摘要
目的对中国健康成年志愿者单剂静脉滴注甲磺酸帕珠沙星氯化钠注射液的药动学研究。方法按GcP指导原则设计试验方案,选择10名健康受试者分别在30min内空腹静脉滴注甲磺酸帕珠沙星氯化钠注射液300和500mg,用HPLC-荧光法测定血浆、尿液中帕珠沙星的浓度,并采用3P97软件进行试验数据统计处理,求出药动学参数。结果帕珠沙星的血药浓度经时变化符合二房室模型,300和500mg的主要药动学参数如下：峰浓度Cmax分别为(7．716±1．373)和(11．652±2．197)μg／ml；半衰期t1/2分别为(2．00±0．26)h和(2．13±0．22)h；药时曲线下面积AUCo-∞分别为(14．170±3．244)和(25．370±3．234)μg·h／ml；表观分布容积Vc分别为(28．83±12．92)L和(31．62±8．91)L。尿药浓度测定结果表明,帕珠沙星0-24 h累积排出量分别为(261．82±30．92)mg和(452．27±32．35)mg,0-24 h累积排出百分比分别为(87．27±10．31)％和(90．45±6．47)％。结论帕珠沙星单次给药在中国健康人体耐受性良好,药时曲线符合二房室模型,帕珠沙星在300-500mg剂量范围内药物体内过程呈线性动力学特征,药物主要经肾脏排泄。
Objective To study the pharmacokinetics of single dose of pazufloxacin injection in healthy volunteers. Method According to the GCP, ten healthy volunteers were enrolled to receive a single dose of pazufloxacin 300 or 500mg winthin 30min infusion in an open randomized crossover study. The concentrations of pazufloxacin in serum and urine were determined by a high-pressure liquid chromatography （HPLC） method. Result Pharmacokinetics profiles were conformed to an open two-compartment model analyzed by using 3P97 and the result of HPLC method were as follows： Cmax= were （7. 716 ± 1. 373） μg/ml and （11. 652±2. 197） μg/ml; t1/2 were （2.00 ± 0.26）h and （2. 13±0,22）h;AUC0-∞ were （14.170＋3.244）μg/（ml· h） and （25.370＋3.234） μg/（ml· h） respectively;Vc were （28.83 ± 12.92） L and （31.62 ± 8.91）L; Urinary recovery rates were （87.27 ＋ 10.31）% and （90.45 ± 6.47）% of two doses, respectively. Conclusion Pazufloxacin was well tolerant in single dose infusion in healthy Chinese volunteers, The pharmacokinetics of the drug in trial dose nearly fit linear dynamic feature, and the drug mailv excreted through kidney.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2006年第4期220-222,246,共4页
Chinese Journal of Antibiotics
