36 results about "Isradipine" patented technology

Sustained release oral formulations of israpidine, methods of preparing same, and methods of using sustained release oral formulations to provide controlled delivery of israpidine. The sustained release oral formulations include israpidine and a sustained release polymer, and provide substantially zero order release of israpidine over an extended period.

A method and composition are provided for the treatment of an anorectal disorder and for controlling the pain associated therewith. The method comprises administering to a subject in need of such treatment therapeutically effective amounts of a calcium channel blocker either alone or together with a nitric oxide donor. Amlodipine, anipamil, barnidipine, benidipine, bepridil, darodipine, diltiazem, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, lidoflazine, manidipine, mepirodipine, nicardipine, nifedipine, niludipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, perhexiline, tiapamil, verapamil and pharmaceutically acceptable salts thereof, are suitable calcium channel blockers.

The present invention relates to an improved method for the manufacture of Isradipine, 4-(4-Benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid methyl 1-methylethyl ester. Which, involves reacting 2,1,3-benzoxadiazole-4-carboxaldehyde with methyl acetoacetate in the presence of acetic acid and piperidine in diisopropyl ether. To obtain the product 2-acetyl-3-benzofurazan-4-yl-acrylic acid methyl ester which is then reacted with isopropyl-β-aminocrotonate in ethanol at 25 to 35° C. to obtain the product.

The present invention provides systems, compositions and methods for treatment of dopaminergic disorders (e.g., Parkinson's disease) using the combination of a first compound that inhibits a voltage-gated calcium channel of the type Cav1.3 (e.g., a dihydropyridine such as isradipine), and a second compound that is monoamine oxidase inhibitor and / or is a nitric oxide synthase inhibitor (e.g., rasagiline or derivative thereof).

The invention discloses a method for preparing an isradipine capsule. The method comprises the following steps: dissolving an isradipine raw material according to the amount of a prescription in prescribed ethanol, and adding povidone K3 to stir and dissolve; putting prescribed pregelatinized starch and microcrystalline cellulose in a fluidized bed, starting a fan, regulating the air volume to excellent fluidizing, setting the air inlet temperature to be 35-40 DEG C, spraying the solution prepared in the step A when the material temperature rises to 25 DEG C to granulate; and finishing the prepared particles through a 30-mesh screen, adding magnesium stearate, uniformly mixing, and filling capsules with the particles. According to the method, the raw materials and the auxiliaries are used for preparing solid dispersion by adopting a spray drying mode, are prepared to form fine particles by one step, and are used for filling capsules, so that the dissolution in vitro of the capsule can be effectively increased, the production cost can be reduced, the bioavailability of the capsule can be improved, and a better clinical curative effect can be achieved.

The invention discloses a method for preparing high-purity isradipine. The method includes dehydrating and condensating 4-formaldehyde benzofuroxan in atent solvent to form 2-acetyl-3-benzofuroxan-4-base-isopropyl acrylate; subjecting methyl acetoacetate to ammonolysis to form 3-amino crotonic acid methyl ester; subjecting 2-acetyl-3-benzofuroxan-4-base-isopropyl acrylate and 3-amino crotonic acid methyl ester to reaction to form isradipine. The method for preparing high-purity isradipine is simple in operation process, convenient to operate, high in yield and capable of preparing high-purity isradipine.

The invention discloses an isradipine controlled-release tablet. The controlled-release tablet consists of an isradipine-containing controlled-release tablet core and a controlled-release coat. The invention provides an isradipine controlled-release tablet capable of delaying the release time, and solves the problem of obvious time dependence of the drug administration for cardiovascular diseases; and meanwhile, phosphatidylcholine is added to the tablet, thus the controlled-release tablet has a certain treatment effect on diabetic nephropathy.

The invention discloses an isradipine composition medicine, aiming at bringing the medicine pair function of isradipine and ferulic acid in medicine combination into play. The medicine comprises active components, namely, isradipine and ferulic acid, in a weight ratio of (5-10): (2-6); the medicine pair function of isradipine and ferulic acid in medicine combination is brought into play; good activity is shown in treating atherosclerosis, and the activity is superior to that of independent medication of isradipine and ferulic acid.

The present invention relates to a method for preparing isradipine, a drug for treating hypertension. Specifically, the method of the present invention comprises: (a) oxidizing 2-amino-3-methylnitrobenzene to close the ring to form 4-methylbenzofurazan oxide; (b) making 4-methylbenzofurazan oxide Reduction of furoxan oxide to form 4-methylbenzofurazan; (c) substituted bromination of 4-methylbenzofurazan to form 4-bromomethylbenzofurazan; (d) 4-methylbenzofurazan bromomethylbenzofurazan is hydrolyzed to form 4-hydroxymethylbenzofurazan; (e) 4-hydroxymethylbenzofurazan is oxidized to form 4-formaldehyde benzofurazan; and (f) ) reacts 4-formaldehyde benzofurazan with β-amino crotonic acid isopropyl ester, etc. to form isradipine. The method of the invention has high yield and simple operation, and can prepare high-purity isradipine.