Altern Ther Health Med. 2024 Apr;30(4):18-23.
Curcuminoids, the major component of which is curcumin, are natural polyphenolic compounds from the rhizome of Curcuma longa Linn. and possess extensive biopharmacological properties that are limited in humans due to poor bioavailability. Currently, most commercial bioavailable turmeric extracts use synthetic excipients or the addition of piperine to enhance bioavailability, and are needed in multiple daily doses to achieve clinical efficacy. This study was conducted to compare the bioavailability of a natural, water-dispersible turmeric extract containing 60% natural curcuminoids, the test product, WDTE60N (1 × 250 mg per day), with the reference product, turmeric extract capsules (500 mg curcuminoids and 5 mg piperine, CPC; 3 × 500 mg per day).
Sixteen healthy adult male subjects fasted overnight for 10 hours and then were dosed with either one capsule of the test product WDTE60N or three capsules of reference product CPC orally (One capsule administered at every 6 hours interval i.e. at 0.00 hrs, 6.00 hrs and at 12.00 hrs) in each study period. Blood sampling before and after dosing was carried out at defined time points at -12.00, -02.00, 00.00 (within 10 minutes prior to dosing) hours in morning before dosing and post-dose (First dose) at 00.50, 01.00, 02.00, 03.00, 04.00, 05.00, 06.50, 07.00, 08.00, 09.00, 10.00, 11.00, 12.50, 13.00, 14.00, 16.00, 18.00, 20.00 and 24.00 hours in each period. Plasma concentration of curcuminoids was determined using a validated liquid chromatography with tandem mass spectrometry bioanalytical method.
The Cmax (GLSM) for the test product WDTE60N was observed to be 74.56 ng/mL; and same for the reference CPC was 22.75 ng/mL. AUC0-t (GLSM) for test WDTE60N was 419.00 h∙ng/mL; and for reference CPC it was 359.86 h∙ng/mL for total curcuminoids.
The test formulation WDTE60N showed improved relative absorption and equivalent exposure at a 10-fold-lower dose of actives than the reference formulation CPC.
姜黄素是从姜黄根茎中提取的主要成分，是一种天然多酚化合物，具有广泛的生物药理学特性，但由于生物利用度低，在人体内的作用有限。目前，大多数商业上可利用的姜黄提取物使用合成赋形剂或添加胡椒碱来提高生物利用度，并且需要每天服用多次才能达到临床疗效。本研究旨在比较一种天然、可分散在水中的姜黄提取物（含 60%天然姜黄素）的生物利用度，即受试产品 WDTE60N（每天 1 次，每次 250mg）与参比产品姜黄提取物胶囊（500mg 姜黄素和 5mg 胡椒碱，CPC；每天 3 次，每次 500mg）。
16 名健康成年男性空腹 10 小时，然后分别口服受试产品 WDTE60N 胶囊 1 粒或参比产品 CPC 胶囊 3 粒（每 6 小时 1 次，即 0 点、6 点和 12 点）。在每个研究期间，在每个给药前 10 分钟内（0 点）和给药后（第一剂量），在早上给药前（-12.00、-02.00、00.00 小时）和给药后（00.50、01.00、02.00、03.00、04.00、05.00、06.50、07.00、08.00、09.00、10.00、11.00、12.50、13.00、14.00、16.00、18.00、20.00 和 24.00 小时）进行采血。采用经验证的液相色谱-串联质谱法测定血浆中姜黄素的浓度。
受试产品 WDTE60N 的 Cmax（GLSM）为 74.56ng/ml；参比产品 CPC 为 22.75ng/ml。受试产品 WDTE60N 的 AUC0-t（GLSM）为 419.00h·ng/ml；参比产品 CPC 为 359.86h·ng/ml，均为总姜黄素。
与参比制剂 CPC 相比，受试制剂 WDTE60N 在低 10 倍剂量的活性物质时表现出更好的相对吸收和等效暴露。
