Chu Dafeng, Liu Wanhui, Li Youxin, Li Pengfei, Gu Jingkai, Liu Ke
Research Center for Drug Metabolism, College of Life Science, Jilin University, Changchun, P. R. China.
Planta Med. 2006 May;72(6):552-5. doi: 10.1055/s-2006-931566.
The pharmacokinetics of huperzine A in dogs after single intravenous and oral administrations was investigated. Concentrations of huperzine A were determined by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Pharmacokinetic parameters were calculated by non-compartmental methods. After single intravenous administration, the Cmax, T1/2, AUC0-t, AUC0-infinity, CL, Vd and Vss were 5.55 +/- 1.61 microg/L, 5.02 +/- 0.31 h, 16.04 +/- 5.24, 16.49 +/- 5.29 microgh/L, 0.66 +/- 0.19 L/h/kg, 4.76 +/- 1.46, and 3.93 +/- 1.54 L/kg, respectively. After single oral administration, the Cmax, Tmax, T1/2, AUC0-t, AUC0-infinity and oral bioavailability were 2.60 +/- 0.60 microg/L, 1.25 +/- 0.50 h, 5.71 +/- 2.25 h, 12.90 +/- 3.19, 13.78 +/- 3.24 microgh/L, and 94.4 +/- 36.5%, respectively. In conclusion, huperzine A had a rapid and nearly complete oral absorption and was extensively distributed into tissues after drug administration in dogs.
研究了石杉碱甲在犬单次静脉注射和口服给药后的药代动力学。采用经过验证的液相色谱 - 串联质谱法（LC-MS/MS）测定石杉碱甲的浓度。通过非房室模型方法计算药代动力学参数。单次静脉注射后，Cmax、T1/2、AUC0-t、AUC0-∞、CL、Vd和Vss分别为5.55±1.61μg/L、5.02±0.31h、16.04±5.24、16.49±5.29μg·h/L、0.66±0.19L/h/kg、4.76±1.46和3.93±1.54L/kg。单次口服给药后，Cmax、Tmax、T1/2、AUC0-t、AUC0-∞和口服生物利用度分别为2.60±0.60μg/L、1.25±0.50h、5.71±2.25h、12.90±3.19、13.78±3.24μg·h/L和94.4±36.5%。总之，石杉碱甲口服吸收迅速且几乎完全，给药后在犬体内广泛分布于组织中。
