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目的:建立高效液相色谱并同时测定人血浆中的顺式和反式头孢丙烯,对头孢丙烯分散片进行人体药物动力学和生物等效性研究。方法:将20名男性健康志愿者随机分两组进行两制剂双周期随机交叉试验,单次口服头孢丙烯分散片受试制剂或参比制剂500 mg,清洗期为7 d。用HPLC法测定血浆中头孢丙烯浓度,计算其药动学参数。结果:血浆中杂质不干扰样品的测定,标准曲线范围为0.10～20.0μg·ml~(-1),线性关系良好(r=0.999 7),最低定量限为0.10μg·ml~(-1);受试制剂和参比制剂中头孢丙烯的AUC_(0～t)分别为(30.26±4.65)μg·h·ml~(-1)和(31.29±5.42)μg·h·ml~(-1),AUC_(0～∞)分别为(30.73±4.75)μg·h·ml~(-1)和(31.78±5.62)μg.h·ml~(-1),C_(max)分别为(9.39±1.29)μg·ml~(-1)和(9.30±1.63)μg·ml~(-1),t_(max)分别为(1.53±0.49)h和(1.70±0.25)h,t_(1/2)分别为(1.52±0.20)h和(1.49±0.20)h,受试制剂的相对生物利用度为:(97.9±13.9)%。结论:分析方法操作简便,结果准确可靠。统计分析表明,两制剂具有生物等效性。
OBJECTIVE: To establish a HPLC method for the simultaneous determination of cis- and trans-cefprozil in human plasma. The pharmacokinetics and bioequivalence of cefprozil dispersible tablets were studied. Methods: Twenty male healthy volunteers were randomly divided into two groups. The two groups were randomized to two cycles of crossover test. The single oral dose of cefprozil dispersible tablets or reference preparations was 500 mg, and the cleaning period was 7 days. The concentration of cefprozil in plasma was determined by HPLC and its pharmacokinetic parameters were calculated. Results: The impurities in the plasma did not interfere with the determination of the sample. The standard curve ranged from 0.10 to 20.0 μg · ml -1 with a good linearity (r = 0.999 7) and the lowest limit of quantification was 0.10 μg · ml -1 ; The AUC_ (0 ~ t) of cefprozil in the test preparation and the reference preparation were (30.26 ± 4.65) μg · h · ml -1 and (31.29 ± 5.42) μg · h · ml -1 ), AUC_ (0 ~ ∞) were (30.73 ± 4.75) μg · h · ml -1 and (31.78 ± 5.62) μg.h · ml -1 and C max were 9.39 ± 1.29 μg · ml -1 and 9.30 ± 1.63 μg · ml -1, respectively, and the t max was (1.53 ± 0.49) h and (1.70 ± 0.25) h respectively, t 1 / 2) were (1.52 ± 0.20) h and (1.49 ± 0.20) h respectively. The relative bioavailability of the test preparation was (97.9 ± 13.9)%. Conclusion: The method is simple, accurate and reliable. Statistical analysis showed that the two formulations were bioequivalent.