Estradiol penetration enhancers

Details Estradiol penetration enhancers Estradiol penetration enhancers

1996-10-11

2000-07-18

Dees, Jose' G.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

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

424449, A61F 1302

Patent

active

060904046

DESCRIPTION:

BRIEF SUMMARY
This application is a 371 of PCT/EP95/00032 filed Jan. 5, 1995.
The present invention relates to an active substance-containing patch for the controlled release of estradiol or its pharmaceutically acceptable derivatives alone or in combination with gestagens to the human or animal skin by using pressure sensitive adhesives and at least one penetration enhancer. The present invention further relates to its use and to a process for its production.


BACKGROUND OF THE INVENTION

Estrogen-containing patches have been known for some time. However, they have the disadvantages that they either contain ethanol, or that there is the potential risk that the active substance recrystallizes in the course of time, or that they do not release estradiol in an amount sufficient for therapy.
It is known from DE-OS 32 05 258 and EP 0 285 563 to administer estradiol and ethanol at the same time in a patch formulation. However, the production of said patch is very expensive and the wearing comfort after application is low due to the lack of flexibility.
EP 0 285 563 describes a transdermal therapeutic system for the combined application of estrogens and gestagens. The reservoir comprises an active substance formulation, optionally a membrane, as well as ethanol used as percutaneous absorption improving agent. The active substance release is mainly controlled by the membrane. In the patch described therein, the adhesive has the mere function of fastening the patch to the skin. The fact that it can contribute to the control of the active substance release is not its main function, what is more, this is merely a side effect--probably not desired at all. The patch described there is a so-called "pouch patch" since the active substance preparation is present in a pouch consisting of an impermeable backing layer and a membrane having an adhesive layer. As a consequence of its complicated structure, the production of this patch is very expensive, since the individual components have to be manufactured separately and then joined to form a patch in an additional process step.
EP 0 275 716 describes a two-layer transdermal therapeutic system for the simultaneous administration of one or several estrogens dissolved or microdispersed in the polymeric layer. In addition to the active agents, the adhesive layer comprises substances improving the transdermal absorption. Polymeric and adhesive layer may consist of polyacrylates, silicones, or polyisobutylenes.
EP 0 072 251 describes a flexible, moisture-absorbing medical bandage. The substrate attached to the flexible backing layer consists of a hydrophilic matrix based on hydrophilic, high-molecular polysaccharides and/or polyacrylic acid, polyacrylamide, ethylene-vinyl-acetate-copolymers, and other polymers, as well as of a liquid phase based on a solution or emulsion of carbohydrate, proteins, and polyhydric alcohols, as well as different active substances, amongst others hormones. An essential feature of this invention is the hygroscopic adhesive.
EP 0 328 806 describes a membrane-free, transdermal therapeutic system whose matrix consists of a polyacrylate adhesive, a solvent, a polyoxyethylene ester as penetration enhancer, and estrogens, the derivatives and combinations thereof.
WO 87/07 138 describes an estradiol patch based on a backing layer, an active substance-containing matrix, and a pressure sensitive adhesive covered with a removable protective layer. The production of the matrix and the adhesive is effected in technologically very expensive operations by homogenizing, degassing, coating, drying and separating. According to an embodiment, the backing layer must be coated with a pressure sensitive adhesive, involving another operational step. The individual parts are joined together in a separate step. For this reason, the manufacture of this patch is very expensive and complicated.
U.S. Pat. No. 4,624,665 describes systems containing the active substance in micro-encapsulated form in the reservoir. The reservoir is embedded between a backing layer and a membrane. The outer edg

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Banakar, Pharmaceutical Dissolution Testing, 1st Editionj, 1991, pp. 330-341 Marcel Dekker, Inc. New York, New York.

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