奥美拉唑抑制胃酸分泌对健康志愿者口服呋喃唑酮相对生物利用度的影响。
Effect of acid secretion blockade by omeprazole on the relative bioavailability of orally administered furazolidone in healthy volunteers.
作者信息
Calafatti S A, Ortiz R A, Deguer M, Martinez M, Pedrazzoli J
机构信息
Clinical Pharmacology and Gastroenterology Unit, São Francisco University Medical School, Bragança Paulista, SP, Brazil.
出版信息
Br J Clin Pharmacol. 2001 Aug;52(2):205-9. doi: 10.1046/j.0306-5251.2001.01435.x.
AIMS
The administration of omeprazole may interfere with the absorption of orally administered drugs by reducing gastric pH and hence tablet dissolution. The aim of this study was to investigate the effects of a 5 day administration of omeprazole on the pharmacokinetics of furazolidone.
METHODS
Eighteen healthy (nine male and nine female) volunteers were selected. The study had an open randomized two-period crossover design with a 21 day washout period between the phases. Serum concentrations of furazolidone were measured by reversed-phase h.p.l.c. with ultraviolet detection.
RESULTS
Administration of omeprazole caused a significant reduction of Cmax [0.34 microg x ml(-1) (range 0.25-0.43) vs 0.24 microg x ml(-1) (range 0.15-0.34)] with no significant delay in absorption tmax [2.5 h (range 1.85-3.0) vs 2.4 h (range 2.06-2.71)].
CONCLUSIONS
Furazolidone was rapidly absorbed after oral administration. Short-term treatment with omeprazole did alter the relative bioavailability of this drug, probably through an effect on absorption kinetics or first-pass metabolism.
目的
奥美拉唑的给药可能会通过降低胃内pH值从而影响口服药物的吸收，进而影响片剂的溶解。本研究的目的是调查连续5天服用奥美拉唑对呋喃唑酮药代动力学的影响。
方法
选取18名健康志愿者（9名男性和9名女性）。本研究采用开放随机两周期交叉设计，两阶段之间有21天的洗脱期。采用反相高效液相色谱法并结合紫外检测测定呋喃唑酮的血清浓度。
结果
服用奥美拉唑导致Cmax显著降低[0.34微克×毫升⁻¹（范围0.25 - 0.43）对比0.24微克×毫升⁻¹（范围0.15 - 0.34）]，吸收tmax无显著延迟[2.5小时（范围1.85 - 3.0）对比2.4小时（范围2.06 - 2.71）]。
结论
呋喃唑酮口服后吸收迅速。短期服用奥美拉唑确实改变了该药物的相对生物利用度，可能是通过影响吸收动力学或首过代谢实现的。
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