Pharmacokinetics, Pharmacodynamics and Safety of Multiple-Infusion Ilaprazole in Healthy Chinese Subjects.

Abstract

Ilaprazole is a novel proton pump inhibitor that provides effective and long lasting inhibition of intragastric acid secretion. The objectives of this study were to investigate the pharmacokinetics, pharmacodynamics, and safety of intravenous ilaprazole after multiple administrations in healthy Chinese subjects. This was an open-label and multiple-dose clinical study. Ten healthy Chinese subjects received 10mg ilaprazole infusion once daily for 5days. Helicobacter pylori status was examined. Blood samples were collected and intragastric pH was recorded for 24h. Safety was assessed throughout the study. There was no accumulation after multiple administrations. The mean steady-state half-life and clearance were comparable to those following single administration. Ilaprazole provided sustainable and significant intragastric pH control in terms of percentage time at pH >4, pH >6 within 24h and mean 24-h pH values. The pH value within 24h was affected by Helicobacter pylori infection in subjects with continuous infusion. Intravenous ilaprazole was safe and there were no serious adverse events. Intravenous ilaprazole provided stable pharmacokinetics and pharmacodynamics at a dose of 10mg once daily for 5days, and was well tolerated in healthy subjects.