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目的 建立生物样本头孢丙烯血浓度HPLC测定方法,进行头孢丙烯颗粒与头孢丙烯片健康志愿者体内药动学和相对生物等效性研究.方法 20名健康男性志愿者随机交叉单剂量口服头孢丙烯颗粒和头孢丙烯片各0.5 g,采用高效液相色谱法测定给药后不同时间血浆浓度,计算其主要药动学参数.结果 头孢丙烯颗粒与头孢丙烯片主要药动学参数 t1/2 为 1.970 ± 0.388 h 和 2.046 ± 0.449 h, Tmax为1.600 ± 0.348 h 和 1.675 ± 0.335 h,Cmax 为 6.643 ± 1.104 μg·mL-1和 6.637 ±1.320 μg·mL-1, AUC0-12为21.586 ± 4.154 μg·mL-1·h 和21.121 ± 4.255 μg·mL-1·h,AUC0-∞为21.814 ± 4.164 μg·mL-1·h和21.388 ± 4.308 μg·mL-1·h, 头孢丙烯颗粒相对生物利用度为103.138 % ± 12.042 %.结论 本文所建立的HPLC方法灵敏,简单,可用于头孢丙烯人体药动学及生物等效性研究.AUC0-12,AUC0-∞, Cmax 和Tmax方差分析,双单侧检验及90%置信限分析显示,两制剂具有生物等效性.“,”Aim To develop a rapid, simple, and sensitive high-performance liquid chromatographic (HPLC) method for the determination of cefprozil in human plasma and to study its pharmacokinetics and bioequivalence after 0.5 g oral doses of cefprozil granules and tablets. Methods The blood concentration of cefprozil was analyzed after extracted with 6% trichloroacetic acid, using tinidazole as internal standard (I.S.). A C18 column was used to separate cefprozil with mobile phase of methanol, purified water and glacial acetic acid (30∶70∶1, V/V/V) at flow rate of 1.0 mL·min-1, and the detection occurred at 280 nm. Pharmacokinetics parameters of cefprozil were calculated and bioequivalence of cefprozil granules and tablets was evaluated. Results The lower detection and quantification limit was 0.05 μg·mL-1, and the calibration curves were linear over a concentration range of 0.05 - 12 μg·mL-1 of cefprozil in plasma. The pharmacokinetic parameters after oral administration of 0.5 g cefprozil granules and tablets were as follows, t1/2 1.970 ± 0.388 h and 2.046 ± 0.449 h; Tmax 1.600 ± 0.348 h and 1.675 ± 0.335 h; Cmax 6.643 ± 1.104 μg·mL-1 and 6.637 ± 1.320 μg·mL-1; AUC0-12 21.586 ± 4.154 μg·mL-1·h and 21.121 ± 4.255 μg·mL-1·h; AUC0-∞ 21.814 ± 4.164 μg·mL-1·h and 21.388 ± 4.308 μg·mL-1·h, respectively. The bioavailability of cefprozil granules to tablets was 103.138 ± 12.042%. Conclusion High resolution HPLC method has been set up and succesfully applied to cefprozil pharmacokinetic studies and bioequivalence evaluation of cefprozil granules and tablets. Cefprozil granules and tablets are bioequivalent.