Transdermal matrix system

Details Transdermal matrix system Transdermal matrix system

1998-03-26

1999-12-28

Harrison, Robert H.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

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

424449, A61K 970

Patent

active

060078359

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The subject of the present invention is a novel transdermal matrix device or system for the prolonged release of an oestrogenic component and/or of a progestogenic component, the said device consisting of a carrier and an adhesive matrix which is composed of a triblock copolymer having A-B-A units of the poly(styrene-isoprene-styrene) [abbreviated to SIS] type and in which there are dissolved the said oestrogenic component and/or the said progestogenic component, propylene glycol laurate combined with a derivative of N-alkyl-2-pyrrolidone and a vinyl acetate/N-vinyl-2-pyrrolidone [abbreviated to VA/VP] copolymer. The invention also relates to a method for preparing the said matrix system and to its therapeutic use.


PRIOR ART

It is known that numerous transdermal systems liberating an oestrogenic component and/or a progestogenic component have already been proposed. Among these, there are so-called "reservoir" systems in which the active ingredient is dissolved a solvent serving as vector for transport across a microporous membrane to the skin. Such is the case of devices based (i) on 17.beta.-oestradiol and (ii) on 17.beta.-oestradiol combined with norethisterone acetate, which are marketed by the company CIBA-GEIGY respectively under the names ESTRADERM.RTM. TTS and ESTRAGEST.RTM. TTS.
In parallel, so-called matrix systems exist in which the active ingredients are dissolved or dispersed within an adhesive matrix based on polymers such as EVA/acrylic copolymers. This is the case for devices based on 17.beta.-oestradiol which are marketed under the names OESCLIM.RTM. and SYSTEN.RTM..
If it is desired to obtain a therapeutically effective final product, it is imperative that all these systems possess a level of delivery of active ingredients for a prolonged period and at a rate sufficient to obtain plasma levels suited to the therapeutic needs.
However, it is known to persons skilled in the art that oestrogenic components and progestogenic components are products which cross the skin barrier with difficulty.
Consequently, the liberated quantities of these active ingredients for obtaining the desired therapeutic effect are in general low compared with the initial quantities present in the transdermal devices, which has as consequence the obtaining of low yields. This causes the use of a quantity of hormone(s) in a large excess relative to that effectively used up.
Likewise, it is known to persons skilled in the art that oestrogenic components and progestogenic components are products which are not very soluble in the polymers used in the so-called matrix transdermal systems.
However, these systems should be relatively small in size and have acceptable adhesion and cohesion properties so as to allow convenient use without impairing clothing by flowing of the mass from the matrix during use. A compromise between an effective rate of transdermal delivery of a hormone, on the one hand, and good physical and ergonomic properties of the systems, on the other, is therefore difficult to achieve and practically impossible in the case of the combined delivery of several hormones. Indeed, in the latter case, the many possible interactions and incompatibilities between the group of components forming the matrix (polymers, resins, solvents, plasticizers, active ingredients, skin absorption enhancers) which should be reconciled with the abovementioned therapeutic dose and physical constraint requirements are multiplied by at least two.
Furthermore, the problem becomes all the more complicated since the hormones exhibit different skin permeabilities and are therefore generally used in different concentrations.
The production of such systems for delivering several hormones rapidly leads to an impasse and very often to products which are not very satisfactory and which are therefore difficult to exploit commercially.
In fact, although, in order to overcome these problems, numerous studies have been carried out using a wide variety of categories of polymers such as EVAs, acrylics, polyisobutenes, sil

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patent: 5254348 (1993-10-01), Hoffmann et al.
patent: 5273757 (1993-12-01), Jaeger et al.
patent: 5411739 (1995-05-01), Jaeger et al.
patent: 5419912 (1995-05-01), Morimoto et al.
patent: 5580572 (1996-12-01), Mikler et al.

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