Abstract: Use of an additive in a transdermal therapeutic system with an active agent-containing layer in the form of a biphasic layer having a hydrophilic inner phase and a hydrophobic outer phase, in which the inner phase comprises the additive and an active agent dissolved therein, the additive has a higher affinity to water than to the active agent, for the control of the permeation rate of the active agent in a manner which is independent from its concentration in the biphasic layer, with the maintenance of the permeation rate proportional to the amount of active agent in the biphasic layer.

Abstract: The present invention relates to the use of an additive in a transdermal therapeutic system with an active agent-containing layer in the form of a biphasic layer having a hydrophilic inner phase and a hydrophobic outer phase, in which the inner phase includes the additive and an active agent dissolved therein. The additive has a higher affinity to water than to the active agent and controls the permeation rate of the active agent in a manner which is independent from its concentration in the biphasic layer, with the maintenance of the permeation rate being proportional to the amount of active agent in the biphasic layer.

Abstract: The present invention relates to a transdermal therapeutic system, comprising (a) a backing layer, (b) a solvent-based self-adhesive matrix layer containing rotigotine as active ingredient, and (c) a release liner, wherein the self-adhesive matrix layer has a coating weight of about 75-400 g/m2 and comprises a reservoir layer containing about 9-25 wt.-% rotigotine based on the weight of the reservoir layer, a kit comprising two transdermal therapeutic systems of the present invention as well as a method for the preparation of the transdermal therapeutic system of the present invention.

Abstract: The present invention relates to a transdermal therapeutic system formed from (a) a backing layer, (b) a solvent-based self-adhesive matrix layer containing rotigotine as active ingredient, and (c) a release liner, in which the self-adhesive matrix layer has a coating weight of about 75-400 g/m2 and comprises a reservoir layer containing about 9-25 wt.-% rotigotine based on the weight of the reservoir layer; a kit containing two transdermal therapeutic systems of the present invention; and methods for the preparation of the transdermal therapeutic system of the present invention. The present invention further relates to methods of treatment based upon the application of the inventive transdermal therapeutic systems once or twice weekly via systems adapted to allow for the transdermal administration of therapeutically effective amounts of rotigotine for at least 3 days.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a nom-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: Use of an additive in a transdermal therapeutic system with an active agent-containing layer in the form of a biphasic layer having a hydrophilic inner phase and a hydrophobic outer phase, wherein the inner phase comprises the additive and an active agent dissolved therein, wherein the additive has a higher affinity to water than to the active agent, for the control of the permeation rate of the active agent in a manner which is independent from its concentration in the biphasic layer, wherein the maintenance of the permeation rate is proportional to the amount of active agent in the biphasic layer.

Abstract: The invention relates to a transdermal therapeutic system (TTS) which contains a rotigotine-containing adhesive layer and is characterized by the fact that the adhesive layer contains a hot-meltable contact adhesive. The invention also relates to the use of rotigotine for producing the adhesive layer of a TTS in a hot melt method, and a method for producing such a TTS.

Abstract: The present invention relates to a transdermal therapeutic system, comprising (a) a backing layer, (b) a solvent-based self-adhesive matrix layer containing rotigotine as active ingredient, and (c) a release liner, wherein the self-adhesive matrix layer has a coating weight of about 75-400 g/m2 and comprises a reservoir layer containing about 9-25 wt.-% rotigotine based on the weight of the reservoir layer, a kit comprising two transdermal therapeutic systems of the present invention as well as a method for the preparation of the transdermal therapeutic system of the present invention.

Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.

Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.

Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fybromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.

Abstract: An improved Transdermal Delivery System (TDS) comprising a backing layer inert to the components of the matrix, a self-adhesive matrix containing rotigotine and a protective foil or sheet to be removed prior to use, characterized in that the self-adhesive matrix consists of a solid or semi-solid semi-permeable polymer (1) wherein rotigotine in its free base form has been incorporated, (2) which is saturated with rotigotine and contains said rotigotine as a multitude of microreservoirs within the matrix, (3) which is highly permeable for the free base of rotigotine, (4) which is impermeable for the protonated form of rotigotine, (5) wherein the maximum diameter of the microreservoirs is less than the thickness of the matrix. is provided. Said TDS provides for enhanced flux of rotigotine across the TDS/skin interface.

Abstract: The present invention relates to a novel polymorphic form of Rotigotine characterized by at least one of the following X-ray powder diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (°2?), measured with a Cu—K? irradiation (1.54060), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's Disease and other dopamine-related disorders.

Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

Abstract: An improved Transdermal Delivery System (TDS) comprising a backing layer inert to the components of the matrix, a self-adhesive matrix containing rotigotine and a protective foil or sheet to be removed prior to use, characterized in that the self-adhesive matrix consists of a solid or semi-solid semi-permeable polymer (1) wherein rotigotine in its free base form has been incorporated, (2) which is saturated with rotigotine and contains said rotigotine as a multitude of microreservoirs within the matrix, (3) which is highly permeable for the free base of rotigotine, (4) which is impermeable for the protonated form of rotigotine, (5) wherein the maximum diameter of the microreservoirs is less than the thickness of the matrix. is provided. Said TDS provides for enhanced flux of rotigotine across the TDS/skin interface.