【摘 要】
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Schistosomiasis is an infectious disease affecting many people in some countries.While praziquantal is the drug of choice,there is an unmet medical need for novel therapies with greater efficacy.DW-3-
【机 构】
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Center for Drug Metabolism and Pharmacokinetics,College of Pharmaceutical Sciences,Soochow Universit
【出 处】
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第十届全国药物和化学异物代谢学术会议暨第三届国际ISSX/CSSX联合学术会议
论文部分内容阅读
Schistosomiasis is an infectious disease affecting many people in some countries.While praziquantal is the drug of choice,there is an unmet medical need for novel therapies with greater efficacy.DW-3-15 is a novel and promising prodrug possessing both adult and juvenile schistosomes killing capability.Its hydrolytic products are artesunate (ARS), dihydroartemisinin (DHA) and 10-hydroxy-praziquantel (10-OH-PZQ), and all are active in preventing schistosomal infection in an animal model.The present study aims to develop a sensitive and rapid LC-MS/MS method for separation and simultaneous determination of the three active components.A LC-MS/MS system consisting AB Sciex AP14000 Qtrap and Shimadzu HPLC is used in this study.Chromatography is performed using an Agela Venusil C18 column (2.1 mm × 50 mm, 5 μm) with a linear gradient (mobile phase A, 10 mM ammonium acetate aqueous solution containing 0.1% formic acid; B, acetonitrile), and a baseline resolution is achieved with a total run time of 6 min.Mass detection is carried out by electrospray ionization in positive MRM mode with ion transitions of m/z 402.1→m/z 267.3 for ARS, m/z 302.2→m/z 163.1 for DHA, and m/z 329.2→m/z 219.4 for 10-OH-PZQ.The method is linear over a concentration range of 2.00-1000 ng/mL for ARS, 5.00-1000 ng/mL for DHA, and 1.00—200 ng/mL for 10-OH-PZQ.The current LC-MS/MS method is being used for pharmacokinetic evaluation of DW-3-15 in mice and rats.
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