DD274357A1 - PROCESS FOR PREPARING A KERATOLYTICALLY SELF-ADHESIVE PREPARATION FOR PERCUTANEOUS APPLICATION - Google Patents

Abstract

The invention relates to a process for the preparation of keratolytic, self-adhesive preparations, with which it is possible to apply high concentrations of active ingredient percutaneously and to provide during the entire treatment period to treat existing grossflächige cornification and / or local skin defects, such as chicken eyes and warts. The preparations according to the invention are obtained by mixing solvent-containing natural rubber mixtures with liquid prepolymers obtained by bulk polymerization and keratolytic substances and applying the active substance-containing pressure-sensitive adhesive thus obtained to carrier materials in a manner known per se. Keratolytic substances are salicylic acid and / or lactic acid.

Description

Field of application of the invention

The invention is applicable in the production of keratolytic acting, solbia-producing preparations with high active ingredient concentrations and their application forms for percutaneous, cosmetic-pharmaceutical treatment of large and / or local keratinization and / or skin defects, such as cornea, warts or corns in ambulatory medical and / or cosmetic care ,

Characteristic of the known technical solutions

For the treatment of keratinization and / or Hautefefekien the human skin, especially on feet and hands, such as the cornea, warts or corns, various forms of application of cosmetic-pharmaceutical preparations are applied. Known: are medicated solutions, gels, emulsions and ointments. As Keratolytisch, - ie corneal detachment - acting substances u. a. Salicylic acid, lactic acid, acetic acid, perchloroacetic acids, formic acid, resorcinol, urea and / or sulfur. As a specific application form of porcaterally acting keratolytic preparations, active ingredient-containing patches are to be regarded. With keratolytic self-adhesive "flaps" is the treatment of cornification and / or skin defects in hard to reach areas of the human body, such as feet, toes, foot pads, etc. and / or in places that are constantly claimed in human activity, such as hands, Fingers, etc., possible. Due to the self-adhesive properties of the patches it is possible to percutaneously attach keratolytic substances to cornification and / or skin defects of the human skin without affecting human activity or freedom of movement.

In terms of application, particularly important are sufficient high bond strengths of the keratolytic plasters (3 N / cm in the 180 ° Abblältest) to follow the various stresses of self-adhesive plaster during movements of the body.

In addition, from a keratolytic point of view, the provision of the largest possible concentration of active substrates is necessary in order to be able to anticipate percutaneous treatments with self-adhesive patches, as described, for example, in US Pat. As in keratolytic solutions is possible in which after evaporation of the solvent, the keratolytic agents are completely present at the percutanone treatment site.

Due to the special formulation structure self-adhesive, keratolytic patches consisting of a polymer base, especially rubber, such as natural rubber, butyl rubber-polyisobutylene, block copolymers, such as styrene-butadiene-styrene rubber, styrene-isoprene-styrene rubber, silicone rubber, polyisoprene, etc., an adhesive resin additive , such as rosin, hydrocarbon resins, semisynthetic rosin derivatives, etc., processing aids such as plasticizers and anti-aging agents, and the active ingredients, have difficulty in producing adhesive and strong keratolytic patches.

Sufficiently good adhesion and thus a good cosmetic-phtimazeutische handling require low drug concentrations of less than 35%, since any addition of non-sticky substances in selfk ibenda Pfla'iterzubereitungen adversely affect the sticking behavior.

High drug concentrations in patches cause poor sticking behavior.

Thus, keratolytic preparations with 35-40% active ingredients are poorly adhesive and percutaneously insufficient.

Keratolytic preparations with more than 50% active ingredients non-sticky.

So z. B. for a 60% salicylic acid-containing preparation fixation with medical plaster in Anwendungsiingshinweis prescribed (prospectus Fa.Beiersdorf, Hamburg, DE).

Another serious disadvantage of highly concentrated ksratolytisch acting preparations with crystalline, homogeneously distributed in the polymer matrix, but not dissolved active ingredients, represents the drug migration to the surface of the self-adhesive preparations. With the accumulation of the active ingredient on the surface, the Kiebrigkeit is reduced; Under extreme conditions (influence of temperature, storage time, etc.), the sticking behavior of keratolytic patches can be totally reduced and the preparation keratolytically ineffective.

Object of the invention

The aim of the invention is an ancestor for the preparation of a keratolytic acting, self-adhesive preparation with a high active ingredient concentration corresponding to the cosmetic-pharmaceutical Anwendungsi'ngsformen.

Explanation of the essence of the invention

The object of the invention is to enter high concentrations of keratolytic substances in self-adhesive preparations to fix the active ingredients homogeneously distributed in the preparation to obtain high bond strengths and good tack (Tack) of the preparation and to produce therefrom cosmetic-pharmaceutical application forms keratolytic preparations, which are always percutan applicable, and not restrict the freedom of movement. It has now been found that keratolytic substances, such as salicylic acid and / or lactic acid, in Konzentratk NEN of 35% to 50%, preferably from 40% to 45%. in self-adhesive preparations, consisting of a polymei base, adhesive resins and plasticizers or processing hemps, can be incorporated, wherein the active ingredient or the active ingredient compositions registered homogeneously distributed and the drug migration is pushed back. From these preparations can be produced without a negative effect on the adhesive behavior application forms that do not restrict its freedom of movement when applied to humans and unfold full keratolytic activity. Erfindungsgernäß this Aufg-ibe is achieved in that an elastomer, preferably natural rubber, in a suitable solvent, preferably gasoline of the Siedelagen 60 ° C to 180 ⁰ C or 80 ° C to 110 ^c C, completely registered to form a homogeneous solution wirtl , wherein by mechanical stress (stirring) a mastifikation effect is achieved. By masticating the absorption capacity of the rubber with respect to the incorporated drug, such. As salicylic acid, significantly improved. By using adhesive resins, the necessary adhesive behavior of the keratolytic preparations is set.

Plasticizers or processing aids, we paraffinic, aromatic and / or naphthenic plasticizers, waxes, ester plasticizers u. a. improve the homogeneous distribution of the components of the preparation, but also lead to a reduced adhesive behavior.

Surprisingly, it has been found that a 1,2-Butadienmassepolymerisat having a molecular weight of about 32,000 and a viscosity of 10Pa in the distribution of 40-45% salicylic acid in a keratolytic preparation has a very good * * softening effect causes a homogeneous Salizylsäureverteilung, the salicylic acid fixed free of migration in the preparation and the adhesive behavior is not affected.

Disse fixation is achieved both in the keratolytic preparations and in the cosmetic-pharmaceutical applications prepared therewith.

embodiments

The above-described invention will be explained with reference to four embodiments.

Belspiol 1

In a planetary mixer is going out

Natural Rubber ADS 20.5%

Rosin 35.0%

1,2-Butadiene-Massepolyrr, erisat 4.5% and

Salicylic acid 40%

prepared a keratolytic preparation in the following manner.

The natural rubber wild in dec same Mentje Siedegrenzenbenzin SB ι 80-110 ⁰ C irr. · Mastic masticated and homogeneously distributed. 4.5% of the viscous 1 ^ -Bu'.adien bulk polymer and the amount of rosin dissolved in the same amount of concentrated petroleum spirit are added to this solution as plasticizer and distributed homogeneously.

The 40% salicylic acid is homogeneously distributed and fixed in portions in the homogeneous mixture.

Example 2

A'jsführungsbeispiel analogous to Example 1 bsi the dia keratolytisch acting preparation 'olgende composition:

Natural Rubber RSS 1 19.5% rosin 32.0% 1 ^ butadiene bulk polymer 3.5% salicylic acid 45%

Example 3

A keratolytic preparation according to Example 1 is applied uniformly on a hydrophobic, textile carrier material made of cotton fabric of a basis weight of about 135 g / m ² with an adhesive application of about 350 g / m ² , below ^: gentle conditions the solvent! Remove big ·. After drying, the carrier material coated with the keratolytic preparation is covered with siliconized paper and cut into sections of 10 cm χ 6 cm.

At a salicylic acid content of 40%, a compressive force of about 10 N / cm and a tack of about 5 N / cm of the administration form could be detected.

This cosmetic-pharmaceutical application form is especially suitable for the treatment of extensive cornification on heavily loaded body parts (foot pads).

Example 4

A preparation according to Example 2, which is applied to a support material analogously to Example 3, is used for the preparation of an application form which is used for the treatment of local skin defects, such as warts and corns.

A binder of the above-mentioned preparation is applied to a medical ZnO rubber patch, and a pressure protective band perforated at regular intervals is placed so that the keratolytic preparation is circularly surrounded by the pressure protective material.

After covering with a foil, individual sections are punched out of this composite, with which corns or warts can be treated specifically and locally.

At a bond strength of keratolytir.ch acting preparation of about 8N / cm in the 180 ° -Abschältest 'jnd 6In stickiness (tack) of 4 N / cm, this application form also has a good cosmetic-pharmaceutical efficacy, since the preparation sn sn treat the ti clings to local skin defects without affecting adjacent skin artefacts.

In the same manner as in Examples 1 to 4be. ohrieben ^C, lactic acid or mixtures alone let m of salicylic acid and lactic acid in behaves iis 10: using 2: 1 to. 1

Claims (8)

1. A process for the preparation of keratolytic acting, self-adhesive preparations for percutaneous application using solvent-containing natural rubber mixtures in conjunction with adhesive resins, characterized in that solvent-containing natural rubber mixtures are mixed with obtained by bulk polymerization, liquid prepolymers and keratolytic substances and the resulting active substance Haftklebstcff known per se Way is applied to substrates. 2. The method according to claim 1, characterized in that are used as liquid prepolymers, bulk polymers of butadiene. 3. The method according to claim 1 and 2, characterized in that the butadiene bulk polymer has a molecular weight of 20,000 to 40,000, preferably 32,000. 4. Process according to claims 1 to 3, characterized in that are used as the solvent Siedegrenzenbenzine. 5. Process according to claims 1 to 3, characterized in that Siedbstenzenbenzine with a boiling point between 60 ⁰ C and 18O ⁰ C, preferably 80 ⁰ C to 110 ⁰ C, are used. 6. Process according to claims 1 to 5, characterized gekannzeichnet that cils keratolytic substances salicylic acid and / or lactic acid are used. 7. Process according to claims 1 to 6, characterized in that the active ingredient concentration between 35% and 50%, preferably between 40% and 45%. 8. Process according to claims 1 to 7, characterized in that in the preparation of the preparations paraffinic and / or aromatic and / or naphthenic plasticizers are added.