78 results about "Fluvastatin" patented technology

A combination of one or more HMG-CoA reductase inhibitors (for example pravastatin, lovastatin, simvastatin, fluvastatin, rivastatin or atorvastatin) with one or more insulin sensitizers (for example troglitazone, pioglitazone, englitazone, BRL-49653, 5-(4-{2-[1-(4-2'-pyridylphenyl)ethylideneaminooxy]ethoxy}benzyl)thiazolidine-2,4-dione, 5-{4-(5-methoxy-3-methylimidazo[5,4-b]pyridin-2-ylmethoxy)benzyl}thiazolidine-2,4-dione or its hydrochloride, 5-[4-(6-methoxy-1-methylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione, 5-[4-(1-methylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione and 5-[4-(5-hydroxy-1,4,6,7-tetramethylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione) exhibits a synergistic effect and is significantly better at preventing and / or treating arteriosclerosis and / or xanthoma than is either of the components of the combination alone.

The present invention provides an aerosol formulation of a 3-hydroxy-3-methyl-glutaryl coenzyme A (HMG-CoA) reductase inhibitor. The HMG-CoA reductase inhibitor can be, for example, a statin such as lovastatin, pravastatin, simvastatin, cerivastatin, fluvastatin, atorvastatin or mevastatin. The invention also provides a method of treating a pulmonary disease with an aerosol formulation of a HMG-CoA reductase inhibitor.

A solid dispersion composition containing fluvastatin and a polymer is provided. Optionally, a surfactant is included. The fluvastatin appears to be amorphous and the solid dispersion composition enables fluvastatin to be constantly released over a time period.

Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, and some are obtained by treating the fermentation products using the methods of chemical synthesis or they are the products of total chemical synthesis. The aforementioned active substances may be destabilised by the environmental factors, their degradation may also be accelerated by interactions with other pharmaceutical ingredients, such as fillers, binders, lubricants, glidants and disintegrating agents, therefore the pharmaceutical ingredients and the process for preparation of the pharmaceutical formulation should be meticulously chosen to avoid the aforementioned undesired interactions and reactions. The present invention relates to a stable solid pharmaceutical formulation for the treatment of hypercholesterolemia and hyperlipidemia. More precisely, the present invention relates to the new stable solid pharmaceutical formulation containing as an active ingredient a HMG-CoA reductase inhibitor, such as atorvastatin, pravastatin, fluvastatin and cerivastatin or pharmaceutically acceptable salts thereof.

The invention belongs to the technical field of gene mutation detection, and concretely discloses a kit for simultaneously detecting SLCO1B1, APOE and LDLR gene multisite mutation. Through meticulous design, multi-time verification, screening and optimization, specific primers and probes based on a Taqman allelic gene resolution analysis method are obtained; eight functional variation of the SLCO1B1, APOE and LDLR genes can be detected; the time from DNA (Deoxyribonucleic Acid) extraction to fluorescent PCR (Polymerase Chain Reaction) to result obtaining is less than four hours; and the manual operation time is less than two hours. The kit comprising the primer pairs and the probe pairs has the advantages that the time is saved; convenience is realized; the sensitivity is high; and both the positive conformity rate and the negative conformity rate of a sample are higher than 99 percent, and the like. A detection method provided by the invention is mainly used for the personalized medication auxiliary diagnosis of statins such as simvastatin, atorvastatin, fluvastatin and rosuvastatin.

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.

The present invention relates to optically active boronate derivatives which are useful as intermediates for the synthesis of HMG-CoA enzyme inhibitors such as atorvastatin, cerivastatin, rosuvastatin, pitavastatin, and fluvastatin.

The present invention relates to new process for preparing as a key chiral intermediate compound of formula (I) obtained from an epoxy-β-hydroxy carboxylic acid ester of formula (II) prepared from epoxide compound of formula (III), in which said compound of formula (I) is useful for preparing the therapeutic agent for hyperlipidemia, such as Astrovastatin and Fluvastatin. Wherein R1 denotes a hydrogen atom, alkyl, aryl or alkylaryl, R2 and R3 which can be identical or different, are a lower alkyl or phenyl and are capable of forming a six-membered ring, R4 stands for hydroxy, amino, alkylamino, azido, cyano, halogeno, aryloxy, alkyloxy, arylalkyloxy, alkyl, alkenyl, aryl, or aminomethyl, etc.

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 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 present invention relates to improved pharmaceutical formulation for oral administration comprising a therapeutically effective quantity of an HMG-CoA reductase inhibitor, and more particularly Fluvastatin, Atorvastatin or salts thereof in combination with a linear sulphated polysaccharide such as Carrageenan and a method for the preparation thereof.

This invention discloses a method of preparing (3R,5S)- fluvastatin(I). The method includes using aldehyde of formula (III) and chiral side chain of formula (II) to carry out condensation reaction. Then obtain (3R,5S)- fluvastatin(I) by undoing protecting group, disoxidation and hydrolysis.

The invention relates to an osmotic pump preparation containing acipimox, fluvastatin and other pharmaceutical excipients, wherein, the acipimox is the controlled-release part, the fluvastatin is the rapid-release part; or the acipimox and the fluvastatin are both the controlled-release parts. In addition, the invention further discloses a preparation method of osmotic pump tablets of the composition, and the osmotic pump table which is prepared by applying the method can better bring the synergy of the acipimox and the fluvastatin into play.

The present invention relates to optically active boronate derivatives which are useful as intermediates for the synthesis of HMG-CoA enzyme inhibitors such as atorvastatin, cerivastatin rosuvastatin, pitavastatin, and fluvastatin.

The invention relates to a statin-double phosphonate coupling compound for curing osteoporosis and other bone calcium metabolic diseases and a preparation process and an application, in particular to an atorvastain or fluvastatin-coupling compound and a synthesis and an application. The invention comprises mixing fluvastatin lactone or atorvastain lactone and double phosphonate according to statin lactone: double phosphonate ester= 1:1-3, obtaining statin double phosphonate coupling compound, and then obtaining salt through the reaction of the 1:4-20:4-20 proportion of double phosphonate coupling compound: 2, 4, 6-trimethyl pyridine: trimethyl bromo-silicane in solution with below 5-10 DEG C of reaction temperature. The synthesis process of the invention is simple, which can synthesize eight new compounds, namely that four new intermediate compounds and four target compounds, and provides an effective medicament for preventing and curing osteoporosis and other bone calcium metabolic diseases.

The invention relates to a choline salt of a hypolipidemic drug and a preparation method and a pharmaceutical use thereof. The invention provides a choline salt of a class of hypolipidemic drugs, and the hypolipidemic drugs include but not limited to clofibrate, libet, fenofibrate, ciprofibrate, gemfibrozil, acipimox, niacin, lovastatin, simvastatin, pravastatin, fluvastatin, atorvastatin, rosuvastatin, pitavastatin, eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) and other unsaturated fatty acids. The choline salt of the hypolipidemic drug can be used for treating hyperlipidemia and other cardiovascular diseases. The invention also provides a preparation method of the choline salt of the hypolipidemic drug.

The invention provides a composition with a lipase inhibitor and a hydroxymethyl-glutaryl coenzyme A reductase inhibitor, and a pharmaceutical preparation with the composition. Preferentially, the lipase inhibitor is one of orlistat and cetilistat, and the hydroxymethyl-glutaryl coenzyme A reductase inhibitor is one of atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin or pharmaceutically-acceptable salt thereof. The composition can have the synergistic antibacterial effect and the synergistic histamine releasing inhibition effect, and therefore thetreatment effect and economic characteristics of bacterial infection-caused allergic disease patients can be improved.

Lovastatin, pravastatin, simvastatin, mevastatin, atorvastatin, fluvastatin and cervastatin and derivatives and analogs thereof are known as HMG-CoA reductase inhibitors and are used as antihypercholesterolemic agents. The majority of them are produced by fermentation using microorganisms of different species identified as species belonging to Aspergillus, Monascus, Nocardia, Amycolatopsis, Mucor or Penicillium genus, some are obtained by treating the fermentation products using the methods of chemical synthesis (simvastatin) or they are the products of total chemical synthesis (fluvastatin, atorvastatin and cervastatin). The present invention relates to a crystalline form of the sodium salt of pravastatin, which is known by the chemical name 1-naphthaleneheptanoic acid, 1,2,6,7,8,8a-hexahydro-β,δ,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, mono sodium salt, which is useful as a pharmaceutical substance. The present invention further relates to the method for its preparation and isolation, to a pharmaceutical formulation containing the sodium salt of pravastatin in the crystalline form and a pharmaceutically acceptable carrier, and to a pharmaceutical method of treatment. The novel crystalline form of the sodium salt of pravastatin is useful in the treatment of hypercholesterolemia and hyperlipidemia.

This invention is directed towards a ready-to-use aqueous composition of fludarabine phosphate. In one embodiment, the invention is directed to an aqueous fludarabine phosphate composition which comprises fludarabine phosphate, a base, and water. The concentration of fludarabine phosphate in the composition may be between about 0.5 mg / mL and about 50 mg / mL. The pH of the composition may be between about 5.5 and about 7.1.

The invention provides a composite pharmaceutical ingredient loaded nanoparticle. The nanoparticle is modified by a cationic surfactant; the nanoparticle is loaded with a composite medicine of heparin, taxol and fluvastatin; and the cationic surfactant is dilauryl dimethyl ammonium bromide. The invention also provides a preparation method and an application of the composite pharmaceutical ingredient loaded nanoparticle. According to the nanoparticle provided by the invention, a polylactic acid-glycolic acid copolymer nano-microsphere which is loaded with the heparin, the taxol and the fluvastatin is adopted, and the nano-microsphere is subjected to surface modification by virtue of the cationic surfactant, namely dilauryl dimethyl bromide, through a physical adsorption method, so that a novel intravascular drug delivery system is formed. The adsorption force of the drug delivery system is enhanced, and the residence time of the system in vascular endothelium is prolonged.

The present invention provides a drug composite for treating hyperlipidemia, the characteristics of which lies in containing effective amount Acipimox and Fluvastatin natrium, the weight ratio is (5~30):1, the optimal selection weight ratio is (5~15):1, the further optimal selection weight ratio is 10:1. The lipid-lowering effect is superior to the simple recipe with same dose significantly, which shows that there is synergistic effect and no distinct toxicity function under taking the Acipimox and the Fluvastatin both.

The invention relates to a fluvastatin intermediate tert-butyl (E)-7-[3'-(4''-fluorophenyl)-1'-methylethyl-indol-2'-yl)-3-oxo-5-hydroxy-6-heptenoate, and relates to improvement of a preparation technology of tert-butyl (E)-7-[3'-(4''-fluorophenyl)-1'-methylethyl-indol-2'-yl)-3-oxo-5-hydroxy-6-heptenoate (I). 2-methyl tetrahydrofuran as a solvent is adopted to replace tetrahydrofuran in the original process, so that not only is the reaction yield increased, but also the solvent recovery rate is greatly improved, and the production cost is reduced. The method is used for producing fluvastatin ketone, the reaction yield is increased by about 15%, the solvent recovery rate is increased from 50% to 80%, and the overall production cost is reduced by more than 30%.

The invention provides a eutectic compound formed by a lipase inhibitor and a hydroxy methylglutaryl coenzyme A reductase inhibitor and composition containing the eutectic compound. The eutectic compound is characterized in that the lipase inhibitor is selected from one of orlistat and cetilistat; the hydroxy methylglutaryl coenzyme A reductase inhibitor is selected from one of atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin or pharmacologically acceptable salts thereof. The eutectic compound can simultaneously have synergistic antibacterial action and synergistic histamine release inhibition function, so that the treatment effect on patients with allergic diseases caused by bacterial infection and the economic characteristics can be improved.

The invention discloses a specific primer probe combination for guiding a fluvastatin drug individualized drug use related gene SNP, and is characterized in that the primer probe combination includesa specific primer probe combination for rs4783961, rs11045819 and rs1922242 genes SNP. The invention also provides a kit containing the primer combination and an application thereof. The beneficial effects comprise that provided are the quick typing kit for guiding the fluvastatin drug individualized drug use related gene SNP and the application thereof. The test result obtained by the kit is accurate and reliable, the cost is low, and the kit has good practicability.

The invention provides an eutectic compound comprising a proton pump inhibitor and a hydroxy-3-methylglutaryl coa reductase inhibitor. The eutectic compound is characterized in that the proton pump inhibitor is selected from one in omeprazole, esomeprazole, pantoprazole, rabeprazole and lansoprazole; the hydroxy-3-methylglutaryl coa reductase inhibitor is selected on or pharmacologically acceptable salt thereof in atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin. The eutectic compound can produce a synergistic bacteriostatic effect.

The present invention relates to pharmaceutical compositions for sustained release comprising a water soluble salt of the HMG-CoA reductase inhibitor fluvastatin as active ingredient, said composition being selected from the group comprising matrix formulations, diffusion-controlled membrane coated formulations; and combinations thereof.

The present invention relates to pharmaceutical compositions for sustained release comprising a water soluble salt of the HMG-CoA reductase inhibitor fluvastatin as active ingredient, said composition being selected from the group comprising matrix formulations, diffusion-controlled membrane coated formulations; and combinations thereof.