Abstract
Objective: The objective of this study was to evaluate the pharmacokinetics and bioequivalence of two formulations (the original capsule (“reference”) and the new tablet (“test”) formulations) of 135-mg choline fenofibrate under fed and fasted conditions. Materials and methods: This was an open-label, randomized, single-dose, crossover bioequivalence study in healthy Korean males. A total of 40 individuals were separately enrolled in the high-fat fed and the fasting study, respectively, and were randomized in a 1:1 ratio into two sequences. Serial blood samples were collected over 72 hours after drug administration. Plasma concentrations of fenofibric acid were determined by a validated LC-MS/MS method. Pharmacokinetic (PK) parameters were estimated using noncompartmental methods. Results: Overall, 37 and 35 individuals completed the fed and the fasting study, respectively, as planned. The estimated Cmax, AUC0–∞, and AUC0–last were comparable between the test and the reference formulations in both fed and fasting studies (p > 0.05). The 90% confidence intervals for the geometric mean ratios of Cmax, AUC0–∞, and AUC0–last were 0.92 – 1.06, 0.95 – 1.01, and 0.95 – 1.01 in the fed study; and 0.94 – 1.12, 0.94 – 1.00, and 0.94 – 1.00 in the fasting study, respectively. For both formulations, tmax was significantly prolonged under fed condition compared to fasting condition (p < 0.0001); all other PK parameters were comparable between the fed and the fasting studies (p > 0.05). Conclusion: The reference and the test formulations of 135 mg choline fenofibrate show comparable pharmacokinetic profiles of fenofibric acid under both fed and fasted conditions and are considered bioequivalent.
Original language | English |
---|---|
Pages (from-to) | 217-228 |
Number of pages | 12 |
Journal | International Journal of Clinical Pharmacology and Therapeutics |
Volume | 57 |
Issue number | 4 |
DOIs | |
Publication status | Published - 2019 |
Bibliographical note
Publisher Copyright:©2019 Dustri-Verlag Dr. K. Feistle
Keywords
- Bioequivalence
- Dyslipidemia
- Fenofibrate
- Pharmacokinetics