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Effects of food on the pharmacokinetics of gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination tablet in healthy male volunteers.
Int J Clin Pharmacol Ther. 2014 May; 52(5):381-91.IJ

Abstract

OBJECTIVES

For patient convenience, a gemigliptin/metformin sustainedrelease fixed-dose combination (FDC) tablet was developed. This study was conducted to investigate the effects of food on the pharmacokinetic (PK) profile of the FDC tablets.

MATERIALS AND METHODS

This was an open-label, randomized, single dose, 2-period, 2-sequence crossover study in 24 healthy male volunteers. The FDC tablets (25/500 mg × 2 tablets) were administered in high-fat fed and fasted states on separate occasions, and each subject was randomly allocated to each sequence with a 7-day washout period. PK blood samplings were conducted from predose to 48 hours after dosing. Tolerability assessments were performed throughout the study.

RESULTS

Nine adverse events (AEs) of mild intensity were reported from 8 subjects after study drug administration, and the AE frequency was similar between treatments. No serious AEs were reported. The PK parameters of gemigliptin and metformin were compared between fasting and fed states. For gemigliptin, the geometric mean ratios (GMRs) (fed : fasted state) of the Cmax and AUClast were 0.886 (90% confidence interval (CI) 0.781 - 1.006) and 1.021 (90% CI 0.949 - 1.099), respectively. For metformin, the GMRs of the Cmax and AUClast were 0.811 (90% CI 0.712 - 0.923) and 1.144 (90% CI 1.013 - 1.291), respectively. A prolonged tmax for metformin was observed. These results are similar to the effects of food on each component.

CONCLUSION

The FDC tablet may have a similar PK profile as that of individual drugs and is generally tolerable when administered with food. These results indicate that the FDC tablet can be administered in the same dosing regimen as each component, especially that of metformin sustained-release.

Authors

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Pub Type(s)

Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24495314

Citation

Choi, Hee Youn, et al. "Effects of Food On the Pharmacokinetics of Gemigliptin/metformin Sustained-release 50/1,000 Mg (25/500 Mg X 2 Tablets) Fixeddose Combination Tablet in Healthy Male Volunteers." International Journal of Clinical Pharmacology and Therapeutics, vol. 52, no. 5, 2014, pp. 381-91.
Choi HY, Noh YH, Kim YH, et al. Effects of food on the pharmacokinetics of gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination tablet in healthy male volunteers. Int J Clin Pharmacol Ther. 2014;52(5):381-91.
Choi, H. Y., Noh, Y. H., Kim, Y. H., Kim, M. J., Lee, S. H., Kim, J. A., Kim, B., Lim, H. S., & Bae, K. S. (2014). Effects of food on the pharmacokinetics of gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination tablet in healthy male volunteers. International Journal of Clinical Pharmacology and Therapeutics, 52(5), 381-91. https://doi.org/10.5414/CP202038
Choi HY, et al. Effects of Food On the Pharmacokinetics of Gemigliptin/metformin Sustained-release 50/1,000 Mg (25/500 Mg X 2 Tablets) Fixeddose Combination Tablet in Healthy Male Volunteers. Int J Clin Pharmacol Ther. 2014;52(5):381-91. PubMed PMID: 24495314.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Effects of food on the pharmacokinetics of gemigliptin/metformin sustained-release 50/1,000 mg (25/500 mg x 2 tablets) fixeddose combination tablet in healthy male volunteers. AU - Choi,Hee Youn, AU - Noh,Yook-Hwan, AU - Kim,Yo Han, AU - Kim,Mi Jo, AU - Lee,Shi Hyang, AU - Kim,Jeong-Ae, AU - Kim,Bogyeong, AU - Lim,Hyeong-Seok, AU - Bae,Kyun-Seop, PY - 2014/04/29/accepted PY - 2014/2/6/entrez PY - 2014/2/6/pubmed PY - 2014/6/18/medline SP - 381 EP - 91 JF - International journal of clinical pharmacology and therapeutics JO - Int J Clin Pharmacol Ther VL - 52 IS - 5 N2 - OBJECTIVES: For patient convenience, a gemigliptin/metformin sustainedrelease fixed-dose combination (FDC) tablet was developed. This study was conducted to investigate the effects of food on the pharmacokinetic (PK) profile of the FDC tablets. MATERIALS AND METHODS: This was an open-label, randomized, single dose, 2-period, 2-sequence crossover study in 24 healthy male volunteers. The FDC tablets (25/500 mg × 2 tablets) were administered in high-fat fed and fasted states on separate occasions, and each subject was randomly allocated to each sequence with a 7-day washout period. PK blood samplings were conducted from predose to 48 hours after dosing. Tolerability assessments were performed throughout the study. RESULTS: Nine adverse events (AEs) of mild intensity were reported from 8 subjects after study drug administration, and the AE frequency was similar between treatments. No serious AEs were reported. The PK parameters of gemigliptin and metformin were compared between fasting and fed states. For gemigliptin, the geometric mean ratios (GMRs) (fed : fasted state) of the Cmax and AUClast were 0.886 (90% confidence interval (CI) 0.781 - 1.006) and 1.021 (90% CI 0.949 - 1.099), respectively. For metformin, the GMRs of the Cmax and AUClast were 0.811 (90% CI 0.712 - 0.923) and 1.144 (90% CI 1.013 - 1.291), respectively. A prolonged tmax for metformin was observed. These results are similar to the effects of food on each component. CONCLUSION: The FDC tablet may have a similar PK profile as that of individual drugs and is generally tolerable when administered with food. These results indicate that the FDC tablet can be administered in the same dosing regimen as each component, especially that of metformin sustained-release. SN - 0946-1965 UR - https://www.unboundmedicine.com/medline/citation/24495314/Effects_of_food_on_the_pharmacokinetics_of_gemigliptin/metformin_sustained_release_50/1000_mg__25/500_mg_x_2_tablets__fixeddose_combination_tablet_in_healthy_male_volunteers_ L2 - http://www.dustri.com/nc/journals-in-english?artId=11244 DB - PRIME DP - Unbound Medicine ER -