微生物转化研究间尼索地平的代谢产物  

Study on metabolites of m-nisoldipine by microbial transformation

作　　者：孔德志[1] 韩学静[2] 景秀娟[1] 王娜[1] 张兰桐[1] 

机构地区：[1]河北医科大学药学院药物分析教研室,石家庄050017 [2]河北省药品检验所,石家庄050012

出　　处：《药物分析杂志》2010年第2期204-207,共4页Chinese Journal of Pharmaceutical Analysis

基　　金：国家自然科学基金(30840098);河北省自然科学基金项目(C2008001073)

摘　　要：目的:建立微生物转化研究间尼索地平(MNS)代谢产物的方法,确定代谢物的结构及转化途径。方法:通过比较15种加药菌液样品和相对应的菌空白、药物空白的HPLC-PDA图谱,发现代谢物并进行放大制备。结果:经1H-NMR、13C-NMR及ESI-MS2确定了MNS2个代谢产物的结构,并推断出MNS的微生物转化途径。结论:微生物转化可模拟间尼索地平的体内代谢,是研究药物代谢的一种切实可行的方法。Objective：To establish the microbial transformation method of m-nisoldipine（MNS ）,identify the chemical structures of the metabolites and propose the possibie metabolic pathways of MNS.Methods：The metabolites were discovered by comparing the HPLC-PDA chromatograms of 15 fungal strains samples with the corresponding blanks.Then they were prepared by preparative liquid chromatography.Rusults：The chemical structures of two metabolites were identified by 1H-NMR,13C-NMR and ESI-MS2.Moreover,the possibie metabolic pathways of MNS were proposed.Conclusion：The method of microbial transformation may simulate the drug metabolism of MNS in vivo,which can be used as effective supplementary tools of drug metabolism research.

关 键 词：间尼索地平 微生物转化 代谢 

分 类 号：R917[医药卫生—药物分析学]