title: Development of a highly sensitive LC-MS/MS method for simultaneous determination of rupatadine and its two active metabolites in human plasma: Application to a clinical pharmacokinetic study.
abstract: An easy LC-ESI-MS/MS method was developed and validated for simultaneous determination of rupatadine (RT) and its two active metabolites, namely desloratadine (DT) and 3-hydroxydesloratadine (3-OH-DT), in human plasma. The chromatographic separation was carried out on a C18 column with gradient elution by using methanol and 10mM ammonium acetate containing 0.1% (v/v) formic acid. The lower limit of quantification (LLOQ) was 0.05, 0.035 and 0.035 ng/mL for RT, DT and 3-OH-DT, respectively. The intra- and inter-day precision of analytes were within the range of 1.0-4.7% and 2.2-12.1%, respectively. The intra- and inter-day accuracy of analytes were within the range of -7.7% to 5.2% and -4.1% to 4.8%, respectively. The method was successfully applied to a pharmacokinetic study of RT and its two metabolite DT and 3-OH-DT in healthy volunteers following single (10, 20, 40 mg) and multiple (10 mg) oral doses of rupatadine fumarate tablets.
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Chenglong
authors.initials: C
authors.lastname: Sun
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Qian
authors.initials: Q
authors.lastname: Li
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Liping
authors.initials: L
authors.lastname: Pan
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Bing
authors.initials: B
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Pan
authors.initials: P
authors.lastname: Gu
authors.affiliation: Department of Pharmaceutics of Traditional Chinese Medicine, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.
authors.forename: Junying
authors.initials: J
authors.lastname: Zhang
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China. Electronic address: dinglidl@hotmail.com.
authors.forename: Li
authors.initials: L
authors.lastname: Ding
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China; Key Laboratory of Drug Quality Control and Pharmacovigilance, Ministry of Education, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China. Electronic address: analysis99@126.com.
authors.forename: Chungyong
authors.initials: C
authors.lastname: Wu
mesh_terms: D002853:Chromatography, Liquid / Q000379:methods*; D003533:Cyproheptadine / Q000031:analogs & derivatives* / Q000737:chemistry; D005260:Female; D005561:Formates / Q000737:chemistry; D006801:Humans; D017336:Loratadine / Q000031:analogs & derivatives / Q000737:chemistry; D008297:Male; D010949:Plasma / Q000737:chemistry*; D015203:Reproducibility of Results; D012680:Sensitivity and Specificity; D013607:Tablets / Q000737:chemistry; D053719:Tandem Mass Spectrometry / Q000379:methods*
chemical_list: D005561:Formates; D013607:Tablets; C030544:formic acid; C103639:rupatadine; D003533:Cyproheptadine; C482880:3-hydroxydesloratadine; D017336:Loratadine
keywords: 3-Hydroxydesloratadine; Desloratadine; LC–MS/MS; Pharmacokinetic; Rupatadine