PDF(Pubmed)
Abstract：
OBJECTIVE: Astaxanthin is a naturally occurring carotenoid with high anti-oxidant properties, but it is a very lipophilic compound with low oral bioavailability. This study was conducted to compare the pharmacokinetic parameters of a novel astaxanthin preparation based on micellar solubilization technology, NovaSOL® 400-mg capsules (Test product), and those of astaxanthin 400-mg capsules (reference product), after single oral dose administration to healthy male adults.
METHODS: A single oral dose (400 mg equivalent to 8 mg astaxanthin) of test and reference astaxanthin were administered with 240 mL of water to 12 volunteers according to crossover design, in two phases, with a washout period of 1 week in between. Blood samples were collected at hourly intervals for the first 12 h, then at 24.0, 48.0, and 72.0 h after administration. Aliquots of plasma were centrifuged and the clear supernatant was injected into the high performance liquid chromatography-diode array detection (HPLC-DAD) system. Plasma concentration of astaxanthin versus time profiles were constructed, and the primary pharmacokinetic parameters, maximum concentration (Cmax), area under concentration time curve from time of administration (0) to time (t) [AUC0-t] or to infinity ∞, [AUC0-∞], half-life (T½) and time to reach Cmax (Tmax) were calculated.
RESULTS: The test micellar astaxanthin reached a Cmax of 7.21 µg/ml after 3.67 h compared to only 3.86 µg/ml after 8.5 h for the reference native astaxanthin.
CONCLUSIONS: Micellar formulation of astaxanthin is capable of producing a high concentration of astaxanthin in plasma in a shorter time, thereby expected to provide faster potential therapeutic efficacy.
METHODS: A single oral dose (400 mg equivalent to 8 mg astaxanthin) of test and reference astaxanthin were administered with 240 mL of water to 12 volunteers according to crossover design, in two phases, with a washout period of 1 week in between. Blood samples were collected at hourly intervals for the first 12 h, then at 24.0, 48.0, and 72.0 h after administration. Aliquots of plasma were centrifuged and the clear supernatant was injected into the high performance liquid chromatography-diode array detection (HPLC-DAD) system. Plasma concentration of astaxanthin versus time profiles were constructed, and the primary pharmacokinetic parameters, maximum concentration (Cmax), area under concentration time curve from time of administration (0) to time (t) [AUC0-t] or to infinity ∞, [AUC0-∞], half-life (T½) and time to reach Cmax (Tmax) were calculated.
RESULTS: The test micellar astaxanthin reached a Cmax of 7.21 µg/ml after 3.67 h compared to only 3.86 µg/ml after 8.5 h for the reference native astaxanthin.
CONCLUSIONS: Micellar formulation of astaxanthin is capable of producing a high concentration of astaxanthin in plasma in a shorter time, thereby expected to provide faster potential therapeutic efficacy.
摘要：
目的：虾青素是一种天然存在的类胡萝卜素，具有高抗氧化性能，但它是一种非常亲脂性的化合物，口服生物利用度低。本研究旨在比较基于胶束增溶技术的新型虾青素制剂的药代动力学参数，NovaSOL®400-mg胶囊（测试产品），和虾青素400毫克胶囊（参考产品），在对健康男性成人单次口服剂量给药后。
方法：根据交叉设计，将测试虾青素和参考虾青素的单次口服剂量（400mg相当于8mg虾青素）与240mL水一起给予12名志愿者，分两个阶段,其间有1周的冲洗期。在最初的12小时内，每小时收集血液样本，然后在给药后24.0、48.0和72.0小时。将血浆的等分试样离心,并将澄清的上清液注射到高效液相色谱-二极管阵列检测(HPLC-DAD)系统中。构建了虾青素的血浆浓度与时间的关系曲线，和主要的药代动力学参数，最大浓度(Cmax),从给药时间（0）到时间（t）[AUC0-t]或无穷大∞的浓度时间曲线下面积，[AUC0-∞]，计算半衰期(T1/2)和达到Cmax的时间(Tmax)。
结果：测试胶束虾青素在3.67h后达到的Cmax为7.21µg/ml，而参考天然虾青素在8.5h后仅为3.86µg/ml。
结论：虾青素的胶束制剂能够在较短的时间内在血浆中产生高浓度的虾青素，从而预期提供更快的潜在治疗功效。
方法：根据交叉设计，将测试虾青素和参考虾青素的单次口服剂量（400mg相当于8mg虾青素）与240mL水一起给予12名志愿者，分两个阶段,其间有1周的冲洗期。在最初的12小时内，每小时收集血液样本，然后在给药后24.0、48.0和72.0小时。将血浆的等分试样离心,并将澄清的上清液注射到高效液相色谱-二极管阵列检测(HPLC-DAD)系统中。构建了虾青素的血浆浓度与时间的关系曲线，和主要的药代动力学参数，最大浓度(Cmax),从给药时间（0）到时间（t）[AUC0-t]或无穷大∞的浓度时间曲线下面积，[AUC0-∞]，计算半衰期(T1/2)和达到Cmax的时间(Tmax)。
结果：测试胶束虾青素在3.67h后达到的Cmax为7.21µg/ml，而参考天然虾青素在8.5h后仅为3.86µg/ml。
结论：虾青素的胶束制剂能够在较短的时间内在血浆中产生高浓度的虾青素，从而预期提供更快的潜在治疗功效。
