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Bioavailability Section

Pharmacokinetic comparison of gemigliptin 50 mg and metformin 500 mg as a fixed-dose combination and loose combination 

Sang Won Lee, Sang-In Park, SeungHwan Lee, Jae-Yong Chung, and Kyung-Sang Yu

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Volume 57 (2019) p. 117 - 124

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 57 – No. 2/2019 (117-124)

Pharmacokinetic comparison of gemigliptin 50 mg and metformin 500 mg as a fixed-dose combination and loose combination 

Sang Won Lee¹, Sang-In Park¹, SeungHwan Lee¹, Jae-Yong Chung², and Kyung-Sang Yu¹

¹Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, ²Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Bundang Hospital, Seongnam, Korea
Background: Metformin and dipeptidyl peptidase-4 (DPP-IV) inhibitors are commonly combined to treat patients with diabetes mellitus (DM). A new fixed-dose combination (FDC) drug containing gemigliptin, a DPP-IV inhibitor, and sustained-release metformin has been developed. This study aimed to compare the PKs and tolerability of FDC versus loose combination of gemigliptin 50 mg and metformin 500 mg. Materials and methods: A randomized, open-label, two-treatment, two-period, two-sequence, crossover study was conducted in 28 healthy subjects, who received a single oral dose of an FDC tablet of gemigliptin (50 mg) and sustained-release metformin (500 mg) or were coadministered gemigliptin (50 mg) and extended-release metformin (500 mg) with a 1-week washout. Serial blood samples were collected up to 48 hours after study drug administration, and the plasma concentrations of gemigliptin, LC15-0636 (active metabolite of gemigliptin), and metformin were determined using a validated LC-MS/MS method. Pharmacokinetic parameters were derived using a noncompartmental method. Safety and tolerability were evaluated based on vital signs, adverse events, clinical laboratory tests, and electrocardiography. Results: The concentration-time profiles of gemigliptin and metformin were similar when they were administered as FDC or were coadministered. The geometric mean ratio (GMR) and its 90% CIs of Cmax for gemigliptin, LC15-0636, and metformin were 0.93 (0.85 – 1.02), 1.00 (0.94 – 1.06), and 1.03 (0.98 – 1.09), respectively. The corresponding values of AUClast were 0.97 (0.93 – 1.01), 1.00 (0.97 – 1.04), and 1.00 (0.95 – 1.05), respectively. There were no clinically meaningful differences in safety and tolerability. Conclusion: When comparing the AUClast and Cmax of gemigliptin, LC15-0636, and metformin, the 90% CIs were all within the range of 0.8 – 1.25, which is the commonly accepted range for evaluating bioequivalence.Correspondence to:
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, Korea 
Email: [email protected]

Original Research

Multiple-dose pharmacokinetics and safety of amoxicillin/clavulanate in healthy elderly subjects 

Sang Won Lee, Yewon Choi, Kyungho Jang, Seo Hyun Yoon, and Jae-Yong Chung

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Volume 58 (2020) p. 634 - 641

Abstract

International Journal of Clinical Pharmacology and Therapeutics, Vol. 58 – No. 11/2020 (634-641)

Multiple-dose pharmacokinetics and safety of amoxicillin/clavulanate in healthy elderly subjects 

Sang Won Lee¹, Yewon Choi², Kyungho Jang³, Seo Hyun Yoon¹, and Jae-Yong Chung⁴

¹Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Hospital, Seoul, Republic of Korea, ²Genosco Inc., Cambridge, MA, USA, ³Center for Clinical Pharmacology, Biomedical Research Institute, Chonbuk National University Hospital, Jeonju, Jeonbuk, and ⁴Department of Clinical Pharmacology and Therapeutics, Seoul National University College of Medicine and Bundang Hospital, Seongnam, Republic of Korea
Background: Amoxicillin/clavulanate is a widely used oral formulation of penicillin combined with a β-lactamase inhibitor. When using amoxicillin/clavulanate in the elderly, the risk of adverse drug reaction may be greater. This study aimed to evaluate the pharmacokinetics (PKs) and safety of multiple-dose amoxicillin/clavulanate administration in healthy elderly subjects and to compare the observed PK profiles with those in healthy younger adults. An open-label, one-sequence, multiple administration study was conducted in 16 healthy elderly subjects.
Materials and methods: Subjects orally received amoxicillin and clavulanate 750/187.5 twice daily for 9 days. For PK analysis, serial blood samples were collected up to 12 hours after the last administration of amoxicillin/clavulanate. The demographic and PK data of this study were compared to those of healthy young adults from a separate study with a similar design. Safety assessments including clinical laboratory tests, physical examination, vital signs, and adverse event (AE) monitoring were performed throughout the study.
Results: All AEs were mild, and no serious AEs were reported in this study. The systemic exposure of amoxicillin and clavulanate was ~ 90% and 60% higher, respectively, in the elderly subjects than in the younger subjects. However, the time required to reach maximum concentration at steady state and the elimination half-life were similar in the two age groups.
Conclusion: Although multiple administration of amoxicillin/clavulanate 750/187.5 mg was safe and well-tolerated, the systemic exposure of amoxicillin and clavulanate was higher in elderly subjects than in younger subjects.Correspondence to:
Jae-Yong Chung, MD, PhD 
Department of Clinical Pharmacology and Therapeutics
Seoul National University College of Medicine  and Bundang Hospital
Seongnam, Republic  of Korea
Email: [email protected]

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