摘要
目的鉴定水苏碱在大鼠体内的代谢物.方法应用高效液相色谱-电喷雾离子阱串联质谱（HPLC-ESI/MSn）技术研究水苏碱的一级质谱电离规律、二级质谱裂解规律及其色谱保留,以此作为水苏碱大鼠体内代谢物分析鉴定的依据;再将健康大鼠空腹灌胃25 mg·kg^-1水苏碱,收集0～24 h的尿样,经C18小柱固相萃取分离纯化后,应用HPLC-ESI/MS分析尿样中水苏碱代谢物.结果在大鼠尿样中发现了母药及其N-去甲基、氧化脱氢、环氧化等6种I相代谢产物及两种环氧化物的甘氨酸轭合Ⅱ相代谢产物.结论HPLC-ESI/MS法灵敏度高,快速,定性能力强,适合于水苏碱大鼠体内代谢物的分析.
Aim To identify the main metabolites of stachydrine in rat. Methods The ionization, cleavage and chromatographic characteristics of stachydrine were studied by using high-performance liquid chromatography-electrospray ionization ion trap tandem mass spectrometry （HPLC-ESI/MS） for the first time. These characteristics of stachydrine were used as the basis for the analyses of metabolites in rat urine. The 0 - 24 h urine samples of rats after ig 25 mg·kg^-1 stachydrine were collected and purified by using C18 solid-phase extraction cartridge, and then analyzed by HPLC-ESI/MS to identify stachydrine and its metabolites. Results The parent drug （stachydrine）, 6 phase Ⅰ metabolites （N-demethyl, dehydrogenation, ring-oxidation） and 2 phase Ⅱ metabolites （glycine conjugates of 2 ring-oxidation products） were identified existing in rat urine. Conclusion The presented method was proved to be sensitive, rapid, high selective and specific for the identification of stachydrine and its metabolites in rat urine.
出处
《药学学报》
CAS
CSCD
北大核心
2006年第5期467-470,共4页
Acta Pharmaceutica Sinica
基金
湖北省杰出青年基金资助项目(2002AC004)
中药生物技术省重点实验室开放基金资助项目(2004CTM001).
