67 results about "Naproxenum" patented technology

The invention relates to a preparation method and application of a typical acidic drug multi-template molecularly imprinted polymer. The adopted template molecules are clofibric acid, diclofenac sodium, ibuprofen, naproxen and ketoprofen. The preparation method and the application of the molecularly imprinted polymer belong to the technical field of analysis, determination and removal of five typical acidic drugs in environmental samples. The preparation method is simple and reliable, and the prepared multi-template molecularly imprinted polymer has a uniform size, a large specific surface area and higher specific selectivity for acidic drugs. The five acidic drugs in the environmental samples can be separated and gathered rapidly and efficiently. The multi-template molecularly imprinted polymer can be directly applied in selective removal of the five acidic drugs in surface water and has better effects than other adsorption materials. The method is an effective method for specific separation of a series of substances with the same attributes and has broad application prospects.

The invention discloses a molecularly imprinted membrane with a selective-separation chiral drug and a preparation method of the membrane. According to the invention, D-naproxen is taken as template molecules, a PVDF (Polyvinylidene Fluoride) hollow fiber separation membrane is taken as a base material, and the D-naproxen imprinted molecules are packaged in a fenestra grafting gel layer in a surface finish process to prepare the D-naproxen imprinted PVDF hollow fiber membrane. The molecularly imprinted separation membrane prepared by the method has good adsorption and separation functions to naproxen chiral drug molecules, has a desorption rate up to 90%-95.78%, can realize the intelligent regulation and control on combination and release of D-naproxen and solves the problem of uncontrollability on the shape and size of cavities and the affinity of template molecules of the conventional molecularly imprinted membrane. According to the invention, the mature PVDF hollow fiber membrane on the market is taken as a base membrane of the molecularly imprinted membrane, and an N-isopropyl acrylamide monomer (NIPAAm) of the conventional thermo-sensitive hydrogel is taken as a functional monomer; and the preparation method is simple, low in production cost as not needing special equipment, and suitable for industrialized application.

The invention discloses a naproxen esomeprazole enteric preparation and a preparation method thereof, wherein the preparation is obtained by filling a naproxen enteric pill and an esomeprazole thin membrane coated tablet into the same capsule, wherein each esomeprazole thin membrane coated tablet contains 20 mg esomeprazole, and the naproxen enteric pill in each capsule contains 375mg or 500mg naproxen. The preparation method for the naproxen esomeprazole enteric preparation is that the naproxen and the esomeprazole are prepared into the enteric pill and tablets respectively, and thus, influences of the acid enteric material on the stability of the esomeprazole are avoided; moreover, the method is reasonable in design, simplified in a coating step and simple in process; and the prepared naproxen esomeprazole enteric preparation has stable quality, high bioavailability, a high economic value and important social meaning.

The invention discloses a degradation prediction method for removing micro-pollutants in secondary effluent by ultraviolet / sodium persulfate. The method includes the following steps: S1, selecting p-chlorobenzoic acid and naproxen as reference materials, and establishing a reaction kinetics model of target pollutants, p-chlorobenzoic acid, naproxen and free redicals under ultraviolet / sodium persulfate; S2, adding the target pollutants, p-chlorobenzoic acid and naproxen into actual water, and oxidative degradation is carried out by using ultraviolet / sodium persulfate advanced oxidation technology; and S3, calculating the free radical content according to a degradation effect of the p-chlorobenzoic acid and naproxen by using the model, and predicting degradation conditions of the target pollutants. The model is established by measuring the degradation of the two reference materials to fit the degradation of the multiple pollutants in the secondary effluent under the ultraviolet / sodium persulfate, thereby evaluating the feasibility of removing the target pollutants in the secondary effluent by the ultraviolet / sodium persulfate and effectively reducing the cost of small tests.

The present invention relates to compositions and methods for providing improved treatment, management or mitigation of cold, cold-like, allergy, sinus and / or flu symptoms by administering a safe and effective amount of a composition comprising naproxen along with cetirizine.

An NSAID formulation for encapsulation into a soft gel capsule with increased stability, concentration and bioavailability of the NSAID. The preferred NSAIDS are naproxen, ibprofen, indomethacin and diclofenac, which are provided in both an acidic and basic form in the fill formulation. The pH values of fill formulations may be adjusted without additional process steps. A process for increasing the achievable concentration of an NASAID pharmaceutical ingredient in a fill composition for dosage units is also provided. The highly concentrated NASAID formulation permits a reduction in the fill volume or dosage unit size or an increase in concentration of the NSAID in each dosage it.

The invention discloses a novel asymmetric catalytic synthesis method of (S)-naproxen. According to the method, racemic 2-halogenated propionate is used as an initial raw material to perform an asymmetric Kumada cross-coupling reaction with 6-methoxyl-naphthyl grignard reagent in the catalysis of bisoxazoline / cobalt to prepare (S)-naproxen ester, and the ee value is increased by using a re-crystallization method, and the (S)-naproxen is prepared by catalytic hydrogenation. The synthetic route is simple and short, is a two-step reaction, the total yield of the whole synergetic route is 43 percent, and the optical purity of the product is more than 99 percent.

The present invention designs and synthesizes the ascorbyl ester derivatives of the aryl (ethanoic) propanoic acid non-steroidal anti-inflammatory medicaments, such as ibuprofen, ketoprofen and naproxen, and addition salt of the derivatives with pharmaceutical acid or pharmaceutical alkaline. The non-steroidal anti-inflammatory medicament which takes the ibuprofen as the representative is a common antipyretic analgesic medicament. The invention has remarkable antipyretic and analgesic effects and good safety except for anti-inflammatory effect, thus being not only suitable for adults, but also suitable for the elderly people, infants and children. The aryl (ethanoic) propanoic acid ascorbyl ester can be converted into ascorbyl ester derivatives and the addition salts of the derivatives with pharmaceutical acid or pharmaceutical alkaline, which can improve the water solubility thereof, facilitate intravenously administration, reduce the onset time, improve the bioavailability, reduce the stimulation effect to gastrointestinal tract, and enhance the penetrating capacity to hemato encephalic barrier, and can be used as a novel medicament to be applied for antiphlogistic, antipyresis, analgesia, treatment of arthritis, dysmenorrheal, multiple sclerosis, pneumonia cystic fibrosis and patent ductus arteriosus of premature infants, and prevention and treatment of cerebral apoplexy, hypoxic-ischemic brain damage, senile dementia and certain cancers.

The invention relates to a medical composition used for the febrifuge, analgesia and anti-inflammation of the animals, a preparation method and the application thereof. The medical composition comprises diclophenac sodium and naproxen. The weight proportion of the diclophenac sodium and the naproxen is 1:10-10:1 while the preferred scope is 1:5-5:1. The invention also provides the preparation method of the injection of the medical composition and the application in the control of livestock and poultry pyrexia. The invention has more thorough febrifuge effect than any single preparation with the characteristics of fast action and uneasy rebound relative to the oral preparation.

The present invention relates to one kind of veterinary medicine composition for eliminating fever, relieving pain and diminishing inflammation and its preparation process and use. The veterinary medicine composition consists of diclofenac sodium and naproxen in the weight ratio of 0.1-10, preferably 0.2-5; or consists of diclofenac sodium and barbitone in the weight ratio of 0.2-10, preferably1-7.5. The veterinary medicine composition is used in preventing and treating feverish animal diseases and has synergistic fever eliminating effect, fast acting and less recurrence.

The invention provides a method for preparing naproxen, which uses a carrier, a catalyst and an organic solvent. The method is characterized in that: ionic liquid is used in place of the conventional catalyst and organic solvent; the hydrophobic carrier is used to cure lipase; isooctane and ethyl ether are used to extract a substrate remaining after reaction and the reaction product; the ethyl ether is removed by a vacuum method; an organic solvent is used for extraction; the recycling of the ionic liquid is realized; and at the same time, quick inactivation caused by the direct contact of the lipase with a polar organic solvent is avoided, the conversion rate is high and cost is saved.

The invention provides a composition consisting essentially of a solid naproxen concentrate, wherein the solid naproxen concentrate comprises (a) a solid naproxen free acid and (b) a solid naproxen alkali salt, and wherein at least 90% of the weight of the solid naproxen concentrate is naproxen free acid and naproxen alkali salt, as well methods of producing such a solid naproxen concentrate.

The invention discloses an aryl naproxen derivative high-valence iodine compound, a preparation method and application thereof, wherein a series of naproxen derivatives are prepared through preparation and derivatization of naproxen high-valence iodine compounds. The compound can realize nucleophilic substitution reaction of specific sites on naproxen molecule aryl, so that the purpose of modifying the drug molecules is achieved, and the variety of the drug molecules is expanded. The invention also provides a preparation method of the compound, wherein the method comprises the following steps:synthesizing a naproxen derivative, and carrying out anion ligand exchange reaction on the naproxen derivative and a koser reagent derivative or an aryl iododiacetic acid compound to prepare the arylnaproxen derivative high-valence iodine compound. The high-valence iodine compound can perform concise and clear structural modification on naproxen molecular aryl, realizes rapid synthesis of structural diversity of drug molecules through accurate modification at specific sites, is convenient for rapid construction of a huge drug-like compound library, and greatly promotes the discovery processof naproxen drug active primers.

The invention relates to a method for separating naproxen enantiomers by adopting a centrifugal extractor and carrying out multi-stage counter current extraction. The invention provides a new method for separating the naproxen enantiomers. The method for separating the naproxen enantiomers is characterized in that the naproxen enantiomers are selectively distributed in an organic phase / aqueous phase in a three-dimensional way due to selective complexation between water-soluble beta-cyclodextrin and the naproxen enantiomers; and the aqueous phase and the organic phase are rapidly mixed and rapidly separated by virtue of a centrifugal acting force of the centrifugal extractor, so that transmission and reaction of the naproxen enantiomers in the aqueous phase and the organic phase are accelerated. The method for separating the naproxen enantiomers has the advantages that the problems that mass transfer efficiency of a general extraction technique is low and product purity is low are overcome; rapid and high-selectivity separation on the naproxen enantiomers is realized by carrying out multi-stage equilibrium extraction; meanwhile, equipment adopted by the method provided by the invention is simple and is easy to operate.

The invention belongs to the technical field of waste water treatment and relates to a device and method for treating naproxen waste water under a low temperature environment. The device is composed of a water distribution chamber, an anaerobic magnetic-force intensified biological filter tank, an electric-biological degradation reaction tank and an aerobic magnetic-force intensified biological filter tank, and a negative plate (13) and a positive plate (14) of the electric-biological degradation reaction tank are in series connection between a spiral coil (11)of an aerobic magnetic biological filter material layer (5) and a spiral coil (11) of an anaerobic magnetic biological filter material layer (6), then are in series connection with a sliding resistor (21) and then are connected with a direct current power source (1). Water is treated through the water distribution chamber, the anaerobic magnetic biological filter material layer (6), a filling particle electrode layer (4) and the aerobic magnetic biological filter material layer (5) in sequence and then drained out. The device is compact in arrangement and simple in structure, and the naproxen waste water is treated physically, chemically and biologically under the low temperature condition, so that the removal purpose is achieved.

The invention discloses an IDO inhibitor, a preparation method, a pharmaceutical composition and application. The structure of the inhibitor is as shown in a formula (I), and the inhibitor comprises isomers, pharmaceutically acceptable salts or a mixture of the isomers and the pharmaceutically acceptable salts. The IDO inhibitor and the pharmaceutical composition thereof have an efficient inhibition effect on IDO, and can be used as a medicine for treating inflammatory diseases such as rheumatoid arthritis and the like; the prepared medicine can exert efficacy at the molecular level and the animal level, the anti-inflammatory activity is superior to that of naproxen, and the compound is simple and convenient in synthesis method and easy to operate.

The invention discloses an injectable naproxen preparation. The injectable naproxen preparation comprises at least one of phosphate or citrate, wherein the phosphate or the citrate is tribasic acid salt, the phosphate (sodium salt or potassium salt) or the citrate (sodium salt or potassium salt) is alkaline after dissolving in water and is a solubilizing agent, the dissolving property of naproxen in a neutral pH value buffer aqueous solution can be improved, and the balance distribution ratio of the content of the effective component naproxen to the content of precursor sodium salt in the solution is obviously improved; and besides the three forms of the phosphate or the citrate also play a role of a stabilizer, so that the storage time of the injectable naproxen preparation can be remarkably prolonged. When the phosphate or the citrate is used together, a pH buffer system formed by the phosphate and the citrate is more stable through the synergistic effect of the phosphate and the citrate. The stable injection with the neutral pH value is expected to be capable of reducing or eliminating untoward effects such as burning sensation generated at injection positions of clinical injections and along veins.

The invention discloses a method for dynamic kinetic resolution of alpha-aryl-alpha-alkyl carboxylic ester and application, and belongs to the technical field of organic synthesis. Pentafluorophenol ester and benzhydrol are taken as reactants, a dynamic kinetic resolution reaction is carried out under the nitrogen-oxygen catalysis of chiral DMAP derived from diphenylmethylamine to obtain alpha-aryl-alpha-alkyl ester, and (S)-naproxen, (S)-ibuprofen, (S)-ketoprofen, (S)-fenopolfen and (S)-flurbiprofen are synthesized. According to the chiral DMAP nitrogen-oxygen catalyst, oxygen atoms in pyridine nitrogen-oxygen serve as nucleophilic sites to participate in a dynamic kinetic resolution reaction, and meanwhile hydrogen in catalyst molecules also plays a key role. The method has the advantages of good yield, high enantioselectivity and the like.

The invention discloses a novel process for synthesizing racemic naproxen based on Heck coupling, which comprises the following steps: (1) carrying out Heck coupling reaction on 2-X substituted-6-methoxynaphthalene and crotonamide in an aprotic organic solvent under the action of a palladium catalyst and alkali to generate 3-(6-methoxynaphthyl-2-)-crotonamide; and (2) carrying out Hofmann degradation reaction on the 3-(6-methoxynaphthyl-2-)-crotonamide in an alkaline solution of hypochlorite to generate 2-(6-methoxynaphthyl-2-)-propionaldehyde, directly adding the 2-(6-methoxynaphthyl-2-)-propionaldehyde into chlorite without separation, and conducting oxidizing at room temperature to obtain racemic naproxen. The process provided by the invention does not need to prepare a highly active Grignard reagent, does not need a harsh anhydrous condition, and is relatively high in conversion rate and easy in product purification.

The invention discloses a naproxen injection and a preparation method thereof. The naproxen injection is prepared from a certain proportion of naproxen, a salt-forming agent, a complexing agent, a stabilizer, an adsorbent and water for injection. The preparation method comprises the following steps: 1) preparing a salt-forming agent solution from the salt-forming agent by using the water for injection; and 2) adding the naproxen into the remaining water for injection, adding the salt-forming agent solution, performing continuous stirring until the naproxen is completely dissolved, adding the complexing agent and the stabilizer, performing uniform stirring, wherein the pH value of the system at the time is 7.5-9.0, adding the adsorbent, performing uniform stirring, allowing the mixture to stand for 20-30 min, performing filtration, performing filling, introducing nitrogen, performing sealing, and finally performing sterilization for 25-35 min at 115-121 DEG C. The injection has high stability, and can be used for intramuscular administration, the administration is convenient and rapid, and the injection has a small preparation volume, and is convenient for transportation, and low intransportation cost.

The invention discloses a capsule preparation for treating arthritis caused by rheumatic fever. The capsule preparation is prepared from the following main raw materials in parts by weight: 5-15 parts of radix clematidis, 4-14 parts of ligusticum wallichii, 0.5-0.9 part of procaine, 1-3 parts of earthworm, 4-11 parts of ephedra, 8-16 parts of myrrh, 2-7 parts of naproxen, 1-5 parts of acetylsalicylic acid, 3-7 parts of indometacin, 6-10 parts of beautiful sweetgum fruit, 3-9 parts of serrate clubmoss herb, 3-8 parts of the seed of Chinese dodder, 1-6 parts of robust leontice rhizome and root and 4-8 parts of tiger bone-glue. The capsule preparation for treating arthritis caused by rheumatic fever disclosed by the invention has the effects of promoting blood circulation to remove blood stasis, clearing and activating the channels and collaterals, strengthening tendons and bones and dissipating blood stasis and relieving pain. The medicinal materials disclosed by the invention are readily available in medicine source and low in cost, most of the selected medicinal materials are mild in medicine properties, and even if the medicine is taken for a long time, the economical and physical burdens of the user are not increased.

The invention includes 2-β-naphthyl-acetic acid derivatives, which are selective AKR1C3 inhibitors. In certain embodiments, the compounds of the invention are (R)-naproxen analogs. The invention further includes methods of treating cancer, such as prostate cancer and / or castration-resistant prostate cancer, using at least one compound of the invention.

An NSAID formulation for encapsulation into a soft gel capsule with increased stability, concentration and bioavailability of the NSAID. The preferred NSAIDS are naproxen, ibprofen, indomethacin and diclofenac, which are provided in both an acidic and basic form in the fill formulation. The pH values of fill formulations may be adjusted without additional process steps. A process for increasing the achievable concentration of an NASAID pharmaceutical ingredient in a fill composition for dosage units is also provided. The highly concentrated NASAID formulation permits a reduction in the fill volume or dosage unit size or an increase in concentration of the NSAID in each dosage it.

The invention discloses a chiral silver nanocluster and preparation and application thereof. The molecular formula of the chiral silver nanocluster is Ag40(TBBM)22(CH3COO)10 which is abbreviated as Ag40, wherein TBBM is p-tert-butyl benzyl mercaptan. The Ag40 nanocluster provided by the invention can realize sensitive, rapid and quantitative reaction with chiral carboxylic acid drugs (such as 2-chloropropionic acid, ibuprofen, naproxen, isoleucine and the like) so as to allow the chiral signals of the chiral carboxylic acid drugs to be transmitted to the Ag40 nanocluster, so the content and the chiral e.e. value of the chiral carboxylic acid drugs can be conveniently measured. According to the invention, reaction conditions are mild; operation is simple; and a substrate can be recycled andhas good universality.

The invention relates to a medical composition used for the febrifuge, analgesia and anti-inflammation of the animals, a preparation method and the application thereof. The medical composition comprises diclophenac sodium and naproxen. The weight proportion of the diclophenac sodium and the naproxen is 1:10-10:1 while the preferred scope is 1:5-5:1. The invention also provides the preparation method of the injection of the medical composition and the application in the control of livestock and poultry pyrexia. The invention has more thorough febrifuge effect than any single preparation with the characteristics of fast action and uneasy rebound relative to the oral preparation.

The invention belongs to the technical field of chemical synthesis, and relates to a synthetic method of chiral 2-aryl propionate, in particular to enantioselective synthesis of 2-aryl propionate. Thesynthetic method comprises the following steps: adding a copper salt, a chiral phosphine ligand, a silicon-hydrogen compound (in terms of SiH), R<1>OH and 2-aryl acrylate in a certain ratio into a reaction bottle, carrying out a reaction in a reaction solvent at -50 to 40 DEG C for 0.25-6 h, and successively performing hydrolyzing, liquid separating, extracting, washing, drying and column chromatography after the reaction is finished, thereby obtaining the target compound 2-aryl propionate. Compared with the prior art, the method has the advantages that the 2-aryl acrylate is reduced by adopting a Cu catalytic system, a catalyst, namely a Cu compound is low in price, and the limitation of hydrogen high-pressure reduction and a noble metal catalyst is broken through. Chiral 2-aryl propionic acid can be obtained through a simple hydrolysis reaction of 2-aryl propionate, and a part of the compounds of 2-aryl propionate are effective components of current commercially-available drugs suchas ibuprofen and naproxen.

The invention relates to a method for determining the excess rate of 1-NEA enantiomers. The method comprises the following steps of: (1) derivatization, and (2) separation and detection. According to the method, (S)-naproxen acyl chloride is adopted as a derivatization reagent to be subjected to a rapid derivatization reaction with the 1-NEA, and then the (S)-naproxen acyl-1-NEA is subjected to qualitative analysis, quantitative analysis and enantiomer excess rate determination by using common reversed-phase HPLC-UV. The method is simple, fast, effective and low in cost.

The invention relates to an efficient recycling method for synthesizing neopentyl glycol by a side product 3, 3-dimethyl propylene oxide of the neopentyl glycol procreant in a naproxen synthetic process. Toluene solution containing 3, 3-dimethyl propylene oxide procreant in the naproxen synthetic process is used as raw material and has a full reaction under the effect of an acid catalyst; and thenepentyl glycol is obtained right after the reaction liquid is separated and purified. The mass ratio of 3, 3-dimethyl propylene oxide to the acid catalyst is 5.6-100:1. The method is used for recycling the neopentyl glycol by the side product 3, 3-dimethyl propylene oxide, which is safe and pollution-free, and has high yield coefficient, simple operation, and extensive industrialization prospect.

The invention relates to carboxylesterase, a coding gene thereof, genetic engineering constructed by the coding gene, and application of the carboxylesterase in preparation of S-naproxen through microbial catalysis. The amino acid sequence of the carboxylesterase is as shown in SEQ ID NO.2, and the nucleotide sequence of the coding gene is as shown in SEQ ID NO.1. An engineering bacterium constructed by the gene is used for producing S-naproxen through enzymic method stereoselective catalysis, the method has the characteristics of high space time yield and stable effect, the conversion efficiency can reach 48% or above within a short time, the optical purity can reach 99% or above, and the method has important significance on production of high-yield and high-purity S-naproxen.