Transdermal therapeutic system comprising active substances repr

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...

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424449, 514822, 514885, A61F 1302

Patent

active

058826742

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/EP95/02119, filed Jun. 03, 1995.


BACKGROUND OF THE INVENTION

The present invention relates to a transdermal therapeutic system (TTS) for the systemic and topical administration of active substances which are suitable to increase the carbon monoxide (CO) concentration in the organism.
Many research works carried out quite recently have shown that CO is of very great importance as a mediator in both physiological and physiopathological processes in the body. This part of CO comprises the regulation of the arterial tone of the vessels, the blood platelet aggregation, the influence on immunological and inflammatory processes, and the function as a messenger substance in the transmission of impulses of the central and peripheral nervous system. CO is also included in physiopathological changes of these functional structures or organ systems; for example, hypertension, coronary stenoses, arteriosclerosis. Moreover, there are indications as to a participation in immunological and inflammatory reactions and to an influence on cell growth.
In addition to the vasodilative and antithrombotic action, CO is said to have the function of a neurotransmitter in the central and peripheral nervous system. The important role as an intercellular and intracellular mediator is rendered possible by the rapid diffusion through cell membranes.
Owing to this finding there is the demand of being able to supply the active substance CO to the organism in a controllable manner without provoking the risk of an intoxication by accumulation to the hemoglobin. The way via the respiratory air, which normally comprises more or less CO, is ruled out because an exact and, in particular, reproducible dosage is difficult to manage. Other parenteral or eternal methods of administration are not known.


BRIEF SUMMARY OF THE INVENTION

It is accordingly the object of the present invention to provide a transdermal therapeutic administration system for active substances which supply human or animal organisms with CO in a specific and reproducible active substance dosage.
This object is achieved by the fact that active substances are administered to an organism through the skin or mucosa by means of a transdermal therapeutic system, and that at least one of the active substances is selected from compounds releasing carbon monoxide (CO) in organisms.


DETAILED DESCRIPTION OF THE INVENTION

A therapeutic system is a drug-containing device or form of administration which continuously releases one or several drugs at a predetermined rate over a definite period of time to a definite site of application (HEILMANN "Therapeutische Systeme", F. Enke Verlag Stuttgart, 1982, p. 26). Therapeutic systems can be used for both topical and systemic applications, and accordingly they have different conceptions.
Among other things, a transdermal therapeutic system according to the present invention is characterized by the following advantages: pharmacologically active form, avoiding metabolism in the gastrointestinal tract. administration routes. pharmacodynamic phase. control.
There are many possibilities of realizing a TTS comprising the active substance(s) according to the present invention; for example, pressure-sensitive adhesive patches, films, sprays, creams, ointments, and the like. The administration form of a pressure-sensitive adhesive patch is particularly preferable. In general, it consists of an impermeable backing layer; an active substance reservoir connected therewith and having a mostly polymeric matrix; in the absence of other control mechanisms, a membrane controlling the active substance release; a pressure-sensitive adhesive device to fix the system on the skin; and, if required, a protective layer removable prior to applying the system as a ready-made drug.
The transdermal pressure-sensitive adhesive patches which can be used for the present invention are known to the skilled artisan from the prior art. Essentially they can be classified into two basic control principles: matrix-diffusion-control and membrane c

REFERENCES:
patent: 3598122 (1971-08-01), Zaffaroni
patent: 4687481 (1987-08-01), Nuwayser
patent: 4708716 (1987-11-01), Sibalis
patent: 5308625 (1994-05-01), Wong
Heilmann, Therapeutische Systeme, Ferdinand Enk, Verlag Stuttgart, Germany 1982 p. 26.

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