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49 results about "Diltiazem" patented technology
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Diltiazem 12-hour sustained-action capsules are used to treat high blood pressure (hypertension).
Chronotherapeutic diltiazem formulations and the administration thereof
InactiveUS7108866B1Maintain the solubility of the DiltiazemImprove bioavailabilityInorganic non-active ingredientsPill deliveryPharmacyControlled release
A controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 120 mg to about 540 mg or more (as desired) of the form of Diltiazem associated with excipients to provide controlled (sustained) release of the form of Diltiazem for providing a Cmax of Diltiazem in the blood at between about 10 hours and about 15 hours after administration, the preparation comprising the form of Diltiazem in oral sustained-release dosage form in which the Diltiazem is adapted to be released after administration over a prolonged period of time and exhibits when given to humans(i) a higher bioavailability when given at night compared to when given in the morning without food according to FDA guidelines or criteria and(ii) bioequivalence when given in the morning with and without food according to the same FDA guidelines or criteria.
Owner:VALEANT INT BERMUDA
Chronotherapeutic diltiazem formulations and the administration thereof
InactiveUS7348028B2Improve bioavailabilityMaintain the solubility of the DiltiazemPowder deliveryPill deliveryPharmacyControlled release
A method of treating or preventing myocardial ischemia in a patient in need thereof comprising administration of a controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 180 mg to about 420 mg of the form of Diltiazem associated with excipients to provide controlled (sustained) release of the form of Diltiazem for providing a Cmax of Diltiazem in the blood at between about 10 hours and about 17 hours after administration, the preparation comprising the form of Diltiazem in oral sustained-release dosage form in which the Diltiazem is adapted to be released after administration over a prolonged period of time and exhibits when given to humans(i) a higher bioavailability when given at night compared to when given in the morning without food according to FDA guidelines or criteria and(ii) bioequivalence when given in the morning with and without food according to the same FDA guidelines or criteria.
Owner:CHANTILLY BIOPHARMA
Controlled absorption diltiazem pharmaceutical formulation
InactiveUS7067151B1Small amountPowder deliveryOrganic active ingredientsDiltiazemBULK ACTIVE INGREDIENT
A controlled absorption diltiazem pellet formulation for oral administration comprises a core having diltiazem or a pharmaceutically acceptable salt thereof as the active ingredient. The core is surrounded by a coating which has only a single layer which is comprised of a relatively major proportion of talc and relatively minor proportion of sodium lauryl sulfate admixed with a minor proportion of a pharmaceutically acceptable film-forming, first polymer permeable to water and diltiazem, and a major proportion of a pharmaceutically acceptable film-forming, second polymer that is less permeable to water and diltiazem than the first polymer. The core and the coating layer both exclude organic acids. The composition of the coating layer as well as the proportion of core to coating layer are effective to permit release of the diltiazem allowing controlled absorption following oral administration. By combining short lag and long lag pellets into a single formulation, the release of diltiazem is controlled over a twenty four hour period.
Owner:ACTAVIS ELIZABETH
Serratia lipase mutant, recombinant expression transformant, enzyme preparation and application
The invention relates to a mutant obtained through molecular modification of serratia marcescens lipase (SmL), a gene of the mutant and an amino acid sequence of the mutant, a recombinant expression plasmid and a recombinant expression transformant containing the gene of the mutant, a preparation method of a recombinant enzyme preparation and application of the enzyme preparation to diltiazem precursor synthesis. Compared with wild serratia marcescens lipase, the activity of the mutant is remarkably improved, excellent stereoselectivity is kept, and the mutant has good application prospects in industrial production of key chiral precursor (-)-(2R,3S)-2,3-epoxy-3-(4methoxyphenyl)propronate of the cardiovascular disease medicine, namely diltiazem.
Owner:EAST CHINA UNIV OF SCI & TECH
Silicon carbide micro-powder recycling agent and preparation method thereof
A silicon carbide micro-powder recycling agent is made of raw materials including, by weight, 30-34 parts of diesel, 4-6 parts of diltiazem nitrile ester, 4-5 parts of isopropyl ethyl ammonium sulfate ester, 2-3 parts of phenethyl cumenyl phenol polyoxyethylene ether, 1-3 parts of benzoquinone dioxime, 3-5 parts of tall oleic acid, 1-2 parts of benzoxazole sulfur alcohol, 30-35 parts of methanol, 4-5 parts of auxiliaries and 35-40 parts of water. By the aid of various solvents and water, a stable emulsion system is formed under the action of surfactants, interfacial tension of silicon and silicon carbide is changed, the silicon is more thoroughly separated from the silicon carbide by the aid of the auxiliaries, and the obtained silicon carbide is higher in purity. Silicon carbide micro-powder is efficiently recycled at low cost, and the economic benefit of enterprises is greatly improved.
Owner:安徽苏源光伏科技有限公司
Flotation agent for separating gold from gold-bearing copper sulfide ores and method for manufacturing flotation agent
Owner:ANHUI CHAOSHAN NEW MATERIAL
Selective synthesis method of diltiazem chiral intermediate
The invention provides a selective synthesis method of diltiazem chiral intermediate. The method is as below: using anisic aldehyde, chloroacetyl chloride and L-menthol as raw materials; first subjecting chloroacetyl chloride and L-menthol to an esterification reaction to obtain an intermediate 1; then subjecting the intermediate 1 with anisic aldehyde to a Darzens condensation reaction to produce diastereomer intermediates 2 and 3; refining to obtain an optically pure intermediate 3; reacting the intermediate 3 with o-aminothiophenol to obtain an intermediate 4; hydrolyzing the intermediate 4 to obtain an intermediate 5; and cyclizing the intermediate 5 to obtain a product. The invention has the advantages that the ester formed by chloroacetyl chloride and L-menthol is selective in the Darzens condensation reaction with anisic aldehyde to generate the more target product, and solubility difference between the target product and the isomer is used to directly obtain optically pure intermediate, without a complicated resolution process, and the yield is greatly improved. The method substantially increases the utilization rate of the main raw material anisic aldehyde and reduces cost.
Owner:SUZHOU KAIYUAN MINSHENG SCI & TECH CORP
Pharmaceutical composition comprising telmisartan salt and calcium ion antagonist
InactiveCN102266559AImprove solubilityHigh dissolution rateOrganic active ingredientsSenses disorderMagnesium saltDiltiazem
The present invention relates to a kind of pharmaceutical composition, it comprises telmisartan salt and calcium ion antagonist or its pharmaceutically acceptable salt and pharmaceutically acceptable carrier; Described telmisartan salt is selected from telmisartan Sodium salt, potassium salt, calcium salt, magnesium salt or amine salt of sartan, described calcium ion antagonist is selected from amlodipine, lacidipine, cilnidipine, lercanidipine, nisoldipine, nica Dipine, azedipine, barnidipine, manidipine, benidipine, verapamil, diltiazem, or a pharmaceutically acceptable salt thereof. The composition is used for preventing, delaying progress or treating patients with hypertension, angina pectoris, atherosclerosis, stroke, cardiac insufficiency, dyslipidemia, diabetes, renal function damage or hypertension accompanied by Alzheimer's disease, reducing Reduce the morbidity and / or mortality of cardiovascular and cerebrovascular diseases, reduce adverse drug reactions, and improve patients' compliance with medication.
Owner:王丽燕
Method for selectively synthesizing diltiazemchiral intermediate
The invention provides a method for selectively synthesizing a diltiazem chiral intermediate. P-methoxy cinnamyl aldehyde is used as a main raw material, firstly performs aldolization reaction with tartaric ester to produce an intermediate product 1, then epoxidation reaction is performed with hydrogen peroxide to form an intermediate product 2, oxidization is performed under acidic conditionby using potassium permanganate to obtain an intermediate product 3, ring closing reaction is performed with 2-amino-4-chloro thiophenol after purification to obtain (2S-cis)-(+)-2,3-dihydrogen-3-hydroxyl-2(4-methoxyphenyl)-1,5-benzosulfoazepine-4 (5H)-ketone, the total yield is up to 88.2%, and the optical purity is up to 99.1%.
Owner:郭彦超
Modified release formulations of diltiazem
Modified release diltiazem compositions and associated methods of preparation and administration are provided.
Owner:CAPRICORN PHARMA INC
Compound catching agent for beneficiation of micro-fine particle porphyry molybdenum ore and application of compound catching agent
The invention discloses a compound catching agent for beneficiation of micro-fine particle porphyry molybdenum ore. The compound catching agent comprises the following components in weight ratio: 1-5 percent of hydrocarbon oil, 0.001-1 percent of dithiophosphate matter, 0.001-1 percent of diltiazem matter and 100-200 percent of water. Moreover, the invention also discloses the application of the compound catching agent in the beneficiation of the micro-fine particle porphyry molybdenum ore. The compound catching agent disclosed by the invention is strong in collecting capacity and good in selectivity, in favor of the improvement of the concentrate grade and the recovery rate of molybdenum when being used for the beneficiation of the micro-fine particle porphyry molybdenum ore, and capable of effectively solving the problem that the use ratio of micro-fine particle porphyry molybdenum ore resources is low. Moreover, the dispersibility of the compound catching agent is good in water, so that the dosage of an agent is reduced, mineralization can be accelerated, the flotation time is shortened, and promotion and application are assisted.
Owner:GUANGDONG INST OF MINERAL APPL
Process for preparing diltiazem using a heterogeneous trifunctional catalyst
InactiveUS20040127704A1High enantioselectivityHigh yieldOrganic chemistryOrganic-compounds/hydrides/coordination-complexes catalysts2-AminothiophenolIon exchange
Owner:COUNCIL OF SCI & IND RES
Preparation and purification method of diltiazem chiral isomer impurity
InactiveCN110407771AEasy Preparative SeparationHigh purityOrganic chemistry methodsPurification methodsDiltiazem
The invention provides a method for preparing and purifying a diltiazem chiral isomer. The method comprises the steps of taking p-methoxybenzaldehyde as a starting raw material, carrying out Darzens condensation, a reaction with o-aminobenzenethiol and a cyclization reaction to prepare an intermediate, carrying out chiral column separation on the intermediate, then carrying out an alkylation and acetylation reaction separately to obtain a diltiazem chiral isomer impurity I. The method is simple to operate and short in period, and the purity of the obtained diltiazem chiral isomer impurity is high, so that a reference substance is provided for quality research and drug synthesis process research of diltiazem drugs, and the method has important significance in control and checking of the chiral purity in the pharmaceutical research of diltiazem.
Owner:SHANDONG XINHUA PHARMA CO LTD
Collecting agent for copper and gold ores and method for manufacturing collecting agent
The invention discloses a collecting agent for copper and gold ores. The collecting agent comprises, by weight, 20-23 parts of diltiazem nitrile ester, 20-23 parts of ammonium dibutyl dithiophosphate, 3-5 parts of naphthenic acid, 2-3 parts of oxidized paraffin soap, 3-4 parts of sodium dodecyl benzene sulfonate, 1-2 parts of sodium napthionate, 3-4 parts of sodium oleate, 3-4 parts of sodium fluoride, 7-9 parts of O-alkyl-N-alkyl sulfide thionic carbamate, 6-9 parts of dimethylglyoxime and 10-12 parts of activator. The collecting agent has the advantages that collecting and foaming effects can be realized by the collecting agent, foams are stable, the collecting agent is high in collecting capacity, gold ores are high in recovery rate, selectivity and grade, a copper suppressing effect can be realized, and copper can be prevented from being collected; owing to the activator, surface hydrophobic properties of the gold ores can be changed, internal structures of the gold ores can be activated, the gold collection performance of the collecting agent can be improved, and gold is high in recovery rate and grade.
Owner:ANHUI CHAOSHAN NEW MATERIAL
Collecting agent for low-grade gold ores and method for manufacturing collecting agent
The invention discloses a collecting agent for low-grade gold ores. The collecting agent comprises, by weight, 30-34 parts of diltiazem nitrile ester, 10-12 parts of alkyl xanthate acrylonitrile ester, 10-12 parts of ammonium dibutyl dithiophosphate, 1-2 parts of sodium hydroxide, 17-19 parts of styrene phosphoric acid, 3-4 parts of 4-butanediol vinyl ether, 1-2 parts of potassium dichromate, 2-3 parts of sodium metasilicate, 2-3 parts of diphenyl ethyl phenol-compounded polyoxyethylene ether, 1-2 parts of oleic acid polyoxyethylene ester, 5-7 parts of 2-peracetic acid-group butyric acid and 10-20 parts of activator. The collecting agent has the advantages that the collecting agent can realize capturing and foaming effects, foams are stable, and the collecting agent is high in collection capacity, so that the gold ores are high in recovery rate, selectivity and grade; owing to the activator, surface hydrophobic properties of the gold ores can be changed, internal structures of the gold ores can be activated, accordingly, the gold ore collection performance of the collecting agent can be improved, characteristics of the collecting agents can be played for the low-grade gold ores, the gold ores are high in recovery rate, and gold is high in grade.
Owner:ANHUI CHAOSHAN NEW MATERIAL
Process for preparing diltiazem intermediate
The invention discloses a preparing method of Dierliuzhuo intermediate, which comprises the following steps: adding NaBH4 and optical activated amygdalic derivant in the flask with anhydrous tetrahydropyran solvent and nitrogen condition through stirring; heating to reflux for 3 h to obtain chiral ligand compound; cooling to 0 deg.c; adding Dierliuzhuo intermediate I; cooling until -10- -20 deg.c; insulating to stir for 3 h; adding water with indoor temperature to stop reacting; removing tetrahydropyran solvent through decompressing and distilling; evolving product to obtain isomer of 88% Dierliuzhuo intermediate II (2S,3S).
Owner:NINGBO UNIVERSITY OF TECHNOLOGY +1
Immobilized Serratia lipase, preparation method and application for catalyzing and splitting diltiazem chiral precursor
The invention discloses an immobilized Serratia lipase, a preparation method and application for catalyzing and splitting diltiazem chiral precursor. The immobilized lipase can catalyze and split the diltiazem chiral precursor-racemic p-methoxyphenyl glycidic acid methyl ester ((plus or minus)-MPGM). The invention uses chitosan as immobilized carrier of Serratia lipase, uses glutaradehyde as crosslinker and binds the Serratia lipase on the immobilized carrier in a covalent manner. The immobilized lipase is applied to reaction of enzymatic hydrolysis and splitting of the (plus or minus)-MPGM, and can be repeatedly used for a plurality of times, thus showing good operation stability and practical application feasibility.
Owner:EAST CHINA UNIV OF SCI & TECH +1
Serration and its use in preparation of chiral precurser for dielzepin
InactiveCN100334198CHigh catalytic activityHigh stereoselectivityBacteriaMicroorganism based processesSerratiaDiltiazem
A Serratia bacillus able to generate the stereoselective lipohydrolase features that after it is fermented and cultured, it can generate the lyolipase, which can be used to split the racemate (+ / -)-methylester of p-methoxyphenyl glycilic acid to obtain the (-)-methylester of p-methoxyphenyl glycilic acid, which is the key chiral precursor of diltiazem for treating cardiovascular diseases.
Owner:EAST CHINA UNIV OF SCI & TECH
Parenteral dosage form of diltiazem
ActiveUS20200246254A1Organic active ingredientsPharmaceutical containersParenteral Dosage FormDiltiazem
The present invention relates to a parenteral dosage form comprising a) a ready-to-infuse, stable aqueous solution comprising diltiazem or its pharmaceutically acceptable salt, pH adjusting agent to provide a pH in the range of 3 to 5 and ethanol, and b) an infusion container filled with said aqueous solution.
Owner:SUN PHARMA INDS
Selective synthesis method of diltiazem chiral intermediate
The invention provides a selective synthesis method of diltiazem chiral intermediate. The method is as below: using anisic aldehyde, chloroacetyl chloride and L-menthol as raw materials; first subjecting chloroacetyl chloride and L-menthol to an esterification reaction to obtain an intermediate 1; then subjecting the intermediate 1 with anisic aldehyde to a Darzens condensation reaction to produce diastereomer intermediates 2 and 3; refining to obtain an optically pure intermediate 3; reacting the intermediate 3 with o-aminothiophenol to obtain an intermediate 4; hydrolyzing the intermediate 4 to obtain an intermediate 5; and cyclizing the intermediate 5 to obtain a product. The invention has the advantages that the ester formed by chloroacetyl chloride and L-menthol is selective in the Darzens condensation reaction with anisic aldehyde to generate the more target product, and solubility difference between the target product and the isomer is used to directly obtain optically pure intermediate, without a complicated resolution process, and the yield is greatly improved. The method substantially increases the utilization rate of the main raw material anisic aldehyde and reduces cost.
Owner:SUZHOU KAIYUAN MINSHENG SCI & TECH CORP
Compound antiarrhythmic
The invention relates to a compound anti-arrhythmic drug which is composed of a calcium antagonist verapamil or diltiazem and digitalis drug. The positive inotropic effect of the digitalis drug can resist the negative inotropic effect of the verapamil or the diltiazem, while the effect of delaying the atrioventricular conduction thereof can strengthen the treatment effect of delaying the atrioventricular conduction of the verapamil or the diltiazem. In the compound drug, the used dose of the verapamil or the diltiazem is reduced, thus increasing safety and expanding scope of application.
Owner:田智华
Process for preparing optically active glycidate esters
This invention relates to a method for the production of (2R,3S)-3-(4-methoxyphenyl)glycidic acids and esters thereof, which are synthetic intermediates for the production of the calcium antagonist diltiazem. The method involves the stereoselective enzymatic ester hydrolysis of racemic trans-3-(4-methoxyphenyl)glycidic acid ester to yield the resolved (2R,3S) compound as the ester. Membrane reactor methods and apparatus for the conduct of this enzymatic resolution process are also disclosed herein, as is the use of bisulfite anion in the aqueous reaction phase as a means of minimizing the inhibitory effect of an aldehyde reaction by-product on the reaction's progress. The benefits of selected solvent systems from which may be obtained highly resolved ester product are also disclosed. These enriched organic solutions may be used in subsequent transformations. Alternatively, optically pure product may be obtained directly therefrom.
Owner:SEPACOR INC
Diltiazem controlled release formulation and method of manufacture
A controlled release diltiazem dosage formulation comprising a plurality of diltiazem pellets and a gel-forming material where the time of maximum diltiazem blood plasma levels occurs more than 8 hours after administration and preferably more than 10 hours after administration.
Owner:ANDRX LABS
Chiral P, N, N ligand based on ferrocene skeleton, metal iridium catalyst containing ligand and application of chiral P, N, N ligand
PendingCN121085967AOrganic compound preparationOrganic-compounds/hydrides/coordination-complexes catalystsEpoxyPtru catalyst
The invention discloses a chiral P, N, N-tridentate ligand based on a ferrocene skeleton as shown in a formula I, a preparation method of an iridium catalyst containing the ligand and application of the ligand in preparation of a carbon-nitrogen axial chiral compound and a diltiazem intermediate. According to the present invention, the chiral P, N, N-tridentate ligand based on the ferrocene skeleton and the metal iridium precursor [Ir (COD) Cl] 2 are subjected to complexation to obtain the complex as the iridium catalyst, and the catalyst can be used as the iridium catalyst with characteristics of high yield (up to 99%), high enantioselectivity (up to gt; 99% ee) and high diastereoselectivity (up to gt; according to the method, N-aryl indolal or N-aryl indolone is subjected to asymmetric hydrogenation by using N-aryl indolal or N-aryl indolone (R1, R2, R3, R4, R5, R6, R7, R7, R8, R9, R9, R9, the catalyst can also be applied to asymmetric synthesis of diltiazem intermediate (2R, 3S)-3-(4-methoxyphenyl)-2, 3-epoxidized propionate, has the advantages of short synthesis route, high yield, good stereoselectivity (as high as 99% ee, 97 / 3dr) and the like, and has better economic and social benefits.
Owner:ZHEJIANG UNIV OF TECH
Antiviral compositions for treating the flu
The present invention relates to a pharmaceutical or veterinary composition for the use thereof in preventing and / or treating infection by the influenza viruses. The composition is characterized in that it contains, in an appropriate pharmaceutical carrier, at least one compound selected from among Etilefrine and Diltiazem.
Owner:UNIV CLAUDE BERNARD LYON 1 +3
Method for fast sol-gel preparation of sulfur and nitrogen co-doped nano-titanium dioxide
ActiveCN104028290BSolve the problem of easy generation of white flocOvercome the shortcoming of long experiment periodPhysical/chemical process catalystsLight ActivityPolymer science
The method for preparing sulfur-nitrogen co-doped nano-titanium dioxide by rapid sol-gel disclosed by the present invention is specifically implemented according to the following steps: Step 1, preparing sulfur-nitrogen co-doped nano-titanium dioxide sol-gel precursor; Step 2, taking deionized Adding water to the sulfur and nitrogen co-doped nano-titanium dioxide sol-gel precursor obtained in step 1, stirring and standing to obtain a wet gel; step 3, putting the wet gel obtained in step 2 into an oven, and Carry out drying treatment at 70°C to 90°C to obtain a xerogel with solvent and moisture removed; step 4, grind and calcinate the xerogel obtained in step 3 in turn to obtain anatase-type sulfur-nitrogen co-doping Nano titanium dioxide. The method for preparing sulfur and nitrogen co-doped nano-titanium dioxide by fast sol-gel of the present invention can prepare a sulfur-nitrogen co-doped nano-titanium dioxide photocatalyst with visible light activity, and not only will no white flocculent precipitate form during the gel process , also shortened the production cycle.
Owner:XI'AN POLYTECHNIC UNIVERSITY
Process for recycling L-cis-lactam as diltiazem intermediate by-product
InactiveCN103755663ANo pollution in the processMild reaction conditionsOrganic chemistryDiltiazemSolvent
The invention relates to a process for recycling L-cis-lactam as a diltiazem intermediate by-product. The process comprises the following steps of: reacting by using L-cis-lactam as a raw material, IBX as an oxidizing agent, and DMSO with the water content of 5-15% as a solvent, performing TLC detection and stopping reaction until the raw material disappears, dissolving in water, stirring for an hour and then performing filtration, collecting filter cakes, washing the filter cakes using ethyl acetate, drying a mother liquor, reducing pressure and concentrating to obtain 2-(4-methoxyphenyl)-1,5-benzothiazepin-3,4(2H,5H)-diketone, drying and recycling the filter cakes, and then obtaining IBA. According to the invention, IBX with high selectivity is used as an oxidizing agent, the reaction condition is moderate, the condition of absolute no water and oxygen is not required, the reaction time is shorter, the post-processing is simple, environmental pollution does not exist, and the reduction product IBA of the IBX can be oxidized as IBX again for recycling use, so that the cost is reduced. Therefore, the method has the characteristics of convenience, high efficiency and economy; the yield of target products can reach more than 90%.
Owner:WUHAN INSTITUTE OF TECHNOLOGY
Diltiazem for use in the treatment of microbial infections
The present invention relates to diltiazem for use as an agent activating the expression of at least one gene coding for type III interferon, for the prevention and / or treatment of infections involving at least one pathogenic micro-organism affecting the epithelia of the respiratory and / or intestinal tracts.
Owner:UNIV CLAUDE BERNARD LYON 1 +4
A kind of silicon carbide powder recovery agent
Owner:安徽苏源光伏科技有限公司
Application of a composite collector for beneficiation of fine-grained porphyry molybdenum ore
ActiveCN103769308BStrong harvesting abilityGood choiceFlotationResource utilizationComposite application
Owner:GUANGDONG INST OF MINERAL APPL