48 results about "Ropinirole" patented technology

The present invention comprises compositions for pharmaceutical drug delivery of an indolone (e.g., ropinirole), or a pharmaceutically acceptable salt thereof. The composition may, for example, be a gel suitable for transdermal application. The compositions of the present invention typically comprise a hydroalcoholic vehicle, one or more antioxidant, and one or more buffering agent, wherein the pH of the gel is usually between about pH 7 and about pH 9. The compositions may include further components, for example, the hydroalcoholic vehicle may further comprise additional solvent(s), antioxidant(s), cosolvent(s), penetration enhancer(s), buffering agent(s), and/or gelling agent(s). The compositions may be used for the treatment of a variety of neurological disorders.

The present invention discloses a novel process and novel intermediates for the Preparation of 4-[2-(di-n-propyl amino) ethyl]-1,3-dihydro-2H-indol-2-one, commonly known as Ropinirole (I) and pharmaceutical composition comprising the same. Further the present invention also discloses a method of treatment for cardiovascular disorders and Parkinson's disease.

The present, invention relates to a transdermal absorption preparation. The transdermal absorption preparation of the present invention comprises a drug-containing adhesive layer, a drug-protective layer and a release layer, wherein the drug-containing adhesive layer contains ropinirole or a salt thereof, rubber, an adhesion-imparting resin, an antioxidant, and a transdermal absorption promoter. Also, the present invention provides a transdermal absorption preparation comprising a drug-containing adhesive layer, a drug-protective layer, and a release layer, wherein the drug-containing adhesive layer contains ropinirole or a salt thereof, acrylic rubber, an anti-crystallisation agent, and a transdermal absorption promoter. When the transdermal absorption preparation of the present invention is used for the treatment of Parkinson's disease or restless leg syndrome, no side effect due to an increase in the initial drug concentration in blood occurs and the skin penetration effect of the drug is excellent.

The invention discloses a ropinirole hydrochloride osmotic pump type controlled release preparation and a preparation method thereof. The osmotic pump controlled release preparation consists of three parts: tablet core, semipermeable membrane and drug release hole. The tablet core is composed of ropinirole, osmotic pressure enhancer and other excipients, the semipermeable membrane contains film-forming materials and plasticizers, and the hole-making methods include mechanical drilling and laser drilling. Through the joint application of osmotic pressure enhancers and the adjustment of semi-permeable membrane parameters, the drug release rate can be controlled. After oral administration, the ropinirole osmotic pump-type controlled-release tablet can release the drug continuously for 24 hours or longer, which is more conducive to the clinical treatment of Parkinson's patients and is convenient for patients to take the drug.

A method for producing a patch comprising a support layer and an adhesive agent layer arranged on at least one surface of the support layer, the method comprising:

• • step A) obtaining an adhesive agent layer composition comprising free ropinirole in an amount which results in a content of 5 to 13.2% by mass in an obtained adhesive agent layer;
  • step B) heating the adhesive agent layer composition at a temperature in a range from 50 to 76° C. for 5 minutes to 24 hours; and
  • step C) cooling the heated adhesive agent layer composition to normal temperature at an average rate of temperature drop of 1 to 20° C./hour, thereby obtaining the adhesive agent layer comprising the free ropinirole at a supersaturated concentration in a dissolved form.

A therapeutic method for preserving the dopaminergic function of patients suffering from Parkinson's disease, which method comprises administering an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof to a human or animal patient in need thereof. Typically, said patient has had Parkinson's disease for a period of less than three years since diagnosis. Preferably the invention comprises administering to said patient an effective amount of ropinirole or a pharmaceutically acceptable salt or solvate thereof, optionally in combination with one or more other dopamine agonists, in the absence of levodopa or any other dopamine precursor, and thereafter treating the patient with levodopa.

The invention discloses a preparation method of a solid pharmaceutical composition containing ropinirole or derivatives of ropinirole. The preparation method is characterized by comprising the following steps: firstly, dissolving the ropinirole or derivatives of ropinirole into a proper solvent, then adding the solution to a pharmaceutically acceptable carrier; evenly mixing, drying and then mixing with other materials, and finally preparing into an oral solid preparation. By adopting the method, ropinirole can be rapidly dissolved out, the problems of complicated preparation process and poor content uniformity in the preparation process of the ropinirole preparation can be effectively solved; meanwhile, the stability of ropinirole is not affected.

The invention relates to a method for purifying ropinirole hydrochloride (4-2-di-n-propylaminoethyl-1,3-dihydro-2H-indole-2-ketohydrochloride). The method comprises the following steps of: adding ropinirole hydrochloride containing an oxidized impurity structural formula (I) into water, adding an organic solvent, stirring and dissolving at room temperature, adding alkali, stirring, standing, demixing, and removing an aqueous layer; drying the obtained organic layer by using anhydrous magnesium sulfate, adding active carbon, stirring, filtering and concentrating; and adding a certain quantity of organic solvent into the obtained oily matter after concentrating to be dry, slowly adding a certain quantity of concentrated hydrochloric acid, stirring, cooling the solution, performing throwing filtration, and drying, thus obtaining the ropinirole hydrochloride. By adopting the method, oxidized impurities (I) can be effectively removed from the ropinirole hydrochloride, and the ropinirole hydrochloride can be obtained with high yield and purity, so that the oxidized impurities are controlled and the purity of the ropinirole hydrochloride reaches the medicinal standard.

The subject invention describes a method of use of Ropinirole™ to alleviate and control menopausal symptoms in women, and in particular, hot flashes. The invention describes the use of Ropinirole as a dopamine agonist with affinity for the dopamine D₂, D₃, or D₄ receptors. Ropinirole may also be used to treat menopausal symptoms in conjunction with Tizanidine™ to further reduce the effects menopausal symptoms by providing a sedative and muscle relaxant effect which aids in sleep. The combination of Ropinirole and Tizanidine provides a useful new compound for treatment of menopausal symptoms that are most disruptive to the functioning in activities of daily living.

The invention discloses an oral solid medicine composition containing ropinirole. The oral solid medicine composition comprises a medicine containing part and hollow white granules, wherein the medicine containing part contains ropinirole and pharmaceutically acceptable carriers, and the hollow white granules contain no ropinirole and are formed by mixing pharmaceutically acceptable carriers. Theoral solid medicine composition can be prepared with simple process, has better uniformity of preparation content and stability and can be used for treating parkinson disease (PD).

The invention belongs to the technical field of medicinal chemistry and organic chemistry, and particularly relates to a method for preparing ropinirole hydrochloride. A novel compound 4 is synthesized by the aid of the method and is used as a raw material for preparing the ropinirole hydrochloride. The particular method includes dissolving the compound 4 in one or a plurality of types of ethyl alcohol/methanol/ethyl acetate to obtain liquid, adding Pd/C into the ethyl alcohol/methanol/ethyl acetate, and carrying out reaction to obtain compounds 5; dissolving the compounds 5, p-toluenesulfonylchloride and pyridine in one or a plurality of types of dichloromethane/trichloromethane/1, 2-dichloroethane/pyridine, and carrying out reaction to obtain compounds 6; dissolving the compounds 6, NaIand dipropyl amine in one or a plurality of types of DMF (dimethyl formamide)/DMSO (dimethylsulfoxide)/Toluene, and carrying out reaction to obtain ropinirole; dissolving the ropinirole in 1, 4 dioxane with hydrochloric acid, and carrying out reduced-pressure compression to obtain the ropinirole hydrochloride. A proportion of the compounds 5 to the p-toluenesulfonyl chloride to the pyridine is equal to 1:1.2:1.2. A proportion of the compounds 6 to the NaI to the dipropyl amine is equal to 1:1:1.2. The novel method for preparing the ropinirole hydrochloride has the advantages that the method includes simple and convenient steps and can be practically put into production, and raw materials for the ropinirole hydrochloride are simple and are easily available.

This invention provides that Ropinirole (4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one) possess potent urease inhibitory potential (in vitro) with 97.3% inhibition and IC₅₀=11.7+0.46 μM, when compared to the standard inhibitors i.e. acetohydroxamic acid (IC₅₀=41.5+1.50 μM), and thiourea (IC₅₀=21.0+0.50 μM).

The invention relates to a process for preparing Ropinirole and its salts.

A ropinirole-containing patch comprising an adhesive agent layer and a backing layer, wherein

• • the adhesive agent layer containing:
  • at least one selected from the group consisting of ropinirole and a pharmaceutically acceptable salt thereof;
  • a fatty acid metal salt having 7 or more carbon atoms; and
  • an adhesive agent.