Transdermal therapeutic system comprising galanthamine as active

Details Transdermal therapeutic system comprising galanthamine as active Transdermal therapeutic system comprising galanthamine as active

1995-09-29

1997-12-23

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Web, sheet or filament bases; compositions of bandages; or...

424449, A61F 1302, A61L 1516, A61K 914

Patent

active

057004803

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to a transdermal therapeutic system (TTS) which comprises as active component galanthamine (4a,5,9,10,11,12-hexahydro-3-methoxy-11-methyl-6H-benzofuro (3a,3,2-ef) (2) benzazepin-6-ol).


BACKGROUND OF THE INVENTION

Owing to its pharmacological properties galanthamine belongs to the group of reversibly acting cholinesterase inhibitors. The effects are similar to those of physostigmine and neostigmine, however, it has specific properties. The therapeutic range of galanthamine is three to six times broader since it is not as toxic as physostigmine or neostigmine.
This advantage compensates for the slightly lower cholinesterase inhibiting-action, relative to the dosage.
The major fields of application of galanthamine are the treatment of the narrow-angle glaucoma and the use as antidote after curare applications. The use of galanthamine in the treatment of the Alzheimer's disease is in an experimental stage.
Lately, galanthamine has been used in the treatment of alcohol dependence (Opitz, K., DE 40 10 079).
Both the therapy of the Alzheimer's disease and that of alcohol dependence require long-acting drug forms taking into account the particular circumstances of the respective disease. Complicated therapeutic plans or prolonged infusions are unsuitable for obvious reasons.
On the contrary, a TTS is the drug form of choice; nevertheless, until today, it has not been possible to succeed in bringing the necessary amount of galanthamine to absorption transdermally.


DESCRIPTION OF THE INVENTION

Accordingly, it is the object of the present invention to provide galanthamine or one of its pharmaceutically acceptable salts in the form of a transdermal therapeutic system which releases galanthamine or its pharmaceutically acceptable salt over a period of at least 24 hours in a controlled manner and ensures that the galanthamine does not noticeably decompose during storage of the prefabricated transdermal therapeutic system and makes sure that the galanthamine penetrates through human skin to the required extent in vivo.
With the present invention this object is achieved in a surprising manner by a transdermal therapeutic system.
This solution is remarkable all the more since the structure of galanthamine is very similar to that of the opiates. Optiates are considered to be a substance class which only insufficiently penetrates human skin.
Without the intention to limit the present invention, the hydrobromide and hydrochloride of galanthamine are to be understood as the preferred pharmaceutically acceptable salts of galanthamine.
Advantageous embodiments of the present invention are further described.
The backing layer which is impermeable to active substances may consist of flexible and inflexible material. Substances suitable for the production include polymer films or foils, such as an aluminum foil, which may be used alone or coated with a polymeric substrate. Textile fabrics may also be used, provided that the components of the reservoir owing to their physical nature may not pass through. According to a preferred embodiment the backing layer is a composite of an aluminized sheet.
The reservoir layer consists of a polymer matrix and the active substance, with the polymer matrix ensuring the cohesion of the system. The polymer matrix consists of a base polymer and, optionally, conventional additives. The choice of the base polymer depends on the chemical and physical properties of the galanthamine. Examples of such polymers include rubber, rubber-like synthetic homopolymers, copolymers or block polymers, polyacrylates and the copolymers thereof, polyurethanes and silicones. In principle, all polymers are suitable which may be used in the production of pressure sensitive adhesives and which are physiologically acceptable. Particularly preferred ones are those consisting of block copolymers based on styrene and 1,3-dienes, polyisobutylenes, silicones and polymers based on acrylate and/or methacrylate.
Among the block copolymers based on styrene and 1,3-dienes, linear styrene-isoprene o

REFERENCES:
patent: 4663318 (1987-05-01), Davis
patent: 5089267 (1992-02-01), Hille et al.

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