Pharmacokinetics And Bioequivalence Of 0.5 Mg Lobeglitazone Tablets In Healthy Male Subjects

Objective: This study was conducted to evaluate the pharmacokinetics and bioequivalence of two formulations of Duvie (TM) (0.5-mg lobeglitazone sulfate). Materials and methods: This study was designed as an open-label, randomized, single-dose, crossover bioequivalence study in healthy male subjects. A total of 28 subjects were randomized into two groups: one group received the test drug, 0.5-mg Duvie (TM) tablets, which have formulations available on the global market; and the other group received the reference drug, the initially-approved 0.5-mg Duvie (TM) tablets. Plasma samples were collected for up to 48 horns after drug treatment and were analyzed for lobeglitazone using validated liquid chromatography-tandem mass spectrometry. Individual pharmacokinetic properties were determined by noncompartmental methods. Safety assessments were performed. Results: 28 subjects completed the study and were included in the pharmacokinetic analysis. The mean (standard deviation) values of AUC(last), for the test and reference formulations were 367.49 (157.92) and 362.40 (140.05) ngxh/mL, respectively. The mean (standard deviation) values of C-max for the test and reference formulations were 50.35 (6.94) and 49.29 (6.71) ng/mL, respectively. The 90% confidence intervals for AUC(last )and C-max were 0.9150 - 1.1088 and 0.9879 - 1.0561, respectively. All adverse events were mild. and there were no serious adverse events. Conclusion: This study suggests that the two lobeglitazone tablet formulations have similar exposure and absorption rates. Therefore, the newly-developed formulation of the 0.5mg Duvie (TM) tablet is expected to contribute to the treatment of patients with type 2 diabetes.