73 results about "Ranolazine" patented technology

This invention relates to methods for treating a patient suffering from neuropathic or nociceptive pain which may be mechanical, visceral, and / or inflammatory in nature, comprising administering a therapeutically effective amount of Ranolazine to a patient in need thereof.

The present invention relates to a method for the treatment or prevention of atrial fibrillation and / or atrial flutter comprising coadministration of a synergistically therapeutic amount of dronedarone or a pharmaceutically acceptable salt or salts thereof and a synergistically therapeutic amount of ranolazine or a pharmaceutically acceptable salt or salts thereof. Also provided are methods for modulating ventricular and atrial rhythm and rate. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

The present invention relates to a method for the treatment of atrial fibrillation comprising the coadministration of a synergistic therapeutically effective amount of amiodarone and synergistic therapeutically effective amount ranolazine. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below pH 4.5 and soluble in aqueous media above pH 4.5. The formulation is suitable for twice daily administration of ranolazine and is useful for controlling the rate of dissolution of ranolazine, and to maintain human plasma ranolazine levels at between 850 and 4000 ng base / mL.

Disclosed are novel ranolazine sustained release pharmaceutical formulations.

The present invention relates to method of reversing left ventricle remodeling by combined administration of therapeutically effective amounts ranolazine and at least one co-remodeling agent, which may be an ACE inhibitor, an ARB, or a beta-blocker. The method finds utility in the treatment of heart failure. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

Disclosed are methods for treating patients suffering from coronary microvascular disease comprising administering ranolazine to the patient. In one embodiment, ranolazine is administered as an oral dose

Disclosed are methods for treating patients suffering from non-coronary microvascular disease comprising administering ranolazine to the patient. In one embodiment, ranolazine is administered as an oral dose.

The present invention relates to method of reversing left ventricle remodeling by combined administration of therapeutically effective amounts ranolazine and at least one co-remodeling agent, which may be an ACE inhibitor, an ARB, or a beta-blocker. The method finds utility in the treatment of heart failure. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

This invention relates to a method for synthesizing ranolazine drug for treating stenocardia. The method comprises: performing amidation and N-monoalkylation on 2, 6-dimethylaniline to obtain N-(2, 6-xylyl)-2-(1-piperazine) acetamide, and then reacting with 2-(2-methoxyphenoxy) epoxyethane generated from o-methoxyphenol and epoxy chloropropane to obtain anolazine. The reactions include the refinery of 2-chloro-N-(2,6-xylyl)acetamide by cyclohexane and the recrystallization of ranolazine by ethanol / ethyl acetate (2:1), thus can raise the yield.

The invention discloses an improved method for synthesizing an antianginal medicine ranolazine and belongs to the field of pharmaceutical chemistry. The method comprises the following steps of: amidating 2,6-dimethylaniline which is taken as a raw material, and alkylating to obtain N-(2,6-dimethylphenyl)-2-(1-piperazino)-acetamide; and reacting the N-(2,6-dimethylphenyl)-2-(1-piperazino)-acetamide and 2-(2-methylphenoxymethyl)ethylene oxide which is obtained by reaction of 2-methoxyphenol and epichlorohydrin to obtain crude ranolazine, and recrystallizing to obtain refined ranolazine. A reaction solvent, the molar ratio of raw materials, a phase transfer catalyst, a recrystallization solvent and the like are optimized; and the improved method is convenient to operate and is suitable for industrialized production, the production cost is reduced, and the yield is improved.

The invention discloses a preparation technology and a refining method of ranolazine, which are more suitable for industrial production. The method comprises the following concrete steps: using 2, 6-dimethylaniline and methylpyrocatechine as original materials; sequentially carrying out four reaction processes of N-acylation, O-alkylation, N-alkylation and N-alkylation to synthesize ranolazine; and then, recrystallizing to obtain a refined product. The refined product obtained by the method has high purity, and the method also has the advantages of simple operation, low production cost and high yield and is more suitable for industrial production.

Preparation of ranolazine and intermediates thereof, for use in pharmaceutical compositions comprising ranolazine.

The invention provides a Ranolazine oral sustained-release preparation and a preparation method. The Ranolazine oral sustained-release preparation comprises Ranolazine, a sustained-release skeleton material, a filling agent, an adhesive and a lubricating agent, and is characterized in that the weight of the Ranolazine is between 35 and 85 percent in the sustained-release preparation; a prescription composition is preferably selected according to a large number of experiments; hydroxypropyl methyl cellulose phthalate and methyl cellulose are served as the sustained-release skeleton material ofthe sustained-release preparation in the preferable weight ratio of 2:1-1.5; and microcrystalline cellulose is served as the filling agent; the 29 / 39 ethanol solution of polyvinyl pyrrolidone K is served as the adhesive, and magnesium stearate is served as the lubricating agent.

The present invention provides a pharmaceutical composition containing active ingredients ivabradine or a pharmacologically acceptable salt thereof and ranolazine or a pharmacologically acceptable salt thereof. Through research, the present invention finds that the combined use of ivabradine and ranolazine effectively alleviates myocardial ischemia, and shows a good synergistic effect on myocardial ischemia diseases such as angina pectoris and coronary heart disease. Therefore, a method for treating myocardial ischemic diseases with better effect and lower adverse reactions has been found, and a good solution has been found for the unsatisfactory treatment effect of myocardial ischemic diseases in clinical practice.

A process for the preparation of Ranolazine (I) and its acid addition salts and the process for the preparation of compound of formula (7).

Disclosed are novel ranolazine sustained release pharmaceutical formulations.

The invention is directed to methods for enhancing endogenous insulin levels in a patient in need thereof which method comprises administering to the patient an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine. It is also directed to methods of treatment comprising racemic ranolazine or the R- or S-enantiomer of ranolazine for enhancing endogenous insulin levels in a patient in need thereof. It is also directed to a composition comprising an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine and at least one anti-diabetic agent.

The invention discloses a method for synthesizing an anti-angina medicament, namely ranolazine, which comprises the following steps that: N-(2,6-dimethylphenyl)chloracetamide is taken as an initial raw material and is condensed with piperazidine, and then the aminolysis reaction of the obtained product and 1-(2-methoxyphenoxyl)-2,3-propylene oxide is performed to obtain a product, namely the ranolazine. During the preparation of an intermediate, namely N-(2,6-dimethylphenyl)-2-(1-piperazinyl)acetamide, the invention improves an operation method, simplifies operation steps, and improves the yield of products.

The present invention relates to a method for reducing the toxicity of cardiac glycosides comprising the coadministration of a therapeutically effective amount of cardiac glycoside and a therapeutically effective amount ranolazine. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

The invention relates to a ranolazine sustained release tablet medicine composition and a preparation method thereof. The composition comprises, by weight, 50%-72% of ranolazine, 20%-25% of pH dependence binding agents, 5%-8% of non-pH-dependence binding agents, 2%-15% of microcrystalline celluloses, 0.1%-0.5% of magnesium stearate and 0.1%-0.5% of sodium hydroxide. The preparation method includes the steps of mixing, palletizing, particle wrapping, drying, tidying, tabletting, tablet core wrapping and the like. The preparation method s easy and convenient, industrialization is easily achieved, and the prepared ranolazine sustained release tablet medicine composition has the beneficial effects of being good in slow-release effect, light in tablet weight and the like.

The invention is directed to methods for enhancing endogenous insulin levels in a patient in need thereof which method comprises administering to the patient an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine. It is also directed to methods of treatment comprising racemic ranolazine or the R- or S-enantiomer of ranolazine for enhancing endogenous insulin levels in a patient in need thereof. It is also directed to a composition comprising an insulin secretion-enhancing amount of racemic ranolazine or the R- or S-enantiomer of ranolazine and at least one anti-diabetic agent.

The invention relates to a Reynolds pyrazine slow-released tablet, which is characterized in that the tablet comprises not more than 50wt% Reynolds pyrazine and at least an independent adhesive with 1-20wt% low viscosity PH and a or a plurality of independent adhesive with 1-20wt% high viscosity PH.

The present invention discloses one kind of slow releasing ranolazine micro pill including ranolazine and supplementary material. It consists of coating and isolating layer in 5-30 %, preferably in 10 % and pill core in 70-95 %, preferably in 90 %. The slow releasing ranolazine micro pill is tested to have release amount of 20-40 % within 2 hr, 50-80 % within 6 hr, and 80-100 % within 12 hr.

An orally-applied ranolazine hydrochloride for treating cardiovascular disease is prepared from ranolazine hydrochloride, diluent, adhesive, disintegrant, antisticking agent and lubricant through adding wetting agent, preparing soft material, granulating and drying.

The invention discloses a method for separating chiral compound ranolazine by adopting a simulated moving bed in a fourth region. The method is characterized by adopting a simulated moving bed chromatography system, taking cellulose-tris(3,5-dimethylphenylcarbamate) as a filler and methanol as a mobile phase and separating high-purity R-ranolazine and S-ranolazine from racemes of ranolazine. The simulated moving bed chromatography system has the advantages of continuous production, high degree of automation and high production efficiency.

The invention provides a medical composition containing ivabradine or pharmacologically acceptable salts and ranolazine or pharmacologically acceptable salts thereof. Proved by research, the medical composition effectively relieves myocardial ischemia and has good synergetic effect on myocardial ischemia diseases, such as angina, coronary heart disease, and the like by the combined use of the ivabradine and the ranolazine. Thus, a method for treating myocardial ischemia diseases with good effect and low adverse reaction is found. The invention finds a good solution for treating myocardial ischemia diseases clinically with poor effect at present.

The invention provides a ranolazine quick-release mini-pill preparation and a preparation method thereof, and relates to the fields of a medicine preparation technology and application. The administration mode of the quick-release mini-pill preparation is oral administration, a blank pill core serves as a carrier, a ranolazine aqueous solution containing a cosolvent and adhesive is a medicine applying solution, and the use amount of the ranolazine is 0.01 to 0.3 percent of the weight of the pill core according to the weight ratio; and the oral dosage of the ranolazine is not more than 100 micrograms. The ranolazine quick-release mini-pill preparation has the characteristics of high medicine applying rate, high content uniformity, quick medicine release, quick response of analgesic effect and the like. Meanwhile, the quick-release mini-pill preparation has the characteristics of high clinical use compliance, high safety and the like. In addition, the blank pill core fluidized bed medicine applying method is suitable for preparation of a ranolazine medicine oral preparation with extremely low specification.