草乌与(生、法)半夏配伍3个毒性成分毒代动力学变化研究  

The study on toxicokinetics of aconite kusnezoffii radix compatible with pinelliae rhizom(1:1)

作　　者：翟兴英[1] 徐国良[1] 张凌[1] 李冰涛[1] 冯育林[1] 欧阳辉[1] 杨世林[1] 金晨[1] Zhai Xingying;Xu Guoliang;Zhang Ling;Li Bingtao;Feng Yulin;Ouyang Hui;YANG Shilin;Jin Chen(Jiangxi University of Traditional Chinese Medicine,Nanehang 33000)

机构地区：[1]江西中医药大学,南昌330004

出　　处：《中药药理与临床》2018年第4期139-144,共6页Pharmacology and Clinics of Chinese Materia Medica

基　　金：国家重点基础研究发展计划(973计划)项目(2011CB505302);江西中医药大学重点学科青年教师培养计划项目(2015jzzdxk013);江西中医药大学博士启动基金项目(2015BS007)

摘　　要：目的:探讨草乌与(生、法)半夏配伍毒代动力学变化。方法:采用雄性SD大鼠48只,随机分为草乌醇提组、草乌与法半夏醇提组、草乌与生半夏醇提组、草乌水提组、草乌与法半夏水提组、草乌与生半夏水提组,分别单次以《中华人民共和国药典》(2015版)中草乌最大剂量给药(0. 06g/kg),设给药前和给药后共13个采血时间点,采用LC-MS/MS检测血浆样品,血药浓度-时间数据经DAS2. 0软件处理计算毒代动力学参数。结果:3个毒性成分的AUC(0-t)变化:乌头碱:与单用醇提草乌相比,醇提草乌与法半夏配伍明显降低;与单用水提草乌相比,与生半夏配伍后增大明显。新乌头碱:与单用醇提草乌相比,在醇提草乌与法半夏配伍明显降低,但与生半夏配伍明显增大;与单用水提草乌相比,水提草乌与生半夏配伍明显增加。次乌头碱:与单用醇提草乌相比,在醇提草乌与法半夏配伍明显降低,水提物的变化与醇提一致。Cmax变化:乌头碱:与单用水提草乌相比,水提草乌与生半夏配伍后显示增大。新乌头碱:与单用醇提草乌相比,醇提草乌与法半夏配伍降低,但与生半夏配伍后增大;与单用水提草乌相比,水提草乌与生半夏配伍后明显增加。次乌头碱:与单用醇提草乌相比,在醇提草乌与法半夏配伍后明显降低。结论:总体可见生半夏可使草乌中双酯型生物碱的吸收程度与速率增加;法半夏可使草乌中双酯型生物碱的吸收程度与速率减小。Objective： To investigate the toxicokinetics change in the compatibility of aconite kusnezoffii radix（CW） and pinelliae rhizoma（SBX,FBX）. Method： Forty-eight SD rats were random divided into six groups ： the alcohol extraction of CW,the alcohol extraction of CW compatible with FBX,the alcohol extraction of CW compatible with SBX,the water extraction of CW,the water extraction of CW compatible with FBX,the water extraction of CW compatible with SBX. Administration to rats of each group one time on the biggest dose of CW in Pharmacopoeia of People’s Republic of China（2015 edition）,plasma samples of thirteen points were got before and after administration,which were detected the content of aconitine,mesaconitine and hypaconitine by LC-MS/MS. Then the data of drug concentration-time were treated by DAS 2. 0 software and calculated the parameters of toxicokinetics. Results： Compared with alcohol extract of CW,the AUC（0-t）and Cmax of aconitine,mesaconitine and hypaconitine were all increased in the alcohol extraction of CW compatible with SBX,but they were all reduced in the alcohol extraction of CW compatible with FBX. Compared with water extract of CW,the AUC（0-t）faconitine,mesaconitine and hypaconitine were basically unchanged,while the Cmax of aconitine and mesaconitine were increased sharply in the water extraction of CW compatible with SBX; the AUC（0-t）of aconitine was decrease,mesaconitine’s basically constant but hypaconitine’s became larger,the Cmax of them all basically unchanged. Conclusion： SBX could increase the absorption and rate of Diester alkaloid in CW,but FBX could reduce them.

关 键 词：草乌 半夏 毒性成分 毒代动力学 

分 类 号：R285.5[医药卫生—中药学]