盐酸头孢他美酯健康人体药动学研究

Study on pharmacokinetics of cefetamet pivoxil in healthy volunteers

目的 研究头孢他美酯在健康人体内的药动学。方法 18名健康志愿者单剂量 po盐酸头孢他美酯片 5 0 0mg ,采用高效液相色谱法测定血浆和尿中活性代谢物头孢他美药物浓度。结果 药动学参数末端相消除半衰期 (t1/2 )、峰浓度 (cmax)、AUC0～ 12 分别为 :( 2 .5 2± 0 .4 7)h ,( 3.6 7± 0 .98) μg·mL-1,( 2 1.10± 5 .19) μg·h·mL-1。结论 头孢他美的体内过程符合二室开放模型 ,主要经肾脏排出体外 ,12h累积尿排百分率为 ( 36 .0 0± 8.6 2 ) %。

OBJECTIVE: To study the pharmacokinetics of cefetamet pivoxil in 18 healthy volunteers after oral administration of 500 mg cefetamet pivoxil hydrochloride tablet. METHOD: The concentrations of cefetamet in plasma and urine were measured by an improved HPLC method. RESULTS: The results showed that the terminal phase plasma elimination half-life (t1/2), peak plasma level (cmax), area under plasma concentration-time curve(AUC) were (2.52 ± 0.47) h, (3.67 ± 0.98) μg&middotmL-1, (21.1 ± 5.19) μg&middoth&middot mL-1, respectively. CONCLUSION: The plasma concentration-time curve of cefetamet conformed to a two-compartment open pharmacokinetic model. Cefetamet is mainly excreted through kidney in unchanged form. The cumulative urinary excretive rate of cefetamet was (36.0 ± 8.62) % within 12 h after administration.