Section 18
Chapter 17,040

Simultaneous determination of 1,5-dicaffeoylquinic acid and its active metabolites in human plasma by liquid chromatography-tandem mass spectrometry for pharmacokinetic studies

Gu, R.; Dou, G.; Wang, J.; Dong, J.; Meng, Z.

Journal of Chromatography. B Analytical Technologies in the Biomedical and Life Sciences 852(1-2): 85-91


ISSN/ISBN: 1570-0232
PMID: 17267301
DOI: 10.1016/j.jchromb.2006.12.055
Accession: 017039325

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1,5-Dicaffeoylquinic acid (1,5-DCQA), a potent HIV-1 integrase inhibitor, is undergoing an evaluation as a promising novel HIV therapeutic agent. Here, we report a simple, rapid and robust LC-MS/MS method for simultaneous determination of 1,5-DCQA and its two active metabolites, 1-caffeoyl-5-feruoylquinic acid (1,5-CFQA) and 1,5-O-diferuoylquinic acid (1,5-DFQA) in human plasma. The quantitation of the target compounds was determined by selected reaction monitoring (SRM) mode using electrospray ionization (ESI). Good linearity was obtained in the 3-500 ng/ml range for each analyte and the analytical method was validated in terms of specificity, precision, accuracy, recovery, stability and matrix effect. These assays gave R.S.D.% values for precision always lower than 13.8% and R.E.% values for accuracy between -8.9 and 0.9%. In addition, the specificity, extraction recovery, stability and matrix effect were satisfactory too. Using the measured plasma concentrations of 1,5-DCQA and its active metabolites in five healthy volunteers, pharmacokinetic profiles of 1,5-DCQA and its active metabolites were evaluated, which supported the clinical pharmacokinetic studies successfully. Due to its high sensitivity, specificity and simplicity, the method could be used for pharmacokinetic studies of both 1,5-DCQA and its active metabolite, and for routine monitoring of their levels in human plasma.

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