Zou Liang, Li Rui, Wang Ping, Xiao Yan, Xu Li-Jia, He Yu-Xin, Zhao Gang, Peng Lian-Xin
College of Biological Industry, Chengdu University, Chengdu, 610106, People's Republic of China.
Eur J Drug Metab Pharmacokinet. 2014 Sep;39(3):165-71. doi: 10.1007/s13318-013-0152-y. Epub 2013 Sep 7.
This paper aims to investigate the portal-vein absorption kinetics of berberine in rat, and the influence of P-gp inhibitors such as verapamil and borneol, to its absorption ability. In the paper, a validated UHPLC method was established to determine the berberine in plasma, and the portal-vein absorption model was applied to conduct the pharmacokinetic study. Animals were divided into four groups as follow: group berberine group (BG); group verapamil + berberine group (VBG); group borneol + berberine group (BBG) and group long-term use of borneol + berberine group (LBBG). Plasma samples were obtained at regular time intervals after administration and separated on Agilent 1290 Infinity UHPLC instrument. The method showed good linearity (r = 0.9988) over wide dynamic ranges (4.08-163.20 ng/mL). Variations within- and between-batch never exceeded 7.58 and 2.21 %, respectively. The extraction recovery rates ranged from 85.34 to 111.62 %. We discovered that the AUC of four group exhibited no significant differences (P > 0.05), and co-administration of berberine with borneol of group BBG and group LBBG in advance could both reduce the T max and C max as compared to group BG (P < 0.05), while co-administration of verapamil seems to have had little influence to berberine's absorption ability.
本文旨在研究大鼠体内小檗碱的门静脉吸收动力学，以及维拉帕米和冰片等P-糖蛋白抑制剂对其吸收能力的影响。本文建立了一种经过验证的超高效液相色谱法来测定血浆中的小檗碱，并应用门静脉吸收模型进行药代动力学研究。将动物分为以下四组：小檗碱组（BG）；维拉帕米+小檗碱组（VBG）；冰片+小檗碱组（BBG）和长期使用冰片+小檗碱组（LBBG）。给药后按固定时间间隔采集血浆样本，并在安捷伦1290 Infinity超高效液相色谱仪上进行分离。该方法在较宽的动态范围（4.08 - 163.20 ng/mL）内显示出良好的线性关系（r = 0.9988）。批内和批间变异分别从未超过7.58%和2.21%。提取回收率在85.34%至111.62%之间。我们发现四组的AUC无显著差异（P > 0.05），与BG组相比，BBG组和LBBG组预先将冰片与小檗碱联合使用均可降低Tmax和Cmax（P < 0.05），而维拉帕米联合使用似乎对小檗碱的吸收能力影响不大。
