国产司帕沙星片在老年人体内的药动学研究

Pharmacokinetics of sparfloxacin in the elderly

目的 研究老年人po司帕沙星片的药动学特点。方法 用HPLC测定 8例老年人po 2 0 0mg司帕沙星片后 12 0h内血样和尿样中司帕沙星浓度 ,采用 3P87药动学程序对血药浓度 时间数据进行线性拟合 ,计算药动学参数。根据尿药浓度和尿量计算该药尿原型药物排泄率。结果 本实验建立的HPLC线性关系、回收率、日内及日间精密度均能满足药动学研究的要求 ,老年人 po司帕沙星片后血药浓度 时间数据符合二室模型 ,主要药动学参数为t1/ 2 β=(2 6 .11± 6 .4 9)h ,tmax=(2 .74±1.4 2 )h ,cmax=(1.15± 0 .14 )mg·L-1,AUC0～∞ =(37.2 9± 11.17)mg·h·L-1。服药后 12 0h平均尿原型药物排泄率为2 4 .14 %。结论 老年人半衰期达 2 6h ,单剂 po 2 0 0mg 4 8h后血药浓度均高于绝大多数细菌的MIC及MBC ,一般感染可考虑 3d 2次或 2d

OBJECTIVE To establish a method to determine the concentrations of sparfloxacin in serum and urine and to study its pharmacokinetics of domestic sparfloxacin tablet after administration in the elderly.METHOD The concentrations of sparfloxacin in serum and urine were determined by HPLC following a single oral dose of sparfloxacin tablet. The pharmacokinetic parameters were fitted by 3P87.The urinary excretion of the parent drug was calculated according to the concentrations of sparfloxacin in urine and urine volume.RESULTS The RSD of intra day and inter day were less than 5%.The serum concentration time curves fitted the two compartment model.The main parameters were as follows: t 1/2β =(26.11±6.49) h, t max =(2.74±1.42) h, c max =(1.15± 0.14 ) mg·L -1 , AUC 0～∞ =(37.29±10.17) mg·h·L -1 .The urinary excretion of sparfloxacin was 24.14%.CONCLUSIONS The t 1/2β in the elderly lasted 26 hours and the serum drug concentrations at the 48th hour was obviously higher than MIC and MBC.It was suggested to take the drug twice every three days or once every two days.