雷贝拉唑肠溶片在健康志愿者体内的相对生物利用度

Bioequivalence of Raberazole enteric-coated tablets in healthy volunteers

目的:研究雷贝拉唑肠溶片的相对生物利用度.方法:采用标准二阶段交叉设计自身对照试验方法,应用反相高效液相色谱法测定18名健康男性志愿受试者单剂量口服20mg雷贝拉唑后的血药浓度,得出相应的药时曲线,计算各药代参数和相对生物利用度.结果:达峰时间(Tmax)分别为(4.3±1.4)和(4.3±1.1)h,半衰期(T1/2)分别为(1.5±0.4)和(1.4±0.4)h,峰值浓度(Cmax)分别为(505±169)和(466±182)μg/L,0→12h药时曲线下面积(AUC(0→12h))分别为(1365±454)和(1263±485)μg·h/L,0→∞药时曲线下面积(AUC0→∞)分别为(1399±471)和(1295±486)μg.h/L.以AUC(0→12h)计算,雷贝拉唑肠溶片的相对生物利用度为(111.1±20.0)%.结论:雷贝拉唑肠溶片与参比制剂为生物等效制剂.

AIM： To compare the relative bioavailability of the Raberazole preparations-sample tablets and reference tablets. METHODS： Raberazole concentrations in plasma of 18 healthy young volunteers were determined after a single oral dose （20 rag） of two Raberazole preparations were given respectively to 18 voluteers in an open randomized standard two-stage crossover self-control test. The Raberazole concentration in plasma was assayed by the HPLC method. The pharmacokinetic parameters were calculated with 3p97 program by computer. RESULTS： Time for peak concentration （Tmax） was （4.3 ±1.4） and （4.3 ±1.1） h, half life time （T1/2） was （1.5±0.4） and （1.4±0.4） h, peak concentration （Cmax） was （505 ± 169） and （466 ± 182） μg/L, 0→ 12 h area under the curve [AUC（0→12h） ] was （1365 ±454） and （1263 ±485） μg · h /L, 0→∞ area under the curve （AUC0→∞） was （1399 ±471） and （1295±486） μg · h/L. The relative bioavailability of Raberazole sample tablets compared with the contrast tablets was 111. 1%. CONCLUSION： The two preparations are bioequivalent.