Pharmacokinetics and Bioequivalence of Single-Oral-Dose Linagliptin: A Randomized, 2-Period Crossover Trial in Chinese Healthy Subjects Under Fasting and Fed Conditions.

Abstract

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.