Sensitive LC-MS/MS method for quantification of Rivaroxaban in plasma: application to pharmacokinetic studies.

Rivaroxaban is an anticoagulant (orally active direct Xa inhibitor) indicated to reduce the risk of stroke and systemic embolism, for treatment and prophylaxis of deep vein thrombosis, for treatment of pulmonary embolism, as well as other cardiovascular complications. Bioanalytical methods for rivaroxaban quantification in plasma are necessary for application in pharmacokinetic studies, as well as in drug therapeutic monitoring. This work developed and validated a sensitive bioanalytical method by LC-MS/MS for rivaroxaban quantification in human plasma using a one-step liquid-liquid extraction. The linear concentration range was 1 to 600 ng/mL. The bioanalytical method was also applied to pharmacokinetic studies in healthy volunteers under fasting and fed conditions. The results demonstrated that the method is rapid, sensitive and adequate for application in pharmacokinetic studies.