Objective: To investigate the major metabolites of ginkgolide A (GA)

ginkgolide B (GB) and ginkgolide K (GK) from ginkgo diterpene lactone meglumine injection in human urine. Method: The urine samples of the volunteers after a single intravenous infusion administration of ginkgo diterpene lactone meglumine injection were collected for 0-6 h

then the samples were prepared with or without acidification treatment and analyzed by LC-MS/MS.The potential metabolites of GA

GB and GK were analyzed through comparing the total ion current (TIC) and extract ion current (EIC) chromatogram of the test samples with the blank urine and analyzing the quasi-molecular ion and secondary fragment ion of all chromatograms. Result: In addition to the prototype drugs

twelve metabolites were found in human urine containing five phase Ⅰ metabolites and one phase Ⅱ metabolite from GA

one phase Ⅰ metabolite and three phase Ⅱ metabolites from GB

one phase Ⅰ metabolite and one phase Ⅱ metabolite from GK. Conclusion: The major metabolic pathways of GA in human are hydroxylation and lactone ring hydrolysis

then hydrolyzation is followed by conjugation with sulfuric acid.The major metabolic pathways of GB are hydroxylation and lactone ring hydrolysis

then hydrolyzation is followed by conjugation with sulfuric acid

glucuronic acid

and glutathione

respectively.The major metabolic pathways of GK is methyl glucuronic acid binding reaction.