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目的:对比丹酚酸B(SAB)和丹酚酸B二甲酯(DMB)在人肝微粒体中的代谢稳定性,并鉴定DMB的代谢产物。方法:应用体外人肝微粒体孵育体系,采用HPLC-MS/MS法测定两者的剩余浓度,考察SAB和DMB的代谢稳定性,并鉴定代谢产物。结果:SAB在人肝微粒体孵育中不代谢;DMB在人肝微粒体和空白孵育液中各得到了4个代谢产物,其中有2个产物相同。结论:SAB在人肝微粒体中稳定;DMB在人肝微粒体和空白孵育液中均不稳定,且人肝微粒体中的代谢速率比空白孵育液快,代谢主要途径为酯键水解。
OBJECTIVE: To compare the metabolic stability of salvianolic acid B (SAB) and salvianolic acid B dimethyl ester (DMB) in human liver microsomes and to identify metabolites of DMB. Methods: The in vitro human liver microsomal incubation system was used to determine the residual concentration of the two drugs by HPLC-MS / MS. The metabolic stability of SAB and DMB were investigated and the metabolites were identified. Results: SAB was not metabolized by human liver microsome. Four metabolites were obtained by DMB in human liver microsomes and blank incubation medium. Two of them were the same. Conclusion: SAB is stable in human liver microsomes. DMB is not stable in both human liver microsomes and blank incubators. The metabolic rate of human liver microsomes is faster than blank incubation medium. The main metabolic pathway is ester hydrolysis.