Synthesis of hydralazine-N-lactose and its metabolites in vitro

VernacularTitle:肼屈嗪-N-乳糖结合物的制备以及体外代谢研究
Author: Xingyu QIN ¹ ; Rui FENG ; Bin DI
Author Information

1. 中国药科大学药学院药物分析系
Keywords: hydralazine-N-lactose; hydralazine; lactose; liver microsomes; LC-MS/MS; metabolism
From: Journal of China Pharmaceutical University 2017;48(6):687-695
CountryChina
Language:Chinese
Abstract: Hydralazine-N-lactose is a main impurity in hydralazine tablets.Hydralazine and lactose were used as raw materials,and silica gel column and preparation column of octadecylsilane bonded silica were selected to pre pare and purify hydralazine-N-lactose.Its in vitro metabolites were identified by utilizing SD rat liver microsomes.The results of samples in vitro were compared with blank group and the resulting metabolites structures were identified by LC-MS/MS.Hydrazine-N-lactose produced six main metabolites,including s-triazolo[3,4-a] phthalazine,3-methyl-s-triazolo [3,4-a] phthalazine,3-(1-hydroxy) methyl-s-triazolo [3,4-a] phthalazine,3-hydroxymethyl-s-triazolo[3,4-a] phthalazine,hydralazine and dehydro-hydralazine-N-lactose after in vitro metabolism.This study will be valuable in hydralazine-lactose conjunctions metabolism research and hydralazine formulation safety.