Transdermal matrix system

Details Transdermal matrix system Transdermal matrix system

1998-03-26

2000-01-11

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...

424443, 424448, 424449, 424487, A61F 1302

Patent

active

060132760

DESCRIPTION:

BRIEF SUMMARY
FIELD OF THE INVENTION

The present invention relates to a novel matrix system for the transdermal administration of an estrogen component and/or a progestin component, said system being formed of a carrier and an adhesive matrix which is composed of an ethylene/vinyl acetate (EVA) copolymer and the specific association of three compounds, namely diethyl phthalate, 2-octyldodecyl myristate and an N-alkyl-2-pyrrolidone, and in which said estrogen component and/or said progestin component are dissolved.
The invention further relates to a method of preparing said matrix system and to its use in therapeutics.


PRIOR ART

Numerous systems for the transdermal administration of a hormone, particularly an estrogen component by itself, are currently available for the treatment of the symptoms of the menopause and osteoporosis in the context of treatments described as "hormone replacement therapy". These systems now include so-called "reservoir" systems, in which the active principle is dissolved in a solvent acting as a vector for transport through a microporous membrane towards the skin. This is the case of the device based on 17.beta.-estradiol which is marketed by CIBA-GEIGY under the name ESTRADERM.RTM. TTS.
At the same time, so-called "matrix" systems exist in which the active principles are dissolved or dispersed in an adhesive matrix based on polymers such as EVA copolymers, acrylic copolymers, styrene/isoprene/styrene copolymers, etc. This is the case of the device based on 17.beta.-estradiol which is marketed by LABORATOIRES FOURNIER S.C.A. under the name OESCLIM.RTM..
On the other hand, the production of systems for the transdermal administration of an estrogen component and a progestin component in these matrix systems still presents numerous problems.
In fact, it is known that estrogens and progestins are products of very low solubility in the polymers used in the formulation of the matrix system. Furthermore, each of these active principles may be partially or totally incompatible with some of the constituents of the formulation (resins, solvents, plasticizers, polymers, skin absorption promoters). They may have different solubilities and stability temperatures and one of the two may recrystallize over time, degrade when used or be usable in the composition only at concentrations which are too low to achieve the desired therapeutic effect. Likewise, no universal skin absorption promoter exists for increasing the transdermal flux of all the active principles. Therefore, to administer different active principles, it is often necessary to use several promoters and/or solvents. Now, the introduction of any new substance may cause or raise new problems of irritation and cohesion or adhesion of the system.
In the same way, taken together, these constraints (compatibility, solubility) also affect the various constituents of the formulation other than the active principles, and therefore exacerbate the difficulties to be resolved.
Furthermore, these demands relating to skin tolerance, adhesion and cohesion of the system are compounded by dosage constraints. In general the active principles have different skin permeating abilities, meaning that each active principle has a different absorption flux. It therefore becomes very complicated to develop a formulation which enables the desired therapeutic dose of each active principle to be administered. In practice, it is very often impossible to develop such a formulation and the development leads to a dead end or to systems which are rather unsatisfactory and hence economically non-viable. This explains why no system of this type has yet been marketed.
In actual fact, the only currently available transdermal system for the administration of two hormones is a "reservoir" system based on 17.beta.-estradiol and norethisterone acetate, which is marketed by CIBA-GEIGY under the name ESTRAGEST.RTM. TTS.
Those skilled in the art are also aware that estrogens and/or progestins are molecules which cannot easily pass through the skin barrier.
Thus the quantities of these act

REFERENCES:
patent: 5286490 (1994-02-01), Goldberg
patent: 5453279 (1995-09-01), Lee et al.
patent: 5605702 (1997-02-01), Teillaud et al.
Patent Abstracts of Japan, vol. 16, No. 93 (C-917), Mar. 6, 1992 and JP 03 275619 A (NITSUSUI), Dec. 6, 1991.

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