34 results about "Rosuvastatin" patented technology

The invention provides a carbonyl reductase mutant. The carbonyl reductase mutant is obtained by performing single-point mutation or multi-point combined mutation on the 17th site, the 40th site and the 64th site of an amino acid sequence as shown in SEQ ID NO.1. The invention also provides a coding gene, a recombinant vector containing the coding gene, a co-expression engineering bacterium and an application of the co-expression engineering bacterium. Compared with a wild type enzyme, the carbonyl reductase mutant has high activity and high stereoselectivity, the enzyme activity can reach more than two times that of the wild type enzyme, the catalytic efficiency on a substrate precursor ketone is remarkably improved, the yield of a statin drug intermediate and chiral alcohol synthesized by an enzyme method of the carbonyl reductase mutant is remarkably improved, and the yield of a rosuvastatin intermediate (3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R, 3R) is remarkably improved. The highest yields of the (3R, 5R)-6-chloro-3, 5-dihydroxyhexanoic acid tert-butyl ester and the atorvastatin intermediate (3R, 5R)-6-cyano-3, 5-dihydroxyhexanoic acid tert-butyl ester reach 99% and 97.6% respectively, e.e. Is larger than 99%, and the method has high industrial application value.

The present invention provides a pharmaceutical composition comprising a) a first phase comprising rosuvastatin, and b) a second phase comprising acetylsalicylic acid, wherein the first phase comprising rosuvastatin is in the form of a coated tablet, and the second phase comprising acetylsalicylic acid is in the form of granules; said pharmaceutical composition solves a set of significant technological challenges due to the physicochemical properties and difference in dosage of each drug. The pharmaceutical composition of the present invention is stable, and also has a comparative bioavailability equivalent to that of the co-administered monodrugs, so that the composition is safe and effective in the treatment of hyperlipidemias and in the prevention of at least one cardiovascular disease. The invention is also directed to a process for manufacturing the pharmaceutical composition.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs.

The present invention relates to a composition for preventing, alleviating or treating metabolic diseases, the composition comprising a rosuvastatin and ursodeoxycholic acid conjugate or a pharmaceutically acceptable salt thereof, in which the statin conjugates to an ursodeoxycholic acid transporter and has the effects of function inhibition, cholesterol level reduction, antilipid toxicity, body weight reduction, blood lipid reduction, fatty liver alleviation, inflammation alleviation, and kidney damage alleviation. The composition, in the form of a single formulation, has the characteristics of maintaining the therapeutic effects of rosuvastatin and ursodeoxycholic acid while reducing the side effects of existing statins, and thus can be widely used as a substitute for complex formulations in the treatment of metabolic diseases.

The invention discloses a rosaxostat orally disintegrating tablet and a preparation method thereof. The preparation method of the orally disintegrating tablet is selected from one of a freeze-drying method, a tabletting method and a melting method. The prescription of the freeze-drying method comprises the rosaxostat or rosaxostat salt, a skeleton supporting agent, an adhesive, a suspending aid and a surfactant. According to the preparation formula and the preparation process, the defect that the content uniformity of the prepared tablets is poor due to the fact that the uniformity of intermediate liquid medicine is poor in the preparation process can be overcome, and the disintegration time limit of the rosaxostat orally disintegrating tablets, especially the rosaxostat freeze-dried orally disintegrating tablets, is further prolonged; the medicine is especially suitable for old people, children, patients with dysphagia and people with inconvenience in taking water to take medicine; the bioavailability is high; the rosaxostat orally disintegrating tablet is simple in material, moderate in tablet weight, good in appearance, good in taste, fast in disintegration, simple in preparation process and suitable for industrial mass production.

1. Name of the product of this design: Packaging box (Rosuvastatin Capsules). 2. Application of this design product: for pharmaceutical packaging. 3. The key design point of this design product lies in the combination of shape and pattern. 4. The picture or photo that best illustrates the design points: three-dimensional picture.

The current difficulty in synthesizing rosuvastatin lies in the preparation of the key intermediate, 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate (or carboxamide), represented by Formula A. To address this issue, the present invention provides a rosuvastatin intermediate and a preparation method thereof. The preparation method comprises the following steps: (1) reacting a compound represented by Formula C with formaldehyde and a halogen acid in the presence of a solvent to obtain a compound represented by Formula B; and (2) reacting the compound represented by Formula B with metal powder in the presence of a solvent to obtain a compound represented by Formula A. This synthesis method has a reasonable route, high yield, and high purity, and is suitable for industrial production.

The invention discloses a synthesis process of an atorvastatin side chain intermediate, which comprises the following synthesis steps: 1, dissolving a compound II in an organic solvent, adding a compound I, adding an alkali reagent, adding a catalyst, heating to react for 2-4 hours, and cooling to room temperature to obtain a mixed solution of a compound III; and 2, slowly introducing hydrogen into the solution of the reaction compound III in the first step, synchronously heating and pressurizing to react for 2-4 hours, and after the reaction is finished, separating a product to obtain a compound V. The preparation method has the beneficial effects that the atorvastatin intermediate A9 is prepared from the rosuvastatin intermediate, so that the synthesis steps of atorvastatin and rosuvastatin are partially combined, the reaction process is more efficient, the efficiency of the whole synthesis route is improved, expensive or scarce raw materials can be saved, and the cost is reduced. By using the existing rosuvastatin intermediate as the starting point, it is possible to avoid the complicated steps required in the conventional synthesis route of the atorvastatin intermediate A9.

The present disclosure provides method of administering sotorasib to a patient, e.g., a patient with a cancer comprising a KRAS G12C mutation, wherein the patient is further in need of treatment with a breast cancer resistance protein (BCRP) substrate. e.g., rosuvastatin.

The utility model relates to the technical field of rosuvastatin production equipment, and discloses a raw material crushing mechanism for rosuvastatin intermediate production. Comprising a grinding roller, a grinding cylinder, a supporting frame, a conical feeding opening, a discharging pipe, a conveying chamber, a high-pressure air pipe, a powder conveying pipe, a first separating cylinder, a second separating cylinder, a vacuum feeding machine, a conduction pipe, a screening net cover, a filter, a material returning opening and a material collecting barrel. According to the crushing mechanism, raw materials are ground through the grinding roller and the grinding cylinder, the particle diameter is gradually reduced, then the ground raw materials are screened through the first separation cylinder and the second separation cylinder, raw material powder meeting the standard is collected and stored, and raw material powder not meeting the standard enters the grinding cylinder again to be ground; the fineness and the reaction efficiency of the raw materials are improved, and the production of the rosuvastatin intermediate is facilitated.

The present invention relates to a pharmaceutical combination preparation, which comprises all of ezetimibe, rosuvastatin and empagliflozin as active ingredients, and thus can be administered as a single drug, and not through co-administration, in the simultaneous treatment of dyslipidemia and diabetes, thereby increasing patient dosing convenience, minimally affecting dissolution between drugs, ensuring biological equivalence, and providing excellent stability of the active ingredients.

A method of treating a wound may include topically administering a statin composition including a statin selected from atorvastatin, fluvastatin, lovastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin, or combination thereof. The statin composition may be administered in an ointment, powder, or liquid format. The method may also include topically administering one or more antimicrobial drugs and / or naltrexone.

The present invention provides a pharmaceutical composition comprising a) a first phase comprising rosuvastatin, and b) a second phase comprising acetylsalicylic acid, wherein the first phase comprising rosuvastatin is a coated tablet and the second phase comprising acetylsalicylic acid is a granule; This pharmaceutical composition solves a set of important technological challenges due to the physicochemical properties and the difference in dosage of each drug. The pharmaceutical composition of the present invention is stable and, moreover, has comparable bioavailability to the single-drug combinations administered concomitantly, such that the composition is safe and effective in the treatment of hyperlipidemia and in the prevention of at least one cardiovascular disease. The invention also relates to a manufacturing process for the pharmaceutical composition.

A stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.

The present invention relates to a modified metal, a preparation method thereof and an application. The modified metal comprises a metal and a film layer located on the surface of the metal. Among them, the metal comprises one or more of titanium, tantalum, and magnesium, and the film layer comprises a statin compound, and the statin compound comprises one or more of simvastatin, pravastatin, atorvastatin, and rosuvastatin. The modified metal of the present invention has good antibacterial properties and can effectively avoid the infection of the orthopedic implants produced.

The invention relates to a stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.

The invention belongs to the technical field of biological medicines, and relates to a traditional Chinese medicine micromolecule composition and application thereof in preparation of medicines for treating metabolism-related fatty liver diseases. Through combined use of two or more of naringin, sophoriol, 8-isopentenyl naringenin and butene-7-O-beta-D-glucopyranoside, especially combined use of the four components, weight gain of MAFLD mice induced by high-fat diet / high-fat and high-sugar diet can be significantly reduced, lipid accumulation in the liver is reduced, and the weight loss of the mice is reduced. The insulin resistance is relieved, and the hepatocyte injury is improved. The composition can improve blood biochemical indexes related to lipid metabolism, relieve oxidative stress, increase fat consumption and improve a metabolic mode, and the effect is superior to that of a western medicine rosuvastatin positive control group and that of a western medicine rosuvastatin single use group.

The utility model discloses an extraction layering reaction kettle for producing a rosuvastatin intermediate, which relates to the technical field of medicine extraction and comprises a sealing barrel and a centrifugal barrel, a conveying pipe is arranged on the sealing barrel, the centrifugal barrel is rotatably arranged in the sealing barrel, and the conveying pipe is connected with the centrifugal barrel. A driving assembly used for driving the centrifugal barrel to rotate is arranged on the sealing barrel, a discharging pipe penetrating through the sealing barrel is arranged at the bottom of the centrifugal barrel, a control valve is fixedly connected to the discharging pipe, and an air pressure balance assembly is arranged at the top of the sealing barrel. When the centrifugal machine is used, the motor can drive the connecting disc to rotate, the rotating connecting disc drives the centrifugal barrel to rotate through the connecting rod, so that a layered solution in the centrifugal barrel generates centrifugal force, and due to the fact that the mass of water is large, the edge of a rotating water layer can gradually rise upwards along the inner wall of the centrifugal barrel, and meanwhile the middle of the water layer is sunken. Therefore, the contact area of the water layer and the toluene layer is increased, and the extraction efficiency is improved.

This invention discloses a process for synthesizing rosuvastatin acetone tert-butyl ester, comprising the following steps: First, compound I is dissolved in an organic solvent, compound II is added, and the reaction is stirred at room temperature. The reaction is monitored by HPLC. After the reaction is complete, the product is separated to obtain compound III. Second, a palladium catalyst is added to the organic solvent, stirred and mixed evenly, and then compound III and compound IV are added and stirred under the action of the palladium catalyst to obtain compound V. The advantages of this invention are: mild reaction conditions, the entire process is carried out at room temperature, eliminating the need for harsh conditions such as high temperature and high pressure, reducing energy consumption and equipment requirements, and making it suitable for industrial-scale production; excellent stereoselectivity, using a palladium-catalyzed reselective Heck reaction to replace the traditional Witting and Julia olefin reactions, avoiding stereoisomer byproducts, and resulting in higher purity of the target product; fewer byproducts and simpler separation.

The invention belongs to the technical field of biological medicine, and particularly relates to a targeted bionic nano-drug loaded with tanshinone IIA and rosuvastatin as well as a preparation method and application of the targeted bionic nano-drug loaded with the tanshinone IIA and the rosuvastatin. And wrapping the outer layer of the loaded polylactic acid-glycolic acid copolymer with a macrophage membrane, and modifying the surface of the macrophage membrane by using the phosphatidylated hyaluronic acid. According to the targeted bionic nano-drug system, the polylactic acid-glycolic acid copolymer is used for loading two drugs at the same time, inhibition of endothelial cell mesenchymal transition by tanshinone IIA and regulation of macrophage lipid metabolism by rosuvastatin are organically combined, and the effect of combined treatment of atherosclerosis is achieved.

The invention relates to a stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.

The invention provides a low-matrix-effect LC-MS / MS method for ultra-trace detection of rosuvastatin in serum, and belongs to the technical field of analysis. Comprising the following steps: (1) preparing a standard stock solution and a standard curve working solution of a target object to be detected; (2) treating the blood sample to obtain a detection sample; and (3) detecting the standard curve working solution by using HPLC-MS / MS, fitting to obtain a standard curve equation corresponding to the target object to be detected, and detecting the detection sample by using HPLC-MS / MS to obtain the content of the target object to be detected in the detection sample. According to the method, the limit of detection (LOD) is about 1.26 ng / m, the limit of quantitation (LOQ) is about 4.19 ng / ml, and the inter-batch precision (RSD) is less than 15%, so that the reproducibility of the method and the stability of a result are ensured.

The invention discloses a conjugate HA-RS obtained by direct esterification of hydroxyls and carboxyls in hyaluronic acid and derivatives thereof, rosuvastatin and prodrug structures thereof, and also discloses a nano-micelle HA-RS-NPs formed by the conjugate, and a preparation method and application of the nano-micelle HA-RS-NPs. The hyaluronic acid and hyaluronic acid derivative loaded rosuvastatin and prodrug nano-micelle disclosed by the invention can be specifically combined to vulnerable plaque cells, and can realize stable and continuous release of drugs.

The invention belongs to the technical field of biological medicine, and particularly relates to an ROS response type liposome composite material and a preparation method and application thereof.The ROS response type liposome composite material is prepared by jointly loading alkannin and rosuvastatin to liposome modified by an ROS sensitive connecting substance DSPE-TK-PEG2000, further wrapping a biomimetic membrane on the outer layer, and preparing the ROS response type liposome composite material. The ROS response type liposome composite material is obtained. According to the present invention, by using the ROS response design characteristic, the specific aggregation and the response type release of the drug at the diseased region are achieved, the blood circulation half-life period of the drug is effectively prolonged, and the anti-atherosclerosis effects of the shikonin and the rosuvastatin with two different mechanisms are combined so as to achieve the effect of effective treatment of the homocysteine induced atherosclerosis.

The present disclosure provides a combination therapy for treating a liver disease or disorder and / or a lipid disease or disorder in a subject in need thereof. Specifically, the combination therapy comprises administration of rosuvastatin and resmetirom to a subject in need thereof.

The invention belongs to the field of medicinal chemistry, and particularly relates to a preparation method of a refined rosaxostat product. The preparation method comprises the following steps: (1) dissolving a raw material rosaxostat in an alkali solution, and heating; (2) adding an acetic acid aqueous solution into the system in the step (1), and controlling the temperature of the system; and (3) cooling and crystallizing the system in the step (2), separating the solid after the crystal is separated out, and drying. Different batches of rosaxostat prepared by the preparation method have high particle size range stability, API with stable quality can be provided for preparation of rosaxostat preparations, and the preparation method is simple and safe to operate and is more suitable for industrial large-scale production.

The present invention relates to a composition for cancer prevention, comprising a statin-based drug as an active ingredient, and disclosed is that a statin drug known for hyperlipidemia treatment may effectively prevent cancer progression. More specifically, a novel use of rosuvastatin is provided so as to enable providing a composition for multiple myeloma (MM) prevention for inhibiting progression from monoclonal gammopathy of undetermined significance (MGUS) to MM. In addition, the composition may exhibit a greater tumor growth inhibition effect when bortezomib and rosuvastatin are co-administered compared to when each medicine is administered alone.

The present disclosure provides methods of administering sotorasib to a patient (e.g., a patient having a cancer containing a KRAS G12C mutation), wherein the patient is further in need of treatment with a breast cancer resistance protein (BCRP) substrate (e.g., rosuvastatin).