title: Simultaneous bioanalysis of rasagiline and its major metabolites in human plasma by LC-MS/MS: Application to a clinical pharmacokinetic study.
abstract: Rasagiline is a selective, irreversible inhibitor of monoamine oxidase type-B (MAO-B) and has been used both as a monotherapy and in addition to levodopa in the treatment of Parkinson's disease (PD). Rasagiline is metabolized by the cytochrome P450 (CYP) system, and the following three major metabolites with potential neuroprotective activity have been identified: 1-aminoindan (AI), 3-hydroxy-N-propargyl-1-aminoindan (3-OH-PAI) and 3-hydroxy-1-aminoindan (3-OH-AI). In this study, a novel liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of rasagiline and its major metabolites in human plasma. This method was validated in terms of specificity, linearity, precision, accuracy, recovery, matrix effect and stability. The validated method was then applied to a clinical pharmacokinetic study after the oral administration of 1mg rasagiline mesylate tablets to six healthy Chinese volunteers.
authors.affiliation: Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Ting
authors.initials: T
authors.lastname: Wang
authors.affiliation: Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Leting
authors.initials: L
authors.lastname: Yang
authors.affiliation: Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Jing
authors.initials: J
authors.lastname: Hua
authors.affiliation: Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Huiru
authors.initials: H
authors.lastname: Xie
authors.affiliation: Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China.
authors.forename: Xuehua
authors.initials: X
authors.lastname: Jiang
authors.affiliation: Department of Clinical Pharmacy and Pharmacy Administration, Key Laboratory of Drug Ministry of Education, West China School of Pharmacy, Sichuan University, Chengdu 610041, Sichuan, China. Electronic address: rebeccawang312@gmail.com.
authors.forename: Ling
authors.initials: L
authors.lastname: Wang
mesh_terms: D002853:Chromatography, Liquid / Q000379:methods*; D006801:Humans; D007189:Indans / Q000097:blood* / Q000493:pharmacokinetics; D015203:Reproducibility of Results; D053719:Tandem Mass Spectrometry / Q000379:methods*
chemical_list: D007189:Indans; C031967:rasagiline
keywords: Determination; Human plasma; LC–MS/MS; Metabolites; Rasagiline