Pharmacokinetics of Single and Multiple Oral Administration of a Self‐emulsifying Formulation of Highly Purified Eicosapentaenoic Acid Ethyl Ester (MND‐2119) Compared With the Nonself‐emulsifying Formulation in Healthy Male Subjects

• Published in: Clinical pharmacology in drug development Vol. 12; no. 1; pp. 107 - 115
• Main Authors: Mori, Takuya, Murasaki, Kagari, Yokoyama, Yuichi
• Format: Journal Article
• Language: English
• Published: United States Wiley Subscription Services, Inc 01.01.2023
• Subjects: absorption; Administration, Oral; Adult; Biological Availability; Eicosapentaenoic Acid; eicosapentaenoic acid ethyl ester; Fasting; Humans; Male; MND‐2119; n‐3 fatty acid; Pharmacokinetics; self‐emulsifying delivery system; pharmacokinetics; MND-2119; self-emulsifying delivery system; absorption; eicosapentaenoic acid ethyl ester; n-3 fatty acid
• ISSN: 2160-763X; 2160-7648; 2160-7648
• DOI: 10.1002/cpdd.1177

MND‐2119 is a self‐emulsifying formulation of highly purified eicosapentaenoic acid ethyl ester (EPA‐E) designed to be administered once daily due to improved absorption compared with the nonself‐emulsifying formulation. In these studies, MND‐2119 was administered to healthy adult males in single or multiple doses. In the single administration study, MND‐2119 (0.5–4 g) was administered under fed and fasted conditions to evaluate MND‐2119 pharmacokinetics and safety under these conditions. This study showed that Cmax and AUC0‐72h of plasma EPA concentration after single administration were higher under fed conditions than under fasted conditions, for all doses. In the multiple administration study, subjects received either MND‐2119 (0.5–4 g) immediately after breakfast or EPA‐E (0.9 g) immediately after breakfast and dinner for 11 days to compare pharmacokinetics and safety of MND‐2119 to EPA‐E. In this study, the rate of rise in Cmin of the plasma EPA concentration with MND‐2119 decreased from days 6 to 8 after administration and was thought to have reached a steady state on day 11. The mean Css,max of MND‐2119 administered as 1 g once daily, and the mean Css,min and the mean AUCss,0‐24h of MND‐2119 administered as 2 g once daily were higher than those of EPA‐E administered as 0.9 g twice daily. No safety‐related issues occurred in either study. These results suggest that MND‐2119 administered once daily may achieve equivalent or higher plasma EPA concentrations compared to the nonself‐emulsifying formulation administered twice daily.