66 results about "Sodium loxoprofen" patented technology

The invention discloses a synthetic method for loxoprofen sodium, which is prepared by taking methyl acetophenone as an initial raw material through reduction, acylation or halogen substituent, cyanation, hydrolysis, bromination, condensation, decarboxylation and salifying. The method has the advantages of easily obtained raw material, unique technology, simple and stable operation, and high productive rate in each step of reaction; and all solvents used in the synthesis process can be recycled, so the production cost is reduced greatly. Tests show that the obtained product has reliable quality and stable performance, and can be further used for making preparation of non-steroidal anti-inflammatory drugs such as the loxoprofen sodium.

The invention discloses an improved substrate of a cataplasma and the application thereof to loxoprofen sodium cataplasma. The substrate of the cataplasma adopts the combined application of two or more cross-linking agents and achieves the purposes of increasing the viscosity of a paste and improving the ductibility and moldability of the paste. The application of the substrate can reduce the variety and usage of thickening accessories or can increase the viscosity of the cataplasma to the extent required by a viscous force even without adding special thickening agents. The substrate has advantages in ensuring the good ductibility and moldability of the cataplasma and quickly establishing analytical methods, and the like, thus being significant for the further promotion and application ofthe cataplasma.

The invention discloses a method for synthesizing high-purity non-steroidal anti-inflammatory drug loxoprofen sodium, 2-(4-bromomethylphenyl) methyl propionate b is synthesized by esterification of raw material a and methanol, intermediate compound c and loxoprofen acid are synthesize sequentially, and the loxoprofen sodium is finally synthesized. The reaction mechanism is simple, by-products arefew, synthesis steps are easy to control, the raw material is easily available, and the impurity content of each step is strictly controlled. The purifying method is easy to operate and suitable for industrial production. The white flake crystal loxoprofen sodium is prepared. Finally, HPLC analysis shows that the loxoprofen sodium content detected by HPLC is as high as 99.95%.

The invention discloses an industrial production method of high purity loxoprofen sodium dehydrate; according to the method, adipic acid diester is taken as a starting material for Dieckmann condensation reaction with 2-(4-bromomethyl phenyl) propionate under strong alkaline conditions, the yield and quality of compound II are effectively improved, because the adipic acid diester on the market is lower in cost than 2-ethoxy carbonyl cyclopentanone, the production cost can be greatly reduced; the compound obtained by reaction is processed sequentially by hydrolysis and decarboxylation under acidic conditions, in the hydrolysis and decarboxylation process, generated low boiling point alcohol solvents and carbon dioxide gas can be removed by atmospheric distillation, the reaction can be effectively promoted, the reaction time is shortened, the conversion rate is improved; and finally the final product loxoprofen sodium dehydrate is generated under the condition of aqueous sodium hydroxide solution. The preparation method can greatly reduce the manufacturing cost of loxoprofen sodium, and is more suitable for the industrialized production than the existing technology.

The invention relates to the technical field of organic synthesis, in particular to a method for preparing loxoprofen sodium. The invention provides a compound with the structure shown in formula 5 and a preparation method and application of the compound, (the formula is defined in the description). The loxoprofen sodium obtained according to the scheme is high in purity, high in industrialized operation, and good in application prospect.

The present invention relates to medicine composition soft capsule with loxoprofen sodium as active component and its preparation process. The soft capsule is prepared through preparing the inclusion with the mixture of loxoprofen sodium and several of diluent, co-solvent, solubilizer, suspending agent and surfactant; and the subsequent preparing soft capsule. The soft capsule has high stability of loxoprofen sodium, raised medicine leaching quantity, high bioavailability, high safety and high effectiveness.

The invention relates to a preparation method of a loxoprofen sodium ring opened impurity, and belongs to the technical field of bulk drug preparation. The preparation method comprises the following steps: step one, carrying out substitution reactions between a compound represented by a formula I and hexamethylene tetramine in an organic solvent A, hydrolyzing the reaction product by inorganic acids to obtain a compound represented by a formula II; carrying out condensation reactions between the compound represented by the formula II and a compound represented by a formula III in an organic solvent B to obtain a compound represented by a formula IV; carrying out oxidation and ring opening reactions of the compound represented by the formula IV under the effect of an oxidant and inorganic alkalis to obtain the loxoprofen sodium ring opened impurity represented by a formula V. The invention provides a preparation method of the loxoprofen sodium ring opened impurity.

The invention discloses a method for detecting related substances in Loxoprofen or sodium salt thereof. The method uses a high performance liquid chromatography, gives unique chromatographic conditions and successfully detects a process impurity in the Loxoprofen sodium salt. According to the method, the impurities in the process are detected by using a reverse chromatography, the peak shape is better, the separation degree between the peak shape and an adjacent chromatographic peak is high, the research and development cost is saved, the experiment difficulty is reduced, and the reproducibility is good.

The invention relates to a novel matrix sustained-release tablet containing loxoprofen sodium, in particular to a locoprofen sodium matrix sustained-release tablet with a regulation layer, which is capable of stably releasing for 8 hours, good in releasing effect, simple in process and low in cost.

The invention relates to a loxoprofen sodium composition. Due to the high viscosity of loxoprofen sodium, on one hand, the dispersible tablet of the loxoprofen sodium is easy to clot after being disintegrated, so that the dispersible tablet cannot completely pass through a 2# sieve easily; and on the other hand, the dispersible tablet is easy to absorb moisture, and after the moisture absorption, the tablet is fluffy, the content of the main medicament is decreased, and particularly, the dissolution rate is decreased obviously. According to the loxoprofen sodium composition, a preparation process is changed, and silicon dioxide in the formula is added by an interior addition, so that the composition with high dispersible uniformity and stability is obtained.

A method for producing a fine powder of loxoprofen sodium dihydrate for pharmaceutical preparations, said method comprising milling loxoprofen sodium dihydrate crystals or a crystalline powder of loxoprofen sodium dihydrate with an impact mill, preferably a pulverizer-type mill, which is provided with a built-in air-classifying system and comprises a pin hammer, to thereby continuously produce a fine powder of loxoprofen sodium dihydrate the volume-average particle size of which is in the range of 20-120 [mu]m, when measured with a laser diffraction particle size analyzer.

The invention discloses a method for separating related substances in loxoprofen or sodium salt thereof. According to the method, unique chromatographic conditions are used, and the related substancesin the loxoprofen sodium salt are successfully separated. According to the method, reversed-phase chromatography is used for detection, the peak shape is good, the degree of separation from adjacentchromatographic peaks is high, the research and development cost is saved, the experimental difficulty is reduced, and the reproducibility is good.

The invention discloses a loxoprofen sodium preparation method, which comprises: directly carrying out alkylation on 2-(p-bromomethyl)isophenylpropionic acid as a starting raw material under a NaOH and DMF system, carrying out hydrolysis decarboxylating to obtain a crude product, separating the by-product produced in the reaction through high-vacuum distillation to obtain loxoprofen acid, and carrying out salt forming to obtain the loxoprofen sodium. According to the present invention, the method has characteristics of less synthesis step, mild reaction condition, reasonable price and easy purchase of the raw material, low pollution and low production cost, and is suitable for industrial production, wherein the product content can reach more than 99.8%, and the single impurity is less than0.05%.

The present invention provides loselofen sodium injection and its preparation. Available loselofen sodium dosage forms include oral tablet, capsule and granule only. The Rosorolfine sodium injection of the present invention is used for relieving pain and diminishing inflammation of chronic rheumatic arthritis, rheumatoid arthritis, lumbago, etc. and especially relieving serious pain of postoperation, fracture, strain, etc. It has obvious effects and no addiction. It is prepared by dissolving Rosorolfine sodium in water, adding proper amount of medicinal supplementary material, eliminating pyretogen, disinfection or filtering and may be prepared into water injection, transfusion agent to freezed dried powder for injection.