分析不同姜黄素创新配方，以提高人体的相对口服生物利用度。
Analysis of different innovative formulations of curcumin for improved relative oral bioavailability in human subjects.
机构信息
Increnovo LLC, 2138 E Lafayette Pl, Milwaukee, WI, 53202, USA.
Department of Health Sciences and Human Performance, The University of Tampa, Tampa, FL, 33606, USA.
出版信息
Eur J Nutr. 2018 Apr;57(3):929-938. doi: 10.1007/s00394-016-1376-9. Epub 2017 Feb 16.
PURPOSE
The optimal health benefits of curcumin are limited by its low solubility in water and corresponding poor intestinal absorption. Cyclodextrins (CD) can form inclusion complexes on a molecular basis with lipophilic compounds, thereby improving aqueous solubility, dispersibility, and absorption. In this study, we investigated the bioavailability of a new γ-cyclodextrin curcumin formulation (CW8). This formulation was compared to a standardized unformulated curcumin extract (StdC) and two commercially available formulations with purported increased bioavailability: a curcumin phytosome formulation (CSL) and a formulation of curcumin with essential oils of turmeric extracted from the rhizome (CEO).
METHODS
Twelve healthy human volunteers participated in a double-blinded, cross-over study. The plasma concentrations of the individual curcuminoids that are present in turmeric (namely curcumin, demethoxycurcumin, and bisdemethoxycurcumin) were determined at baseline and at various intervals after oral administration over a 12-h period.
RESULTS
CW8 showed the highest plasma concentrations of curcumin, demethoxycurcumin, and total curcuminoids, whereas CSL administration resulted in the highest levels of bisdemethoxycurcumin. CW8 (39-fold) showed significantly increased relative bioavailability of total curcuminoids (AUC) in comparison with the unformulated StdC.
CONCLUSION
The data presented suggest that γ-cyclodextrin curcumin formulation (CW8) significantly improves the absorption of curcuminoids in healthy humans.
目的
姜黄素在水中的溶解度低，肠道吸收相应较差，因此其最佳健康益处有限。环糊精（CD）可以在分子基础上与亲脂性化合物形成包合物，从而提高水溶解度、分散性和吸收度。在本研究中，我们研究了一种新型γ-环糊精姜黄素配方（CW8）的生物利用度。将该配方与标准化的未配方姜黄素提取物（StdC）以及两种据称生物利用度增加的市售配方进行比较：姜黄素植物甾醇配方（CSL）和姜黄中姜黄提取的精油配方（CEO）。
方法
12 名健康志愿者参加了一项双盲、交叉研究。在口服给药后 12 小时的各个时间点测定了存在于姜黄中的单个姜黄素类化合物（即姜黄素、脱甲氧基姜黄素和双脱甲氧基姜黄素）的血浆浓度。
结果
CW8 显示出最高的姜黄素、脱甲氧基姜黄素和总姜黄素类化合物的血浆浓度，而 CSL 给药导致双脱甲氧基姜黄素水平最高。CW8（39 倍）与未配方的 StdC 相比，总姜黄素类化合物（AUC）的相对生物利用度显著增加。
结论
所呈现的数据表明，γ-环糊精姜黄素配方（CW8）可显著提高健康人群中姜黄素类化合物的吸收度。
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