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基于功能性食品成分药代动力学特性的制剂开发研究

[Study of Formulation Development Based on the Pharmacokinetic Properties of Functional Food Components].

作者信息

Sato Yuki

机构信息

Faculty of Pharmaceutical Sciences, Hokkaido University.

出版信息

Yakugaku Zasshi. 2019;139(3):341-347. doi: 10.1248/yakushi.18-00140.

DOI:10.1248/yakushi.18-00140
PMID:30828009
Abstract

Preventive medicine and anti-aging medicine have received much attention recently due to an increase in the proportion of elderly people in the population, and to an increase in patients with lifestyle diseases. Oxidative stress is involved in the onset of lifestyle diseases, and various antioxidant supplements and antioxidant-fortified functional foods have recently become available. Many epidemiological studies have shown relationships between the consumption of polyphenol and carotenoid-rich foods and the prevention of lifestyle diseases. We have focused on the absorption mechanism of these food components that show low bioavailability, and have made efforts to improve their poor absorption based on their pharmacokinetic properties. In this report, as examples, we describe the enhancement of the absorption of coenzyme Q10 (CoQ10) and lutein. To improve the absorption of CoQ10, we focused on the component of emulsion. We found that a higher plasma concentration of CoQ10 could be obtained by creating an emulsion containing a surfactant with a higher hydrophile-lipophile balance (HLB) value. For the improvement of lutein absorption, we prepared a solid dispersion and self-emulsifying drug delivery system. It was shown that the plasma concentrations of lutein in these two formulation groups were increased compared with that in the powder group. The absorption of lutein was also evaluated by its cumulative amount in the lymph system. Our data showed that lutein is transferred from the small intestine into the lymph stream, rather than into the blood stream. Further investigations to improve the absorption of these components are in progress.

摘要

由于人口老龄化比例上升以及生活方式疾病患者增多,预防医学和抗衰老医学近来备受关注。氧化应激与生活方式疾病的发病有关,各种抗氧化剂补充剂和富含抗氧化剂的功能性食品近来已面市。许多流行病学研究表明,食用富含多酚和类胡萝卜素的食物与预防生活方式疾病之间存在关联。我们关注这些生物利用度低的食物成分的吸收机制,并基于其药代动力学特性努力改善其吸收不佳的情况。在本报告中,作为示例,我们描述了辅酶Q10(CoQ10)和叶黄素吸收的增强。为提高CoQ10的吸收,我们关注了乳剂成分。我们发现,通过制备含有亲水亲油平衡(HLB)值较高的表面活性剂的乳剂,可以获得更高的CoQ10血浆浓度。为改善叶黄素吸收,我们制备了固体分散体和自乳化药物递送系统。结果表明,这两个制剂组中叶黄素的血浆浓度与粉末组相比有所增加。叶黄素的吸收也通过其在淋巴系统中的累积量进行评估。我们的数据表明,叶黄素从小肠转移到淋巴中,而不是进入血液。进一步改善这些成分吸收的研究正在进行中。

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