关键词: 头孢丙烯, 头孢丙烯, 头孢丙烯, 药动学, 药动学, 药动学, 生物等效性, 生物等效性, 生物等效性, 高效液相色谱, 高效液相色谱, 高效液相色谱

Abstract: 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, t_1/2 1.970 ± 0.388 h and 2.046 ± 0.449 h; T_max 1.600 ± 0.348 h and 1.675 ± 0.335 h; C_max 6.643 ± 1.104 μg·mL^-1 and 6.637 ± 1.320 μg·mL^-1 ; AUC_0-12 21.586 ± 4.154 μg·mL^-1·h and 21.121 ± 4.255 μg·mL^-1·h; AUC_0-∞ 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.

Key words: cefprozil, cefprozil, pharmacokinetics, pharmacokinetics, bioequivalence, bioequivalence, HPLC, HPLC