Ingestion of 150 to 900mg doses of naringenin is safe in healthy adults, and serum concentrations are proportional to the dose administered. - GreenMedInfo Summary

AIMS: This study evaluated the safety and pharmacokinetics of naringenin in healthy adults, consuming a whole orange (Citrus Sinensis) extract.

METHODS: In a single ascending dose randomized crossover trial, 18 adults ingested 150mg (NAR150), 300mg (NAR300), 600mg (NAR600), and 900mg (NAR900) doses of naringenin or placebo. Each dose or placebo was followed by a wash-out period of at least one week. Blood safety markers were evaluated pre-dose and 24 hours post-dose. Adverse events were recorded. Serum naringenin concentrations were measured before and over 24 hours following ingestion of placebo, NAR150, and NAR600. Four and 24-hour serum measurements were obtained after placebo, NAR300, and NAR900 ingestion. Data were analyzed using a mixed effects linear model.

RESULTS: There were no relevant adverse events or changes in blood safety markers following ingestion of all naringenin doses. The pharmacokinetic parameters were: Maximal concentration: 15.76±7.88μM (NAR150) and 48.45±7.88μM (NAR600); Time to peak: 3.17±0.74h (NAR150) and 2.41±0.74h (NAR600); Area under the 24-hour concentration-time curve: 67.61±24.36μM×h (NAR150) and 199.06±24.36μM×h (NAR600); and Apparent oral clearance: 10.21±2.34L/h (NAR150) and 13.70±2.34L/h (NAR 600). Naringenin half-life was 3.0h (NAR150) and 2.65h (NAR600). After NAR300 ingestion, serum concentrations were 10.67±5.74μM (4h) and 0.35±0.30μM (24h). After NAR900 ingestion, serum concentrations were 43.11±5.26μM (4h) and 0.24±0.30μM (24h).

CONCLUSIONS: Ingestion of 150 to 900mg doses of naringenin is safe in healthy adults, and serum concentrations are proportional to the dose administered. Since naringenin (8μM) is effective in primary human adipocytes, ingestion of 300mg naringenin twice/day will likely elicit a physiologic effect. This article is protected by copyright. All rights reserved.