CAJ | 학술논문

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(1011.69±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。
목적：：평개장용미환뢰패랍서납효낭적인체생물이용도급생물등효성。방법：32명건강남성지원자수궤교차단제량구복장용미환뢰패랍서납효낭(수시제제)여뢰패랍서납장용효낭(삼비제제)각20 mg,분별재불동시간점채집혈장양본,청세기7 d。채용LC-MS/MS법측정혈장중뢰패랍서농도,채용DAS 3.0연건통계분석약동학삼수。결과：수시자찬후구복장용미환뢰패랍서납효낭여장용효낭적주요약동학삼수여하：T1/2분별위(2.20±0.83) h화(1.95±0.52) h ；Tmax (3.88±1.11) h화(4.64±1.50)h；Cmax분별위(401.06±170.75)ng·ml-1화(394.63±215.64)ng·ml-1；AUC0→t분별위(918.42±427.39) ng·h·ml-1화(994.49±520.73)ng·h·ml-1；AUC0→∞분별위(937.30±445.13)ng·h·ml-1화(1011.69±534.78)ng·h· ml-1。수거분석현시：량충제제적주요약동학삼수제Tmax(P<0.05)외,기여차이균무통계학의의(P>0.05)。장용미환뢰패랍서납효낭적상대생물이용도위(99.80±7.20)%。결론：장용미환뢰패랍서납효낭교삼비제제분산정도고、수식물영향소、약물석방쾌、흡수신속；수시제제여삼비제제구유생물등효성。
Objective: To evaluate the bioavallability and bioequivalence of rabeprazole sodium enteric-coated pellets capsules. Methods:A randomized crossover design was performed in 32 healthy male volunteers. A single oral dose of 20 mg rabeprazole sodium enteric-coated pellets capsules ( test preparation) or enteric-coated shell capsules ( the reference capsules) was administrated under fed conditions. The wash period was 7 days. The blood samples were collected at different time points. The concentration of rabeprazole in plasma was determined by an LC-MS/MS method. The pharmacokinetic parameters were calculated by DAS 3. 0 software and the bio-equivalence was evaluated. Results:The maln pharmacokinetic parameters of the two formulations were shown as follows:T1/2 of (2. 20 ± 0. 83)h and(1. 951 ± 0. 515)h,Tmax of (3. 88 ± 1. 11)h and(4. 64 ± 1. 504)h,Cmax of (401. 06 ± 170. 75)ng·ml-1 and(394. 63 ± 215.64)ng·ml-1,AUC0→t of (918.42 ±427.39)ng·h·ml-1 and (994.49 ±520.73)ng·h·ml-1, and AUC0→∞ of(937.30 ± 445.13)ng·h·ml-1 and(1 011.69 ±534.77)ng·h·ml-1. The analysis showed that the maln pharmacokinetic parameters of the two formulations had no significant differences(P>0. 05) except for Tmax(P<0. 05). The relative bioavallability of rabeprazole sodium enteric-coated pellets capsules was (99. 80 ± 7. 20) %. Conclusion:Compared with the reference capsules, rabeprazole sodium enter-ic-coated pellets capsules show the property of higher dispersion degree, milder influence from food, more rapid release and absorption. The enteric-coated pellets capsules and the reference capsules are bioequivalence.