Pharmacokinetics and Food Effect Between a 100‐mg Sustained‐Release Tablet and a 50‐mg Immediate‐Release Tablet of Vildagliptin in Healthy Subjects

Abstract

AbstractVildagliptin is one of the dipeptidyl peptidase‐4 inhibitors. This study aimed to compare vildagliptin exposure between 50‐mg immediate‐release (IR) and 100‐mg new sustained‐release (SR) tablets, and evaluate the food effect on the pharmacokinetics (PKs) of vildagliptin. A randomized, open‐label, 3‐period, 3‐treatment, 6‐sequence crossover study was conducted on healthy subjects. During each period, subjects received the SR tablet either in the fasted (T1) or high‐fat fed (T2) state once a day, or IR tablets administered twice a day in the fasted state (R). Blood samples for PK analysis were obtained serially up to 24 hours after dosing. Thirty‐four subjects completed the study. The geometric mean ratios for the Cmax and AUC0‐24h of T1 to R were 1.15 and 0.89, respectively. The corresponding values of T2 to T1 were 0.94 and 1.07, respectively. Vildagliptin exposure over 24 hours was similar between the SR and IR tablets. In addition, the PK profiles of the SR tablets were not altered by food. The SR tablets can be administered without a food effect and be an alternative option to IR tablets.