364 results about "Simvastatin" patented technology

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 provides a stable simvastatin oral tablet which is prepared from the following components in percentage by weight: 10-20% of simvastatin, 0.01-0.04% of antioxidant, 0.5-2.0% of acidifier, 70-80% of filler, 5-10% of disintegrant, 1-1.2% of lubricant and 0.5-2% of binder. The invention also provides a method for preparing the stable simvastatin oral tablet. By strictly controlling the moisture of a finished product, the doses of the antioxidant and acidifier in the components are obviously reduced, the product stability is better, and the safety is higher.

The invention discloses a simvastatin tablet and a preparation method thereof. The simvastatin tablet comprises an active ingredient simvastatin and pharmaceutical excipients, wherein the pharmaceutical excipients are spherical lactose, cross-linked sodium carboxymethyl cellulose, butylhydroxyanisole, hydroxypropyl methyl cellulose, silicon dioxide, magnesium stearate and film coating premix, which are added according to a specific mass ratio and process. The simvastatin and the pharmaceutical excipients are incompatible, and are prone to hydrolysis and oxidation, lactone bonds break to open loop to generate an active metabolite simvastatin hydroxy acid under the high-humidity condition, the intramolecular diene bond is subjected to a slow oxidative copolymerization reaction to generate a dimer or polymer under the high-temperature condition, and the preparation of a stable preparation is greatly difficult. In recent years, with the continuous disclosure of information, the difference between the quality standards of simvastatin tablets produced by different manufacturers is great, wherein the dissolution behavior difference is more significant, so that the situation that the simvastatin tablets have the same name but have different quality is very obvious. The prescription process determined by the study can continuously produce the simvastatin tablet at large scale, and the prepared simvastatin tablet has a good dissolution performance in various PH-value dissolution media, and keeps good stability in the long-term storage process.

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.

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.

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 belongs to the technical field of bone repairing materials, and relates to a PLGA/HA/S (Poly(Lactic-co-Glycolic Acid)/Hydroxyapatite/Simvastatin) medicament-carrying composite nano fiber support material as well as a preparation method and application in the bone repairing aspect. The material is prepared by preparing a carrier polymer mixed solution containing simvastatin from hydroxyapatite, simvastatin and PLGA, and processing by a high-voltage electrostatic spinning device, wherein the mass ratio of hydroxyapatite to PLGA and simvastatin to PLGA is (1:100)-(1:10) respectively. The physical and chemical performances and degradation rate of the material are controlled by controlling the blending ratio, reaction temperature, time and other factors; the PLGA/HA/S blended medicament-carrying nano fiber has good biocompatibility; the shape of the material is similar to extracellular matrix, thereby being beneficial to the adhesion and growth of cells; and the material has better biodegradability, and can release the main ingredient of bone tissues, namely hydroxyapatite and a medicament for promoting osteogenesis, namely simvastatin, thus the biomaterial is particularly suitable to be used as a bone repairing material.

The invention discloses a regenerated active artificial implant for osteoporosis therapy and a preparation method thereof. The regenerated active man-made implant comprises a tooth implant with titanium or titanium alloy as a base and an artificial bone joint medical hard tissue implant material. The base material surface is subjected to serial nano-micron treatment and simvastatin-containing improved bionic liquid treatment to form a nano bionic coating structure with regeneration activity and bone mass formation promoting effect; the nano coating crystal grains on the surface of the implant are bone-like hydroxyapatite substance rich in calcium and phosphorous; the nano-micron bionic coating implant has bone regeneration promoting activity and high affinity, and compared with coating-free materials, the nano-micron bionic coating implant has remarkably increased binding force with bone so as to effectively prevent the implant from loose and fallout phenomena; the simvastatin-containing calcium/phosphorus bionic coating implant is a novel medical implant material with bone mass formation promoting effect and regeneration activity.

The invention relates to a method that a functional drug is enveloped into a polymeric material with biodegradability to form a nano-micron microsphere system. The method comprises that the polymeric material and simvastatin are dissolved in an organic liquor to form uniform dispersion which is then added into an liquor containing emulsifier Tween 80 and biologically nontoxic electrolytic polyvinyl alcohol or sodium dodecyl benzene sulfonate (SDBS), and then the obtained liquor is stirred, evaporated at a reduced pressure, centrifugalized, washed and vacuum dried, finally the simvastatin-contained delayed-release microsphere system is obtained. The surface of the microsphere is smooth and round, the granule thereof is regular without conglutination, and the granule diameter, the drug-loading rate (1-10 percent) and the encapsulation rate (above 40 percent) are all controllable, and the delayed-release time exceeds 2 months. The prepared simvastatin-contained delayed-release microsphere system can be processed into various preparations used in bony tissue absorption or bony defect parts, the microsphere system is degraded at a proper speed, thus the simvastatin can be further released; the degradation of the polymer can provide bony tissue with subsequent recuperating space to complete the repair of the bony defect parts.

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.

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 relates to an application of an HMGCoA reductase inhibitor in preparation of a medicine used for treating xerophthalmia and belongs to the field of medicines. The inventor finds that a frequently-used lipid regulation medicine, the HMGCoA reductase inhibitor, can obviously prolong SIT time and BUT time and obviously reduce an FLS score when being used for treating the xerophthalmia, and the HMGCoA reductase inhibitor is better than ciclosporin or artificial tears in the aspect of improving the indexes, wherein simvastatin and lovastatin have the best treatment effect. The HMGCoA reductase inhibitor also can be prepared into oral preparation used for treatment or adjuvant therapy of the xerophthalmia. The HMGCoA reductase inhibitor has a definite curative effect and less toxic and side effects, compliance of a patient is high, and clinical ophthalmic drugs are further enriched.

The invention relates to the medical technology field, and particularly relates to a solid self-microemulsion based on a spherical crystallization technique and a preparation method thereof. The solid self-microemulsion is characterized in that: with the use of the spherical crystallization technique, the solid self-microemulsifying micoparticles are prepared from poorly water soluble drugs in a liquid phase by one step. The solid self-microemulsion with the poorly water soluble drugs comprises the components, by weight: 0.1 to 1.5 g of the poorly water soluble drugs, 4.0 g of a polyoxyethylene hydrogenated castor oil, 2.0 g of capric caprylic triglyceride, 2.0 g of tpropylene glycol, 1.0 ml of ethanol, 4.0 ml of dichloromethane, 0.5 to 1.1 g of ethylcellulose (or Eudragit RS100, RL100), 0.05 g of PEG4000, and 0.5 g of colloidal silicon dioxide. The poorly water soluble drugs include cyclosporine A, fenofibrate, glimepiride, cilnidipine, isradipine, simvastatin, baicalein, neogambogic acid, puerarin, cyclovirobuxine D, silymarin and the like.