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Detection method of ticagrelor in human plasma and active metabolite concentration thereof

A technology for ticagrelor and metabolites, applied in the field of drug analysis, can solve the problems of expensive instruments and equipment, unfavorable promotion, and small laboratory coverage.

Active Publication Date: 2019-04-16
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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  • Detection method of ticagrelor in human plasma and active metabolite concentration thereof
  • Detection method of ticagrelor in human plasma and active metabolite concentration thereof
  • Detection method of ticagrelor in human plasma and active metabolite concentration thereof

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 detection method of ticagrelor in human plasma and active metabolite concentration thereof. The method comprises the following steps: (1) preparing a standard working solution; (2) treating a sample; (3) manufacturing a standard curve; (4) quantitatively analyzing: treating a test sample according to the method of step (2), and computing according to a standard curve equation obtained in the step (3) to obtain the ticagrelor in the human plasma and the concentration of the active metabolite concentration thereof. The ticagrelor in the human plasma and the concentration of the active metabolite concentration thereof are determined by applying the high-performance liquid chromatography (HPLC), the ticagrelor in the human plasma and the concentration of the active metabolite concentration thereof can be accurately quantified; through the reasonable selection of a chromatographic column, a pre-treatment method, mobile phase and a mass spectrum condition and the optimization of the flow velocity, the mobile phase proportion, the chromatographic condition and like experimental conditions, the series of methodology verifies that the whole quantitative detection method is practicable, simple and convenient for operation, good in repeatability, good in accuracy, and strong in operability, and can be directly applied to the plasma sample detection analysis of the clinical patient and the related pharmacokinetics 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 Applications(China)
IPC IPC(8): G01N30/88
CPCG01N30/88G01N2030/8822
Inventor 钱钊海鑫
Owner HARBIN MEDICAL UNIVERSITY
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