LAUSR

The bioequivalence of the reference and test linagliptin formulations was assessed in healthy Chinese subjects under fasting and fed conditions. The study was designed as a single‐dose, randomized, open‐label, 2‐period crossover study with a 35‐day washout period between 2 administrations. Forty‐eight healthy subjects received 5 mg of test and reference linagliptin formulation orally under fasting condition. The geometric mean of the maximum observed linagliptin concentration (Cmax) for the test formulation was 4.9 ng/mL (reference, 5.0 ng/mL), the area under the plasma concentration–time curve from 0 to 72 hours (AUC0‐72) was 154.7 ng · h/mL (reference, 157.4 ng · h/mL). Thirty‐six subjects received 5 mg of test and reference linagliptin formulation orally under fed conditions. The geometric mean of Cmax for the test linagliptin formulation was 2.8 ng/mL (reference, 2.8 ng/mL), AUC0‐72 was 133.5 ng · h/mL (reference, 136.6 ng · h/mL). The 90%CIs for the test/reference ratio for Cmax and AUC0‐72 met the bioequivalence criteria (80%‐125%). The test and reference formulations of linagliptin were well tolerated and bioequivalent under fasting and fed conditions.