Determination of rivaroxaban - a novel, oral, direct Factor Xa inhibitor - in human plasma by high-performance liquid chromatography-tandem mass spectrometry

被引：120

作者：

Rohde, G. ^{[1
]}

机构：

[1] Bayer HealthCare, Drug Metab & Pharmacokinet Bioanalyt, D-42096 Wuppertal, Germany

来源：

JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES | 2008年 / 872卷 / 1-2期

关键词：

rivaroxaban; Factor Xa inhibitor;

D O I：

10.1016/j.jchromb.2008.07.015

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

A high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method allowing the sensitive and specific quantification of rivaroxaban (BAY 59-7939), a Factor Xa inhibitor in advanced development for the prevention and treatment of thromboembolic disorders, in human plasma is described. After precipitation of plasma proteins with methanol containing the internal standard followed by centrifugation, the plasma supernatant was injected directly onto the HPLC-MS/MS system. Concentrations could be determined between 0.50 and 500 mu g/L. Inter-assay precision was <= 7.4% and inter-assay accuracy was between 96.3 and 102.9% throughout the entire working range. The method was applied successfully in several clinical studies, which allowed an accurate determination of rivaroxaban pharmacokinetics in human plasma. (c) 2008 Elsevier B.V. All rights reserved.

引用

页码：43 / 50

页数：8

共 15 条

[1] Treatment of proximal deep-vein thrombosis with the oral direct factor Xa inhibitor rivaroxaban (BAY 59-7939) - The ODIXa-DVT (oral direct factor Xa inhibitor BAY 59-7939 in patients with acute symptomatic deep-vein thrombosis) study
Agnelli, Giancarlo
Gallus, Alexander
Goldhaber, Samuel Z.
Haas, Sylvia
Huisman, Menno V.
Hull, Russel D.
Kakkar, Ajay K.
Misselwitz, Frank
Schellong, Sebastian
[J]. CIRCULATION, 2007, 116 (02) : 180 - 187
[2] *BAYER HEALTHC AG, DAT FIL BAYER HEALTH
[3] Prevention and treatment of experimental thrombosis in rabbits with rivaroxaban (BAY 597939) -: an oral, direct factor Xa inhibitor
Biemond, Bart J.
Perzborn, Elisabeth
Friederich, Philip W.
Levi, Marcel
Buetehorn, Ulf
Buller, Harry R.
[J]. THROMBOSIS AND HAEMOSTASIS, 2007, 97 (03) : 471 - 477
[4] Buller HR, 2006, EUR HEART J, V27, P761
[5] *COMM EUR COMM, 1989, 11184487EN COMM EUR
[6] A once-daily, oral, direct Factor Xa inhibitor, rivaroxaban (BAY 59-7939), for thromboprophylaxis after total hip replacement
Eriksson, Bengt I.
Borris, Lars C.
Dahl, Ola E.
Haas, Sylvia
Huisman, Menno V.
Kakkar, Ajay K.
Muehlhofer, Eva
Dierig, Christoph
Misselwitz, Frank
Kalebo, Peter
[J]. CIRCULATION, 2006, 114 (22) : 2374 - 2381
[7] Oral, direct Factor Xa inhibition with BAY 59-7939 for the prevention of venous thromboembolism after total hip replacement
Eriksson, BI
Borris, L
Dahl, OE
Haas, S
Huisman, MV
Kakkar, AK
Misselwitz, F
Kälebo, P
[J]. JOURNAL OF THROMBOSIS AND HAEMOSTASIS, 2006, 4 (01) : 121 - 128
[8] Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct factor Xa inhibitor
Kubitza, D
Becka, M
Voith, B
Zuehlsdorf, M
Wensing, G
[J]. CLINICAL PHARMACOLOGY & THERAPEUTICS, 2005, 78 (04) : 412 - 421
[9] Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939 - an oral, direct Factor Xa inhibitor - after multiple dosing in healthy male subjects
Kubitza, D
Becka, M
Wensing, G
Voith, B
Zuehlsdorf, M
[J]. EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 2005, 61 (12) : 873 - 880
[10] LASSEN MR, 2007, J THROMB HAEMOST, V5

← 1 2 →