雷贝拉唑胶囊和片剂的药动学和生物利用度

目的:研究雷贝拉唑胶囊和片剂的药动学与相对生物利用度,评价其生物等效性。方法:18名男性健康志愿者随机分2组,按双周期交叉口服雷贝拉唑的2种制剂,剂量40mg,用高效液相色谱法测定给药后不同时间点血浆中雷贝拉唑的浓度,计算2种制剂药动学参数和相对生物利用度,并评价其生物等效性。结果:口服雷贝拉唑片和雷贝拉唑胶囊的药动学参数:cmax分别为(1050±s470)和(1149±750)μg·L-1;tmax分别为(3.3±1.1)和(3.2±0.8)h;t12ke分别为(1.7±0.9)和(1.6±0.7)h;AUC0～t分别为(4211±3225)和(4373±3578)μg·h·L-1;AUC0～∞分别为(4340±3568)和(4478±3732)μg·h·L-1。2制剂间无显著差异(P>0.05)。雷贝拉唑胶囊相对生物利用度F0～t为(103±29)%。结论:方差分析及双单侧t检验表明,雷贝拉唑胶囊和片剂具有生物等效性。

Pharmacokinetics and bioequivalence of rabeprazole capsule and tablet

AIM: To evaluate the bioequivalence of rabeprazole capsule and tablet by pharmacokinetics and relative biological availability in human beings. METHODS: A single oral dose of 40 mg rabeprazole capsules or tablet was given to 18 healthy male volunteers in double alterrative periode for an open randomized cross-over test. The plasma levels of rabeprazole were detected by RP-HPLC method. The relative bioavailability and bioequivalence of rabeprazole were calculated and compared. RESULTS: The pharmacokinetic parameters of rabeprazole capsule and tablet were as follows:c_(max) were(1 050±s 470)μg·L~(-1) and(1 149±750)(μg·)L~(-1),t_(max) were(3.3±(1.1) h) and(3.2±0.8)h,t__(12ke) were(1.7±0.9) h and((1.6±0.7)) h,AUC_(0-t) were (4 211±3 225) μg·h·L~(-1) and (4 373±3 578)μg·h·L~(-1),AUC_(0-∞) were ((4 340±)3 568) μg·h·L~(-1) and (4 478±3 732) μg·h·L~(-1), respectively. The relative bioavailability of rabeprazole capsules F_(0-t) was (103±29) % comparing with the tablets. Variance analysis and two one-sided t test were performed on parameters c_(max), AUC_(0-t) and AUC_(0-∞). The results showed that the parameters demonstrated no significant statistical differences. CONCLUSION: The results of statistical analysis show that the two preparations of rabeprazole are bioequivalent. ing