9 results about "Cefditoren" patented technology

The invention provides a cefditoren pivoxil sustained-release tablet which comprises cefditoren pivoxil, a crystal transformation inhibiting material, a framework material, a pore-foaming agent, an adhesive, an antioxidant and a lubricant, the crystal transformation inhibiting material, the framework material and the adhesive are all polyoxyethylene, the pore-foaming agent is polyethylene glycol 8000, the antioxidant is polyethylene glycol 8000, and the lubricant is polyethylene glycol 8000. The cefditoren pivoxil crystal form can effectively overcome the defect that an existing cefditoren pivoxil preparation is taken many times, can ensure the stability of the cefditoren pivoxil crystal form, can reduce the variety of auxiliary materials in the preparation, and is suitable for commercial production.

The invention provides cefditoren pivoxil granules and a preparation method thereof.The cefditoren pivoxil granules are prepared from raw material medicine, a filler, a flavoring agent, a disintegrating agent, a stabilizer, a surfactant, a suspending aid, a flow aid and essence, the raw material medicine comprises amorphous cefditoren pivoxil, and the filler is a filler, a flavoring agent, a disintegrating agent, a stabilizing agent, a surfactant, a suspending aid, a flow aid and essence; the surfactant comprises vitamin E polyethylene glycol succinate, and the flow aid comprises silicon dioxide. The mixed powder is prepared from the TPGS and the silicon dioxide, the TPGS is a non-ionic surfactant, has the function of an antioxidant and is used for improving the wettability of cefditoren pivoxil particles to water, and the problem that the dissolution rate is low due to the fact that dry granulation particles float on the water surface is solved; the TPGS can also be preferentially adsorbed on the surface of a cefditoren pivoxil crystal nucleus to prevent further growth of the crystal nucleus, so that an amorphous raw material medicine is prevented from being converted into a crystal-form raw material medicine, and the TPGS has an antioxidant function, so that the physical and chemical stability of the granules in the storage process is improved.

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 invention discloses a quality analysis and optimization method and system for cefditoren pivoxil based on artificial intelligence, and relates to the technical field of pharmaceutical manufacturing, the method comprises the following steps: step S1, collecting process parameters and quality data of the whole production process of cefditoren pivoxil in real time; step S2, preprocessing the collected process parameters and quality data; s3, establishing a quantitative relation model between the key process parameters and the quality attributes based on a machine learning algorithm, and identifying the key process parameters and key operation intervals; s4, establishing a multi-objective optimization model to synchronously optimize product quality attributes and production cost, and adding a quality standard which must be met by an optimal solution as a constraint condition; and S5, outputting the optimized process parameters and the corresponding quality control standards to a production control system. According to the invention, by integrating artificial intelligence and a multi-objective optimization method, precise control of a production process and precise prediction of product quality are realized.

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.

The invention discloses a cefditoren pivoxil granular preparation and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations. Comprising the following raw materials in parts by weight: 50-60 parts of a cefditoren pivoxil self-microemulsion drug delivery system, 30-50 parts of a filling agent, 0.5-3 parts of a disintegrating agent, 0.1-2 parts of an adhesive, 1-7 parts of a sweetening agent, 0.1-2 parts of a flavoring agent, 0.1-2 parts of a thickening agent and 0.01-0.05 part of an aromatic. According to the invention, a novel oral administration system, namely a self-emulsifying administration system, is adopted, so that the problem of dissolvability of an indissolvable drug, namely the cefditoren pivoxil, can be well solved, and the prepared cefditoren pivoxil granules have good dissolution release rate and are affirmative in the aspect of improving the oral bioavailability of the drug. In addition, the prepared cefditoren pivoxil particles are uniform in particle size distribution and good in taste, content, content uniformity and preparation stability.