Randomized Pharmacokinetic Crossover Study Comparing 2 Curcumin Preparations in Plasma and Rectal Tissue of Healthy Human Volunteers

• Published in: Journal of clinical pharmacology Vol. 57; no. 2; p. 185
• Main Authors: Asher, Gary N, Xie, Ying, Moaddel, Ruin, Sanghvi, Mitesh, Dossou, Katina S S, Kashuba, Angela D M, Sandler, Robert S, Hawke, Roy L
• Format: Journal Article
• Language: English
• Published: England 01.02.2017
• Subjects: Adolescent; Adult; Aged; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - classification; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Area Under Curve; Biological Availability; Biotransformation; Cross-Over Studies; Curcumin - administration & dosage; Curcumin - analogs & derivatives; Curcumin - classification; Curcumin - metabolism; Curcumin - pharmacokinetics; Female; Glucuronides; Healthy Volunteers; Humans; Intestinal Absorption; Male; Middle Aged; Rectum - metabolism; Young Adult; clinical trial; steady state; pharmacokinetics; human; curcumin
• ISSN: 1552-4604
• DOI: 10.1002/jcph.806

Curcumin is poorly absorbed, which is interest in new preparations. However, little is known about variations in its pharmacokinetics and tissue bioavailability between formulations. In this randomized, crossover study we evaluated the relationship between steady-state plasma and rectal tissue curcuminoid concentrations using standard and phosphatidylcholine curcumin extracts. There was no difference in the geometric mean plasma AUCs when adjusted for the 10-fold difference in curcumin dose between the 2 formulations. Phosphatidylcholine curcumin extract yielded only 20% to 30% plasma demethoxycurcumin and bisdemethoxycurcumin conjugates compared to standard extract, yet yielded 20-fold greater hexahydrocurcumin. When adjusting for curcumin dose, tissue curcumin concentrations were 5-fold greater for the phosphatidylcholine extract. Improvements in curcuminoid absorption due to phosphatidylcholine are not uniform across the curcuminoids. Furthermore, curcuminoid exposures in the intestinal mucosa are most likely due to luminal exposure rather than to plasma disposition. Finally, once-daily dosing is sufficient to maintain detectable curcuminoids at steady state in both plasma and rectal tissues.