241 results about "Rosuvastatin" patented technology

A pharmaceutical composition comprising, in relation to 100% by weight of a total amount of a self-emulsifying composition, 70 to 90% by weight of eicosapentaenoic acid ethyl ester as a first medicinal component, 0.5 to 6% by weight of water, 1 to 29% by weight of polyoxyethylene sorbitan fatty acid ester (optionally further comprising polyoxyethylene castor oil) as an emulsifier, 1 to 25 parts by weight of lecithin in relation to 100 parts by weight of the eicosapentaenoic acid ethyl ester, and pitavastatin, rosuvastatin, or a salt thereof as a second medicinal component. The composition is excellent in any one of self-emulsifying property, dispersibility of the composition, emulsion stability, absorbability, and storage stability of the medicinal components and a preparation.

Intermediate compounds for preparing rosuvastatin are prepared by a process comprising oxidizing hydroxy groups to aldehyde groups, using sodium hypochlorite and 2,2,6,6-tetramethyl piperidinyl oxy free radical (TEMPO) as a catalyst.

The present invention relates to pharmaceutical compositions in particulate form or in solid dosage forms comprising a combination of fenofibrate and the HMG CoA reductase inhibitor rosuvastatin or a pharmaceutically active salt thereof, which upon oral administration provides a relative AUC_0-24 value (AUC_{fibric acid}/AUC_rosuvastatin) of between about 150 and about 12,000. The solid compositions are manufactured without any need of addition of water or aqueous medium and comprise at least 80% of the active substances fenofibrate and rosuvastatin in dissolved form, or, optionally, atorvastatin in micronized form, in order to ensure suitable bioavailability.

The present invention relates to a preparation method of medicine for reducing blood-lipid-Reshufatadine compound. Said method uses side chain aldehyde compound and triphenyl phosphorus ylide reagent compound and makes them undergo the condensation reaction so as to obtain Reshufatadine compound with high yield. Said invention also provides its key intermediate compound.

The present invention relates to a cost effective and industrially advantageous process for the preparation of 4-4(fluorophenyl)-6-isopropyl-2-(N-methyl-N-methylsulphonylamino)-5-pyrimidinecarboxaldehyde, referred to here as pyrimidine aldehyde of structural Formula I and to the use of this compound as intermediate for the preparation of rosuvastatin.

The present invention discloses new preparation process of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfothio) amino] pyrimidyl-5-radical] -(3R.5S)-3,5-dihydroxy heptyl-6-olefine acid (Rosuvastatin) and its medicinal salt, and new intermediate. The preparation process has short period, less reaction steps, high yield and low cost.

The present invention relates to formulations comprising therapeutically effective amounts of at least one acid-stable, carrier-mediated transport statin, at least one poorly water-soluble, carrier-mediated transport statin, or at least one large molecular weight, carrier-mediated transport statin, such as atorvastatin and rosuvastatin, or a pharmaceutically acceptable salt thereof, and methods of their use. The present formulations and methods are designed to exhibit a controlled-release of a therapeutic amount of the statin in the small intestine, thereby limiting systemic exposure of the statin and maximizing liver-specific absorption of the drug. The formulations and methods of the present invention are particularly useful for treating and/or preventing conditions that are benefited by decreasing levels of lipids and/or cholesterol in the body.

The invention discloses a quinolinic compound showed in the formula A and pharmacy acceptable solvate, optical isomers or polymorphic substance and a reaction intermediate compound showed in the formula D; wherein, R1, R2 and R3 are respective and independent H, halogen or group showed in the formula H; wherein, the R is H, the halogen, alkyl of C1-C4 or alkoxide of C1-C4. The invention further discloses a preparation method thereof and application for preparing medicines for inhibiting HMG CoA reductase and treating hyperlipemia related diseases. Compared with the existing fuvastatin, rosuvastatin and pitavastatin in the prior art, the quinolinic compound of the invention can better inhibiting the activity of the HMG CoA reductase and can be used for treating hyperlipemia related diseases.

Provided are intermediates and process for the preparation of statins, preferably rosuvastatin.

The invention provides a method for preparing a Rosuvastatin intermediate, 4-Fluorophenyl-6-isopropyl-2-(N-methyl-N-methylsulfonyl amino) pyrimidinyl-5-formyl. The method uses isobutyryl acetonitrile, 4-Fluorobenzaldehyde and carbamide as raw materials and is obtained by steps of cyclization, oxidation, substitution and reduction etc. The method of the invention dose not need expensive raw materials and has the advantages of low technological cost, simple reaction, high product yield and being applicable to industrialized production.

Provided is a composite formulation comprising: (i) a core including a first pharmacological component; and (ii) a film coating layer formed on a surface of the core, which contains rosuvastatin or a pharmaceutically acceptable salt thereof as a second pharmacological component and a polyvinyl alcohol-polyethylene glycol graft copolymer and polyvinyl alcohol as a coating material. In the composite formulation of the present invention, tension and fluidity of the film coating layer are excellent, and thus breakage and a defective ratio are low. Accordingly, a composite agent containing rosuvastatin effective to relieve and treat a hyperlipemia symptom, or its pharmaceutically acceptable salt can be provided with high efficiency, and is present in a composite formulation form, and thus compliance of a patient can be improved.

The invention belongs to the filed of medicine and discloses a pharmaceutical composition using fimasartan and rosuvastatin or medicinal salt thereof as active components, wherein a mass ratio of rosuvastatin or medicinal salt thereof to fimasartan is 1:0.25-250 and preferably 1:10-100. The pharmaceutical composition containing rosuvastatin medicinal salt thereof and fimasartan has obvious synergism on treating hypertension and complications thereof, low treatment cost, little side-effect and good clinic application prospect.

The invention relates to a method for preparing a rosuvastatin intermediate which is (R)-3-hydroxy-monomethyl glutarate and hydroxyl-protected (R)-3-hydroxy- monomethyl glutarate. According to the method, (R)-4-cyano-3-hydroxy-methyl butyrate which servers as a substrate is subjected to reaction under the action of an enzyme to generate the (R)-3-hydroxy- monomethyl glutarate, and particularly the enzyme is the recombinant nitrilase, and the reaction is carried out in a aqueous-phase buffering solution with the pH value of 7.0-9.0 at the temperature of 25-35 DEG C. Because the specific recombinant nitrilase is adopted by the method, the problems of ultralow concentration of the substrate and low conversion rate in the existing method for preparing the rosuvastatin intermediate through biological catalysis are solved. The method has the characteristics of mild reaction conditions and high reaction efficiency, is easy and convenient to operate and has important industrial application value.

A pharmaceutical composition is an organic salt formed by an organic acid rosuvastatin and an organic base azelnidipine with a molar ratio of 1:1. The pharmaceutical composition can be made into any dosage forms together with a pharmaceutically-acceptable carrier for reducing blood pressure and blood lipid, reducing myocardial infarction and treating cerebral apoplexy. The inventive pharmaceutical composition has the advantages of stable physiochemical indexes, controllable product quality, and convenient administration.

The invention relates to a double-layer tablet which contains ezetimibe and rosuvastatin serving as effective components and has a lipid-lowering effect and a preparation method thereof. Aiming at the problems poor water solubility of ezetimibe, instability of rosuvastatin to acid and oxygen and the like, the method adopts a micronization technology to improve the dissolution rate of ezetimibe and adopts an anti-oxidizing agent and a double-layer tabletting technology to improve the stability of rosuvastatin in a human body, further, ingredients of a medicine is enabled to take effect sufficiently, and the best synergistic effect is achieved; and a compound preparation agent is mainly applied to treatment of diseases relative to hypercholesteremia.

The invention relates to a pharmaceutical composition containing a calcium channel blocker (CCB) or the mixture thereof, an angiotonin 3II receptor blocker (ARB) or the mixture thereof, statins or the mixture thereof and a pharmaceutically acceptable carrier, wherein the CCB is selected from l-amlodipine, amlodipine, lacidipine, nitrendipine or the mixture thereof; the angiotonin II receptor blocker is selected from telmisartan, losartan, irbesartan, candesartan or the mixture thereof; and the statins are selected from atorvastatin, simvastatin, ruishufatadine, fluvastatin or the mixture thereof. The pharmaceutical composition is used for treating various high blood pressures and preventing or treating cardiovascular and cerebrovascular diseases relevant to the hypertension, reduces the disease rate and/or mortality rate of the cardiovascular and cerebrovascular diseases and also improves the adaptability for a sufferer taking medicine.

The invention relates to a pharmaceutical composition containing amlodipine besylate, and a statins compound or a pharmaceutically acceptable salt thereof, a preparation method and a medicine box for drug combination of the medicine composition. The composition comprises the following components: a) a certain amount of the amlodipine besylate; b) a certain amount of one or more statins compounds or pharmaceutically acceptable salts thereof; and c) a pharmaceutically acceptable carrier or a diluting agent. The composition or the medicine box can be used for treating patients suffering from angina pectoris, atherosclerosis and/or accompanied hypertension and hyperlipoidemia, and treating patients (including human beings) having heart risky symptoms.

The present invention provides rosuvastatin and intermediates thereof having a low level of alkylether impurity and processes for the preparation thereof.

The present invention relates to a medicine composition conlaining resulvatatine or pivatatine compound and vitamins B, in which the resulvatatine or pivatatine content is 1-40 mg and vitamins B content is 0.1-50 mg. Said invention also provides the application of said medicine composition in preparation of medicine for preventing and curing the diseases of atherosclerosis, angiocardiopathy and cerebrovascular disease.

The invention relates to a new method of biologically synthesizing (R)-3-hydroxylglutarate monoester and more particularly provides a method of preparing the (R)-3-hydroxylglutarate monoester from (S)-4-chloro-3-hydroxybutyrate through halogenohydrin dehalogenase recombinant bacteria and nitrilase recombinant bacteria, or double-enzyme co-expression recombinant bacteria, in a one-pot manner. The (R)-3-hydroxylglutarate monoester is a key intermediate of statin medicines such as fluvastatin, rosuvastatin, pitavastatin and the like. The method is mild in reaction conditions, is free of pollution and is simple in process route.

The invention relates to commercially viable process for the preparation of Rosuvastatin by an early introduction of the correct absolute stereochemistry at C-5 (S) of Rosuvastatin side chain followed by regioselective chain extension using novel side chain building blocks. It is yet another object of the invention is to provide novel intermediates that may be used for the preparation of Rosuvastatin. Formula (I).