A simple, sensitive and reliable LC–MS/MS method was developed for assessing the total amount and prototype-form lactone of ginkgolides in rat.

Using this method, the concentrations of the hydrolysed carboxylic forms of the ginkgolides were calculated.

For the first time, pharmacokinetic properties of GA, GB, and GK was systematically assessed after intravenous administration of the commercially available drug, ginkgo diterpene lactones meglumine injection, in rats.

For the first time, we showed that GB and GA primarily existed in the carboxylic form in the plasma, while dramatically increased levels of the prototype GB and GA lactone were detected in the tissues, e.g., liver and heart.

GA, GB, and GK were found the highest levels in the kidneys, liver and intestine, and the lowest levels in the brain, indicating that ginkgolides have difficulty crossing the blood–brain barrier.