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Application of preclinical pharmacokinetic key technology and research system in cefoperazone sodium and sulbactam sodium

A technology of cefoperazone sodium sulbactam sodium and key technologies, applied in preclinical pharmacokinetics key technology and research system in the field of application of cefoperazone sodium sulbactam sodium, can solve the problem of not being able to give full play to structural design and not being able to adapt to the development of new drug research and development models Change and other issues to achieve the effect of improving sensitivity

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

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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 key preclinical pharmacokinetics technology and research system in cefoperazone sodium sulbactam sodium, which includes:

[0019] (1) After administering a certain concentration of cefoperazone sodium and sulbactam 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...

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Abstract

The invention provides application of a preclinical pharmacokinetic key technology and research system in cefoperazone sodium and sulbactam sodium, comprising the steps of (1) after the cefoperazone sodium and sulbactam 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 corresponding solutions; (3) analyzing the prepared solutions 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 cefoperazone sodium and sulbactam sodium. Background technique [0002] Cefoperazone sodium and sulbactam sodium are indicated for the treatment of the following infections caused by sensitive bacteria: respiratory tract infection (upper and lower respiratory tract), urinary tract infection (upper and lower urinary tract), peritonitis, cholecystitis, cholangitis and other abdominal Internal infection, sepsis, meningitis, skin and soft tissue infection, eye infection, bone and joint infection, pelvic inflammatory disease, endometritis, gonorrhea and other genital and tract infections; prevention of abdominal, gynecological, cardiovascular, orthopedic and Postoperative infection caused by plastic surgery. [0003] Pharmacokinetics is a discipline that studies the absorption, distribution, metabolism and excretion process and laws of drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N30/02G01N33/50
CPCG01N30/02G01N33/5008G01N2030/027
Inventor 卢婷刘晓东
Owner 刘晓东
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