头孢泊肟酯片人体药动学及生物等效性评价

Study on the pharmacokinetics and bioequivalence of cefpodoxime proxetil tablets in healthy volunteers

目的 :研究国产和进口头孢泊肟酯片在人体的药动学和生物等效性。方法 :2 0名健康男性志愿者随机交叉口服单剂量国产和进口头孢泊肟酯片 2 0 0mg ,采用高效液相色谱法测定其活性代谢产物头孢泊肟的经时血药浓度 ,计算其药动学参数和相对生物利用度 ,评价两种制剂的生物等效性。结果 :国产和进口头孢泊肟酯片的主要药动学参数t1 / 2 分别为 (2 .6±0 .9)h和 (2 .7± 1 .1 )h ,tmax分别为 (3.0± 0 .6 )h和 (3.0± 0 .5 )h ,Cmax分别为 (4.3± 0 .7)mg·L-1 和 (4.2± 0 .8)mg·L-1 ,AUC0→ 1 2 分别为 (2 1 .1± 4 .8)mg·h·L-1 和 (2 1 .9± 5 .5 )mg·h·L-1 ,AUC0→∞ 分别为 (2 3.1± 6 .1 )mg·h·L-1 和 (2 4 .0± 6 .6 )mg·h·L-1 ,国产头孢泊肟酯片的相对生物利用度为 (97.8± 1 3.5 ) %(F0→ 1 2 )和 (97.2± 1 5 .9) %(F0→∞)。结论 :经统计学分析 ,两种制剂具有生物等效性。

OBJECTIVE To study the pharmacokinetic profiles and bioequivalence of domestic and imported cefpodoxime proxetil tablets in healthy volunteers. METHODS A single oral dose of 200 mg domestic or imported cefpodoxime proxetil tablets were given to 20 healthy male volunteers in an open randomized crossover design. Cefpodoxime concentrations in plasma were determined by HPLC. The pharmacokinetic parameters and relative bioavailability were calculated by 3P97 program to evaluate the bioequivalence of the two preparations. RESULTS The main pharmacokinetic parameters of the two preparations were as follow: t 1/2 were( 2.6 ± 0.9)h and( 2.7 ± 1.1)h , t max were( 3.0 ± 0.6)h and( 3.0 ± 0.5)h , C max were( 4.3 ± 0.7)mg ·L -1 and( 4.2 ± 0.8 )mg·L -1 ,AUC 0→12 were( 21.1 ± 4.8)mg ·h·L -1 and( 21.9 ± 5.5)mg ·h·L -1 ,AUC 0→∞ were ( 23.1 ± 6.1)mg ·h·L -1 and( 24.0 ± 6.6)mg ·h·L -1 ,respectively. The relative bioavailability of domestic to imported tablets was( 97.8 ± 13.5 )%( F 0→12 )and( 97.2 ± 15.9 )%( F 0→∞ ). CONCLUSIONS The statistical analysis of the result shows that the two preparations are bioequivalent .