SK22698A3 - Transdermal therapeutical system for silatran compounds - Google Patents

Abstract

A preparation containing a silatran is, in the form of a transdermal therapeutical system, suitable for the prevention and/or treatment of hair or wool loss.

Description

Technical field

The invention relates to a transdermal therapeutic system (TTS) for the prophylaxis and treatment of hair and hair loss.

BACKGROUND OF THE INVENTION

The efficacy of substituted silatranes as a hair and hair growth agent is known from German Patent 26 15 654. In particular, the good compatibility of the compound used is emphasized. Administration according to this document is carried out either in the form of a food additive, which is particularly suitable in the case of animals or incorporated into ointments or suspensions. For multiple applications per week, treatment times are in the range of months. Because of the high demands placed on patient compliance and, moreover, it is difficult to control the amount of active ingredient administered due to known drawbacks in the application of ointments or suspensions, it cannot satisfy the prior art.

Accordingly, it is an object of the invention to provide a new dosage form which overcomes the aforementioned disadvantages of using substituted silatranes for the prophylaxis and / or treatment of hair and hair loss.

SUMMARY OF THE INVENTION

This object is achieved by providing a transdermal therapeutic system formulation containing substituted silatranes of the formula

in which:

R is H or CH 3,

Z is optionally a chlorine-substituted divalent group containing 1 to 3 C-atoms, and

X is H, lower alkyl, aryl, halogen, CF 3, CN, NH 2, SH, CNS, R 1M, (R 2 O) 2 P (O), R 3 C (O) M, wherein R 1 is straight or branched alkyl of 1 to 4 C atoms, aryl, aralkyl, alkaryl, M is O, S, R 2 is methyl, ethyl, R 3 is C 1 -C 4 alkyl, C 1 -C 4 fluoroalkyl, or aryl.

Therapeutic systems (TTS) contain one or more active substances which they deliver continuously at predetermined doses at a specified time at a specified site of application (Heilmann, Therapeutische Systeme - Konzept und Realization programierter Arzneiverabreichung, 4th edition, Ferdinand Enke Stuttgart, 1984) 26).

Among these therapeutic systems, the transdermal patches of the present invention also have the advantage that silatranes are suitable for penetration into the skin due to the rounded shape of the molecule. TTS in the form of a patch are known to those skilled in the art. In general, the impermeable backsheet, the active substance reservoir associated therewith, comprise a membrane that controls the dosage of the active agent unless other control mechanisms are available, a self-adhesive portion for attaching the patch to the skin and, if necessary, a protective layer removable prior to application. If the active substance reservoir itself is sufficiently tacky, the TTS can be made by mixing the active ingredient, the adjuvant and the contact adhesive polymers in a suitable solvent, coating the backing layer, removing the solvent and attaching the protective layer. The order of the layers can be reversed.

In principle, the active substance reservoir can also be formed from a melt.

The synthesis of the active compounds applicable according to the invention is described in German patent 25 22 982. Because of their good compatibility, 1 (chloromethyl) silatran and 1- (ethoxy) silatran are particularly preferred.

The concentration of at least one active substance from the group of silatranes in the reservoir ranges from 0.1 to 50% by weight. %, preferably from 3 to 25 wt. % and particularly preferred is from 5 to 15 wt. %. The dose for the patch can be adjusted by the choice of layer thickness and the reservoir wide area and is governed, inter alia, by the age and surface of the patient's skin, and by the manner and degree of hair loss.

Similar considerations apply to application in animals.

With TTS containing silatran, a dosage form is provided for a long-term, useful agent for the prophylaxis and treatment of hair and hair loss, allowing duration of action over weeks and months in a single application while providing the desired dosage of the active ingredient. Moreover, the systemic action of silatranes does not make topical application necessary.

Claims (6)

A preparation for the prophylaxis and / or treatment of hair and hair loss, comprising as active substance silatran of the formula: R is H or CH 3, Z is optionally a chlorine-substituted divalent group containing 1 to 3 catomas, and X is H, lower alkyl, aryl, halogen, CF 3, CN, NH 2, SH, CNS, R 1 M, (R 2 O) 2 P (O), R 3 C (O) M, wherein R 1 is straight or branched alkyl of 1 to 4 C- atoms, aryl, aralkyl, alkaryl, M is O, S, R 2 is methyl, ethyl, R 3 is C 1 -C 4 alkyl, C 1 -C 4 fluoroalkyl, or aryl, characterized in that it is in the form of a transdermal therapeutic system. The composition according to claim 1, characterized in that it is in the form of a patch. The formulation according to claim 2, characterized in that the patch comprises an impermeable backing layer, an active substance reservoir associated therewith, a membrane which controls the dosage of the active substance, unless other control mechanisms are available, a contact adhesive for attaching the patch to the skin and if necessary, a removable protective layer before applying the patch. Composition according to one or more of Claims 1 to 3, characterized in that it contains the active substance in an amount of 0.1 to 50% by weight. %, preferably 3 to 25 wt. % and in particular 5 to 15 wt. %. Composition according to one or more of Claims 1 to 4, characterized in that it contains 1- (chloromethyl) silatran as the active substance. \ Preparation according to one or more of Claims 1 to 4, characterized in that it contains 1- (ethoxy) silatran as active substance.