茴三硫的代谢产物及其相互转化研究  

Anethol trithione metabolites and their mutual transformation

作　　者：陈民辉[1] 刘旻虹[2] 狄斌[3] 苏梦翔[3] 

机构地区：[1]江苏省食品药品检验所,南京210008 [2]江苏省常州药品检验所,常州213002 [3]中国药科大学药物质量与安全预警教育部重点实验室,南京210009

出　　处：《中国新药杂志》2013年第19期2328-2331,共4页Chinese Journal of New Drugs

摘　　要：目的:研究茴三硫的代谢产物及其相互转化。方法:采用大鼠肝微粒体体外温孵,结合液相色谱质谱联用技术推测代谢物结构,并用高效液相色谱法测定原型药物与代谢产物的相互转化关系。结果:温孵体系中,茴三硫迅速脱甲基代谢为对羟基苯基三硫酮,并且均存在氧化产物,随后茴三硫及其氧化产物峰面积之和与代谢物对羟基苯基三硫酮及其氧化产物的峰面积之和是基本恒定的,而这时原型药物及3种代谢产物峰面积随时间的变化,是由于原型药物及脱甲基代谢物的氧化产物在温孵体系中被重新还原所引起的。结论:在体外温孵体系中,茴三硫存在脱甲基化、氧化和氧化产物的再还原3种反应。Objective： To study anethol trithione metabolites and their mutual transformation. Methods： Rat liver microsomes were incubated in vitro. The metabolite structures were determined by liquid chromatography combined with mass spectrometry. Concentrations of the drug and metabolites were detected by high performance liquid chromatography to clarify the relationship of their mutual transformation. Results： In the in vitro incubation system, anethol trithione was rapidly demethylated and converts to 4-hydroxy-anethol trithione. The oxidation prod- ucts of both anethol trithione and 4-hydroxy-anethol trithione existed as well. The peak areas of anethol trithione, 4- hydroxy-anethol trithione and their oxidation products was basically constant. Meanwhile the peak areas of anethol trithione and its three metabolites were varying due to reduction of the oxidation products of anethol trithione and its demethylated metabolites. Conclusion： Three metabolic pathways of anethol trithione, namely demethylation, oxi- dation and reduction of the oxidation products, have been detected in the in vitro incubation system.

关 键 词：茴三硫 对羟基苯基三硫酮 代谢产物 

分 类 号：R975.5[医药卫生—药品]