论文部分内容阅读
目的:评价肠溶微丸雷贝拉唑钠胶囊的人体生物利用度及生物等效性。方法:32名健康男性志愿者随机交叉单剂量口服肠溶微丸雷贝拉唑钠胶囊(受试制剂)与雷贝拉唑钠肠溶胶囊(参比制剂)各20 mg,分别在不同时间点采集血浆样本,清洗期7 d。采用LC-MS/MS法测定血浆中雷贝拉唑浓度,采用DAS 3.0软件统计分析药动学参数。结果:受试者餐后口服肠溶微丸雷贝拉唑钠胶囊与肠溶胶囊的主要药动学参数如下:T1/2分别为(2.20±0.83)h和(1.95±0.52)h;Tmax(3.88±1.11)h和(4.64±1.50)h;Cmax分别为(401.06±170.75)ng·ml-1和(394.63±215.64)ng·ml-1;AUC0→t分别为(918.42±427.39)ng·h·ml-1和(994.49±520.73)ng·h·ml-1;AUC0→∞分别为(937.30±445.13)ng·h·ml-1和(1 011.69±534.78)ng·h·ml-1。数据分析显示:两种制剂的主要药动学参数除Tmax(P<0.05)外,其余差异均无统计学意义(P>0.05)。肠溶微丸雷贝拉唑钠胶囊的相对生物利用度为(99.80±7.20)%。结论:肠溶微丸雷贝拉唑钠胶囊较参比制剂分散程度高、受食物影响小、药物释放快、吸收迅速;受试制剂与参比制剂具有生物等效性。
OBJECTIVE: To evaluate the bioavailability and bioequivalence of enteric-coated microballoon rabeprazole sodium capsules. Methods: Twenty-two healthy male volunteers were randomized crossover single oral dose of oral rabeprazole sodium capsules (test preparation) and rabeprazole sodium enteric-coated capsules (reference preparation) of 20 mg, respectively, at different times Point collection of plasma samples, washing 7d. Plasma concentration of rabeprazole was determined by LC-MS / MS. Pharmacokinetic parameters were analyzed by DAS 3.0 software. Results: The main pharmacokinetic parameters of rabeprazole sodium capsules and enteric capsules after oral administration were as follows: T1 / 2 (2.20 ± 0.83) h and (1.95 ± 0.52) h respectively; Tmax (3.88 ± 1.11) h and (4.64 ± 1.50) h respectively; C max were (401.06 ± 170.75) ng · ml-1 and (394.63 ± 215.64) ng · ml-1 respectively; AUC0 → t were (918.42 ± 427.39) ng (937.30 ± 445.13) ng · h · ml-1 and (1 011.69 ± 534.78) ng · h · ml-1 · h · ml-1 and (994.49 ± 520.73) ng · h · ml- 1. Data analysis showed that the main pharmacokinetic parameters of the two preparations had no significant difference except Tmax (P <0.05) (P> 0.05). The relative bioavailability of rabeprazole sodium capsules was (99.80 ± 7.20)%. Conclusion: The rabeprazole sodium capsule has a higher degree of dispersion than the reference formulation, less affected by food, fast release of drug and rapid absorption; and bioequivalence of the test preparation and the reference preparation.