Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects

Shaiju K. Vareed, Madhuri Kakarala, Mack Ruffin, James A. Crowell, Daniel P. Normolle, Zora Djuric, Dean E. Brenner

Research output: Contribution to journalArticle

255 Citations (Scopus)

Abstract

Background: Curcumin is a polyphenol, found in the spice turmeric, that has promising anticancer properties, but previous studies suggest that absorption of curcumin may be limited. Methods: This study examined the pharmacokinetics of a curcumin preparation in healthy human volunteers 0.25 to 72 h after a single oral dose. Curcumin was administered at doses of 10 g (n = 6) and 12 g (n = 6). Subjects were randomly allocated to dose level for a total of six subjects at each dose level. Serum samples were assayed for free curcumin, for its glucuronide, and for its sulfate conjugate. The data were fit to a one-compartment absorption and elimination model. Results: Using a high-performance liquid chromatography assay with a limit of detection of 50 ng/mL, only one subject had detectable free curcumin at any of the 14 time points assayed, but curcumin glucuronides and sulfates were detected in all subjects. Based on the pharmacokinetic model, the area under the curve for the 10 and 12 g doses was estimated (mean F SE) to be 35.33 F 3.78 and 26.57 F 2.97 μg/mL x h, respectively, whereas Cmax was 2.30 ± 0.26 and 1.73 ± 0.19 Mg/mL. The Tmax and t1/2 were estimated to be 3.29 ± 0.43 and 6.77 ± 0.83 h. The ratio of glucuronide to sulfate was 1.92:1. The curcumin conjugates were present as either glucuronide or sulfate, not mixed conjugates. Conclusion: Curcumin is absorbed after oral dosing in humans and can be detected as glucuronide and sulfate conjugates in plasma.

Original languageEnglish (US)
Pages (from-to)1411-1417
Number of pages7
JournalCancer Epidemiology Biomarkers and Prevention
Volume17
Issue number6
DOIs
StatePublished - Jun 1 2008

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Curcumin
Healthy Volunteers
Pharmacokinetics
Sulfates
Glucuronides
Curcuma
Spices
Polyphenols
Area Under Curve
Limit of Detection
High Pressure Liquid Chromatography
Serum

All Science Journal Classification (ASJC) codes

  • Epidemiology
  • Oncology

Cite this

Vareed, S. K., Kakarala, M., Ruffin, M., Crowell, J. A., Normolle, D. P., Djuric, Z., & Brenner, D. E. (2008). Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. Cancer Epidemiology Biomarkers and Prevention, 17(6), 1411-1417. https://doi.org/10.1158/1055-9965.EPI-07-2693
Vareed, Shaiju K. ; Kakarala, Madhuri ; Ruffin, Mack ; Crowell, James A. ; Normolle, Daniel P. ; Djuric, Zora ; Brenner, Dean E. / Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. In: Cancer Epidemiology Biomarkers and Prevention. 2008 ; Vol. 17, No. 6. pp. 1411-1417.
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Vareed, SK, Kakarala, M, Ruffin, M, Crowell, JA, Normolle, DP, Djuric, Z & Brenner, DE 2008, 'Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects', Cancer Epidemiology Biomarkers and Prevention, vol. 17, no. 6, pp. 1411-1417. https://doi.org/10.1158/1055-9965.EPI-07-2693

Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects. / Vareed, Shaiju K.; Kakarala, Madhuri; Ruffin, Mack; Crowell, James A.; Normolle, Daniel P.; Djuric, Zora; Brenner, Dean E.

In: Cancer Epidemiology Biomarkers and Prevention, Vol. 17, No. 6, 01.06.2008, p. 1411-1417.

Research output: Contribution to journalArticle

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T1 - Pharmacokinetics of curcumin conjugate metabolites in healthy human subjects

AU - Vareed, Shaiju K.

AU - Kakarala, Madhuri

AU - Ruffin, Mack

AU - Crowell, James A.

AU - Normolle, Daniel P.

AU - Djuric, Zora

AU - Brenner, Dean E.

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Y1 - 2008/6/1

N2 - Background: Curcumin is a polyphenol, found in the spice turmeric, that has promising anticancer properties, but previous studies suggest that absorption of curcumin may be limited. Methods: This study examined the pharmacokinetics of a curcumin preparation in healthy human volunteers 0.25 to 72 h after a single oral dose. Curcumin was administered at doses of 10 g (n = 6) and 12 g (n = 6). Subjects were randomly allocated to dose level for a total of six subjects at each dose level. Serum samples were assayed for free curcumin, for its glucuronide, and for its sulfate conjugate. The data were fit to a one-compartment absorption and elimination model. Results: Using a high-performance liquid chromatography assay with a limit of detection of 50 ng/mL, only one subject had detectable free curcumin at any of the 14 time points assayed, but curcumin glucuronides and sulfates were detected in all subjects. Based on the pharmacokinetic model, the area under the curve for the 10 and 12 g doses was estimated (mean F SE) to be 35.33 F 3.78 and 26.57 F 2.97 μg/mL x h, respectively, whereas Cmax was 2.30 ± 0.26 and 1.73 ± 0.19 Mg/mL. The Tmax and t1/2 were estimated to be 3.29 ± 0.43 and 6.77 ± 0.83 h. The ratio of glucuronide to sulfate was 1.92:1. The curcumin conjugates were present as either glucuronide or sulfate, not mixed conjugates. Conclusion: Curcumin is absorbed after oral dosing in humans and can be detected as glucuronide and sulfate conjugates in plasma.

AB - Background: Curcumin is a polyphenol, found in the spice turmeric, that has promising anticancer properties, but previous studies suggest that absorption of curcumin may be limited. Methods: This study examined the pharmacokinetics of a curcumin preparation in healthy human volunteers 0.25 to 72 h after a single oral dose. Curcumin was administered at doses of 10 g (n = 6) and 12 g (n = 6). Subjects were randomly allocated to dose level for a total of six subjects at each dose level. Serum samples were assayed for free curcumin, for its glucuronide, and for its sulfate conjugate. The data were fit to a one-compartment absorption and elimination model. Results: Using a high-performance liquid chromatography assay with a limit of detection of 50 ng/mL, only one subject had detectable free curcumin at any of the 14 time points assayed, but curcumin glucuronides and sulfates were detected in all subjects. Based on the pharmacokinetic model, the area under the curve for the 10 and 12 g doses was estimated (mean F SE) to be 35.33 F 3.78 and 26.57 F 2.97 μg/mL x h, respectively, whereas Cmax was 2.30 ± 0.26 and 1.73 ± 0.19 Mg/mL. The Tmax and t1/2 were estimated to be 3.29 ± 0.43 and 6.77 ± 0.83 h. The ratio of glucuronide to sulfate was 1.92:1. The curcumin conjugates were present as either glucuronide or sulfate, not mixed conjugates. Conclusion: Curcumin is absorbed after oral dosing in humans and can be detected as glucuronide and sulfate conjugates in plasma.

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