130 results about "Pramipexole" patented technology

The present invention is directed to compositions comprising pramipexole and the use of such compositions to treat neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). As shown in FIG. 6B the mean + / − SEM serum 2,3-DHBA levels for the 12 ALS participants decreased significantly after pramipexole treatment.

Formulations and methods of use thereof for restoring neuronal, muscular (cardiac and striated) and / or retinal tissue function in children and adults afflicted with chronic neurodegenerative diseases, such as neurodegenerative movement disorders and ataxias, seizure disorders, motor neuron diseases, and inflammatory demyelinating disorders, are described herein. Examples of disorders include Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). The method involves administering a pharmaceutical composition containing an effective amount of a tetrahydrobenzathiazole, preferably a formulation consisting substantially of the R(+) enantiomer of pramipexole. R(+) pramipexole is generally administered in doses ranging from 0.1-300 mg / kg / daily, preferably 0.5-50 mg / kg / daily, and most preferably 1-10 mg / kg / daily for oral administration. Daily total doses administered orally are typically between 10 mg and 500 mg. Alternatively, R(+) pramipexole can be administered parenterally to humans with acute brain injury in single doses between 10 mg and 100 mg, and / or by continuous intravenous infusions between 10 mg / day and 500 mg / day.

Formulations and methods of use thereof for restoring neuronal, muscular (cardiac and striated) and / or retinal tissue function in children and adults afflicted with chronic neurodegenerative diseases, such as neurodegenerative movement disorders and ataxias, seizure disorders, motor neuron diseases, and inflammatory demyelinating disorders, are described herein. Examples of disorders include Alzheimer's disease (AD), Parkinson's disease (PD), and amyotrophic lateral sclerosis (ALS). The method involves administering a pharmaceutical composition containing an effective amount of a tetrahydrobenzathiazole, preferably a formulation consisting substantially of the R(+) enantiomer of pramipexole. R(+) pramipexole is generally administered in doses ranging from 0.1-300 mg / kg / daily, preferably 0.5-50 mg / kg / daily, and most preferably 1-10 mg / kg / daily for oral administration. Daily total doses administered orally are typically between 10 mg and 500 mg. Alternatively, R(+) pramipexole can be administered parenterally to humans with acute brain injury in single doses between 10 mg and 100 mg, and / or by continuous intravenous infusions between 10 mg / day and 500 mg / day.

An extended release tablet formulation comprising pramipexole or a pharmaceutically acceptable salt thereof in a matrix comprising at least one water swelling polymer other than pregelatinized starch.

The invention discloses a preparation process of pramipexole, namely enantiomers or racemates of 2-amino-6-acrylamido-4,5,6,7-tetrahydrobenzothiazole. The pramipexole is prepared from 2-amino-6-propionylamino-4,5,6,7-tetrahydrobenzothiazole as the raw material by the reduction reaction with a reducing agent. The process has easy operation, and mild reaction condition, is easy to control, and greatly improve the safety of production.

An extended release pellet comprising an active ingredient selected from pramipexole and the pharmaceutically acceptable salts thereof, and at least one release-modifying excipient.

The invention relates to a method for preparing 4- substituted acylamino cyclohexanone through oxidizeing 4- substituted acylamino cyclohexanol. The 4- substituted acylamino cyclohexanone prepared by the method can be used for preparing Pramipexole. The method comprises the following steps: adding 4- substituted acylamino cyclohexanol as is shown in formula I, catalyst 2, 2, 6, 6- tetramethyl piperidine - nitrogen - oxide, NaBr, into organic solvent, then dropwise adding sodium hypochlorite water solution for reaction until oxidation reaction is complete, and obtaining the 4- substituted acylamino cyclohexanone shown in formula II after separation and purification to reaction solution; and the method provided by the invention mainly has the following benefits: a novel chemical synthesis method for producing key intermediate of medicine Pramipexole is found, the route is enabled to be more reasonable, the reaction conditions are milder, the yield is higher, and the method is environment-friendly and suitable for large scale industrial production.

Pharmaceutical compositions of (R)-pramipexole and methods and kits of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.

A pharmaceutical composition for transdermal or transmucosal delivery of an active agent to treat a movement disorder such as Parkinson's disease. The composition provides enhanced transdermal or transmucosal delivery of the active agent by including an alkanolamine as a permeation enhancer with a carrier of water and at least one short-chain alcohol and with the composition having a neutral pH. The composition provides controlled and sustained release of the active agent suitable for daily administration.

The invention relates to a pramipexole preparation which comprises pramipexole or a medicinal salt thereof which accounts for 0.05 to 1.5% of the total weight of the preparation and is used as an active component, microcrystalline cellulose and pregelatinized starch, wherein a weight ratio of microcrystalline cellulose and pregelatinized starch is 1:1 to 1: 5. The invention also relates to a preparation method for the pramipexole preparation. The preparation prepared by using the preparation method has low hygroscopicity and is beneficial for storage; and the preparation method has good production feasibility and is suitable for commercial production.

Modified release pharmaceutical compositions (controlled release, sustained release, and / or extended release) of the R-(+) enantiomer of pramipexole (RPPX) and methods of using such compositions for the treatment of neurodegenerative diseases, or those related to mitochondrial dysfunction or increased oxidative stress are disclosed.

The invention relates to an active substance combination consisting of clonidine and pramipexole for treating Restless Leg Syndrome.

The invention relates to a pramipexole sustained-release preparation for injection and a preparation method thereof, belonging to the technical field of medicines. The preparation method comprises thefollowing steps: dissolving a main drug and an internal water phase additive into water for injection so as to form a main drug-containing internal water phase solution; dissolving PLGA and an organic phase additive into an organic solvent so as to form an organic phase solution; mixing the main drug-containing internal water phase solution with the organic phase solution and carrying out ultrasonic treatment so as to form a primary water-in-oil emulsion; adding the primary water-in-oil emulsion into an external water phase solution, and carrying out stirring so as to form a water-in-oil-in-water multiple emulsion; solidifying the water-in-oil-in-water multiple emulsion so as to form microspheres, carrying out centrifugal washing, and collecting the microspheres so as to obtain wet microspheres; adding a gel solution and a freeze-drying protective agent into the wet microspheres so as to obtain a microsphere gel solution; and subjecting the microsphere gel solution to freeze-drying. The pramipexole sustained-release preparation for injection provided by the invention has high drug loading capacity and good temperature sensitivity and biological compatibility, sustainably and stably releases drugs, can effectively reduce the occurrence of motor complications, and improves the compliance of a patient.

The invention discloses a transdermal patch containing pramipexole. The transdermal patch comprises a medicine carrying pressure-sensitive adhesive layer, the pramipexole, solvent and penetration enhancer, wherein the medicine carrying pressure-sensitive adhesive layer comprises acrylate pressure-sensitive adhesive containing carboxyl base groups and acrylate pressure-sensitive adhesive containing hydroxyl base groups, which form mixed pressure-sensitive adhesive; the pramipexole is dissolved in the acrylate mixed pressure-sensitive adhesive, with the content being 10 to 30 weight percent; the content of the mixed pressure-sensitive adhesive is 50 to 80 weight percent; the content of the solvent is 5 to 20 weight percent; the content of the penetration enhancer is 2 to 15 weight percent. The pramipexole can be dissolved in a mixed pressure-sensitive adhesive patch in a high concentration way and is not crystallized, the medicine availability is high, the pramipexole has good stability in pressure-sensitive adhesive matrix, and can be continuously administrated for 5 to 7 days in a transdermal way at a relatively stable permeation rate of being larger than 5.0 micrograms / cm2 / h, and the application area of a pramipexole patch is smaller than 40cm2.

The invention relates to the use of dopamine receptor agonists for preparing a pharmaceutical composition for reducing excessive food intake.