Dataset Information

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

ABSTRACT:

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 (C(max)) and the area under the concentration-time curve from 0 h to 12 h (AUC(0?12)) of ilaprazole were significantly decreased, as compared with the single medication group (C(max):1025.0±319.6 vs 1452.3±324.6 ng/mL; AUC(0?12): 9777.7±3789.8 vs 11363.1±3442.0 ng·h/mL). Similar changes were found for ilaprazole sulfone (C(max): 5.9±0.5 vs 9.3±1.7 ng/mL; AUC(0?12): 201.4±32.1 vs 277.1±66.2 ng·h/mL). The triple therapy significantly elevated the C(max) 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.

SUBMITTER: Cao S

PROVIDER: S-EPMC4011320 | biostudies-literature | 2012 Aug

REPOSITORIES: biostudies-literature

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Publications

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

Cao Shan S Zhou Gan G Ou-Yang Dong-sheng DS Wu Hui-zi HZ Xiao Kui K Chen Yao Y Guo Dong D Fan Lan L Tan Zhi-rong ZR Hu Hai-tang HT Qin Xiang-hong XH Zhou Hong-hao HH Zhang Wei W

Acta pharmacologica Sinica 20120723 8

<h4>Aim</h4>To investigate the drug interactions between ilaprazole, a new proton pump inhibitor, and clarithromycin following ilaprazole, clarithromycin and amoxicillin combination therapy.<h4>Methods</h4>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 c ...[more]

PMID: 22820908

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Project description:PURPOSE:Ilaprazole, the latest proton pump inhibitor, can be used with clarithromycin and amoxicillin as a triple therapy regimen for eradicating Helicobacter pylori. The aim of this study was to evaluate pharmacokinetic drug interactions and safety profiles after coadministration of clarithromycin, amoxicillin, and ilaprazole. METHODS:A randomised, open-label, one-way crossover, two parallel sequences study was conducted in 32 healthy subjects. In part 1, the subjects received a single dose of ilaprazole 10 mg in period 1 and clarithromycin 500 mg and amoxicillin 1000 mg twice daily for 6 days in period 2. In part 2, the subjects received clarithromycin 500 mg and amoxicillin 1000 mg once in period 1 and ilaprazole 10 mg twice daily for 6 days in period 2. In both sequences, the three drugs were coadministrated once on day 5 in period 2. Pharmacokinetic evaluations of ilaprazole (part 1), and clarithromycin and amoxicillin (part 2) were conducted. RESULTS:Twenty-eight subjects completed the study. For ilaprazole, the peak concentration (Cmax) slightly decreased from 479 (ilaprazole alone) to 446 ng/mL (triple therapy) [Geometric least square mean ratio (90% confidence interval), 0.93 (0.70-1.22)]. The area under the concentration-time curve from 0 h to the last measurable concentration (AUClast) slightly increased from 3301 to 3538 ?g·h/mL [1.07 (0.85-1.35)]. For clarithromycin, the Cmax slightly decreased from 1.87 to 1.72 ?g/mL [0.90 (0.70-1.15)], and AUClast slightly increased from 14.6 to 16.5 ?g·h/mL [1.09 (0.87-1.37)]. For amoxicillin, the Cmax slightly decreased from 9.37 to 8.14 ?g/mL [0.86 (0.74-1.01)], and AUClast slightly decreased from 27.9 to 26.7 ?g·h/mL [0.98 (0.83-1.16)]. These changes in the PK parameters of each drug were not statistically significant. CONCLUSIONS:The coadministration of ilaprazole, clarithromycin, and amoxicillin was tolerable and did not cause a significant PK drug interaction. Thus, a triple therapy regimen comprising ilaprazole, clarithromycin, and amoxicillin may be an option for the eradication of H. pylori. Clinicaltrials.gov number: NCT02998437.

Dataset Information

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

Aim

Methods

Results

Conclusion

Publications

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

Similar Datasets

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