Kroon Maurice A G M, van Laarhoven Hanneke W M, Swart Eleonora L, van Tellingen Olaf, Kemper E Marleen
Department of Pharmacy and Clinical Pharmacology, Amsterdam University Medical Center, AMC, 1105AZ Amsterdam, the Netherlands.
Department of Medical Oncology, Amsterdam University Medical Center, University of Amsterdam, 1081HV Amsterdam, the Netherlands.
iScience. 2025 May 3;28(6):112575. doi: 10.1016/j.isci.2025.112575. eCollection 2025 Jun 20.
This independent crossover study assessed curcumin bioavailability and excretion in nine healthy males receiving three formulations (AOV, Longvida, and NovaSOL) at about 570 mg, while AOV was also tested at 2280 mg, with and without piperine. Plasma levels of unconjugated curcumin remained below 2 nM in most cases, including high-dose AOV and piperine combinations. NovaSOL achieved the highest levels (6.7-38 nM at 30 min), but these rapidly declined and were still 100-fold lower than concentrations used to show biological effects. Curcumin conjugates exceeded 10 nM with all formulations, particularly NovaSOL, which showed 100-fold higher levels. Fecal recovery mainly included unconjugated curcuminoids and was high, except for NovaSOL, suggesting better intestinal absorption. However, even when using a formulation with enhanced uptake, plasma levels of unconjugated curcumin remained minimal. Piperine addition provided no benefit. The findings underscore that bioavailability claims should be based on unconjugated curcumin and not on its poorly membrane permeable conjugates.
这项独立交叉研究评估了9名健康男性在服用三种约570毫克制剂（AOV、Longvida和NovaSOL）时姜黄素的生物利用度和排泄情况，同时还对2280毫克的AOV进行了测试，测试时添加或不添加胡椒碱。在大多数情况下，包括高剂量AOV与胡椒碱联合使用时，未结合姜黄素的血浆水平仍低于2纳摩尔。NovaSOL达到了最高水平（30分钟时为6.7 - 38纳摩尔），但这些水平迅速下降，仍比显示生物学效应所用的浓度低100倍。所有制剂的姜黄素结合物均超过10纳摩尔，特别是NovaSOL，其水平高出100倍。粪便回收率主要包括未结合的姜黄素类化合物，除NovaSOL外回收率较高，这表明肠道吸收较好。然而，即使使用具有增强摄取作用的制剂，未结合姜黄素的血浆水平仍然很低。添加胡椒碱并无益处。这些发现强调，生物利用度的说法应以未结合的姜黄素为依据，而不是以其膜通透性差的结合物为依据。
