加替沙星在人体内的药动学和血药浓度测定

Pharmacokinetics and plasma concentration of gatifloxacin in healthy voluntees

目的 :用HPLC 紫外法测定人体内加替沙星的血药浓度和药动学。方法 :用HPLC 紫外法测定加替沙星的血药浓度 ,1 0名男性受试者口服单剂量 4 0 0mg加替沙星片后 ,研究人体内药动学。结果 :HPLC 紫外法测定检测波长 2 93nm ,血浆标准曲线回归方程 :Y =0 .5 90C +0 .0 6 1 ,r =0 .9998。检测浓度范围 :0 .0 5 7～ 5 .2 2mg·L-1 ,相对回收率在 97.1 2 %～1 0 2 .5 6 %之间 ,日内、日间RSD均在 1 5 %以内。 1 0名男性受试者口服单剂量 4 0 0mg加替沙星 ,药时曲线符合二房室模型 ,主要药动学参数Tmax为 1 .97h ,Cmax为 3.0 1mg·L-1 ,t1 / 2 ( β) 为 9.83h ,AUC为 2 8.77mg·h·L-1 ,与国外文献基本一致。结论 :HPLC 紫外法测定加替沙星血药浓度 ,操作简便易行 ,重现性好 ,符合血药浓度监测及人体内药动学研究要求。

OBJECTIVE To determine the plasma concentration and pharmacokinetics of gatifloxacin in healthy voluntees.METHODS The plasma concentration of gatifloxacin was determined by HPLC with the detection wavelength of 293 nm . Its pharmacokinetics was studied after oral administration of a single dose of 400mg to healthy voluntees.RESULTS The linear range was 0.057 ～ 5.22 mg ·L -1 , recovery was between 97.12% ～ 105.56% ,within day and between day RSD was less than 15%.The drug time curve after oral dose of 400 mg gatifloxacin in 10 male voluntees fitted to a two conpartment model.The main pharmacokinetic parameters of gatifloxacin were as follows: T max was 1.97 h ; C max was 3.01 mg ·L -1 ; t 1/2(β) was 9.83 h ;AUC was 28.77 mg ·h·L -1 .CONCLUSIONS The HPLC we developed for gatifloxacin determination is simple and is suitable for plasma drug concentration monitoring and human pharmacokinetic research.