碘化N-正丁基氟哌啶醇在大鼠的药代动力学及组织分布

目的　研究碘化N 正丁基氟哌啶醇 (F2 )在大鼠体内的药代动力学和组织分布特征。方法　大鼠尾静脉给予F2后 ,采用高效液相 -质谱联用技术检测各时间点血浆和组织器官药物浓度 ,并用 3 p97软件计算药代动力学参数。 结果　静脉给药后药时曲线符合二室开放模型。 1、2、4mg·kg- 13个剂量主要药动学参数为 :分布半衰期T1/2α分别为 0 3 2、0 2 1、0 3 2h ,消除半衰期T1/2 β分别为 5 75、5 68、5 98h ,曲线下面积AUC分别为 71 9、83 6、166 7μg·L- 1·h- 1,血浆清除率CL分别为 13 9、2 3 9、2 4 0L·h- 1。结论　F2 是一种分布迅速 ,Vc较大 ,T1/2 β较长 ,消除相浓度较低的药物。符合一级动力学特征。除脑、睾丸中分布较少外 ,其它器官组织中浓度均远高于血浆药物浓度

Pharmacokinetics of N-n-butyl haloperidol iodide

AIMTo study the pharmacokinetics of N-n-butyl ha loperidol iodide (F 2). METHODSThe plasma and tissue concentrat ion of F 2 was detected by HPLC-MS method after intravenous bolus doses of 1, 2 and 4 mg·kg -1 . The pharmacokinetics parameters were calculated by the p rocedure of 3p97. RESULTSThe concentration-time curves were con formed to two-compartment model. The pharmacokinetics parameters of the three d oses were: T 1/2α : 0 32,0 21,0 32 h;T 1/2β : 5 75,5 68, 5 98 h;AUC: 71 9,83 6,166 7 μg·L -1 ·h -1 ; CL:13 9,23 9,24 0 L·h -1 . CONCLUSIONThe pharmacokinetics of F 2 belongs t o the first-order kinetics. The characters of F 2 are quick distribution, long terminal half-life, large Vc and low concentration during distribution phase. The concentration of F 2 in all tissues except brain and testis is higher than that in plasma.