氟嗪酸在呼吸道和尿路感染病人中的药代动力学研究

PHARMACOKINETICS OF OFLOXACIN IN PATIENTS WITH RESPIRATORY TRACT AND URINARY TRACT INFECTION

本文目的是通过对14例呼吸道感染(Dose 300mg×2/d),10倒尿路感染病人(Dose 200mg×1/d),口服氟嗪酸片的药代动力学特性进行研究。血和尿中的氟嗪酸浓度测定用HPLC—离子对色谱荧光检测法。本法最小检测限0.03μmol/l,血和尿中平均回收率分别为96.8±5.9%和99.5±1.1%。呼吸道和尿路感染病人中氟嗓酸的药代动力学特性为一房室模型,其主要药代动力学参数为:t1/2 4.70±0.65h,5.25±0.75h;Vd 34.75±9.70l,38.20±15.70l;Cmax 7.85±3.35μmol/l(300mg×2/d),4.15±1.70μmol/1(200mg×1/d);t_(max)2.85±0.81h,1.44±1.04h;Clt 5.7±2.2 l/h,9.3±4.1 1/h。24h尿中氟嗪酸累积排出率分别为69.34±13.80,72.58±11.9%。

ofloxacin is a new quinolone carhoxylic acid derivative showing a broad antimicrobialspectrum against gram-positive and gram-negative bacteria. Its favorable pharmacokinetic features include ex-cellent oral absorption and a long half-life. Pharmacokinetic parameter of ofloxacin tablet have been reportedpreviously. The purpose of this study was to investigate the pharmacokinetic properties of ofloxacin tablet ofthe Chinese in 14 respiratory tract and 10 urinary tract infection in patients. The concentration of ofloxacin in patients serum and urine were determined by HPLC with flurometericdetector. The limit of detection of this method was 0.03 μmol/l. The mean recovery rates in serum and urinewere 96.8±5.9% and 99.5±1.1%, respectively. After oral administration pharmacokinetic model was de-scribed open one-compartmental model. The pharmacokinetic parameters of ofloxacin were separately as fol-low:t1/24.70±0.65h and 5.25±0.75h;Vd 34.75±9.70 l and 38.20±15.70 l;t_(max) 2.85±0.81 h and 1.44±1.04 h; Cmax 7.85±3.35μmol/l (Dose 300mg×2/d )and 4.15±1.70μmol/l (Dose 200mg×1/d);Cl_t5.7±2.2l/h and 9.3±4.1 l/h. The mean cumulative excretion of 24 h urine in 14 respiratory tract and 10 urinary tract infected patientswere 69.34±13.80% and 72.58±11.91%.