Device for the transdermal administration of a rotigotine base

Abstract

The invention relates to a polymer matrix suitable for the transdermal administration of rotigotine [(−)-5, 6, 7, 8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino)-1-naphtol], containing a matrix for the transdermal administration of rotigotine [(−)-5,6,7,8-tetrahydro-6-[propyl[2-(2-thienyl)ethyl]amino]-1naphtol], containing a matrix polymer which is supersaturated with a rotigotine base. Said polymer matrix is characterised in that the part of the rotigotine which is not dissolved in the matrix polymer is dispersed in the matrix polymer as amorphous particles having a maximum mean diameter of 30 ?m, and the matrix is free of solubilisers, crystallisation inhibitors and dispersants. The invention also relates to a flat device for the transdermal administration of rotigotine, containing the above-mentioned, preferably silicon-based polymer matrix which is supersaturated with rotigutine, and a rear layer which is impermeable to the active ingredient.

1 - 11 . (canceled)  
     
     
         12 . A matrix for transdermal administering of rotigotine containing a matrix polymer supersaturated with rotigotine base, 
 wherein a portion of the rotigotine not dissolved in the matrix polymer is dispersed in the matrix polymer as amphorous particles with a maximum mean diameter of 30 μm and    the matrix is free of solvents, crystallization inhibitors and dispergents.    
     
     
         13 . A matrix for transdermal administering of rotigotine, consisting of: 
 (a) matrix polymer,    (b) rotigotine base in a concentration above the solubility limit of the matrix polymer, wherein a portion of the rotigotine not dissolved in the matrix polymer is dispersed in matrix polymer as amphorous particles with a maximum mean diameter of 30 μm and    (c) optionally one or more antioxidants.    
     
     
         14 . A matrix according to  claim 12  or  13  wherein the matrix polymer is an amino-resistant silicon or a mixture of amino-resistant silicons.  
     
     
         15 . A matrix according to  claim 12  or  13  wherein the matrix is self-adhesive.  
     
     
         16 . A matrix according to  claim 12  or  13  wherein the matrix consists of: 
 (a) about 60 to about 95 weight percent of an amino-resistant silicon or an amino-resistant silicon mixture,    (b) about 5 to about 40 weight percent amorphous rotigotine base dispersed in the silicon and    (c) 0 to about 2 weight percent antioxidant.    
     
     
         17 . A system for transdermal administering of rotigotine comprising a matrix of claims  12  or  13  and a backing.  
     
     
         18 . The system of  claim 17  wherein the backing is impermeable to rotigotine.  
     
     
         19 . The system of  claim 17  wherein the rotigotine charge is between 0.3 to 6 mg/cm 3 .  
     
     
         20 . A method for treating a patient suffering from or susceptible to Morbus Parkinson comprising administering rotigotine to the patient with a matrix of  claim 12  or  13 .  
     
     
         21 . The method of  claim 20  wherein the patient has been identified as suffering from Morbus Parkinson and rotigotine is administered to the identified patient.  
     
     
         22 . A method for treating a patient suffering from or susceptible to Restless Leg Syndrome comprising administering rotigotine to the patient with a matrix of  claim 12  or  13 .  
     
     
         23 . The method of  claim 20  wherein the patient has been identified as suffering from Restless Leg Syndrome and rotigotine is administered to the identified patient.  
     
     
         24 . A method for treating a patient suffering from or susceptible to depression comprising administering rotigotine to the patient with a matrix of  claim 12  or  13 .  
     
     
         25 . The method of  claim 24  wherein the patient has been identified as suffering from depression and rotigotine is administered to the identified patient.  
     
     
         26 . A method for producing a pharmaceutical matrix for transdermal administering of rotigotine, comprising: 
 (a) dissolving matrix polymer in one or more solvents;    (b) adding rotigotine base in crystalline form in a quantity above the solubility limit of the matrix polymer;    (c) removing solvent and heating the matrix produced in (b) to at least about 74° C. for a time sufficient to melt rotigotine;    (d) cooling the matrix.    
     
     
         27 . The method of  claim 26  wherein the rotigotine polymer matrix produced in (b) is applied on a substrate impermeable to rotigotine.  
     
     
         28 . The method of  claim 27  wherein after applying the rotigotine polymer matrix on the substrate solvent is removed.