Journal
JOURNAL OF PHARMACY AND PHARMACOLOGY
Volume 64, Issue 3, Pages 337-343Publisher
WILEY-BLACKWELL
DOI: 10.1111/j.2042-7158.2011.01411.x
Keywords
food effect; iptakalim; pharmacokinetics; phase I; safety
Categories
Funding
- major national science and technology special projects for new drug [2008ZX09101-006]
- major projects of Beijing science and technology [D0204003040721]
- national technical innovation projects [02C26213200052]
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Objectives To investigate the safety, pharmacokinetics and food effect of iptakalim in healthy adult Han Chinese volunteers. Methods Study 1 was a randomized open-label, Latin square designed, single-dose, three-period, self-control crossover study. Six men and six women received 5, 10 and 20 mg of iptakalim orally. Study 2 was a randomized, open-label, single-dose, two-period, self-control crossover study. Ten men were included and each subject received 5 mg iptakalim orally, fasting and nonfasting. Key findings No adverse effects were reported and no clinically meaningful changes in vital signs were found. Cmax, AUC(0-t) and AUC(0-infinity) were proportional over the dose levels of 5, 10 and 20 mg. Tmax, t1/2 and CL/F were similarly independent of dose level. In the 5 mg and 20 mg group, the Cmax, AUC0-t and AUC(0-infinity) in women were significantly higher than in men, although they showed no difference after correction by mg/kg doses in the 5 mg group. At the 5-mg dose level, no significant difference in pharmacokinetics was found in nonfasting and fasting subjects. Conclusions Single-dose pharmacokinetics of iptakalim showed dose proportionality over the dose levels of 5-20 mg. The pharmacokinetics showed gender differences in the 5 and 20 mg groups. Food had almost no impact on the pharmacokinetics at the 5 mg level.
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