60 results about "Cefradine" patented technology

Disclosed is a slow release injection containing cephalosporin, which comprises slow release microballoons and dissolvent, wherein the slow release microballoons include slow release auxiliary materials and cephalosporin, the dissolvent being specific one containing suspension adjuvant such as sodium carboxymethyl cellulose, the slow release auxiliary materials are selected from EVAc, PLA, PLGA, sebacylic acid copolymer, albumen glue or gelatin, the slow release microballoons can also be made into slow release implantation agent or ointment.

The invention provides a cefradine capsule and a preparation method thereof. The capsule comprises the following components in weight percentage: 70-90 wt% of cefradine, 5-15 wt% of partial pregelatinized starch, 5-15 wt% of microcrystalline cellulose and 0.1-1 wt% of magnesium stearate. The components in the capsule have good compatibility; the prepared cefradine capsule is good in dissolution and high in stability; the provided preparation method is simple in process and easy in quality control.

The invention discloses a specific monoclonal antibody capable of distinguishing cefalexin, cefadroxil and cefradine, and an enzyme-linked immunosorbent assay method and kit for detecting the cefalexin, the cefadroxil and the cefradine. According to the invention, the monoclonal antibody is secreted by a hybridoma cell strain 3A6 of which the preservation number is CCTCC No.C201340. Compared with the prior art, the monoclonal antibody, prepared by the invention, can be used for distinguishing the cefalexin, the cefadroxil and the cefradine at the same time. The enzyme-linked immunosorbent assay method and kit disclosed by the invention have the advantages of high detection efficiency, high sensitivity, high precision, high accuracy and the like.

The invention provides a medicine for treating epistaxis through oral administration and external use and a method thereof. The following components are combined for use as the medicine in parts by weight: 0.5 part of chloramphenicol tablets, 0.5 part of cefradine injection powder, 0.5 part of furazolidone tablets, 30 parts of radix rehmanniae, 30 parts of prepared rhizome of rehmannia, 25 parts of garden burnet root, 30 parts of golden cypress, 30 parts of fructus forsythiae, 25 parts of caulis spatholobi and 25 parts of liquorice, wherein western medicines, namely the chloramphenicol tablets, the cefradine and the furazolidone tablets, are bactericidal medicines for external use, and wherein traditional Chinese medicines, namely radix rehmanniae, prepared rhizome of rehmannia, garden burnet root, golden cypress, 30 parts of fructus forsythiae, caulis spatholobi and liquorice are decocted with water and used as medicines for oral administration. The medicine provided by the invention is obvious in medicine treatment effect, quick to stop bleeding and worthy of popularization and utilization.

The invention discloses a cefradine compound prepared by adopting a high-flux medicine crystal form rapid screening technology. The 'high-end medicine product refined crystallization technology development and industrialization project' won the second prize of the national scientific and technological process in 2015, and the high-flux medicine crystal form rapid screening technology belongs to one of the high-end medicine product refined crystallization technology. The cefradine compound is measured by adopting X-ray powder diffraction, and main characteristic peaks represented by a diffraction angle 2 theta in an atlas are 11.46+/-0.2 degrees, 18.47+/-0.2 degrees, 20.85+/-0.2 degrees, 23.21+/-0.2 degrees and 29.32+/-0.2 degrees. The compound is high in purity, low in impurity content and good in flowability and stability. Meanwhile, the invention discloses a preparation prepared by adopting cefradine, and the preparation is the cefradine for injection. The preparation is simple in preparation process, does not need any excipient, has the better solubility and stability and is smaller in side effect compared with an existing preparation.

The invention discloses a cefradine compound containing half water and a preparation method thereof. Each mole of cefradine comprises a half mole of water. The cefradine compound has characteristic peaks at the positions with the X-ray diffraction spectrum diffraction angle 2 theta of 7.25+/-0.2 degrees, 10.98+/-0.2 degrees, 14.53+/-0.2 degrees, 16.28+/-0.2 degrees, 17.80+/-0.2 degrees, 19.38+/-0.2 degrees, 20.21+/-0.2 degrees, 22.06+/-0.2 degrees and 22.90+/-0.2 degrees. A crude cefradine product is dissolved in water and adsorbed by activated carbon, and a dissolving and precipitation agentis added for crystallization to obtain a cefradine crystal; the crystal is dissolved in a mixed solution of water and methanol, seed crystals are added, and crystallization is performed to obtain thecefradine compound containing half water. The operation is simple, reactants are easy to obtain, the reaction conditions are mild, and the yield is high. The cefradine compound containing half water has great particle size distribution, high fluidity, low impurity content, high stability and a wider application prospect.

The invention discloses a cefradine synthetase mutant and a coding gene thereof. A protein shown as A) or B) or C) is provided, wherein A) is obtained by substitution of twenty-fourth-site phenylalanine of the beta chain of Escherichia coli natural penicillin G acylase into alanine and substitution of sixty-seventh-site serine of the beta chain of the Escherichia coli natural penicillin G acylase into the alanine; B) is obtained by substitution of 142nd-site methionine the alpha chain of the Escherichia coli natural penicillin G acylase into leucine, substitution of twenty-fourth-site phenylalanine of the beta chain into the alanine, and substitution of sixty-seventh-site serine of the beta chain into the alanine; and C) is a protein derived from the A) or B) by substitution and / or deletion and / or addition of one or a plurality of amino acid residue of the protein defined by the A) or B), and has the ability of synthesis of cefradine. The protein provided on has high activity for synthesis of the cefradine and Vs / Vh and lower alpha, and lays a foundation for the industrialization of the enzyme method synthesis of the cefradine.

The invention discloses a cefradine pharmaceutical composition, which is prepared from the following raw materials in parts by weight: 40 to 50 parts of cefradine, 10 to 20 parts of cyclodextrin, 10 to 20 parts of pregelatinized starch, 2 to 8 parts of sodium hydrogen carbonate, 0.5 to 1.1 parts of citric acid, 0.4 to 1 part of magnesium stearate, 2 to 8 parts of fatty acid sorbitan, 1 to 5 parts of lecithin, 2 to 6 parts of PVC (polyvinyl chloride) and 1 to 5 parts of aerosil. The cefradine pharmaceutical composition is simple and scientific in prescription and high in stability, and has little pharmacological toxic or side effects; in addition, a preparation process is simple and suitable for large-scale production.

The invention belongs to the technical field of prevention and treatment of bovine enterovirus, and particularly relates to application of cefradine as a bovine enterovirus inhibitor. The bovine enterovirus can cause gastrointestinal diseases and respiratory symptoms of cattle, and has serious harm to the breeding industry, research on the bovine enterovirus is little at present, and moreover, effective prevention and treatment drugs have are not disclosed yet. The invention provides application of the cephradine in inhibiting and killing the bovine enterovirus. The research shows that the cefradine can inhibit and kill the bovine enterovirus on an in-vitro MDBK cell model, can effectively inhibit invasion and replication of the bovine enterovirus, has low cytotoxicity, can be used as a new class of bovine enterovirus resisting drugs, lays a foundation for prevention and control of the bovine enterovirus and research and development of the drugs, and also lays an experimental foundation and provides a new visual field for development of high-efficiency specific bovine enterovirus resisting drugs.

The invention discloses a cefradine compound containing one-fifth water and a pharmaceutical composition preparation thereof. Each mole of cefradine contains one-fifth mole of water. The cefradine compound has characteristic peaks at the positions with the X-ray diffraction spectrum diffraction angle 2 theta of 5.50+/-0.2 degrees, 7.21+/-0.2 degrees, 14.49+/-0.2 degrees, 15.69+/-0.2 degrees, 16.24+/-0.2 degrees, 16.66+/-0.2 degrees, 20.16+/-0.2 degrees and 22.04+/-0.2 degrees. First, a dichloromethane solution and mixed anhydride of 7-ADCA tetramethylguanidine are separately synthesized and then reacted with each other to obtain the cefradine compound containing one-fifth water. The operation is simple, reactants are easy to obtain, the reaction conditions are mild, and the yield is high.The cefradine compound containing one-fifth water has low hygroscopicity and impurity content, high fluidity and thermodynamic stability and a wider application prospect.

The invention discloses a preparation method of cefradine with an original research quality on the basis of KR840002043 (B1) and US4235900 (A). The preparation method comprises steps as follows: (1) dihydrophenylglycine chloride hydrochloride is added to a solvent, the mixture is cooled, protected 7-ADCA is added to the mixture, and the mixture is subjected to a condensation reaction after being mixed; (2) water and hydrochloric acid are added after the reaction ends, the mixture is subjected to a hydrolysis reaction, an organic phase layer is left to stand for use, a water layer is subjected to vacuum distillation, and non-distillate is retained; (3) the non-distillate is crystallized and filtered, filtrate is left to stand for use, a filter cake is washed and dried, and cefradine is obtained; (4) the organic phase layer and the filtrate are combined, and cefradine is recycled and extracted. The invention further discloses composition of cefradine with the original research quality. The prepared cefradine and the cefradine composition have the original research quality, the preparation method is simple, the reaction conditions of the whole procedure are relatively mild, the cost of raw materials is low, little pollution is caused, and the prepared cefradine composition has stable and high quality.

The invention provides a method for detecting impurity methyl acetoacetate in cefradine. A GC external standard method is adopted to qualitatively and quantitatively analyze methyl acetoacetate in cefradine, experimental operation is simple, water is used as a solvent in the analysis and detection process, pollution is avoided, chromatographic peaks are free of interference, peak patterns are symmetrical, methodological verification results all meet requirements, and it is shown that the detection method is good in specificity, high in sensitivity and accurate in quantification. The detectionmethod provided by the invention is suitable for detection of methyl acetoacetate in cefradine, and is convenient for large-scale production and control of product quality in a quality control process.

The invention discloses a method for determining the concentration of cefradine in blood plasma through liquid chromatography-tandem mass spectrometry. The method comprises the following steps: (1) carrying out pretreatment on a blood plasma sample; (2) determining the concentration of cefradine in the plasma sample subjected to pretreatment in the step (1) by adopting a liquid chromatography-tandem mass spectrometry method, wherein the liquid chromatography-tandem mass spectrometry comprises chromatographic conditions and mass spectrometry conditions, the chromatographic conditions comprise that an aqueous solution containing 0.1% formic acid and 5mM ammonium acetate is adopted as a mobile phase A, acetonitrile is adopted as a mobile phase B, and a volume ratio of the mobile phase A to the mobile phase B is 70: 30; performing isocratic elution, and the elution time is 3.0 min. By adopting the method disclosed by the invention, the rapid and sensitive detection of the cefradine in theblood plasma can be realized; the plasma consumption is low, and the sample pretreatment is simple.

The invention discloses high-selectivity mutant of cefradine synthesizing enzyme and a coding gene thereof. The invention provides the following protein obtained by the steps of substituting 142-sitemethionine of an alpha chain of natural penicillin G acylase of escherichia coli with phenylalanine, substituting 24-site phenylalanine of a beta chain with alanine and substituting 67-site serine ofthe beta chain with alanine. The protein provided by the invention has higher activity and Vs/Vh for synthesizing the cefradine and lower alpha and lays foundation for industrialization of enzymatic synthesis of the cefradine.

The invention discloses a process method for preparing cefradine through a microreactor. The process method comprises the following main raw materials: mixed anhydride and 7-ADCA. According to the process, a mixed anhydride solution with a certain temperature and a certain flow rate is used as a mobile phase, a 7-ADCA solution with a certain temperature and a certain flow rate is used as a dispersion phase, uniform and rapid mixing and reaction are performed through a membrane dispersion microreactor, and a cefradine solution is prepared. Compared with the prior art, the method has the advantages that various conditions in production can be more accurately controlled, the mass transfer rate is increased, a fine, rapid and controllable continuous production mode is achieved, the productionefficiency is improved, meanwhile, zero application of liquid nitrogen in the production process is achieved, the production cost is reduced, the discharge amount of dichloromethane is reduced, and the pollution to the environment is reduced.