人血浆中盐酸氟桂利嗪的HPLC测定及药代动力学研究  

Determination of Flunarizine Hydrochloride in Human Plasma by HPLC and Its Pharmacokinetics

作　　者：何海霞[1] 周远大[1] 姚高琼[1] 朱治本[1] 

机构地区：[1]重庆医科大学附属第一医院临床药理研究室,重庆400016

出　　处：《药物分析杂志》2000年第3期157-160,共4页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的 :建立血浆中盐酸氟桂利嗪浓度的反相HPLC测定法 ,并用此方法研究盐酸氟桂利嗪在人体内的药代动力学。方法 :内标安定为内标 ,血浆经戊烷 -异丙醇、盐酸溶液、二氯甲烷等多步提取后 ,采用C18分析柱 ,以甲醇 -水 (含 0 0 2mol·L-1四丁基溴化铵 ) (74∶2 6 )为流动相 ,流速为 0 8mL·min-1;在紫外 2 5 4nm处检测。所得数据用 3p87药代动力学程序处理 ,求出有关的参数。结果 :盐酸氟桂利嗪在 2 34～ 15 0ng·mL-1范围内线性关系良好 (r =0 9985 ) ,最低检测浓度 2ng·mL-1;平均回收率 99 94%。应用本法对单剂量口服盐酸氟桂利嗪后的药代动力学进行了初步探讨。结果表明药时曲线符合一室药动学模型 ,药动学的主要参数t1/2 (Ka) =1 6 1h、t1/2 (Ke) =4 0 9h、tp=2 82h、Cmax=5 9 5 4ng·mL-1。结论 :本方法以安定为内标 ,灵敏、可靠 ,回收率高 ,结果准确 ,适用于临床血药浓度监测及药代动力学研究。Objective:To establish a HPLC method for the determination of flunarizine hydrochloride in human plasma and investigate its pharmacokinetic characteristics dichloromethane in healthy volunteers after a single oral dose.Methods:The drug and internal standard(Diazepam,DZP)were extracted from plasma with n -pentane—iso-propyl alcohol,1 mol·L -1 hydrochloric acid,and then detected by UV detector at 254 nm with the C 18 column and methanol-water (containing 0 02 mol·L -1 tetrabutyl ammonium bromide)(74∶26) as mobile phase at a flow rate of 0 8 mL·min -1 .The data obtained were fitted with 3p87 program on computer.Result:The calibration curve was linear in the range of 2 34 and 150 ng·mL -1 with a correlation coefficient of 0 998 5.The limit of detection of flunarizine hydrochloride in plasma was 2 ng·mL -1 .The mean recovery of flunarizine hydrochloride was 99 94% in plasma.This assay procedure has been applied to pharmacokinetic study of flunarizine hydrochloride.The results showed that the drug concentration-time profile conformed to the one-compartment model.The pharmacokinetic parameters were estimated as follows: t 1/2( K a) =1 61 h, t 1/2( K e) =4 09 h, t p=2 82 h, C max=59 54 ng·mL -1 .Conclusion:The method was sensitive,precise and reliable. It is suitable for the monitoring of blood drug concentration and its pharmacokinetic studies.

关 键 词：盐酸氟桂利唪 血药浓度 药物动力学 HPLC 

分 类 号：R972[医药卫生—药品] R969.1[医药卫生—药学]