Hung Te-Yu, Davis Timothy M E, Ilett Kenneth F
School of Medicine and Pharmacology, The University of Western Australia, Crawley 6009, Australia.
J Chromatogr B Analyt Technol Biomed Life Sci. 2003 Jul 5;791(1-2):93-101. doi: 10.1016/s1570-0232(03)00209-5.
Piperaquine (PQ) is an antimalarial drug enjoying a resurgence of use in combination with an artemisinin derivative because of parasite resistance to standard treatments. Its pharmacokinetic properties have not been characterised. An assay for PQ in plasma was developed using solvent extraction and liquid chromatographic separation on a Waters XTerra RP(18) column, with a mobile phase of 7% acetonitrile in water (containing 0.025% trifluoroacetic acid, 0.1% NaCl and 0.008% triethylamine) and UV detection at 340 nm. The assay was linear up to 1000 microg/l. Intra- and inter-day relative standard deviations were <10% (5-500 microg/l) and <21% (5-500 microg/l), respectively. Inter-day limits of quantitation and detection were 5 microg/l and 3 microg/l, respectively. A preliminary pharmacokinetic study in a patient who received 2.56 g of PQ phosphate orally with dihydroartemisinin as four doses over 32 h found an apparent steady-state volume of distribution of 447 l/kg, an apparent oral clearance 0.93 l/h/kg and a terminal half-life of 17.3 days.
哌喹（PQ）是一种抗疟药物，由于疟原虫对标准治疗产生耐药性，它与青蒿素衍生物联合使用的情况正在重新兴起。其药代动力学特性尚未得到表征。采用溶剂萃取和在沃特世XTerra RP(18)柱上进行液相色谱分离的方法，开发了一种血浆中PQ的测定方法，流动相为7%乙腈的水溶液（含有0.025%三氟乙酸、0.1%氯化钠和0.008%三乙胺），在340 nm处进行紫外检测。该测定方法在高达1000 μg/l时呈线性。日内和日间相对标准偏差分别<10%（5 - 500 μg/l）和<21%（5 - 500 μg/l）。日间定量限和检测限分别为5 μg/l和3 μg/l。在一名患者中进行的初步药代动力学研究发现，该患者在32小时内分四次口服2.56 g磷酸哌喹与双氢青蒿素，其表观稳态分布容积为447 l/kg，表观口服清除率为0.93 l/h/kg，末端半衰期为17.3天。
