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A method for detecting the concentration of ticagrelor and its active metabolites in human plasma

A technology for ticagrelor and metabolites, applied in the field of drug analysis, can solve problems such as unfavorable promotion, expensive equipment, and small laboratory coverage, and achieve the effects of good specificity, high accuracy, and rapid detection process

Active Publication Date: 2021-05-04
HARBIN MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, after comprehensive analysis of relevant domestic and foreign literature retrieved, there is an HPLC-MS / MS method for the determination of the concentration of ticagrelor in biological samples. Although this method has the advantages of good sensitivity and specificity, the equipment is expensive Laboratory coverage is small, which is not conducive to promotion

Method used

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  • A method for detecting the concentration of ticagrelor and its active metabolites in human plasma
  • A method for detecting the concentration of ticagrelor and its active metabolites in human plasma
  • A method for detecting the concentration of ticagrelor and its active metabolites in human plasma

Examples

Experimental program
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Effect test

Embodiment 1

[0073] Example 1: Detection of the concentration of ticagrelor and its active metabolite AR-C124910XX in human plasma

[0074] 1. Instrument

[0075] U3000 high performance liquid chromatography (Thermo Fisher, Germany);

[0076] D-37520 high-speed centrifuge (Abbott, USA);

[0077] Vortex Genius 3 vortex mixer (Germany IKA company);

[0078] XS205DU electronic balance (China Mettler-Toledo Instrument Shanghai Co., Ltd.);

[0079] KQ-600 CNC ultrasonic cleaner (Kunshan Ultrasonic Instrument Co., Ltd., China).

[0080] 2. Reagents

[0081] Standard products: ticagrelor (McLean), AR-C124910XX (Toronto Research Chemicals), voriconazole (China Institute for Food and Drug Control);

[0082] Acetonitrile (chromatographically pure, Thermo Fisher Scientific);

[0083] Ultrapure water: self-made.

[0084] 3. Detection method

[0085] Including the following steps:

[0086] (1) Preparation of standard working solution: Accurately weigh ticagrelor and AR-C124910XX, add 50v / v% ac...

Embodiment 2

[0126] Example 2 A detection kit for detecting the concentration of ticagrelor and its active metabolites in human plasma using high performance liquid chromatography (HPLC)

[0127] 1. Assembly of kit

[0128] The kit contains the following ingredients:

[0129] (1) Ticagrelor working solution with gradient concentration of 500, 1000, 2000, 5000, 7500, 10000ng / mL

[0130] Precisely weigh ticagrelor, add 50v / v% acetonitrile solution to prepare a ticagrelor stock solution with a concentration of 2000 μg / mL, dilute the ticagrelor stock solution with 50v / v% acetonitrile solution to a gradient concentration of 500, 1000, 2000, 5000, 7500, 10000ng / mL working solution of ticagrelor;

[0131] (2) AR-C124910XX working solution with gradient concentration of 200, 500, 1000, 2000, 3000, 5000ng / mL

[0132] Accurately weigh AR-C124910XX, add 50v / v% acetonitrile solution to prepare AR-C124910XX stock solution with a concentration of 1000μg / mL, dilute AR-Cl24910XX stock solution with 50v...

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Abstract

The invention discloses a method for detecting the concentration of ticagrelor and its active metabolites in human plasma, which comprises the following steps: (1) preparation of a standard working solution; (2) sample processing; (3) preparation of a standard curve; 4) Quantitative analysis: take the test sample and process it according to the method of step (2), and calculate according to the standard curve equation obtained in step (3), to obtain the concentration of ticagrelor and its active metabolite in the sample to be tested. The present invention uses high-performance liquid chromatography (HPLC) to measure the concentration of ticagrelor and its active metabolites in human plasma, and accurately quantifies the concentration of ticagrelor and its active metabolites in human plasma. Reasonable selection of methods, mobile phases, mass spectrometry conditions, etc., optimization of experimental conditions such as flow rate, mobile phase ratio, and chromatographic conditions, etc. After a series of methodological verifications, the entire quantitative detection method is practical, easy to operate, high in repeatability, and good in accuracy , strong operability, and can be directly applied to the detection and analysis of plasma samples of clinical patients and related pharmacokinetic analysis.

Description

technical field [0001] The invention relates to a method for detecting the concentration of ticagrelor and its active metabolites in human plasma by using high-performance liquid chromatography (HPLC), which can be used for clinical drug concentration monitoring. The invention belongs to the technical field of drug analysis. Background technique [0002] Ticagrelor, also known as Belinda, is a novel, oral, reversible platelet adenosine diphosphate (ADP) P2Y receptor antagonist. At the same time, the active metabolite AR-C124910XX can be rapidly generated after ticagrelor is absorbed. Both ticagrelor itself and its metabolites are active, and the activity of the drug itself is stronger than that of its metabolites. Therefore, it can rapidly Potently inhibits ADP-mediated platelet aggregation. As a platelet inhibitor, ticagrelor is widely used in patients with acute coronary syndrome, including those receiving drug therapy and percutaneous coronary intervention (PCI), to red...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): G01N30/88
CPCG01N30/88G01N2030/8822
Inventor 钱钊海鑫
Owner HARBIN MEDICAL UNIVERSITY
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