Pharmacokinetics and bioequivalence of 0.5 mg lobeglitazone tablets in healthy male subjects

• Published in: International journal of clinical pharmacology and therapeutics Vol. 56; no. 9; pp. 426 - 433
• Main Authors: Lee, So Jin, Kim, Min-Gul, Park, Shin-Jung, Jeon, Ji-Young
• Format: Journal Article
• Language: English
• Published: Germany Dustri - Verlag Dr. Karl Feistle GmbH & Co. KG 01.09.2018
• Subjects: Administration, Oral; Adult; Area Under Curve; Bioequivalence; Chromatography, High Pressure Liquid; Cross-Over Studies; Drug Compounding; Half-Life; Healthy Volunteers; Humans; Hypoglycemic Agents - administration & dosage; Hypoglycemic Agents - blood; Hypoglycemic Agents - pharmacokinetics; Male; Metabolic Clearance Rate; Models, Biological; Pharmacokinetics; Pyrimidines - administration & dosage; Pyrimidines - blood; Pyrimidines - pharmacokinetics; Republic of Korea; Spectrometry, Mass, Electrospray Ionization; Tablets; Tandem Mass Spectrometry; Therapeutic Equivalency; Thiazolidinediones - administration & dosage; Thiazolidinediones - blood; Thiazolidinediones - pharmacokinetics; Young Adult; Republic of Korea
• ISSN: 0946-1965
• DOI: 10.5414/CP203134

This study was conducted to evaluate the pharmacokinetics and bioequivalence of two formulations of -DuvieTM (0.5-mg lobeglitazone sulfate). 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 DuvieTM tablets, which have formulations available on the global market; and the other group received the reference drug, the initially-approved 0.5-mg DuvieTM tablets. Plasma samples were collected for up to 48 hours 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. 28 subjects completed the study and were included in the pharmacokinetic analysis. The mean (standard deviation) values of -AUClast for the test and reference formulations were 367.49 (157.92) and 362.40 (140.05) ng×h/mL, respectively. The mean (standard deviation) values of Cmax for the test and reference formulations were 50.35 (6.94) and 49.29 (6.71) ng/mL, respectively. The 90% confidence intervals for AUClast and Cmax were 0.9150 - 1.1088 and 0.9879 - 1.0561, respectively. All adverse events were mild, and there were no serious adverse events. This study suggests that the two lobeglitazone tablet formulations have similar exposure and absorption rates. Therefore, the newly-developed formulation of the 0.5-mg DuvieTM tablet is expected to contribute to the treatment of patients with type 2 diabetes.
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