Pharmacokinetics and bioequivalence of two fenofibrate choline formulations in healthy subjects under fed and fasted condition

• Published in: International journal of clinical pharmacology and therapeutics Vol. 57; no. 4; pp. 217 - 228
• Main Authors: Park, Ji-Min, Chae, Soo-In, Noh, Young Su, Lee, Seung-Jun, Shim, Wang-Seob, Yoon, Ji-Min, Hwang, Se Jung, Lee, Kyung-Tae, Chung, Eun Kyoung
• Format: Journal Article
• Language: English
• Published: Germany Dustri - Verlag Dr. Karl Feistle GmbH & Co. KG 01-04-2019
• Subjects: Acids; Bioavailability; Bioequivalence; Cholesterol; Clinical medicine; Drug dosages; Drug therapy; Generic products; Low density lipoprotein; Pharmacokinetics; Pharmacy; Statins; Studies
• ISSN: 0946-1965
• DOI: 10.5414/CP203353

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.
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.
Overall, 37 and 35 individuals completed the fed and the fasting study, respectively, as planned. The estimated C
, AUC
, and AUC
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 C
, AUC
, and AUC
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, t
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).
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.
.