■类姜黄素,其中主要成分是姜黄素,是姜黄根茎中的天然多酚化合物。并且具有广泛的生物制药特性,由于生物利用度差而在人类中受到限制。目前,大多数商业生物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,并且需要每日多次剂量才能达到临床疗效。这项研究是为了比较自然的生物利用度,含有60%天然姜黄素的水分散性姜黄提取物,测试产品,WDTE60N(每天1×250毫克),参考产品,姜黄提取物胶囊(500毫克姜黄素和5毫克胡椒碱,CPC;每天3×500毫克)。
■16名健康成年男性受试者禁食过夜10小时,然后口服1粒测试产品WDTE60N胶囊或3粒参考产品CPC胶囊(每6小时即0.00小时给予1粒胶囊,在每个研究期间为6.00小时和12.00小时)。在给药之前和给药后在规定的时间点-12.00、-02.00、00.00(给药前10分钟内)小时在给药前早晨和给药后(第一剂)在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各16.00和24小时使用经过验证的液相色谱与串联质谱生物分析方法确定类姜黄素的血浆浓度。
观察到测试产品WDTE60N的Cmax(GLSM)为74.56ng/mL;并且参考CPC的Cmax为22.75ng/mL。测试WDTE60N的AUC0-t(GLSM)为419.00h·ng/mL;对于参考CPC,总类姜黄素为359.86h·ng/mL。
测试制剂WDTE60N在比参考制剂CPC低10倍的活性物质剂量下显示出改善的相对吸收和等效暴露。
UNASSIGNED: 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).
UNASSIGNED: 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.
UNASSIGNED: 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.
UNASSIGNED: The test formulation WDTE60N showed improved relative absorption and equivalent exposure at a 10-fold-lower dose of actives than the reference formulation CPC.