DE102004059674A1 - Transdermal delivery system to treat movement disease and post-operative illness comprises scopolamine and a matrix comprising styrene-butadiene-copolymer-bonding adhesive - Google Patents
Transdermal delivery system to treat movement disease and post-operative illness comprises scopolamine and a matrix comprising styrene-butadiene-copolymer-bonding adhesive Download PDFInfo
- Publication number
- DE102004059674A1 DE102004059674A1 DE102004059674A DE102004059674A DE102004059674A1 DE 102004059674 A1 DE102004059674 A1 DE 102004059674A1 DE 102004059674 A DE102004059674 A DE 102004059674A DE 102004059674 A DE102004059674 A DE 102004059674A DE 102004059674 A1 DE102004059674 A1 DE 102004059674A1
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- Germany
- Prior art keywords
- delivery system
- transdermal delivery
- matrix
- scopolamine
- styrene
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- 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
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Bereits
auf dem Markt befindliche Scopolamin-TDS, wie z.B. Transderm Scop®,
weisen relativ komplizierte Zusammensetzungen auf. US-Patent 4,031,894
[2] beschreibt ein Pflaster mit vier unterschiedlichen Schichten,
eine Trägerfolie,
eine gelierte Mineralöl-Polyisobuten-Scopolamin
Reservoirschicht, eine mikroporöse
Membran und schließlich eine
gelierte Mineralöl-Polyisobutan-Scopolamin
Klebeschicht. Wie in den folgenden Patenten
Transderm Scop®, wie in US-Patent 4,904,475 [6] beschrieben, besteht aus 4 Schichten, einer Trägerfolie, einem Arzneimittelreservoir, einer die Geschwindigkeit kontrollierenden Membran und einem Kontaktkleber. Dies ist ein verhältnismäßig komplizierter Aufbau und deshalb werden die Herstellungskosten deutlich höher sein, da der Herstellungsprozess komplexer sein wird und länger zur Fertigstellung braucht. Ein weiterer Nachteil des Transderm Scop® TDS ist der kalte Fluss, der zur Verunreinigung der Kleidung oder Hände mit der "toxischen" Substanz während des Anbringens und/oder Tragens des TDS führt.Transderm Scop described ®, as described in U.S. Patent 4,904,475 [6], consists of 4 layers, a backing film, a drug reservoir, a rate controlling membrane and a contact adhesive. This is a relatively complicated construction and therefore the manufacturing cost will be significantly higher as the manufacturing process will be more complex and take longer to complete. Another disadvantage of the Transderm Scop ® TDS is the cold flow, which leads to contamination of clothing or hands with the "toxic" substance during the attachment and / or wearing of the TDS.
Die Erfindung betrifft ein transdermales Abgabesystem, umfassend Scopolamin als Wirkstoff und eine Matrix, umfassend einen Styrol-Butadien-Copolymer Haftkleber.The The invention relates to a transdermal delivery system comprising scopolamine as an active ingredient and a matrix comprising a styrene-butadiene copolymer Pressure sensitive adhesive.
Die Matrix des transdermalen Abgabesystems kann einen Styrol-Butadien-Styrol-Blockcopolymer Haftkleber umfassen.The Matrix of the transdermal delivery system may be a styrene-butadiene-styrene block copolymer Include pressure-sensitive adhesive.
Des Weiteren kann das transdermale Abgabesystem eine Trägerfolie, die Matrix und eine Schutzdecklage umfassen und keine die Geschwindigkeit kontrollierende Membran.Of Furthermore, the transdermal delivery system may include a carrier foil, the matrix and a protective cover layer and not the speed controlling membrane.
Des Weiteren kann das transdermale Abgabesystem eine Trägerfolie, die Matrix und eine Schutdecklage und eine die Geschwindigkeit kontrollierende Membran umfassen.Of Furthermore, the transdermal delivery system may include a carrier foil, the matrix and a protective layer and a speed controlling Membrane include.
Des Weiteren kann die Matrix des transdermalen Abgabesystems einen Permeationsförderer umfassen, vorzugsweise einen Permeationsförderer ausgewählt aus der Gruppe, bestehend aus
- – Ethanol,
- – Aloe Vera,
- – Labrafil,
- – Cremophor,
- – Polyethylenglycol und dessen Derivate,
- – Löslichmacher Gamma,
- – Glycerol,
- – Stearin,
- – Tocopherol (Vitamin E),
- – Macrogol,
- – Oleyloleat,
- – Pluronic,
- – Polyoxyethylensorbitanester,
- – Cholsäureester,
- – Benzalkoniumchlorid,
- – Capryl/Caprin-Triglyceride,
- – Dodecanol,
- – Natriumstearat,
- – Myristylmyristinsäureester,
- – Linolensäure,
- – Mineralöl,
- – Crovol,
- – Carbopol,
- – Controx,
- – Olivenöl,
- – Texapon,
- – Cetiol,
- – Labrasol,
- – Octyldodecyllactat,
- – Softcutol und
- – Tween
- Ethanol,
- - aloe vera,
- - Labrafil,
- - Cremophor,
- Polyethylene glycol and its derivatives,
- Solubilizer gamma,
- - glycerol,
- - stearin,
- - tocopherol (vitamin E),
- - Macrogol,
- Oleyl oleate,
- - Pluronic,
- - polyoxyethylene sorbitan ester,
- - cholic acid ester,
- - benzalkonium chloride,
- Caprylic / capric triglycerides,
- - dodecanol,
- Sodium stearate,
- Myristyl myristic acid ester,
- - linolenic acid,
- - mineral oil,
- - Crovol,
- - Carbopol,
- - Controx,
- - olive oil,
- - Texapon,
- - Cetiol,
- - Labrasol,
- Octyldodecyl lactate,
- - Softcutol and
- - Tween
Des Weiteren kann, was das transdermale Abgabesystem betrifft, der Scopolamingehalt 5 bis 15 und insbesondere etwa 10 Gew.% sein, basierend auf der Matrix.Of Further, as far as the transdermal delivery system is concerned, the level of scopolamine may be 5 to 15 and especially about 10 wt.% Be based on the Matrix.
Des Weiteren kann, was das transdermale Abgabesystem betrifft, der Scopolamingehalt einer Abgabe von 500 μg bis 2 mg und insbesondere etwa 1 mg über mindestens bis zu 72 h entsprechen.Of Further, as far as the transdermal delivery system is concerned, the level of scopolamine may be a delivery of 500 μg to 2 mg and especially about 1 mg for at least up to 72 h correspond.
Des Weiteren kann, was das transdermale Abgabesystem betrifft, der Scopolamingehalt einer Abgabe entsprechen, die einem Blutspiegel von etwa 87 pg/ml über mindestens bis zu 72 h entspricht.Of Further, as far as the transdermal delivery system is concerned, the level of scopolamine may be corresponding to a blood level of about 87 pg / ml over at least up to 72 h.
Des Weiteren kann das transdermale Abgabesystem ein kreisförmiges, ovales, rechteckiges oder quadratisches Matrixpflaster sein.Of Further, the transdermal delivery system may be a circular, oval, rectangular or square matrix plaster.
Des Weiteren kann das transdermale Abgabesystem eine Größe von 1,0 bis 3,0 und insbesondere 1,5 bis 2,5 cm2 haben.Furthermore, the transdermal delivery system may have a size of 1.0 to 3.0 and in particular 1.5 to 2.5 cm 2 .
Des Weiteren kann, was das transdermale Abgabesystem betrifft, die Matrix ein Flächengewicht von 40 bis 140, vorzugsweise 80 bis 100, und insbesondere etwa 90 g/m2 haben.Furthermore, as far as the transdermal delivery system is concerned, the matrix may have a basis weight of 40 to 140, preferably 80 to 100, and most preferably about 90 g / m 2 .
Das erfindungsgemäße transdermale Abgabesystem kann für die Behandlung von Bewegungskrankheit bereitgestellt werden.The Transdermal according to the invention Dispensing system can for the treatment of motion sickness will be provided.
Schließlich kann das erfindungsgemäße transdermale Abgabesystem für die Behandlung von postoperativer Übelkeit bereitgestellt werden.Finally, can the transdermal invention Delivery system for the treatment of postoperative nausea will be provided.
Überraschend
wurde festgestellt, dass ein linearer Fluss mit den benötigten Spiegeln über 72 Stunden
mit a) einem weitaus geringeren Matrixgewicht und b) sogar ohne
die Verwendung einer die Geschwindigkeit kontrollierenden Membran
erreicht werden konnte. Der Fluss von Scopolamin aus dem hierin
beschriebenen Scopolamin-TDS wurde festgestellt, ähnlich zu
dem aus Transderm Scop® zu sein (Verweis auf
Ein transdermales Abgabesystem (TDS) für Scopolamin wurde für die Behandlung von Bewegungskrankheit entwickelt. Das Abgabeziel für Scopolamin ist annähernd 1 mg über 72 Stunden, um Blutspiegel von annähernd 87 pg/ml zu ergeben.One transdermal delivery system (TDS) for scopolamine was used for the treatment developed from motion sickness. The delivery target for scopolamine is approximate 1 mg over 72 hours to give blood levels of approximately 87 pg / ml.
Das
Scopolamin-TDS besteht aus einem kreisförmigen Matrixpflaster mit einer
Fläche
von 1,5 bis 2,5 cm2 und einem Flächengewicht
von etwa 90 g/m2, die Aktivmatrix enthält einen
Styrol-Butadien-Styrol-Copolymer Haftkleber (PSA) (DT-6173) mit 10
% Scopolamin. Verweis auf
- 1. Fachinformation, Scopoderm TTS®, Novartis Consumer Health GmbH, 2003.
- 2. J. E. Shaw, J. Urquhart & S. K. Chandrasekaran: Verband zur transdermalen Verabreichung von Scopolamin, um Übelkeit zu verhindern, US-Patent 4,031,894.
- 3. J. W. Dohner & S. A. Bura: Verbessertes Verfahren zur Verhinderung der Kristallbildung in einer Dispersion einer Flüssigkeit in einer Matrix, EP-Patent 0 863 751.
- 4. J. W. Dohner, S. A. Bura & R. E. Ford: Verfahren zur Verhinderung der Kristallbildung in einer Dispersion einer Flüssigkeit in einer Matrix, US-Patent 6,238,700, 1998 5. J. W. Dohner, S.A. Bura & R. E. Ford: Verfahren zur Verhinderung der Kristallbildung in einer Dispersion einer Flüssigkeit in einer Matrix, US-Patent 6,569,448.
- 6. R. M. Gale & D. J. Enscore: Transdermale Abgabe aus einem wässrigen Reservoir, US-Patent 4,904,475.
- 1. prescribing information, Scopoderm TTS ®, Novartis Consumer Health GmbH., 2003
- 2. JE Shaw, J. Urquhart & SK Chandrasekaran: Association for transdermal administration of scopolamine to prevent nausea, U.S. Patent 4,031,894.
- 3. JW Dohner & SA Bura: Improved method of preventing crystal formation in a dispersion of a liquid in a matrix, EP patent 0 863 751.
- 4. JW Dohner, SA Bura & RE Ford: Method for Preventing Crystal Formation in a Dispersion of a Liquid in a Matrix, US Pat. No. 6,238,700, 1998. 5. JW Dohner, SA Bura & RE Ford: Method of Preventing Crystal Formation in a Dispersion a liquid in a matrix, U.S. Patent 6,569,448.
- 6. RM Gale & DJ Enscore: Transdermal Delivery from an Aqueous Reservoir, U.S. Patent 4,904,475.
Claims (13)
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102004059674A DE102004059674B4 (en) | 2004-12-10 | 2004-12-10 | Transdermal delivery system for scopolamine |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE102004059674A DE102004059674B4 (en) | 2004-12-10 | 2004-12-10 | Transdermal delivery system for scopolamine |
Publications (2)
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DE102004059674A1 true DE102004059674A1 (en) | 2006-06-14 |
DE102004059674B4 DE102004059674B4 (en) | 2010-05-06 |
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DE102004059674A Active DE102004059674B4 (en) | 2004-12-10 | 2004-12-10 | Transdermal delivery system for scopolamine |
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2667861A2 (en) * | 2011-01-26 | 2013-12-04 | CSI GmbH | Extended-release beta agonist/anticholinergic transdermal patches and methods for using the same |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE102018118507A1 (en) | 2018-07-31 | 2020-02-06 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system for the delivery of scopolamine without a membrane |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4904475A (en) * | 1985-05-03 | 1990-02-27 | Alza Corporation | Transdermal delivery of drugs from an aqueous reservoir |
EP0356382A2 (en) * | 1988-08-02 | 1990-02-28 | Ciba-Geigy Ag | Multilayer plaster |
DE3910543A1 (en) * | 1989-04-01 | 1990-10-11 | Lohmann Therapie Syst Lts | TRANSDERMAL THERAPEUTIC SYSTEM WITH INCREASED ACTIVE FLUID AND METHOD FOR THE PRODUCTION THEREOF |
DE19825499A1 (en) * | 1998-06-08 | 1999-12-09 | Beiersdorf Ag | Patches containing active ingredient |
US20010006628A1 (en) * | 1997-06-26 | 2001-07-05 | Govil Sharad K. | Adhesive mixture for transdermal delivery of highly plasticizing drugs |
DE69622780T2 (en) * | 1995-04-28 | 2003-04-03 | Lead Chem Co Ltd | Transdermal therapeutic system with controlled drug release |
WO2004098472A1 (en) * | 2002-08-30 | 2004-11-18 | Watson Pharmaceuticals, Inc. | Transdermal delivery systems and methods |
Family Cites Families (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU5325000A (en) * | 1999-06-05 | 2000-12-28 | David Houze | Solubility enhancement of drugs in transdermal drug delivery systems and methodsof use |
-
2004
- 2004-12-10 DE DE102004059674A patent/DE102004059674B4/en active Active
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4904475A (en) * | 1985-05-03 | 1990-02-27 | Alza Corporation | Transdermal delivery of drugs from an aqueous reservoir |
EP0356382A2 (en) * | 1988-08-02 | 1990-02-28 | Ciba-Geigy Ag | Multilayer plaster |
DE3910543A1 (en) * | 1989-04-01 | 1990-10-11 | Lohmann Therapie Syst Lts | TRANSDERMAL THERAPEUTIC SYSTEM WITH INCREASED ACTIVE FLUID AND METHOD FOR THE PRODUCTION THEREOF |
DE69622780T2 (en) * | 1995-04-28 | 2003-04-03 | Lead Chem Co Ltd | Transdermal therapeutic system with controlled drug release |
US20010006628A1 (en) * | 1997-06-26 | 2001-07-05 | Govil Sharad K. | Adhesive mixture for transdermal delivery of highly plasticizing drugs |
DE19825499A1 (en) * | 1998-06-08 | 1999-12-09 | Beiersdorf Ag | Patches containing active ingredient |
WO2004098472A1 (en) * | 2002-08-30 | 2004-11-18 | Watson Pharmaceuticals, Inc. | Transdermal delivery systems and methods |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP2667861A2 (en) * | 2011-01-26 | 2013-12-04 | CSI GmbH | Extended-release beta agonist/anticholinergic transdermal patches and methods for using the same |
EP2667861A4 (en) * | 2011-01-26 | 2014-07-16 | Csi Gmbh | Extended-release beta agonist/anticholinergic transdermal patches and methods for using the same |
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DE102004059674B4 (en) | 2010-05-06 |
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Legal Events
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OP8 | Request for examination as to paragraph 44 patent law | ||
8127 | New person/name/address of the applicant |
Owner name: ACINO AG, 83714 MIESBACH, DE |
|
8181 | Inventor (new situation) |
Inventor name: MCLEOD, SARAH, 81675 MUENCHEN, DE Inventor name: MEYER, ELISABETH, 83714 MIESBACH, DE |
|
8364 | No opposition during term of opposition | ||
R081 | Change of applicant/patentee |
Owner name: LUYE PHARMA AG, DE Free format text: FORMER OWNER: ACINO AG, 83714 MIESBACH, DE |
|
R082 | Change of representative |
Representative=s name: BEETZ & PARTNER MBB PATENTANWAELTE, DE Representative=s name: BEETZ & PARTNER MBB PATENT- UND RECHTSANWAELTE, DE |