2009 (v.17 no.1)
The Journal of Korean Society for Clinical Pharmacology and Therapeutics
Korean Society for Clinical Pharmacology and Therapeutics
Pharmacokinetics of Irsogladin Maleate in Healthy Korean Volunteers
J Korean Soc Clin Pharmacol Ther | v.17, no.1, pp.35-43, Jun, 2009
Background: Irsogladin maleate, increasing gastric
mucosal blood flow and cAMP in mucosal epithelial cells, is being marketed for
the treatment of gastric ulcer and gastritis. The object of this study was to
evaluate the pharmacokinetic characteristics and safety profiles of irsogladin
maleate in Koreans.
Methods: An open-label, dose-escalation, parallel group study was conducted in 28 healthy male Korean volunteers. Irsogladin maleate was administered as a single dose of 4 mg (n=16), 8 mg (n=6) or 16 mg (n=6). Serial blood samples for pharmacokinetic analysis were taken over 504 h. Plasma concentration of irsogladin was measured by high performance liquid chromatography-tandem mass spectrometry (LC-MS/MS). Pharmacokinetic parameters were determined using noncompartmental methods. Laboratory tests, ECGs, vital signs and physical examinations were performed for clinical safety evaluation.
Results: Maximum observed irsogladin plasma concentration (Cmax) (mean ± SD) of 4 mg, 8 mg and 16 mg dosage group were 82.9 ± 12.5 μg /L, 161.4 ± 25.9 μg /L and 292.6 ± 51.2 μg /L, respectively. Area under the plasma concentration versus time curve from dosing to the last quantifiable concentration (AUClast) of three dosage groups were 12694.4 ± 2906.2 μg *h/L, 24970.0 ± 5253.8 μg *h/L, 47125.3 ± 8676.7 μg *h/L, respectively. Apparent clearance (0.30 ± 0.07L/h, 0.31 ± 0.10 L/h, 0.31 ±0.06 L/h, respectively) was unaffected by dosage. The 95% CI of slope of Dose-Cmax and Dose-AUClast linear regression were 15.4-19.6 and 2485.2-3262.0. All adverse events reported were mild and no clinically significant abnormalities of safety evaluation were observed.
Conclusions: The pharmacokinetic characteristics of Irsogladin maleate after single dose administration was explored in healthy Korean volunteers. Irsogladin maleate displayed linear plasma pharmacokinetics over the dose range 4-16 mg. Irsogladin maleate was well tolerated after single dose administration in Koreans.