三种奥美拉唑胶囊健康人的生物利用度及其对胃内24小时pH值的影响

Bioavailability of three brands of omeprazole capsule and their effects on 24 hour intragastric pH in healthy volunteers

目的 比较 3种奥美拉唑胶囊产品 (洛赛克、奥克、奥美拉唑 ) 4 0mg在健康人的生物利用度及对胃内 2 4小时pH值的影响。方法 交叉试验设计 :18例健康志愿者 (男 12例 ,女 6例 )被随机分成 3组 ,每组交叉服用洛赛克、奥克、奥美拉唑胶囊 1次 4 0mg ,交叉间隔时间 7天。结果 药代动力学研究结果表明相对于奥克胶囊与奥美拉唑胶囊 ,洛赛克胶囊有吸收速度快、血药浓度高与持续时间长及生物利用度高的优点。胃内 2 4小时pH值研究表明 3种不同胶囊服用后都会引起胃内pH值的升高并增加pH值大于 4的持续时间。 3组相比 ,洛赛克胶囊起效时间最快 ,为 2 .5 3小时 ,胃内pH值升高最多 ,为 3 .3 7,胃内pH值大于 4的增加持续时间最长 ,为 15 .3小时 ,表明其抑制胃酸分泌作用最强 ;而奥克胶囊与奥美拉唑胶囊抑制胃酸分泌的作用基本相同。结论 3种不同奥美拉唑胶囊产品在健康人体内的药代动力学过程及升高胃内pH值的作用有明显差异。相比而言 ,洛赛克胶囊具有生物利用度高、起效快、作用强与药效持续时间长的优点。

Objective To compare the bioavailability of three brands of omeprazole capsule (Losec, Aoke Changzhou No.4 Pharm, Omeprazole Sanye Pharm) and their effects on 24 hour intragastric pH in healthy volunteers. Methods With crossover design (washout period of 7 days), 18 healthy volunteers (12 men, 6 women) were randomly divided into three groups. Each subject was given the three different brands of omeprazole capsule 40 mg respectively. Results The pharmacokinetic study revealed that Losec had an advantage over other two brands of omeprazole capsule in that it was absorbed more rapidly and to a greater extent, resulting in higher plasma concentration and longer staying time in blood. It also showed the shortest latent time in elevating intragastric pH (2.53 hours), the largest net increment in mean gastric pH (3.37), and the greatest prolongation of time with pH>4 (15.3 hours) among the three products. Conclusion The three brands of omeprazole capsule are significantly different with respect to their pharmacokintic process and effects on 24 hour intragastric pH profile. Losec is superior to other two brands of omeprazole capsule in view of its better bioavailbility, quicker onset of action, more potent and lasting antisecretory effect.