Pharmacokinetic study of mangiferin in human plasma after oral administration

Mangiferin, an active component of traditional Chinese herbal medicine, although it is reported to have various pharmacological effects, the limited number of pharmacokinetic studies limit its wide application. To evaluate the pharmacokinetics of mangiferin in human, a sensitive high performance liquid chromatography-mass spectrometry (HPLC-MS) method for the determination of mangiferin in human plasma was developed. The proposed HPLC-MS method is selective, precise and accurate enough and enables the identification and quantification of mangiferin for the use in clinical studies. After single oral administration of 0.1, 0.3 and 0.9 g mangiferin, respectively, the method was successfully applied for the pharmacokinetics of mangiferin in 21 healthy male Chinese volunteers. The pharmacokinetic of mangiferin was fit to the non-compartmental model. The pharmacokinetics parameters were calculated. Mangiferin concentration in plasma reached 38.64 +/- 6.75 ng/mL about 1 h after oral administration of 0.9 g mangiferin and the the apparent elimination half-life (t(1/2)) was 7.85 +/- 1.72 h. The absorption of mangiferin was increased with the administration of a large dose and it was concluded that the pharmacokinetics of mangiferin in human was nonlinear. (C) 2011 Elsevier Ltd. All rights reserved.

芒果苷是一种传统中草药的活性成分，尽管据报道它具有多种药理作用，但药代动力学研究数量有限，限制了其广泛应用。为了评估芒果苷在人体内的药代动力学，建立了一种灵敏的高效液相色谱 - 质谱（HPLC - MS）法用于测定人血浆中的芒果苷。所建立的HPLC - MS方法具有足够的选择性、精密度和准确度，能够对芒果苷进行鉴定和定量，可用于临床研究。分别单次口服0.1、0.3和0.9 g芒果苷后，该方法成功应用于21名健康中国男性志愿者的芒果苷药代动力学研究。芒果苷的药代动力学符合非房室模型。计算了药代动力学参数。口服0.9 g芒果苷约1小时后，血浆中芒果苷浓度达到38.64 ± 6.75 ng/mL，表观消除半衰期（t(1/2)）为7.85 ± 1.72 h。芒果苷的吸收随着给药剂量的增加而增加，由此得出芒果苷在人体内的药代动力学是非线性的结论。（C）2011爱思唯尔有限公司。保留所有权利。