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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 investigate the quantitative distribution of 3H-Achyranthes ecdysterone in mice and its relationship with pharmacokinetics and regression. Methods: Triterpenoids from the genus Achyranthes of the genus Achyranth were used as tracer. Trabeculectomyosterone was injected into the tail vein of mice to determine the content of tracer in nine different tracer samples during 36 h. To observe the dynamic quantitative distribution, excretion and pharmacokinetics of 3H-Achyranthes ecdysterone in vivo, and to explore its relationship with the recovery. Results: The tracer contents of different organs in the same organ with different tracer phases and in the same tracer phase were significantly different (P <0.01). 3H-Achyranthes ecdysterone is more concentrated in the liver, kidney, adrenal, small intestine and lung and other organs. The drug-time course accords with the characteristics of two-compartment open model, in line with the linear kinetics, t1 / 2β was (778.65 ± 12.36) min. CONCLUSION: The selective distribution of ecdysterone on 3H-Achyranthes bidentata is basically the same as that of the organ of Achyranthes bidentata. The experimental results provide some scientific evidences for the traditional theory of bovine knee.