PurposeIlaprazole, 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.MethodsA 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.ResultsTwenty-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 μg·h/mL [1.07 (0.85–1.35)]. For clarithromycin, the Cmax slightly decreased from 1.87 to 1.72 μg/mL [0.90 (0.70–1.15)], and AUClast slightly increased from 14.6 to 16.5 μg·h/mL [1.09 (0.87–1.37)]. For amoxicillin, the Cmax slightly decreased from 9.37 to 8.14 μg/mL [0.86 (0.74–1.01)], and AUClast slightly decreased from 27.9 to 26.7 μg·h/mL [0.98 (0.83–1.16)]. These changes in the PK parameters of each drug were not statistically significant.ConclusionsThe 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.Electronic supplementary materialThe online version of this article (10.1007/s00228-018-2489-2) contains supplementary material, which is available to authorized users.
In this open‐label, single‐dose, parallel‐group study, we compared the pharmacokinetic profile and safety of lobeglitazone, a thiazolidinedione acting as an agonist for peroxisome proliferator‐activated receptors, in patients with hepatic impairment (HI) and healthy matched controls for age, sex, and body weight. After a single oral dose of lobeglitazone (0.5 mg), the lobeglitazone (parent drug) and M7 (major metabolite) plasma concentrations and pharmacokinetic parameters were analyzed and compared between the HI patient groups and healthy matched control groups. The geometric mean ratio (GMR; 90% confidence interval [CI]) for maximum concentration (Cmax) and area under the plasma concentration–time curve from time 0 extrapolated to infinity (AUCinf) of lobeglitazone was 1.06 (0.90‐1.24) and 1.07 (0.82‐1.40), respectively, for mild HI vs control A. The GMR (90%CI) of Cmax and AUCinf was 0.70 (0.56‐0.88) and 1.00 (0.72‐1.37), respectively, for moderate HI vs control B. For M7, the GMR (90%CI) of Cmax and AUCinf was 1.09 (0.75‐1.57) and 1.18 (0.71‐1.97), respectively, for mild HI vs control A and 1.50 (0.95‐2.38) and 1.79 (1.06‐3.04), respectively, for moderate HI vs control B. Notable adverse events or tolerability issues were not observed. Lobeglitazone may be safely used in patients with mild or moderate HI without dose adjustment.
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