Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1995-05-16
1997-09-02
Phelan, D. Gabrielle
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424448, 424449, A61L 1500
Patent
active
056629230
DESCRIPTION:
BRIEF SUMMARY
THIS APPLICATION IS A 371 OF PCT/EP93/02182, FILED AUG. 16, 1993.
DESCRIPTION
The invention relates to a self-adhesive plaster for the transdermal application of systemically active steroid hormones, comprising an active substance-impermeable backing layer, an active substance-containing pressure-sensitive adhesive layer and a removable protective layer covering said pressure-sensitive adhesive layer prior to application to the skin.
Active substance plasters as therapeutic systems (TTS) are self-adhesive devices to be applied to the skin, having a defined application surface and releasing one or more drugs contained therein to the human or animal body in a controlled manner as to time and amount.
However, it is a prerequisite for transdermal active substance absorption, that the active substance in the galenic formulation be provided in a form permitting its absorption by the skin, which means that the active substance must be at least partially dissolved in the formulation. The steroid hormones, and in particular the active substance estradiol, which among the substances of this group is the one most thoroughly tested for transdermal administration, are known to exhibit only a very low solubility in those formulations which are commonly suitable for transdermal active substance release and are commonly used for this purpose. In such formulations, wherein as base polymers for example polyacrylates or polyisobutylenes are utilized, generally recrystallisation of the active substance occurs during storage of the plaster, which alters the release behaviour and thus the resorption behaviour.
In principle, there is a possibility to maintain the solubility of the active substance during storage and to prevent recrystallization by employing solubilizers.
In estradiol TTS which have been available on the market under the trademark "Estraderm", estradiol and ethanol are administered as solvents for estradiol in a plaster formulation containing the active substance solution in a bag (EP 0 285 563). Disadvantages of this plaster are first its complicated structure and complicated, costly manufacture, and secondly the fact that, in particular in the case of application over a period of several days, skin irritations may occur caused by the solubilizer ethanol.
In transdermal therapeutic systems of common construction-comprising single-layered, self-adhesive active substance matrices, for example--the use of solubilizers at a concentration which is at least equal to that required results in loss of cohesion, i.e. in the matrices becoming "mushy". This especially applies to dexpanthenol, a liquid which is highly viscous at room temperature and which in common formulations has a highly softening effect, even at comparatively low concentrations. EP 0 380 989 describes dexpanthenol as a penetration auxiliary substance in the transdermal administration of systemically effective, pharmaceutic active substances. It is stated to be a particular advantage of the use of dexpanthenol that dexpanthenol does not only have a penetration enhancing effect but also suppresses or reduces the skin irritating influence of active substances and auxiliary substances.
In addition, tests carried out by the applicant of the present application have shown that dexpanthenol is a good solvent and a good solubilizer for steroid hormones.
It was thus the object of the present invention to provide an application of steroid hormones for a plaster for transdermal formulation permitting incorporation into the formulations of dexpanthenol at concentrations not below those required for solubilizatlon while avoiding both loss of cohesion and deliquescence of the active substance-containing plaster component during application.
Surprisingly, this object was achieved in that the active substance-containing pressure-sensitive layer contains a pressure-sensitive hot melt adhesive with a processing temperature of 60.degree. to 100.degree. C., and a portion of dexpanthenol of from 15 to 25%-wt.
Since, commonly, formulations for the transdermal application
REFERENCES:
patent: 4994267 (1991-02-01), Sablotsky
The Merck Index, 9th ed., Martha Windholz Editor p. 386, 1976.
LTS Lohmann Therapie-Systeme GmbH & Co.
Phelan D. Gabrielle
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