标准虾青素及其胶束制剂在健康男性志愿者中的药代动力学比较研究

IF 1.9 4区 医学 Q3 PHARMACOLOGY & PHARMACY
Mohamed T Khayyal, Mahmoud H Teaima, Hoda M Marzouk, Rania M El -Hazek, Frank Behnam, Dariush Behnam
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引用次数: 0

摘要

背景和目的:虾青素是一种天然类胡萝卜素,具有很强的抗氧化性,但它是一种非常亲脂的化合物,口服生物利用度较低。本研究旨在比较基于胶束增溶技术的新型虾青素制剂 NovaSOL® 400 毫克胶囊(试验产品)和虾青素 400 毫克胶囊(参照产品)在健康男性成年人中单次口服后的药代动力学参数:根据交叉设计,分两个阶段给 12 名志愿者口服单次剂量(400 毫克,相当于 8 毫克虾青素)的测试虾青素和参比虾青素,加 240 毫升水,中间有 1 周的冲洗期。在最初的 12 小时内,每隔一小时采集一次血样,然后在给药后的 24.0、48.0 和 72.0 小时采集血样。等量血浆离心后,将清澈的上清液注入高效液相色谱-二极管阵列检测(HPLC-DAD)系统。构建虾青素的血浆浓度与时间曲线,并计算主要药代动力学参数、最大浓度(Cmax)、从给药时间(0)到时间(t)的浓度时间曲线下面积[AUC0-t]或到无穷大∞,[AUC0-∞]、半衰期(T½)和达到Cmax的时间(Tmax):结果:测试的胶束虾青素在3.67小时后达到7.21微克/毫升的Cmax,而参考原生虾青素在8.5小时后仅为3.86微克/毫升:结论:虾青素的微胶囊配方能够在较短时间内在血浆中产生高浓度的虾青素,因此有望提供更快的潜在疗效。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Comparative Pharmacokinetic Study of Standard Astaxanthin and its Micellar Formulation in Healthy Male Volunteers.

Comparative Pharmacokinetic Study of Standard Astaxanthin and its Micellar Formulation in Healthy Male Volunteers.

Background and 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.

Conclusion: 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.

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来源期刊
CiteScore
3.70
自引率
0.00%
发文量
64
审稿时长
>12 weeks
期刊介绍: Hepatology International is a peer-reviewed journal featuring articles written by clinicians, clinical researchers and basic scientists is dedicated to research and patient care issues in hepatology. This journal focuses mainly on new and emerging diagnostic and treatment options, protocols and molecular and cellular basis of disease pathogenesis, new technologies, in liver and biliary sciences. Hepatology International publishes original research articles related to clinical care and basic research; review articles; consensus guidelines for diagnosis and treatment; invited editorials, and controversies in contemporary issues. The journal does not publish case reports.
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