麻黄汤中麻黄生物碱在人尿中的排泄研究

目的:研究人体口服中药复方麻黄汤煎液后,麻黄生物碱在人体内的代谢及排泄情况。方法:健康志愿者口服麻黄汤煎液后,收集不同时间的尿液,采用GC-MS法测定麻黄汤煎液以及人体口服麻黄汤煎液后尿液中的各麻黄生物碱的含量。结果:口服麻黄汤煎液中含去甲基伪麻黄碱(Norpseudoephedrine,NMP)4.38 mg,去甲基麻黄碱(Norephedrine,NME)3.24 mg,麻黄碱(Ephedrine,E)97.45 mg,伪麻黄碱(Pseudoephedrine,PE)26.15 mg,甲基麻黄碱(Methylephedrine,ME)6.16 mg。健康志愿者口服麻黄汤24 h后,尿液中NMP,NME,E,PE和ME的平均排泄量分别为5.20,9.46,68.39,23.73和2.35 mg,其平均累积排泄率分别为118.84%,291.96%,70.18%,90.74%和38.10%。结论:E作为麻黄汤煎液的主要活性成分之一,其在服药后(0~24)h各时间段排泄最快,而ME排泄最慢。口服麻黄汤煎液后,除一小部分的ME以原形排泄外,NMP,NME,E和PE则主要以原形代谢,通过肾脏从尿液中排出。

Excretion of Ephedrines in Human Urine after Oral Administration of Mahuang Tang Decoction

Objective:To study excretion of ephedrines in human urine after oral administration of traditional chinese medicine Mahuang Tang decoction.Methods:After consuming a double clinical dose of Mahuang Tang decoction,urine samples from healthy volunteers were collected at different time.The urine sample and Mahuang Tang decoction were subjected to KOH(5 mol/L)alkalization and acetic ether extraction before gas chromatography-mass spectrometry(GC-MS)analysis.Results:The amount of NMP,NME,E,PE and ME in Mahuang Tang decoction was 4.38,3.24,97.45,26.15 and 6.16 mg,respectively.At 24 h post-administration,the average accumulated excretion rate of ephedrines were 118.84,291.96,70.18,90.74 and 38.10%,respectively.Conclusions:As one of the main active components of Mahuang Tang decoction,E excreted most quickly.ME excreted most slowly.NMP,NME,E,PE and ME were metabolites of Mahuang Tang decoction in human body.NMP,NME,E and PE mainly metabolized as unchanged parent compounds,while a small amount for ME,and then excreted in urine with assistance of kidney.