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Method for detecting concentration of metacavir and metabolites thereof in biological sample

A technology for biological samples and metabolites, applied in measuring devices, instruments, scientific instruments, etc., can solve the problems of unreported content determination

Active Publication Date: 2013-10-23
GUANGZHOU YIPINHONG PHARMA +4
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] There are many preclinical studies on PNA. After intragastric administration of PNA to rats, it quickly reaches its peak and is quickly eliminated in the body. It seems that the prototype drug does not exert its medicinal effect. However, consulting domestic and foreign literature, PNA and its metabolism in human biological samples Product DDG and O 6 -The content determination of methylguanine and the study of its pharmacokinetics have not been reported

Method used

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  • Method for detecting concentration of metacavir and metabolites thereof in biological sample
  • Method for detecting concentration of metacavir and metabolites thereof in biological sample
  • Method for detecting concentration of metacavir and metabolites thereof in biological sample

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] 1 Instruments, materials and reagents

[0020] 1.1 Instrument Agilent 1290 ultra-high performance liquid chromatograph equipped with 6460 triple quadrupole mass spectrometer, Agilent Company of the United States.

[0021] 1.2 Sample and reagent PNA (content is 100% based on anhydrous substance), provided by Nanjing Changao Pharmaceutical Technology Co., Ltd.; DDG was purchased from Sigma; O 6 -Methylguanine (purity 97%) was purchased from Sigma; tinidazole (purity 99.8%) was purchased from China Institute for the Control of Pharmaceutical and Biological Products; ethyl acetate (HPLC grade) was purchased from Tedia, USA; other chemical reagents All are analytically pure.

[0022] 2 Experimental part

[0023] 2.1 Pretreatment of plasma samples

[0024] Take a 10mL glass centrifuge tube, add 20μL of 1μg / mL internal standard solution, add 1mL of human plasma, vortex mix for 30s, add 5mL of ethyl acetate, vortex for 3min, centrifuge at 3500rpm for 10min, put 4mL of supern...

Embodiment 2

[0074] 1 Instruments, materials and reagents

[0075] 1.1 Instrument Agilent 1290 ultra-high performance liquid chromatograph equipped with 6460 triple quadrupole mass spectrometer, Agilent Company of the United States.

[0076] 1.2 Sample and reagent PNA (content is 100% based on anhydrous substance), provided by Nanjing Changao Pharmaceutical Technology Co., Ltd.; DDG was purchased from Sigma; O 6 -Methylguanine (purity 97%) was purchased from Sigma; tinidazole (purity 99.8%) was purchased from China Institute for the Control of Pharmaceutical and Biological Products; ethyl acetate (HPLC grade) was purchased from Tedia, USA; other chemical reagents All are analytically pure.

[0077] 2 Experimental part

[0078] 2.1 Pretreatment of urine samples

[0079] Take a 10mL glass centrifuge tube, add 20μL of 0.9μg / mL internal standard solution, add 1mL human urine sample, vortex mix for 30s, add 4mL ethyl acetate, vortex for 3min, centrifuge at 3500rpm for 10min, supernatant 3.5m...

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Abstract

The invention provides a method for detecting the concentration of metacavir and metabolites thereof in a biological sample. According to the method, the metacavir, the metabolites and tinidazole (internal standard) are extracted with ethyl acetate, and a UPLC-MS / MS (ultra-performance liquid chromatography-tandem mass spectrometry) method is adopted for performing separation and determination. The method provided by the invention is proved to be accurate and reliable by methodology and can be used for analyzing the content of the metacavir and the metabolites thereof in the biological sample.

Description

technical field [0001] The invention relates to a method for detecting the concentration of 2,3-dideoxyguanosine and its metabolites in biological samples, in particular to a method for analyzing metacavir and its metabolites 2,3-bis Deoxyguanosine and O 6 - Method for methylguanine content. Background technique [0002] At present, hepatitis B has become a global threat, and long-term application of nucleoside analogue drug antiviral therapy is still a feasible treatment so far. 2,3-Dideoxyguanosine (code name: PNA) Drugs for hepatitis B virus infection, the possible pharmacological action mechanism includes direct action and indirect action. Direct action means that PNA, as a guanine analogue, can directly enter liver cells and be phosphorylated in the cells to form an active triphosphate, which competes with the natural substrate of HBV polymerase, deoxyguanosine triphosphate, Thereby inhibiting the HBV DNA replication process. The indirect effect means that PNA is qu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): G01N30/02
Inventor 谢少斐余成霞周东颜黄海燕李纬
Owner GUANGZHOU YIPINHONG PHARMA