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Application of preclinical pharmacokinetic key technology and research system in ceftizoxime sodium

A technology of ceftizoxime sodium and key technology, which is applied in the field of application of ceftizoxime sodium in the key technology and research system of preclinical pharmacokinetics, which can solve the problem of not being able to give full play to the structure design and not being able to adapt to the development and transformation of new drug research and development models, etc. problem, to achieve the effect of improving sensitivity

Inactive Publication Date: 2016-04-20
刘晓东 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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.

Method used

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Embodiment Construction

[0018] The present invention provides the application of the key technology and research system of preclinical pharmacokinetics in ceftizoxime sodium, which includes:

[0019] (1) After administering a certain concentration of ceftizoxime sodium to the experimental animals for a certain period of time, collect one or more biological samples in blood, urine and feces;

[0020] (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;

[0021] (3) Analyze the solution prepared in step (2) by liquid chromatography-mass spectrometry (LC-MS) or liquid chromatography-tandem mass spectrometry (LC-MS / MS).

[0022] The experimental animals of the present invention may be rats, mice, guinea pigs, rabbits or dogs.

[0023] The certain concentration and certain time are determined according to the experimental animals.

[0024] In a preferred embodiment, in step (2...

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Abstract

The invention provides application of a preclinical pharmacokinetic key technology and research system in ceftizoxime sodium, comprising the steps of (1) after the ceftizoxime sodium with a certain concentration is administrated to an experimental animal for a certain time, collecting one or more biological samples in blood, urine and faeces; (2) treating the biological samples obtained in step (1) by adopting liquid-liquid extraction, albumen precipitation, and solid phase extraction technologies to obtain a corresponding solution; (3) analyzing the prepared solution in step (2) by adopting an LC-MS(liquid chromatography-mass spectrography) and an LC-MS / MS((liquid chromatography-tandem mass spectrometry). According to the application provided by the invention, the Caco-2 cell can also be adopted to detect the membrane permeability of the medicine and cell absorptive capacity; or the medicine with a certain concentration treats primary culture cerebral microvascular endothelial cells to detect the blood-brain barrier permeability of the medicine; or by adopting a whole animal, S9, human intestinal microsome and monoclonal purified enzyme, in vitro metabolism stability of the medicine is detected and a metabolite is identified.

Description

technical field [0001] The invention relates to the application of the key technology and research system of preclinical pharmacokinetics in ceftizoxime sodium. Background technique [0002] The indications for ceftizoxime sodium are lower respiratory tract infection, urinary tract infection, abdominal infection, pelvic infection, sepsis, skin and soft tissue infection, bone and joint infection caused by sensitive bacteria, meningitis caused by Streptococcus pneumoniae or Haemophilus influenzae and uncomplicated gonorrhea. [0003] Pharmacokinetics is a discipline that studies the absorption, distribution, metabolism and excretion process and laws of drugs in organisms, and corresponds to pharmacodynamics, which studies the biological activities of drugs on organisms. Pharmacokinetics focuses on the study of the body's disposal of drugs, but with the development of disciplines and the improvement of research technology, the effect of drugs on the drug disposal system of org...

Claims

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Application Information

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IPC IPC(8): G01N30/02G01N33/50A61K31/546A61P31/04
CPCG01N30/02A61K31/546G01N33/5008G01N2030/027
Inventor 卢婷刘晓东
Owner 刘晓东
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