摘要
目的 :建立测定体液中他唑巴坦浓度的 HPLC方法 ,并应用于哌拉西林 /他唑巴坦健康人体的药代动力学研究。方法 :10名男性健康志愿者单剂量静脉滴注 4.5 g哌拉西林 /他唑巴坦钠 ,采用反相高效液相色谱 ( RP-HPLC)法测定血浆样品和尿中他唑巴坦药物浓度。 结果 :滴注完成即刻浓度 ( cm ax)为 ( 3 4.3 3± 8.0 5 )μg/m l,清除半衰期 ( t1 /2β)为 ( 0 .94± 0 .16) h,分布容积 ( Vd)为 ( 15 .43± 3 .82 ) L/kg,清除率 ( Clr)为 ( 15 .2 0± 2 .5 4) L /h,血药浓度 -时间曲线下面积 ( AUC)为 ( 4 2 .41±7.45 ) h·μg· ml-1 。结论 :他唑巴坦的体内过程符合二室开放模型 ,他唑巴坦主要以原形经肾脏排出体外 ,8h累积尿排百分率为 ( 78.68± 5 .84) %。
Objective: To establish a RP HPLC method for determining the concentration of tazobactam in body fluids, and to investigate the pharmacokinetics of tazobactam in healthy volunteers by this method. Methods: Ten healthy male volunteers were given a single dose of piperacillin/tazobactam 4.5 g by infusion. Tazobactam concentrations in plasma and urine were measured by RP HPLC method. Results: The peak plasma level ( c max ), plasma elimination half life ( t 1/2β ), volume of distribution (V d), clearance (Clr) and area under plasma concentration time curve (AUC) were (34 33±8 05) μg/ml, (0 94±0 16) h, (15 43±3 82) L/kg, (15 20±2 54) L/h and (42 41±7 45) h·μg·ml -1 , respectively. Conclusion: The disposition of tazobactam can be discribed with a two compartment open pharmacokinetic model. Tazobactam is mainly excreted through kidney in unchanged form. The cumulative urinary excretive rate of tazobactam is (78 68±5 84)% in 8 h after administration. [
出处
《药学服务与研究》
CAS
CSCD
2003年第2期98-101,共4页
Pharmaceutical Care and Research
关键词
他唑巴坦
药代动力学
色谱法
高压液相
tazobactam
pharmacokinetics
chromatography, high pressure liquid
