Bliesath H, Huber R, Hartmann M, Lühmann R, Wurst W
Research Division, Byk Gulden Pharmaceuticals, Konstanz, Germany.
Int J Clin Pharmacol Ther. 1996 May;34(1 Suppl):S18-24.
Pantoprazole is a specific inhibitor of the H+/K(+)-ATPase of the gastric parietal cell. The dose-dependency of a range of pantoprazole pharmacokinetic characteristics was studied. Twelve healthy male subjects were given 10, 20, 40 and 80 mg pantoprazole intravenously according to a randomized, single blind, 4-period change-over scheme. The area under the concentration vs time curve (AUC) and the maximum serum concentration (Cmax) showed a linear increase in line with the dose. Apparent volume of distribution (Vd area), clearance (Cl) and terminal half-life (t1/2) were independent of the dose. The dose-independent elimination of pantoprazole was attributed to the lack of interaction of the drug with cytochrome P450. In clinical practice, a good predictable response, as well as a low potential for interaction with other drugs might be expected.
泮托拉唑是胃壁细胞H⁺/K⁺-ATP酶的特异性抑制剂。研究了一系列泮托拉唑药代动力学特征的剂量依赖性。12名健康男性受试者按照随机、单盲、4期交叉方案静脉注射10、20、40和80mg泮托拉唑。浓度-时间曲线下面积(AUC)和血清最大浓度(Cmax)随剂量呈线性增加。表观分布容积(Vd area)、清除率(Cl)和末端半衰期(t1/2)与剂量无关。泮托拉唑的非剂量依赖性消除归因于该药物与细胞色素P450缺乏相互作用。在临床实践中,可以预期有良好的可预测反应以及与其他药物相互作用的可能性较低。