论文部分内容阅读
目的:建立HPLC法测定人血浆中头孢丙烯,研究国产头孢丙烯片(受试制剂A)在健康人体内的药动学特点,并评价其与参比制剂R的生物等效性。方法:20名男性健康受试者随机分为2组,进行单剂量双周期双交叉试验,分别口服500mg头孢丙烯受试制剂和参比制剂,2次试验间隔时间为7d。用HPLC法测定血浆中头孢丙烯浓度,计算其药动学参数。结果:受试制剂和参比制剂的主要药动学参数Cmax分别为(8.7±1.3)和(8.4±1.2)μg.mL-1;tmax分别为(1.9±0.5)和(1.7±0.5)h;t1/2分别为(1.30±0.16)和(1.31±0.12)h;CL/F分别为(16.2±2.8)和(14.1±2.4)L.h-1;MRT0-10分别为(2.83±0.28)和(2.8±0.3)h;MRT0-∞分别为(3.0±0.3)和(3.0±0.4)h;AUC0-10分别为(30.3±5.1)和(28.4±4.6)μg.h.mL-1;AUC0-∞分别为(31.0±5.2)和(29.2±4.6)μg.h.mL-1;由AUC0-10、AUC0-∞估算的受试制剂的相对生物利用度分别为(106.5±7.8)%和(106.2±7.2)%。结论:本实验方法准确、灵敏、特异性强、操作简便,适于头孢丙烯片的药动学和生物等效性研究,试验结果表明两制剂具有生物等效性。
OBJECTIVE: To establish a HPLC method for the determination of cefprozil in human plasma and to study the pharmacokinetic characteristics of domestic cefprozil tablets (Formulation A) in healthy volunteers and to evaluate the bioequivalence of cefprozil with reference formulation R. Methods: Twenty male healthy subjects were randomly divided into two groups. The single-dose, two-cycle, double-crossover study was conducted. Oral administration of 500 mg cefprozil test and reference formulation was given orally. The interval between the two tests was 7 days. The concentration of cefprozil in plasma was determined by HPLC and its pharmacokinetic parameters were calculated. RESULTS: The main pharmacokinetic parameters Cmax were (8.7 ± 1.3) and (8.4 ± 1.2) μg.mL-1, respectively; the tmax were (1.9 ± 0.5) and (1.7 ± 0.5) h (1.30 ± 0.16) and (1.31 ± 0.12) h for t1 / 2; (16.2 ± 2.8) and (14.1 ± 2.4) Lh-1 for CL / F; (2.8 ± 0.3) h and (3.0 ± 0.3) and (3.0 ± 0.4) h for MRT0-∞, respectively. AUC0-10 was (30.3 ± 5.1) and (28.4 ± 4.6) μg.h.mL- -∞ were (31.0 ± 5.2) and (29.2 ± 4.6) μg.h.mL-1, respectively. The relative bioavailabilities of the tested formulations estimated by AUC0-10 and AUC0-∞ were (106.5 ± 7.8)% and (106.2 ± 7.2)%. Conclusion: The experimental method is accurate, sensitive, specific and easy to operate. It is suitable for the study of pharmacokinetics and bioequivalence of cefprozil tablets. The results show that the two preparations have bioequivalence.