Composition containing rotigotine and use thereof and transdermal patch containing the composition

Abstract

A Rotigotine-containing composition having a matrix mixture system formed from a polyvinylpyrrolidone and a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive. The polyvinylpyrrolidone may be present in an amount of about 1-10% by weight in the matrix mixture system. The acrylic pressure-sensitive adhesive may be present in an amount of about 1-25% by weight in the matrix mixture system. The silicone pressure-sensitive adhesive may be present in an amount of about 65-98% by weight in the matrix mixture system. The composition further includes 1-40% of Rotigotine on the basis of the total weight of the composition. The composition provides improved properties in the solubility, release and initial penetration level of Rotigotine. Also disclosed is a transdermal patch that includes the Rotigotine-containing composition, as well as methods of manufacturing and using the Rotigotine-containing composition.

1 . A rotigotine-containing transdermal patch comprising a matrix layer composition,
 wherein the matrix layer composition comprises, on the basis of the total weight of the matrix layer composition, 60-99% by weight of a matrix mixture system and 1-40% by weight of rotigotine,   wherein the matrix mixture system is formed from a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive, and polyvinylpyrrolidone,   
       wherein
 (1) the acrylic pressure-sensitive adhesive is present in an amount of 5-19% by weight in the matrix mixture system, 
 (2) the silicone pressure-sensitive adhesive is present in an amount of 79-94% by weight in the matrix mixture system, and 
 (3) the polyvinylpyrrolidone is present in an amount of 1-10% by weight in the matrix mixture system; and 
 wherein the rotigotine is in the form of free base or a pharmaceutically acceptable salt. 
 
     
     
         2 . The rotigotine-containing transdermal patch of  claim 1 , wherein the matrix layer composition further comprises at least one auxiliary selected from the group consisting of permeation enhancers and antioxidants. 
     
     
         3 . The rotigotine-containing transdermal patch of  claim 2 , wherein the permeation enhancer is selected from the group consisting of surfactants, organic solvents including alcohols, polyols, esters, dimethyl sulfoxide, fatty acids, fatty alcohols, fatty acid esters, azones, pyrrolidone derivatives selected from the group consisting of N-methylpyrrolidone, 1,5-dimethylpyrrolidone and 5-carboxylpyrrolidone, salicylic acid and terpenes. 
     
     
         4 . The rotigotine-containing transdermal patch of  claim 2 , wherein the antioxidant is selected from the group consisting of vitamin E, ascorbyl palmitate, sodium metasulfite and mixtures thereof. 
     
     
         5 . The rotigotine-containing transdermal patch of  claim 1 , wherein the acrylic pressure-sensitive adhesive is selected from the group consisting of an acrylic pressure-sensitive polymer and a combination of an acrylic pressure sensitive polymer with an acrylic resin. 
     
     
         6 . The rotigotine-containing transdermal patch of  claim 5 , wherein the acrylic pressure-sensitive polymer is copolymerized from a soft monomer, a hard monomer and a functional monomer, wherein the soft monomer is selected from the group consisting of ethyl acrylate, 2-ethylhexyl acrylate, isooctyl acrylate, and butyl acrylate, the hard monomer is selected from the group consisting of vinyl acetate, methyl acrylate, styrene, acrylonitrile, methyl methacrylate, ethyl methacrylate, and n-butyl methacrylate, and the functional monomer is selected from the group consisting of (meth)acrylic acid, (meth)acrylamide, β-hydroxyethyl (meth)acrylate, β-hydroxypropyl (meth)acrylate, glycidyl (meth)acrylate and N-hydoxylmethylacrylamide. 
     
     
         7 . The rotigotine-containing transdermal patch of  claim 6 , wherein the acrylic pressure-sensitive polymer is copolymerized from the monomers: butyl acrylate, isooctyl acrylate, vinyl acetate, acrylamide and α-methacrylic acid. 
     
     
         8 . The rotigotine-containing transdermal patch of  claim 2 , wherein the matrix layer composition comprises, on the basis of the total weight of the matrix layer composition, 75-90% by weight of the matrix mixture system, 5-15% by weight of rotigotine and 5-11% by weight of the permeation enhancer. 
     
     
         9 . The rotigotine-containing transdermal patch of  claim 8 , wherein the matrix layer composition comprises, on the basis of the total weight of the matrix layer composition, 79-84% by weight of a matrix mixture system, 8-11% by weight of rotigotine and 8-10% by weight of the permeation enhancer, wherein the acrylic pressure-sensitive adhesive is present in an amount of 6-12.5% by weight in the matrix mixture system, the silicone pressure-sensitive adhesive is present in an amount of 86.5-93% by weight in the matrix mixture system, and the polyvinylpyrrolidone is present in an amount of 1-1.5% by weight in the matrix mixture system. 
     
     
         10 . The rotigotine-containing transdermal patch of  claim 8 , wherein the permeation enhancer is selected from the group consisting of isopropyl myristate, lauryl acid and N-methylpyrrolidone. 
     
     
         11 . The rotigotine-containing transdermal patch of  claim 1 , wherein the polyvinylpyrrolidone is present in an amount of 1-2% by weight in the matrix mixture system.