Mohammadi A, Kanfer I, Sewram V, Walker R B
Faculty of Pharmacy, Rhodes University, Grahamstown 6140, South Africa.
J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Sep 25;824(1-2):148-52. doi: 10.1016/j.jchromb.2005.07.015.
Cyclizine is a piperazine derivative with anti-emetic activity that is useful in the prevention and treatment of nausea and vomiting associated with motion sickness. A liquid chromatography-tandem mass spectrometry (LC-MS-MS) method is presented for the quantitation of cyclizine in serum. Sample pretreatment involved liquid-liquid extraction of 200 microl of serum with dichloromethane after the addition of 100 microl each of ammonium hydroxide and internal standard solutions. The extracts were analyzed by HPLC on a Luna C18 reversed-phase column and an ion-trap mass spectrometer with an electrospray interface. A limit of detection of 1 ng/ml was determined which allowed for the reliable measurement of cyclizine in the serum of human subjects. The method was found to be linear over the calibration range of 2.5-100 ng/ml. The applicability of this method was demonstrated by the analysis of serum obtained from a human volunteer following administration of a single 50 mg cyclizine hydrochloride tablet. The reported method was observed to have the necessary sensitivity, selectivity, precision and accuracy for monitoring cyclizine concentrations in human subjects following oral administration.
赛克利嗪是一种具有抗呕吐活性的哌嗪衍生物，可用于预防和治疗与晕动病相关的恶心和呕吐。本文介绍了一种液相色谱-串联质谱（LC-MS-MS）法用于定量血清中的赛克利嗪。样品预处理包括在加入100微升氢氧化铵和内标溶液后，用二氯甲烷对200微升血清进行液-液萃取。萃取物通过HPLC在Luna C18反相柱上以及带有电喷雾接口的离子阱质谱仪上进行分析。确定检测限为1纳克/毫升，这使得能够可靠地测量人体受试者血清中的赛克利嗪。该方法在校准范围2.5-100纳克/毫升内呈线性。通过分析一名人类志愿者口服一片50毫克盐酸赛克利嗪片后获得的血清，证明了该方法的适用性。观察到所报道的方法对于监测口服给药后人体受试者中的赛克利嗪浓度具有必要的灵敏度、选择性、精密度和准确度。
