Pharmacokinetics of a Single Intake of a Self-Emulsifying Drug Delivery System Containing the Triglyceride Form of DHA: A Randomized, Double-Blinded, Crossover Study.

Abstract

BACKGROUND

The health benefits of n-3 (ω-3) PUFAs are well studied. A self-emulsifying drug delivery system (SEDDS) is expected to improve n-3 PUFA absorption.

OBJECTIVES

The present study investigated how a single ingestion of a new SEDDS containing the triglyceride (TG) form of DHA (22:6n-3) (DHA/TG) would affect the plasma DHA concentration in healthy participants.

METHODS

Fifteen healthy participants (age: 20-65 y; BMI: 18.5-25 kg/m(2)) were enrolled in this randomized, double-blind, crossover study. Participants in a fasting state consumed a single dose of 920 mg DHA and 80 mg epa (20:5n-3) in SEDDS soft capsules (SEDDS capsule) or non-emulsifying soft capsules (control capsule). Blood was sampled at 0, 1.5, 3, 5, 7, and 9 h after dosing. The primary outcome was the baseline-adjusted incremental AUC (iAUC) for plasma DHA concentrations (iAUC_DHA).

RESULTS

The iAUC_DHA was significantly higher for the SEDDS capsule (147.9 ± 15.8 µg·h/mL) than for the control capsule (106.4 ± 18.1 µg·h/mL) (P = 0.018;

SEDDS/control ratio

1.4:1). However, plasma epa concentrations and iAUC values did not significantly differ between the SEDDS and control capsules. Cmax was significantly higher with the SEDDS capsule for both DHA (P = 0.019) and epa (P = 0.012) than with the control capsule.

CONCLUSIONS

These results suggest that a SEDDS improves the absorbability of DHA/TG in healthy participants. This indicates that SEDDS capsules would be beneficial for efficient ingestion of DHA.

This trial was registered at https

//www.umin.ac.jp/ctr/ as UMIN000044188.