香附四物汤挥发油β-环糊精包合物的药动学研究  

Pharmacokinetic Study on Xiangfu Siwu Decoction Essential Oil/β-Cyclodextrin Inclusion Complex

作　　者：席骏钻 钱大玮[2] 刘培[2] 朱振华[2] 黄婧[3] XI Jun-Zuan;QIAN Da-Wei;LIU Pei;ZHU Zhen-Hua;HUANG Jing(Rugao People＇s Hospital,Rugao 226500 Jiangsu,China;Pharmaceutical School,Nanjing University of Chinese Medicine Nanjing 210023 Jiangsu,China;Dept.of Pharmacy,Nanjing General Hospital of Nanjing Military Command,Nanjing 210002 Jiangsu,China)

机构地区：[1]如皋市人民医院,江苏如皋226500 [2]南京中医药大学药学院,江苏南京210023 [3]南京军区南京总医院制剂室,江苏南京210002

出　　处：《广州中医药大学学报》2018年第6期1088-1094,共7页Journal of Guangzhou University of Traditional Chinese Medicine

摘　　要：【目的】研究香附四物汤挥发油(XSDO)经β-环糊精包合后,其主要活性成分药物代谢动力学的变化情况。【方法】采集雌性SD大鼠分别灌胃香附四物汤挥发油及香附四物汤挥发油β-环糊精包合物(XSDO/β-CD)后不同时间点的血浆样本,采用超高效液相色谱—串联质谱(UPLC-MS/MS)测定血浆中洋川芎内酯A、正丁基苯酞、藁本内酯、去氢木香内酯、α-香附酮的浓度,以DAS软件计算主要药动学参数。【结果】XSDO/β-CD中各指标成分的C_(max)、T_(1/2)、平均滞留时间(MRT)、AUC0-24h较香附四物汤挥发油有显著增加,而除藁本内酯、去氢木香内酯外,T_(max)值均有所减小,2组的药动学参数间存在显著性差异。【结论】将香附四物汤挥发油制成β-CD包合物可显著提高其主要活性成分的口服吸收及生物利用度。Objective To observe the pharmacokinetic characteristics of main active components of Xiangfu Siwu Decoction essential oil（XSDO）included by β-cyclodextrin（β-CD）. Methods The plasma samples were collected from the female SD rats at different time points after the rats were given intragastric administration of XSDO andXSDO/β-CD inclusion complex（XSDO/β-CD）respectively. The contents of senkyunolide A,3-n-butylphthalide,Z-ligustilide, dehydrocostus lactone and α-cyperone in the plasma were detected by ultra-high performanceliquid chromatography tandem mass spectrometry（UPLC-MS/MS）method,and the pharmacokinetic parameterswere calculated by DAS software. Results The maximum plasma concentration（Cmax）,half-time（T1/2）,mean-residence-time（MRT）and area under the concentration-time curve（AUC0-24 h）in various components of XSDO/β-CD was increased as compared with those in XSDO. Except for Z-ligustilide and dehydrocostus lactone,Tmax in theother components was reduced,the difference of the pharmacokinetic parameters between the two groups beingsignificant. Conclusion XSDO/β-CD made from XSDO is effective on significanting increasing the oral absorption and bioavailability of the active components of XSDO.

关 键 词：香附四物汤 挥发油 包合物 药动学 

分 类 号：R282.6[医药卫生—中药学]