Abstract

Objectives: The aim of this study was to compare the pharmacokinetic (PK) characteristics of evogliptin and metformin following the administration of 2 evogliptin/metformin extended-release (XR) 2.5/500 mg FDC tablets with the coadministration of separate evogliptin 5-mg and metformin XR 1,000-mg tablets (separate formulations). Methods: A randomized, two-period, two-sequence crossover study was conducted. Subjects were randomly assigned to receive 2 FDC tablets or the individual tablets, followed by a 14-day washout period and the administration of the alternate treatment. Blood samples were collected predose and up to 72 hours postdose for each period. PK parameters including C_max and AUC_last were calculated. The geometric mean ratios (GMRs) and the 90% confidence intervals (CIs) between FDC and the separate formulations were calculated for the C_max and AUC_last of evogliptin and metformin. Results: 33 subjects completed the study. The GMR (90% CI) values of C_max and AUC_last for evogliptin were 1.011 (0.959 – 1.066) and 1.010 (0.977 – 1.043), respectively. The GMR (90% CI) values of C_max and AUC_last for metformin were 0.892 (0.827 – 0.963) and 0.893 (0.841 – 0.947), respectively. There was no significant difference between the FDC and separate formulations regarding the occurrence of adverse events. All drug-related adverse events were considered to be mild and resolved without any treatment. Conclusions: Two FDC tablets of evogliptin/metformin XR 2.5/500 mg showed a similar PK profile to the separate formulations of evogliptin 5 mg and metformin XR 1,000 mg. All of the 90% CIs of GMR satisfied the regulatory bioequivalence criteria of 0.800 – 1.250.


Author Details

Authors

• Sumin Yoon¹
• Su-jin Rhee¹
• Sang-In Park¹
• Seo Hyun Yoon¹
• Joo-Youn Cho¹
• In-Jin Jang¹
• SeungHwan Lee¹,²
• Kyung-Sang Yu¹


Departments

• ¹ Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, and
• ² Clinical Trials Center, Seoul National University Biomedical Research Institute, Seoul, Republic of Korea

Address

Kyung-Sang Yu, MD, PhD

Department of Clinical Pharmacology and Therapeutics
Seoul National University College of Medicine and Hospital
101 Daehak-ro, Jongno-gu, Seoul 03080, Republic of Korea

Email: [email protected]

Log in for Subscribers

Citation