Wu Mishan, Zhao Suzhi, Ren Lizhong, Wang Ru, Bai Xia, Han Hongwei, Li Bin, Chen Huayue
Department of Formulaology, Hebei Medical University, Shijiazhuang 050091, China.
Zhongguo Zhong Yao Za Zhi. 2011 Nov;36(21):3018-22.
To study the relationship between tissue quantitative distribution and pharmacokinetics of 3H-achyranthes bidentata ecdysterone and the channel-tropism of herbal drugs in mice.
3H-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 3H-achyranthes bidentata ecdysterone and to understand the channel-tropism of herbal drugs achyranthes bidentata.
3H-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 achyranthes 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) min, the elimination of achyranthes bidentata ecdysterone from plasma was found to be in accord with linear kinetics.
The above mentioned selective distribution of 3H-achyranthes 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.
研究3H-牛膝蜕皮甾酮在小鼠体内的组织定量分布、药代动力学特征以及中药的归经趋向性。
以3H-牛膝蜕皮甾酮为示踪剂,经小鼠尾静脉注射,于36小时内测定9个不同示踪时段的各样本及各器官或组织中示踪剂的含量,观察3H-牛膝蜕皮甾酮的动态定量分布、排泄及药代动力学特征,了解中药牛膝的归经趋向性。
不同示踪时段同一器官的3H-牛膝蜕皮甾酮含量以及同一示踪时段不同器官的3H-牛膝蜕皮甾酮含量差异均有统计学意义(P<0.01)。3H-牛膝蜕皮甾酮主要分布于肝脏、肾脏、肾上腺、小肠和肺。尾静脉注射3H-牛膝蜕皮甾酮后,其在小鼠体内的药-时曲线符合二室开放模型,半衰期为(778.65±12.36)分钟,血浆中3H-牛膝蜕皮甾酮的消除符合线性动力学。
上述3H-牛膝蜕皮甾酮的选择性分布基本与中药牛膝的经络亲和性及脏腑选择性相吻合。本研究将为牛膝的归经研究提供科学依据。