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’-dimethylaminomethorphan in rats and to understand the process of drug change in animals and to provide evidence for clinical trials. Methods: The tail vein of rats were injected with 3’-dimethylaminomethylene puerarin (saline solution, 50 mg / kg) and the tissues were treated by mechanical homogenization. Excretion tests collect all feces, urine and bile samples at different time points. The content of 3’-dimethylaminomethylene puerarin in each tissue, feces, urine and bile was determined by a validated LC / MS / MS. RESULTS: After administration, the dose of the urine collected from the feces was (13.6 ± 2.8)% within 12 days, (65.4 ± 11.5)% in the urine and 79.0 ± 14.3% (5) d collected within the bile (14.8 ± 4.4)%. 3’-dimethylaminomethylene puerarin was detected in all tissues of rats, and the contents of the large intestine, contents of small intestine and liver were higher. CONCLUSION: 3’-Dimethylaminomethylenepuerarin is widely distributed in various tissues of rats, mainly excreted by urine and feces.