Bioavailability Study of an Innovative Orobuccal Formulation of Glutathione
Bioavailability Study of an Innovative Orobuccal Formulation of Glutathione
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DOI：
10.1155/2016/3286365
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发表时间：
2016-01-01
影响因子：
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通讯作者：
Marzatico, Fulvio
中科院分区：
文献类型：
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作者：
Buonocore, Daniela;Grosini, Matteo;Marzatico, Fulvio
普遍存在的硫醇三肽谷胱甘肽（GSH）的改变参与氧化应激，在衰老中起作用；因此，谷胱甘肽与这一生理功能效率逐渐下降和对疾病易感性增加的过程密切相关。当循环谷胱甘肽减少时，口服可能被认为是一种治疗益处。不幸的是，由于肠道γ -谷氨酰转移酶对三肽的水解，饮食中的谷胱甘肽并不是其增加的主要决定因素。本研究的目的是评价优化后的含纯稳定谷胱甘肽的口口腔快缓释制剂片在体外和体内系统利用度测试中的改进。体外对创新GSH释放制剂的渗透能力评价表明，重建的口腔上皮对GSH有良好的吸收，其吸收具有时间依赖性。此外，从15名健康志愿者身上获得的体内结果表明，血液中谷胱甘肽水平的提高显示出（在30和60分钟后）通过口腔粘膜的快速吸收。综上所述，经优化后的口腔快缓释片配制的谷胱甘肽摄入对提高谷胱甘肽血药浓度有积极作用。
Alteration of the ubiquitous thiol tripeptide glutathione (GSH) is involved in oxidative stress, which plays a role in ageing; consequently, GSH is closely related to this process characterized by progressive decline in the efficiency of physiological function and increased susceptibility to disease. When circulating GSH decreases, oral administration might be considered a therapeutic benefit. Unfortunately, due to the hydrolysis of the tripeptide by intestinal gamma-glutamyltransferase, dietary glutathione is not a major determinant for its increase. Aim of this work was to evaluate improvement of GSH systemic availability testing, in vitro and in vivo, an optimized orobuccal fast-slow release formulation tablet containing pure stabilized GSH. In vitro evaluation of the penetration capability of the innovative GSH-release formulation showed that GSH was well absorbed by the reconstructed oral epithelium and its absorption has features of time-dependence. In addition, in vivo results, obtained from 15 healthy volunteers, were in favor of GSH level improvement in blood showing fast (after 30 and 60 minutes) absorption through oral mucosa. In conclusion, the intake of GSH formulated through optimized orobuccal fast-slow release tablets gave positive results in raising GSH blood concentration.