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α-生育酚静脉注射和口服给予大鼠后的药代动力学和生物利用度研究。

Pharmacokinetic and bioavailability studies of α-viniferin after intravenous and oral administration to rats.

机构信息

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.

Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin 301617, China.

出版信息

J Pharm Biomed Anal. 2020 Sep 5;188:113376. doi: 10.1016/j.jpba.2020.113376. Epub 2020 May 25.

Abstract

Alpha-viniferin is a trimer of resveratrol and has various pharmacological activities including anti-Alzheimer's disease, anti-tuberculosis, anti-tumor, anti-inflammatory and anti-diabetic. To investigate the pharmacokinetic characteristics and absolute bioavailability of α-viniferin in rats, using naringenin as an internal standard (IS), a rapid HPLC-MS/MS method of 5 min complete run time was developed. The chromatographic separation of α-viniferin and naringenin were accomplished with Waters XBridge™ C column (2.1 mm × 100 mm, 3.5 μm) and the mobile phase were acetonitrile and 0.1 % formic acid at a flow rate of 0.3 mL/min. Plasma samples were pretreated by ethyl acetate. The negative ion mode with electrospray ionization (ESI) source was used for detecting the sample. Oral bioavailability of α-viniferin was 4.2 %. This study will be beneficial in better understanding the pharmacological properties and the further development of α-viniferin.

摘要

白藜芦醇三聚体 α-viniferin 具有多种药理活性,包括抗老年痴呆症、抗结核、抗肿瘤、抗炎和抗糖尿病。为了研究 α-viniferin 在大鼠体内的药代动力学特征和绝对生物利用度,采用以柚皮素为内标(IS),建立了一种快速高效液相色谱-串联质谱法(HPLC-MS/MS),在 5 分钟内完成整个运行时间。采用 Waters XBridge™ C 柱(2.1mm×100mm,3.5μm)和乙腈-0.1%甲酸作为流动相(流速 0.3mL/min)实现 α-viniferin 和 naringenin 的色谱分离。采用乙酸乙酯预处理血浆样品。采用电喷雾电离(ESI)源的负离子模式检测样品。α-viniferin 的口服生物利用度为 4.2%。本研究将有助于更好地了解 α-viniferin 的药理特性及其进一步开发。

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