目的 研究消岩汤中的有效成分并分析其在正常大鼠体内的代谢情况,从而初步探究消岩汤中抗肿瘤有效成分及其代谢规律。方法 取12只雄性Wistar大鼠随机分为实验组及对照组,实验组ig消岩汤浓缩液,对照组ig单药黄芪(消岩汤中君药)浓缩液;给药后于不同时间点目内眦取血0.5mL,采用液质联用(LC-MS)技术测定大鼠体内不同时间点黄芪甲苷、咖啡酸的浓度,得血药浓度-时间数据,采用DSA2.0软件计算血浆药动学参数。结果 实验组大鼠血浆中黄芪甲苷的消除速率常数(K10)、清除率(CL/F)均小于对照组(P<0.05、0.01),消除半衰期(t_tl/2β)、表观分布容积(V/F)、C_max、药时曲线下面积(AUC)均大于对照组(P<0.05、0.01、0.001),两组的达峰时间(t_max)相同。实验组大鼠血浆中咖啡酸的CL/F小于对照组(P<0.01),t_tl/2β、V/F、AUC、K10、C_max均大于对照组(P<0.05、0.01、0.001)。结论 消岩汤能够促进其抗肿瘤成分黄芪甲苷、咖啡酸的吸收代谢。

Objective To study the effective components in Xiaoyan Decoction (消岩汤) and analyze its metabolism in normal rats, so as to preliminarily explore the anti-tumor effective components in Xiaoyan Decoction and its metabolism law. Methods Twelve male Wistar rats were randomly divided into experimental group and control group. Rats in experimental group were ig Xiaoyan Decoction and control group was ig principal drug in Xiaoyan Decoction-Huangqi (Astragali Radix). After administration, 0.5 mL of blood was collected from canthus at different time points. The concentrations of astragaloside IV and caffeic acid in rats at different time points were determined by LC-MS, and blood concentration-time data were obtained. The plasma pharmacokinetic parameters were calculated by DSA 2.0 software. Results The elimination rate constant (K10) and clearance rate (CL/F) of astragaloside IV in experimental group were lower than those in control group (P< 0.05, 0.01), and elimination half-life (tt_l/2β), apparent distribution volume (V/F), Cmax and area under the drug-time curve (AUC) were higher than those in control group (P< 0.05, 0.01, 0.001), peak time (t_max) of two groups was the same. CL/F of caffeic acid in plasma of rats in experimental group was lower than that of control group (P< 0.01), while tt_l/2β, V/F, AUC, K10 and Cmax were higher than those of control group (P< 0.05, 0.01, 0.001). Conclusion Xiaoyan Decoction can promote the absorption and metabolism of anti-tumor components astragaloside IV and caffeic acid.

R285.61

国家自然科学基金资助项目（81904151）