Abstract

BackgroundThe potential health benefits of curcumin are limited by its poor solubility, low absorption from the gut, rapid metabolism and rapid systemic elimination. The purpose of this study was the comparative measurement of the increases in levels of curcuminoids (curcumin, demethoxycurcumin, bisdemethoxycurcumin) and the metabolite tetrahydrocurcumin after oral administration of three different curcumin formulations in comparison to unformulated standard.MethodsThe relative absorption of a curcumin phytosome formulation (CP), a formulation with volatile oils of turmeric rhizome (CTR) and a formulation of curcumin with a combination of hydrophilic carrier, cellulosic derivatives and natural antioxidants (CHC) in comparison to a standardized curcumin mixture (CS) was investigated in a randomized, double-blind, crossover human study in healthy volunteers. Samples were analyzed by HPLC-MS/MS.ResultsTotal curcuminoids appearance in the blood was 1.3-fold higher for CTR and 7.9-fold higher for CP in comparison to unformulated CS. CHC showed a 45.9-fold higher absorption over CS and significantly improved absorption over CP (5.8-fold) and CTR (34.9-fold, all p < 0.001).ConclusionA formulation of curcumin with a combination of hydrophilic carrier, cellulosic derivatives and natural antioxidants significantly increases curcuminoid appearance in the blood in comparison to unformulated standard curcumin CS, CTR and CP.

Highlights

  • Despite its demonstrated effects, the potential health benefits of curcumin are limited by its poor solubility, low absorption from the gut, rapid metabolism and rapid systemic elimination [17]

  • The purpose of this study was the comparative measurement of the increases in levels of curcuminoids and the metabolite tetrahydrocurcumin in plasma after the administration of a single dose of the above mentioned novel water soluble curcumin formulation containing turmeric extract 20-28%, a hydrophilic carrier 63-75%, cellulosic derivatives 10-40% and natural antioxidants 1-3% (CHC), in comparison to curcumin phytosome formulation (CP), CTR and standard curcumin (CS) in healthy volunteers

  • Absorption of curcumin, demethoxycurcumin, bisdemethoxycurcumin, and appearance in the blood of tetrahydrocurcumin was measured in 12 healthy volunteers (n = 12) in a randomized, double-blind, crossover study

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Summary

Introduction

The potential health benefits of curcumin are limited by its poor solubility, low absorption from the gut, rapid metabolism and rapid systemic elimination. The purpose of this study was the comparative measurement of the increases in levels of curcuminoids (curcumin, demethoxycurcumin, bisdemethoxycurcumin) and the metabolite tetrahydrocurcumin after oral administration of three different curcumin formulations in comparison to unformulated standard. Despite its demonstrated effects, the potential health benefits of curcumin are limited by its poor solubility, low absorption from the gut, rapid metabolism and rapid systemic elimination [17]. While the major portion of ingested curcumin is excreted through the feces unmetabolized, the small portion that is absorbed is extensively converted to its water-soluble metabolites, glucuronides and sulfates. Curcumin and its reduced metabolites are conjugated with monoglucuronide via beta-glucuronidase, a monosulfate via sulfatase enzymes and a mixed sulfate/glucuronide, resulting in curcumin-glucuronoside, dihydocurcumin glucuronoside, tetrahydrocurcumin glucuronoside or corresponding monosulfate and mixed sulfate/glucuronoside (see Figure 1) [18,19]

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