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...

Examples

Embodiment Construction

[0017] The present invention provides the application of key preclinical pharmacokinetics technology and research system in cefoxitin, which includes:

[0018] (1) After administering a certain concentration of cefoxitin to the experimental animals for a certain period of time, collect one or more biological samples in blood, urine and feces;

[0019] (2) Process the biological sample obtained in step (1) by liquid-liquid extraction, protein precipitation, and solid-phase extraction techniques to prepare a corresponding solution;

[0020] (3) Analyze the solution prepared in step (2) by liquid chromatography-mass spectrometry (LC-MS) or liquid chromatography-tandem mass spectrometry (LC-MS / MS).

[0021] The experimental animals of the present invention may be rats, mice, guinea pigs, rabbits or dogs.

[0022] The certain concentration and certain time are determined according to the experimental animals.

[0023] In a preferred embodiment, in step (2), the liquid-liquid extr...

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...

Examples

Embodiment Construction

[0017] The present invention provides the application of key preclinical pharmacokinetics technology and research system in cefoxitin, which includes:

[0018] (1) After administering a certain concentration of cefoxitin to the experimental animals for a certain period of time, collect one or more biological samples in blood, urine and feces;

[0019] (2) Process the biological sample obtained in step (1) by liquid-liquid extraction, protein precipitation, and solid-phase extraction techniques to prepare a corresponding solution;

[0020] (3) Analyze the solution prepared in step (2) by liquid chromatography-mass spectrometry (LC-MS) or liquid chromatography-tandem mass spectrometry (LC-MS / MS).

[0021] The experimental animals of the present invention may be rats, mice, guinea pigs, rabbits or dogs.

[0022] The certain concentration and certain time are determined according to the experimental animals.

[0023] In a preferred embodiment, in step (2), the liquid-liquid extr...