Pharmacokinetics of (-)-Epigallocatechin-3-gallate in Conscious and Freely Moving Rats and Its Brain Regional Distribution

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• 作者：Lei-Chwen Lin ; Meng-Nan Wang ; Ting-Yu Tseng ; Jung-Sung Sung ; Tung-Hu Tsai
• 刊名：Journal of Agricultural and Food Chemistry
• 出版年：2007
• 出版时间：February 21, 2007
• 年：2007
• 卷：55
• 期：4
• 页码：1517 - 1524
• 全文大小：133K
• 年卷期：v.55,no.4(February 21, 2007)
• ISSN：1520-5118

文摘

A liquid chromatography technique coupled with tandem mass spectrometry (LC-MS/MS) electrosprayionization was used to measure (-)-epigallocatechin-3-gallate (EGCG) in rat plasma. This methodwas applied to investigate the pharmacokinetics of EGCG in a conscious and freely moving rat by anautomated blood sampling device. Multiple reaction monitoring (MRM) was used to monitor thetransition of the deprotonated molecule m/z of 457 [M - H]^- to the product ion 169 for EGCG andthe m/z of 187 to 164 for the internal standard. The limit of quantification (LOQ) of EGCG in ratplasma was determined to be 5 ng/mL, and the linear range was 5-5000 ng/mL. The protein bindingof EGCG in rat plasma was 92.4 ± 2.5%. The brain distribution result indicated that EGCG maypotentially penetrate through the blood-brain barrier at a lower rate. The disposition of EGCG in therat blood was fitted well by the two-compartmental model after intravenous administration (10 mg/kg, iv). The elimination half-life of EGCG was 62 ± 11 and 48 ± 13 min for intravenous (10 mg/kg)and oral (100 mg/kg) administration, respectively. The pharmacokinetic data indicate that the oralbioavailability of EGCG in a conscious and freely moving rat was about 4.95%.