刘力榕, 贾志鑫, 闫晓宁, 朱美霞, 方聪, 冯梦晗, 黄蓓蓓, 刘洁, 李乾, 肖红斌. 川芎对白芷中4种香豆素类化合物吸收及清除的影响J. 药学学报, 2021,56(7): 1804-1810. doi: 10.16438/j.0513-4870.2021-0592
引用本文: 刘力榕, 贾志鑫, 闫晓宁, 朱美霞, 方聪, 冯梦晗, 黄蓓蓓, 刘洁, 李乾, 肖红斌. 川芎对白芷中4种香豆素类化合物吸收及清除的影响J. 药学学报, 2021,56(7): 1804-1810. doi: 10.16438/j.0513-4870.2021-0592
LIU Li-rong, JIA Zhi-xin, YAN Xiao-ning, ZHU Mei-xia, FANG Cong, FENG Meng-han, HUANG Bei-bei, LIU Jie, LI Qian, XIAO Hong-bin. Effect of Chuanxiong Rhizoma on the absorption and clearance of four coumarins in Angelicae Dahuricae RadixJ. Acta Pharmaceutica Sinica, 2021,56(7): 1804-1810. doi: 10.16438/j.0513-4870.2021-0592
Citation: LIU Li-rong, JIA Zhi-xin, YAN Xiao-ning, ZHU Mei-xia, FANG Cong, FENG Meng-han, HUANG Bei-bei, LIU Jie, LI Qian, XIAO Hong-bin. Effect of Chuanxiong Rhizoma on the absorption and clearance of four coumarins in Angelicae Dahuricae RadixJ. Acta Pharmaceutica Sinica, 2021,56(7): 1804-1810. doi: 10.16438/j.0513-4870.2021-0592

川芎对白芷中4种香豆素类化合物吸收及清除的影响

Effect of Chuanxiong Rhizoma on the absorption and clearance of four coumarins in Angelicae Dahuricae Radix

  • 摘要: 为研究白芷配伍川芎前后其中4种香豆素类化合物(佛手柑内酯、氧化前胡素、欧前胡素、异欧前胡素)在大鼠体内的药代动力学行为变化,建立超高效液相色谱-荧光检测法(UPLC-FLD法)并对大鼠单次给药后不同时间点血浆中的药物浓度进行测定,使用DAS 3.2.8求算药物的药代动力学参数,SPSS 20.0软件分析白芷配伍川芎前后主要药代动力学参数的变化。结果表明:配伍川芎后,佛手柑内酯、氧化前胡素及欧前胡素的药时曲线下面积(AUC0-24 h)分别增加177.2%、97.14%和54.43%,AUC0-分别增加282.3%、104.2%和75.40%,清除率(CLZ/F)分别降低68.26%、51.08%和43.98%;4种香豆素类化合物药峰浓度(Cmax)均显著升高;佛手柑内酯的表观分布容积(VZ/F)显著减小。该结果表明川芎可以促进白芷中香豆素类化合物的吸收,同时减缓其在体内的消除速率,提高其生物利用度。本研究中动物实验方案已获得北京中医药大学实验动物伦理委员会的批准(批准号:BUCM-4-2020083105-3072)。

     

    Abstract: To study the changes in the pharmacokinetic behavior of four coumarins (bergapten, oxypeucedanin, imperatorin and isoimperatorin) in rats before and after combinating Angelicae Dahuricae Radix with Chuanxiong Rhizoma. The plasma concentrations of the drugs were determined by ultra performance liquid chromatography-fluorescence detection (UPLC-FLD) for dose response and time dependent curves. The pharmacokinetic parameters were calculated by DAS 3.2.8, and SPSS 20.0 was used to analyze the differences of main pharmacokinetic parameters between the two groups. The result showed:comparing with Angelicae Dahuricae Radix group, the area under drug time curve (AUC0-24 h) of bergapten, oxypeucedanin and imperatorin increased by 177.2%, 97.14% and 54.43% respectively, AUC0-∞ increased by 282.3%, 104.2%, and 75.40% respectively, and clearance rate (CLZ/F) decreased by 68.26%, 51.08% and 43.98% respectively; the peak drug concentration (Cmax) of four coumarins was significantly increased; the distribution volume (VZ/F) of bergapten was significantly decreased. These data indicated that Chuanxiong Rhizoma can promote the absorption of coumarins in Angelicae Dahuricae Radix, slow down the elimination of coumarins, and increase their bioavailability in vivo. The animal experiment scheme in this study has been approved by the Experimental Animal Ethics Committee of Beijing University of Chinese Medicine (approval number:BUCM-4-2020083105-3072).

     

/

返回文章
返回