85 results about "Rotigotine" patented technology

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.

The present application relates to the use of rotigotine or salts and prodrugs thereof for the manufacture of a medicament for the treatment or prevention of dopaminergic cell destruction in diseases associated with increased dopaminergic cell destruction. In particular, the present application also relates to the use of rotigotine as a drug for the preventive treatment of Parkinson's disease.

This invention provides the use of a silicone-based transdermal therapeutic system having an area of 10 to 40 cm2 and containing 0.1 to 3.15 mg/cm2 of rotigotine as active ingredient, for the preparation of an anti-Parkinson medicament which induces a mean plasma concentration of rotigotine in the range of 0.4 to 2 ng/ml 24 h after administration.

The present invention relates to a novel polymorphic form of rotigotine characterized by at least one of the following powder X-ray diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (° 2θ), measured with a Cu—K_α irradiation (1.54060 Å), 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.

This invention pertains to a liquid intranasal pharmaceutical formulation comprising a pharmaceutically acceptable acid addition salt of rotigotine and α-cyclodextrin, preferably in the form of a buffered aqueous solution having a viscosity of 0.5-1.5 mm²/s

The invention provides a transdermal therapeutic system (TTS) containing rotigotine as the active ingredient. The TTS is useful in the treatment of Parkinson's Disease because it induces a pharmacokinetic profile where the rotigotine plasma level is high and stable.

The present invention relates to a composition containing Rotigotine and the use thereof in the manufacture of a Rotigotine-containing transdermal patch, wherein said composition is based on a matrix mixture system formed from a combination of an acrylic pressure-sensitive adhesive with a silicone pressure-sensitive adhesive, and polyvinylpyrrolidone which are present in a particular weight ratio, wherein (1) the acrylic pressure-sensitive adhesive is present in an amount of about 1-25% by weight in the matrix mixture system, (2) the silicone pressure-sensitive adhesive is present in an amount of about 65-98% by weight in the matrix mixture system, and (3) the polyvinylpyrrolidone is present in an amount of about 1-10% by weight in the matrix mixture system, and comprises 1-40% of Rotigotine on the basis of the total weight of the composition. The present invention further relates to an improved transdermal patch containing Rotigotine comprising said composition. Said patch has improved properties in the solubility, release and initial penetration level of Rotigotine.

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.

The invention discloses a novel process for preparing rotigotine based on 2-amino-5-methoxynaphthalene as a material. The process comprises the steps of splitting to obtain (S)-2-amino-5-methoxynaphthalene (II) by L-tartaric acid, reacting (S)-2-amino-5-methoxynaphthalene (II) with bromopropane to obtain (S)-2-(N-n-propyl)amido-5-methoxynaphthalene (III); reacting (S)-2-(N-n-propyl)amido-5-methoxynaphthalene (III) with 2-(2-bromethyl) thiophene to obtain (S)-2-[N-propyl-N-[2-(2-thiophene)ethyl]amino]-5-methoxyl-1,2,3,4-tetrahydronaphthalene (IV), and removing methyl of the (IV) under the effect of hydrobromic acid to obtain a target product rotigotine (-)-(S)-2-[N-propyl group-N-[2-(2-thiophene)ethyl]amino]-5-hydroxy-1,2,3,4-tetrahydronaphthalene (I), wherein the purity is higher than 99%. The novel process is simple in synthetic route, simple and convenient to operate and high in yield, and large-scale industrial production is easy to carry out.

The disclosure provides a composition comprising rotigotine or a pharmaceutically acceptable salt thereof; at least one poly(lactide-co-glycolide) (PLGA); and at least one fatty acid, wherein the at least one fatty acid is at least 0.5% in weight relative to the total weight of the composition. The composition as disclosed herein has significantly reduced burse release effect. The disclosure also provides a method of treating Parkinson's disease comprising administering an effective amount of the composition as disclosed to a subject in need thereof.

The invention provides a method for separating enantiomers of rotigotine and trihexyphenidyl. The method comprises the steps of dissolving dextran sulfate in a buffer solution, obtaining an operational buffer solution containing the dextran sulfate as a chiral selector, dissolving rotigotine to be separated and trihexyphenidyl as samples to be separated in the operational buffer solution and separating enantiomers of two medicaments through a capillary electrophoresis instrument. The method is characterized in that the adopted chiral selector is the dextran sulfate of which the molecular weight is 500,000 or 1,000,000, and is low in background ultraviolet absorption, cheap and readily available. The adopted method has the advantages of high separation efficiency, low reagent consumption, environment-friendly property, convenient operation, capability of realizing the chiral separation of the enantiomers in a forward or backward voltage mode, as well as opposite transfer order of the enantiomers in two modes. The method is high in the degree of separating the enantiomers of the two medicaments.

The invention belongs to the technical field of medicine, and relates to a rotigotine percutaneous absorption patch, and preparation and application thereof. The patch can obviously relieve a crystalseparation phenomenon of a rotigotine patch and provides good skin penetration delivery performance. The rotigotine percutaneous absorption patch consists of a back lining layer, a medicine loaded pressure-sensitive adhesive layer and an anti-bonding layer, wherein the medicine loaded pressure-sensitive adhesive layer comprises rotigotine free alkali or rotigotine organic acid ionic liquid, pressure-sensitive adhesives and a percutaneous absorption enhancing agent, wherein the weight of the rotigotine free alkali or rotigotine organic acid ionic liquid accounts for 2.0 to 20 weight percent ofthe total weight of the medicine loaded pressure-sensitive adhesive layer; the weight of the pressure-sensitive adhesives accounts for 77 to 90 weight percent of the total weight of the pressure-sensitive adhesive layer; and the consumption of the percutaneous absorption enhancing agent accounts for 0 to 10 weight percent of the total weight of the pressure-sensitive adhesive layer. In the rotigotine organic acid ionic liquid, a mol ratio of the rotigotine free alkali to different organic acids is 0.5:1-2:1. The rotigotine percutaneous absorption patch has the advantages that the accumulated penetration amount of rotigotine in 24h can reach 0.5mg/cm<2>. The preparation technology of the patch is simple; the stability of the patch is high; and the use is convenient.

The invention discloses a transdermal patch composition containing rotigotine, and more specifically discloses a transdermal patch containing rotigotine, and a preparation method thereof. The transdermal patch composition contains effective doses of rotigotine and a self-adhesive matrix; the self-adhesive matrix comprises a polyisobutylene pressure-sensitive adhesive and a colloid softener. According to the preparation method, the polyisobutylene pressure-sensitive adhesive is adopted, the C-H skeleton of the polyisobutylene pressure-sensitive adhesive is long and straight, only the terminal groups contain unsaturated bonds, double bond content is low, and reaction sites are few, so that the transdermal patch containing rotigotine is extremely stable, is excellent in weatherability, heat resistance, and aging resistance, is low in cost; the materials are easily available; the operationality is high; the colloid softener is added, so that the stability of the transdermal patch containing rotigotine is improved, and precipitation of drug active components out from the transdermal patch containing rotigotine is prevented; and in addition, an adhesiveness conditioning agent is added, so that the permeability of the transdermal patch containing rotigotine is excellent.

The present invention describes a novel process for the preparation of (6S)-(−)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine) comprising: (a) acetylating (S)-(−)-5-hydroxy-N-n-propyl-2-aminotetraline to afford the acetate; (b) reacting this acetate, (−)-5-acetoxy-N-n-propyl-2-aminotetraline, with 2-(2-thienyl)ethanol 2-nitrobenzenesul-fonate; (d) hydrolyzing (6S)-(−)-1-acetoxy-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthalene to afford (6S)-(−)-5,6,7,8-tetrahydro-6-[propyl-(2-thienypethyl]amino-1-naphthol (Rotigotine) and (d) purifying rotigotine either by the acetylation reaction and subsequent hydrolysis of the formed acetate or by salification of rotigotine through hydrochloride or hydrobromide formation and subsequent base release. Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.