Bioequivalence of a fixed-dose repaglinide/metformin combination tablet and equivalent doses of repaglinide and metformin tablets
| Autor: | Hea-Young Cho, Yoon Ho Choi, Lien Ngo, Sang-Ki Kim, Yong-Bok Lee |
|---|---|
| Rok vydání: | 2018 |
| Předmět: |
Adult
Male Cmax 02 engineering and technology Pharmacology Bioequivalence 030226 pharmacology & pharmacy law.invention 03 medical and health sciences 0302 clinical medicine Piperidines Randomized controlled trial law Humans Medicine Pharmacology (medical) Cross-Over Studies business.industry 021001 nanoscience & nanotechnology Repaglinide Crossover study Metformin Drug Combinations Therapeutic Equivalency Tolerability Drug Therapy Combination Carbamates 0210 nano-technology business Tablets Blood sampling medicine.drug |
| Zdroj: | Int. Journal of Clinical Pharmacology and Therapeutics. 56:292-300 |
| ISSN: | 0946-1965 |
| DOI: | 10.5414/cp203199 |
| Popis: | Objective This study was conducted to determine whether a fixed-dose combination (FDC) tablet of repaglinide/metformin (2/500 mg) is equivalent to coadministration of equivalent doses of individual (EDI) tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. Materials and methods This study was conducted as an open-label, randomized, single-dose, two-period, two-sequence crossover design in 50 healthy Korean male subjects who received an FDC tablet or EDI tablets. Plasma concentrations of repaglinide and metformin were determined for up to 24 hours using a validated UPLC-MS/MS method. Bioequivalence was assessed according to current guidelines issued by the U.S. Food and Drug Administration (FDA) and Korean legislation. Tolerability was also evaluated throughout the study via subject interview, vital signs, and blood sampling. Results Point estimates (90% CIs) for AUC0-t, AUC0-∞, and Cmax based on EDI tablets were 110.07 (102.25 - 118.49), 109.90 (101.70 - 118.39), and 112.60 (101.49 - 124.85), respectively, for repaglinide. They were 95.18 (89.62 - 101.05), 95.00 (89.74 - 100.65), and 98.44 (92.72 - 104.50), respectively, for metformin. These results satisfied the bioequivalence criteria of 80.00 - 125.00% proposed by the FDA and Korean legislation. Conclusion Results of pharmacokinetic analysis suggested that repaglinide and metformin in FDC tablets were bioequivalent to EDI tablets of repaglinide (2 mg) and metformin (500 mg) in healthy Korean male subjects. Both formulations appeared to be well tolerated. . |
| Databáze: | OpenAIRE |
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