GGCSSNBKKAUURC-UHFFFAOYSA-N 0.000 description 8
- 229960004739 sufentanil Drugs 0.000 description 8
- 230000001070 adhesive effect Effects 0.000 description 7
- 230000007062 hydrolysis Effects 0.000 description 7
- 238000006460 hydrolysis reaction Methods 0.000 description 7
- 239000007791 liquid phase Substances 0.000 description 7
- 229920000642 polymer Polymers 0.000 description 7
- 102000004169 proteins and genes Human genes 0.000 description 7
- 108090000623 proteins and genes Proteins 0.000 description 7
- 239000002994 raw material Substances 0.000 description 7
- 239000000203 mixture Substances 0.000 description 6
- 229920000058 polyacrylate Polymers 0.000 description 6
- 239000007790 solid phase Substances 0.000 description 6
- 239000011541 reaction mixture Substances 0.000 description 5
- 229920001684 low density polyethylene Polymers 0.000 description 4
- 239000004702 low-density polyethylene Substances 0.000 description 4
- 239000000463 material Substances 0.000 description 4
- 238000000034 method Methods 0.000 description 4
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 239000012223 aqueous fraction Substances 0.000 description 3
- 239000008346 aqueous phase Substances 0.000 description 3
- 229940099191 duragesic Drugs 0.000 description 3
- 238000009434 installation Methods 0.000 description 3
- 239000011505 plaster Substances 0.000 description 3
- -1 polyethylene Polymers 0.000 description 3
- 239000005020 polyethylene terephthalate Substances 0.000 description 3
- 229920000139 polyethylene terephthalate Polymers 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 2
- 239000002998 adhesive polymer Substances 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 230000001747 exhibiting effect Effects 0.000 description 2
- 229920001903 high density polyethylene Polymers 0.000 description 2
- 239000004700 high-density polyethylene Substances 0.000 description 2
- 230000003301 hydrolyzing effect Effects 0.000 description 2
- 229920001179 medium density polyethylene Polymers 0.000 description 2
- 239000004701 medium-density polyethylene Substances 0.000 description 2
- 102000004196 processed proteins & peptides Human genes 0.000 description 2
- 108090000765 processed proteins & peptides Proteins 0.000 description 2
- 235000013311 vegetables Nutrition 0.000 description 2
- IDBPHNDTYPBSNI-UHFFFAOYSA-N N-(1-(2-(4-Ethyl-5-oxo-2-tetrazolin-1-yl)ethyl)-4-(methoxymethyl)-4-piperidyl)propionanilide Chemical compound C1CN(CCN2C(N(CC)N=N2)=O)CCC1(COC)N(C(=O)CC)C1=CC=CC=C1 IDBPHNDTYPBSNI-UHFFFAOYSA-N 0.000 description 1
- 239000004698 Polyethylene Substances 0.000 description 1
- 229920001328 Polyvinylidene chloride Polymers 0.000 description 1
- ZTVQQQVZCWLTDF-UHFFFAOYSA-N Remifentanil Chemical compound C1CN(CCC(=O)OC)CCC1(C(=O)OC)N(C(=O)CC)C1=CC=CC=C1 ZTVQQQVZCWLTDF-UHFFFAOYSA-N 0.000 description 1
- 229960001391 alfentanil Drugs 0.000 description 1
- 230000004907 flux Effects 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 230000000415 inactivating effect Effects 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- IMYHGORQCPYVBZ-NLFFAJNJSA-N lofentanil Chemical compound CCC(=O)N([C@@]1([C@@H](CN(CCC=2C=CC=CC=2)CC1)C)C(=O)OC)C1=CC=CC=C1 IMYHGORQCPYVBZ-NLFFAJNJSA-N 0.000 description 1
- 229950010274 lofentanil Drugs 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 239000003961 penetration enhancing agent Substances 0.000 description 1
- 229920001707 polybutylene terephthalate Polymers 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920000098 polyolefin Polymers 0.000 description 1
- 229920002635 polyurethane Polymers 0.000 description 1
- 239000004814 polyurethane Substances 0.000 description 1
- 229920002689 polyvinyl acetate Polymers 0.000 description 1
- 239000011118 polyvinyl acetate Substances 0.000 description 1
- 239000005033 polyvinylidene chloride Substances 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 229960003394 remifentanil Drugs 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000002699 waste material Substances 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
-
- 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
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/22—Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
-
- 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
-
- 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
-
- 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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Dermatology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Inorganic Chemistry (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pain & Pain Management (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Rheumatology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Hydrogenated Pyridines (AREA)
Description
DK 2005 00030 W
Krav 1. Anlæg til kontinuerlig hydrolyse af en reaktionsblanding af et proteinholdigt animalsk eller vegetabilsk råmateriale, fortrinsvis et råmateriale i form af bieller affaldsprodukter fra oparbejdning af levnedsmidler, til mindst en flydende fase (13) og mindst en fast fase (12) hvor anlægget omfatter en klargøringssektion (1), en dermed forbundet hydrolysesektion (4), en med hydrolysesektionen (4) forbundet inaktiveringssektion (7) og en med inaktiveringssektionen (7) forbundet slut-bearbejdningssektion (17), hvor hydrolysesektionen (4) er af den type, der omfatter mindst én i hovedsagen rørformet hydrolysereaktor (6) med en første fremføringssnegl (20) til at drive en reaktionsblanding af enzym og råmateriale gennem den mindst ene rørformede hydrolysereaktor (6) og videre over i inaktiveringssektionen (7), der har mindst én med hydrolysesektionen (4) forbundet inaktiveringsreaktor (8) med en indløbsende (9) og en modsat denne lokaliseret udløbsende (10), kendetegnet ved, - at den mindst ene inaktiveringsreaktor (8) udløbsende (10) har mindst et udtag (14) til den faste fase (12) og mindst et i afstand fra udtaget (14) til den faste fase (12) lokaliseret udtag (16) til den flydende fase (13), at inaktiveringsreaktoren (8) har en anden fremføringssnegl (24) til at forskyde indholdet i inaktiveringsreaktoren (8) frem mod udtaget (16), - at inaktiveringsreaktoren (8) har en ved sin bund arrangeret tredje fremføringssnegl (25) til at forskyde sedimenteret fast stof frem og ud gennem udtaget (14) for den faste fase (12), og at der ved udtaget (16) til den flydende fase (13) er arrangeret midler (15) til at blande en vandig fase med en fedtfase.
5 2 5 2 3 10 4 15 20 5 25 6 30 7 35 8
DK 2005 00030 W
Anlæg ifølge krav 1, kendetegnet ved, at mindst én af fremføringssneglene (20,24,25) er af den type, der er indrettet til at rotere med uret i et fastlagt første tidsrum, og mod uret i fastlagt andet efterfølgende tidsrum.
Anlæg ifølge ethvert af kravene 1 eller 2, kendetegnet ved, at mindst én af fremføringssneglene (20,24,25) er udformet med skovle eller plader (22) i et område ved periferien på fremføringssneglens (20,24,25) vindinger (21) .
Anlæg ifølge ethvert af kravene 1, 2 eller 3, kendetegnet ved, at udtagene (16) til den flydende fase (13) omfatter et fedtudtag til en fedtfraktion og mindst et proteinudtag, til en vandig fraktion, der indeholder bestanddele valgt fra gruppen af vandopløselige aminosyrer, peptider og/eller proteiner, vanduopløselige eller tungtopløselige aminosyrer, peptider og/eller protein, eller blandinger af disse bestanddele.
Anlæg ifølge ethvert af kravene 1-4, kendetegnet ved, at den vandige fase omfatter opløste og uopløste bestanddele af proteinoprindelse.
Anlæg ifølge krav 5, kendetegnet ved, at midlerne til at blande den vandige fase med fedtfasen er en blandepropel (15 ) eller en cirkulationspumpe.
Anlæg ifølge krav 6, kendetegnet ved, at vandopløselige og vanduopløselige bestanddele af proteinoprindelse og fedtfraktionen skilles fra hinanden i en kontinuerligt virkende dekanter eller trikanter.
Fremgangsmåde til kontinuerligt at hydrolysere en reaktionsblanding af et proteinholdigt animalsk eller
DK 2005 00030 W
vegetabilsk råmateriale til en flydende fase (13) og en fast fase (12) i et anlæg ifølge krav 1 - 7, omfattende trinnene at neddele råmaterialet, at blande råmaterialet med enzym, enzymatisk at hydrolysere råmaterialet i et fastlagt tidsrum, at inaktivere enzymer, der er tilstede i reaktionsblandingen, i en inaktiveringsreaktor (8), kontinuerligt at udtage den faste fase (12) og den flydende fase (13) fra reaktionsblandingen i inaktiveringsreaktoren (8), kendetegnet ved, at den flydende fase (13) omfatter en fedtfraktion og en vandig fraktion med et indhold af opløste og uopløste bestanddele af proteinoprindelse, at fedtfraktionen og vandfraktionen udtages fra inaktiveringsreaktoren (8) kontinuerligt enten hver for sig med ens eller forskellig hastighed eller som en samlet homogeniseret suspension.
9. Fremgangsmåde ifølge krav 8, kendetegnet ved, at de opløste og uopløste bestanddele af proteinoprindelse og fedtfasen efterfølgende separeres i en trikanter eller dekanter.
10. Fremgangsmåde ifølge krav 8 eller 9, kendetegnet ved, at fremgangmåden omfatter et indledende trin hvor metaldele udskilles fra råmaterialet.
DK 2005 00030 W
KRAV
1. Et transdermalt plaster til indgivelse af fentanyl eller en analog deraf gennem huden omfattende (a) et bagsidelag; (b) et reservoir fordelt på bagsidelaget, idet i det mindste den hudkontaktende overflade af reservoiret er selvklæbende; hvori reservoiret omfatter en enkeltfase polymersammensætning fri for uopløste bestanddele indeholdende en tilstrækkelig mængde fentanyl eller en analog deraf til at inducere og vedligeholde smertelindring hos et menneske i mindst tre dage.
2. Et plaster ifølge krav 1, som indeholder fentanyl.
3. Et plaster ifølge krav 1, som indeholder alfentanil, lofentanil, remifentanil eller sufentanil som fentanylanalog.
4. Et plaster ifølge krav 3, hvori fentanylanalogen er sufentanil.
5. Et plaster ifølge et hvilket som helst af krav 1 til 4, som er bioækvivalent til det transdermale DURAGESIC® fentanylsystem.
6. Et plaster ifølge et hvilket som helst af krav 1 til 5, hvori reservoiret er dannet af et klæbestof.
7. Et plaster ifølge krav 6, hvori reservoiret er dannet på grundlag af en klæbende polymer.
8. Et plaster ifølge krav 7, hvori den klæbende polymer er et polyacrylatklæbestof.
9. Et plaster ifølge krav 8, hvori polyacrylatklæbestoffet har et Tg mindre end -10eC.
10. Et plaster ifølge et hvilket som helst af krav 1 til 9, hvori plasteret udviser et normaliseret Cmax på 3,3 til 82,5 ng/ml-(mg/time).
11. Et plaster ifølge krav 10, hvori plasteret udviser et steady-state lægemiddelflux på 0,1 til 20 pg/cm2/time, fortrinsvis 1 til 10 pg/cm2/time.
DK 2005 00030 W
12. Et plaster ifølge et hvilket som helst af krav 1 til 11, hvori plasteret udviser et standardiseret Cmax på 0,001 til 0,2 ng/ml-cm.
13. Et plaster ifølge et hvilket som helst af krav 1 til 12, hvori reservoiret omfatter en tilstrækkelig mængde opløst fentanyl eller analog deraf til at inducere og vedligeholde smertelindring i 3-7 dage.
14. Et plaster ifølge krav 13, hvori reservoiret omfatter en polymer med en solubilitet for fentanyl eller en analog deraf på 1 vægt-% til 25 vægt-%, fortrinsvis 7 vægt-% til 12 vægt-%.
15. Et plaster ifølge krav 13 eller 14, hvori reservoiret omfatter 0,05 til 1,75 mg/cm2, fortrinsvis 0,08 til 1,25 mg/cm2, mere foretrukket 0,1 til 0,75 mg/cm2, mest foretrukket 0,12 til 0,5 mg/cm2 fentanyl eller en analog deraf.
16. Et plaster ifølge et hvilket som helst af krav 13 til 15, hvori reservoiret har en tykkelse på 0,0125 mm (0,5 mil) til 0,1 mm (4 mil).
17. Et plaster ifølge et hvilket som helst af krav 1 til 16, hvori reservoiret yderligere omfatter et permeationsforøgende middel.
18. Et plaster ifølge et hvilket som helst af krav 1 til 17, hvori bagsidelaget omfatter et polyurethan, polyvinylacetat, polyvinylidenchlorid, polyethylen, polyethylenterephthalat (PET), PET-polyolefinlaminat eller en polybutylenterephthalatpolymer.
19. Et plaster ifølge krav 18, hvori bagsidelaget omfatter et lav densitet polyethylen (LDPE) materiale, et middel densitet polyethylen (MDPE) materiale elleret høj densitet polyethylen (HDPE) materiale.
20. Et plaster ifølge krav 19, hvori bagsidelaget omfatter et lav densitet polyethylen (LDPE) materiale.
21. Et plaster ifølge et hvilket som helst af krav 18 til 20, hvori bagsidelaget har en tykkelse på 0,012 mm (0,5 mil) til 0,125 mm (5 mil).
22. Et transdermalt plaster ifølge et hvilket som helst af krav 1 til 21 til indgivelse af fentanyl omfattende et selvklæbende fentanylreservoir på et bagsidelag; idet reservoiret omfatter en enkeltfase polymersammensætning fri for uopløste bestanddele indeholdende et polyacrylatklæbestof med tilstrækkelig solubilitet for fentanyl til at indeholde opløst fentanyl i en tilstrækkelig mængde til at inducere og vedligeholde smer-
DK 2005 00030 W
telindring hos et menneske i mindst tre dage, idet plasteret udviser et normaliseret
Cmax på 3,3 til 82,5 ng/ml-{mg/time).
23. Et transdermalt plaster ifølge et hvilket som helst af krav 1 til 22 til indgivelse af fentanyl omfattende et selvklæbende fentanylreservoir på et bagsidelag; idet reservoiret omfatter en enkeltfase polymersammensætning fri for uopløste bestanddele indeholdende et polyacrylatklæbestof med tilstrækkelig solubilitet for fentanyl til at indeholde opløst fentanyl i en tilstrækkelig mængde til at inducere og vedligeholde smertelindring hos et menneske i mindst tre dage, idet plasteret udviser et standardiseret Cma)( på 0,01 til 0,2 ng/ml-cm2.
24. Et transdermalt plaster ifølge et hvilket som helst af krav 1 til 22 til indgivelse af sufentanil omfattende et selvklæbende fentanylreservoir på et bagsidelag; idet reservoiret omfatter en enkeltfase polymersammensætning fri for uopløste bestanddele indeholdende et polyacrylatklæbestof med tilstrækkelig solubilitet for sufentanil til at indeholde opløst sufentanil i en tilstrækkelig mængde til at inducere og vedligeholde smertelindring hos et menneske i mindst tre dage, idet plasteret udviser et normaliseret Cmax på fra 0,04 til 10 ng/ml-(mg/time).
25. Et transdermalt plaster ifølge et hvilket som helst af krav 1 til 22 til indgivelse af sufentanil omfattende et selvklæbende fentanylreservoir på et bagsidelag; idet reservoiret omfatter en enkeltfase polymersammensætning fri for uopløste bestanddele indeholdende et polyacrylatklæbestof med tilstrækkelig solubilitet for sufentanil til at indeholde opløst sufentanil i en tilstrækkelig mængde til at inducere og vedligeholde smertelindring hos et menneske i mindst tre dage, idet plasteret udviser et standardiseret Cmax på fra 0,001 til 0,05 ng/ml-cm2.
26. Et plaster ifølge et hvilket som helst af krav 1 til 25, som er fuldstændig fri for en hastighedsregulerende membran.
DK 2005 00030 W
FIG. 2
DK 2005 00030 W
O N. II 2: <N Φ ' 11 "ΪΧ io. to^ s: ..α to co CL- i LU11 £qφ Φ o c; C S, ctj ctf ra C C g^ Æ § =3 =3 uz co co _p -^P v^p θ'- θ'- o'' CO O) Co '5 '5 ’£ S -G -S c: c; c: •s ^ « co co co v^p o * θ'- o'- CO 'sr 03 Φ φ <jl· φ Φ Φ
co
(QLUjj/zUJQ/Bri) xny . 24_.:_ J6_______48_ Middel-Tider (Timer) FIG. 4 " (euji)/zLUD/6rl) xny
DK 2005 00030 W
C3 lC (dLU!i/zUJD/6r1) xny
Vægt % Lægemiddel φω!ΐ/ζωο/6ί1) xn/j>
DK 2005 00030 W
DURAGESIC® Plaster (100 '/tlme)^40.cm Fentanyl Plaster 20 cm2 Fentanyl Plaster 40 cm2
/uj/I5u uoi)ej)udouo}i turnes
DK 2005 00030 W
DURAGESIC® 100 pg/time Fentanyl Plaster 100 pg/time (n=31) -
Tid (Timer)
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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US27683701P | 2001-03-16 | 2001-03-16 |
Publications (3)
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DK200500030U1 DK200500030U1 (da) | 2005-05-13 |
DK200500030U3 true DK200500030U3 (da) | 2005-07-22 |
DK200500030Y4 DK200500030Y4 (da) | 2006-07-28 |
Family
ID=23058257
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Application Number | Title | Priority Date | Filing Date |
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DK02715112T DK1381352T3 (da) | 2001-03-16 | 2002-03-15 | Plaster til transdermal indgivelse af fentanyl |
DK200500030U DK200500030Y4 (da) | 2001-03-16 | 2005-01-25 | Transdermalt plaster til indgivelse af fentanyl |
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Application Number | Title | Priority Date | Filing Date |
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DK02715112T DK1381352T3 (da) | 2001-03-16 | 2002-03-15 | Plaster til transdermal indgivelse af fentanyl |
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US (11) | US20030026829A1 (da) |
EP (1) | EP1381352B1 (da) |
JP (7) | JP5354763B2 (da) |
KR (1) | KR100904158B1 (da) |
CN (2) | CN101524339A (da) |
AT (4) | ATE364380T1 (da) |
CA (1) | CA2440884C (da) |
CY (1) | CY1106834T1 (da) |
CZ (1) | CZ307857B6 (da) |
DE (3) | DE02715112T1 (da) |
DK (2) | DK1381352T3 (da) |
ES (1) | ES2270746T3 (da) |
FI (2) | FI6962U1 (da) |
HK (1) | HK1068545A1 (da) |
IL (3) | IL157822A0 (da) |
MX (1) | MXPA03008349A (da) |
NZ (1) | NZ528148A (da) |
PL (1) | PL363079A1 (da) |
PT (1) | PT1381352E (da) |
RU (2) | RU2708563C2 (da) |
WO (1) | WO2002074286A1 (da) |
ZA (1) | ZA200308026B (da) |
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