HPLC-MS法研究碘化N-正丁基氟哌啶醇在兔体内的药代动力学

Pharmacokinetics of N-n-butyl haloperidol iodide determined by HPLC-MS method in rabbits

目的 :研究碘化N 正丁基氟哌啶醇 (F2 )在兔体内的药代动力学过程。方法 :6只新西兰兔耳缘静脉注射碘化N 正丁基氟哌啶醇 (F2 ) 2 .0mg·kg-1后采集血样 ,用高效液相色谱 质谱 (HPLC MS)联用技术测定血浆药物浓度 ,并用 3p97软件拟合计算药代动力学参数。结果和结论 :兔耳缘静脉给药后的血药浓度 时间曲线符合二室开放模型 ,其主要药动学参数为 :分布半衰期T1 2α 是 0 .10h ,消除半衰期Τ1 2 β 是 6 .4h ,曲线下面积AUC为 183μg·h-1·L-1,中央室分布容积VC 为 4L ,清除率Cl为12 .9L·h-1。HPLC MS联用方法测定F2 血药浓度 ,灵敏度高 ,专属性强。

AIM: To study pharmacokinetics of N-n-butyl haloperidol iodide (F 2) in rabbits. METHODS: Blood samples were collected at different time points after six rabbits were given F 2 2.0 mg·kg -1, iv. Then the plasma concentrations of F 2 were detected by HPLC-MS method. And pharmacokinetic parameters were calculated using the 3p97 program. RESULTS AND CONCLUSION: The open two-compartment model can best describe the concentration-time curve of F 2. The major pharmacokinetic parameters are listed as following: the half-life of distribution phase T 1/2α= 0.10 h, the half-life of elimination phase Τ 1/2β= 6.4 h, the volume of the central compartment Vc=4 L, the total areas under the concentration-time curve AUC=183 μg·h -1·L -1, and the plasma clearance CL= 12.9 L·h -1. HPLC-MS is a sensitive and specific method in this study.