Application of preclinical drug metabolism and pharmacokinetics key technology and research system to cefoxitin

Abstract

The invention provides an application of the preclinical drug metabolism and pharmacokinetics key technology and a research system to cefoxitin. The application includes the steps that 1, after cefoxitin in a certain concentration is fed to an experimental animal for a certain time, one or more biological samples are collected from blood, urine and feces; 2, the biological samples obtained in the step 1 are treated with the liquid-liquid extraction technology, the protein precipitation technology and the solid phase extraction technology, and corresponding solutions are prepared; 3, the solutions prepared in the step 2 are analyzed with liquid chromatogram-mass spectrum (LC-MS) and liquid chromatogram-tandem mass spectrum (LC-MS / MS). According to the application, the membrane permeation performance and the cell absorbing capacity of the cefoxitin can be further detected through Caco-2 cells, or detection of the in-vitro metabolism stability and identification of metabolite of the cefoxitin are achieved through the whole animal, S9, human intestine microsome and monoclonal purifying enzymes.

Description

technical field [0001] The invention relates to the application of the key technology and research system of preclinical pharmacokinetics to cefoxitin. Background technique [0002] Cefoxitin is weak against Gram-positive bacteria and strong against Gram-negative bacteria. Cefoxitin has antibacterial effects on Escherichia coli, Klebsiella, Haemophilus influenzae, Neisseria gonorrhoeae, Proteus mirabilis, and indole-positive Proteus; it also has a good effect on anaerobic bacteria, such as Peptococcus, digestive Most strains of Streptococcus, Clostridium, Bacteroides (including Bacteroides fragilis); Pseudomonas aeruginosa, Enterococcus and Cloacae are not sensitive to cefoxitin. It is clinically used in infection of the lower respiratory tract, genitourinary system, abdominal cavity, bone and joints, skin and soft tissue, endocardial infection and sepsis caused by sensitive Gram-negative bacteria and anaerobic bacteria. It is especially suitable for aspiration pneumonia c...

AI Technical Summary

Problems solved by technology

With the transformation of my country's new drug R&D model from "imitation-based" to "combination of imitation and innovation" and "innovation-based", the original pharmacokinetic research and evaluation system in my country can no longer meet the needs of the development and transformation of new drug R&D models. Cannot give full play to the guiding role of pharmacokinetic research in the structural design and optimization of lead compounds, the design and modification of new dosage forms, the prediction of drug interactions, and the clinical safety and rational use of drugs, etc.