头孢他美酯人体内药动学研究

Pharmacokinetics of cefetamet in healthy volunteers

目的 研究头孢他美酯体内活性物头孢他美体内药动学。方法 利用HPLC DAD检测器三维色谱分析法及保留时间结合光谱分析对体内活性物头孢他美进行定性 ,测定志愿者口服头孢他美酯胶囊及片剂后头孢他美的血药浓度 ,研究其药动学。结果 头孢他美酯经口服给药后在肠道内迅速分解释放出游离头孢他美酸活性物 ,经DAD三维色谱对比发现其体内活性物的色谱行为及峰纯度与体外头孢他美标准对照品完全一致 ,对 18名健康志愿者口服 375mg头孢他美酯胶囊和片剂的药动学参数分别为Ke(0 .31± 0 .0 5 )和 (0 .32± 0 .0 6 )h-1,t1/2 (2 .33± 0 .42 )和 (2 .2 6± 0 .43)h ,tmax(2 .5 0± 0 .6 6 )和 (2 .44± 0 .45 )h ,cmax(3.5 7± 0 .97)和 (3.79± 1.15 ) μg·mL-1,AUC(18.0 4± 5 .83)和 (18.39± 6 .17) μg·mL-1。结论 所建立的HPLC方法简便、快速。

OBJECTIVE: To establish a HPLC method for the determination of plasma cefetamet levels after cefetamet pivoxil was administered. The pharmacokinetics of it was also evaluated. METHODS: Cefetamet was identified in plasma by 3-D chromatography behavior, retention time and spectrum analysis. With this methods, the pharmacokinetics of cefetame in 18 male volunteers was studied after administration of cefetamet pivoxil capsule or tablets. RESULTS: Cefetamet pivoxil was hydrolysised in intestine into active metabolite, cefetamet. There were no significant difference between the two preparations. CONCLUSION: Verificated the active metabolite, cefetamet by 3-D chromatography analysis, is simple and rapid. It can be used for its pharmacokinetic study.