5 results about "Cefditoren" patented technology

The invention provides a cefditoren pivoxil particle and a preparation method thereof, the particle comprises a cefditoren pivoxil amorphous substance, hydroxypropyl methylcellulose, croscarmellose sodium, sucrose, aspartame, sucrose fatty acid ester, a coloring agent, sodium chloride and fruity essence, and the particle is obtained through a fluidized bed rotational flow side spraying granulation coating technology. The cefditoren pivoxil granules are round, controllable in particle size distribution range, fast in dissolution, good in stability, good in taste, good in in-vivo bioavailability and suitable for clinical use of children and old patients.

The present application relates to the technical field of cefditoren mother nucleus synthesis, in particular to a kind of enzyme method removes 7-position protection cefditoren mother nucleus synthesis process, steps include: 7-position protection cefditoren mother nucleus precursor is dispersed in phosphate buffer, and substrate suspension is obtained;Substrate suspension temperature is controlled, and immobilized acylase is added, and water phase mixture is prepared;Emulsifying agent and extractant are added to organic solvent, stirred and mixed, and oil phase system is obtained;Oil phase system is added to water phase mixture, mixed and emulsified, and oil-in-water emulsion system is formed, temperature is controlled, and enzymatic deprotection reaction is carried out;After enzymatic reaction is finished, immobilized acylase is separated and recovered, and filtrate is demulsified, and after standing and layering, it is separated into water phase and organic phase;Cefditoren mother nucleus is separated from the obtained water phase.The present application uses enzyme catalysis deprotection, avoids the destruction of strong acid and strong base environment to cefditoren mother nucleus β-lactam ring by chemical method, byproduct generation amount is significantly reduced, and reaction condition is mild.

The invention relates to the technical field of test analysis, in particular to a cefditoren pivoxil related substance detection method, which adopts a high performance liquid chromatograph for testing, takes a sodium dihydrogen phosphate solution-acetonitrile-methanol system as a mobile phase, and adds an alkyl sodium sulfonate anion pair reagent into the mobile phase. A neutral ion pair with higher hydrophobicity is formed by the cefditoren acid and the-NH2 group in the cefditoren acid delta 3 isomer, and is in a molecular form, so that the retention time of the neutral ion pair on a chromatographic column is prolonged; meanwhile, the pH value of a sodium dihydrogen phosphate solution is controlled to enable a mobile phase to be acidic, so that-COOH ionization is inhibited, the interaction between ion pairs and a hydrophobic stationary phase in a reversed-phase chromatographic column is improved, proper retention of 14 related substances including the cefditoren acid and the cefditoren acid delta 3 isomer is realized, meanwhile, the 14 related substances are effectively separated, and the quality of the related substances is improved. The detection accuracy and the detection efficiency of the cefditoren pivoxil related substances are improved.

The application provides cefditoren pivoxil granules and a preparation method thereof. The raw materials for preparing the cefditoren pivoxil granules include: a raw drug, a filler, a flavoring agent, a disintegrating agent, a stabilizing agent, a surface active agent, a suspending agent, a glidant and a perfume. The raw drug includes amorphous cefditoren pivoxil, the surface active agent includes vitamin E polyethylene glycol succinate, and the glidant includes silicon dioxide. The application adopts TPGS and silicon dioxide to prepare mixed powder. TPGS is a non-ionic surface active agent and has antioxidant function. The TPGS is used to improve the wettability of the cefditoren pivoxil granules to water, solves the problem of low dissolution caused by the floating of the dry granulation particles on the water surface, prevents the amorphous raw drug from being converted into a crystal raw drug by preferentially adsorbing on the surface of the cefditoren pivoxil crystal nucleus to prevent the crystal nucleus from further growing, and increases the physical and chemical stability of the granules during storage by virtue of the antioxidant function of TPGS.

The application discloses a preparation method of a novel MOM-protected C3 side chain of cefodizime, and belongs to the technical field of pharmaceutical synthesis intermediates. The method is as follows: 2-chloro-3,4-dihydroxybenzaldehyde is used as raw material, and chloromethyl methyl ether (MOMCl) or bromomethyl methyl ether (MOMBr) is used to protect two phenolic hydroxyl groups. After the aldehyde group is oxidized into a carboxylic acid by using a Pinnick method, the carboxylic acid is condensed with 2-chloroethylamine to obtain an amide, and finally, the amide is reacted with tetrahydropyrrole to obtain the target product: 2-chloro-3,4-bis(methoxymethoxy)-(2-(pyrrol-1-yl)ethyl)benzamide. N The application has mild reaction conditions and simple operation, and is suitable for industrialized production of cefodizime.