6 results about "Cefepime" patented technology

The invention provides a fluorenyl alcohol derivative which can be used as an antibiotic adjuvant with a broad-spectrum synergistic effect. According to the compound, bacteria outer membrane asymmetric protein MlaC and phospholipase A1 PldA are taken as targets, and a series of fluorenyl alcohol derivatives targeting the bacteria outer membrane asymmetric protein MlaC and phospholipase A1 PldA are obtained through screening. The preferable compound WTU-15 can improve the antibacterial activity of antibiotics such as polymyxin, cefepime, tetracycline and the like on negative bacteria such as sensitive and drug-resistant escherichia coli, salmonella, klebsiella pneumoniae, acinetobacter baumannii and the like, and can also improve the in-vivo treatment effect of cefepime on mice infected by the drug-resistant acinetobacter baumannii. And the visceral organs of the mice survived after administration have fewer bacteria, and the mice are better after being healed. Normal physiological and visceral organ functions of the mouse are not affected by single and continuous administration of the WTU-15.

The application belongs to the technical field of biological medicine, and particularly relates to a sterile cefepime hydrochloride and a direct preparation method thereof. The method comprises the following steps: firstly, 7-MPCA solution and AE active ester solution are simultaneously subjected to condensation reaction through a solid alkali catalyst column; then, the condensation liquid is subjected to extraction and phase separation, twice pH adjustment and crystallization, active carbon decolorization and sodium sulfite reduction to obtain cefepime hydrochloride to be crystallized; then, a part of the cefepime hydrochloride to be crystallized is prepared into a seed crystal mixed solution, the remaining cefepime hydrochloride to be crystallized and a crystallization solvent are added into the seed crystal mixed solution at a specific speed to obtain sterile cefepime hydrochloride. The method realizes continuous production of sterile cefepime hydrochloride, greatly shortens the preparation period of sterile cefepime hydrochloride, reduces side reactions and product degradation, and the obtained cefepime hydrochloride product is high in quality and yield and stable, and is beneficial to industrial production.

The application discloses a preparation method of high-purity cephalosporin bipu ester side chain (1a), and a reaction route is shown as follows. The method is characterized in that 2a is used as a starting material to react with triphosgene to generate compound 3a, and then the compound 3a is used to react with p-nitrophenol to generate compound 1a. The product has high purity and high reaction yield, and is suitable for industrial production.

The invention provides a synthesis method of cefepime starting material oxidation impurities, and belongs to the field of medicinal chemistry. The cefepime is prepared by modifying a 7-site amino side chain of D-7-ACA, oxidizing a 3-site hydroxyl, carrying out wittig reaction with a starting material, and then carrying out deprotection. When the starting material is subjected to wittig reaction, the ylide generated by the starting material can be oxidized to generate oxidized impurities. The method comprises the following steps: reacting a cefepime starting material with a strong base to generate a ylide intermediate, and continuously introducing new oxygen into the ylide intermediate to prepare the cefepime starting material oxide impurity. The preparation and separation method of the cefepime starting material oxidation impurity provided by the invention has the advantages of simplicity in operation, environmental friendliness, low cost and high purity of the obtained impurity, and lays a good foundation for quality research and control of cefepime.

This invention discloses a method for simultaneously detecting cefepime and its metabolites, as well as prednisolone residues in milk. The method includes the following steps: taking a milk sample, extracting with acetonitrile, centrifuging, and collecting the supernatant; adding acetonitrile-saturated n-hexane for liquid-liquid extraction to remove fat; concentrating the extracted solution, reconstituted with phosphate buffer at pH 8.5 ± 0.2, purifying with a hydrophilic-lipophilic equilibrium solid-phase extraction column, eluting, concentrating, and reconstituted to obtain the test solution; and detecting the test solution using ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS / MS). This invention, through optimized pretreatment processes, particularly the dual purification strategy of "n-hexane degreasing + HLB solid-phase extraction" combined with precise pH adjustment, effectively removes complex fat and protein matrix interferences in milk, significantly reducing matrix effects; combined with optimized gradient elution procedures and multiple reaction monitoring (MRM) mass spectrometry conditions, it achieves simultaneous, rapid, and highly sensitive detection of cefepime, deacetylated cefepime, and prednisolone.

The application discloses a detection kit for simultaneously determining the concentrations of 12 kinds of antibiotic drugs in trace serum and application, the 12 kinds of antibiotics including vancomycin, meropenem, imipenem, cilastatin, trimethoprim, linezolid, voriconazole, piperacillin, cefoperazone, sulfamethoxazole, cefepime and ceftazidime; the detection kit comprises pretreatment reagents and a liquid chromatography mobile phase; the pretreatment reagents comprise a protein precipitant and purified water; the protein precipitant comprises 50v / v% of methanol and 50v / v% of acetonitrile; the liquid chromatography mobile phase comprises phase A and phase B, the phase A comprises 0.02% of formic acid and 99.98% of water, and the phase B comprises 100% of acetonitrile. The method of the application only needs 10 muL of human serum sample, and can complete the detection within 4 min, can quantitatively determine 12 kinds of antibiotics with significant structural differences, and is simple, rapid, sensitive, accurate and specific.