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薬理と治療
Abstract
Bioequivalence of orally disintegrating(OD)tolvaptan tablets to conventional ones at 15 and 30 mg was evaluated in an open-label, three-period, three-way crossover trial. Total 84 healthy adult male volunteers were divided into two cohorts and randomized to three groups: conventional tablet(CT)first, OD tablet with water (ODT+W)first, and OD tablet without water(ODT-W)first. 90% confidence intervals(CIs)for geometric mean ratios(GMRs)of AUCt and Cmax of tolvaptan for 15 mg of ODT-W to those for 15 mg of CT were log(0.95)―log(1.06)and log(1.07)―log(1.23), respectively. Those for the GMRs of the AUCt and Cmax of tolvaptan for 15 mg of ODT+W to those for 15 mg of CT were log(0.94)―log (1.05)and log(0.89)―log(1.02), respectively. Those for the GMRs of the AUCt and Cmax of tolvaptan for 30 mg of ODT-W to those for 30 mg of CT were log (0.97)―log(1.06)and log(1.04)―log(1.17), respectively. Those for the GMRs of the AUCt and Cmax of tolvaptan for 30 mg of ODT+W to those for 30 mg of CT were log(0.95)―log(1.05)and log(0.94)―log(1.06), respectively. These results were within the range of log(0.80)―log(1.25)specified for bioequivalence, indicating that the two formulations were bioequivalent. All observed adverse events were mild and resolved spontaneously. There were no consistent trends indicating clinical concerns in clinical laboratory tests, vital signs, body weight, or 12-lead electrocardiogram.
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