【摘要】 目的比较3种国产头孢丙烯制剂(第2代头孢类抗生素)在健康人体内的药代动力学,并评价3种制剂的生物等效性。方法21名健康志愿者三交叉单剂量口服头孢丙烯片、干混悬剂和对照头孢丙烯片500mg后,用HPLC-UV法测定血药浓度,计算其药代力学参数及评价3者生物等效性。结果头孢丙烯片、干混悬剂和头孢丙烯片对照品的主要药代动力学参数:AUC0-9分别为(21.12±2.33)、(21.38±2.60)和(21.68±2.34)μg.h.mL-1;AUC0-∞分别为(21.41±2.36)、(21.63±2.66)和(21.94±2.36)μg.h.mL-1;Cmax分别为(6.82±1.01)、(7.06±0.95)和(7.11±1.14)μg.mL-1;tmax分别为(1.71±0.46)、(1.45±0.38)和(1.64±0.36)h;t1/2分别为(1.23±0.12)、(1.25±0.16)和(1.21±0.13)h;MRT分别为(2.82±0.35)、(2.55±0.15)和(2.77±0.32)h;CL/F分别为(11.82±0.32)、(11.72±1.40)和(11.52±1.20)L.h-1。由AUC0-9、AUC0-∞估算的受试制剂的相对生物利用度分别为(98.2±13.3)%、(98.4±13.5)%及(99.2±12.4)%、(99.1±12.2)%。结论头孢丙烯片、干混悬剂和头孢丙烯片对照品3种制剂生物等效。更多还原

【Abstract】 Objective To study the pharmacokinetics and bioequivalence of cefprozil tablets and cefprozil for dry suspension in healthy volunteers. Methods The study was conducted in twenty-one healthy volunteers. After receiving a single dose of 500 mg cefprozil tablets 、dry suspension and the reference tablets by three crossed way.The blood drug concentration were determined by HPLC-UV and the pharmacokinetic parameters and relative bioavailability were calculated.Results The pharmacokinetic parameters for cefprozil tablets dry suspension and the reference tablets were as follows: AUC0-9 were (21.12±2.33),(21.38±2.60)and(21.68±2.34)μg.h.mL-1;AUC0-∞ were(21.41±2.36),(21.63±2.66)and(21.94±2.36)μg.h.mL-1;Cmax were (6.82±1.01),(7.06±0.95)and(7.11±1.14)μg.mL-1;tmax were (1.71±0.46),(1.45±0.38)and(1.64±0.36)h;t1/2 were (1.23±0.12),(1.25±0.16) and (1.21±0.13)h; MRT were (2.82±0.35),(2.55±0.15) and (2.77±0.32)h; CL/F were(11.82±0.32),(11.72±1.40)and(11.52±1.20)L.h-1. The relative bioavailability of AUC0-9 and AUC0-∞ tablets and for dry suspension are (98.2±13.3)%,(98.4±13.5)% and (99.2±12.4)%,(99.1±12.2)%,respectively.Conclusion The cefprozil tablets,dry suspension and the reference tablets were bioequivalent.更多还原