title: Randomized Pharmacokinetic Crossover Study Comparing 2 Curcumin Preparations in Plasma and Rectal Tissue of Healthy Human Volunteers.
abstract: 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.
authors: Department of Family Medicine, University of North Carolina School of Medicine, Chapel Hill, NC, USA.
authors: Gary N
authors: GN
authors: Asher
authors: State Key Laboratory of Quality Research in Chinese Medicine, Macau University of Science and Technology, Taipa, Macau.
authors: Ying
authors: Y
authors: Xie
authors: Laboratory of Clinical Investigation, Division of Intramural Research Programs, National Institute on Aging, National Institutes of Health, Baltimore, MD, USA.
authors: Ruin
authors: R
authors: Moaddel
authors: Laboratory of Clinical Investigation, Division of Intramural Research Programs, National Institute on Aging, National Institutes of Health, Baltimore, MD, USA.
authors: Mitesh
authors: M
authors: Sanghvi
authors: Laboratory of Clinical Investigation, Division of Intramural Research Programs, National Institute on Aging, National Institutes of Health, Baltimore, MD, USA.
authors: Katina S S
authors: KS
authors: Dossou
authors: Division of Pharmacotherapy and Experimental Therapeutics, University of North Carolina Eshelman School of Pharmacy, Chapel Hill, NC, USA.
authors: Angela D M
authors: AD
authors: Kashuba
authors: Division of Gastroenterology and Hepatology, University of North Carolina School of Medicine, Chapel Hill, NC, USA.
authors: Robert S
authors: RS
authors: Sandler
authors: Division of Pharmacotherapy and Experimental Therapeutics, University of North Carolina Eshelman School of Pharmacy, Chapel Hill, NC, USA.
authors: Roy L
authors: RL
authors: Hawke
mesh_terms: D000293:Adolescent; D000328:Adult; D000368:Aged; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000145:classification / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D001711:Biotransformation; D018592:Cross-Over Studies; D003474:Curcumin / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000145:classification / Q000378:metabolism / Q000493:pharmacokinetics*; D036381:Diarylheptanoids; D005260:Female; D020719:Glucuronides; D064368:Healthy Volunteers; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D008875:Middle Aged; D012007:Rectum / Q000378:metabolism*; D055815:Young Adult
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D036381:Diarylheptanoids; D020719:Glucuronides; C569902:hexahydrocurcumin; D003474:Curcumin; C050229:demethoxycurcumin
keywords: clinical trial; curcumin; human; pharmacokinetics; steady state