十二指肠溃疡患者长期治疗前后奥美拉唑的口服生物利用度。
Oral bioavailability of omeprazole before and after chronic therapy in patients with duodenal ulcer.
作者信息
Ching M S, Mihaly G W, Angus P W, Morgan D J, Devenish-Meares S, Yeomans N D, Smallwood R A
机构信息
Department of Medicine, University of Melbourne, Austin Hospital, Heidelberg, Australia.
出版信息
Br J Clin Pharmacol. 1991 Feb;31(2):166-70. doi: 10.1111/j.1365-2125.1991.tb05506.x.
Abstract
- This study investigated the mechanism of the increase in oral bioavailability of omeprazole during repeated oral dosing. Eight patients with duodenal ulcer received an i.v. dose of omeprazole before and after a 4-week course of oral omeprazole, 20 mg daily, given as enteric-coated granules. 2. AUCoral and oral bioavailability (F) increased during omeprazole treatment by 50% (P less than 0.01) and 35% (P less than 0.05), respectively. 3. There was no change in the systemic clearance of omeprazole after i.v. dosage following the course of treatment. 4. We conclude that the increased omeprazole AUC observed on repeated administration of enteric-coated granules is due to increased systemic availability rather than decreased systemic elimination. The increased availability appears to be due to increased gastrointestinal absorption rather than decreased first-pass hepatic extraction.
摘要
- 本研究调查了重复口服给药期间奥美拉唑口服生物利用度增加的机制。8例十二指肠溃疡患者在接受为期4周、每日20mg肠溶颗粒剂口服奥美拉唑治疗前后接受了静脉注射剂量的奥美拉唑。2. 在奥美拉唑治疗期间，口服AUC和口服生物利用度（F）分别增加了50%（P<0.01）和35%（P<0.05）。3. 治疗疗程后静脉给药后奥美拉唑的全身清除率没有变化。4. 我们得出结论，重复给予肠溶颗粒剂后观察到的奥美拉唑AUC增加是由于全身可用性增加而非全身消除减少。可用性增加似乎是由于胃肠道吸收增加而非首过肝提取减少。
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