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Bioequivalence evaluation of pioglitazone orally disintegrating tablet formulation

Shinzo Hiroi, Kumi Matsuno, Masashi Hirayama, Takaki Hayakawa,Norihito Yoshioka & Koji Kawakami

Three studies were performed in healthy Japanese men to compare the bioavailability of an orally disintegrating tablet formulation of pioglitazone (pioglitazone OD tablet) with pioglitazone commercial tablets, and to determine the extent of oral mucosal absorption. In two bioequivalence studies (both n = 64), pioglitazone OD tablets 30 mg were administered without (Study 1) or with water (Study 2), and bioavailability was compared with pioglitazone 30-mg commercial tablets administered with water. In Study 3 (n = 12), the oral mucosal absorption of pioglitazone OD tablet 30 mg was determined by keeping it in the mouth for 2 min. In each study, subjects were randomized into two groups, each receiving the two regimens in a two-sequence, two-period crossover design with a 6-day washout period. Blood samples were collected over 72 h to determine plasma concentrations of unchanged pioglitazone. The 90% confidence interval for the difference in AUC0–72 and Cmax of unchanged pioglitazone following administration of pioglitazone OD tablets with or without water and compared with pioglitazone commercial tablets given with water was always in the range of 0.80–1.25, indicating bioequivalence. Oral mucosal absorption was approximately 4%. In healthy Japanese men, the pioglitazone OD tablet was bioequivalent to pioglitazone commercial tablets, and had low oral mucosal absorption. The pioglitazone OD tablet is expected to provide an alternative treatment option for patients with Type 2 diabetes mellitus who have difficulty swallowing or are unable to swallow a conventional tablet.