Simultaneous determination of desloratadine and its active metabolite 3-hydroxydesloratadine in human plasma by LC/MS/MS and its application to pharmacokinetics and bioequivalence.
A rapid and simple liquid chromatographic-tandem mass spectrometric (LC/MS/MS) method was developed and validated for the simultaneous determination of desloratadine and its active metabolite 3-hydroxydesloratadine concentrations in human plasma. After liquid-liquid extraction with ethyl ether for sample preparation, the chromatographic separation was achieved on a CAPCELL PAK C18 column (50 mm x 2.0mm, 5 microm, Shiseido). [(2)H(4)]desloratadine and [(2)H(4)]3-OH desloratadine were used as internal standards. A mobile phase consisted of 5mM ammonium formate in water, methanol and acetonitrile (50:30:20). Detection was by positive ion electrospray tandem mass spectrometry on a Sciex API3000. A quadratic regression (weighted 1/concentration) gave the best fit for calibration curves over the concentration range 0.05-10 ng/mL for both desloratadine and 3-OH desloratadine. The method was shown to be accurate, rapid and sufficiently sensitive to be successfully applied to a pharmacokinetic and bioequivalent study.
Xu
Hong-Rong
HR
Department of Clinical Pharmacology, ZhongShan Hospital, Fudan University, 180 FengLin Road, Shanghai 200032, China. hrxu@zshospital.com
Li
Xue-Ning
XN
Chen
Wei-Li
WL
Chu
Nan-Nan
NN
D000284:Administration, Oral; D002853:Chromatography, Liquid; D018592:Cross-Over Studies; D004355:Drug Stability; D006801:Humans; D017336:Loratadine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D008297:Male; D012015:Reference Standards; D012680:Sensitivity and Specificity; D013607:Tablets; D053719:Tandem Mass Spectrometry; D013810:Therapeutic Equivalency
D013607:Tablets; C482880:3-hydroxydesloratadine; D017336:Loratadine; C121345:desloratadine