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Pharmacokinetics in rat plasma and tissue distribution in mice of galangin determined by UHPLC–MS/MS

Ye Weijian, Sun Wei, Chen Ruijie, Wang Zhe, Cui Xiao, Zhang Hui, Qian Shuyi, Zheng Qi, Zhou Yangfeng, Wan Jiafeng, Xu Jiali, Wang Xianqin, Zhou Yunfang

Acta Chromatographica

2019

Vol. 31, no. 2

120--125

Galangin (GAL), the major bioactive flavonol extracted from Alpinia officinarum Hance (Zingiberaceae), has attracted much attention due to its multiple biological activities. To develop a fast, reliable, and sensitive ultrahigh-performance liquid chromatography–tandem mass spectrometry (UHPLC–MS/MS) method for the quantification of GAL in rat plasma and mouse tissues. UHPLC–MS/MS using electrospray ionization operating in negative-ion mode was used to determinate GAL in 18 rats receiving three doses of GAL (2 and 9 mg/kg by intravenous injection, 5 mg/kg by oral administration), with six rats for each dose. Blood samples were collected at 0.0333, 0.25, 0.5, 1, 2, 4, 6 and 8 h. A total of 25 mice received 18 mg/kg GAL by intraperitoneal injection. Liver, heart, lung, spleen, brain, and kidney tissue samples were collected at 0.25, 0.5, 2, 4, and 6 h. The precision of the method was better than 12.1%, while the accuracy ranged from −4.8% to 8.1%. The results of pharmacokinetics demonstrated rapid GAL absorption (tmax of 0.25 h), fast elimination (t1/2 <1.1 h) after three different dosages, and an absolute bioavailability of ~7.6%. Tissue distribution analysis revealed abundant GAL in liver, kidney, spleen, and lung and smaller amounts in brain. The developed method proved fast (3 min), efficient, and reliable, with high selectivity for the quantitative analysis of GAL in biological samples. This is the first study to identify the target tissues of GAL, and the results may help to elucidate the mechanisms underlying its therapeutic effects in vivo.