国产头孢拉定临床药代动力学及其胶囊剂的生物等效性

Clinical pharmacokinetics and relative bioequivalence of domestic cephradine cap sule

目的 :研究口服国产头孢拉定胶囊在 18名健康志愿者中的药代动力学和相对生物利用度。方法 :18名健康志愿者分别双交叉口服单剂量国产头孢拉定胶囊和进口头孢拉定胶囊各 0 .5 g ,用反相高效液相 (RP HPLC)法测定血浆中头孢拉定浓度。采用双向单侧t检验进行生物等效性评价。结果 :国产品和进口品t1/ 2 分别为 (1.0 9± 0 .2 6 )和 (1.0 8± 0 .30 )h ,tmax分别为 (0 .86± 0 .15 )和 (0 .85± 0 .13)h ,cmax分别为 (18.5 9± 3.6 9)和 (17.35± 3.81)mg/L ,AUC0 5分别为 (30 .4 0± 4 .2 8)和(2 9.92± 3.2 6 )mg·h/L。国产品的相对生物利用度为 10 1.5 3%± 8.4 6 % ,ln(AUC0 5)、ln(AUC0 ∞)、ln(cmax)经双向单侧t检验 :接受生物等效的假设。结论 :国产品与进口品具有生物等效性。

Objective: To study the pharmacokinetics and relative bioavailability of cephrad ine capsule in 18 healthy volunteers. Methods: According to crossover design, each volunteer was given a single dose of 0.5?g domestic or imported cephradine capsule. The plasma concentrations were determined by RP-HPLC. Pharmacokinetic parameters were calculated based on noncompartment model. Bioequivalence was analysed by two one-sided t test. Results: The phamacokinetic parameters of the domestic and imported cephradine capsule we re as follows: t 1/2 1.09±0.26 and 1.08±0.30 h, C max 18.59±3.69 and 17.35±3.81 mg/L at 0.86±0.15 and 0.85±0.13 h and AUC 0-5 30.40±4.28 and 29.92±3.26 mg·h/L, respectively. The relative bioavailability of the domest ic cephradine capsule was 105.84%±9.63%. The results of two one-sided t t est showed no significant difference. Conclusions: The results show that the two capsules are bioequi valent.