AU701327B2 - Preperation for the prophylaxis and/or treatment of wool and hair loss - 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

This object is achieved by the fact that the preparation comprising substituted silatranes of the formula

N

R- -R 0/ x is made in the form of a transdermal therapeutic system.

With the following meanings: R H or CH 3 Z a double-bond group comprising 1 to 3 C-atoms and optionally substituted by chlorine, and X H, low alkyl, aryl, halogen, CF 3 CN, NH 2 SH, CNS, R 1

M,

(R

2 0) 2

R

3 C(O)M with R, alkyl, straight-chain or branched, with 1 to 4 C-atoms, aryl, aralkyl, alkaryl, M O, S R2 methyl, ethyl, R 3 alkyl with 1 to 4 C-atoms, fluoroalkyl with 1 to 4 C-atoms, or aryl.

Therapeutic systems (TTS) comprise one or several active substances which are continuously released at a predetermined rate over a definite period of time to a definite site of application (Heilmann, Therapeutische Systeme Konzept und Realisation programmierter Arzneiverabreichung, 4th edition, Ferdinand Enke Verlag Stuttgart, 1984, p. 26).

Among these therapeutic systems, patches having a transdermal action are preferred according to the present invention, one reason is that silatranes are suitable for skin penetration because of their globular molecular shape.

TTSs in patch form are known to the skilled artisan. In general, they comprise an impermeable backing layer, an active substance reservoir connected therewith, a membrane controlling the release of the active substance in the absence of other control :mechanisms, a pressure-sensitive adhesive device to fix the patch to the skin, and, if necessary, a protective layer removable prior to application. If the active substance reservoir is self-adhesive by itself, the TTS may be manufactured by homogeneously mixing the active substance, auxiliary agents, and pressure-sensitive adhesive polymers in a suitable solvent, spreading the solution on the backing layer, removing the solvent, and applying a protective layer. It is also possible to reverse the succession of layers.

On principle the reservoir may also be manufactured from the melt.

A synthesis of the active substances to be used according to the present invention is described in German patent specification 22 982. 1-(chloromethyl) silatrane and 1-(ethoxy)-silatrane are particularly preferred because of their good tolerance.

The concentration of at least one active substance from the silatrane group within the reservoir amounts to about 0.1 to preferably to about 3 to 25%-wt., and most preferably to 5 to The dose per patch may then be adjusted by the selection of the layer thickness and the dimension of the reservoir; among other things, it depends on the age and the skin surface of the patient, as well as on the kind and degree of hair loss.

p:\WPDOCS\NEH\SPEC\69293-96.SPE -27111/98 When used for animals, similar considerations are applicable.

The silatrane-containing TTS provides an application form for an agent that can be used over a longer period for the prophylaxis and treatment of wool and hair loss, which makes the duration of effect of one single administration last over several weeks and months and ensures a desired dosage of the active substance.

Moreover, the systemic action of silatranes does not necessarily require a topical application.

0* 0 0000 0* 0 0 0 0 09 0 0 0 0 0 0 .0 Throughout this specification and the claims which follow, unless the context requires otherwise, the word "comprise", or variations such as "comprises" or "comprising", will be understood to imply the inclusion of a stated integer or step or group of integers or steps but not the exclusion of any other integer or step or group of integers or steps.

1. A preparation for the prophylaxis and/or treatment of wool or hair loss comprising the active substance silatrane of the formula 0

N

R-R

R 0 -R R- /Z 0 1

X

wherein R H or CH 3 Z a double-bond group comprising 1 to 3 C-atoms and optionally substituted by chlorine, and X H, low alkyl, aryl, halogen, CF., CN, NH 2 SH, CNS, R 1

M,

(R

2 0) 2

R

3 C(O)M with R, alkyl, straight-chain or branched, with 1 to 4 C-atoms, aryl, aralkyl, alkaryl, M O, S, R 2 methyl, ethyl, R 3 alkyl with 1 to 4 C-atoms, fluoroalkyl with 1 to 4 C-atoms, or aryl, characterized in that it is present in the form a transdermal therapeutic system.

2. The preparation according to claim 1 characterized in that it is present as a patch.

3. The preparation according to claim 2 characterized in that the patch comprises an impermeable backing layer, an active substance reservoir connected therewith, a membrane controlling the

Claims (4)

1. 4. The preparation according to one or several claims 1 to 3 characterized in that it comprises 0.1 to 50%-wt, of active substance. 0. 0 0 0 0 The preparation according to one or several of claims 1 to 4 characterized in that it comprises 1-(chloromethyl)-silatrane as active substance.
2. 6. The preparation according to one or several of claims 1 to 4 characterized in that it comprises 1-(ethoxy)-silatrane as active substance.
3. 7. The preparation according to claim 4 which comprises 3 to 25%-wt of active substance.
4. 8. The preparation according to claim 4 which comprises 5 to 15%-wt of active substance. 00 0 0 00* 0* 0* 0* 000 00 0 0 0 DATED this 27th day of November 1998 LTS LOHMANN THERAPIE-SYSTEME GmbH By their Patent Attorneys DAVIES COLLISON CAVE ~zzc~ ~zzc~ 7 ABSTRACT A preparation comprising a silatrane is, in the form of a transder- mal therapeutic system, suitable for the prophylaxis and/or treat- ment of wool and hair loss.