3′-二甲氨基亚甲基葛根素在大鼠体内组织分布与排泄研究

Tissue distribution and excretion of 3′-dimethylaminomethylene puerarin in rat

目的:研究3′-二甲氨基亚甲基葛根素在大鼠体内的组织分布与排泄情况,了解药物在动物体内变化过程,为临床试验提供药代依据。方法:大鼠尾静脉注射3′-二甲氨基亚甲基葛根素(生理盐水溶液,剂量50 mg/kg),采用机械匀浆处理组织。排泄实验是在不同时间点收集全部粪、尿、胆汁样品。用经验证的LC/MS/MS联用测定各组织、粪、尿、胆汁中3′-二甲氨基亚甲基葛根素的含量。结果:大鼠给药后,12 d内从粪中收集到给药剂量的(13.6±2.8)%,尿液中回收到(65.4±11.5)%,粪尿合计(79.0±14.3)%,5 d内胆汁中收集到(14.8±4.4)%。3′-二甲氨基亚甲基葛根素在大鼠各组织中均检测到,大肠内容物、小肠内容物和肝中浓度较高。结论:3′-二甲氨基亚甲基葛根素广泛分布于大鼠各组织中,主要以原形经尿和粪便排泄。

Objective： To study the tissue distribution and excretion of 3′-dimethylaminomethylene puerarin in rats, in order to provide data for clinical study. Methods ：3′-Dimethylaminomethylene puerarin was administrated intravenously （50 mg/kg in physiological saline）. Tissue samples were mechanically homogenized. Feces, urine and bile samples were completely collected at different time points. The concentrations of 3′-dimethylaminomethylene puerarin in biological samples was determined by LC/MS/MS. Results,The cumulative excretion rate of the dose in rat feces, urine and bile was（ 13.6 ± 2.8） % , （65.4 ±11.5 ） % and （ 14.8 ± 4.4 ） % , respectively. The total excretion rate in feces and urine was （79.0 ± 14.3 ）%. 3′-Dimethylaminomethylene puerarin was extensively distributed in rat tissues. The higher concentrations existed in the large intestinal content, small intestinal content and liver. Condusion：3′-Dimethylaminomethylene puerarin was widely distributed in most of rat tissues. The unchanged compound is mainly excreted in urine and feces.