摘要
目的:探讨3H-牛膝蜕皮甾酮在小鼠体内组织定量分布及药动学和归经的关系。方法:采用氚标记苋科植物牛膝的有效成分牛膝蜕皮甾酮为示踪剂,经小鼠尾静脉注入,测定36 h期间9个不同示踪时相器官组织样品中示踪剂含量。观察3H-牛膝蜕皮甾酮在体内动态定量分布、排泄状况和药动学,并探讨其与归经的关系。结果:同一器官的不同示踪时相和同一示踪时相的不同器官,其示踪剂含量呈现显著性差异(P<0.01)。3H-牛膝蜕皮甾酮较集中分布于肝脏、肾脏、肾上腺、小肠和肺脏等器官。其药-时过程符合二室开放模型特征,符合线性动力学,t1/2β为(778.65±12.36)min。结论:3H-牛膝蜕皮甾酮对器官组织选择性分布的特点与牛膝归经的脏腑络属关系基本一致,实验结果为牛膝的传统归经理论提供了一定的现代科学依据。
Objective: To study the relationship between tissue quantitative distribution and pharmacokinetics of H-achyranthes bidentata ecdysterone and the channel-tropism of herbal drugs in mice. Method: 3 H-achyranthes bidentata ecdysterone was used as a tracer agent and injected into mice by the caudal vein. In 36 hours, the contents of the tracer agent of samples involving 9 different tracing phases and organ or tissue were determined in order to observe the dynamic quantitative distribution and excretion and pharmacokinetics of 3 H-achyranthes bidentata ecdysterone and to understand the channel-tropism of herbal drugs achyranthes bidentata. Result: 3 H-achyranthes bidentata ecdysterone of same organs in different tracing phases and the contents of 3H-achyranthes bidentata ecdysterone in same tracing phases of different organs were significantly different ( P 〈 0. 01 ). 3H-achyranthes bidentata ecdysterone was mainly distributed, in the liver, kidney, adrenal gland, small intestine and lung. The concentration-time profiles of aehyranthes bidentata ecdysterone in rats injected into mice by the caudal vein were shown to fit a two-compartment open model with half-lives of (778. 65 ± 12. 36 ) rain, the elimination of achyranthes bidentata ecdysterone from plasma was found to be in accord with linear kinetics. Conclusion: The above mentioned selective distribution of 3H-aehyranthes bidentata ecdysterone basically coincides with the meridian affinity and zang fu selection of the traditional Chinese medicine drug Achyranthes bidentata. This study will provide a scientific basis for the channel-tropism of A. bidentata.
出处
《中国中药杂志》
CAS
CSCD
北大核心
2011年第21期3018-3022,共5页
China Journal of Chinese Materia Medica
基金
国家自然科学基金项目(81073074
30472200)
河北省引进留学人员经费项目(200828)
关键词
牛膝蜕皮甾酮
示踪剂
定量分布
药代动力学
归经
Achyranthe.s bidentata ecdysterone
tracer agent
quantitative distribution
pharmacokinetics
channel-tropism of herbal drugs