266 results about "Lovastatin" 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 invention discloses a red yeast rice extract and a preparation method and a quality test method thereof. The main active ingredient of the extract is lovastatin, the content of which is more than 3 percent. The extract is prepared by subjecting a medical material of red yeast rice to extraction with an organic solvent, water decoction after the volatilization of the solvent, precipitation collection by siphonage and configuration, mixing with excipients and drying. The preparation method improves the content of lovastatin. The invention also provides a quality control method for identifying the ingredients and measuring content.

This invention provides an easy and efficient process for producing a simvastatin of great use as an HMG-CoA reductase inhibitor, which comprises deacylation of lovastatin with an inorganic base and a secondary or tertiary alcohol and subjecting the resulting diol lactone to selective protection with a ketal or acetal protective group, acylation and deprotection-lactonization to give simvastatin.

The invention relates to a fermentated food processing method, in particular to a method for manufacturing tartary buckwheat monascus fermented teat, which comprises the following steps: 1, cleaning tartary buckwheat, adding water, steaming the material and inoculating test-tube aspergillus orzae for cultivation for 72 hours at 28 to 40 DEG C; 2, preserving heat, performing saccharification for 4 to 5 hours and inoculating monascus strains under an aseptic condition; and 3, performing solid fermentation on tartary buckwheat powder with turning monascus for drying, mixing the tartary buckwheat and xylitol powder and packing the mixture into bags to obtain finished products. The tartary buckwheat monascus fermented product tastes sweet, is convenient to take, combines functional components, contains flavonoid substances, chitosan, lovastatin and the like, and has remarkable health care efficacy.

The invention discloses a lovastatin-containing enteric coated sustained-release pellet capsule and a preparation method thereof. The lovastatin-containing enteric coated sustained-release pellet capsule comprises two parts, namely, an enteric coated sustained-release pellet and a hollow capsule, wherein the enteric coated sustained-release pellet comprises 55-86% of medicine-containing pellet core, 2-5% of isolation coating layer, 2-15% of a sustained-release coating layer and 10-25% of enteric-coated coating layer by weight. The prepared lovastatin enteric coated sustained-release pellet capsule is uniform in granule size and stable in medicine release; the medicine is not released in gastric acid but is slowly and constantly released in intestinal tracts and livers, has the characteristic of targeted medicine release, is small in irritation to gastrointestinal tracts, and can reduce the toxic and side effects of the medicine and reduce the number of the medicine administrations, so that the compliance of patients is improved; and meanwhile as the enteric coated sustained-release pellet preparation is composed of hundreds of pellets of uniform granule sizes, the sudden release of the whole preparation is not caused by the breakage of individual pellets, so that the medicine is safer than a sustained-release tablet, smaller in irritation to gastrointestinal tracts and more stable in blood concentration, and the clinical effectiveness and security are effectively improved.

the invention discloses a new strain of Monascus Purpureus Went and preparing method of traditional Chinese medicine antihyperglycemic Monascus color, which is composed of 15-30mg / g open, close ring structured Luovastatin, 3-6mg / g unsaturated fatty acid and not more than 100ppb orange mycin, wherein the content of open-structured Luovastatin is 15-90%.

The invention relates to a production method of a monascus vinegar rich in lovastatin. The production method comprises the following steps: soaking, steaming and sprinkling cold water on high-quality glutinous rice, mixing the rice with a composite yeast solution, a former batch of fermented red yeast rice wine mash and functional red yeast, then carrying out diastatic fermentation at a low temperature to obtain mature red yeast rice wine mash; mixing bran, cavings, the former batch of fermented monascus vinegar culture and acetic acid bacteria liquid into the wine mash to perform solid-state acetic fermentation, adding lovastatin in a later period of fermentation with an adding amount being 0.03-0.05% of mass of a raw material, and fermenting for a total of 28-30 days to obtain mature monascus vinegar culture; and adding salt in the vinegar culture, pouring vinegar in the vinegar culture, sterilizing the vinegar culture, clarifying the and then filling the vinegar culture in jars and sealing to obtain the finished product, namely the monascus vinegar rich in lovastatin. The production method of the monascus vinegar rich in the lovastatin has the characteristics that the obtained monascus vinegar is rich in fragrance, mellow in taste and excellent in color and luster, and has a content of the lovastatin being 560-600mg / L.

The invention relates to a Monascus ruber for the high generation of lovastatin and gamma-aminobutyric acid and the low generation of a pigment. The Monascus ruber is named as C002, belongs to Monascus sp., has a preservation number of CGMCC NO.6860, is preserved at China General Microbiological Culture Collection Center in Institute of Microbiology, Chinese Academy of Sciences on Datun Road, Chaoyang District of Beijing on November 26, 2012. The Monascus ruber has the advantages of high generation of lovastatin and gamma-aminobutyric acid, no generation or extremely-low generation of citrinin, no bitterness, and low generation of a Monascus pigment. Strains of the Monascus ruber CGMCC NO.6860 can utilize a plurality of culture mediums comprising rice, coarse rice, corn, cassava and the like to produce functional red yeast rice; and the Monascus ruber is especially suitable for the exploitation of relevant functional beverage products because of the Monascus pigment low-generation characteristic.

The invention discloses a method for biotransformation of Panax notoginseng (Burk.) F. H. Chen medicinal materials by using Monascus purpureus. The method mainly comprises the following operating steps of: 1) preparation of Monascus purpureus strains; 2) preparation of Panax notoginseng (Burk.) F. H. Chen culture medium; and 3) fermentation and culture to obtain fermentation products containing active components, product post-treatment and detection of major efficacy components. By using the method for fermenting the Panax notoginseng (Burk.) F. H. Chen by using the Monascus purpureus provided by the invention and by directly using Panax notoginseng (Burk.) F. H. Chen raw medicinal materials as fermentation substrate, through one-step fermentation process, medicinal components, i.e. Panax notoginseng (Burk.) F. H. Chen and Monascus purpureus are simultaneously obtained, the culture is enabled to have dual effects of the Panax notoginseng (Burk.) F. H. Chen and the Monascus purpureus, the products contain lovastatin which is a lipid-decreasing active component according to experiments, the type and the content of saponin are obviously changed, and rare saponin with higher pharmacological activity is produced.

The present invention provides a new type balloon dilation catheter which includes ballon and medication material coated on stent. Said medication material comes from one or two and more than two mixtures of heparin sodium, fiber degrading enzyme, serine proteinase, batroxobin, aspirin, genistein, hirudin and its recombined product, colchicine, sirolimus, biolimus, zotarolimus, tracrolimus, pimecrolimus, simvastatin, atorvastatin, pravastatin, ciclosporin, Anti-CD34, dexamethasone, bleomycin, plicamycin, daunomycin, mitomycin C, actinomycin D, taxol, celastrol, methopterin, 5-fluorouracil, cytarabine and 6-purinethol. The balloon is made of macromolecule nylon material, and the stimulation to blood vessel is far lower than the stent with metal structure.

A Chinese medicine 'Red koji' containing lovestatin as its main active component in the form of tablet, capsule, powder, dripping pill, or particles for preventing and treating cardiovascular and cerebrovascular diseases is prepared through fermenting and extracting.

The present invention relates to a process for preparing lovastatin and simvastatin which comprises (1) performing step of a lactonization of mevinic acid and analog thereof compounds in the presence of a dehydrating agent and without an acid catalyst under nitrogen sweep; and then (2) making step of crystals at a high temperature. In the process of the present invention, lovastatin and simvastatin highly purified can be produced in a high yield and especially, heterodimers formed as a by-product can be reduced in an amount remarkably. Therefore, the process of the present invention is convenient and economical.

The present invention is directed to nanoparticulate compositions comprising statin such as lovastatin or simvastatin. The statin particles of the composition have an effective average particle size of less than about 2000 nm. In another aspect of this invention, novel combinations of statins and other cholesterol lowering agents are described and methods of using same are taught.

The invention relates to a health-care food composite with a function of assisting in reducing blood fat and a preparation method thereof. According to the invention, 100-200 parts by weight of freeze-dried natto powder, 100-200 parts by weight of red yeast, 100-220 parts by weight of phytosterol and clinically acceptable auxiliary materials are prepared into hard capsules, tablets, granules and powder. According to the invention, a complementary concept is adopted, and through the combination of three kinds of raw materials, the serum total cholesterol can be effectively reduced, and the triglyceride can be reduced, therefore, the health-care food composite has a health-care function of assisting in reducing blood fat; and in each 100g of the health-care food composite, the weight of the efficacy component phytosterol is higher than 10 g, and the weight of lovastatin is higher than 0.1 g.

The invention discloses a preparation method for simvastatin. Wherein, using inorganic base to hydrolyze lovastatin and obtain trioxyacidic intermediate with formulate (3); then, etherifying directly the intermediate to prepare simvastatin derivative with formulate (4), taking ring-opening reaction with catalyst to obtain open-loop ester with formulate (6), catalyzing, acidifying, and obtaining the product; or, improving existing technique with this invention, such as, converting the intermediate into ketal intermediate with six membered ring, catalyzing, etherifying to obtain the simvastatin derivative with formulate (8), using acid-catalysis de-preserving reaction to obtain product. This invention simplifies greatly existing technique.

The invention relates to a microorganism, in particular to a monascus strain capable of obtaining high content of gamma-reanal and Lovastatin, the strain is named Monascus ruber Danxi-1, which is preserved in SIPO designated China General Microbiological Culture Collection Center with a docket number of CGMCC No: 1405, the preservation date being June 10, 2005.

The invention discloses a making method of monascus and tartary buckwheat functional food and an application thereof, and belongs to the field of biological fermentation and medicine. The preparation method comprises the steps that monascus serves as original strains, liquid shake-flask culture is conducted on the monascus, liquid seed amplification culture is conducted, tartary buckwheat solid fermentation is conducted, and the functional food containing flavone, lovastatin and monascus pigments is obtained. The food comprises 2-10 mg / g of the flavone, 0.5-5 mg / g of the lovastatin and 0.4-6 mg / g of the monascus pigments. The functional food produced through the making method can be used for producing health care foods capable of regulating blood sugar and blood fat, or the active components of the flavone, the lovastatin and the monascus pigments of the functional food can be extracted to be used for producing drugs for treating hyperlipidemia and diabetes mellitus.

A process for manufacturing Simvastatin is provided comprising reacting lovastatin with an organic boronic acid to produce a derivative of lovastatin (lovastatin phenylboronate) methylating the 2-methylbutyryloxy group on the lovastatin derivative to form a 2,2-dimethylbutyryloxy group on the lovastatin derivative and thereafter removing the boronate group to produce simvastatin.

The invention relates to monascus selenium-rich millet powder, which is fermented by using monascus as a fermentation strain and selenium-rich millet as fermentation substrate. The invention also provides a preparation method of the monascus selenium-rich millet powder. The monascus selenium-rich millet powder of the invention contains rich lovastatin and organic selenium. And monascus selenium-rich millet cakes made by using the millet powder have the functions of reducing blood fat, sugar and pressure and resisting and preventing cancers and are good products of homologous food and medicine.

The invention discloses a new application of Luovastatin, in particular to an application to prepare the drug to inhibit stem cell death among bone marrow, which is characterized by the following: treating ischemic heart disease and other limb ischemic disease; accelerating the existence of cell; improving the treating effect of the transplanted stem cell.

The invention discloses a method for extracting and purifying lovastatin. The method comprises the following steps of: acidizing the pH of a fermentation liquor for producing lovastatin to 1-3; filtering or centrifugally separating; collecting bacterium slags; extracting the bacterium slags with an organic solvent; washing an extracting solution with an alkaline aqueous solution, an acid aqueous solution and deionized water in sequence; concentrating the washed extracting solution, and crystalizing; separating and drying the crystal to obtain a crude product; and recrystallizing the crude product to obtain purified lovastatin. Due to the adoption of the method, the problem of emulsion during the extraction of lovastatin is solved, and the dissolubility of a lovastatin product in acetone, chloroform and methanol is increased.

The invention provides monascus fagopyrum-tataricum tea prepared by taking monascus and fagopyrum tataricum as main raw materials. The characteristics of the monascus fagopyrum-tataricum tea comprise that the monascus fagopyrum-tataricum tea is ruddy in color, keeps delicate fragrance of fagopyrum tataricum, is good in mouthfeel, also is relatively high in both lovastatin content and total flavonoid content, and has the substantial effects of reducing blood pressure, reducing blood fat, reducing cholesterol, improving immunity and the like under the synergic effect of monascus and fagopyrum tataricum.

The invention describes lovastatin, simvastatin and simvastatin-6-oxide (L-669262) nitro-oxo-derivative of which the general formula is shown in formula (I) and the drugs can increase the non-lipid activity of statins such as anti-inflammatory and the like. The invention also relates to a preparation method of the drugs.

The invention relates to a lovastatin-generating fungus and the application thereof in the production of Pu'er tea, belonging to the biotechnology field. The production strain of the invention is obtained by separating, purifying and primarily filtering through thin layer chromatography and high efficiency liquid phase secondarily filtering. The production strain is lovastatin-generating Monascus purpurevs MPT13 with the preservation No. of CCTCC M 2010123, and is preserved on May 20, 2010, in the preservation department of China center for type culture collection located in Wuhan University, Wuhan. The lovastatin-generating fungus of the invention is applied to the production of Pu'er tea. The invention has the advantages that Monascus purpurevs is proportionally vaccinated and applied to the fermentation process of Pu'er tea to obtain the lovastatin-contained Pu'er tea with new characteristics in aspects of aroma and soup on a basis of keeping the flavor of traditional Pu'er tea, the processing time is shortened, and the invention plays an important role in the development of new Pu'er tea products and specific Pu'er tea.

Highly pure simvastatin can be prepared economically in a high yield using the method comprising the steps of treating lovastatin with potassium hydroxide dissolved in a mixture of water and methanol to obtain a triol acid; relactonizing the triol acid, and protecting the hydroxy group on the lactone ring; and acylating the resulting compound with 2,2-dimethylbutyryl chloride or 2,2-dimethylbutyryl bromide in the presence of an acylation catalyst in an organic solvent, followed by removing the silyl protecting group on the lactone ring to obtain simvastatin.

A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2'-position group of lovastatin without requiring protection / deprotection of 13-OH of lovastatin and lactone ring opening / closure.

The invention discloses a method for preparing simvastatin. The method is as follows: a. lovastatin and alkylamine are prepared into lovastatin amide; b. hydroxyl groups in lovastatin amide molecules are protected, and lovastatin amide di-(trimethyl) silyl ether is generated; c. the lovastatin amide dimethyl (trimethyl) silyl ether is subjected to methylation, so as to obtain simvastatin amide di-silyl ether; d. the simvastatin amide di-silyl ether is protected, and simvastatin amide is generated; e. the simvastatin amide is subjected to hydrolysis and is added with ammonia gas, and simvastatin ammonium salt is obtained; and f. the simvastatin ammonium salt is subjected to ring closure to generate the simvastatin. The method takes a composite solvent of tetrahydrofuran and cyclonexane as a solvent for the protective reaction; the lovastatin amide di-(trimethyl) silyl ether can directly perform methylation reaction without alkaline washing and water scrubbing; after water scrubbing of methylate, protective groups are automatically fallen off, thereby the reaction for removing the protective groups is saved and the products can directly perform ammonium salt reaction. The method simplifies the synthesis technique of the simvastatin.

The invention discloses a method for utilizing monascus to convert yam to produce a functional food and relates to the technical field of bioengineering. According to the preparation method, sequentially through the steps of enlarged culture in a test tube, liquid shake-flask culture and enlarged culture in a seed tank, solid fermental cultivation, drying and smashing, the functional food which regulates blood lipids, blood sugar and blood pressure, resists radiation and inhibits tumor is obtained. According to the method, the yam, rice, wheat, corn and sorghum and the like are taken as solid substrates, monascus is taken as a strain to convert yam saponins through solid fermentation, monascus pigment and monascus polysaccharides are synthesized; in the obtained product, the content of the saponins is 2-20 mg / g of dry substrate, the content of the monascus polysaccharides is 10-100 mg / g of dry substrate, the content of lovastatin is 0.5-10 mg / g of dry substrate, the content of the monascus pigment is 1-20 mg / g of dry substrate, and the method can be used for extracting the saponins, the monascus polysaccharides, lovastatin and the monascus pigment and producing tablets or capsules for treating blood lipids, blood sugar and blood pressure, resisting radiation and inhibiting tumor.

The current invention discloses novel methods for the inhibition of inducible nitric oxide synthesis (iNOS) and the production of NO. Methods of inhibiting the induction of proinflammatory cytokines are also described. Methods of treating various disease states, such as X-linked adrenoleukodystrophy, multiple sclerosis, Alzheimer's and septic shock using inhibitors of iNOS and cytokine induction are disclosed. The inhibitors include the exemplary compounds lovastatin, a sodium salt of phenylacetic acid (NaPA), FPT inhibitor II, N-acetyl cysteine (NAC), and cAMP.