Kolade Yetunde T, Babalola Chinedum P, Scriba Gerhard K E
Department of Pharmaceutical Chemistry, School of Pharmacy, University of Jena, Philosophenweg 14, 07743 Jena, Germany.
J Pharm Biomed Anal. 2006 Apr 11;41(1):315-9. doi: 10.1016/j.jpba.2005.11.002. Epub 2005 Dec 6.
The determination of halofantrine and its major metabolite N-desbutylhalofantrine in human plasma by reversed phase high-pressure liquid chromatography is described. The method involves protein precipitation of plasma samples by acetonitrile followed by basification with sodium hydroxide and subsequent liquid-liquid extraction using hexane-diethyl ether (1:1, v/v). The chromatographic separation was carried out on a C-18 column with a mobile phase consisting of methanol/0.05 M KH2PO4 (78:22, v/v) containing 55 mM perchloric acid. Chlorprothixen was used as internal standard. The relative standard deviations of intraday and interday precision for both compounds were less than 7%, the relative standard deviation of the accuracy did not exceed 7.1% at concentrations of 50 and 300 ng/ml. This method is simple, rapid, sensitive and cost effective and was applied to the determination of the pharmacokinetics of halofantrine and N-desbutylhalofantrine in two healthy male volunteers after an oral administration of 500 mg halofantrine. Moreover, the influence of the frequently consumed kolanut on the pharmacokinetics of halofantrine was investigated.
本文描述了用反相高效液相色谱法测定人血浆中卤泛群及其主要代谢物N-去丁基卤泛群的方法。该方法包括用乙腈对血浆样品进行蛋白沉淀，然后用氢氧化钠碱化，随后用正己烷-乙醚（1:1，v/v）进行液-液萃取。色谱分离在C-18柱上进行，流动相由含55 mM高氯酸的甲醇/0.05 M KH2PO4（78:22，v/v）组成。氯丙嗪用作内标。两种化合物日内和日间精密度的相对标准偏差均小于7%，在50和300 ng/ml浓度下，准确度的相对标准偏差不超过7.1%。该方法简单、快速、灵敏且成本效益高，应用于两名健康男性志愿者口服500 mg卤泛群后卤泛群和N-去丁基卤泛群的药代动力学测定。此外，还研究了经常食用可乐果对卤泛群药代动力学的影响。
