Device for the transdermal administration of a rotigotine base
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/381
A61K-009/70
출원번호
US-0020414
(2011-02-03)
등록번호
US-8545872
(2013-10-01)
우선권정보
DE-102 61 696 (2002-12-30)
발명자
/ 주소
Breitenbach, Armin
출원인 / 주소
UCB Pharma GmbH
대리인 / 주소
Harness, Dickey & Pierce, P.L.C.
인용정보
피인용 횟수 :
3인용 특허 :
56
초록▼
The invention relates to a polymer matrix suitable for the transdermal administration of rotigotine (−)-5, 6, 7, 8-tetrahydro-6-propyl2-(2-thienyl)ethylamino-1-naphtol, containing a matrix for the transdermal administration of rotigotine (−)-5, 6, 7, 8-tetrahydro-6-propyl2-(2-thienyl)ethylamino-1 na
The invention relates to a polymer matrix suitable for the transdermal administration of rotigotine (−)-5, 6, 7, 8-tetrahydro-6-propyl2-(2-thienyl)ethylamino-1-naphtol, containing a matrix for the transdermal administration of rotigotine (−)-5, 6, 7, 8-tetrahydro-6-propyl2-(2-thienyl)ethylamino-1 naphtol, containing a matrix polymer which is supersaturated with a rotigotine base. Said polymer matrix is characterised in that the part of the rotigotine which is not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles having a maximum mean diameter of 30 μm, and the matrix is free of solubilisers, crystallisation inhibitors and dispersants. The invention also relates to a flat device for the transdermal administration of rotigotine, containing the above-mentioned, preferably silicon-based polymer matrix which is supersaturated with rotigotine, and a rear layer which is impermeable to the active ingredient.
대표청구항▼
1. A matrix for transdermal administration of rotigotine that is storage-stable for at least 6 months, the matrix comprising (a) a matrix polymer, and(b) rotigotine base in a concentration above the solubility limit of rotigotine base in the matrix polymer,wherein a portion of the rotigotine base no
1. A matrix for transdermal administration of rotigotine that is storage-stable for at least 6 months, the matrix comprising (a) a matrix polymer, and(b) rotigotine base in a concentration above the solubility limit of rotigotine base in the matrix polymer,wherein a portion of the rotigotine base not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles with a maximum mean diameter of 30 μm, and wherein the matrix is free of solubilizer, crystallization inhibitor and dispersant. 2. A matrix for transdermal administration of rotigotine that is storage-stable for at least 6 months, the matrix consisting of: (a) matrix polymer that is an amine-resistant silicone or a mixture of amine-resistant silicones,(b) rotigotine base in a concentration above the solubility limit of rotigotine base in the matrix polymer, wherein a portion of the rotigotine base not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles with a maximum mean diameter of 30 μm, and(c) optionally one or more antioxidants. 3. The matrix of claim 1, wherein the matrix polymer is an amine-resistant silicone or a mixture of amine-resistant silicones. 4. The matrix of claim 1 or 2 wherein the matrix is self-adhesive. 5. The matrix of claim 1 or 2 wherein the matrix consists of: (a) about 60 to about 95 weight percent of an amine-resistant silicone or an amine-resistant silicone mixture,(b) about 5 to about 40 weight percent amorphous rotigotine base dispersed in the silicone, and(c) zero to about 2 weight percent antioxidant. 6. A system for transdermal administration of rotigotine comprising a matrix of claim 1 or 2 and a backing. 7. The system of claim 6 wherein the backing is impermeable to rotigotine. 8. The system of claim 6 wherein the rotigotine is present in an amount of 0.3 to 6 mg/cm2. 9. The system of claim 6, wherein the rotigotine base is present in an amount permitting a flow rate of rotigotine through human skin that is therapeutically effective, upon application of the system at intervals of 1 to 7 days, for treatment of Morbus Parkinson. 10. The system of claim 6, wherein the rotigotine base is present in an amount permitting a flow rate of rotigotine through human skin that is therapeutically effective, upon application of the system at intervals of 1 to 7 days, for treatment of restless leg syndrome. 11. The system of claim 6, wherein the rotigotine base is present in an amount permitting a flow rate of rotigotine through human skin that is therapeutically effective, upon application of the system at intervals of 1 to 7 days, for treatment of depression.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (56)
Jaeger Halvor (Neu-Ulm DEX) Hoffmann Hans-Rainer (Neuwied DEX) Meconi Reinhold (Neuwied DEX) Klein Robert-Peter (Neuwied DEX), Apparatus for the delivery of substances, processes for the production thereof and use thereof.
Thomas E. Conn ; Russell Ford ; Pravin L. Soni ; Michael J. Tierney ; Prema Vijayakumar, Collection assemblies, laminates, and autosensor assemblies for use in transdermal sampling systems.
Gueret Jean-Louis H.,FRX, Cosmetic or dermopharmaceutical patch containing, in an anhydrous polymeric matrix, at least one active compound which is, in particular, unstable in oxidizing mediums, and at least one water-absorbi.
Michael J. Butler ; Thomas E. Conn ; David M. Liu ; Norman A. Parris ; Michael Reidy ; Pravin L. Soni, Device and methods for the application of mechanical force to a gel/sensor assembly.
Wong Ooi (Fremont CA) Nguyen Thuytien N. (Hayward CA), Enhancement of transdermal drug delivery using monoalkyl phosphates and other absorption promoters.
Hoffmann Hans-Rainer (Neuwied DEX) Klein Robert P. (Neuwied DEX) Meconi Reinhold (Neuwied DEX) Cordes Gunter (Leichingen DEX) Wolff Hans M. (Monheim DEX), Estrogen-containing active substance plaster.
Roreger Michael (Neuwied DEX) Herrmann Fritz (Neuwied DEX) Hoffmann Hans-Rainer (Neuwied DEX) List Harald (Neuwied DEX), Flexible, hydrophilic gel film, the process for its production and the use of it.
Rimpler,Stephan; Grapatin,Sabine; Krein,Cliff; Thelen,Markus, Injectable pharmaceutical composition for systematic administration of pharmacologically active ingredients.
Roos Eric J. (Marlborough MA) Chiang Chia-Ming (Foster City CA) Hsu Tsung-Min (Taipei TWX), Low flux matrix system for delivering potent drugs transdermally.
Colley Kenneth J. (San Francisco CA) Wilson Donald R. (San Francisco CA) Cleary Gary W. (San Mateo CA) Lammintausta Risto (Turku FIX) Jalonen Harry (Turku FIX), Method and device for administering dexmedetomidine transdermally.
Maignan Jean (Tremblay les Gonesse FRX) Malle Grard (Villiers sur Morin FRX) Deflandre Andr (Orry-La-Ville FRX) Lang Grard (Saint Gratien FRX), New derivatives of 5,6,7,8-tetrahydro-1-naphthalenol, a process for their preparation and cosmetic and pharmaceutical co.
Patel Dinesh C. (Murray UT) Chang Yunik (Lakewood NJ), Penetration enhancement with binary system of oleic acid, oleins, and oleyl alcohol with lower alcohols.
Chen Tung-Fen ; Chiang Chia-Ming ; Jona Janan ; Joshi Priti ; Ramdas Asha, Polyurethane hydrogel drug reservoirs for use in transdermal drug delivery systems, and associated methods of manufactu.
Sylvia Rossi-Montero ; Juan Mantelle ; David Kanios ; David Houze, Solubility enhancement of drugs in transdermal drug delivery systems and methods of use.
Fallon Renee A. (Sunnyvale CA) Venkatraman Subbu S. (Palo Alto CA) Cleary Gary W. (San Mateo CA), Transdermal drug delivery device using a membrane-protected microporous membrane to achieve delayed onset.
Venktrama Subbu S. (Palo Alto CA) Fallon Renee A. (Sunnyvale CA) Cleary Gary W. (San Mateo CA), Transdermal drug delivery device using a polymer-filled microporous membrane to achieve delayed onset.
Chiang Chia-Ming (Foster City CA) Colley Kenneth J. (Washington DC) Cleary Gary W. (San Mateo CA), Transdermal drug delivery device using an unfilled microporous membrane to achieve delayed onset.
Ma Xinghang ; Audett Jay ; Soni Pravin L. ; Singh Noel ; Bailey Susan E., Transdermal drug delivery sytem for the administration of tamsulosin, and related compositions and methods of use.
Jona Janan ; Audett Jay ; Singh Noel, Transdermal patch and method for administering 17-deacetyl norgestimate alone or in combination with an estrogen.
Muller, Walter; Peck, James V., Transdermal therapeutic system which contains a d2 agonist and which is provided for treating parkinsonism, and a method for the production thereof.
Quan Danyi (Salt Lake City UT) Deshpanday Ninad A. (Salt Lake City UT) Venkateshwaran Srinivasan (Salt Lake City UT) Ebert Charles D. (Salt Lake City UT), Triacetin as a penetration enhancer for transdermal delivery of a basic drug.
Quan Danyi ; Deshpanday Ninad A. ; Venkateshwaran Srinivasan ; Ebert Charles D., Triacetin as a penetration enhancer for transdermal delivery of a basic drug.
Bouwstra, Johanna Aaltje; Ackaert, Oliver; Eikelenboom, Jacob; Wolff, Hans-Michael, Pharmaceutical composition comprising rotigotine salts (acid or Na), especially for iontophoresis.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.