Original Article

Pharmacokinetic interactions between ilaprazole and clarithromycin following ilaprazole, clarithromycin and amoxicillin triple therapy

Authors: Shan Cao, Gan Zhou, Dong-sheng Ou-YANG, Hui-zi Wu, Kui Xiao, Yao Chen, Dong Guo, Lan Fan, Zhi-rong Tan, Hai-tang Hu, Xiang-hong Qin, Hong-hao Zhou, Wei Zhang
DOI: 10.1038/aps.2012.64


Aim: To investigate the drug interactions between ilaprazole, a new proton pump inhibitor, and clarithromycin following ilaprazole, clarithromycin and amoxicillin combination therapy.
Methods: Twelve healthy Chinese volunteers were recruited in a randomized, open-label, 3-period crossover study. All subjects were administered ilaprazole (5 mg), clarithromycin (500 mg) or a triple therapy, including ilaprazole (5 mg), clarithromycin (500 mg) and amoxicillin (1 g), twice daily for 6 consecutive days. On the 7th day, the drugs were given once, and blood samples were collected and analyzed using a well-validated HPLC/MS/MS method.
Results: Following the triple therapy, the peak concentration (Cmax) and the area under the concentration-time curve from 0 h to 12 h (AUC0→12) of ilaprazole were significantly decreased, as compared with the single medication group (Cmax: 1025.0±319.6 vs. 1452.3±324.6 ng/mL; AUC0→12: 9777.7±3789.8 vs. 11363.1±3442.0 ng·h/mL). Similar changes were found for ilaprazole sulfone (Cmax: 5.9±0.5 vs. 9.3±1.7 ng/mL; AUC0→12: 201.4±32.1 vs. 277.1±66.2 ng·h/mL). The triple therapy significantly elevated the Cmax of clarithromycin (3161.5±702.2 vs. 2541.9±476.2 ng/mL).
Conclusion: The H pylori eradication therapy with clarithromycin, amoxicillin and ilaprazole may cause pharmacokinetic interactions that decrease the amount of ilaprazole and its metabolites and elevate that of clarithromycin.

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