Li Wei, Gao Jun, Zhao Hong-Zhi, Liu Chang-Xiao
School of Chemical Engineering and Technology, Tianjin University, Tianjin, China.
Eur J Drug Metab Pharmacokinet. 2006 Oct-Dec;31(4):265-70. doi: 10.1007/BF03190466.
To develop a new HPLC-UV method of determining silybin in human plasma and to study the pharmacokinetic of silybin-phosphatidylcholine complex (silybinin capsules) in healthy male Chinese volunteers using the new developed method. The assays were validated over the concentration range of 3.5-14336.0 ng x ml(-1) in human plasma. In either matrix, the lower limit of quantitation was 3.5 ng x ml(-1). The intra- and inter-day precision were less than 10% in terms of RSD. The absolute recovery was more than 90%. The validated assay was suitable for pharmacokinetic studies of silybin. In order to assess its pharmacokinetic profile in human, plasma silybin levels were determined after administration of single oral doses of silybin-phosphatidylcholine complex (equivalent to 280 mg silybin) to 20 subjects. Silybin was absorbed rapidly, the times to reach peak plasma concentration (Tmax) ranged from 0.67 to 2.67 h, and the mean was 1.4 h. Other Pharmacokinetic parameters of silybin in human were Cmax 4242.1 +/- 2252.9 ng x ml(-1); AUC(0-infinity) 5946.6 +/- 1898.9 ng x h x ml(-1); K(el) 0.31 +/- 0.08 h(-1); t1/2 2.38 +/- 0.76 h; Ka 5.48 +/- 2.00 h(-1); CL 55.0 +/- 28.1 L x h(-1); Vd 191.7 +/- 125.1 L, respectively.
建立一种测定人血浆中水飞蓟宾的高效液相色谱 - 紫外新方法，并使用该新方法研究水飞蓟宾 - 磷脂酰胆碱复合物（水飞蓟宾胶囊）在健康中国男性志愿者体内的药代动力学。该分析方法在人血浆中3.5 - 14336.0 ng x ml(-1)的浓度范围内进行了验证。在任何一种基质中，定量下限均为3.5 ng x ml(-1)。日内和日间精密度的相对标准偏差（RSD）均小于10%。绝对回收率超过90%。验证后的分析方法适用于水飞蓟宾的药代动力学研究。为了评估其在人体内的药代动力学特征，对20名受试者单次口服给予水飞蓟宾 - 磷脂酰胆碱复合物（相当于280 mg水飞蓟宾）后测定血浆水飞蓟宾水平。水飞蓟宾吸收迅速，达峰时间（Tmax）为0.67至2.67 h，平均为1.4 h。水飞蓟宾在人体内的其他药代动力学参数分别为：Cmax 4242.1 +/- 2252.9 ng x ml(-1)；AUC(0 - 无穷大) 5946.6 +/- 1898.9 ng x h x ml(-1)；K(el) 0.31 +/- 0.08 h(-1)；t1/2 2.38 +/- 0.76 h；Ka 5.48 +/- 2.00 h(-1)；CL 55.0 +/- 28.1 L x h(-1)；Vd 191.7 +/- 125.1 L。
