Department of Pharmacology and Toxicology, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
Eur J Drug Metab Pharmacokinet. 2024 Jul;49(4):467-475. doi: 10.1007/s13318-024-00898-0. Epub 2024 May 15.
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.
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 (C), area under concentration time curve from time of administration (0) to time (t) [AUC] or to infinity ∞, [AUC], half-life (T) and time to reach C (T) were calculated.
The test micellar astaxanthin reached a C 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.
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.
虾青素是一种天然存在的类胡萝卜素，具有很强的抗氧化特性，但它是一种非常亲脂的化合物，口服生物利用度低。本研究旨在比较新型胶束增溶技术制备的虾青素制剂（NovaSOL 400mg 胶囊，试验品）和虾青素 400mg 胶囊（参比品）单次口服给药后健康男性成年人的药代动力学参数。
按照交叉设计，12 名志愿者单次口服（400mg 相当于 8mg 虾青素）试验品和参比品，用 240ml 水送服，两阶段之间有 1 周洗脱期。给药后 12 小时内每小时采集血样，然后在 24.0、48.0 和 72.0 小时采集。取血浆等分试样离心，上清液注入高效液相色谱-二极管阵列检测（HPLC-DAD）系统。绘制虾青素血药浓度-时间曲线，计算主要药代动力学参数，即最大浓度（C）、给药至 t 时间（0）的浓度-时间曲线下面积[AUC]或至无穷大∞，[AUC]，半衰期（T）和达峰时间（T）。
试验用胶束虾青素在 3.67 小时后达到 7.21µg/ml 的 C，而参比天然虾青素在 8.5 小时后仅达到 3.86µg/ml。
虾青素胶束制剂能够在较短时间内使血浆中虾青素达到较高浓度，从而有望更快地发挥潜在的治疗效果。
