Transdermal therapeutic systems containing 4-n-butyl-resorcinol

Abstract

A method for the treatment of a local pigmentation disorder comprises applying to skin affected by the disorder a transdermal therapeutic system which comprises 4-n-butylresorcinol as an active ingredient.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]The present application is a divisional of U.S. application Ser. No. 13 / 499,861, the entire disclosure of which is expressly incorporated by reference herein, which is a National Stage entry of PCT / EP2010 / 04272, filed Jul. 14, 2010, which claims priority under 35 U.S.C. 119 of German Patent Application 10 2009 048 073.8, filed Oct. 9, 2009.BACKGROUND OF THE INVENTION1. Field of the Invention[0002]The present invention relates to transdermal therapeutic systems, self-adhesive flat bandages, in particular cosmetic and medicinal plasters, containing 4-n-butylresorcinol.2. Discussion of Background Information[0003]Melanocytes are responsible for the pigmenting of the skin; these are found in the lowest layer of the epidermis, the Stratum basale, alongside the basal cells as pigment-forming cells which, depending on the skin type, occur either individually or in clusters of varying size.[0004]Melanocytes contain, as characteristic cell organel...

AI Technical Summary

Benefits of technology

The present invention is a transdermal therapeutic system that uses 4-n-butylresorcinol as the main active ingredient. The system can be applied in the form of a self-adhesive flat bandage or a matrix system. The system can release 4-n-butylresorcinol at a rate of >30% / 24 h. The therapeutic system can be used to treat local pigmentation disorders such as age spots, freckles, and melasma. Nonpolar matrices based on synthetic and natural rubber, polar wet adhesive films based on polyacrylic acid / polyvinyl alcohol, and polar water gel matrices based on agar agar / polyacrylic acid can be used as the matrix system. The system can also contain penetration accelerators such as isopropyl palmitate and isopropyl myristate.

Problems solved by technology

This can lead either to post-inflammatory hyperpigmentations or hypopigmentations.

Problems with post-inflammatory hyperpigmentation often occur in darker skin types.

Particularly in colored males, the problem of Pseudofollikulitis barbae is known, which is associated with cosmetically undesired incorrect pigmentation and / or leads to this.

In practical use are essentially preparations based on hydroquinone, although, on the one hand, these only exhibit their effect after application for several weeks, and, on the other hand, their excessively long application is unacceptable for toxicological reasons.

However, this formulation too is highly disputed on account of possible irreversible changes in the pigmentation system of the skin.

In addition, skin-peeling methods (chemical and mechanical peels) are used, although these often lead to inflammatory reactions and, on account of post-inflammatory hyperpigmentations which may subsequently arise, can even lead to greater pigmentation instead of reduced pigmentation.

All of these customary methods, which are also used for treating post-inflammatory hyperpigmentations, are characterized by distinct side effects.

4-n-Butylresorcinol has the formulatory disadvantage that it has a tendency to discolor—and to discolor cosmetic or dermatological preparations comprising it.

A disadvantage of TTS is that usually only ca.

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