Abstract
Background and Objectives
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.
Methods
This was an open-label and multiple-dose clinical study. Ten healthy Chinese subjects received 10 mg ilaprazole infusion once daily for 5 days. Helicobacter pylori status was examined. Blood samples were collected and intragastric pH was recorded for 24 h. Safety was assessed throughout the study.
Results
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 24 h and mean 24-h pH values. The pH value within 24 h was affected by Helicobacter pylori infection in subjects with continuous infusion. Intravenous ilaprazole was safe and there were no serious adverse events.
Conclusion
Intravenous ilaprazole provided stable pharmacokinetics and pharmacodynamics at a dose of 10 mg once daily for 5 days, and was well tolerated in healthy subjects.
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Funding
This study was funded by the National Science and Technology Major Project of China (2012ZX09303006-002) and by Livzon Pharmaceutical Group Inc. (Zhuhai Guangdong, China).
Conflict of interest
Hongyun Wang, Liwei Lang, Pei Hu, and Ji Jiang are employees of Peking Union Medical College Hospital. Ning Ou and Ruihua Shi are employees of Jiangsu Province Hospital. Chengyun Su and Haitang Hu are employees of Livzon Pharmaceutical Co., Ltd.
Ethical approval
All procedures in this study were carried out in accordance with the Declaration of Helsinki and its amendments and the ethics committee or institutional review board which approved the study.
Informed consent
Written informed consent was obtained from the subjects prior to the conduct of the study.
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Wang, H., Lang, L., Ou, N. et al. Pharmacokinetics, Pharmacodynamics and Safety of Multiple-Infusion Ilaprazole in Healthy Chinese Subjects. Clin Drug Investig 36, 463–470 (2016). https://doi.org/10.1007/s40261-016-0390-2
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DOI: https://doi.org/10.1007/s40261-016-0390-2