Active ingredient patch

Details Active ingredient patch Active ingredient patch

1995-12-15

1997-11-04

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...

424487, A61F 1300, A61K 970, A61K 914

Patent

active

056837119

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

1. Field of the Invention
The transdermal administration, i.e. systemic intake following dermal application, of drugs, such as oestradiol, nitroglycerol, nicotine, selegiline, piroxicam, oestradiol valerate, norethisterone, norethisterone acetate, levonorgestrel etc., to name only a few examples, has the advantage over oral administration of absorption bypassing the gastrointestinal tract and therefore of avoidance of metabolism of the drugs during the first hepatic pass. Hepatic metabolism can result in undesirable concentration ratios between the parent substance and metabolites. Another advantage of transdermal administration lies in the uniformity of the blood levels after absorption of the active ingredients through the skin, since influences such as a varying degree of filling of the gastrointestinal tract, interactions with foods or restricted or accelerated intestinal mobility such as occur with peroral administration do not exist. In the event of any active ingredient-related side effects which occur, a technical system for systemic administration of active ingredient via the skin (transdermal therapeutic system TTS, transdermal (drug) delivery system TD(D)S), called active ingredient patches or patches below, can be removed from the skin and the administration of active ingredient can therefore be interrupted immediately. The systems currently commercially available, for example for oestradiol, the combination of oestradiol and norethisterone acetate, nitroglycerol and scopolamine, or systems undergoing clinical trials, such as systems for testosterone, mainly comprise the active ingredients dissolved in alcoholic solution. Alcohol in direct, prolonged contact with the skin in many cases leads to skin irritation or even to allergies, which force discontinuation of the therapy. This was the reason for the systems described below with alternative absorption promoters or supersaturated systems (in the storage state) without absorption promoters. However, it is precisely the supersaturated systems which are physically unstable. In these patches, the active ingredient or ingredients can recrystallize unpredictably and the permeation of these active ingredients through the skin can thus be reduced in an unpredictable manner. Associated with this is then an inadequate permeation of the active ingredient through the skin, which under certain circumstances can lead to levels falling below the blood level concentration which is therapeutically necessary. Supersaturated patches are metastable and therefore in principle unstable.
As a rule, chemical absorption promoters, azones being the best-known example, modify the structure of the skin such that the skin loses its natural barrier function. The absorption promoters undergo interaction with components of the skin, so that in many cases skin irritation and allergic symptoms result. There is thus an urgent need for skin-compatible, therapeutically reliable and stable active ingredient patches for drugs.
2. Background Art
According to the prior art, the patches for systemic administration of hormones can be divided into three classes: supersaturated state
Patches with absorption promoters are by far the largest group, since in the technical literature, for example, oestradiol or gestagenic hormones have been described as substances which permeate with difficulty.
EP-A-0 474 647 describes the use of hydrated aluminium silicate for increasing adhesive strength. A glycol, which also serves as an absorption promoter, is used as the solvent. In addition to their absorption-promoting property, glycols have the side effect of drying out the skin. U.S. Pat. No. 5,023,084 claims progesterones and oestrogens in separate layers, each with the absorption promoter n-decanol. Decanol is a skin-irritating and unpleasantly smelling substance which is not approved for pharmaceuticals. EP-A-0 371 496 (=U.S. Ser. No. 278,625) describes the use of oleic acid, a linear alcohol/lactic acid ester, dipropylene glycol or N-methyl-2-pyrrolidone as absorpti

REFERENCES:
patent: 4913905 (1990-04-01), Fankhauser et al.
patent: 5128124 (1992-07-01), Fankhauser et al.
patent: 5204119 (1993-04-01), Shiobara et al.
patent: 5300291 (1994-04-01), Sablotsky et al.
patent: 5352457 (1994-10-01), Jenkins

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