Wang Changhe, Wang Sicen, Chen Qinhua, He Langchong
School of Medicine, Xi'an Jiaotong University, Xi'an 710061, PR China.
J Chromatogr B Analyt Technol Biomed Life Sci. 2008 Mar 1;863(2):215-22. doi: 10.1016/j.jchromb.2008.01.004. Epub 2008 Jan 16.
The aim of this paper is to investigate the characteristics of atractylenolide I (AO-I) in the body by a GC-MS method. All bio-samples were cleared up with a liquid-liquid extraction procedure. The calibration curves were linear within a range of 5-1000 ng/mL for plasma samples, 0.06-16.00 microg/g for cerebellum samples, and 0.03-8.00 microg/g for other tissue samples. The limit of quantification (LOQ) for AO-I was 1.0 ng/mL or 1.0 ng/g (S/N>micro=10) in the bio-samples. In the applications, the main pharmacokinetic parameters were firstly obtained as follows: Tmax=0.37+/-0.19 h, Cmax=0.26+/-0.05 microg/mL, AUC=1.95+/-0.30 microgh/mL and ka=10.08+/-5.60 h(-1). The tissue distribution of AO-I in rats after the oral administration of 50.0mg/kg was from 0.225 to 0.031microg/g with a decreasing tendency in different tissues like liver>kidney>spleen>cerebellum>heart>cerebrum>lung. The protein binding in rat plasma, human plasma and bovine serum albumin was 80.8+/-3.9, 90.6+/-3.1 and 60.9+/-5.1%, respectively.
本文旨在通过气相色谱-质谱联用（GC-MS）法研究白术内酯Ⅰ（AO-I）在体内的特性。所有生物样品均采用液-液萃取法进行处理。血浆样品校准曲线在5-1000 ng/mL范围内呈线性，小脑样品校准曲线在0.06-16.00 μg/g范围内呈线性，其他组织样品校准曲线在0.03-8.00 μg/g范围内呈线性。AO-I在生物样品中的定量限（LOQ）为1.0 ng/mL或1.0 ng/g（S/N>10）。在应用中，首先获得的主要药代动力学参数如下：Tmax=0.37±0.19 h，Cmax=0.26±0.05 μg/mL，AUC=1.95±0.30 μg·h/mL，ka=10.08±5.60 h-1。大鼠口服50.0mg/kg后，AO-I在不同组织中的分布为0.225至0.031 μg/g，且在肝脏>肾脏>脾脏>小脑>心脏>大脑>肺等不同组织中呈下降趋势。大鼠血浆、人血浆和牛血清白蛋白中的蛋白结合率分别为80.8±3.9%、90.6±3.1%和60.9±5.1%。
