Objective: To investigate the metabolites of Tongluo Qingnao injection in urine of rats after tail vein administration. Method: An UPLC-Q-TOF-MS method was used to analysis the metabolites of 12 h urine samples of rats after tail vein administration of Tongluo Qingnao injection. Result: Seven prototype components (baicalin

geniposide

notoginsenoside R1

ginsenoside Rg1

Rb1

Rd

Re) and 10 metabolites (4 from baicalin and 6 from geniposide) were detected and identified in rat urine

including glycosylated metabolites (B-M1

G-M2 and G-M4)

glucuronide metabolite (B-M2)

methylated metabolite (B-M3)

hydrolytic metabolite (B-M4)

demethylation metabolite (G-M1)

dehydrogenation metabolite (G-M3) and hydroxylated metabolites (G-M5 and G-M6)

while the ginsenosides were temporarily unable to detect metabolites in the urine. Conclusion: Prototype components and metabolites of multiple metabolic pathways of baicalin and geniposide are detected in rat urine after tail vein administration of Tongluo Qingnao injection

but notoginseng total saponins are only detected in the prototype and temporarily failed to detect metabolites.